ATE546452T1 - Pyrazolopyrrolderivate als proteinkinaseinhibitoren - Google Patents

Pyrazolopyrrolderivate als proteinkinaseinhibitoren

Info

Publication number: ATE546452T1
Authority: AT; Austria
Prior art keywords: compounds; protein kinase; pyrazolopyrrol; derivatives; kinase inhibitors
Prior art date: 2003-09-23

Application number

AT04785111T

Other languages

English (en)

Inventor

Hayley Binch

Simon Everitt

Francesca Mazzei

Daniel Robinson

Original Assignee

Vertex Pharma

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.)

2003-09-23

Filing date

2004-09-23

Publication date

2012-03-15

2004-09-23 Application filed by Vertex Pharma filed Critical Vertex Pharma

2012-03-15 Application granted granted Critical

2012-03-15 Publication of ATE546452T1 publication Critical patent/ATE546452T1/de

Links

229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
239000003909 protein kinase inhibitor Substances 0.000 title 1
GZTPJDLYPMPRDF-UHFFFAOYSA-N pyrrolo[3,2-c]pyrazole Chemical class N1=NC2=CC=NC2=C1 GZTPJDLYPMPRDF-UHFFFAOYSA-N 0.000 title 1
150000001875 compounds Chemical class 0.000 abstract 4
102000001253 Protein Kinase Human genes 0.000 abstract 2
239000003112 inhibitor Substances 0.000 abstract 2
238000000034 method Methods 0.000 abstract 2
108060006633 protein kinase Proteins 0.000 abstract 2
101000600756 Homo sapiens 3-phosphoinositide-dependent protein kinase 1 Proteins 0.000 abstract 1
101001117146 Homo sapiens [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Proteins 0.000 abstract 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
239000000203 mixture Substances 0.000 abstract 1
208000015122 neurodegenerative disease Diseases 0.000 abstract 1
239000008194 pharmaceutical composition Substances 0.000 abstract 1
230000002062 proliferating effect Effects 0.000 abstract 1

Classifications

- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

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)
Diabetes (AREA)
Epidemiology (AREA)
Hematology (AREA)
Immunology (AREA)
Cardiology (AREA)
Pain & Pain Management (AREA)
Heart & Thoracic Surgery (AREA)
Emergency Medicine (AREA)
Endocrinology (AREA)
Virology (AREA)
Obesity (AREA)
Oncology (AREA)
Rheumatology (AREA)
Communicable Diseases (AREA)
Gastroenterology & Hepatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

AT04785111T 2003-09-23 2004-09-23 Pyrazolopyrrolderivate als proteinkinaseinhibitoren ATE546452T1 (de)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US50523603P	2003-09-23	2003-09-23
PCT/US2004/031610 WO2005030776A1 (en)	2003-09-23	2004-09-23	Pyrazolopyrrole derivatives as protein kinase inhibitors

Publications (1)

Publication Number	Publication Date
ATE546452T1 true ATE546452T1 (de)	2012-03-15

Family

ID=34392996

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT04785111T ATE546452T1 (de)	2003-09-23	2004-09-23	Pyrazolopyrrolderivate als proteinkinaseinhibitoren

Country Status (7)

Country	Link
US (2)	US7652135B2 (de)
EP (1)	EP1668013B1 (de)
JP (1)	JP2007506787A (de)
AT (1)	ATE546452T1 (de)
AU (1)	AU2004276341B2 (de)
CA (1)	CA2539549A1 (de)
WO (1)	WO2005030776A1 (de)

