[go: up one dir, main page]

AR099363A1 - Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil y pirrolo[2,3-d]piridinil acrilamidas - Google Patents

Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil y pirrolo[2,3-d]piridinil acrilamidas

Info

Publication number
AR099363A1
AR099363A1 ARP140104517A ARP140104517A AR099363A1 AR 099363 A1 AR099363 A1 AR 099363A1 AR P140104517 A ARP140104517 A AR P140104517A AR P140104517 A ARP140104517 A AR P140104517A AR 099363 A1 AR099363 A1 AR 099363A1
Authority
AR
Argentina
Prior art keywords
straight
branched chain
chain alkyl
alkyl
aryl
Prior art date
Application number
ARP140104517A
Other languages
English (en)
Inventor
I TRUJILLO John
Jal Unwalla Rayomand
Thorarensen Atli
Telliez Jean
Ian Baptiste - Montgomery Justin
David Langille Jonathan
Merrill Hayward Matthew
Matthew Gilbert Adam
Edward Flanagan Mark
Wadsworth Coe Jotham
Che Ye
Casimiro-Garca Agustin
Frank Brown Matthew
Original Assignee
Pfizer
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=52144776&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR099363(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of AR099363A1 publication Critical patent/AR099363A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61P1/04—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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P25/08—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/08—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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • A61P9/10—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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—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
    • C07D498/02—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 two hetero rings
    • C07D498/04—Ortho-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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

