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1. 发明申请

WO2005028452A9 SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：取代三唑衍生物作为氧化蛋白拮抗剂
公开(公告)号：WO2005028452A9
公开(公告)日：2005-07-21
申请号：PCT/IB2004002977
申请日：2004-09-10
申请人： PFIZER LTD , BROWN ALAN DANIEL , ELLIS DAVID , SMITH CHRISTOPHER RONALD , PFIZER
发明人： BROWN ALAN DANIEL , ELLIS DAVID , SMITH CHRISTOPHER RONALD
IPC分类号： A61P5/10 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , A61K31/4196
CPC分类号： C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04
摘要： The present invention relates to a class of substituted 1,2,4-triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing, said, inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).
摘要翻译：本发明涉及一类具有活性作为催产素拮抗剂的式（I）的取代的1,2,4-三唑，其用途，其制备方法和含有所述抑制剂的组合物。这些抑制剂可用于各种治疗领域，包括性功能障碍，特别是早泄（P.E.）。

2. 发明申请

WO2005082866A3 SUBSTITUTED 1, 2, 4- TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：取代1,2,4-三唑衍生物作为氧化物拮抗剂
公开(公告)号：WO2005082866A3
公开(公告)日：2006-04-13
申请号：PCT/IB2005000313
申请日：2005-02-07
申请人： PFIZER LTD , PFIZER , BROWN ALAN DANIEL , CALABRESE ANDREW ANTHONY , ELLIS DAVID , SMITH CHRISTOPHER RONALD
发明人： BROWN ALAN DANIEL , CALABRESE ANDREW ANTHONY , ELLIS DAVID , SMITH CHRISTOPHER RONALD
IPC分类号： C07D249/08 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , A61K31/4196 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/496 , A61P5/10
CPC分类号： C07D249/08 , C07D401/04 , C07D401/14 , C07D403/06 , C07D405/04 , C07D405/12 , C07D405/14
摘要： The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).
摘要翻译：本发明涉及一类具有活性作为催产素拮抗剂的式（I）的取代三唑，其用途，其制备方法和含有所述抑制剂的组合物。这些抑制剂可用于各种治疗领域，包括性功能障碍，特别是早泄（P.E.）。

