[go: up one dir, main page]

AR056892A1 - Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa - Google Patents

Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa

Info

Publication number
AR056892A1
AR056892A1 ARP060105619A ARP060105619A AR056892A1 AR 056892 A1 AR056892 A1 AR 056892A1 AR P060105619 A ARP060105619 A AR P060105619A AR P060105619 A ARP060105619 A AR P060105619A AR 056892 A1 AR056892 A1 AR 056892A1
Authority
AR
Argentina
Prior art keywords
heterocycloalkyl
heteroaryl
cycloalkyl
alkyl
aryl
Prior art date
Application number
ARP060105619A
Other languages
English (en)
Original Assignee
Astra Ab
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=38188915&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR056892(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astra Ab filed Critical Astra Ab
Publication of AR056892A1 publication Critical patent/AR056892A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/28—Cinnolines
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/04—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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos compuestos se utilizan en el tratamiento o prevencion de los trastornos de la ansiedad, trastornos y/o trastornos del estado de ánimo. También son utilizados en composiciones farmacéuticas y en la fabricacion de medicamentos con actividad moduladora de GABAA. Se proveen además métodos de síntesis de los mismos. Reivindicacion 1: Un compuesto de la formula (1), o una de sus sales, tautomeros, atropisomeros o precursores hidrolizables in vivo farmacéuticamente aceptables, donde R1 es alquilo C1-6, haloalquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 o 5 R7; R2 es H, C(=O)Rb, C(=O)NRcRd, C(O)ORa, S(O)2Rb, alquilo C1-6, haloalquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde cada uno de los alquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4 o 5 R8; R3, R4 y R5 son cada uno, de modo independiente, H, halo, Si(alquilo C1- 10)3, CN, NO2, ORa, SRa, OC(=O)Ra, OC(=O)ORb, OC(=O)NRcRCd, C(=O)Ra, C(=O)ORb, C(=O)NRcRd, NRcRd, NRcC(=O)Ra, N RcC(O)ORb, NRcS(O)2Rb, S(=O)Ra, S(=O)NRcRd, S(=O)2Ra, S(=O)2NRcRd, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2 o 3 R9; R6 es arilo, cicloalquilo, heteroarilo o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 o 5 A1; R7, R8 y R9 son cada uno, de modo independiente, halo, alquilo C1-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', SRa', C(=O)Rb', C(=O)NRc'Rd', C(=O)ORa', OC(=O)Rb', OC(=O)NRc'Rd', NRc'Rd', NRc'C(=O)Rb', NRc'C(=O)ORa', NRc'S(=O)2Rb', S(=O)Rb', S(=O)NRc'Rd', S(=O)2Rb' o S(=O)2NRc'Rd'; A1 es halo, CN, NO2, ORa, SRa, C(=O)Rb, C(=O)NRcRd, C(=O)ORa, OC(=O)Rb, OC(=O)NRcRd, NRcRd, NRcC(=O)Rd, NRcC(=O)ORa, NRcS(=O)Rb, NRcS(=O)2Rb, S(=O)Rb, S(=O)NRcRd, S(=O)2Rb, S(O)2NRcRd, alcoxi C1-4, haloalcoxi C1-4, amino, alquil C1-4-amino, dialquil C2-4-amino, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, donde cada uno de los alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo, arilo, cicloalquilo, heterocicloalquilalquilo, heteroarilo o heterocicloalquilo está opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados, de modo independiente, de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', SRa', C(=O)Rb', C(=O)NRc'Rd', C(=O)ORa', OC(=O)Rb', OC(=O)NRc'Rd', NRc'Rd', NRc'C(=O)Rb', NRc'C(=O)ORa', NRc'S(=O)Rb', NRc'S(=O)2Rb', S(=O)Rb', S(O)NRc'Rd', S(=O)2Rb' o S(=O)2Rc'Rd'; Ra y Ra' son cada uno, de modo independiente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; Rb y Rb' son cada uno, de modo independiente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; Rc y Rd son cada uno, de modo independiente, H, alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; o Rc y Rd junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; y Rc' y Rd' son cada uno, de modo independiente, H, alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; o Rc' y Rd' junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; con la condicion de que, cuando R2, R3, R4 y R5 son cada uno H, entonces R6 sea distinto de fenilo no sustituido o cicloalquilo no sustituido.
ARP060105619A 2005-12-20 2006-12-19 Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa AR056892A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US75213705P 2005-12-20 2005-12-20
US82369306P 2006-08-28 2006-08-28