La presente proporciona pirrolo[2,3-d]pirimidinil y pirrolo[2,3-d]piridinil acrilamidas farmacéuticamente activas y análogos de estas. Estos compuestos son útiles para la inhibición de la quinasa Janus (JAK). También se refiere a composiciones que comprenden métodos para obtener tales compuestos, y a métodos para el tratamiento y la prevención de afecciones mediadas por JAK. Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1) o una sal o un solvato aceptables desde el punto de vista farmacéutico de aquel, o un enantiómero o diastereómero de aquel, y en donde R² se selecciona del grupo que consiste en hidrógeno, deuterio, C₁₋₆ alquilo de cadena lineal o ramificada, C₃₋₆ cicloalquilo, C₆₋₁₀ arilo, heteroarilo monocíclico o bicíclico, que comprende anillos de 5 y/o 6 miembros, (aril)C₁₋₆ alquilo de cadena lineal o ramificada, (heteroaril)C₁₋₆ alquilo de cadena lineal o ramificada, (heterociclil)C₁₋₆ alquilo de cadena lineal o ramificada, (C₁₋₆ alquil de cadena lineal o ramificada)arilo, (C₁₋₆ alquil de cadena lineal o ramificada)heteroarilo, (C₁₋₆ alquil cadena lineal o ramificada)heterociclilo, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, C₁₋₆ alcoxi de cadena lineal o ramificada, C₁₋₆ perfluoroalcoxi de cadena lineal o ramificada, halógeno, ciano, hidroxilo, amino, carboxi, aminocarbonilo, (C₁₋₆ alquil de cadena lineal o ramificada)aminocarbonilamino, (C₁₋₆ alquil de cadena lineal o ramificada)aminocarbonilo, -SOR¹², -SO₂R¹², -NR¹³SO₂R¹², -SO₂NR¹³R¹⁴ y -NR¹³SO₂NR¹⁴R¹⁵; en donde tal alquilo, arilo y heteroarilo se sustituyen, independientemente y de manera opcional, con uno o más sustituyentes seleccionados del grupo que consiste en halo, hidroxi, metoxi, amino, ciano, alquilamino, dialquilamino, CF₃, aminocarbonilo, (C₁₋₆ alquil de cadena lineal o ramificada)aminocarbonilo y C₃₋₆cicloalquilo; R³ se selecciona del grupo que consiste en hidrógeno, deuterio, C₁₋₆ alquilo de cadena lineal o ramificada, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, halógeno y ciano; A es --(CRᵃRᵇ)q-(CRᶜRᵈ)ʳ--, en donde Rᵃ, Rᵇ, Rᶜ y Rᵈ se seleccionan independientemente de hidrógeno, C₁₋₆ alquilo de cadena lineal o ramificada, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, C₆₋₁₀ arilo, heteroarilo monocíclico o bicíclico, que comprende anillos de 5 y/o 6 miembros, alquilarilo, (aril)C₁₋₆ alquilo de cadena lineal o ramificada, (heteroaril)C₁₋₆ alquilo de cadena lineal o ramificada, halógeno, ciano, hidroxilo, C₁₋₆ alcoxi de cadena lineal o ramificada, amino, carboxi, aminocarbonilo, (heterociclil)C₁₋₆ alquilo de cadena lineal o ramificada, (C₁₋₆ alquilo de cadena lineal o ramificada)arilo, (C₁₋₆ alquilo de cadena lineal o ramificada)heteroarilo y (C₁₋₆ alquilo de cadena lineal o ramificada)heterociclilo, en donde tal alquilo también se sustituye opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste en halo, hidroxi, metoxi, amino, alquilamino, dialquilamino, CF₃ y C₃₋₆ cicloalquilo; R⁰, R¹, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹ y R¹⁰ se seleccionan independientemente de hidrógeno, C₁₋₆ alquilo de cadena lineal o ramificada, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, C₆₋₁₀ arilo, heteroarilo monocíclico o bicíclico, que comprende anillos de 5 y/o 6 miembros, (aril)C₁₋₆ alquilo de cadena lineal o ramificada, (heteroaril)C₁₋₆ alquilo de cadena lineal o ramificada, heteroarilo, halógeno, ciano, hidroxilo, C₁₋₆ alcoxi de cadena lineal o ramificada, amino, carboxi, aminocarbonilo, (heterociclil)C₁₋₆ alquilo de cadena lineal o ramificada, (C₁₋₆ alquilo de cadena lineal o ramificada)arilo, (C₁₋₆ alquilo de cadena lineal o ramificada)heteroarilo y (C₁₋₆ alquilo de cadena lineal o ramificada)heterociclilo, en donde tal alquilo también se sustituye opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste en halo, hidroxi, metoxi, amino, alquilamino, dialquilamino, CF₃, y C₃₋₆ cicloalquilo; en donde, de manera alternativa, R⁰ o R¹, y/o R⁶ o R⁷, respectivamente juntos con cualquiera de R⁴, R⁵, Rᵃ, Rᵇ, Rᶜ o Rᵈ, pueden formar independientemente un enlace o una cadena C₁₋₆ alquilo lineal; y/o, de manera alternativa, R⁴ o R⁵, respectivamente juntos con cualquiera de Rᵃ, Rᵇ, Rᶜ o Rᵈ, pueden formar independientemente un enlace o una cadena C₁₋₆ alquilo lineal; y/o, de manera alternativa, R⁸ y R⁹ pueden forman juntos un anillo de 3 - 6 miembros que contiene opcionalmente uno o dos átomos de O ó N; R¹¹ es hidrógeno o deuterio; R¹², R¹³, R¹⁴ y R¹⁵ se seleccionan independientemente de hidrógeno, C₁₋₆ alquilo de cadena lineal o ramificada, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, C₆₋₁₀ arilo, alquilarilo y (aril)C₁₋₆ alquilo de cadena lineal o ramificada; Y es O ó N, en donde cuando Y es O, n es 0; uno y solo uno de los enlaces punteados a Z y Z constituye un enlace simple, en donde el otro se encuentra ausente, y Z es C cuando el enlace punteado a Z es un enlace simple, y Z es N o CR¹⁶; o Z es CR¹⁶ o N cuando el enlace punteado a Z es un enlace simple, y Z es C; en donde R¹⁶ es C₁₋₄ alquilo, C₆₋₁₀ arilo, heteroarilo monocíclico o bicíclico, que comprende anillos de 5 y/o 6 miembros, (aril)C₁₋₆ alquilo de cadena lineal o ramificada, (heteroaril)C₁₋₆ alquilo de cadena lineal o ramificada, (heterociclil)C₁₋₆ alquilo de cadena lineal o ramificada, (C₁₋₆ alquilo de cadena lineal o ramificada)arilo, (C₁₋₆ alquilo de cadena lineal o ramificada)heteroarilo o (C₁₋₆ alquilo de cadena lineal o ramificada)heterociclilo, en donde tal alquilo también se sustituye con uno o más sustituyentes seleccionados del grupo que consiste en halo, hidroxi, metoxi, amino, CF₃ y C₃₋₆ cicloalquilo; X y los enlaces punteados a este pueden estar presentes o ausentes, en donde (a) si X está presente, Y es N, y X es O ó --(CRᵉRᶠ)ₛ--, en donde Rᵉ y Rᶠ son independientemente hidrógeno, deuterio, halo, hidroxi, C₁₋₄ alcoxi, amino, CF₃, C₁₋₆ alquilo de cadena lineal o ramificada, C₃₋₆ cicloalquilo, C₆₋₁₀ arilo, heteroarilo monocíclico o bicíclico, que comprende anillos de 5 y/o 6 miembros, (aril)C₁₋₆ alquilo de cadena lineal o ramificada, (C₁₋₆ alquilo de cadena lineal o ramificada)heteroarilo, (heteroaril)C₁₋₆ alquilo de cadena lineal o ramificada, o (heterociclil)C₁₋₆ alquilo de cadena lineal o ramificada, y tales enlaces punteados están presentes y son enlaces simples, en donde cuando n es 0, y X es O, tal O se une a H, y tal enlace punteado entre X y --(CH₂)ₙ-- está ausente, y cuando X es --(CRᵉRᶠ)ₛ--, y X se une directamente a Y; y (b) si X está ausente, tales enlaces punteados están ausentes, y n es 0, en donde cuando Y es N, (i) tal átomo de N se sustituye con H, (ii) Z es C, Z es C o N, el enlace punteado a Z es un enlace simple, el enlace punteado a Z está ausente, o (iii) Z es C o N, Z es C, el enlace punteado a Z es un enlace simple, el enlace punteado a Z está ausente, en donde tal Y es un átomo de N y puede formar, junto con R² y los átomos intervinientes entre ellos, un anillo de 6 miembros opcionalmente sustituido con C₁₋₆ alquilo de cadena lineal o ramificada o C₃₋₆ cicloalquilo; y n, p, q, r y s son independientemente 0, 1 ó 2.
ARP140104517A 2013-12-05 2014-12-04 Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil y pirrolo[2,3-d]piridinil acrilamidas AR099363A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361912074P 2013-12-05 2013-12-05

