JP2004509857A5 - - Google Patents
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- Publication number
- JP2004509857A5 JP2004509857A5 JP2002515891A JP2002515891A JP2004509857A5 JP 2004509857 A5 JP2004509857 A5 JP 2004509857A5 JP 2002515891 A JP2002515891 A JP 2002515891A JP 2002515891 A JP2002515891 A JP 2002515891A JP 2004509857 A5 JP2004509857 A5 JP 2004509857A5
- Authority
- JP
- Japan
- Prior art keywords
- dimethylethyl
- oxazolyl
- thiazolyl
- thio
- methyl
- 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.)
- Withdrawn
Links
- 150000003839 salts Chemical class 0.000 description 12
- 239000012453 solvate Substances 0.000 description 11
- 150000001875 compounds Chemical class 0.000 description 10
- 125000000217 alkyl group Chemical group 0.000 description 8
- 229910052739 hydrogen Inorganic materials 0.000 description 7
- 239000001257 hydrogen Substances 0.000 description 7
- 125000000753 cycloalkyl group Chemical group 0.000 description 5
- 150000002431 hydrogen Chemical class 0.000 description 5
- 125000000547 substituted alkyl group Chemical group 0.000 description 5
- 239000003937 drug carrier Substances 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- USAKOZCUIYTREA-LLVKDONJSA-N (3r)-n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-3-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)[C@H]1CNCCC1 USAKOZCUIYTREA-LLVKDONJSA-N 0.000 description 2
- 0 C*(C)c1cnc(CSc2cnc(NC(C3CN(*)CCC3)=O)[s]2)[o]1 Chemical compound C*(C)c1cnc(CSc2cnc(NC(C3CN(*)CCC3)=O)[s]2)[o]1 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- OUSFTKFNBAZUKL-UHFFFAOYSA-N N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CCNCC1 OUSFTKFNBAZUKL-UHFFFAOYSA-N 0.000 description 2
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 description 2
- USAKOZCUIYTREA-UHFFFAOYSA-N n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-3-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CNCCC1 USAKOZCUIYTREA-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- USAKOZCUIYTREA-NSHDSACASA-N (3s)-n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-3-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)[C@@H]1CNCCC1 USAKOZCUIYTREA-NSHDSACASA-N 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- SXDBWCPKPHAZSM-UHFFFAOYSA-M bromate Inorganic materials [O-]Br(=O)=O SXDBWCPKPHAZSM-UHFFFAOYSA-M 0.000 description 1
- SXDBWCPKPHAZSM-UHFFFAOYSA-N bromic acid Chemical compound OBr(=O)=O SXDBWCPKPHAZSM-UHFFFAOYSA-N 0.000 description 1
- -1 dihydrochloride Chemical compound 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- ICIWUVCWSCSTAQ-UHFFFAOYSA-M iodate Chemical compound [O-]I(=O)=O ICIWUVCWSCSTAQ-UHFFFAOYSA-M 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- LURBGHNXFQSPMM-UHFFFAOYSA-N n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]-1-(2,3-dihydroxypropyl)piperidine-4-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CCN(CC(O)CO)CC1 LURBGHNXFQSPMM-UHFFFAOYSA-N 0.000 description 1
- NASKBLMGBFRGIF-UHFFFAOYSA-N n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]-1-(2-hydroxyethyl)piperidine-4-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CCN(CCO)CC1 NASKBLMGBFRGIF-UHFFFAOYSA-N 0.000 description 1
- BMJRSDXYHRHHKI-UHFFFAOYSA-N n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]-1-cyclopropylpiperidine-4-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CCN(C2CC2)CC1 BMJRSDXYHRHHKI-UHFFFAOYSA-N 0.000 description 1
- JJJVIPYJUNRQTI-UHFFFAOYSA-N n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]-1-propan-2-ylpiperidine-4-carboxamide Chemical compound C1CN(C(C)C)CCC1C(=O)NC(S1)=NC=C1SCC1=NC=C(C(C)(C)C)O1 JJJVIPYJUNRQTI-UHFFFAOYSA-N 0.000 description 1
- IYLMWEFXWOERFM-UHFFFAOYSA-N n-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]cyclohexanecarboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CCCCC1 IYLMWEFXWOERFM-UHFFFAOYSA-N 0.000 description 1
- 230000023603 positive regulation of transcription initiation, DNA-dependent Effects 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
Applications Claiming Priority (4)
| 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 |
| PCT/US2001/015081 WO2002010162A1 (en) | 2000-07-26 | 2001-05-09 | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl] carboxamide inhibitors of cyclin dependent kinases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004509857A JP2004509857A (ja) | 2004-04-02 |
| JP2004509857A5 true JP2004509857A5 (enExample) | 2008-06-19 |
Family
ID=27417184
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002515891A Withdrawn JP2004509857A (ja) | 2000-07-26 | 2001-05-09 | サイクリン依存性キナーゼのｎ−［５−［［［５−アルキル−２−オキサゾリル］メチル］チオ］−２−チアゾリル］カルボキサミドインヒビター |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP1303513A1 (enExample) |
| JP (1) | JP2004509857A (enExample) |
| KR (1) | KR20030016429A (enExample) |
| CN (1) | CN100457753C (enExample) |
| AR (1) | AR030563A1 (enExample) |