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ES2319539T3 (es) *	2003-09-17	2009-05-08	Janssen Pharmaceutica Nv	Compuestos heterociclicos condensados como moduladores del receptor de serotonina.
NZ568692A (en)	2005-12-21	2011-07-29	Pfizer Prod Inc	Carbonylamino pyrrolopyrazoles, potent kinase inhibitors
WO2007099171A2 (en)	2006-03-03	2007-09-07	Nerviano Medical Sciences S.R.L.	Bicyclo-pyrazoles active as kinase inhibitors
EP2001455A2 (de)	2006-03-15	2008-12-17	Theralogics, Inc.	Verfahren zur behandlung von muskelschwunderkrankungen mithilfe von hemmern der nf-kb-aktivierung
AR060358A1 (es)	2006-04-06	2008-06-11	Novartis Vaccines & Diagnostic	Quinazolinas para la inhibicion de pdk 1
US20070286864A1 (en) *	2006-06-09	2007-12-13	Buck Elizabeth A	Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors
WO2008070823A2 (en)	2006-12-07	2008-06-12	University Of South Florida	Substrate-mimetic akt inhibitor
AU2008237660B2 (en) *	2007-04-12	2011-12-22	Pfizer Inc.	3-amido-pyrrolo [3, 4-C] pyrazole-5 (1H, 4H, 6H) carbaldehyde derivatives as inhibitors of protein kinase C
AU2008256940A1 (en) *	2007-05-25	2008-12-04	Elan Pharmaceuticals, Inc.	Pyrazolopyrrolidines as inhibitors of gamma secretase
KR101438293B1 (ko)	2009-09-21	2014-09-05	에프. 호프만-라 로슈 아게	Ｊａｋ의 매크로사이클릭 억제자
KR102020485B1 (ko)	2013-01-11	2019-09-11	삼성디스플레이 주식회사	블록 공중합체, 그 형성 방법 및 패턴 형성 방법
CN112472699A (zh)	2013-07-26	2021-03-12	种族肿瘤学公司	改善比生群及衍生物的治疗益处的组合方法
WO2016109684A2 (en) *	2014-12-30	2016-07-07	Novira Therapeutics, Inc.	Derivatives and methods of treating hepatitis b infections
AU2016355303B2 (en) *	2015-11-20	2021-10-07	Mingsight Pharmaceuticals, Inc.	Treatment of autoimmune disease
EP3397643A1 (de)	2015-12-30	2018-11-07	Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.	Pt(iv)-prodrugs
MY205440A (en)	2018-09-28	2024-10-21	Janssen Pharmaceutica Nv	Monoacylglycerol lipase modulators
JP7539382B2 (ja) *	2019-07-29	2024-08-23	武田薬品工業株式会社	複素環化合物
JP7697934B2 (ja)	2019-09-30	2025-06-24	ヤンセンファーマシューティカエヌ．ベー．	放射線標識されたｍｇｌｐｅｔリガンド
CN115073471B (zh) *	2021-03-11	2023-03-21	沈阳药科大学	吡唑并四氢吡咯类衍生物、其制备方法和在医药上的应用

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DK27383A (da)	1982-02-17	1983-08-18	Lepetit Spa	Fremgangsmaade til fremstilling af pyrazol(4,3-c)pyridiner
US5843912A (en) *	1994-07-06	1998-12-01	Universy Of Maryland	Ring-expanded nucleosides and nucleotides
US6677310B1 (en) *	1999-04-21	2004-01-13	Nabi	Ring-expanded nucleosides and nucleotides
DE4337611A1 (de) *	1993-11-04	1995-05-11	Boehringer Ingelheim Kg	Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337609A1 (de)	1993-11-04	1995-05-11	Boehringer Ingelheim Kg	Neue Pyrazincarboxamidderivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
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CA2374947A1 (en)	1999-05-24	2000-11-30	Robert M. Scarborough	Inhibitors of factor xa
JP2003502314A (ja)	1999-06-14	2003-01-21	イーライ・リリー・アンド・カンパニー	化合物
US7217722B2 (en)	2000-02-01	2007-05-15	Kirin Beer Kabushiki Kaisha	Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
DE10023486C1 (de)	2000-05-09	2002-03-14	Schering Ag	Ortho substituierte Anthranilsäureamide und deren Verwendung als Arzneimittel
US6897231B2 (en)	2000-07-31	2005-05-24	Signal Pharmaceuticals, Inc.	Indazole derivatives as JNK inhibitors and compositions and methods related thereto
DK1320531T3 (da) *	2000-08-10	2011-01-03	Pfizer Italia Srl	Bicyclo-pyrazoler, der er aktive som kinase inhibitorer, fremgangsmåde til fremstilling deraf og farmaceutiske sammensætninger, der indeholder disse
WO2002022605A1 (en) *	2000-09-15	2002-03-21	Vertex Pharmaceuticals Incorporated	Pyrazole compounds useful as protein kinase inhibitors
CN1300116C (zh)	2001-04-16	2007-02-14	卫材株式会社	1h－吲唑化合物
WO2002100833A1 (en)	2001-06-12	2002-12-19	Sumitomo Pharmaceuticals Company, Limited	Rho KINASE INHIBITORS
TW200306819A (en) *	2002-01-25	2003-12-01	Vertex Pharma	Indazole compounds useful as protein kinase inhibitors
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CA2493637A1 (en) *	2002-07-25	2004-02-12	Manuela Villa	Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
EP1526852A1 (de)	2002-07-25	2005-05-04	Pharmacia Italia S.p.A.	Bizyklische pyrazole wirksam als kinase inhibitoren, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zusammensetzungen
UA81790C2 (uk)	2002-12-19	2008-02-11	Фармация Италия С.П.А.	Заміщені піролопіразольні похідні як інгібітори кінази
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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