3. 发明申请

WO2005060963A8 BENZENESULFONYLAMINO-PYRIDIN-2-YL DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 (11-BETA-HSD-1) FOR THE TREATMENT OF DIABETES AND OBESITY 审中-公开
标题翻译：作为用于治疗糖尿病和肥胖症的11-β-羟基脱氢酶脱氢酶1型（11-BETA-HSD-1）的抑制剂的苯并呋喃亚胺基吡啶-2-基衍生物及其相关化合物
公开(公告)号：WO2005060963A8
公开(公告)日：2005-12-01
申请号：PCT/IB2004004056
申请日：2004-12-06
申请人： PFIZER , EDWARDS MARTIN PAUL , JOHNSON THEODORE OTTO JR , NAIR SAJIV KRISHNAN , SIU MICHAEL , TAYLOR WENDY DIANNE , CRIPPS STEPHAN JAMES , WANG YONG , CHENG HENGMIAO , SMITH CHRISTOPHER RONALD
发明人： EDWARDS MARTIN PAUL , JOHNSON THEODORE OTTO JR , NAIR SAJIV KRISHNAN , SIU MICHAEL , TAYLOR WENDY DIANNE , CRIPPS STEPHAN JAMES , WANG YONG , CHENG HENGMIAO , SMITH CHRISTOPHER RONALD
IPC分类号： A61K31/44 , A61K31/4436 , A61K31/4545 , C07C311/36 , C07C311/37 , C07D209/08 , C07D213/02 , C07D213/76 , C07D215/38 , C07D235/06 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04 , A61P3/04 , A61P3/10
CPC分类号： C07D209/08 , C07D213/76 , C07D215/38 , C07D235/06 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04
摘要： The present invention relates to compounds with the formula (I), or a pharmaceutically acceptable salt thereof, wherein: R is selected from the group consisting of (C1-C6)alkyl, -(CR R )t(C3-C12)cycloalkyl, -(CR R )t(C6-C12)aryl, and -(CR R )t(4-10)-membered heterocyclyl; b and k are each independently selected from 1 and 2; j is selected from the group consisting of 0, 1, and 2; t, u, p, q, and v are each independently selected from the group consisting of 0, 1, 2, 3, 4, and 5; T is a (6-10)-membered heterocyclyl containing at least one nitrogen atom; R is selected from the group consisting of H, (C1-C6)alkyl, -(CR R )t(C3-C12)cycloalkyl, -(CR R )t(C6-C12)aryl, and -(CR R )t(4-10)-membered heterocyclyl; each R and R is independently selected from H and (C1-C6)alkyl, the carbon atoms of T, R , R , R and R may each be optionally, substituted by I to 5 R groups; R is defined in the claims; The compounds of the present invention are 11 ß-hsd-1 inhibitors, and are therefore believed to be useful in the treatment of diabetes, obesity, glaucoma, osteoporosis, cognitive disorders, immune disorders, depression, hypertension, and metabolic diseases.
摘要翻译：本发明涉及具有式（I）化合物或其药学上可接受的盐，其中：R 1选自（C 1 -C 6）烷基， - （CR 3 R 4））（C 3 -C 12）环烷基， - （CR 3 R 4）t（C 6 -C 12）芳基和 - （CR 3 R 4）t（4-10） - 杂环基; b和k各自独立地选自1和2; j选自0，1和2; t，u，p，q和v各自独立地选自0,1,2,3,4和5; T是含有至少一个氮原子的（6-10） - 杂环基; R 2选自H，（C 1 -C 6）烷基， - （CR 3 R 4）t（C 3 -C 12）环烷基， - （CR 3 R 4） t（C 6 -C 12）芳基和 - （CR 3 R 4）t（4-10） - 杂环基; 每个R 3和R 4独立地选自H和（C 1 -C 6）烷基，T，R 1，R 2，R 3和R 4的碳原子，可各自任选被I至5个R 5基团取代; R 5定义在权利要求中; 本发明的化合物是11β-hsd-1抑制剂，因此被认为可用于治疗糖尿病，肥胖，青光眼，骨质疏松症，认知障碍，免疫疾病，抑郁症，高血压和代谢疾病。

4. 发明申请

WO2006100588A8 SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：取代三唑衍生物作为氧化蛋白拮抗剂
公开(公告)号：WO2006100588A8
公开(公告)日：2007-10-04
申请号：PCT/IB2006000676
申请日：2006-03-08
申请人： PFIZER LTD , BROWN ALAN DANIEL , ELLIS DAVID , SMITH CHRISTOPHER RONALD
发明人： BROWN ALAN DANIEL , ELLIS DAVID , SMITH CHRISTOPHER RONALD
IPC分类号： A61K31/4439 , A61K31/4196 , A61P15/00 , C07D249/08 , C07D401/04 , C07D403/06 , C07D403/14
CPC分类号： C07D249/08 , A61K31/4196 , A61K31/4439 , C07D401/04 , C07D401/14 , C07D403/06
摘要： The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytoci antagonists, uses thereof, processes for the preparation thereof and compositions containing sai inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction particularly premature ejaculation (P.E.).
摘要翻译：本发明涉及一类具有活性作为催产素拮抗剂的式（I）的取代三唑，其用途，其制备方法和含有sai抑制剂的组合物。这些抑制剂可用于各种治疗领域，包括性功能障碍，特别是早泄（P.E.）。

