-
公开(公告)号:EP1425258A4
公开(公告)日:2005-02-16
申请号:EP02761383
申请日:2002-09-09
申请人: TAISHO PHARMA CO LTD , UNIV TEXAS
发明人: FALCK JOHN R , MIYATA NORIYUKI , ONO NAOYA , CHONAN TOMOMICHI , HIRANO HITOMI , TODA YOSHIHISA , TANAMI TOHRU , OKUYAMA SHIGERU
IPC分类号: C07D277/20 , A61K31/047 , A61K31/08 , A61K31/16 , A61K31/18 , A61K31/185 , A61K31/201 , A61K31/231 , A61K31/275 , A61K31/41 , A61K31/426 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/00 , A61P15/06 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07C33/04 , C07C33/044 , C07C33/42 , C07C59/01 , C07C59/42 , C07C59/46 , C07C59/60 , C07C69/708 , C07C69/732 , C07C235/28 , C07C255/15 , C07C255/16 , C07C259/06 , C07C309/08 , C07C309/10 , C07C309/20 , C07C309/23 , C07C309/24 , C07C309/68 , C07C311/04 , C07C311/17 , C07C311/51 , C07C317/44 , C07C323/52 , C07C323/66 , C07D257/04 , C07D277/34 , C07C59/00 , A61K31/42 , A61K31/425 , C07C255/00 , C07D277/00
CPC分类号: C07D257/04 , C07C33/044 , C07C33/423 , C07C33/426 , C07C59/42 , C07C59/46 , C07C59/60 , C07C69/708 , C07C235/28 , C07C255/15 , C07C259/06 , C07C309/10 , C07C309/20 , C07C309/23 , C07C309/24 , C07C309/68 , C07C311/17 , C07C311/51 , C07C317/44 , C07C323/52 , C07C323/66 , C07C2601/08 , C07C2601/14 , C07D277/34
摘要: A hydroxyeicosenoic acid analog represented by the following Formula (I), the bond represents a cis-vinylene group or an ethynylene group; Y represents CH2, O or S(O)p wherein p is 0, 1 or 2; m represents an integer of 1 to 4 inclusive; n represents an integer of 0 to 3 inclusive; the sum of m and n is an integer of 3 to 7 inclusive; R1 represents a C1-4 alkyl group or a C3-8 cycloalkyl group; R2 represents a hydrogen atom or a methyl group; R3 represents COR4, a nitrile group, a halogen atom, a tetrazole group or a thiazolidinedione group; R4 represents OR6, NHR6, N(OH)R?6, NHSO2R5¿, glycerol or functionalized glycerols; R5 represents a C¿1-15? alkyl group, a C6-10 aryl group or a C7-14 aryl group substituted with alkyl groups, halogens or amino groups; R?6¿ represents a hydrogen, a C¿1-10? alkyl group or a C1-10 alkyl group substituted with a hydroxyl group, or a pharmaceutically acceptable salt or hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.
摘要翻译: 由下式(I)表示的羟基二十碳烯酸类似物,该键代表顺式亚乙烯基或亚乙炔基; Y代表CH 2,O或S(O)p,其中p是0,1或2; m表示1〜4的整数, n表示0〜3的整数, m和n的总和是3〜7的整数, R1代表C1-4烷基或C3-8环烷基; R2代表氢原子或甲基; R3代表COR4,腈基,卤素原子,四唑基或噻唑烷二酮基; R4代表OR6,NHR6,N(OH)R6 6,NHSO2R5,甘油或官能化甘油; R5代表C 1-15? 烷基,被烷基,卤素或氨基取代的C 6-10芳基或C 7-14芳基; R 6表示氢,C 1-10 - 烷基或被羟基取代的C1-10烷基,或其药学上可接受的盐或水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。
-
公开(公告)号:EP1219601A4
公开(公告)日:2004-10-27
申请号:EP00957063
申请日:2000-09-08
申请人: TAISHO PHARMA CO LTD , SATO FUMIE
发明人: SATO FUMIE , TANAMI TOHRU , TANAKA HIDEO , ONO NAOYA , YAGI MAKOTO , HIRANO HITOMI
IPC分类号: A61P9/08 , A61P43/00 , C07C405/00 , A61K31/5575 , C07D295/22
CPC分类号: C07C405/00
摘要: Novel prostaglandin derivatives represented by general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both, wherein X is CH2, O, S, or the like; Y is ethylene, vinylene, ethynylene, or the like; Z is ethylene, vinylene, or ethynylene; R is hydrogen, alkyl, or cycloalkyl; R is alkyl, alkenyl, alkynyl, cycloalkyl, or the like; and R is hydrogen, alkyl, or the like. The prostaglandin derivatives exhibit an excellent inhibitory activity against the proliferation of vascular smooth muscle and are useful as preventive or therapeutic drugs for post-PTCA restenosis and so on.