Publications (1)

Publication Number Publication Date
AR099363A1 true AR099363A1 (es) 2016-07-20

Family

ID=52144776

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140104517A AR099363A1 (es) 2013-12-05 2014-12-04 Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil y pirrolo[2,3-d]piridinil acrilamidas

Country Status (47)

Country Link
US (4) US9617258B2 (es)
EP (2) EP3077395B1 (es)
JP (2) JP6192839B2 (es)
KR (1) KR101930603B1 (es)
CN (2) CN107417684A (es)
AP (1) AP2016009269A0 (es)
AR (1) AR099363A1 (es)
AU (1) AU2014358792C1 (es)
BR (1) BR112016012262B1 (es)
CA (1) CA2932425C (es)
CL (1) CL2016001216A1 (es)
CR (1) CR20160250A (es)
CU (1) CU24396B1 (es)
CY (3) CY1119778T1 (es)
DK (2) DK3318565T3 (es)
DO (1) DOP2016000124A (es)
EA (1) EA030472B1 (es)
ES (2) ES2654051T3 (es)
FI (1) FIC20230035I1 (es)
FR (1) FR23C1042I2 (es)
GE (1) GEP20186840B (es)
GT (1) GT201600098A (es)
HR (2) HRP20171846T1 (es)
HU (3) HUE054560T2 (es)
IL (1) IL246038B (es)
LT (3) LT3077395T (es)
MA (1) MA39092B1 (es)
MD (1) MD4649C1 (es)
ME (1) ME02883B (es)
MX (1) MX368464B (es)
MY (1) MY187446A (es)
NI (1) NI201600075A (es)
NL (1) NL301245I2 (es)
NO (2) NO3134430T3 (es)
NZ (1) NZ720092A (es)
PE (1) PE20161246A1 (es)
PH (1) PH12016500938B1 (es)
PL (2) PL3318565T3 (es)
PT (2) PT3318565T (es)
RS (2) RS61897B9 (es)
SI (2) SI3318565T1 (es)
SV (1) SV2016005209A (es)
TN (1) TN2016000227A1 (es)
TW (1) TWI548636B (es)
UA (1) UA117040C2 (es)
UY (1) UY35861A (es)
WO (1) WO2015083028A1 (es)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015039612A1 (zh) 2013-09-18 2015-03-26 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
ES2654051T3 (es) * 2013-12-05 2018-02-12 Pfizer Inc. Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo y pirrolo[2,3-d]piridinil acrilamidas
CN105777756B (zh) * 2014-07-02 2019-03-01 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
JP6563017B2 (ja) 2014-08-28 2019-08-21 エースニューロン・ソシエテ・アノニム グリコシダーゼ阻害剤
CN105712998B (zh) * 2014-12-05 2019-12-13 上海润诺生物科技有限公司 氮杂吲哚类衍生物、其制备方法及其在医药上的应用
EP3247353A4 (en) * 2015-01-23 2018-07-04 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
CN105837574B (zh) * 2015-02-02 2018-03-02 四川大学 N‑(3‑哌啶基)‑芳香胺衍生物及其制备方法和用途
WO2016178110A1 (en) * 2015-05-01 2016-11-10 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, pyrrolo[2,3-b]pyridinyl acrylamides and epoxides thereof
UA118822C2 (uk) * 2015-05-29 2019-03-11 Вуксі Фортуне Фармасьютікал Ко., Лтд Інгібітор янус-кінази
CN106432246B (zh) * 2015-08-05 2020-07-07 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
KR101771219B1 (ko) * 2015-08-21 2017-09-05 양지화학 주식회사 야누스 키나제 1 선택적 억제제 및 그 의약 용도
TWI710560B (zh) 2015-11-03 2020-11-21 美商施萬生物製藥研發Ｉｐ有限責任公司 用於治療呼吸疾病之jak激酶抑制劑化合物
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
MX2018010191A (es) 2016-02-25 2019-05-20 Asceneuron S A Inhibidores de glucosidasa.
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
MA43677A (fr) 2016-02-25 2018-11-28 Asceneuron Sa Inhibiteurs de glycosidases
EP3419976B1 (en) 2016-02-25 2021-04-07 Asceneuron SA Acid addition salts of piperazine derivatives
CN113135920A (zh) * 2016-06-30 2021-07-20 株式会社大熊制药 吡唑并嘧啶衍生物作为激酶抑制剂
JP2019530650A (ja) 2016-08-24 2019-10-24 アークル インコーポレイテッド アミノ−ピロロピリミジノン化合物およびその使用方法
CA3033456C (en) * 2016-11-23 2021-03-09 Wuxi Fortune Pharmaceutical Co., Ltd Crystal forms and salt forms of 7h-pyrrolo[2,3-d]pyrimidine compounds and preparation method thereof
CA3040981A1 (en) * 2016-11-23 2018-05-31 Bing Liu Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative
RU2764980C2 (ru) 2017-01-20 2022-01-24 Лео Фарма А/С Бициклические амины в качестве новых ингибиторов jak-киназы
CN110325535A (zh) 2017-02-27 2019-10-11 詹森药业有限公司 经哌啶、吗啉或哌嗪取代的作为oga抑制剂的[1,2,4]-三唑[1,5-a]-嘧啶基衍生物
