AU2001235844A1 - Imidazol-2-carboxamide derivatives as raf kinase inhibitors - Google Patents
Imidazol-2-carboxamide derivatives as raf kinase inhibitorsInfo
- Publication number
- AU2001235844A1 AU2001235844A1 AU2001235844A AU3584401A AU2001235844A1 AU 2001235844 A1 AU2001235844 A1 AU 2001235844A1 AU 2001235844 A AU2001235844 A AU 2001235844A AU 3584401 A AU3584401 A AU 3584401A AU 2001235844 A1 AU2001235844 A1 AU 2001235844A1
- Authority
- AU
- Australia
- Prior art keywords
- sub
- sup
- alkyl
- hydrogen
- optionally substituted
- 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.)
- Abandoned
Links
- 102000009929 raf Kinases Human genes 0.000 title abstract 2
- 108010077182 raf Kinases Proteins 0.000 title abstract 2
- NMIZONYLXCOHEF-UHFFFAOYSA-N 1h-imidazole-2-carboxamide Chemical class NC(=O)C1=NC=CN1 NMIZONYLXCOHEF-UHFFFAOYSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P35/00—Antineoplastic 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Compounds of formula (I): wherein X is O, CH<SUB>2</SUB>, S or NH, or the moiety X-R<SUP>1 </SUP>is hydrogen; V is CH or N; R<SUP>1 </SUP>is hydrogen, C<SUB>1-6</SUB>alkyl, C<SUB>3-7</SUB>cycloalkyl, aryl, arylC<SUB>1-6</SUB>alkyl, heterocyclyl, heterocyclyl-C<SUB>1-6</SUB>alkyl, heteroaryl, or heteroarylC<SUB>1-6</SUB>alkyl any of which except hydrogen may be optionally substituted; R<SUP>2 </SUP>and R<SUP>3 </SUP>independently represent hydrogen, C<SUB>1-6</SUB>alkyl, C<SUB>3-7</SUB>cycloalkyl, aryl, arylC<SUB>1-6</SUB>alkyl, heteroaryl, heteroarylC<SUB>1-6</SUB>alkyl, heterocyclyl, or heterocyclylC<SUB>1-6</SUB>alkyl any one of which except hydrogen may be optionally substituted, or R<SUP>2 </SUP>and R<SUP>3 </SUP>together with the nitrogen atom to which they are attached form a 4- to 10-membered optionally substituted monocyclic or bicyclic ring; Ar is an aryl or heteroaryl ring either of which may be optionally substituted; one of X<SUB>1 </SUB>and X<SUB>2 </SUB>is N and the other is NR<SUP>4</SUP>, wherein R<SUP>4 </SUP>is hydrogen, C<SUB>1-6</SUB>alkyl, or arylC<SUB>1-6</SUB>alkyl; or pharmaceutically acceptable salts thereof; their use as inhibitors of Raf kinases and pharmaceutical compositions containing them.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0005357.9A GB0005357D0 (en) | 2000-03-06 | 2000-03-06 | Compounds |
| GB0005357 | 2000-03-06 | ||
| PCT/GB2001/000916 WO2001066540A1 (en) | 2000-03-06 | 2001-03-02 | Imidazol-2-carboxamide derivatives as raf kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2001235844A1 true AU2001235844A1 (en) | 2001-09-17 |
Family
ID=9887051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2001235844A Abandoned AU2001235844A1 (en) | 2000-03-06 | 2001-03-02 | Imidazol-2-carboxamide derivatives as raf kinase inhibitors |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6987119B2 (en) |
| EP (1) | EP1261602B1 (en) |
| JP (1) | JP2003525937A (en) |
| AT (1) | ATE266021T1 (en) |
| AU (1) | AU2001235844A1 (en) |
| DE (1) | DE60103133T2 (en) |
| DK (1) | DK1261602T3 (en) |
| ES (1) | ES2217118T3 (en) |
