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1. 发明授权

US06740772B1 Prostaglandin derivatives 失效
标题翻译：前列腺素衍生物
公开(公告)号：US06740772B1
公开(公告)日：2004-05-25
申请号：US10070643
申请日：2002-03-11
申请人： Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi , Hitomi Hirano
发明人： Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi , Hitomi Hirano
IPC分类号： C07C17700
CPC分类号： C07C405/00 , C07C405/0016
摘要： A prostaglandin derivative represented by the formula: wherein X is a halogen atom in the &agr;- or &bgr;-position, Y is an ethylene group, a vinylene group or an ethynylene group, A is a group represented by the formula: 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), R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, and m is 0, 1 or 2], a pharmaceutically acceptable salt thereof or a hydrate thereof. The present invention is to provide novel PG derivatives having an excellent PGD2-like agonistic activity and a sleep-inducing action.
摘要翻译：由下式表示的前列腺素衍生物：其中X是α-位或β-位的卤素原子，Y是亚乙基，亚乙烯基或亚乙炔基，A是由下式表示的基团：O（CH 2）（O）p（CH2）q（O）p（CH2）q（O）p（CH2）q（O）p（CH2） CH 2）r或S（O）p（CH 2）q O（CH 2）r（其中n为1〜5的整数，p为0,1或2，q为1〜3的整数，r为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烯基基团，C5-10炔基或桥连环烃基，R 2是氢原子，C 1-10烷基或C 3-10环烷基，m是0,1或2]，药学上可接受的其盐或其水合物。本发明提供具有优异的PGD 2样激动活性和睡眠诱导作用的新型PG衍生物。

2. 发明授权

US06455584B1 Prostaglandin E1 derivatives 失效
标题翻译：前列腺素E1衍生物
公开(公告)号：US06455584B1
公开(公告)日：2002-09-24
申请号：US09937782
申请日：2002-01-04
申请人： Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi , Hitomi Hirano
发明人： Fumie Sato , Tohru Tanami , Hideo Tanaka , Naoya Ono , Makoto Yagi , Hitomi Hirano
IPC分类号： C07C17700
CPC分类号： C07C405/00 , A61K31/5575 , C07C405/0033
摘要： To provide a prostaglandin derivative represented by the formula: wherein A is an ethylene group, a vinylene group, an ethynylene group, O(CH2)q or S(O)r(CH2)q, R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C1-10 alkyl group, a C1-10 alkyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkenyl group, a C2-10 alkenyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkynyl group, a C2-10 alkynyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s) or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 1 to 5, n is an integer of 1 to 4, p is 0, 1 or 2, q is an integer of 1 to 5 and r is 0, 1 or 2; a pharmaceutically acceptable salt thereof or a hydrate thereof exhibit excellent action in inhibiting the growth of vascular smooth muscle and is useful as a drug for inhibition of restenosis after percutaneous transluminal coronary angioplasty.
摘要翻译：提供由下式表示的前列腺素衍生物：其中A是亚乙基，亚乙烯基，亚乙炔基，O（CH 2）q或S（O）r（CH 2）q，R 1是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 1-10烷基，被羟基或C 1-4烷氧基取代的C 1-10烷基 C2-10链烯基，被羟基或C1-4烷氧基取代的C2-10烯基，C2-10炔基，被羟基取代的C2-10炔基基团或C 1-4烷氧基或桥连环烃基，R 2是氢原子，C 1-10烷基或C 3-10环烷基，m是1至5的整数，n 是1〜4的整数，p为0,1或2，q为1〜5的整数，r为0,1或2。其药学上可接受的盐或其水合物在抑制血管平滑肌的生长中表现出优异的作用，并且可用作用于抑制经皮腔内冠状动脉成形术后再狭窄的药物。

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