JP2007506787A - プロテインキナーゼインヒビターとしてのピラゾロピロール誘導体 - Google Patents
プロテインキナーゼインヒビターとしてのピラゾロピロール誘導体 Download PDFInfo
- Publication number
- JP2007506787A JP2007506787A JP2006528284A JP2006528284A JP2007506787A JP 2007506787 A JP2007506787 A JP 2007506787A JP 2006528284 A JP2006528284 A JP 2006528284A JP 2006528284 A JP2006528284 A JP 2006528284A JP 2007506787 A JP2007506787 A JP 2007506787A
- Authority
- JP
- Japan
- Prior art keywords
- independently selected
- ring
- nitrogen
- sulfur
- oxygen
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 0 CC*(C)(C)C(**1)=C2C1=N*(**)*2 Chemical compound CC*(C)(C)C(**1)=C2C1=N*(**)*2 0.000 description 48
- QYHNFKWLJQKJIT-UHFFFAOYSA-N CC(N(C1)CC2=C1C(c(nc1)ccc1C(O)=O)N2)=O Chemical compound CC(N(C1)CC2=C1C(c(nc1)ccc1C(O)=O)N2)=O QYHNFKWLJQKJIT-UHFFFAOYSA-N 0.000 description 1
- ONAHKLZOTLAZRE-UHFFFAOYSA-N CC(N(C1)CC2=C1C(c1ccc(C(O)=O)[s]1)N2)=O Chemical compound CC(N(C1)CC2=C1C(c1ccc(C(O)=O)[s]1)N2)=O ONAHKLZOTLAZRE-UHFFFAOYSA-N 0.000 description 1
- WPHSVQYNYWDLKM-UHFFFAOYSA-N CCC(C(N(C1)CC2=C1C(c(nc1)ccc1C(O)=O)N2)=O)c1ccccc1 Chemical compound CCC(C(N(C1)CC2=C1C(c(nc1)ccc1C(O)=O)N2)=O)c1ccccc1 WPHSVQYNYWDLKM-UHFFFAOYSA-N 0.000 description 1
- SVPJLIYAHZYRGO-UHFFFAOYSA-N CCC(CCN)c1ccccc1 Chemical compound CCC(CCN)c1ccccc1 SVPJLIYAHZYRGO-UHFFFAOYSA-N 0.000 description 1
- VDHHIJGKIWFRQZ-UHFFFAOYSA-N NCCC(C(N(C1)CC(N)=C1C(c1ccccc1)N)=O)c1ccccc1 Chemical compound NCCC(C(N(C1)CC(N)=C1C(c1ccccc1)N)=O)c1ccccc1 VDHHIJGKIWFRQZ-UHFFFAOYSA-N 0.000 description 1
- LESPWGZLAJLZMG-UHFFFAOYSA-N NCCC(C(N(C1)CC2=C1C(C1C=CC(Cl)=CC1)=N2)=O)c1ccccc1 Chemical compound NCCC(C(N(C1)CC2=C1C(C1C=CC(Cl)=CC1)=N2)=O)c1ccccc1 LESPWGZLAJLZMG-UHFFFAOYSA-N 0.000 description 1
- QYXGTVMMFSEMRC-UHFFFAOYSA-N NCCC(C(N(C1)CC2=C1C(c(cc1)ccc1C(N)=O)=N2)=O)c1ccccc1 Chemical compound NCCC(C(N(C1)CC2=C1C(c(cc1)ccc1C(N)=O)=N2)=O)c1ccccc1 QYXGTVMMFSEMRC-UHFFFAOYSA-N 0.000 description 1
- HMWBLRZJYZJWGM-UHFFFAOYSA-N NCCC(C(N(C1)CC2=C1C(c(cc1)ccc1C(O)=O)N2)=O)c1ccccc1 Chemical compound NCCC(C(N(C1)CC2=C1C(c(cc1)ccc1C(O)=O)N2)=O)c1ccccc1 HMWBLRZJYZJWGM-UHFFFAOYSA-N 0.000 description 1
- OTWQQZSFYCJDRP-UHFFFAOYSA-N OC(c1ccc(C2=NC3=C2CN(Cc2ccccc2)C3)nc1)=O Chemical compound OC(c1ccc(C2=NC3=C2CN(Cc2ccccc2)C3)nc1)=O OTWQQZSFYCJDRP-UHFFFAOYSA-N 0.000 description 1
- CUOBCWXONRZGFY-UHFFFAOYSA-N OC(c1ccc(C2NC3=C2CN(Cc2ccccc2)C3)[s]1)=O Chemical compound OC(c1ccc(C2NC3=C2CN(Cc2ccccc2)C3)[s]1)=O CUOBCWXONRZGFY-UHFFFAOYSA-N 0.000 description 1
- LFGPREURINDXQE-UHFFFAOYSA-N OCC(C(N(C1)CC2=C1C(c(nc1)ccc1C(O)=O)N2)=O)c1ccccc1 Chemical compound OCC(C(N(C1)CC2=C1C(c(nc1)ccc1C(O)=O)N2)=O)c1ccccc1 LFGPREURINDXQE-UHFFFAOYSA-N 0.000 description 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)
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 (2)
| Publication Number | Publication Date |
|---|---|
| JP2007506787A true JP2007506787A (ja) | 2007-03-22 |
| JP2007506787A5 JP2007506787A5 (https=) | 2007-11-08 |
Family
ID=34392996
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006528284A Pending JP2007506787A (ja) | 2003-09-23 | 2004-09-23 | プロテインキナーゼインヒビターとしてのピラゾロピロール誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US7652135B2 (https=) |
| EP (1) | EP1668013B1 (https=) |
