[go: up one dir, main page]

AR073900A1 - Compuestos de espiro-oxindol y su uso como agentes terapeuticos. - Google Patents

Compuestos de espiro-oxindol y su uso como agentes terapeuticos.

Info

Publication number
AR073900A1
AR073900A1 ARP090104004A ARP090104004A AR073900A1 AR 073900 A1 AR073900 A1 AR 073900A1 AR P090104004 A ARP090104004 A AR P090104004A AR P090104004 A ARP090104004 A AR P090104004A AR 073900 A1 AR073900 A1 AR 073900A1
Authority
AR
Argentina
Prior art keywords
methyl
trifluoromethyl
pyridin
benzyl
ylmethyl
Prior art date
Application number
ARP090104004A
Other languages
English (en)
Inventor
Jianyu Sun
Mikhail Chafeev
Jianmin Fu
Shifeng Liu
Sultan Chowdhury
Lauren Fraser
Serguei Sviridov
Shaoyi Sun
Jean-Jacques Cadieux
Qi Jia
Mark Wood
Alla Zenova
Jonathan Langille
Simon J Gauthier
Nagasree Chakka
Tom Hsieh
Amy Frances Douglas
Zoran Cikojevic
Original Assignee
Xenon Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41395034&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR073900(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Xenon Pharmaceuticals Inc filed Critical Xenon Pharmaceuticals Inc
Publication of AR073900A1 publication Critical patent/AR073900A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4747—Quinolines; Isoquinolines spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/499—Spiro-condensed pyrazines or piperazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)

