DK2791138T3 - Substituted pyrazole [1,5-a] pyridines as tropomyosin receptor kinase (TRK) inhibitors. - Google Patents

Substituted pyrazole [1,5-a] pyridines as tropomyosin receptor kinase (TRK) inhibitors. Download PDF

Info

Publication number
DK2791138T3
DK2791138T3 DK12832784.8T DK12832784T DK2791138T3 DK 2791138 T3 DK2791138 T3 DK 2791138T3 DK 12832784 T DK12832784 T DK 12832784T DK 2791138 T3 DK2791138 T3 DK 2791138T3
Authority
DK
Denmark
Prior art keywords
carboxamide
pyridine
pyrrolidin
pyrazole
difluorophenyl
Prior art date
Application number
DK12832784.8T
Other languages
Danish (da)
English (en)
Inventor
Ashok Tehim
Pradip Kumar Sasmal
Shahadat Ahmed
Vidyadhar Paradkar
Prasanna M Dattatreya
Nanjegowda Jagadeesh Mavinahalli
Original Assignee
Dr Reddys Laboratories Ltd
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
Application filed by Dr Reddys Laboratories Ltd filed Critical Dr Reddys Laboratories Ltd
Application granted granted Critical
Publication of DK2791138T3 publication Critical patent/DK2791138T3/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
DK12832784.8T 2011-12-12 2012-12-12 Substituted pyrazole [1,5-a] pyridines as tropomyosin receptor kinase (TRK) inhibitors. DK2791138T3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN4329CH2011 2011-12-12
PCT/IB2012/003012 WO2013088256A1 (en) 2011-12-12 2012-12-12 Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (trk) inhibitors

Publications (1)

Publication Number Publication Date
DK2791138T3 true DK2791138T3 (en) 2018-09-17

Family

ID=47902312

Family Applications (1)

Application Number Title Priority Date Filing Date
DK12832784.8T DK2791138T3 (en) 2011-12-12 2012-12-12 Substituted pyrazole [1,5-a] pyridines as tropomyosin receptor kinase (TRK) inhibitors.

Country Status (16)