JP7134990B2 (ja) 2017-03-09 2022-09-12 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー 縮合イミダゾ－ピペリジンｊａｋ阻害剤
CN108794480A (zh) * 2017-04-28 2018-11-13 天津药物研究院有限公司 吡咯并嘧啶类化合物、其制备方法和用途
WO2018204236A1 (en) 2017-05-01 2018-11-08 Theravance Biopharma R&D Ip, Llc Crystalline forms of a jak inhibitor compound
MX388748B (es) 2017-05-01 2025-03-20 Theravance Biopharma R&D Ip Llc Métodos de tratamiento mediante el uso de un compuesto inhibidor de jak.
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
MY200629A (en) 2017-08-01 2024-01-06 Theravance Biopharma R&D Ip Llc Pyrazolo and triazolo bicyclic compounds as jak kinase inhibitors
US11213525B2 (en) 2017-08-24 2022-01-04 Asceneuron Sa Linear glycosidase inhibitors
MX2020004946A (es) 2017-11-03 2020-09-25 Aclaris Therapeutics Inc Inhibidores jak de pirrolopiridina sustituidos y metodos para producir y utilizar los mismos.
KR20250036962A (ko) * 2017-11-07 2025-03-14 더 리젠츠 오브 더 유니버시티 오브 미시건 공유 에피토프-칼레티쿨린 상호 작용의 소분자 억제제 및 사용 방법
CN107857778B (zh) * 2017-11-21 2020-03-24 江苏乐斯化学有限公司 含膦酰基的α-氨基腈的制备方法
KR102577241B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체
KR102577242B1 (ko) * 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체
CN111527091B (zh) * 2017-12-28 2023-03-28 株式会社大熊制药 作为激酶抑制剂的氧基-氟哌啶衍生物
WO2019182924A1 (en) * 2018-03-21 2019-09-26 Xibin Liao Jak inhibitors
CN108358797A (zh) * 2018-04-20 2018-08-03 南京农业大学 一种烷基甘氨酸的合成方法
CN108640923A (zh) * 2018-07-09 2018-10-12 湖南天地恒制药有限公司 一种托法替布关键中间体的制备方法
AU2019316858B2 (en) * 2018-08-06 2024-03-28 Moexa Pharmaceuticals Limited Smad3 inhibitors
US11021482B2 (en) 2018-08-10 2021-06-01 Adaris Therapeutics, Inc. Pyrrolopyrimidine ITK inhibitors
WO2020039028A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Tetrahydro-benzoazepine glycosidase inhibitors
US11731972B2 (en) 2018-08-22 2023-08-22 Asceneuron Sa Spiro compounds as glycosidase inhibitors
WO2020039027A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Pyrrolidine glycosidase inhibitors
BR112021003022A2 (pt) 2018-08-22 2021-05-11 Asceneuron Sa sais de adição de ácido de ácido succínico ou ácido fumárico, de ácido monossuccínico, de ácido monofumárico e de adição de ácido succínico ou sal de adição de ácido fumárico, métodos para preparar um sal de adição de ácido do ácido succínico ou ácido fumárico, para tratar uma tauopatia e para inibir uma glicosidase, e, forma de dosagem oral sólida
AU2019335200A1 (en) 2018-09-04 2021-03-11 Theravance Biopharma R&D Ip, Llc 5 to 7 membered heterocyclic amides as JAK inhibitors
KR102826491B1 (ko) 2018-09-04 2025-06-27 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 억제제로서 디메틸 아미노 아제티딘 아마이드
AR116116A1 (es) 2018-09-04 2021-03-31 Theravance Biopharma R&D Ip Llc Proceso para elaborar inhibidores de jak e intermediarios de los mismos
WO2020067887A1 (en) 2018-09-24 2020-04-02 Erasmus University Medical Center Rotterdam Specific inhibition of janus kinase 3 (jak3) for modulating anti-tumor immune responses
JP6944496B2 (ja) * 2018-10-22 2021-10-06 ファイザー・インク ピロロ［２，３−ｄ］ピリミジントシル酸塩、その結晶形態、ならびにその製造方法および中間体
AU2019373059A1 (en) 2018-10-29 2021-05-06 Theravance Biopharma R&D Ip, Llc 2-azabicyclo hexane compound as JAK inhibitor
CN113498352A (zh) 2019-01-23 2021-10-12 施万生物制药研发Ip有限责任公司 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪
US12398141B2 (en) 2019-03-14 2025-08-26 Shanghai Synergy Pharmaceutical Sciences Co., Ltd JAK kinase inhibitor, preparation method for same, and applications thereof in field of medicine
EP3946606B1 (en) 2019-03-27 2025-01-01 Insilico Medicine IP Limited Bicyclic jak inhibitors and uses thereof
KR20220004726A (ko) * 2019-05-02 2022-01-11 어클라리스 쎄라퓨틱스, 인코포레이티드 Jak 억제제로서의 치환된 피롤로피리딘
EP3969458A4 (en) 2019-05-13 2023-05-17 Borah, Inc. CHEMICAL COMPOUNDS