| GB (1) | GB0005357D0 (en) |
| PT (1) | PT1261602E (en) |
| TR (1) | TR200401903T4 (en) |
| WO (1) | WO2001066540A1 (en) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| ATE538794T1 (en) | 1999-01-13 | 2012-01-15 | Bayer Healthcare Llc | GAMMA CARBOXYARYL SUBSTITUTED DIPHENYL UREA COMPOUNDS AS P38 KINASE INHIBITORS |
| IL149150A0 (en) * | 1999-11-22 | 2002-12-01 | Smithkline Beecham Plc | 2-(4-(6-methoxy-naphthalene-2-yl)-5-pyridin-4-yl-1h-imidazole-2-yl)-2-methyl-derivatives, pharmaceutical compositions comprising them and use thereof as tie2 receptor kinase inhibitors |
| JP2003525936A (en) * | 2000-03-06 | 2003-09-02 | スミスクライン ビーチャム パブリック リミテッド カンパニー | Imidazole derivatives as RAF kinase inhibitors |
| GB0112348D0 (en) | 2001-05-19 | 2001-07-11 | Smithkline Beecham Plc | Compounds |
| GB0121494D0 (en) | 2001-09-05 | 2001-10-24 | Smithkline Beecham Plc | Compounds |
| GB0121488D0 (en) | 2001-09-05 | 2001-10-24 | Smithkline Beecham Plc | Compounds |
| WO2003022837A1 (en) * | 2001-09-05 | 2003-03-20 | Smithkline Beecham P.L.C. | Heterocycle-carboxamide derivatives as raf kinase inhibitors |
| US7446106B2 (en) | 2001-09-05 | 2008-11-04 | Smithkline Beecham Plc | Pyridylfurans and pyrroles as Raf kinase inhibitors |
| MXPA04007832A (en) | 2002-02-11 | 2005-09-08 | Bayer Pharmaceuticals Corp | Aryl ureas with angiogenesis inhibiting activity. |
| AR038966A1 (en) * | 2002-03-18 | 2005-02-02 | Solvay Pharm Bv | DERIVATIVES OF TIAZOL THAT HAVE ANTAGONIST, AGONIST OR PARTIAL AGONIST ACTIVITY OF CB1 |
| AU2003262911A1 (en) | 2002-08-29 | 2004-03-19 | Scios Inc. | Methods of promoting osteogenesis |
| EP1636585B2 (en) | 2003-05-20 | 2012-06-13 | Bayer HealthCare LLC | Diaryl ureas with kinase inhibiting activity |
| HRP20060073B1 (en) | 2003-07-23 | 2014-03-14 | Bayer Healthcare Llc | Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions |
| US7244441B2 (en) | 2003-09-25 | 2007-07-17 | Scios, Inc. | Stents and intra-luminal prostheses containing map kinase inhibitors |
| US20050282909A1 (en) * | 2003-11-14 | 2005-12-22 | Diks Sander H | Guanylhydrazones in methods of treatment or diagnosis as modulators of signal transduction |
| BRPI0514691A (en) * | 2004-08-31 | 2008-06-17 | Astrazeneca Ab | compound or a pharmaceutically acceptable salt thereof, process for preparing it, pharmaceutical composition, and use of a compound or pharmaceutically acceptable salt thereof |
| AU2005278961A1 (en) * | 2004-09-01 | 2006-03-09 | Astrazeneca Ab | Quinazolinone derivatives and their use as B-Raf inhibitors |
| EP1676574A3 (en) | 2004-12-30 | 2006-07-26 | Johnson & Johnson Vision Care, Inc. | Methods for promoting survival of transplanted tissues and cells |
| EA200801118A1 (en) * | 2005-10-18 | 2008-10-30 | Янссен Фармацевтика Н.В. | FLT3 KINASE INHIBITION METHOD |
| US8697716B2 (en) * | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| WO2007124322A1 (en) | 2006-04-20 | 2007-11-01 | Janssen Pharmaceutica N.V. | Inhibitors of c-fms kinase |
