GEP20043367B - N-[5-[[[5-Alkyl-2-Oxazolyl]Methyl]Thio]-2-Thiazolyl Carboxamide Inhibitors of Cyclin Dependent Kinases - Google Patents
N-[5-[[[5-Alkyl-2-Oxazolyl]Methyl]Thio]-2-Thiazolyl Carboxamide Inhibitors of Cyclin Dependent KinasesInfo
- Publication number
- GEP20043367B GEP20043367B GE5063A GEAP2001005063A GEP20043367B GE P20043367 B GEP20043367 B GE P20043367B GE 5063 A GE5063 A GE 5063A GE AP2001005063 A GEAP2001005063 A GE AP2001005063A GE P20043367 B GEP20043367 B GE P20043367B
- Authority
- GE
- Georgia
- Prior art keywords
- oxazolyl
- thiazolyl
- thio
- alkyl
- methyl
- Prior art date
Links
- SCVJRXQHFJXZFZ-KVQBGUIXSA-N 2-amino-9-[(2r,4s,5r)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3h-purine-6-thione Chemical compound C1=2NC(N)=NC(=S)C=2N=CN1[C@H]1C[C@H](O)[C@@H](CO)O1 SCVJRXQHFJXZFZ-KVQBGUIXSA-N 0.000 title 1
- 108091007914 CDKs Proteins 0.000 title 1
- 102000003903 Cyclin-dependent kinases Human genes 0.000 title 1
- 108090000266 Cyclin-dependent kinases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000002062 proliferating effect Effects 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000022605 chemotherapy-induced alopecia Diseases 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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 two hetero rings
- C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61P1/04—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/14—Heterocyclic 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61662700A | 2000-07-26 | 2000-07-26 | |
| US09/727,957 US6515004B1 (en) | 1999-12-15 | 2000-12-01 | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases |
| US09/746,060 US6414156B2 (en) | 1998-10-21 | 2000-12-22 | Process for preparing azacycloalkanoylaminothiazoles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GEP20043367B true GEP20043367B (en) | 2004-06-10 |
Family
ID=27417184
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GE5063A GEP20043367B (en) | 2000-07-26 | 2001-05-09 | N-[5-[[[5-Alkyl-2-Oxazolyl]Methyl]Thio]-2-Thiazolyl Carboxamide Inhibitors of Cyclin Dependent Kinases |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP1303513A1 (OSRAM) |
| JP (1) | JP2004509857A (OSRAM) |
| KR (1) | KR20030016429A (OSRAM) |
| CN (1) | CN100457753C (OSRAM) |
| AR (1) | AR030563A1 (OSRAM) |
| AU (1) | AU2001259704A1 (OSRAM) |
| BG (1) | BG65132B1 (OSRAM) |
| BR (1) | BR0112674A (OSRAM) |
| CA (1) | CA2417254A1 (OSRAM) |
| CZ (1) | CZ2003237A3 (OSRAM) |
| EE (1) | EE200300041A (OSRAM) |
| EG (1) | EG24409A (OSRAM) |
| GE (1) | GEP20043367B (OSRAM) |
| HR (1) | HRP20030116A2 (OSRAM) |
| HU (1) | HUP0303698A2 (OSRAM) |
| IL (2) | IL153591A0 (OSRAM) |
| LV (1) | LV13037B (OSRAM) |
| MX (1) | MXPA03000774A (OSRAM) |
| MY (1) | MY129635A (OSRAM) |
| NO (1) | NO20030394L (OSRAM) |
| PL (1) | PL365170A1 (OSRAM) |
| SI (1) | SI21099A (OSRAM) |
| SK (1) | SK18392002A3 (OSRAM) |
| TW (1) | TWI302533B (OSRAM) |
| WO (1) | WO2002010162A1 (OSRAM) |
| YU (1) | YU4903A (OSRAM) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6414156B2 (en) | 1998-10-21 | 2002-07-02 | Bristol-Myers Squibb Company | Process for preparing azacycloalkanoylaminothiazoles |
| AR038703A1 (es) | 2002-02-28 | 2005-01-26 | Novartis Ag | Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3 |