BR112021022682A2 (pt) 2019-05-14 2022-02-22 Provention Bio Inc Métodos e composições para prevenir diabetes do tipo 1
CN110183455B (zh) * 2019-06-18 2021-04-20 中国医科大学 氮杂双环[3.2.1]辛-3-酮类化合物及其制备方法与其用途
CN112430235B (zh) * 2019-08-26 2024-04-05 东莞市东阳光仿制药研发有限公司 一种pf-06651600中间体的制备方法
WO2021062163A1 (en) 2019-09-27 2021-04-01 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
KR102228668B1 (ko) 2019-10-08 2021-03-17 (주)부흥산업사 메틸피퍼리딘 아미노피롤로 피리미딘의 제조방법
EP4057989A1 (en) 2019-11-14 2022-09-21 Pfizer Inc. 1-(((2s,3s,4s)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide combinations and oral dosage forms
CN112824381B (zh) * 2019-11-21 2024-04-26 广东东阳光药业股份有限公司 一种哌啶胺的制备方法
CN115023221B (zh) * 2019-12-31 2024-05-28 辉瑞英国研发有限公司 1-((2s,5r)-5-((7h-吡咯并[2,3-d]嘧啶-4-基)氨基)-2-甲基哌啶-1-基)丙-2-烯-1-酮的稳定立即释放片剂和胶囊制剂
CN113121539A (zh) * 2019-12-31 2021-07-16 江苏艾立康医药科技有限公司 一种pf06651600的制备方法
CN113121413B (zh) * 2019-12-31 2024-04-09 江苏艾立康医药科技有限公司 一种jak3酶抑制剂关键中间体的制备方法
CN111138361B (zh) * 2020-01-03 2022-05-06 中国医科大学 取代苯氧基-2-氮杂双环[3.2.1]辛烷类化合物及其制备方法和应用
CN115244055B (zh) * 2020-01-21 2024-09-03 江苏先声药业有限公司 嘧啶并五元环类衍生物及其应用
US20230126204A1 (en) * 2020-02-03 2023-04-27 Boehringer Ingelheim International Gmbh [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS
TW202144343A (zh) 2020-03-02 2021-12-01 美商施萬生物製藥研發 Ip有限責任公司 Jak抑制劑化合物之結晶水合物
EP4125900A1 (en) 2020-04-04 2023-02-08 Pfizer Inc. Methods of treating coronavirus disease 2019
WO2021231798A1 (en) 2020-05-13 2021-11-18 Disc Medicine, Inc. Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
CA3182445A1 (en) 2020-06-11 2021-12-16 Francisco Leon Methods and compositions for preventing type 1 diabetes
CN114835715B (zh) * 2020-06-15 2024-04-05 江苏艾立康医药科技有限公司 Pf-06651600马来酸盐及其制备方法
CN111620880B (zh) * 2020-06-15 2022-06-10 江苏艾立康医药科技有限公司 Pf-06651600 dl-酒石酸盐，晶型及其制备方法
WO2022002210A1 (zh) * 2020-07-02 2022-01-06 南京明德新药研发有限公司 嘧啶并吡咯基类氘代化合物
WO2022012587A1 (zh) * 2020-07-14 2022-01-20 苏州晶云药物科技股份有限公司 丙烯酮类化合物的丙二酸盐晶型及其制备方法
CN111995623A (zh) * 2020-08-18 2020-11-27 上海毕得医药科技有限公司 一种7-溴-4-氯-1-甲基-1H-咪唑并[4,5-c]吡啶的合成方法
KR102473645B1 (ko) 2020-08-28 2022-12-05 (주)부흥산업사 (2S,5R)-벤질 5-(t-부톡시카르보닐아미노)-2-메틸피페리딘-1-카르복실레이트의 제조방법
CN113061137B (zh) * 2021-04-02 2022-08-02 广西医科大学 含氮杂环衍生物或其药学上可接受的盐和用途
JP2024524214A (ja) 2021-06-25 2024-07-05 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー Ｊａｋ阻害剤としてのイミダゾロインダゾール化合物
CN113429427A (zh) * 2021-07-05 2021-09-24 湖南南新制药股份有限公司 杂环化合物及其制备方法和药物用途
CN118084939A (zh) * 2021-08-25 2024-05-28 杭州禹泓医药科技有限公司 一种五元杂环骈合杂环烷基类化合物、含其的药物组合物及应用
WO2023029943A1 (zh) * 2021-09-03 2023-03-09 星药科技(北京)有限公司 一种芳杂环化合物及其制备方法和用途
WO2023151069A1 (zh) * 2022-02-14 2023-08-17 湖南南新制药股份有限公司 吡咯并[2,3-d]六元杂芳环衍生物、其制备方法和药物用途
EP4605076A1 (en) 2022-10-18 2025-08-27 Pfizer Inc. Patatin-like phospholipase domain-containing protein 3 (pnpla3) modifiers
EP4604955A1 (en) 2022-10-18 2025-08-27 Pfizer Inc. Use of patatin-like phospholipase domain-containing protein 3 compounds
EP4648776A1 (en) 2023-01-11 2025-11-19 Pfizer Inc. Compositions and methods for the treatment and/or prevention of type 1 diabetes
CN116120347B (zh) * 2023-01-18 2024-08-23 杭州禹泓医药科技有限公司 芳杂环类化合物的晶型、其组合物、制备方法及其应用
CN116496280B (zh) * 2023-06-25 2023-09-08 北京科翔中升医药科技有限公司 氘代丙烯酰胺类jak3抑制剂药物及用途
WO2025146702A1 (en) * 2024-01-03 2025-07-10 Msn Laboratories Private Limited, R&D Center Solid state forms of 1-{(2s,5r)-2-methyl-5-[(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino] piperidine-1-yl}prop-2-en-1-one 4-methylbenzene-1-sulfonic acid
WO2025181247A1 (en) * 2024-02-28 2025-09-04 Almirall, S.A. Heterobicyclic derivatives as itk inhibitors
WO2025257773A1 (en) 2024-06-11 2025-12-18 Assia Chemical Industries Ltd. Processes for the preparation of ritlecitinib and intermediates thereof