Country Link
US (7) US9045478B2 (https=)
EP (2) EP2791139B1 (https=)
JP (1) JP5990595B2 (https=)
KR (2) KR20140105508A (https=)
CN (1) CN104114553B (https=)
AU (1) AU2012351748B2 (https=)
BR (1) BR112014014276A2 (https=)
CA (1) CA2858958C (https=)
CL (1) CL2014001529A1 (https=)
CO (1) CO7071124A2 (https=)
DK (1) DK2791138T3 (https=)
EA (1) EA025352B1 (https=)
ES (1) ES2686501T3 (https=)
IL (1) IL233067B (https=)
MX (1) MX356401B (https=)
WO (2) WO2013088256A1 (https=)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010033941A1 (en) 2008-09-22 2010-03-25 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
MY169791A (en) 2008-10-22 2019-05-15 Array Biopharma Inc Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
ME03376B (me) 2010-05-20 2020-01-20 Array Biopharma Inc Makrociklička jedinjenja kао inhibiтori trk kinaze
AU2012351748B2 (en) * 2011-12-12 2016-04-14 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors
TWI731317B (zh) 2013-12-10 2021-06-21 美商健臻公司 原肌球蛋白相關之激酶(trk)抑制劑
EP3083602A1 (en) 2013-12-20 2016-10-26 Pfizer Limited N-acylpiperidine ether tropomyosin-related kinase inhibitors
CN103819343B (zh) * 2014-02-17 2016-03-23 青岛农业大学 化合物2-烯丙基-4-氟-6-硝基苯酚的制备方法和农用生物活性
WO2015143652A1 (en) * 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015159175A1 (en) 2014-04-15 2015-10-22 Pfizer Inc. Tropomyosin-related kinase inhibitors containing both a 1h-pyrazole and a pyrimidine moiety
WO2015170218A1 (en) 2014-05-07 2015-11-12 Pfizer Inc. Tropomyosin-related kinase inhibitors
CN106661022B (zh) * 2014-05-08 2018-05-04 拜耳作物科学股份公司 作为杀线虫剂的吡唑并吡啶磺酰胺
WO2015200341A1 (en) 2014-06-23 2015-12-30 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
WO2016009296A1 (en) 2014-07-16 2016-01-21 Pfizer Inc. N-acylpiperidine ether tropomyosin-related kinase inhibitors
WO2016020784A1 (en) 2014-08-05 2016-02-11 Pfizer Inc. N-acylpyrrolidine ether tropomyosin-related kinase inhibitors
CN113354649B (zh) 2014-11-16 2024-12-10 阵列生物制药公司 一种新的晶型
EA201791336A1 (ru) 2014-12-18 2017-10-31 Джензим Корпорейшн Фармацевтические составы на основе ингибиторов тропомиозин-родственных киназ (trk)
CN104672121B (zh) * 2015-02-16 2017-10-24 上海华默西医药科技有限公司 2r‑(2,5‑二氟苯基)吡咯烷盐酸盐的制备方法
KR102081272B1 (ko) * 2015-05-29 2020-02-25 우시 포춘 파마슈티컬 컴퍼니 리미티드 Janus 키나아제 억제제
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
FI3439662T3 (fi) 2016-04-04 2024-09-04 Loxo Oncology Inc (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
EP3458456B1 (en) 2016-05-18 2020-11-25 Loxo Oncology Inc. Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
ES2896943T3 (es) * 2016-10-28 2022-02-28 Chia Tai Tianqing Pharmaceutical Group Co Ltd Compuesto de amino pirazolopirimidina usado como inhibidor de receptores con actividad tirosina quinasa de factores neurotróficos
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
AU2018266911C1 (en) * 2017-05-12 2022-10-20 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218042A1 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10246439B2 (en) 2017-05-25 2019-04-02 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2018218051A1 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10800760B2 (en) 2017-05-31 2020-10-13 Nantbio, Inc. Trk inhibition
US10738033B2 (en) 2017-05-31 2020-08-11 Nantbio, Inc. Trk inhibition
CN107286070B (zh) * 2017-07-19 2019-07-16 浙江师范大学 (r)-2-(2,5-二氟苯基)吡咯烷的合成方法及中间体
US10597382B2 (en) 2017-08-28 2020-03-24 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2019084285A1 (en) 2017-10-26 2019-05-02 Qian Zhao FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR
CN109867668B (zh) * 2017-12-02 2021-03-26 广东东阳光药业有限公司 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途
CN109867672B (zh) * 2017-12-02 2020-07-07 广东东阳光药业有限公司 吡唑[1,5-a]吡啶衍生物的盐及其用途
CN109867671B (zh) * 2017-12-02 2020-07-07 广东东阳光药业有限公司 一种吡唑[1,5-a]吡啶化合物的晶型及其药物组合物和用途
US11179376B2 (en) * 2017-12-20 2021-11-23 Sunshine Lake Pharma Co., Ltd. Salts of pyrazolo[1,5-a]pyridine derivative and use thereof
CN108218754B (zh) * 2018-01-23 2021-05-07 广东赛烽医药科技有限公司 一种2-(2,5-二氟苯基)吡咯烷的制备方法