Publications (1)

Publication Number Publication Date
AR056892A1 true AR056892A1 (es) 2007-10-31

Family

ID=38188915

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060105619A AR056892A1 (es) 2005-12-20 2006-12-19 Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa

Country Status (18)

Country Link
US (2) US7425556B2 (es)
EP (1) EP1966158B1 (es)
JP (2) JP5148507B2 (es)
KR (1) KR20080080206A (es)
CN (1) CN104592128A (es)
AR (1) AR056892A1 (es)
AU (1) AU2006327300A1 (es)
BR (1) BRPI0620126A2 (es)
CA (1) CA2634305A1 (es)
EC (1) ECSP088585A (es)
ES (1) ES2391472T3 (es)
IL (1) IL191762A0 (es)
NO (1) NO20083197L (es)
NZ (1) NZ569607A (es)
RU (1) RU2008122405A (es)
SA (1) SA06270474B1 (es)
UY (1) UY30032A1 (es)
WO (1) WO2007073283A1 (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104592128A (zh) * 2005-12-20 2015-05-06 阿斯利康(瑞典)有限公司 作为gabaa受体调节剂的取代的噌啉衍生物及其合成方法
US7465795B2 (en) * 2005-12-20 2008-12-16 Astrazeneca Ab Compounds and uses thereof
US20100105614A1 (en) 2006-10-25 2010-04-29 Somaxon Pharmaceuticals, Inc. Ultra low dose doxepin and methods of using the same to treat sleep disorders
WO2008070795A2 (en) * 2006-12-06 2008-06-12 Somaxon Pharmaceuticals, Inc. Combination therapy using low-dose doxepin for the improvement of sleep
TW200911760A (en) * 2007-06-19 2009-03-16 Astrazeneca Ab Compounds and uses thereof
WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
US9173864B2 (en) * 2008-10-22 2015-11-03 House Ear Institute Treatment and/or prevention of inner ear conditions by modulation of a metabotropic glutamate receptor
WO2010123441A1 (en) * 2009-04-21 2010-10-28 Astrazeneca Ab Crystalline form of 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n-propylcinnoline-3- carboxamide hydrogen sulphate, for treatment of anxiety disorders
WO2010123443A1 (en) * 2009-04-21 2010-10-28 Astrazeneca Ab Pharmaceutical composition comprising 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n- propylcinnoline-3-carboxamide hydrogen sulphate.
WO2010123440A1 (en) * 2009-04-21 2010-10-28 Astrazeneca Ab Pharmaceutical composition comprising 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n- propylcinnoline-3-carboxamide hydrogen sulphate and rate-controlling polymer
WO2011021979A1 (en) * 2009-08-18 2011-02-24 Astrazeneca Ab Cinnoline compounds, their preparation, and their use
CN103124496B (zh) 2010-10-06 2016-03-30 葛兰素史密丝克莱恩有限责任公司 作为pi3激酶抑制剂的苯并咪唑衍生物
EP2726465A1 (en) * 2011-05-23 2014-05-07 Elan Pharmaceuticals Inc. Inhibitors of lrrk2 kinase activity
US9365566B2 (en) 2012-03-27 2016-06-14 Takeda Pharmaceutical Company Limited Cinnoline derivatives
JP6152260B2 (ja) 2012-11-01 2017-06-21 昭和電工パッケージング株式会社 電池用外装材及び電池
US9844551B2 (en) * 2015-01-14 2017-12-19 Children's Hospital Medical Center Compositions and methods for treatment of fragile X syndrome
PL3615527T3 (pl) * 2017-06-30 2024-07-01 Elanco Animal Health Gmbh Nowe pochodne azachinoliny
WO2020065642A1 (en) 2018-09-25 2020-04-02 Pepticom Ltd. Positive allosteric modulators of gabaa receptor
WO2021204930A1 (en) 2020-04-09 2021-10-14 Bayer Animal Health Gmbh Substituted condensed azines as anthelmintic compounds
GB202016245D0 (en) * 2020-10-13 2020-11-25 Univ College Cardiff Consultants Ltd Compounds
WO2024222712A1 (zh) * 2023-04-24 2024-10-31 上海赛默罗生物科技有限公司 咪唑并吡啶或咪唑并吡嗪类化合物、其制备方法、药物组合物和用途

