HRP20130986T1 - Aminopirazol triazolotiadiazol inhibitori c-met protein kinaze - Google Patents

Aminopirazol triazolotiadiazol inhibitori c-met protein kinaze Download PDF

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Publication number
HRP20130986T1
HRP20130986T1 HRP20130986AT HRP20130986T HRP20130986T1 HR P20130986 T1 HRP20130986 T1 HR P20130986T1 HR P20130986A T HRP20130986A T HR P20130986AT HR P20130986 T HRP20130986 T HR P20130986T HR P20130986 T1 HRP20130986 T1 HR P20130986T1
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HR
Croatia
Prior art keywords
hydrogen
compound according
compound
methyl
fluoro
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HRP20130986AT
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English (en)
Inventor
David Lauffer
Pan Li
Kira Mcginty
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Vertex Pharmaceuticals Incorporated
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42346870&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20130986(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HRP20130986T1 publication Critical patent/HRP20130986T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • A61K31/43Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • 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
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (17)

1. Spoj koji ima formulu: [image] ili njegova farmaceutski prihvatljiva sol, u kojem R1 je C1-3 alifatik; R2 je vodik, fluoro ili metil; R3 je vodik, fluoro ili metil; svaki R4 je, nezavisno, vodik ili fluoro; i R5 je vodik, kloro, ciklopropil ili C1-4 alifatik, izborno supstituiran sa 1-3 atoma fluora.
2. Spoj prema patentnom zahtjevu 1, naznačen time što je R2 jednak metil i R3 je vodik.
3. Spoj prema patentnom zahtjevu 2, naznačen time što je R1 jednak metil i R5 je vodik.
4. Spoj prema patentnom zahtjevu 1, naznačen time što je R2 jednak vodik i R3 je metil.
5. Spoj prema patentnom zahtjevu 4, naznačen time što je R1 jednak metil i R5 je vodik.
6. Spoj prema patentnom zahtjevu 1, naznačen time što je svaki od R2 i R3 jednak fluoro.
7. Spoj prema patentnom zahtjevu 6, naznačen time što je R1 jednak metil i R5 je vodik.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time što je R4 jednak vodik.
9. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time što je R4 jednak fluoro.
10. Spoj prema patentnom zahtjevu 1, naznačen time što ima slijedeću strukturu: [image] [image] [image]
11. Spoj prema patentnom zahtjevu 1, naznačen time što ima slijedeću strukturu: [image]
12. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 11, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač, adjuvant ili prenositelj.
13. Kompozicija prema patentnom zahtjevu 12, naznačena time što dodatno sadrži kemoterapeutsko ili anti-proliferativno sredstvo, anti-inflamatorno sredstvo, sredstvo za liječenje ateroskleroze ili sredstvo za liječenje plućne fibroze.
14. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11, ili farmaceutska kompozicija prema patentnom zahtjevu 12 ili 13 koja sadrži navedeni spoj, za uporabu u liječenju ili smanjenju težine proliferativnog poremećaja kod pacijenta.
15. Spoj ili kompozicija, za uporabu prema patentnom zahtjevu 14, pri čemu je navedeni poremećaj metastazirajući kancer.
16. Spoj ili kompozicija, za uporabu prema patentnom zahtjevu 14, pri čemu je navedeni poremećaj glioblastom; karcinom želudca; ili kancer izabran od kancera debelog crijeva, dojke, prostate, mozga, jetre, pankreasa ili pluća.
17. Spoj ili kompozicija, za uporabu prema patentnom zahtjevu 14, pri čemu je navedeni poremećaj hepatostanični karcinom.
HRP20130986AT 2009-05-28 2013-10-17 Aminopirazol triazolotiadiazol inhibitori c-met protein kinaze HRP20130986T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18178609P 2009-05-28 2009-05-28
PCT/US2010/036312 WO2010138665A1 (en) 2009-05-28 2010-05-27 Aminopyrazole triazolothiadiazole inhibitors of c-met protien kinase

Publications (1)

Publication Number Publication Date
HRP20130986T1 true HRP20130986T1 (hr) 2013-11-22

Family

ID=42346870

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20130986AT HRP20130986T1 (hr) 2009-05-28 2013-10-17 Aminopirazol triazolotiadiazol inhibitori c-met protein kinaze

Country Status (26)