Abstract

Compuestos de espiro-oxindol, como estereoisomeros, enantiomeros, tautomeros de los mismos o mezclas de los mismos; o sales, solvatos o prodrogas farmacéuticamente aceptables de los mismos, para el tratamiento y/o la prevencion de enfermedades o condiciones mediadas por canales de sodio, tal como el dolor. Reivindicacion 1: Un compuesto caracterizado porque es de formula (1) en donde n es 1 o 2; uno de J y K es -CH2- y el otro es -O-; o ambos J y K son cada uno -CH2-; R1 es hidrogeno, metilo, ciclopropilo, carboximetilo, (3-carboxi)bencilo, (3-metilsulfonilamino)bencilo, [(3-metilsulfonilamino)piridin-2-il]metilo, [(3-carboxi)piridin-2-il]metilo, [(etoxi)carbonil]metilo, 2-ciclopropiletilo, 1,3-tiazol-5-ilmetiIo, 3-metoxipropilo, (6-metilpiridin-2-il)metilo, piridin-3-ilmetilo, [3-(ciano)piridini-2-il]metilo, [3-(difluorometil)piridin-2-il]metilo, 3-(5-metil-1,2,4-oxadiazoI-3-il)bencilo, 4-(5-metil-1,2,4-oxadiazol-3-il)bencilo, [5-(trifluorometil)-1,2,4-oxadiazoI-3-il]metilo, [5-(trifluorometil)-1,3,4-oxadiazol-2-il]metilo, [4-(trifluorometil)piridin-2-il]metilo, (4-metil-1,2,5-oxadiazol-3-il)metilo, pirazin-2-ilmetilo, pirimidin-2-ilmetilo, (1-metil-1H-benzotriazol-5-il)metilo, [2-(tert-butoxicarbonilamino)piridin-5-il]metilo, [6-(dimetilamino)piridin-3-il]metilo, [6-(dimetilamino)piridin-2-il]metilo, {6-[(difeniImetiliden)amino]piridin-2-il}metilo, (5-morfolin-4-ilpiridin-2-il)metilo, [5-(dimetilamino)piridin-2-il]metilo, (6-aminopiridin-2-il)metilo, (6-oxo-1,6-dihidropiridin-3-il)metilo, (2-hidroxipirimidin-5-il)metilo, (1-metil-6-oxo-1,6-dihidropiridin-3-il)metilo, (6-aminopiridin-3-il)metilo, [1,2,4]triazolo[1,5-a]piridin-6-ilmetilo, (5-hidroxipiridin-2-il)metilo, (5-bromopiridin-2-il)metilo, hidrazinocarbonilmetilo, [6-desoxi-D-gaIactopiranosa]-6-ilo, (6-morfolin-4-ilpiridin-3-il)metilo, [3-(metilsulfonil)piridin-2-il]metilo, (4S)-2,2-dimetil-1,3-dioxolan-4-il]metilo, (3-bromopiridin-2il)metilo, [(2-imidoformamido)piridin-5-il]metilo, (6-cianopiridin-2-il)metilo, (6-aminocarbonilpiridin-2-il)metilo, difeniImetilo, 4-metoxibencilo, 2-(fluorometil)bencilo, 2-etoxietilo, 4-fluorofenilo, (2-fluorofenilaminocarbonil)metilo, 2-(2-metoxietoxi)etilo, 4-isoxazoI-5-iIbencilo, 3-(benciloxi)propilo, (2S)-2,3-dihidroxipropilo, 4-metoxibutilo, pentilo, isopentilo, hexilo, 3-nitrobencilo, [3-(trifluorometil)piridin-2-il]metilo, [5-(trifluorometil)piridin-2-il]metilo, [(tert-butoxicarbonilamino)piridin-2-il]metilo, (3-(trifluorometil)piridin-2-il)metilo, (5-(trifluorometil)furan-2-il)metilo, tetrahidrofuran-2-ilmetilo, 3-metilbutilo, cianometilo, 4-hidroxibencilo, 3-cianobencilo, 4-fluoro-3-metoxibencilo, 4-cianobencilo, [6-(trifluorometil)piridin-3-il]metilo, [4-(trifluorometil)-1,3-tiazol-2-il]metilo, (3-fluoropiridin-2-il)metilo, (4-fluoropiridin-2-il)metilo, (5-fluoropiridin-3-il)metilo, (5-fluoropiridin-2-il)metilo, (3-cloropiridin-2-il)metilo, (3,5-difluoropiridin-2-il)metilo, (3-piridin-3-ilisoxazol-5-il)metilo, (2,2-difluorociclopropilo)metilo, 2-oxobutilo, 2,1,3-benzotiadazol-5-ilmetilo, 2,1,3-benzoxadiazol-5-ilmetilo, 1,3-benzotiazol-2-ilmetilo, (1-metil-1H-bencimidazol-2-il)metilo, [2-(1-metiletil)-1,3-tiazol-4-il]metilo, tert-butoxicarbonilo, [1-(tert-butoxicarbonil)piperidin-4-il]metilo, (2-metoxipirimidin-5-il)metilo, (6-metoxipiridin-3-il)metilo, (1-oxidopiridin-2-il)metilo, (3-aminopiridin-2-il)metilo, piperidin-4-ilmetilo, [1-(1-metiletil)piperidin-4-il]metilo, (1-metilpiperidin-4-il)metilo, morfolin-2-ilmetilo, [4-(1-metiletil)morfolin-2-il]metilo, (4-metilmorfolin-2-il)metilo, (2S)-morfolin-2-ilmetilo, [(2S)-4-metilmorfolin-2-il]metilo, [5-(difluorometil)furan-2-il]metilo, tetrahidro-2H-piran-4-iImetilo, tetrahidro-2H-piran-2-ilmetilo, (5-cloro-1-metil-1H-imidazol-2-il)metilo, (6-cloropiridin-2-il)metilo, (4,6-dimetoxipirimidin-2-il)metilo, [(3-metilaminocarbonil)piridin-2-il]metilo, 1-[2-(aminoetil)aminocarbonilpiridin-3-il]metilo, piridin-2-ilmetilo, (2R)-1,4-dioxan-2-ilmetilo, 1,4-dioxan-2-ilmetilo, 3,4-dimetoxibencilo, 3,5-dimetoxibencilo, 3-hidroxipropiIo, 3-ftalimidopropilo, 3-aminobencilo, (3-aminocarboniI)bencilo, (4-aminocarbonil)bencilo, (3-N,N-dimetilaminocarbonil)bencilo, 4-(benciloxi)bencilo, 4-fluorobencilo, 2,3-difluorobencilo, 3,5-difluorobencilo, 2-cloro-4-fluorobencilo, [3-(2-fluorofenil)aminocarbonil]bencilo, 3-(metoxicarbonil)bencilo, 4-(metoxicarbonil)bencilo, 4-(etoxicarbonil)bencilo, 3-(dimetilamino-sulfonil)bencilo, 3-(3-metil-1,2,4-oxadiazoI-5iI)bencilo, 4-(3-amino-1H-pirazol-5-il)bencilo, 4-(3-metil-1,2,4-oxadiazol-5-il)bencilo, 3-(morfolin-4-ilsuIfoniI)bencilo, 2-(difluorometil)bencilo, (3-trifluorometoxi)bencilo, (2-fluoro-5-trifluorometil)bencilo, (2-fluoro-5-trifluorometil)bencilo, (2-trifluorometoxi)bencilo, S-(amino(hidroxiimino)metil)bencilo, 2-amino-2-(hidroxiimino)etilo, (6-(N'-hidroxiformimidamido)piridin-3-il)metilo, 2-(2,2,5-trimetil-1,3-dioxan-2-il)etilo, (4-bencilmorfolin-2-il)metilo, [(2S)-4-bencilmorfolin-2-il]metilo, 2,3-dihidro-1,4-benzodioxin-6-ilmetilo, [5-(trifluorometil)furan-2-il]metilo, 