MX2020008273A (es) 2018-02-06 2020-11-24 Univ Miami Inhibidores de la cinasa del complejo de activacion transcripcional notch ("nack") y metodos para el uso de los mismos.
WO2019191659A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
WO2019213239A1 (en) 2018-05-02 2019-11-07 Enanta Pharmaceuticals Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
ES3004523T3 (en) 2018-05-02 2025-03-12 Enanta Pharm Inc Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
GB201811825D0 (en) 2018-07-19 2018-09-05 Benevolentai Bio Ltd Organic compounds
CN108794370A (zh) * 2018-07-31 2018-11-13 上海弈柯莱生物医药科技有限公司 一种拉罗替尼中间体的制备方法
WO2020041417A1 (en) 2018-08-22 2020-02-27 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
GB201813791D0 (en) 2018-08-23 2018-10-10 Benevolental Bio Ltd Organic compounds
CN111171019A (zh) * 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
WO2020106707A1 (en) 2018-11-19 2020-05-28 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
CN109593802B (zh) * 2018-12-24 2021-10-01 上海健康医学院 一种(r)-2-(2,5-二氟苯基)吡咯烷或其盐的制备方法
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
US11466033B2 (en) 2019-03-25 2022-10-11 Enanta Pharmaceuticals, Inc. Substituted pyridines as apoptosis signal-regulating kinase 1 inhibitors
CN110015980A (zh) * 2019-05-14 2019-07-16 大连联化化学有限公司 一种合成叔丁基亚磺酰胺的方法
US12351590B2 (en) 2019-06-05 2025-07-08 Guangzhou Joyo Pharmatech Co., Ltd. Pyrrolopyrimidine compound and use thereof
CN110751853B (zh) * 2019-10-25 2021-05-18 百度在线网络技术(北京)有限公司 停车位数据的有效性识别方法和装置
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
CN114829345A (zh) * 2019-12-27 2022-07-29 日本烟草产业株式会社 酰基磺酰胺化合物及其医药用途
AU2021209418A1 (en) 2020-01-22 2022-07-21 Benevolentai Bio Limited Topical pharmaceutical compositions comprising imidazo[1,2-b]pyridazine compounds
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021148807A1 (en) 2020-01-22 2021-07-29 Benevolentai Bio Limited Pharmaceutical compositions and their uses
JP7495998B2 (ja) * 2020-05-15 2024-06-05 石薬集団中奇制薬技術(石家庄)有限公司 アザ縮合環状アミド化合物及びその用途
WO2022026565A1 (en) * 2020-07-29 2022-02-03 Ideaya Biosciences, Inc. Cyclized acetamido derivatives as dna polymerase theta inhibitors
CN112979646B (zh) * 2021-03-08 2022-01-14 北京富龙康泰生物技术有限公司 一种咪唑并吡啶类衍生物
WO2022234287A1 (en) 2021-05-06 2022-11-10 Benevolentai Bio Limited Imidazopyridazine derivatives useful as trk inhibitors
WO2023083362A1 (zh) * 2021-11-15 2023-05-19 石药集团中奇制药技术(石家庄)有限公司 一种治疗肿瘤的药物
WO2023083356A1 (zh) * 2021-11-15 2023-05-19 石药集团中奇制药技术(石家庄)有限公司 固体形式的氮杂稠环酰胺类化合物及其用途
CN115772170B (zh) * 2021-12-03 2025-05-16 徐诺药业(南京)有限公司 一种吡唑并[1,5-a]吡啶衍生物及其制备方法和应用
IL321144A (en) * 2022-11-30 2025-07-01 Blueprint Medicines Corp History of N-phenyl-pyrazolo[5,1-A]pyridine-3-carboxamide as wild-type C-KIT kinase inhibitors for the treatment of erectile dysfunction
WO2024123966A1 (en) * 2022-12-07 2024-06-13 Third Harmonic Bio, Inc. Compounds and compositions as c-kit kinase inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9809591A (pt) * 1997-05-03 2001-09-11 Smithkline Beecham Plc Derivados de tetraidoisoquinolina como moduladores de receptores de dopamina d3
JP2003231687A (ja) 2002-02-04 2003-08-19 Japan Tobacco Inc ピラゾリル縮合環化合物及びその医薬用途
AU2003240488A1 (en) * 2002-06-04 2003-12-19 Neogenesis Pharmaceuticals, Inc. Pyrazolo` 1,5a! pyrimidine compounds as antiviral agents
EP1527071A1 (en) 2002-07-25 2005-05-04 Pfizer Products Inc. Isothiazole derivatives useful as anticancer agents
US7141568B2 (en) 2003-07-09 2006-11-28 Pfizer Italia S.R.L. Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
CA2629743A1 (en) * 2005-12-08 2007-06-14 Novartis Ag Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
CA2692653A1 (en) 2007-07-11 2009-01-15 Auckland Uniservices Limited Pyrazolo[1,5-.alpha.]pyridines and their use in cancer therapy
KR101324804B1 (ko) 2008-05-13 2013-11-01 아이알엠 엘엘씨 키나제 억제제로서의 질소 함유 융합 헤테로사이클 및 그의 조성물
MY169791A (en) 2008-10-22 2019-05-15 Array Biopharma Inc Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors
MA34969B1 (fr) * 2011-02-25 2014-03-01 Irm Llc Composes et compositions en tant qu inibiteurs de trk
AU2012351748B2 (en) * 2011-12-12 2016-04-14 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors