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
HRP20000885B1 (hr) 1998-06-19 2007-03-31 Pfizer Products Inc. PIROLO[2,3-d]PIRIMIDINSKI SPOJEVI
JP4078074B2 (ja) 1999-12-10 2008-04-23 ファイザー・プロダクツ・インク ピロロ［２，３−ｄ］ピリミジン化合物
CA2412560C (en) * 2000-06-26 2008-12-30 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
JP2006508976A (ja) 2002-11-21 2006-03-16 ファイザー・プロダクツ・インク ３−アミノ−ピペラジン誘導体及び製造法
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
RU2384583C2 (ru) 2005-07-29 2010-03-20 Пфайзер Продактс Инк. ПИРРОЛО[2,3-d]ПИРИМИДИНОВЫЕ ПРОИЗВОДНЫЕ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ И СИНТЕЗ
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
EP2343298B9 (en) 2005-12-13 2020-05-06 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
ES2585902T3 (es) 2006-09-22 2016-10-10 Pharmacyclics Llc Inhibidores de tirosina cinasa de Bruton
JO3041B1 (ar) 2008-07-25 2016-09-05 Galapagos Nv مركبات جديدة مفيدة لمعالجة الأمراض التنكسية والالتهابية
ATE542813T1 (de) 2008-08-06 2012-02-15 Pfizer 6-substituierte 2- heterocyclylaminopyrazinverbindungen als chk-1- inhibitoren
MY156789A (en) 2008-09-05 2016-03-31 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
EP2962566A1 (en) 2008-10-31 2016-01-06 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
MX2011005597A (es) 2008-12-05 2011-06-16 Hoffmann La Roche Pirrolopirazinil-ureas como inhibidores de cinasas.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
EP2440559B1 (en) * 2009-05-05 2018-01-10 Dana-Farber Cancer Institute, Inc. Egfr inhibitors and methods of treating disorders
JO3030B1 (ar) 2009-06-26 2016-09-05 Galapagos Nv مركب جديد مفيد لمعالجة الامراض التنكسية والالتهابات
WO2011002904A2 (en) 2009-06-30 2011-01-06 Edwards Lifesciences Corporation Systems and methods for monitoring and displaying a patient's status
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
CA2767079A1 (en) 2009-07-08 2011-01-13 Leo Pharma A/S Heterocyclic compounds as jak receptor and protein tyrosine kinase inhibitors
FR2948946B1 (fr) 2009-08-07 2015-08-07 Metaleach Ltd Procede de lixiviation de cobalt a partir de minerais de cobalt oxydes
US8785440B2 (en) 2009-09-04 2014-07-22 Biogen Idec Ma, Inc. Bruton's tyrosine kinase inhibitors
WO2011072174A1 (en) 2009-12-09 2011-06-16 Agios Pharmaceuticals, Inc. Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
RU2012152352A (ru) * 2010-05-20 2014-06-27 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРАЗИН-7-КАРБОКСАМИДА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ JAK И SYK
US9586961B2 (en) 2010-07-09 2017-03-07 Leo Pharma A/S Homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof
WO2012054364A2 (en) * 2010-10-22 2012-04-26 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
EP2788000B1 (en) * 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
EP2796460B1 (en) 2011-12-21 2018-07-04 Jiangsu Hengrui Medicine Co. Ltd. Pyrrole six-membered heteroaryl ring derivative, preparation method therefor, and medicinal uses thereof
ES2889757T3 (es) * 2012-09-06 2022-01-13 Plexxikon Inc Compuestos y procedimientos para la modulación de quinasas e indicaciones para estos
CA2891009A1 (en) 2012-11-16 2014-05-22 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
AU2013348116A1 (en) 2012-11-20 2015-06-11 Principia Biopharma Inc. Azaindole derivatives as JAK3 inhibitors
CN103896946B (zh) * 2012-12-28 2018-04-03 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物
ES2654051T3 (es) * 2013-12-05 2018-02-12 Pfizer Inc. Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo y pirrolo[2,3-d]piridinil acrilamidas
US10144737B2 (en) * 2014-05-19 2018-12-04 Jiangsu Hengrui Medicine Co., Ltd. Substituted ethynyl heterobicyclic compounds as tyrosine kinase inhibitors