3-(trifluorometil)bencilo, [3-(trifluorometil)pirazin-2-il]metilo, [4-(trifluorometil)piridin-3-il]metilo, (5-metoxicarbonilfuran-2-il)metilo, 5-carboxifuran-2-ilmetilo, 5-(dimetilaminocarbonil)furan-2-iImetilo, [2-(trifluorometil)piridin-3-il]metilo, metilcarbonilo, etoxicarbonilo, tert-butoxicarbonilo o [(3aR,5R,5aS,8aS,8bR)-2,2,7,7-tetrametiltetrahidro-3aH-bis[1,3]dioxolo[4,5-b:4',5'-d]piran-5-il]metilo; cada R2 es en forma independiente hidrogeno, hidroxi, amino, (hexanilaminocarbonil)amino, (ciclopentilaminocarbonil)amino, bencilamino, (ciclohexilaminocarbonil)amino, metilsulfonilamino, (metil)carbonilamino, N-N-dimetilaminocarboniio, (etil)carbonilamino, (butil)carbonilamino, (tert-butil)carbonilamino, (pentanil)carbonilamino, (hexanil)carbonilamino, (metoximetil)carbonilamino, ciclobutilcarbonilamino, [2-metoxi(etoximetil)]carbonilamino, (metilsulfonil)amino, (2-trifluorometilfenil)carbonilamino, (ciclohexaniI)carbonilamino, (ciclopentanil)carbonilamino, (ciclopropanil)carbonilamino, (fenil)carbonilamino, bromo, ciano, fluoro, metilo, metoxi, hidroxicarbonilo, metilcarbonilo, pirrolidinilcarbonilo, aminocarbonilo, metilaminocarbonilo, (2-metoxietil)aminocarbonilo, (ciclopropil)aminocarbonilo, pentilaminocarbonilo, (ciclobutil)aminocarbonilo, (ciclopentil)aminocarbonilo, hexanilaminocarbonilo, (ciclohexil)aminocarbonilo, (4-fluorofenil)aminocarbonilo, (4-fluorobencil)aminocarbonilo, (piridin-2-ilmetil)aminocarbonilo, 2-(2-metoxietoxi)etoxi, [3-(trifluorometil)piridin-2-il]oxilo, quinolinilo, fenoxicarbonilo, 2-oxocromenilo, 2-oxopirrolidinilo, morfolinilo, 2-oxopiridinilo, benciloxilo, [3-(trifluorometil)piridin-2-il]metoxi, piridin-2-ilmetoxi, piridin-2-iloxi, 4-(trifluorometil)fenoxi, 2-metil-1,3-tiazol-4-ilo, 2-amino-1,3-tiazol-4-ilo, 6-(dimetilamino)piridin-3-ilo, furan-3-ilo, 1H-pirazol-3-ilo, 1H-pirazol-4-ilo, 1-metil-1H-pirazol-4-ilo, 5-hidroxi-1H-pirazol-3-ilo, 5-metil-1,2,4-oxadiazoil-3-ilo, (6-metoxipiridin-3-il)oxi, 1,3-benzodioxol-5-iloxi, 4-fluorobenciloxi, 3,5-dimetilisoxazol-4-ilo, fenoxi, 3-metoxifenoxi, 4-metoxifenoxi, 3-morfolin-4-ilfenoxi, 4-fluorofenoxi, 4-metoxifenilo o 4-fenoxifenilo; o dos R2 adyacentes, junto con los átomos de carbono a los cuales están unidos, forman un anillo tiazolilo fusionado, un anillo piridilo fusionado o un anillo dioxinilo fusionado; como estereoisomero, enantiomero, tautomero de los mismos o sus mezclas; o una sal aceptable para uso farmacéutico, solvato o prodroga del mismo. Reivindicacion 8: Un compuesto caracterizado porque tiene la formula (2) en donde cada R3a es hidrogeno o fluor; R3 es hidrogeno, metilo, 3-(trifluorometil)piridin-2-il]metilo, 2,5-dimetil-1-(1-metiletil)-1H-pirrol-3-il]metilo, (3-isopropilisoxazol-5-il)metilo, (4-bromo-2-tienil)metilo, 1-benzofuran-2-ilmetilo, [2-metil-5-(trifluorometil)-1,3-oxazol-4-il]metilo, [5-(4-cIorofeniI)-2-(trifluorometil)furan-3-il]metilo, [5-cloro-1-metil-3-(trifluorometil)-1H-pirazol-4-il]metilo, 5-metoxipiridin-3-ilo, 4-bromobencilo, [(2S)-5-oxopirrolidin-2-il]metilo, tert-butoxicarbonilo, cianometilo, [5-(trifluorometil)-2-furil]metilo, (5-cloro-2-tienil)metilo, (3-clorotiofen-2-il)metilo, [3-(2,6-dicIorofenil)-5-metilisoxazol-4-il]metilo, {2-[4-(trifluorometil)fenil]-1,3-tiazol-4-il}metilo, (5-fenil-1,3,4-oxadiazol-2-il)metilo, [5-(4-clorofenil)-1,3,4-oxadiazoI-2-il]metilo, [1,3]oxazolo[4,5-b]piridin-2-ilmetilo, (2-isopropil-1,3-tiazol-5-il)metilo, (2-isopropil-1,3-oxazol-5-il)metilo, 3-(tert-butoxicarbonilamino)-3-(ciclopropil)propilo, 4-(metilsulfanil)bencilo, 2-cianoetilo, (2-bromo-1,3-tiazol-5-il)metilo, [2-amino-4-(trifluorometil)-1,3-tiazol-5-il]metilo, (2-amino-1,3-tiazol-4-il)metilo, (5-clorotiofen-2-il)metilo, [2-(1-metiletil)-1,3-tiazoI-4-il]metilo, (5-cloro-1,2,4-tiadazol-3-il)metilo, (5-cloro-1,2,4-tiadiazol-3-il)metilo, 4-metoxibencilo, (2S)-1,4-dioxan-2-ilmetilo, (2-cloro-1,3-tiazoI-5-il)metilo, [2-(dimetilamino)-1,3-tiazol-5-il]metilo, (2-morfolin-4-il-1,3-tiazoI-5-il)metilo, (2-piperidin-1-il-1,3-tiazol-5-il)metilo, (2-metoxi-1,3-tiazol-5-il)metilo, 2-[5-(trifluorometil)-1,2,4-oxadiazol-3-il]etilo, [5-(trifluorometil)-1,2,4-oxadiazol-3-il]metilo, (5-ciclopropil-1,2,4-oxadiazol-3-il)metilo, [5-(difluorometil)-1,2,4-oxadiazoI-3-il]metilo, (5-tert-butil-1,2,4-oxadiazoI-3-il)metilo, [5-(1-metiletil)-1,2,4-oxadiazol-3-il]metilo, (4-metilpiperazin-1-il)metilo, (3-metil-2-oxo-1,3-oxazoIidin-5-il)metilo, 2-(1-(metiletil)aminocarbonilpiperidin-3-il)etilo, (4-cianotien-2-il)metilo, [5-trifluorometil-4-(metil)aminocarboniIfuran-2-il]metilo, (5-trifluorometil-4-aminocarboniIfuran-2-il)metilo, [5-trifluorometil-4-(dimetil)aminocarbonilfuran-2-il]metilo, [4-(ciclopropil)aminocarbonil-1,3-oxazol-2-il]metilo, (2,4-dioxo-1,2,3,4-tetrahidropirimidin-5-il)metilo, o [4-(metiletil)aminocarbonil-1,3-oxazol-2-il]metilo; cada R4 es en forma independiente hidrogeno, cloro, bromo, trifluorometilo, ciano, 6-(dimetilamino)piridin-3-ilo, tetrahidrofuran-3-ilo o furan-3-ilo
ARP090104004A 2008-10-17 2009-10-16 Compuestos de espiro-oxindol y su uso como agentes terapeuticos. AR073900A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10646408P 2008-10-17 2008-10-17