| JP (1) | JP2007506787A (https=) |
| AT (1) | ATE546452T1 (https=) |
| AU (1) | AU2004276341B2 (https=) |
| CA (1) | CA2539549A1 (https=) |
| WO (1) | WO2005030776A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010523643A (ja) * | 2007-04-12 | 2010-07-15 | ファイザー・インク | 新規な3−アミド−ピロロ[3,4−c]ピラゾール−5(1H,4H,6H)カルバルデヒド誘導体 |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 (en) | 2006-03-15 | 2008-12-17 | Theralogics, Inc. | Methods of treating muscular wasting diseases using nf-kb activation inhibitors |
| 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 |
| 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 (en) | 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mgl pet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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002012242A2 (en) * | 2000-08-10 | 2002-02-14 | Pharmacia Italia S.P.A. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| WO2002022603A1 (en) * | 2000-09-15 | 2002-03-21 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US5508300A (en) * | 1994-01-14 | 1996-04-16 | Pfizer Inc. | Dihydro pyrazolopyrroles, compositions and use |
| US6187774B1 (en) * | 1996-03-04 | 2001-02-13 | Yoshitomi Pharmaceutical Industries, Ltd. | Fused heterocyclic compounds and pharmaceutical applications thereof |
| NZ511674A (en) | 1998-12-23 | 2003-11-28 | Du Pont Pharm Co | Nitrogen containing heterobicycles as factor Xa inhibitors |
| 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 |
| 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 |
| US7429609B2 (en) | 2002-05-31 | 2008-09-30 | Eisai R & D Management Co., Ltd. | Pyrazole compound and medicinal composition containing the same |
| 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 (en) | 2002-07-25 | 2005-05-04 | Pharmacia Italia S.p.A. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| UA81790C2 (uk) | 2002-12-19 | 2008-02-11 | Фармация Италия С.П.А. | Заміщені піролопіразольні похідні як інгібітори кінази |
| US20070037790A1 (en) * | 2003-03-11 | 2007-02-15 | Francesca Abrate | Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| 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/en 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
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002012242A2 (en) * | 2000-08-10 | 2002-02-14 | Pharmacia Italia S.P.A. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| US20030171357A1 (en) * | 2000-08-10 | 2003-09-11 | Deniele Fancelli | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| WO2002022603A1 (en) * | 2000-09-15 | 2002-03-21 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010523643A (ja) * | 2007-04-12 | 2010-07-15 | ファイザー・インク | 新規な3−アミド−ピロロ[3,4−c]ピラゾール−5(1H,4H,6H)カルバルデヒド誘導体 |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2539549A1 (en) | 2005-04-07 |
| ATE546452T1 (de) | 2012-03-15 |
| US7652135B2 (en) | 2010-01-26 |
| US8642779B2 (en) | 2014-02-04 |
| EP1668013A1 (en) | 2006-06-14 |
| AU2004276341A1 (en) | 2005-04-07 |
| US20050101594A1 (en) | 2005-05-12 |
| US20100087467A1 (en) | 2010-04-08 |
| WO2005030776A1 (en) | 2005-04-07 |
| EP1668013B1 (en) | 2012-02-22 |
| AU2004276341B2 (en) | 2011-04-14 |
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