2004
- 2004-09-23 JP JP2006528284A patent/JP2007506787A/ja active Pending
- 2004-09-23 CA CA002539549A patent/CA2539549A1/en not_active Abandoned
- 2004-09-23 AT AT04785111T patent/ATE546452T1/de active
- 2004-09-23 WO PCT/US2004/031610 patent/WO2005030776A1/en not_active Ceased
- 2004-09-23 EP EP04785111A patent/EP1668013B1/de not_active Expired - Lifetime
- 2004-09-23 US US10/949,714 patent/US7652135B2/en not_active Expired - Fee Related
- 2004-09-23 AU AU2004276341A patent/AU2004276341B2/en not_active Ceased
2009
- 2009-12-09 US US12/634,136 patent/US8642779B2/en not_active Expired - Fee Related

Also Published As

Publication number	Publication date
CA2539549A1 (en)	2005-04-07
JP2007506787A (ja)	2007-03-22
US7652135B2 (en)	2010-01-26
US8642779B2 (en)	2014-02-04
EP1668013A1 (de)	2006-06-14
AU2004276341A1 (en)	2005-04-07
US20050101594A1 (en)	2005-05-12
US20100087467A1 (en)	2010-04-08
WO2005030776A1 (en)	2005-04-07
EP1668013B1 (de)	2012-02-22
AU2004276341B2 (en)	2011-04-14

Publication	Publication Date	Title
ATE546452T1 (de)	2012-03-15	Pyrazolopyrrolderivate als proteinkinaseinhibitoren
DE60333387D1 (de)	2010-08-26	Triazolopyridazine als proteinkinase-inhibitoren
TW200607505A (en)	2006-03-01	Fused heterocyclic kinase inhibitors
LTC1934174I2 (lt)	2018-01-10	Azetinidai kaip MEK inhibitoriai, skirti proliferacinių ligų gydymui
NO20043531L (no)	2004-10-25	Indazolforbindelser som er nyttige som proteinkinaseinhibitorer
NO20071915L (no)	2007-05-18	Diaminotriazolforbindelser nyttige som proteinkinaseinhibitorer
DE60214703D1 (de)	2006-10-26	Thiazolverbindungen, die sich als inhibitoren von proteinkinasen eignen
SE0402735D0 (sv)	2004-11-09	Novel compounds
ATE371656T1 (de)	2007-09-15	Heteroaryl-pyrimidinderivate als jak-inhibitoren
EA200501849A1 (ru)	2006-06-30	Производные пиразолохиназолина: способ получения и применение в качестве ингибиторов киназ
DE602004011199D1 (de)	2008-02-21	5-phenylthiazolderivate und deren verwendung als p13-kinase-inhibitoren
EA201070167A1 (ru)	2013-07-30	Замещенные производные индазола, активные как ингибиторы киназы
DK1427708T3 (da)	2008-11-24	Amino-phthalazinon-derivater som kinase-inhibitorer, fremgangsmåde til deres fremstilling og farmaceutiske sammensætninger der indeholder det samme
MX2008012422A (es)	2008-10-09	Derivados de furano y tiofeno, pirrol substituido con pirimidinil y piridil como inhibidores de cinasa.
MXPA03010961A (es)	2004-02-27	Compuestos de tiazol utiles como inhibidores de proteinas cinasas.
IL184898A0 (en)	2007-12-03	Pyrrolopyrimidine derivatives and pharmaceutical compositions containing the same
ATE514699T1 (de)	2011-07-15	Substituierte pyrrolopyrazolderivate als kinaseinhibitoren
ATE532789T1 (de)	2011-11-15	Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
ATE493418T1 (de)	2011-01-15	Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren
EA200600209A1 (ru)	2006-06-30	ПРОИЗВОДНЫЕ ПИРРОЛО[3,4-c]ПИРАЗОЛА, ОБЛАДАЮЩИЕ АКТИВНОСТЬЮ КАК ИНГИБИТОРЫ КИНАЗЫ
IL188942A0 (en)	2008-04-13	Benzimidazole derivatives and pharmaceutical compositions containing the same
TW200700392A (en)	2007-01-01	Novel compounds
MX2007004248A (es)	2007-06-12	Derivados heterociclicos de bisarilurea sustituidos como inhibidores de cinasa.
DE60106409D1 (de)	2004-11-18	3-aminopyrazole als inhibitoren von cyclinabhängigen kinasen
IL179206A0 (en)	2007-03-08	Pyrrolylpyrimidine derivatives and pharmaceutical compositions containing the same