Publications (1)

Publication Number Publication Date
AR073900A1 true AR073900A1 (es) 2010-12-09

Family

ID=41395034

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104004A AR073900A1 (es) 2008-10-17 2009-10-16 Compuestos de espiro-oxindol y su uso como agentes terapeuticos.

Country Status (30)

Country Link
US (5) US8263606B2 (es)
EP (2) EP2942350A1 (es)
JP (2) JP5554337B2 (es)
KR (1) KR101286323B1 (es)
CN (5) CN106928247A (es)
AR (1) AR073900A1 (es)
AU (1) AU2009303468B2 (es)
BR (1) BRPI0920448A2 (es)
CA (1) CA2741029A1 (es)
CL (1) CL2011000835A1 (es)
CY (1) CY1116628T1 (es)
DK (1) DK2350090T3 (es)
ES (1) ES2546302T3 (es)
HK (3) HK1215572A1 (es)
HR (1) HRP20150882T1 (es)
HU (1) HUE025938T2 (es)
IL (2) IL212400A (es)
JO (1) JO3032B1 (es)
MX (1) MX2011004055A (es)
MY (1) MY155255A (es)
NZ (1) NZ592275A (es)
PE (1) PE20110586A1 (es)
PL (1) PL2350090T3 (es)
PT (1) PT2350090E (es)
RU (1) RU2011119626A (es)
SG (2) SG10201703086VA (es)
SI (1) SI2350090T1 (es)
SM (1) SMT201500206B (es)
TW (1) TW201020257A (es)
WO (1) WO2010045251A2 (es)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR053710A1 (es) * 2005-04-11 2007-05-16 Xenon Pharmaceuticals Inc Compuestos espiroheterociclicos y sus usos como agentes terapeuticos
MY158766A (en) 2005-04-11 2016-11-15 Xenon Pharmaceuticals Inc Spiro-oxindole compounds and their uses as therapeutic agents
RU2009117642A (ru) * 2006-10-12 2010-11-20 Ксенон Фармасьютикалз Инк. (Ca) Применение спирооксиндоловых соединений в качестве терапевтических средств
US20110294842A9 (en) * 2006-10-12 2011-12-01 Xenon Pharmaceuticals Inc. Spiro (furo [3, 2-c] pyridine-3-3' -indol) -2' (1'h)-one derivatives and related compounds for the treatment of sodium-channel mediated diseases, such as pain
HRP20150882T1 (hr) 2008-10-17 2015-09-25 Xenon Pharmaceuticals Inc. Spirooksindolski spojevi i njihova upotreba kao terapijska sredstva
US8101647B2 (en) * 2008-10-17 2012-01-24 Xenon Pharmaceuticals Inc. Spiro-oxindole compounds and their use as therapeutic agents
CN101906093B (zh) * 2009-06-05 2013-07-10 中国医学科学院医药生物技术研究所 苯并五元不饱和杂环类化合物及其制备方法
AR077252A1 (es) 2009-06-29 2011-08-10 Xenon Pharmaceuticals Inc Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos
NZ599334A (en) * 2009-10-14 2014-03-28 Xenon Pharmaceuticals Inc Synthetic methods for spiro-oxindole compounds
WO2011047173A2 (en) * 2009-10-14 2011-04-21 Xenon Pharmaceuticals Inc. Pharmaceutical compositions for oral administration
CN102946859B (zh) 2010-02-26 2016-03-02 泽农医药公司 用于局部给药的螺-羟吲哚化合物的药物组合物及其作为治疗剂的用途
WO2012049555A1 (en) 2010-10-13 2012-04-19 Lupin Limited Spirocyclic compounds as voltage-gated sodium channel modulators
CN102584860B (zh) * 2011-01-17 2014-12-10 苏州大学 含吲哚结构的螺杂环化合物及其制备方法
CA2853826C (en) 2011-10-28 2021-03-23 Vanderbilt University Substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m1
WO2013071201A1 (en) * 2011-11-11 2013-05-16 Vanderbilt University Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m1
US9029563B2 (en) 2012-01-06 2015-05-12 Vanderbilt University Substituted 1-benzylindolin-2-one analogs as positive allosteric modulators of muscarinic acetylcholine M1 receptors
WO2013106795A1 (en) 2012-01-12 2013-07-18 Vanderbilt University Substituted 4-(1h~pyrazol-4.yl)benzyl analogues as positive allosteric modulators of machr m1 receptors
KR20150002794A (ko) * 2012-04-12 2015-01-07 제논 파마슈티칼스 인크. 치료제로서 유용한 스파이로-옥시인돌 화합물을 위한 비대칭적 합성
CN102838610B (zh) * 2012-08-28 2014-09-10 吕叶叶 双吲哚二氧杂双环辛二酮
CN103554121B (zh) * 2013-10-16 2015-06-24 华东师范大学 3,3-螺(2-四氢呋喃)氧化吲哚多环状化合物及其应用
CN103554120B (zh) * 2013-10-16 2015-06-24 华东师范大学 3,3-螺(2-四氢呋喃)氧化吲哚多环状化合物的制备方法
EP3126360A1 (en) 2014-03-29 2017-02-08 Lupin Limited Sulfonamide compounds as voltage gated sodium channel modulators
JP6616934B2 (ja) * 2014-05-22 2019-12-04 株式会社 資生堂 レナリドミドの光学分割方法
AR103636A1 (es) 2015-02-05 2017-05-24 Teva Pharmaceuticals Int Gmbh Métodos de tratamiento de neuralgia postherpética con una formulación tópica de un compuesto de espiro-oxindol
TW201722938A (zh) 2015-09-04 2017-07-01 魯賓有限公司 作為電位閘控鈉通道調節子之磺醯胺化合物
CN107416958A (zh) * 2015-09-17 2017-12-01 温州泓呈祥科技有限公司 去除醇酸树脂车间废水中对二甲苯、邻二甲苯和间二甲苯的方法
MX2018004038A (es) 2015-10-02 2019-07-18 Syngenta Participations Ag Derivados de oxadiazol microbicidas.
JP2018537426A (ja) 2015-10-28 2018-12-20 シンジェンタ パーティシペーションズ アーゲー 殺微生物オキサジアゾール誘導体
JP6930972B2 (ja) 2015-12-02 2021-09-01 シンジェンタ パーティシペーションズ アーゲー 殺微生物性オキサジアゾール誘導体
JP6572392B2 (ja) 2015-12-18 2019-09-11 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 電位作動型ナトリウムチャネルにおいて選択的活性を有する、ヒドロキシアルキルアミンおよびヒドロキシシクロアルキルアミンで置換されたジアミン−アリールスルホンアミド化合物
CN108698991B (zh) 2016-01-20 2022-08-23 凯莫森特里克斯股份有限公司 2-氧代吲哚化合物
CN109071520B (zh) 2016-03-24 2022-06-14 先正达参股股份有限公司 杀微生物的噁二唑衍生物
WO2017178549A1 (en) 2016-04-12 2017-10-19 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
US10100060B2 (en) 2016-06-16 2018-10-16 Xenon Pharmaceuticals Inc. Asymmetric synthesis of funapide
CN114409665A (zh) 2016-06-16 2022-04-29 泽农医药公司 螺-吲哚酮化合物的固态形式
AR108745A1 (es) 2016-06-21 2018-09-19 Syngenta Participations Ag Derivados de oxadiazol microbiocidas
EP3487855A1 (en) 2016-07-22 2019-05-29 Syngenta Participations AG Microbiocidal oxadiazole derivatives
WO2018015449A1 (en) 2016-07-22 2018-01-25 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
WO2018029242A1 (en) 2016-08-11 2018-02-15 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
CN106299140A (zh) * 2016-09-21 2017-01-04 广西南宁荣威德新能源科技有限公司 一种新型宽光谱太阳能电池材料
CN109923112A (zh) 2016-09-23 2019-06-21 先正达参股股份有限公司 杀微生物的噁二唑衍生物
JP7077313B2 (ja) 2016-10-06 2022-05-30 シンジェンタ パーティシペーションズ アーゲー 殺微生物オキサジアゾール誘導体
UY37623A (es) 2017-03-03 2018-09-28 Syngenta Participations Ag Derivados de oxadiazol tiofeno fungicidas
WO2018163077A1 (en) 2017-03-08 2018-09-13 Lupin Limited Indanyl compounds as voltage gated sodium channel modulators
EP3592747A1 (en) 2017-03-10 2020-01-15 Council of Scientific and Industrial Research Spirooxindole compounds as gsk3 inhibitors and process for preparation thereof
US20200187502A1 (en) 2017-03-10 2020-06-18 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
BR112019020134B1 (pt) 2017-03-31 2023-05-09 Syngenta Participations Ag Composições fungicidas
CN113979962A (zh) 2017-03-31 2022-01-28 先正达参股股份有限公司 杀真菌组合物
BR112019020693B1 (pt) 2017-04-03 2023-11-28 Syngenta Participations Ag Compostos derivados de oxadiazol microbiocidas, suas composições, método para controlar ou prevenir a infestação de plantas úteis por microrganismos fitopatogênicos utilizando tais compostos e seus usos
WO2018184984A1 (en) 2017-04-05 2018-10-11 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
WO2018184985A1 (en) 2017-04-05 2018-10-11 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
WO2018184982A1 (en) 2017-04-05 2018-10-11 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
BR112019021019B1 (pt) 2017-04-05 2023-12-05 Syngenta Participations Ag Compostos derivados de oxadiazol microbiocidas, composição agrícola, método para controlar ou prevenir a infestação de plantas úteis por microrganismos fitopatogênicos e uso de um composto derivado de oxadiazol
BR112019020734B1 (pt) 2017-04-05 2023-12-05 Syngenta Participations Ag Compostos derivados de oxadiazol, composição agroquímica, método para controlar ou prevenir a infestação de plantas úteis por microrganismos fitopatogênicos e uso dos referidos compostos
WO2018184988A1 (en) 2017-04-05 2018-10-11 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
WO2018185211A1 (en) 2017-04-06 2018-10-11 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
US11447481B2 (en) 2017-06-02 2022-09-20 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
WO2018219773A1 (en) 2017-06-02 2018-12-06 Syngenta Participations Ag Fungicidal compositions
EP3644743B1 (en) 2017-06-28 2022-10-26 Syngenta Participations AG Fungicidal compositions
WO2019011926A1 (en) 2017-07-11 2019-01-17 Syngenta Participations Ag MICROBIOCIDE OXADIAZOLE DERIVATIVES
WO2019011929A1 (en) 2017-07-11 2019-01-17 Syngenta Participations Ag MICROBIOCIDE OXADIAZOLE DERIVATIVES
WO2019011928A1 (en) 2017-07-11 2019-01-17 Syngenta Participations Ag MICROBIOCIDE OXADIAZOLE DERIVATIVES
WO2019011923A1 (en) 2017-07-11 2019-01-17 Syngenta Participations Ag MICROBIOCIDE OXADIAZOLE DERIVATIVES
BR112020000371A2 (pt) 2017-07-12 2020-07-14 Syngenta Participations Ag derivados de oxadiazol microbiocidas
BR112020000414A2 (pt) 2017-07-12 2020-07-21 Syngenta Participations Ag derivados de oxadiazol microbicidas
BR112020000463A2 (pt) 2017-07-13 2020-07-21 Syngenta Participations Ag derivados oxadiazol microbiocidas
CN111356679A (zh) 2017-11-20 2020-06-30 先正达参股股份有限公司 杀微生物的噁二唑衍生物
WO2019207062A1 (en) 2018-04-26 2019-10-31 Syngenta Participations Ag Microbiocidal oxadiazole derivatives
CN108586495B (zh) * 2018-06-12 2020-07-14 广州大学 一种二氟代c2-螺环吲哚啉类化合物及其制备方法
US20210269426A1 (en) 2018-06-29 2021-09-02 Syngenta Crop Protection Ag Microbiocidal oxadiazole derivatives
CN112714764A (zh) 2018-07-02 2021-04-27 先正达农作物保护股份公司 作为农用化学杀真菌剂的3-(2-噻吩基)-5-(三氟甲基)-1,2,4-噁二唑衍生物
JP7349491B2 (ja) * 2018-07-12 2023-09-22 ユーシービー バイオファルマ エスアールエル Ｉｌ－１７モジュレーターとしてのスピロ環状インダン類似体
EP3823966A1 (en) 2018-07-16 2021-05-26 Syngenta Crop Protection AG Microbiocidal oxadiazole derivatives
CN108976243B (zh) * 2018-08-23 2020-03-03 青岛农业大学 通过二甲基呋喃与含氧化吲哚邻羟基苄醇合成螺-色满-4,3′-氧化吲哚的合成方法
WO2020078732A1 (en) 2018-10-17 2020-04-23 Syngenta Crop Protection Ag Microbiocidal oxadiazole derivatives
EP3912625A1 (en) * 2020-05-20 2021-11-24 Kaerus Bioscience Limited Novel maxi-k potassium channel openers for the treatment of fragile x associated disorders
CA3261448A1 (en) 2022-07-21 2024-01-25 Syngenta Crop Protection Ag CRYSTALLINE FORMS OF 1,2,4-OXADIAZOLE FUNGICIDES
US11944604B1 (en) 2023-03-10 2024-04-02 King Saud University Nanoformulation of spriooxindole and methods for treating hepatocellular carcinoma
US11840545B1 (en) * 2023-07-14 2023-12-12 King Faisal University Spirooxindole-copper complex as novel efficient anticorrosion agent for C-steel
WO2025031913A1 (en) 2023-08-04 2025-02-13 Syngenta Crop Protection Ag Methods of controlling or preventing infestation of plants by the phytopathogenic microorganism corynespora cassiicola
CN117736637B (zh) * 2023-10-18 2024-06-11 山东卓高新材料有限公司 一种自修复防水涂料及其制备方法
WO2025257413A1 (en) 2024-06-13 2025-12-18 Syngenta Crop Protection Ag Pecticidally active dihydroazole derivatives
WO2025256333A1 (en) 2024-06-13 2025-12-18 Syngenta Crop Protection Ag Pesticidally active aminoheterocycle derivatives