| AU (1) | AU2001259704A1 (enExample) |
| BG (1) | BG65132B1 (enExample) |
| BR (1) | BR0112674A (enExample) |
| CA (1) | CA2417254A1 (enExample) |
| CZ (1) | CZ2003237A3 (enExample) |
| EE (1) | EE200300041A (enExample) |
| EG (1) | EG24409A (enExample) |
| GE (1) | GEP20043367B (enExample) |
| HR (1) | HRP20030116A2 (enExample) |
| HU (1) | HUP0303698A2 (enExample) |
| IL (2) | IL153591A0 (enExample) |
| LV (1) | LV13037B (enExample) |
| MX (1) | MXPA03000774A (enExample) |
| MY (1) | MY129635A (enExample) |
| NO (1) | NO20030394L (enExample) |
| PL (1) | PL365170A1 (enExample) |
| SI (1) | SI21099A (enExample) |
| SK (1) | SK18392002A3 (enExample) |
| TW (1) | TWI302533B (enExample) |
| WO (1) | WO2002010162A1 (enExample) |
| YU (1) | YU4903A (enExample) |
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 |
| 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 |
| AR038703A1 (es) | 2002-02-28 | 2005-01-26 | Novartis Ag | Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3 |
| EP1545533A1 (en) | 2002-09-04 | 2005-06-29 | Schering Corporation | Pyrazolopyrimidines 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 |
| US8673924B2 (en) | 2002-09-04 | 2014-03-18 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| RU2380369C9 (ru) | 2002-09-04 | 2011-07-10 | Шеринг Корпорейшн | Новые пиразолопиримидины как ингибиторы циклин-зависимой киназы |
| JP4799864B2 (ja) | 2002-09-23 | 2011-10-26 | シェーリング コーポレイション | サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン |
| KR20060010709A (ko) | 2002-09-23 | 2006-02-02 | 쉐링 코포레이션 | 사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진 |
| 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 |
| EP1928865A1 (en) * | 2005-08-17 | 2008-06-11 | Schering Corporation | Novel high affinity thiophene-based and furan-based kinase ligands |
| CA2621983A1 (en) | 2005-09-09 | 2007-03-22 | Schering Corporation | Azafused cyclin dependent kinase inhibitors |
| PE20070543A1 (es) | 2005-10-06 | 2007-06-14 | Schering Corp | Pirazolopirimidinas como inhibidores de protein quinasas |
| JP2009539846A (ja) * | 2006-06-06 | 2009-11-19 | ブリストル−ミエルス スクイッブ カンパニー | Ｎ−［５−［［［５−（１，１−ジメチルエチル）−２−オキサゾリル］メチル］チオ］−２−チアゾリル］−４−ピペリジンカルボキサミドの結晶形 |
| US20090175852A1 (en) | 2006-06-06 | 2009-07-09 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| EP2078003B1 (en) | 2006-10-31 | 2017-03-08 | Merck Sharp & Dohme Corp. | Anilinopiperazine derivatives and methods of use thereof |
| KR20090082440A (ko) | 2006-10-31 | 2009-07-30 | 쉐링 코포레이션 | 단백질 키나제 억제제로서의 2-아미노티아졸-4-카복실산 아미드 |
| CA2686848A1 (en) | 2007-05-08 | 2008-11-20 | Schering Corporation | 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 |
| EP2470183B1 (en) | 2009-08-26 | 2015-09-16 | Merck Sharp & Dohme Corp. | Heterocyclic amide compounds as protein kinase inhibitors |
| ES2685709T3 (es) | 2012-03-30 | 2018-10-10 | Merck Sharp & Dohme Corp. | Biomarcador predictivo mediado por un inhibidor de CDK útil para la terapia contra el cáncer |
| EP3078671A4 (en) * | 2013-12-04 | 2017-05-31 | Hangzhou Minsheng Institutes for Pharma Research Co., Ltd. | Gemcitabine derivative, composition containing the derivative and pharmaceutical use of the derivative |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6262096B1 (en) * | 1997-11-12 | 2001-07-17 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| US6040321A (en) * | 1997-11-12 | 2000-03-21 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| AU768751B2 (en) * | 1998-06-18 | 2004-01-08 | 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 WO PCT/US2001/015081 patent/WO2002010162A1/en not_active Ceased
- 2001-05-09 SK SK1839-2002A patent/SK18392002A3/sk unknown
- 2001-05-09 HR HR20030116A patent/HRP20030116A2/hr not_active Application Discontinuation
- 2001-05-09 IL IL15359101A patent/IL153591A0/xx unknown
- 2001-05-09 GE GE5063A patent/GEP20043367B/en unknown
- 2001-05-09 CZ CZ2003237A patent/CZ2003237A3/cs unknown
- 2001-05-09 EE EEP200300041A patent/EE200300041A/xx 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 AU AU2001259704A patent/AU2001259704A1/en not_active Abandoned
- 2001-05-09 HU HU0303698A patent/HUP0303698A2/hu unknown
- 2001-05-09 CN CNB018133673A patent/CN100457753C/zh not_active Expired - Fee Related
- 2001-05-09 MX MXPA03000774A patent/MXPA03000774A/es unknown
- 2001-05-09 PL PL01365170A patent/PL365170A1/xx not_active Application Discontinuation
- 2001-05-09 JP JP2002515891A patent/JP2004509857A/ja not_active Withdrawn
- 2001-05-09 SI SI200120051A patent/SI21099A/sl not_active IP Right Cessation
- 2001-05-09 YU YU4903A patent/YU4903A/sh unknown
- 2001-05-09 CA CA002417254A patent/CA2417254A1/en not_active Abandoned
- 2001-05-09 EP EP01933266A patent/EP1303513A1/en not_active Withdrawn
- 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
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