Also Published As

Publication number Publication date
EA025352B1 (ru) 2016-12-30
KR20140105508A (ko) 2014-09-01
KR20170005894A (ko) 2017-01-16
MX356401B (es) 2018-05-21
US9670207B2 (en) 2017-06-06
US20140371217A1 (en) 2014-12-18
JP2015500275A (ja) 2015-01-05
US20180354951A1 (en) 2018-12-13
IL233067B (en) 2018-03-29
US10344031B2 (en) 2019-07-09
US20170267677A1 (en) 2017-09-21
AU2012351748A1 (en) 2014-07-17
CA2858958A1 (en) 2013-06-20
JP5990595B2 (ja) 2016-09-14
US9045479B2 (en) 2015-06-02
CN104114553B (zh) 2017-03-01
BR112014014276A2 (pt) 2017-06-13
EA201400701A1 (ru) 2014-11-28
AU2012351748B2 (en) 2016-04-14
US10047087B2 (en) 2018-08-14
US20150164869A1 (en) 2015-06-18
EP2791138B1 (en) 2018-06-06
CN104114553A (zh) 2014-10-22
US9402833B2 (en) 2016-08-02
EP2791138A1 (en) 2014-10-22
KR101849143B1 (ko) 2018-04-16
CO7071124A2 (es) 2014-09-30
ES2686501T3 (es) 2018-10-18
US20150005280A1 (en) 2015-01-01
US20160264572A1 (en) 2016-09-15
WO2013088257A1 (en) 2013-06-20
US20150258076A1 (en) 2015-09-17
WO2013088256A1 (en) 2013-06-20
CL2014001529A1 (es) 2015-06-26
EP2791139B1 (en) 2017-11-08
NZ626306A (en) 2015-05-29
US9289419B2 (en) 2016-03-22
US9045478B2 (en) 2015-06-02
MX2014006980A (es) 2015-04-08
IL233067A0 (en) 2014-07-31
EP2791139A1 (en) 2014-10-22
CA2858958C (en) 2016-10-04

Similar Documents

Publication Publication Date Title
DK2791138T3 (en) Substituted pyrazole [1,5-a] pyridines as tropomyosin receptor kinase (TRK) inhibitors.
CA2953177C (en) Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
AU2017208998B2 (en) Bruton's tyrosine kinase inhibitors
JP7346441B2 (ja) 置換ピリジン及びピリミジン並びにglun2b受容体調節物質としてのそれらの使用
EP3414234A1 (en) Bruton's tyrosine kinase inhibitors
KR102603203B1 (ko) 히스타민 h4-수용체 저해제로서 피리도피리미딘류
IL303320A (en) C-myc mrna translation modulators and uses thereof in the treatment of cancer
CA3008653C (en) Bruton's tyrosine kinase inhibitors
JP2025536295A (ja) ムスカリン性アセチルコリン受容体m1のポジティブアロステリックモジュレーター
NZ626306B2 (en) Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (trk) inhibitors
NZ711699B2 (en) P2x7 modulators
NZ711699A (en) P2x7 modulators