Family Cites Families (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3189617A (en) 1961-02-03 1965-06-15 Sterling Drug Inc 1-aryloxindoles and their preparation
DE1956237A1 (de) 1969-11-08 1971-05-13 Basf Ag Spiro-pyrrolizidon-oxindole
DE2113343A1 (de) 1971-03-19 1972-09-21 Thiemann Chem Pharm Fab Indolo[2,3-b] chinolone und Verfahren zu ihrer Herstellung
US3723459A (en) 1971-04-23 1973-03-27 Mc Neil Labor Inc 2-oxospiro (indoline -3,4{40 -thiochroman) derivatives
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
CH577461A5 (es) 1975-08-13 1976-07-15 Robins Co Inc A H
US4670566A (en) 1979-07-12 1987-06-02 A. H. Robins Company, Incorporated 3-methyl-hio-4-(5-, 6-, or 7-)phenylindolindolin-2-ones
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US4440785A (en) 1980-10-30 1984-04-03 A. H. Robins Company, Inc. Methods of using 2-aminobiphenylacetic acids, esters, and metal salts thereof to treat inflammation
US4438130A (en) 1981-11-12 1984-03-20 The Upjohn Company Analgesic 1-oxa-, aza- and thia-spirocyclic compounds
JPS60142984A (ja) 1983-12-28 1985-07-29 Kyorin Pharmaceut Co Ltd 新規なスピロピロリジン−２，５−ジオン誘導体およびその製造法
US4569942A (en) 1984-05-04 1986-02-11 Pfizer Inc. N,3-Disubstituted 2-oxindole-1-carboxamides as analgesic and antiinflammatory agents
JPS6130554A (ja) 1984-07-23 1986-02-12 Ono Pharmaceut Co Ltd プロスタグランジン類似化合物のある特定の立体配置を有する異性体及びそれらを有効成分として含有する治療剤
US4690943A (en) 1984-09-19 1987-09-01 Pfizer Inc. Analgesic and antiinflammatory 1,3-diacyl-2-oxindole compounds
US4721721A (en) 1984-12-18 1988-01-26 Rorer Pharmaceutical Corporation 6-(4-thiazole) compounds, cardiotonic compositions including the same, and their uses
DE3608088C2 (de) 1986-03-07 1995-11-16 Schering Ag Pharmazeutische Präparate, enthaltend Cyclodextrinclathrate von Carbacyclinderivaten
WO1993012786A1 (en) 1986-07-10 1993-07-08 Howard Harry R Jr Indolinone derivatives
CA1322197C (en) 1987-07-17 1993-09-14 Bernd Buchmann 9-halogen-(z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents
JPH0195766A (ja) 1987-10-08 1989-04-13 Tamanoisu Kk 無蒸煮アルコール醪からの食酢の製造法
US5182289A (en) 1988-06-14 1993-01-26 Schering Corporation Heterobicyclic compounds having antiinflammatory activity
DK0429685T3 (da) 1989-07-25 1997-12-15 Taiho Pharmaceutical Co Ltd Oxoindolderivat
DE3932953A1 (de) 1989-10-03 1991-04-11 Boehringer Mannheim Gmbh Neue 2-bicyclo-benzimidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
DE3935514A1 (de) 1989-10-25 1991-05-02 Boehringer Mannheim Gmbh Neue bicyclo-imidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5023265A (en) 1990-06-01 1991-06-11 Schering Corporation Substituted 1-H-pyrrolopyridine-3-carboxamides
US5484778C1 (en) 1990-07-17 2001-05-08 Univ Cleveland Hospitals Phthalocynine photosensitizers for photodynamic therapy and methods for their use
AU648359B2 (en) 1990-11-22 1994-04-21 Janssen Pharmaceutica N.V. Isonicotinic acid derivatives
US5116854A (en) 1991-06-28 1992-05-26 Pfizer Inc. Anti-inflammatory 1-heteroaryl-3-acyl-2-oxindoles
FR2686878B1 (fr) 1992-01-30 1995-06-30 Sanofi Elf Derives du n-sulfonyl oxo-2 indole, leur preparation, les compositions pharmaceutiques en contenant.
US5686624A (en) 1992-01-30 1997-11-11 Sanofi 1-benzenesulfonyl-1,3-dihydro-indol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present
US5663431A (en) 1992-01-30 1997-09-02 Sanofi 1-benzenesulfonyl-1,3-dihydro-indol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present
FR2708605A1 (fr) 1993-07-30 1995-02-10 Sanofi Sa Dérivés du N-sulfonylindol-2-one, leur préparation, les compositions pharmaceutiques en contenant.
US5849780A (en) 1992-01-30 1998-12-15 Sanofi 1-benzenesulfonyl-1-1,3-dihydroindol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present
US5314685A (en) 1992-05-11 1994-05-24 Agouron Pharmaceuticals, Inc. Anhydrous formulations for administering lipophilic agents
WO1994003427A1 (en) 1992-08-06 1994-02-17 Warner-Lambert Company 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties
US5278162A (en) 1992-09-18 1994-01-11 The Du Pont Merck Pharmaceutical Company 3,3'-disubstituted-1,3-dihydro-2H-pyrrolo[2,3-b]heterocyclic-2-one useful in the treatment of cognitive disorders of man
US5296478A (en) 1992-10-07 1994-03-22 The Dupont Merck Pharmaceutical Co. 1-substituted oxindoles as cognition enhancers
US5776936A (en) 1992-11-13 1998-07-07 Pharmacia & Upjohn Company Marcfortine/paraherquamide derivatives useful as antiparasitic agents
DE4242451A1 (de) 1992-12-16 1994-06-23 Basf Ag Verfahren zur Herstellung von 5-Ringheterocyclen
US5298522A (en) 1993-01-22 1994-03-29 Pfizer Inc. 6-chloro-5-fluoro-3-(2-thenoyl)-2-oxindole-1-carboxamide as an analgesic and anti-inflammatory agent while maintaining a normal urine protein/creatinine ratio
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
FR2708606B1 (fr) 1993-07-30 1995-10-27 Sanofi Sa Dérivés du N-phénylalkylindol-2-one, leur préparation, les compositions pharmaceutiques en contenant.
US5502072A (en) 1993-11-26 1996-03-26 Pfizer Inc. Substituted oxindoles
AT400950B (de) 1994-02-04 1996-04-25 Immodal Pharmaka Gmbh Verfahren zur technischen herstellung definierter isomerengemische aus verbindungen mit spirozyklischen - aminocarboxyl- und/oder spirozyklischen - aminocarbonyl-systemen
AU2310895A (en) 1994-04-07 1995-10-30 Cemaf Novel spiro{indole-pyrrolidine} derivatives as melatoninergic agonists, method for preparing same and use thereofas a drug
US5618819A (en) 1994-07-07 1997-04-08 Adir Et Compagnie 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-(3H)-one compounds
FR2722195B1 (fr) 1994-07-07 1996-08-23 Adir Nouveaux derives de 1,3-dihydro-2h-pyrrolo(2,3-b) pyridin-2-ones et oxazolo(4,5-b) pyridin-2(3h)-ones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JPH10510821A (ja) 1994-12-22 1998-10-20 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 四環式スピロ化合物、その製法およびその５ｈｔ１ｄレセプターアンタゴニストとしての使用
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