| AR066845A1 (en) | 2007-06-05 | 2009-09-16 | Takeda Pharmaceutical | DERIVATIVES OF TRIAZOLOPIRIDINE AND IMIDAZOPIRIDINE A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND THEIR USE IN THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OF CANCER |
| BRPI0814423B1 (en) | 2007-07-17 | 2022-04-19 | Plexxikon, Inc | Kinase modulating compounds and pharmaceutical composition comprising the same |
| EP2181987B9 (en) | 2007-08-23 | 2014-09-03 | Takeda Pharmaceutical Company Limited | 2-Carbonylaminobenzothiazoles and their use for the prophylaxis and treatment of cancer |
| EP2184285B1 (en) | 2007-08-29 | 2015-11-04 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and use thereof |
| CN102015686B (en) | 2008-03-21 | 2014-07-02 | 诺华股份有限公司 | Novel heterocyclic compounds and uses therof |
| US8865732B2 (en) | 2008-03-21 | 2014-10-21 | Novartis Ag | Heterocyclic compounds and uses thereof |
| WO2010064611A1 (en) | 2008-12-01 | 2010-06-10 | 武田薬品工業株式会社 | Heterocyclic compound and use thereof |
| JO3101B1 (en) | 2008-12-02 | 2017-09-20 | Takeda Pharmaceuticals Co | Benzothiazole derivatives as anticancer agents |
| KR20140011780A (en) * | 2012-07-19 | 2014-01-29 | 한미약품 주식회사 | Isoquinoline-5-carboxamide derivatives having inhibitory activity for protein kinases |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| WO2015041534A1 (en) | 2013-09-20 | 2015-03-26 | Stichting Het Nederlands Kanker Instituut | P90rsk in combination with raf/erk/mek |
| EP3046557A1 (en) | 2013-09-20 | 2016-07-27 | Stichting Het Nederlands Kanker Instituut | Rock in combination with mapk-pathway |
| US20170027940A1 (en) | 2014-04-10 | 2017-02-02 | Stichting Het Nederlands Kanker Instituut | Method for treating cancer |
| WO2015178770A1 (en) | 2014-05-19 | 2015-11-26 | Stichting Het Nederlands Kanker Instituut | Compositions for cancer treatment |
| UY36294A (en) | 2014-09-12 | 2016-04-29 | Novartis Ag | COMPOUNDS AND COMPOSITIONS AS QUINASA INHIBITORS |
| CA3037456A1 (en) | 2016-09-19 | 2018-03-22 | Novartis Ag | Therapeutic combinations comprising a raf inhibitor and a erk inhibitor |
| IL270224B1 (en) | 2017-05-02 | 2024-04-01 | Novartis Ag | Combination therapy using trametinib and a defined RAF inhibitor |
| EP4563150A3 (en) | 2019-05-13 | 2025-07-23 | Novartis AG | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD201677A5 (en) | 1980-07-25 | 1983-08-03 | Ciba Geigy | PROCESS FOR THE PREPARATION OF TRISUBSTITUTED IMIDAZOLE DERIVATIVES |
| US5236917A (en) | 1989-05-04 | 1993-08-17 | Sterling Winthrop Inc. | Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof |
| US5620999A (en) | 1994-07-28 | 1997-04-15 | Weier; Richard M. | Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation |
| US5514505A (en) | 1995-05-15 | 1996-05-07 | Xerox Corporation | Method for obtaining improved image contrast in migration imaging members |
| US6342510B1 (en) | 1995-06-12 | 2002-01-29 | G. D. Searle & Co. | Treatment of inflammation and inflammation-related disorders with a combination of a cyclooxygenase-2 inhibitors and a leukotriene B4 receptor antagonist |
| EE03681B1 (en) * | 1995-10-06 | 2002-04-15 | Merck & Co., Inc. | Substituted imidazoles with anticancer and cytokine inhibitory activity |