| EP2311818B1 (en) * | 2002-02-28 | 2013-01-16 | Novartis AG | Combination of a 5-phenylthiazole compound as PI3 kinase inhibitor with an antiinflammatory, bronchodilatory or antihistamine drug |
| AR041137A1 (es) | 2002-09-04 | 2005-05-04 | Pharmacopeia Drug Discovery | Pirazolopirimidinas como inhibidores de quinasa dependientes de ciclinas |
| US7084271B2 (en) | 2002-09-04 | 2006-08-01 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US8673924B2 (en) | 2002-09-04 | 2014-03-18 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| US8580782B2 (en) | 2002-09-04 | 2013-11-12 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| DE60317353T2 (de) | 2002-09-23 | 2008-08-28 | Schering Corp. | Imidazopyrazine als cdk-inhibitoren |
| AU2003275031B2 (en) | 2002-09-23 | 2006-08-17 | Schering Corporation | Novel imidazopyrazines as cyclin dependent kinase inhibitors |
| GB0320197D0 (en) * | 2003-08-28 | 2003-10-01 | Novartis Ag | Organic compounds |
| EP1555264A1 (en) * | 2004-01-15 | 2005-07-20 | Sireen AG | Five-membered heterocyclic compounds as inhibitors of SRC family protein kinase. |
| DE102005008310A1 (de) * | 2005-02-17 | 2006-08-24 | Schering Ag | Verwendung von CDKII Inhibitoren zur Fertilitätskontrolle |
| US7446195B2 (en) | 2005-08-17 | 2008-11-04 | Schering Corporation | High affinity thiophene-based and furan-based kinase ligands |
| US7700773B2 (en) | 2005-09-09 | 2010-04-20 | Schering Corporation | 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridines, pyrazolo[1,5-c]pyrimidines and 2H-indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridines, and imidazo[1,5-a]pyrazines as cyclin dependent kinase inhibitors |
| CA2624882C (en) | 2005-10-06 | 2014-05-20 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| US20090175852A1 (en) | 2006-06-06 | 2009-07-09 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| EP2044066A2 (en) * | 2006-06-06 | 2009-04-08 | Bristol-Myers Squibb Company | Crystalline forms of n-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl] thio]-2-thiazolyl]-4-piperidinecarboxamide |
| AR063531A1 (es) | 2006-10-31 | 2009-01-28 | Schering Corp | Derivados de anilinopiperazina y composicion farmaceutica |
| MX2009004786A (es) | 2006-10-31 | 2009-06-05 | Schering Corp | Derivados de anilinopiperazina y sus metodos de uso. |
| NZ580982A (en) | 2007-05-08 | 2012-05-25 | Schering Corp | Methods of treatment using intravenous formulations comprising temozolomide |
| TW200922564A (en) | 2007-09-10 | 2009-06-01 | Curis Inc | CDK inhibitors containing a zinc binding moiety |
| WO2010075542A1 (en) | 2008-12-23 | 2010-07-01 | Curis, Inc. | Cdk inhibitors |
| US8669259B2 (en) | 2009-08-26 | 2014-03-11 | Merck Sharp & Dohme Corp. | Heterocyclic amide compounds as protein kinase inhibitors |
| US20150051227A1 (en) | 2012-03-30 | 2015-02-19 | Merck Sharp & Dohme Corp. | Predictive biomarker useful for cancer therapy mediated by a cdk inhibitor |
| JP6212831B2 (ja) * | 2013-12-04 | 2017-10-18 | 杭州源昶医薬科技有限公司 | ゲムシタビン誘導体、該誘導体を含む組成物及び該誘導体の製薬用途 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6040321A (en) * | 1997-11-12 | 2000-03-21 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| US6262096B1 (en) * | 1997-11-12 | 2001-07-17 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| EP1087951B9 (en) * | 1998-06-18 | 2006-09-13 | Bristol-Myers Squibb Company | Carbon substituted aminothiazole inhibitors of cyclin dependent kinases |