CA2235686C (en) 1995-10-24 2007-06-26 Sanofi Indolin-2-one derivatives, process for their production and the pharmaceutical compositions containing them
FR2740136B1 (fr) 1995-10-24 1998-01-09 Sanofi Sa Derives d'indolin-2-one, procede pour leur preparation et les compositions pharmaceutiques les contenant
HUP9600855A3 (en) 1996-04-03 1998-04-28 Egyt Gyogyszervegyeszeti Gyar Process for producing tenidap
JPH1095766A (ja) 1996-09-19 1998-04-14 Sanwa Kagaku Kenkyusho Co Ltd アセトアミド誘導体、及びその用途
FR2757157B1 (fr) 1996-12-13 1999-12-31 Sanofi Sa Derives d'indolin-2-one, procede pour leur preparation et compositions pharmaceutiques les contenant
EP0989856B1 (de) 1997-01-20 2010-05-12 IMMODAL PHARMAKA GESELLSCHAFT m.b.H. Verfahren und stoffe zur freisetzung eines wachstumsfaktors aus endothelzellen, und nach dem verfahren freigesetzter wachstumsfaktor sowie seine verwendung
NO317155B1 (no) 1997-02-04 2004-08-30 Ono Pharmaceutical Co <omega>-cykloalkyl-prostagladin-E<N>2</N>-derivater
PT1008588E (pt) 1997-02-10 2003-09-30 Ono Pharmaceutical Co Derivados da 11,15-o-diaklquil-prostaglandina e processo de producao dos mesmos e farmaco que os contem como ingrediente activo
JP2001524124A (ja) 1997-05-07 2001-11-27 ガレン（ケミカルズ）リミティド テストステロンおよびテストステロン前駆体の投与のための膣内薬物送達用具
WO1999033794A1 (en) 1997-12-25 1999-07-08 Ono Pharmaceutical Co., Ltd. φ-CYCLOALKYL-PROSTAGLANDIN E2 DERIVATIVES
JP4087938B2 (ja) 1998-02-04 2008-05-21 高砂香料工業株式会社 ヒノキチオ−ル類の分岐サイクロデキストリン包接化合物からなる抗菌剤およびそれを含有する組成物
EP1422217A3 (en) 1998-04-01 2004-06-16 Cardiome Pharma Corp. Aminocyclohexyl ether compounds and uses thereof
DE69904595T2 (de) * 1998-06-12 2003-11-27 Societe De Conseils De Recherches Et D'applications Scientifiques S.A., Paris Betacarbolinverbindungen
US20040038970A1 (en) 1998-06-12 2004-02-26 Societe De Conseils De Recherches Etd' Application Scientifiques, S.A.S. A Paris, France Corp. Beta-carboline compounds
US6235780B1 (en) 1998-07-21 2001-05-22 Ono Pharmaceutical Co., Ltd. ω-cycloalkyl-prostaglandin E1 derivatives
WO2000006556A1 (en) 1998-07-27 2000-02-10 Abbott Laboratories Substituted oxazolines as antiproliferative agents
SE9900100D0 (sv) 1999-01-15 1999-01-15 Astra Ab New compounds
US6407101B1 (en) 1999-05-04 2002-06-18 American Home Products Corporation Cyanopyrroles
US6355648B1 (en) 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
AU770377B2 (en) 1999-05-21 2004-02-19 Bristol-Myers Squibb Company Pyrrolotriazine inhibitors of kinases
ATE264330T1 (de) 1999-07-21 2004-04-15 Astrazeneca Ab Verbindungen
ES2306665T3 (es) 1999-07-21 2008-11-16 Boehringer Ingelheim Pharmaceuticals Inc. Pequeñas moleculas utiles en el tratamiento de la enfermedad inflamatoria.
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
DE1252330T1 (de) 1999-11-26 2003-11-27 Mcgill University, Montreal Loci der idiopathischen epilepsie, mutationen derselben und verfahren zu deren verwendung zur feststellung, prognose und behandlung von epilepsie
FR2807038B1 (fr) 2000-04-03 2002-08-16 Sanofi Synthelabo Nouveaux derives d'indolin-2-one, leur preparation et les compositions pharmaceutiques les contenant
AU2002213204A1 (en) 2000-10-13 2002-04-22 Bristol-Myers Squibb Company Selective maxi-K- potassium channel openers functional under conditions of high intracellular calcium concentration, methods and uses thereof
US6825220B2 (en) 2000-11-10 2004-11-30 Eli Lilly And Company 3-Substituted oxindole β 3 agonists
US6670357B2 (en) 2000-11-17 2003-12-30 Bristol-Myers Squibb Company Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors
US20030078278A1 (en) 2001-06-26 2003-04-24 Pfizer Inc. Spiropiperidine compounds as ligands for ORL-1 receptor
JP2005507872A (ja) 2001-08-14 2005-03-24 イーライ・リリー・アンド・カンパニー ３−置換オキシインドールβ３アゴニスト
US7244744B2 (en) 2001-11-01 2007-07-17 Icagen, Inc. Piperidines
EP1451160B1 (en) 2001-11-01 2010-01-13 Icagen, Inc. Pyrazole-amides for use in the treatment of pain
ES2242890T3 (es) 2001-11-20 2005-11-16 Eli Lilly And Company Agonistas beta 3 de oxindol 3-sustituido.
SE0104341D0 (sv) 2001-12-20 2001-12-20 Astrazeneca Ab New use
WO2003064425A1 (en) 2002-01-28 2003-08-07 Pfizer Japan Inc. N-substituted spiropiperidine compounds as ligands for orl-1 receptor
US7659082B2 (en) * 2002-02-19 2010-02-09 Xenon Pharmaceuticals Inc. Methods for identifying analgesic agents
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
US7250442B2 (en) 2002-03-15 2007-07-31 Eli Lilly And Company Dihydroindol-2-one derivatives as steroid hormone nuclear receptor modulators
US7595311B2 (en) 2002-05-24 2009-09-29 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
GB0213715D0 (en) 2002-06-14 2002-07-24 Syngenta Ltd Chemical compounds
MXPA04012419A (es) 2002-06-25 2005-04-19 Wyeth Corp Uso de derivados de tio-oxindol en el tratamiento de condiciones relacionadas con la hormona.
JP2005535625A (ja) 2002-06-25 2005-11-24 ワイス 皮膚障害の治療におけるチオオキシインドール誘導体の使用
US7256218B2 (en) 2002-11-22 2007-08-14 Jacobus Pharmaceutical Company, Inc. Biguanide and dihydrotriazine derivatives
KR20120102571A (ko) 2003-02-24 2012-09-18 미쓰비시 타나베 파마 코퍼레이션 테나토프라졸의 거울상 이성질체 및 치료를 위한 그 용도
CA2525866A1 (en) 2003-05-16 2004-11-25 Pfizer Products Inc. Treatment of psychotic and depressive disorders
WO2004100955A1 (en) 2003-05-16 2004-11-25 Pfizer Products Inc. Anxiety treatments with ziprasidone
CA2525323A1 (en) 2003-05-16 2004-11-25 Pfizer Products Inc. Method for enhancing cognition using ziprasidone
KR20060009938A (ko) 2003-05-16 2006-02-01 화이자 프로덕츠 인코포레이티드 양극성 장애 및 연관된 증상의 치료
PT1651620E (pt) 2003-07-30 2012-02-10 Xenon Pharmaceuticals Inc Derivados de piperizina e sua utilização como agentes terapêuticos
DE10337184A1 (de) 2003-08-13 2005-03-10 Gruenenthal Gmbh Substituierte 3-Pyrrolidin-Indol-Derivate
WO2005016913A1 (en) 2003-08-19 2005-02-24 Pfizer Japan, Inc. Tetrahydroisoquinoline or isochroman compounds as orl-1 receptor ligands for the treatment of pain and cns disorders
WO2005035498A1 (ja) 2003-10-08 2005-04-21 Dainippon Sumitomo Pharma Co., Ltd. 含窒素二環性化合物の摂食調節剤としての用途