5. 发明专利

OA13344A Benzenesulfonylamino-pyridin-2-yl derivatives and related compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD-1) for the treatment of diabetes and obesity. 未知
公开(公告)号：OA13344A
公开(公告)日：2007-04-13
申请号：OA1200600201
申请日：2004-12-06
申请人： PFIZER
发明人： CHENG HENGMIAO , CRIPPS STEPHEN JAMES , EDWARDS MARTIN PAUL , JOHNSON THEODORE OTTO JR , NAIR SAJIV KRISHNAN , SIU MICHAEL , SMITH CHRISTOPHER RONALD , TAYLOR WENDY DIANNE , WANG YONG
IPC分类号： A61K31/44 , A61K31/4436 , A61K31/4545 , C07C311/36 , C07C311/37 , C07D209/08 , C07D213/02 , C07D213/76 , C07D215/38 , C07D235/06 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04
摘要： Bensulfonylaminopyridin-2-yl derivatives, their salts and solvate are new. Bensulfonylaminopyridin-2-yl derivatives of formula R 1-SO bN(R 4)T(CR 7R 6) n-C(R 5)(R 6)W (I), their salts and solvate are new. R 11-6C alkyl, (CR 7R 8) t-3-10C cycloalkyl, (CR 7R 8) t-3-10C aryl or (CR 7R 8) t-4-10C membered heteroaryl (all optionally substituted by 1 -5 R 9 groups); b and k : 1 or 2; n and j : 0 - 2; t,u,p,q and v : 0 - 5; T : 6-10 membered heterocycle containing at least one N; W : C(O)N(R 2)(R 3), C(O)OR 2 or 5 membered heterocyclyl (optionally substituted by 1 -5 R 9 groups); R 2 - R 6H or R 1; R 2R 3N : 4-10 membered heterocyclyl; R 5C+R 6C : 3-6 membered cycloalkyl ring or 3-7 menbered heterocyclyl ring; R 7 or R 8H or 1-6C alkyl (optionally substituted by 1 -5 R 9 groups); R 9halo, CN, NO 2, CF 3, CHF 2, OCF 3, azido, OH, 1-6C alkoxy, 1-6C alkyl, 2-8C alkenyl, 2-6C alkynyl, C(O)R 10, C(O)OR 11, OC(O)R 11, N(R 11)C(O)R 12, C(O)N(R 11)(R 12), N(R 11)(R 12), N(R 11)(OR 12), S(O)-1-6C alkyl, S(O) kN(R 11)(R 12), OS(O) 2R 10, NR 11S(O) k(R 12), (CR 13R 14) v-1-6C aryl, (CR 13R 14) v-4-10 membered heterocyclyl, (CR 13R 14) qC(O)(CR 13R 14) v-6-10C aryl, (CR 13R 14) qC(O)(CR 13R 14) v-4-10 membered heterocyclyl, (CR 13R 14) v-O-(CR 13R 14) q-6-10C aryl, (CR 13R 14) v-O-(CR 13R 14) q-4-10 membered heterocyclyl, (CR 13R 14) qS(O) j- (CR 13R 14) v-8-10C aryl or (CR 13R 14) qS(O) j- (CR 13R 14) v-4-10 membered heterocyclyl (where any carbon of 1-6C alkyl, 6-10C aryl or 4-10 membered heterocyclyl is optionally substituted by halo, CN, NO 2, CF 3, CHF 2, OCF 3, azido, OR 15, C(O)R 15, C(O) OR 15, OC(O)R 15, NR 15C(O)R 16, C(O)NR 15R 16, NR 15R 16, NR 15(OR 16), 1-6C alkyl, 2-8C alkenyl, 2-6C alkynyl, (CR 17R 18) u(6-10C aryl) or(CR 17R 18) u(4-10 membered heterocyclyl); R 10 - R 181-6C alkyl, (CR 19R 20) p(6-10C aryl) (both alkyl and aryl optionally substituted by (S 1), (CR 19R 20) p-4-10 membered heterocyclyl (optionally substituted by 1 - 3 (S 1) and oxo); S 1halo, CN, NO 2, CF 3, CHF 2, OCF 3, NR 21R 22, CH 2F, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, OH or 1-6C alkoxy; and R 19 - R 22H or 1-6C alkyl. Where any of the above substituents comprising methyl, methylene, methine which is not attached to halo, SO or SO 2, or N, O or S, optionally bears on the group a substituent Oh, halo, 1-6C alkyl, 1-0C alkoxy, amino, NH(1-6C alkyl) or N(alkyl)(1-6C alkyl) ACTIVITY : Antidiabetic; Anorectic; ophthalmological; Antilipemic; Osteopathic; Antitubercular, Tuberculostatic; Antiarteriosclerotic; Nootropic; Antidepressant; Virucide; Antiinflammatory; Hepatotropic; Hypotensive. MECHANISM OF ACTION : 11-beta -Hydroxysteroid dihydrogenase inhibitor. Test details are not given. (I) Showed Ki values less than 1 to 480 nm.