| US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| GB2306108A (en) | 1995-10-13 | 1997-04-30 | Merck & Co Inc | Treatment of Raf-mediated cancers with imidazole derivatives |
| CA2250232A1 (en) | 1996-04-03 | 1997-10-09 | Allen I. Oliff | A method of treating cancer |
| ES2239357T3 (en) | 1996-06-10 | 2005-09-16 | MERCK & CO., INC. | REPLACED IMIDAZOLS THAT HAVE INHIBITING ACTIVITY OF CYTOKINS. |
| NZ334921A (en) | 1996-10-15 | 2001-03-30 | G | Use of cyclooxygenase-2 inhibitors for the treatment and preparation of a medicament for prevention of neoplasia |
| EP0994858A1 (en) | 1997-06-30 | 2000-04-26 | Ortho-McNeil Pharmaceutical, Inc. | 2-substituted imidazoles useful in the treatment of inflammatory diseases |
| DE69821132T2 (en) | 1997-10-27 | 2004-10-21 | Takeda Chemical Industries Ltd | 1,3-THIAZOLE AS ADENOSINE A3 RECEPTOR ANTAGONISTS FOR TREATING ASTHMA, ALLERGIES AND DIABETES |
| HU227711B1 (en) | 1997-12-22 | 2011-12-28 | Bayer Healthcare Llc | Inhibition of raf kinase using symmetrical and unsymmetrical substituted diphenyl ureas and pharmaceutical compositions containing them |
| KR20010025087A (en) | 1998-05-22 | 2001-03-26 | 스튜어트 알. 수터 | Novel 2-Alkyl Substituted Imidazole Compounds |
| IL149150A0 (en) | 1999-11-22 | 2002-12-01 | Smithkline Beecham Plc | 2-(4-(6-methoxy-naphthalene-2-yl)-5-pyridin-4-yl-1h-imidazole-2-yl)-2-methyl-derivatives, pharmaceutical compositions comprising them and use thereof as tie2 receptor kinase inhibitors |
| ES2289004T3 (en) | 2000-11-20 | 2008-02-01 | Smithkline Beecham Corporation | NEW COMPOUNDS. |
-
2000
- 2000-03-06 GB GBGB0005357.9A patent/GB0005357D0/en not_active Ceased
-
2001
- 2001-03-02 TR TR2004/01903T patent/TR200401903T4/en unknown
- 2001-03-02 AT AT01907980T patent/ATE266021T1/en not_active IP Right Cessation
- 2001-03-02 JP JP2001565356A patent/JP2003525937A/en not_active Withdrawn
- 2001-03-02 PT PT01907980T patent/PT1261602E/en unknown
- 2001-03-02 WO PCT/GB2001/000916 patent/WO2001066540A1/en not_active Ceased
- 2001-03-02 DK DK01907980T patent/DK1261602T3/en active
- 2001-03-02 US US10/220,675 patent/US6987119B2/en not_active Expired - Fee Related
- 2001-03-02 ES ES01907980T patent/ES2217118T3/en not_active Expired - Lifetime
- 2001-03-02 DE DE60103133T patent/DE60103133T2/en not_active Expired - Fee Related
- 2001-03-02 AU AU2001235844A patent/AU2001235844A1/en not_active Abandoned
- 2001-03-02 EP EP01907980A patent/EP1261602B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| US6987119B2 (en) | 2006-01-17 |
| EP1261602A1 (en) | 2002-12-04 |
| ATE266021T1 (en) | 2004-05-15 |
| WO2001066540A1 (en) | 2001-09-13 |
| PT1261602E (en) | 2004-08-31 |
| ES2217118T3 (en) | 2004-11-01 |
| DE60103133T2 (en) | 2004-10-14 |
| TR200401903T4 (en) | 2004-09-21 |
| DK1261602T3 (en) | 2004-08-30 |
| GB0005357D0 (en) | 2000-04-26 |
| EP1261602B1 (en) | 2004-05-06 |
| DE60103133D1 (en) | 2004-06-09 |
| JP2003525937A (en) | 2003-09-02 |
| US20030134837A1 (en) | 2003-07-17 |
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