EP1557166A1 (en) 2004-01-21 2005-07-27 Newron Pharmaceuticals S.p.A. Alpha-aminoamide derivatives useful in the treatment of lower urinary tract disorders
US7507760B2 (en) 2004-01-22 2009-03-24 Neuromed Pharmaceuticals Ltd. N-type calcium channel blockers
GB0406867D0 (en) 2004-03-26 2004-04-28 F2G Ltd Antifungal agents
JP2007530656A (ja) 2004-03-29 2007-11-01 ファイザー株式会社 ＯＲＬ１受容体拮抗薬としてのαアリールまたはヘテロアリールメチルβピペリジノプロパンアミド化合物
CA2560796A1 (en) 2004-03-29 2005-10-20 Merck & Co., Inc. Biaryl substituted pyrazinones as sodium channel blockers
WO2005099689A1 (en) 2004-04-01 2005-10-27 Case Western Reserve University Topical delivery of phthalocyanines
GT200500063A (es) 2004-04-01 2005-10-14 Metodo para tratar la esquizofrenia y/o anormalidades glucoregulatorias
US20070299102A1 (en) 2004-04-08 2007-12-27 Topo Target A/S Diphenyl Ox-Indol-2-One Compounds and Their Use in the Treatment of Cancer
WO2005104711A2 (en) 2004-04-27 2005-11-10 Wyeth Purification of progesterone receptor modulators
WO2005105753A2 (en) 2004-05-05 2005-11-10 Unibioscreen S.A. Naphthalimide derivatives, methods for their production and pharmaceutical compositions therefrom
TWI350168B (en) 2004-05-07 2011-10-11 Incyte Corp Amido compounds and their use as pharmaceuticals
CA2566477A1 (en) 2004-05-14 2005-11-24 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
AU2005267331A1 (en) 2004-06-24 2006-02-02 Incyte Corporation Amido compounds and their use as pharmaceuticals
GT200500186A (es) 2004-07-07 2006-03-02 Regimenes anticonceptivos con antagonistas del receptor de progesterona y kits
GT200500183A (es) 2004-08-09 2006-04-10 Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
GT200500185A (es) 2004-08-09 2006-04-10 Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
BRPI0515470A (pt) 2004-09-17 2008-07-22 Schering Ag processos e intermediários para preparação de inibidores de cisteìna protease
JP4677323B2 (ja) 2004-11-01 2011-04-27 キヤノン株式会社 画像処理装置及び画像処理方法
BRPI0518281A2 (pt) 2004-11-18 2008-11-18 Incyte Corp inibidores de 11-beta hidroxilesteràide desidrogenase do tipo i e mÉtodos uso dos mesmos
DE102005007694A1 (de) 2005-02-18 2006-09-21 Henkel Kgaa Mittel zum Färben von keratinhaltigen Fasern
CA2598690C (en) 2005-02-22 2011-11-15 The Regents Of The University Of Michigan Small molecule inhibitors of mdm2 and uses thereof
AR053710A1 (es) 2005-04-11 2007-05-16 Xenon Pharmaceuticals Inc Compuestos espiroheterociclicos y sus usos como agentes terapeuticos
MY158766A (en) 2005-04-11 2016-11-15 Xenon Pharmaceuticals Inc Spiro-oxindole compounds and their uses as therapeutic agents
AR056317A1 (es) 2005-04-20 2007-10-03 Xenon Pharmaceuticals Inc Compuestos de oxindol y composicion farmaceutica
AR053713A1 (es) 2005-04-20 2007-05-16 Xenon Pharmaceuticals Inc Compuestos heterociclicos y sus usos como agentes terapeuticos
GT200600179A (es) 2005-04-29 2006-11-22 Proceso para preparar oxindoles y tio-oxindoles 3,3-disustituidos
TW200716632A (en) 2005-05-16 2007-05-01 Gilead Sciences Inc Integrase inhibitor compounds
PL1924264T3 (pl) 2005-09-01 2014-03-31 Hoffmann La Roche Diaminopirymidyny jako modulatory P2X<sub>3</sub> I P2X<sub>2/3</sub>
US7888345B2 (en) 2006-06-09 2011-02-15 Merck Sharp & Dohme Corp. Benzaepinones as sodium channel blockers
TW200812962A (en) * 2006-07-12 2008-03-16 Astrazeneca Ab New compounds I/418
WO2008046065A1 (en) * 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Spiroheterocyclic compounds and their uses as therapeutic agents
RU2009117642A (ru) 2006-10-12 2010-11-20 Ксенон Фармасьютикалз Инк. (Ca) Применение спирооксиндоловых соединений в качестве терапевтических средств
WO2008046087A2 (en) 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Spiro compounds and their uses as therapeutic agents
WO2008046084A2 (en) * 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Spiroheterocyclic compounds and their uses as therapeutic agents
WO2008046082A2 (en) 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Use of heterocyclic compounds as therapeutic agents
US20110294842A9 (en) 2006-10-12 2011-12-01 Xenon Pharmaceuticals Inc. Spiro (furo [3, 2-c] pyridine-3-3' -indol) -2' (1'h)-one derivatives and related compounds for the treatment of sodium-channel mediated diseases, such as pain
WO2008046083A2 (en) 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Use of oxindole compounds as therapeutic agents
CA2666136A1 (en) * 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Tricyclic spiro-oxindole derivatives and their uses as therapeutic agents
GB0704846D0 (en) 2007-03-13 2007-04-18 Futura Medical Dev Ltd Topical pharmaceutical formulation
WO2008117050A1 (en) 2007-03-27 2008-10-02 Astrazeneca Ab Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer
MX2009012834A (es) 2007-05-29 2010-05-17 Intrexon Corp Ligandos quirales de diacilhidrazina para modular la expresion de genes exogenos por medio de un complejo receptor de ecdisona.
US8101647B2 (en) 2008-10-17 2012-01-24 Xenon Pharmaceuticals Inc. Spiro-oxindole compounds and their use as therapeutic agents
HRP20150882T1 (hr) 2008-10-17 2015-09-25 Xenon Pharmaceuticals Inc. Spirooksindolski spojevi i njihova upotreba kao terapijska sredstva
WO2010053998A1 (en) * 2008-11-05 2010-05-14 Xenon Pharmaceuticals, Inc. Spiro-condensed indole derivatives as sodium channel inhibitors
US20110269788A1 (en) 2008-12-29 2011-11-03 Xenon Pharmaceuticals Inc. Spiro-oxindole-derivatives as sodium channel blockers
WO2010132352A2 (en) 2009-05-11 2010-11-18 Xenon Pharmaceuticals Inc. Spiro compounds and their use as therapeutic agents
AR077252A1 (es) 2009-06-29 2011-08-10 Xenon Pharmaceuticals Inc Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos
WO2011047173A2 (en) 2009-10-14 2011-04-21 Xenon Pharmaceuticals Inc. Pharmaceutical compositions for oral administration
NZ599334A (en) 2009-10-14 2014-03-28 Xenon Pharmaceuticals Inc Synthetic methods for spiro-oxindole compounds
CN102946859B (zh) 2010-02-26 2016-03-02 泽农医药公司 用于局部给药的螺-羟吲哚化合物的药物组合物及其作为治疗剂的用途
KR20150002794A (ko) 2012-04-12 2015-01-07 제논 파마슈티칼스 인크. 치료제로서 유용한 스파이로-옥시인돌 화합물을 위한 비대칭적 합성