6. 发明专利

BRPI0414663A 未知
公开(公告)号：BRPI0414663A
公开(公告)日：2006-11-21
申请号：BRPI0414663
申请日：2004-09-10
申请人： PFIZER
发明人： BROWN ALAN DANIEL , ELLIS DAVID , SMITH CHRISTOPHER RONALD
IPC分类号： A61P5/10 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , A61K31/4196

8. 发明专利

CA2549651A1 BENZENESULFONYLAMINO-PYRIDIN-2-YL DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 (11-BETA-HSD-1) FOR THE TREATMENT OF DIABETES AND OBESITY 未知
公开(公告)号：CA2549651A1
公开(公告)日：2005-07-07
申请号：CA2549651
申请日：2004-12-06
申请人： PFIZER LTD
发明人： CHENG HENGMIAO , CRIPPS STEPHAN JAMES , WANG YONG , EDWARDS MARTIN PAUL , JOHNSON THEODORE OTTO JR , NAIR SAJIV KRISHNAN , SMITH CHRISTOPHER RONALD , TAYLOR WENDY DIANNE , SIU MICHAEL
IPC分类号： A61K31/44 , A61K31/4436 , A61K31/4545 , A61P3/04 , A61P3/10 , C07C311/36 , C07C311/37 , C07D209/08 , C07D213/02 , C07D213/76 , C07D215/38 , C07D235/06 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04
摘要： The present invention relates to compounds with the formula (I), or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of (C1-C6)alkyl, -(CR3R4)t(C3-C12)cycloalkyl, -(CR3R4)t(C6- C12)aryl, and -(CR3R4)t(4-10)-membered heterocyclyl; b and k are each independently selected from 1 and 2; j is selected from the group consisting of 0, 1, and 2; t, u, p, q, and v are each independently selected from the group consisting of 0, 1, 2, 3, 4, and 5; T is a (6-10)-membered heterocycly l containing at least one nitrogen atom; R2 is selected from the group consisting of H, (C1-C6)alkyl, -(CR3R4)t(C3-C12)cycloalkyl, -(CR3R4)t(C6- C12)aryl, and -(CR3R4)t(4-10)-membered heterocyclyl; each R3 and R4 is independently selected from H and (C1-C6)alkyl, the carbon atoms of T, R1, R 2, R3 and R4 may each be optionally, substituted by I to 5 R5 groups; R5 is defined in the claims; The compounds of the present invention are 11 .szlig. - hsd-1 inhibitors, and are therefore believed to be useful in the treatment o f diabetes, obesity, glaucoma, osteoporosis, cognitive disorders, immune disorders, depression, hypertension, and metabolic diseases.

9. 发明专利

GT200400187A DERIVADOS DE TRIAZOL SUSTITUIDOS COMO ANTAGONISTAS DE OXITOCINA. 未知
公开(公告)号：GT200400187A
公开(公告)日：2005-05-02
申请号：GT200400187
申请日：2004-09-22
申请人： PFIZER
发明人： BROWN ALAN DANIEL , ELLIS DAVID , SMITH CHRISTOPHER RONALD
IPC分类号： A61K31/4196 , C07D249/08 , C07D249/10 , C07D249/14
摘要： LA PRESENTE INVENCION SE REFIERE A UNA CLASE DE 1,2,4TRIAZOLES SUSTITUIDOS DE FORMULA (I) CON ACTIVIDAD COMO ANTAGONISTAS DE OXITOCINA, A SUS USOS, A PROCESOS PARA SU PREPARACION Y A COMPOSICIONES QUE CONTIENEN DICHOS INHIBIDORES. ESTOS INHIBIDORES TIENEN UNA UTILIDAD EN UNA DIVERSIDAD DE AREAS TERAPEUTICAS INCLUYENDO LA DISFUNCION SEXUAL, PARTICULARMENTE LA EYACULACION PRECOZ (P.E.).

10. 发明专利

CA2539297A1 SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS 未知
公开(公告)号：CA2539297A1
公开(公告)日：2005-03-31
申请号：CA2539297
申请日：2004-09-10
申请人： PFIZER LTD
发明人： BROWN ALAN DANIEL , SMITH CHRISTOPHER RONALD , ELLIS DAVID
IPC分类号： C07D249/08 , A61K31/4196 , A61P5/10 , C07D401/04 , C07D401/14 , C07D403/04

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