Country Link
EP (1) EP2435443B1 (hr)
JP (1) JP5686796B2 (hr)
KR (1) KR20120030110A (hr)
CN (1) CN102459283B (hr)
AR (1) AR076617A1 (hr)
AU (1) AU2010254055B2 (hr)
BR (1) BRPI1012037A2 (hr)
CA (1) CA2762190A1 (hr)
CL (1) CL2011002946A1 (hr)
DK (1) DK2435443T3 (hr)
ES (1) ES2433090T3 (hr)
HK (1) HK1169105A1 (hr)
HR (1) HRP20130986T1 (hr)
IL (1) IL216581A (hr)
MX (1) MX2011012521A (hr)
NZ (1) NZ596616A (hr)
PL (1) PL2435443T3 (hr)
PT (1) PT2435443E (hr)
RS (1) RS53011B (hr)
RU (1) RU2552993C2 (hr)
SG (1) SG176574A1 (hr)
SI (1) SI2435443T1 (hr)
TW (1) TWI491614B (hr)
UA (1) UA106082C2 (hr)
WO (1) WO2010138665A1 (hr)
ZA (1) ZA201108655B (hr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102448968A (zh) * 2009-05-28 2012-05-09 沃泰克斯药物股份有限公司 C-met蛋白激酶的取代的吡唑抑制剂
US8263777B2 (en) 2010-05-27 2012-09-11 Vertex Pharmaceuticals Incorporated Aminopyrazole triazolothiadiazole inhibitor of c-Met protein kinase
TR201113223A2 (tr) * 2011-12-29 2012-06-21 Koçak Farma İlaç Ve Ki̇mya Sanayi̇ A. Ş. Pemetrekset disodyum hazırlanmasına yönelik tek basamaklı işlem.
KR101373912B1 (ko) 2012-03-26 2014-03-13 중앙대학교 산학협력단 Shp-2의 활성을 특이적으로 저해하는 조성물 및 이의 제조방법
CN108853108A (zh) * 2015-12-31 2018-11-23 北京浦润奥生物科技有限责任公司 化合物在制备用于治疗脑胶质瘤的药物中的用途
CN109897054B (zh) * 2017-12-08 2021-12-10 中国药科大学 三唑并噻二唑类c-Met激酶抑制剂的制备方法及其用途

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5716981A (en) 1993-07-19 1998-02-10 Angiogenesis Technologies, Inc. Anti-angiogenic compositions and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
ZA200501536B (en) * 2002-08-14 2006-10-25 Vertex Pharma Protein kinase inhibitors and uses thereof
US7122548B2 (en) * 2003-07-02 2006-10-17 Sugen, Inc. Triazolotriazine compounds and uses thereof
JO2629B1 (en) * 2004-08-19 2012-06-24 افينتيس فارما سوتيكالز انك Branched carboxylic acid amides containing thienobirol, carboxylic acid amides containing pyrolithiazole, and the like as kinase inhibitors casein epsilon
WO2007064797A2 (en) * 2005-11-30 2007-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of c-met and uses thereof
ZA200804681B (en) * 2005-11-30 2009-11-25 Vertex Pharma Inc Inhibitors of C-Met and uses thereof
NL2000613C2 (nl) * 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
KR101156845B1 (ko) * 2007-05-21 2012-06-18 에스지엑스 파마슈티컬스, 인코포레이티드 헤테로시클릭 키나제 조절제
EP2365977B1 (en) * 2008-11-19 2012-10-03 Vertex Pharmaceuticals Incorporated A triazolothiadiazole derivative as inhibitor of c-met protein kinase
CN102448968A (zh) * 2009-05-28 2012-05-09 沃泰克斯药物股份有限公司 C-met蛋白激酶的取代的吡唑抑制剂

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Publication number Publication date
WO2010138665A1 (en) 2010-12-02
CA2762190A1 (en) 2010-12-02
HK1169105A1 (en) 2013-01-18
EP2435443A1 (en) 2012-04-04
IL216581A0 (en) 2012-02-29
PT2435443E (pt) 2013-10-31
TWI491614B (zh) 2015-07-11
RU2011153613A (ru) 2013-07-10
NZ596616A (en) 2013-05-31
DK2435443T3 (da) 2013-10-28
SG176574A1 (en) 2012-01-30
EP2435443B1 (en) 2013-07-31
SI2435443T1 (sl) 2013-12-31
UA106082C2 (uk) 2014-07-25
PL2435443T3 (pl) 2014-01-31
ZA201108655B (en) 2013-01-30
CL2011002946A1 (es) 2012-07-27
CN102459283A (zh) 2012-05-16
IL216581A (en) 2014-02-27
AU2010254055B2 (en) 2016-01-14
BRPI1012037A2 (pt) 2016-05-17
ES2433090T3 (es) 2013-12-09
MX2011012521A (es) 2012-01-30
RS53011B (en) 2014-04-30
JP5686796B2 (ja) 2015-03-18
KR20120030110A (ko) 2012-03-27
AR076617A1 (es) 2011-06-22
JP2012528186A (ja) 2012-11-12
TW201100436A (en) 2011-01-01
CN102459283B (zh) 2014-11-12
AU2010254055A1 (en) 2011-12-15
RU2552993C2 (ru) 2015-06-10

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