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4230713A (en) * 1979-01-19 1980-10-28 Ici Americas Inc. Heterocyclic tetrahydro-1-alkyl-4-oxo-1H-imidazol-2-ylidene urea and phenyl esters of tetrahydro-1-alkyl-4-oxo-1H-imidazol-2-ylidene carbamic acid compounds
US4511568A (en) * 1982-05-12 1985-04-16 Ici Americas Inc. CNS-Depressant pyrazolopyridines
US4552883A (en) * 1982-06-15 1985-11-12 Ici Americas Inc. Pyrazolo[3,4-b]pyridine carboxylic acid esters and their pharmaceutical use
US4563525A (en) * 1983-05-31 1986-01-07 Ici Americas Inc. Process for preparing pyrazolopyridine compounds
GB8329531D0 (en) * 1983-11-04 1983-12-07 Ici America Inc Pyrazolopyridine cycloalkanones
GB8421116D0 (en) * 1984-08-20 1984-09-26 Ici America Inc Alkynyl derivatives
GB8425104D0 (en) * 1984-10-04 1984-11-07 Ici America Inc Amide derivatives
GB8513639D0 (en) * 1985-05-30 1985-07-03 Ici America Inc Cinnoline compounds
GB8610980D0 (en) * 1986-05-06 1986-06-11 Ici America Inc Heterocyclic fused tricyclic compounds
DD249011A5 (de) 1986-06-20 1987-08-26 Ici Americas Inc,Us Verfahren zur herstellung von cinnolin-verbindungen
ES2051996T3 (es) * 1988-02-09 1994-07-01 Ici America Inc Producto farmaceutico.
US4925844A (en) * 1988-02-09 1990-05-15 Ici Americas Inc. Antagonizing the pharmacological effects of a benzodiazepine receptor agonist
US5190951A (en) * 1990-10-19 1993-03-02 Ss Pharmaceutical Co., Ltd. Quinoline derivatives
US5240934A (en) * 1990-10-19 1993-08-31 Ss Pharmaceutical Co., Ltd. Quinoline derivatives
WO1992016497A1 (fr) 1991-03-22 1992-10-01 Japan Tobacco Inc. Derive d'acide amine ayant une activite inhibant la renine
DE69222637T2 (de) 1991-05-10 1998-02-26 Rhone Poulenc Rorer Int Bis mono- und bicyclische aryl- und heteroarylderivate mit inhibierender wirkung auf die egf und/oder pdgf-rezeptor tyrosinkinase
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5750088A (en) * 1993-03-30 1998-05-12 The Dupont Merck Pharmaceutical Company Stable hydrazones linked to a peptide moiety as reagents for the preparation of radiopharmaceuticals
DE59607957D1 (de) 1995-07-25 2001-11-22 Clariant Gmbh Katalysatoren zur durchführung von kreuzkupplungsreaktionen
DE19620023C2 (de) * 1996-05-17 2001-03-08 Celanese Chem Europe Gmbh Verfahren zur Herstellung von Phosphinat- oder Phosphonatgruppen enthaltenden tertiären Phosphanen und neue Phosphinatgruppen enthaltende tertiäre Phosphane
GB9607219D0 (en) 1996-04-04 1996-06-12 Smithkline Beecham Plc Novel compounds
AU2825899A (en) 1998-03-12 1999-09-27 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
ES2183532T3 (es) * 1998-03-18 2003-03-16 Ciba Sc Holding Ag Reacciones de copulacion con catalizadores de paladio.