| US6414156B2 (en) * | 1998-10-21 | 2002-07-02 | Bristol-Myers Squibb Company | Process for preparing azacycloalkanoylaminothiazoles |
| MY125768A (en) * | 1999-12-15 | 2006-08-30 | Bristol Myers Squibb Co | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases |
-
2001
- 2001-05-09 CN CNB018133673A patent/CN100457753C/zh not_active Expired - Fee Related
- 2001-05-09 PL PL01365170A patent/PL365170A1/xx not_active Application Discontinuation
- 2001-05-09 SK SK1839-2002A patent/SK18392002A3/sk unknown
- 2001-05-09 CA CA002417254A patent/CA2417254A1/en not_active Abandoned
- 2001-05-09 EE EEP200300041A patent/EE200300041A/xx unknown
- 2001-05-09 IL IL15359101A patent/IL153591A0/xx unknown
- 2001-05-09 AU AU2001259704A patent/AU2001259704A1/en not_active Abandoned
- 2001-05-09 GE GE5063A patent/GEP20043367B/en unknown
- 2001-05-09 HU HU0303698A patent/HUP0303698A2/hu unknown
- 2001-05-09 HR HR20030116A patent/HRP20030116A2/hr not_active Application Discontinuation
- 2001-05-09 WO PCT/US2001/015081 patent/WO2002010162A1/en not_active Ceased
- 2001-05-09 SI SI200120051A patent/SI21099A/sl not_active IP Right Cessation
- 2001-05-09 JP JP2002515891A patent/JP2004509857A/ja not_active Withdrawn
- 2001-05-09 CZ CZ2003237A patent/CZ2003237A3/cs unknown
- 2001-05-09 BR BR0112674-1A patent/BR0112674A/pt not_active Application Discontinuation
- 2001-05-09 KR KR10-2003-7001141A patent/KR20030016429A/ko not_active Ceased
- 2001-05-09 YU YU4903A patent/YU4903A/sh unknown
- 2001-05-09 EP EP01933266A patent/EP1303513A1/en not_active Withdrawn
- 2001-05-09 MX MXPA03000774A patent/MXPA03000774A/es unknown
- 2001-05-16 TW TW090111741A patent/TWI302533B/zh not_active IP Right Cessation
- 2001-05-22 MY MYPI20012414A patent/MY129635A/en unknown
- 2001-05-23 EG EG20010550A patent/EG24409A/xx active
- 2001-05-24 AR ARP010102516A patent/AR030563A1/es unknown
-
2002
- 2002-12-23 IL IL153591A patent/IL153591A/en not_active IP Right Cessation
-
2003
- 2003-01-16 BG BG107468A patent/BG65132B1/bg unknown
- 2003-01-24 NO NO20030394A patent/NO20030394L/no not_active Application Discontinuation
- 2003-02-26 LV LVP-03-24A patent/LV13037B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2001259704A1 (en) | 2002-02-13 |
| KR20030016429A (ko) | 2003-02-26 |
| WO2002010162A1 (en) | 2002-02-07 |
| EG24409A (en) | 2009-05-20 |
| CN100457753C (zh) | 2009-02-04 |
| CA2417254A1 (en) | 2002-02-07 |
| JP2004509857A (ja) | 2004-04-02 |
| HUP0303698A2 (hu) | 2004-04-28 |
| IL153591A (en) | 2009-07-20 |
| TWI302533B (en) | 2008-11-01 |
| NO20030394D0 (no) | 2003-01-24 |
| EP1303513A1 (en) | 2003-04-23 |
| LV13037B (en) | 2003-11-20 |
| IL153591A0 (en) | 2003-07-06 |
| BG65132B1 (bg) | 2007-03-30 |
| BR0112674A (pt) | 2003-12-30 |
| NO20030394L (no) | 2003-03-03 |
| MY129635A (en) | 2007-04-30 |
| HRP20030116A2 (en) | 2005-02-28 |
| CZ2003237A3 (cs) | 2003-06-18 |
| SI21099A (sl) | 2003-06-30 |
| PL365170A1 (en) | 2004-12-27 |
| YU4903A (sh) | 2006-03-03 |
| EE200300041A (et) | 2005-04-15 |
| CN1444584A (zh) | 2003-09-24 |
| BG107468A (en) | 2004-01-30 |
| AR030563A1 (es) | 2003-08-27 |
| SK18392002A3 (sk) | 2003-09-11 |
| MXPA03000774A (es) | 2003-09-10 |
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