Also Published As

Publication number Publication date
SI2350090T1 (sl) 2015-10-30
JP5554337B2 (ja) 2014-07-23
MY155255A (en) 2015-09-30
CY1116628T1 (el) 2017-03-15
JO3032B1 (ar) 2016-09-05
US20120295897A1 (en) 2012-11-22
JP2015010090A (ja) 2015-01-19
SMT201500206B (it) 2015-10-30
PT2350090E (pt) 2015-11-13
BRPI0920448A2 (pt) 2018-10-23
US8263606B2 (en) 2012-09-11
HK1160470A1 (en) 2012-08-17
IL212400A (en) 2017-05-29
SG10201703082XA (en) 2017-06-29
HK1215572A1 (en) 2016-09-02
HK1219272A1 (zh) 2017-03-31
CN106928247A (zh) 2017-07-07
US20100137299A1 (en) 2010-06-03
EP2350090A2 (en) 2011-08-03
EP2942350A1 (en) 2015-11-11
JP2012505895A (ja) 2012-03-08
CN103664973A (zh) 2014-03-26
HK1218294A1 (zh) 2017-02-10
EP2350090B1 (en) 2015-06-03
CN105175433A (zh) 2015-12-23
CA2741029A1 (en) 2010-04-22
KR20110086051A (ko) 2011-07-27
RU2011119626A (ru) 2012-11-27
JP5834104B2 (ja) 2015-12-16
NZ592275A (en) 2013-04-26
AU2009303468A1 (en) 2010-04-22
US20170114075A1 (en) 2017-04-27
CN105218565A (zh) 2016-01-06
KR101286323B1 (ko) 2013-07-15
TW201020257A (en) 2010-06-01
CN102256983B (zh) 2017-04-05
MX2011004055A (es) 2011-06-24
HUE025938T2 (en) 2016-05-30
DK2350090T3 (en) 2015-09-07
HRP20150882T1 (hr) 2015-09-25
CN102256983A (zh) 2011-11-23
ES2546302T3 (es) 2015-09-22
IL249941A0 (en) 2017-03-30
IL212400A0 (en) 2011-06-30
US9458178B2 (en) 2016-10-04
US20150291623A1 (en) 2015-10-15
PE20110586A1 (es) 2011-09-03
WO2010045251A2 (en) 2010-04-22
CN103664973B (zh) 2017-04-19
US8916580B2 (en) 2014-12-23
CL2011000835A1 (es) 2011-07-22
AU2009303468B2 (en) 2014-08-28
SG10201703086VA (en) 2017-05-30
US8415370B2 (en) 2013-04-09
US20130252962A1 (en) 2013-09-26
PL2350090T3 (pl) 2015-11-30
WO2010045251A3 (en) 2010-11-18

Similar Documents

Publication Publication Date Title
AR073900A1 (es) Compuestos de espiro-oxindol y su uso como agentes terapeuticos.
JP2012505895A5 (es)
RU2491285C2 (ru) Органические соединения
DK3002283T3 (en) THIAZOLE DERIVATIVES.
IL258577A (en) 2,4-dihydroxy-nicotinamides as apj agonists
JP2013545744A5 (es)
RU2014152625A (ru) Конденсированные с гетероарилкетонами азадекалины - модуляторы глюкокортикоидных рецепторов
JP2018530591A5 (es)
RU2018147424A (ru) Новые (гетеро)арил-замещенные пиперидинильные производные, способ их получения и фармацевтические композиции, содержащие их
RU2017118562A (ru) Соединения-антагонисты дофаминового d3-рецептора
SI2978755T1 (en) New pyridine derivatives
RU2426731C2 (ru) Производные арил-изоксазоло-4-ил-оксадиазола
JP2019512482A5 (es)
JP2015517580A5 (es)
JP2015521999A5 (es)
RU2012102908A (ru) Азаадамантановые производные и способы применения
RU2019132212A (ru) Селективные ингибиторы hdac6
JP2016523911A5 (es)
JP2015510938A5 (es)
JP2013544873A5 (es)
RU2007107177A (ru) Соединения и композиции, как модуляторы ядерных рецепторов стероидных гормонов
JP2019528247A5 (es)
JP2015522002A5 (es)
HRP20211380T1 (hr) Derivati pirimidina kao modulatori receptora pge2
JP2019524732A5 (es)

Legal Events

Date Code Title Description
FB Suspension of granting procedure