US6362216B1 (en) * 1998-10-27 2002-03-26 Array Biopharma Inc. Compounds which inhibit tryptase activity
DE19916222A1 (de) 1999-04-10 2000-10-19 Aventis Res & Tech Gmbh & Co Verfahren zur Herstellung von Biarylen
GB9919957D0 (en) 1999-08-23 1999-10-27 Merck Sharp & Dohme Therapeutic agents
GB9921150D0 (en) 1999-09-07 1999-11-10 Merck Sharp & Dohme Therapeutic agents
GB9921351D0 (en) 1999-09-09 1999-11-10 Merck Sharp & Dohme Therapeutic agents
GB9927687D0 (en) 1999-11-23 2000-01-19 Merck Sharp & Dohme Therapeutic agents
FR2801584B1 (fr) * 1999-11-26 2003-05-30 Rhodia Chimie Sa Procede de preparation d'un compose polyaromatique
GB9929687D0 (en) 1999-12-15 2000-02-09 Merck Sharp & Dohme Therapeutic agents
GB9929685D0 (en) 1999-12-15 2000-02-09 Merck Sharp & Dohme Therapeutic agents
EP1265872A1 (en) 2000-03-21 2002-12-18 PHARMACIA & UPJOHN COMPANY 4-hydroxycinnoline-3-carboxyamides as antiviral agents
MY145722A (en) * 2000-04-27 2012-03-30 Abbott Lab Diazabicyclic central nervous system active agents
AU2001259052B2 (en) 2000-05-19 2006-03-02 Eli Lilly And Company A process for preparing biphenyl compounds
US6984756B2 (en) * 2000-05-19 2006-01-10 Eli Lilly And Company Process for preparing biphenyl compounds
US6642229B2 (en) 2000-05-24 2003-11-04 Merck Sharp & Dohme Ltd. 3-Phenyl-imidazo-pyrimidine derivatives as ligands for GABA receptors
AUPQ841300A0 (en) 2000-06-27 2000-07-20 Fujisawa Pharmaceutical Co., Ltd. New aminoalcohol derivatives
GB0018473D0 (en) 2000-07-27 2000-09-13 Merck Sharp & Dohme Therapeutic agents
AU2001297674A1 (en) 2000-11-01 2002-08-19 Primarion, Inc. Method and apparatus for detecting valid signal information
EP1343788B1 (en) 2000-11-10 2005-11-23 MERCK SHARP & DOHME LTD. Imidazo-triazine derivatives as ligands for gaba receptors
GB0027561D0 (en) 2000-11-10 2000-12-27 Merck Sharp & Dohme Therapeutic agents
GB0111191D0 (en) 2001-05-08 2001-06-27 Merck Sharp & Dohme Therapeutic agents
WO2003003009A1 (en) 2001-06-29 2003-01-09 7Tm Pharma A/S Use of metal-ion chelates in validating biological molecules as drug targets in test animal models
GB0117060D0 (en) 2001-07-12 2001-09-05 Merck Sharp & Dohme Therapeutic agents
GB0119828D0 (en) 2001-08-14 2001-10-10 Merck Sharp & Dohme Therapeutic agents
GB0119803D0 (en) 2001-08-14 2001-10-10 Merck Sharp & Dohme Therapeutic agents
GB0120345D0 (en) 2001-08-21 2001-10-17 Merck Sharp & Dohme Therapeutic agents
AUPR738301A0 (en) 2001-08-30 2001-09-20 Starpharma Limited Chemotherapeutic agents
GB0122696D0 (en) 2001-09-20 2001-11-14 Merck Sharp & Dohme Therapeutic agents
EP1513522A2 (en) 2002-01-18 2005-03-16 Sri International Methods of treating conditions associated with an edg receptor