-
公开(公告)号:EP1436252A4
公开(公告)日:2005-02-09
申请号:EP02761382
申请日:2002-09-09
申请人: TAISHO PHARMA CO LTD , UNIV TEXAS
发明人: FALCK JOHN R , MIYATA NORIYUKI , ONO NAOYA , CHONAN TOMOMICHI , HIRANO HITOMI , TODA YOSHIHISA , TANAMI TOHRU , OKUYAMA SHIGERU
IPC分类号: C07D277/20 , A61K31/047 , A61K31/08 , A61K31/16 , A61K31/18 , A61K31/185 , A61K31/201 , A61K31/231 , A61K31/275 , A61K31/41 , A61K31/426 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/00 , A61P15/06 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07C33/04 , C07C33/044 , C07C33/42 , C07C59/01 , C07C59/42 , C07C59/46 , C07C59/60 , C07C69/708 , C07C69/732 , C07C235/28 , C07C255/15 , C07C255/16 , C07C259/06 , C07C309/08 , C07C309/10 , C07C309/20 , C07C309/23 , C07C309/24 , C07C309/68 , C07C311/04 , C07C311/17 , C07C311/51 , C07C317/44 , C07C323/52 , C07C323/66 , C07D257/04 , C07D277/34 , C07C309/01 , C07C303/36 , C07C309/02 , C07C309/03 , C07C309/04 , C07C309/07 , C07C309/63 , C07C309/64 , C07C309/65 , C07C309/67
CPC分类号: C07D257/04 , C07C33/044 , C07C33/423 , C07C33/426 , C07C59/42 , C07C59/46 , C07C59/60 , C07C69/708 , C07C235/28 , C07C255/15 , C07C259/06 , C07C309/10 , C07C309/20 , C07C309/23 , C07C309/24 , C07C309/68 , C07C311/17 , C07C311/51 , C07C317/44 , C07C323/52 , C07C323/66 , C07C2601/08 , C07C2601/14 , C07D277/34
摘要: A hydroxyfattysulfonic acid analog represented by Formula (I): wherein X is an ethylene group, a vinylene group or an ethynylene group; Y is an ethylene group, a vinylene group, an ethynylene group, OCH2 or S(O)pCH2 wherein p is 0, 1 or 2; m is an integer of 1 to 5 inclusive; n is an integer of 0 to 4 inclusive;R1 is a C¿1-8? alkyl group, a C3-8 cycloalkyl group, a C1-4 alkyl group substituted with a C3-8 cycloalkyl group, a C1-4 alkyl group substituted with an aryl group or a C1-4 alkyl group substituted with an aryloxy group; R?2¿ is a hydrogen atom or a methyl group; R?1 and R2¿ together with the carbon atom to which they are attached may form a C¿3-8? cycloalkyl group; R?3¿ is a hydrogen atom or a C¿2-8? acyl group; R?4 is OR5 or NHR6¿, wherein R5 is a hydrogen atom, a C¿1-4? alkyl group, an alkali metal, an alkaline earth metal or an ammonium group and R?6¿ is a hydrogen atom or a C¿1-4? alkyl group; or a pharmaceutically acceptable salt or a hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.
摘要翻译: 由式(I)表示的羟基甲磺酸类似物:其中X是亚乙基,亚乙烯基或亚乙炔基; Y是亚乙基,亚乙烯基,亚乙炔基,OCH 2或S(O)pCH 2,其中p是0,1或2; m是1〜5的整数, n是0〜4的整数,R 1是C 1-8〜 烷基,C3-8环烷基,被C3-8环烷基取代的C1-4烷基,被芳基取代的C1-4烷基或被芳氧基取代的C1-4烷基; R 2是氢原子或甲基; R 1和R 2'与它们所连接的碳原子一起可形成C 3-8 - 环烷基; R 3是氢原子或C 2-8 - 酰基; R 4是OR 5或NHR 6,其中R 5是氢原子,C 1-4 - 烷基,碱金属,碱土金属或铵基,R 6是氢原子或C 1〜4 - 烷基; 或其药学上可接受的盐或水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。
-
公开(公告)号:EP1845095A4
公开(公告)日:2008-06-25
申请号:EP06711505
申请日:2006-01-10
申请人: TAISHO PHARMA CO LTD
发明人: KAKINUMA HIROYUKI , HASHIMOTO YUKO , OI TAKAHIRO , HIRANO HITOMI
IPC分类号: C07D335/00 , A61K31/382 , A61K31/4178 , A61P3/10 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D417/10 , C07D495/04
CPC分类号: C07D409/14 , A61K31/382 , A61K31/7004 , A61K45/06 , C07D335/02 , C07D409/04 , C07D409/10 , C07D417/10 , C07D495/04 , A61K2300/00
摘要: It is intended to provide a 1-thio-D-glucitol compound represented by the following formula which shows an effect of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt thereof or a hydrate thereof; and a drug containing such a compound as the active ingredient, in particular, a preventive or a remedy for diabetes, diabetes-associated diseases or diabetic complications. It is also intended to provide a method of producing the 1-thio-D-glucitol compound and an intermediate thereof.