Also Published As

Publication number Publication date
RS61897B1 (sr) 2021-06-30
US9617258B2 (en) 2017-04-11
LTC3077395I2 (es) 2025-09-10
US11111242B2 (en) 2021-09-07
HRP20171846T1 (hr) 2018-01-12
EP3077395B1 (en) 2017-11-15
CY2024002I1 (el) 2024-09-20
NO2024001I1 (no) 2024-01-09
CA2932425A1 (en) 2015-06-11
CY1124793T1 (el) 2022-11-25
PT3318565T (pt) 2021-05-28
JP6192839B2 (ja) 2017-09-06
LT3077395T (lt) 2018-02-12
WO2015083028A1 (en) 2015-06-11
PH12016500938A1 (en) 2016-06-27
BR112016012262B1 (pt) 2021-04-13
NL301245I2 (nl) 2023-11-20
CR20160250A (es) 2016-09-19
EA201600373A1 (ru) 2016-10-31
CY1119778T1 (el) 2018-06-27
CN106061973A (zh) 2016-10-26
FR23C1042I1 (fr) 2023-12-29
PL3318565T3 (pl) 2021-10-04
EP3318565B1 (en) 2021-04-14
RS61897B9 (sr) 2021-09-30
NZ720092A (en) 2019-05-31
FIC20230035I1 (fi) 2023-11-22
IL246038A0 (en) 2016-08-02
RS56728B1 (sr) 2018-03-30
PH12016500938B1 (en) 2016-06-27
US20170247372A1 (en) 2017-08-31
EP3318565A1 (en) 2018-05-09
HUE054560T2 (hu) 2021-09-28
KR101930603B1 (ko) 2018-12-18
MY187446A (en) 2021-09-22
NI201600075A (es) 2016-08-09
AU2014358792C1 (en) 2021-08-26
HRP20210770T1 (hr) 2021-06-25
CL2016001216A1 (es) 2017-01-20
NO3134430T3 (es) 2018-08-18
DOP2016000124A (es) 2016-10-31
HUE035264T2 (hu) 2018-05-02
MD4649B1 (ro) 2019-09-30
US12077533B2 (en) 2024-09-03
ME02883B (me) 2018-04-20
KR20160092012A (ko) 2016-08-03
UY35861A (es) 2015-07-31
CA2932425E (en) 2015-06-11
LTPA2023537I1 (es) 2024-01-10
CU24396B1 (es) 2019-04-04
UA117040C2 (uk) 2018-06-11
PE20161246A1 (es) 2016-11-25
EP3077395A1 (en) 2016-10-12
CU20160077A7 (es) 2017-01-10
MA39092A1 (fr) 2018-06-29
SV2016005209A (es) 2018-04-11
MD20160058A2 (ro) 2016-11-30
TN2016000227A1 (fr) 2017-10-06
US20150158864A1 (en) 2015-06-11
ES2871524T3 (es) 2021-10-29
BR112016012262A2 (pt) 2020-06-30
CN107417684A (zh) 2017-12-01
SI3077395T1 (en) 2018-03-30
MA39092B1 (fr) 2018-09-28
PL3077395T3 (pl) 2018-04-30
JP2016539137A (ja) 2016-12-15
AU2014358792A1 (en) 2016-06-02
CA2932425C (en) 2018-07-17
MX2016007156A (es) 2016-07-21
PT3077395T (pt) 2018-01-03
JP2018008996A (ja) 2018-01-18
CY2024002I2 (el) 2024-09-20
EA030472B1 (ru) 2018-08-31
LT3318565T (lt) 2021-06-25
TWI548636B (zh) 2016-09-11
IL246038B (en) 2020-10-29
HUS2300040I1 (hu) 2023-12-28
GT201600098A (es) 2019-10-17
CN106061973B (zh) 2019-07-09
ES2654051T3 (es) 2018-02-12
TW201524977A (zh) 2015-07-01
US20250134869A1 (en) 2025-05-01
SI3318565T1 (sl) 2021-07-30
GEP20186840B (en) 2018-04-10
MX368464B (es) 2019-10-02
DK3077395T3 (en) 2018-01-02
AU2014358792B2 (en) 2017-06-08
MD4649C1 (ro) 2020-04-30
AP2016009269A0 (en) 2016-06-30
FR23C1042I2 (fr) 2024-11-15
DK3318565T3 (da) 2021-05-25
US20230009153A1 (en) 2023-01-12

Similar Documents

Publication Publication Date Title
AR099363A1 (es) Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil y pirrolo[2,3-d]piridinil acrilamidas
AR104461A1 (es) Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil, pirrolo[2,3-b]piridinil acrilamidas y epóxidos de estas
AR123089A2 (es) Compuesto de piridinona
AR088760A1 (es) Derivados de pirrolopirimidina y purina
AR092742A1 (es) Piridinonas antifibroticas
AR096979A1 (es) Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen
AR100438A1 (es) Pirazolopiridinas y pirazolopirimidinas
AR094857A1 (es) Derivados de pirrolo[2,3-d]pirimidina
AR096684A1 (es) Compuestos para tratar atrofia muscular espinal
AR100418A1 (es) Compuestos y composiciones para inducir condrogénesis
PE20171240A1 (es) Derivados de 4h-pirrol[3,2-c]piridin-4-ona
AR091424A1 (es) Compuestos triciclicos sustituidos como inhibidores de receptores del factor de crecimiento del fibroplasto (fgfr)
AR099228A1 (es) Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos
EA201390163A1 (ru) Гетеробициклические производные в качетстве ингибиторов hcv
AR098337A1 (es) Triazolopirazina
AR091781A1 (es) Antagonistas del receptor de 5-ht3
AR090230A1 (es) Derivados macrociclicos para el tratamiento de enfermedades
AR095192A1 (es) Quinolina y quinazolinamidas como modulares de canales de sodio
AR097571A1 (es) Compuestos espirocíclicos como inhibidores de la triptofano hidroxilasa
AR105392A1 (es) Inhibidores del receptor del factor estimulador de colonias 1 (csf-1r)
MX343274B (es) Inhibidores de la replicacion del vih.
AR084553A1 (es) DERIVADOS IMIDAZOLICOS HETEROCICLICOS INHIBIDORES DE b-SECRETASA, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USO DE LOS MISMOS PARA TRATAR ENFERMEDADES NEURODEGENERATIVAS, EN PARTICULAR ALZHEIMER
AR098492A1 (es) Derivados de purina
EA201491376A1 (ru) Производные 1h-пирроло[2,3-b]пиридина и их применение в качестве ингибиторов киназы
AR103232A1 (es) ANTAGONISTAS DE TGFbR

Legal Events

Date Code Title Description
FG Grant, registration