US20050113283A1 (en) * 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
GB0208394D0 (en) 2002-04-11 2002-05-22 Merck Sharp & Dohme Therapeutic agents
PL189894B1 (pl) * 2002-04-15 2005-10-31 Univ Medyczny W Lodzi Sposób wytwarzania 6,7,8-podstawionych kwasów 4-hydroksycynnolino-3-karboksylowych
GB0210127D0 (en) 2002-05-02 2002-06-12 Merck Sharp & Dohme Therapeutic agents
GB0210124D0 (en) 2002-05-02 2002-06-12 Merck Sharp & Dohme Therapeutic agents
GB0212049D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
GB0212048D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
EP1525030A1 (en) 2002-07-17 2005-04-27 Warner-Lambert Company LLC Combination of an allosteric alkyne inhibitor of matrix metalloproteinase-13 with a selective inhibitor of cyclooxygenase-2 that is not celecoxib or valdecoxib
GB0218876D0 (en) 2002-08-13 2002-09-25 Merck Sharp & Dohme Therapeutic agents
DE60325865D1 (de) 2002-08-13 2009-03-05 Merck Sharp & Dohme Phenylpyridazin derivative als liganden für gaba-rezeptoren
SE0202461D0 (sv) * 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
CA2500952C (en) 2002-10-04 2011-04-26 Prana Biotechnology Limited Neurologically-active compounds
US20040102360A1 (en) * 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
EP1556053A4 (en) * 2002-10-31 2006-04-19 Amgen Inc ANTI-INFLAMMATORY AGENTS
GB0225501D0 (en) 2002-11-01 2002-12-11 Merck Sharp & Dohme Therapeutic agents
GB0226462D0 (en) 2002-11-13 2002-12-18 Merck Sharp & Dohme Therapeutic agents
US20040167165A1 (en) * 2003-01-16 2004-08-26 Geetha Shankar Methods of treating conditions associated with an Edg-7 receptor
GB0301350D0 (en) 2003-01-21 2003-02-19 Merck Sharp & Dohme Therapeutic agents
WO2004076452A1 (en) 2003-02-26 2004-09-10 Merck Sharp & Dohme Limited 5,8-DIFLUOROIMIDAZO[1,2-a]PYRIDINES AS GABA-A α2/α3 LIGANDS FOR TREATING ANXIETY AND/OR DEPRESSION
TW200505902A (en) * 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
US7767817B2 (en) 2003-09-05 2010-08-03 Binghe Wang Water soluble boronic acid fluorescent reporter compounds and methods of use thereof
JP2007505121A (ja) 2003-09-08 2007-03-08 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
BRPI0416692A (pt) 2003-11-19 2007-01-30 Array Biopharma Inc inibidores heterocìclicos de mek e métodos de emprego destes
WO2006124996A2 (en) * 2005-05-17 2006-11-23 Supergen, Inc. Inhibitors of polo-like kinase-1
US7465795B2 (en) * 2005-12-20 2008-12-16 Astrazeneca Ab Compounds and uses thereof
CN104592128A (zh) * 2005-12-20 2015-05-06 阿斯利康(瑞典)有限公司 作为gabaa受体调节剂的取代的噌啉衍生物及其合成方法
TW200911760A (en) * 2007-06-19 2009-03-16 Astrazeneca Ab Compounds and uses thereof