摘要翻译: 旨在提供下式所示的1-硫代-D-葡萄糖醇化合物,其显示出抑制SGLT2,其药学上可接受的盐或其水合物的活性的作用; 和含有这种化合物作为活性成分的药物,特别是用于糖尿病,糖尿病相关疾病或糖尿病并发症的预防剂或治疗剂。 还意图提供一种生产1-硫代-D-葡萄糖醇化合物及其中间体的方法。
-
公开(公告)号:EP1211242A4
公开(公告)日:2004-11-03
申请号:EP00957064
申请日:2000-09-08
申请人: TAISHO PHARMA CO LTD
发明人: SATO FUMIE , TANAMI TOHRU , TANAKA HIDEO , ONO NAOYA , YAGI MAKOTO , HIRANO HITOMI
IPC分类号: A61P9/10 , A61P25/20 , A61P27/06 , A61P43/00 , C07C405/00 , A61K31/5575
CPC分类号: C07C405/00 , C07C405/0016
摘要: Prostaglandin derivatives of general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both: [wherein X is alpha a- or beta -substituent halogeno; Y is ethylene, vinylene, or ethynylene; A is O(CH2)n, S(O)p(CH2)n, O(CH2)qO(CH2)r, O(CH2)qS(O)p(CH2)r, S(O)p(CH2)qS(O)p(CH2)r, or S(O)p(CH2)qO(CH2)r (wherein n is an integer of 1 to 5; p is 0, 1 or 2; q is an integer of 1 to 3; and r is 0 or 1); R is C3-10 cycloalkyl, C1-4 alkyl C3-10 cycloalkyl, C3-10 cycloalkyl C1-4 alkyl, C5-10 alkyl, C5-10 alkenyl, C5-10 alkynyl, or a bridged cyclic hydrocarbon group; R is H, C1-10 alkyl, or C3-10 cycloalkyl; and m is 0, 1 or 2]. These compounds are novel and exhibit excellent prostaglandin D2-like agonism and a sleep-inducing effect.
摘要翻译: 通式(I)的前列腺素衍生物,其药学上可接受的盐或两者的水合物:[其中X是α-或β-取代基卤代; Y是亚乙基,亚乙烯基或亚乙炔基; (O)p(CH 2)n,O(CH 2)q O(CH 2)r,O(CH 2)q S(O)p qS(O)p(CH 2)r或S(O)p(CH 2)q O(CH 2)r(其中n是1至5的整数; p是0,1或2; q是1至 3;并且r是0或1); R 1为C 3-10环烷基,C 1-4烷基C 3-10环烷基,C 3-10环烷基C 1-4烷基,C 5-10烷基,C 5-10烯基,C 5-10炔基或桥环烃基; R 2是H,C 1-10烷基或C 3-10环烷基; 并且m是0,1或2]。 这些化合物是新颖的并且表现出优异的前列腺素D 2样激动作用和睡眠诱导作用。
-
公开(公告)号:EP1170286A4
公开(公告)日:2003-05-28
申请号:EP00915427
申请日:2000-04-07
申请人: TAISHO PHARMA CO LTD , SATO FUMIE
发明人: SATO FUMIE , TANAMI TOHRU , TANAKA HIDEO , ONO NAOYA , YAGI MAKOTO , HIRANO HITOMI
IPC分类号: A61K31/5575 , A61P9/00 , C07C405/00
CPC分类号: C07C405/00 , A61K31/5575 , C07C405/0033
摘要: Prostaglandin E1 derivatives represented by general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same wherein A represents ethylene, vinylene, ethynylene, O(CH2)q or S(O)r(CH2)q; R represents C3-10 cycloalkyl, (C1-4 alkyl)(C3-10 cycloalkyl), (C3-10 cycloalkyl)(C1-4 alkyl), C1-10 alkyl optionally substituted by hydroxy or C1-4 alkoxy, C2-10 alkenyl, optionally substituted by hydroxy or C1-4 alkoxy, C2-10 alkynyl, optionally substituted by hydroxy or C1-4 alkoxy, or crosslinked hydrocarbyl; R represents a hydrogen atom, C1-10 alkyl or C3-10 cycloalkyl; m is an integer of from 1 to 5; n is an integer of from 1 to 4; p is 0, 1 or 2; q is an integer of from 1 to 5; and r is 0, 1 or 2. These compounds are novel PG derivatives having an excellent inhibitory effect on vascular smooth muscle proliferation and being useful as preventives for post-PTCA reconstriction.
-
-
-
-
-