Also Published As

Publication number Publication date
JP2009520021A (ja) 2009-05-21
JP5148507B2 (ja) 2013-02-20
US20070142328A1 (en) 2007-06-21
CA2634305A1 (en) 2007-06-28
EP1966158A4 (en) 2011-01-26
JP5474153B2 (ja) 2014-04-16
UY30032A1 (es) 2007-07-31
AU2006327300A1 (en) 2007-06-28
IL191762A0 (en) 2008-12-29
JP2012255041A (ja) 2012-12-27
NO20083197L (no) 2008-09-10
WO2007073283A1 (en) 2007-06-28
BRPI0620126A2 (pt) 2011-11-01
ECSP088585A (es) 2008-07-30
SA06270474B1 (ar) 2010-12-07
EP1966158B1 (en) 2012-08-08
ES2391472T3 (es) 2012-11-27
RU2008122405A (ru) 2010-01-27
KR20080080206A (ko) 2008-09-02
NZ569607A (en) 2011-06-30
US20090036454A1 (en) 2009-02-05
US7425556B2 (en) 2008-09-16
EP1966158A1 (en) 2008-09-10
CN104592128A (zh) 2015-05-06

Similar Documents

Publication Publication Date Title
AR056892A1 (es) Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa
AR078786A1 (es) Derivados de la cromenona
AR036659A1 (es) Compuestos derivados de fenil-piperazina, fenil-piperidina y fenil-tetrahidropiridina como inhibidores de la reabsorcion de la serotonina, una composicion farmaceutica y utilizacion de los mismos para la preparacion de medicamentos
AR073701A1 (es) Derivados de indol y de indolicina, metodos para su preparacion, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades neurodegenerativas.
AR043508A1 (es) 1-amino 1-h-imidazoquinolinas y su uso como inmunomoduladores
AR067027A1 (es) Derivados de 2, 3-dihidro-1h-pirrol[3, 4b]quinolin-1-ona, una composicion farmaceutica que los comprende y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la modulacion de la actividad del receptor gaba a.
AR052903A1 (es) Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno.
AR057131A1 (es) Derivados de purina como inmunomodulador
AR083849A1 (es) Antagonistas de mdm2 de espiro-oxindol
AR049399A1 (es) Difenilimidazopirimidina e -imidazol aminas como inhibidores de b-secretasa y metodo de obtencion de los mismos
AR094300A1 (es) Derivados de quinolonas
AR087760A1 (es) Heterociclilaminas como inhibidores de pi3k
RU2012110246A (ru) Замещенные бензоазепины в качестве модуляторов toll-подобного рецептора
AR083367A1 (es) Compuestos de tipo quinazolinona como antagonistas de crth
AR045955A1 (es) Compuestos benzoimidazolicos
RU2016135922A (ru) Терапевтические соединения и композиции
AR084976A1 (es) Compuestos de bifenileno sustituidos y metodos de uso de los mismos para el tratamiento de enfermedades virales
PE20212253A1 (es) Compuestos de piperidina urea 4-metilsulfonil-sustituidos para el tratamiento de miocardiopatia dilatada (mcd)
AR063804A1 (es) Compuestos de azoniabiciclo[2.2.2]octano
RU2008126245A (ru) Комбинация ингибитора асне и антагониста 5-нт для лечения когнитивной дисфункции
AR044614A1 (es) Composiciones de sulfonamida que modulan la actividad del receptor de quinioquinas (ccr4)
AR086100A1 (es) Compuestos de cromenona y composiciones farmaceuticas que los contienen
AR048789A1 (es) Derivados de oxazol y sus composiciones como moduladores de receptor activado de proliferador de peroxisoma (ppar)
AR073043A1 (es) Compuestos de azetidinas polisustituidos, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de los mismos en el tratamiento de enfermedades respiratorias, metabolicas y del sistema nervioso central, entre otras.
AR116474A1 (es) DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV

Legal Events

Date Code Title Description
FA Abandonment or withdrawal