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    .alpha.-methylenecyclopentanone derivative and process for producing the same
    1.
    发明授权
    .alpha.-methylenecyclopentanone derivative and process for producing the same 失效
    α-亚甲基环戊酮衍生物及其制备方法

    公开(公告)号：US5380900A

    公开(公告)日：1995-01-10

    申请号：US834348

    申请日：1992-02-12

    申请人： Fumie Sato ,  Kazutaka Arai ,  Katsuaki Miyaji

    发明人： Fumie Sato ,  Kazutaka Arai ,  Katsuaki Miyaji

    IPC分类号： C07C45/61 ,  C07C49/707 ,  C07C405/00 ,  C07F7/18 ,  C07F7/08 ,  C07F7/10

    CPC分类号： C07C405/00 ,  C07F7/1856 ,  Y02P20/55

    摘要： Disclosed herein is an .alpha.-methylene-cyclopentanone derivative represented by the formula [I] below which is useful as an intermediate for pharmaceuticals and insecticides, especially prostaglandins. Also disclosed herein is a process for producing the derivative advantageously on an industrial scale. ##STR1## where X denotes (.alpha.-OZ, .beta.-H) or (.alpha.-H, .beta.-OZ), with Z representing a protecting group for the hydroxyl group; U denotes (.alpha.-H, .beta.-R.sup.1) or (.beta.-R.sup.1, .alpha.-H); R.sup.1 denotes ##STR2## where R.sup.2 denotes a protected hydroxyl group, a substituted or unsubstituted C.sub.1-15 alkyl group, a substituted or unsubstituted C.sub.2-15 alkenyl group, a substituted or unsubstituted C.sub.2-15 alkynyl group, or a substituted or unsubstituted C.sub.6-15 aryl group; Z' denotes a protecting group for the hydroxyl group; and k is 0 or 1).

    摘要翻译： 本文公开了下式[I]表示的α-亚甲基 - 环戊酮衍生物，其可用作药物和杀虫剂，特别是前列腺素的中间体。 本文还公开了有利于工业规模生产衍生物的方法。 其中X表示（α-OZ，β-H）或（α-H，β-OZ），其中Z表示羟基的保护基; U表示（α-H，β-R1）或（β-R1，α-H）; R1表示，其中R2表示被保护的羟基，取代或未取代的C1-15烷基，取代或未取代的C2-15烯基，取代或未取代的C2-15炔基，或取代或未取代的C6- 15芳基; Z'表示羟基的保护基; k为0或1）。

    Preparation of cis—olefins
    7.
    发明授权
    Preparation of cis—olefins 失效
    顺式烯烃的制备

    公开(公告)号：US06333441B1

    公开(公告)日：2001-12-25

    申请号：US08026681

    申请日：1993-03-04

    申请人： Fumie Sato ,  Katsuaki Miyaji ,  Takehiro Amano

    发明人： Fumie Sato ,  Katsuaki Miyaji ,  Takehiro Amano

    IPC分类号： C07C505

    CPC分类号： C07D309/12 ,  C07B35/02 ,  C07B2200/09 ,  C07C5/09 ,  C07C29/17 ,  C07C51/36 ,  C07C69/007 ,  C07C2523/44 ,  C07F7/1892 ,  C07C33/03

    摘要： A cis-olefin of the formula: R1—CH═CH—R2 is prepared by reducing an alkyne of the formula: R1—C≡C—R2 with formic acid in the presence of a palladium catalyst. R1 and R2 are independently selected from the group consisting of a hydrogen atom, ester group, substituted silyl group, carboxyl group, cyano group, aliphatic C1-C20 hydrocarbon group, and phenyl group. The cis-olefin which is a useful intermediate for the synthesis of fine chemicals is selectively produced in high yields.

    摘要翻译： 通过在钯催化剂存在下用甲酸还原具有下式的R 1 -C = C-R 2的炔来制备下式的顺式烯烃：R1-CH = CH-R2。 R1和R2独立地选自氢原子，酯基，取代的甲硅烷基，羧基，氰基，脂族C1-C20烃基和苯基。 作为合成精细化学品的有用中间体的顺式烯烃以高产率选择性地生产。

    Prostaglandin derivatives
    9.
    发明申请
    Prostaglandin derivatives 审中-公开
    前列腺素衍生物

    公开(公告)号：US20060270740A1

    公开(公告)日：2006-11-30

    申请号：US10545785

    申请日：2004-02-19

    申请人： Fumie Sato ,  Tohru Tanami ,  Naoya Ono ,  Makoto Yagi ,  Takayuki Seki ,  Mariko Sato

    发明人： Fumie Sato ,  Tohru Tanami ,  Naoya Ono ,  Makoto Yagi ,  Takayuki Seki ,  Mariko Sato

    IPC分类号： A61K31/557

    CPC分类号： C07C405/0016

    摘要： A prostaglandin derivative represented by the formula (wherein X is a halogen atom; Y is ethylene group, vinylene group or ethylylene group; Z is a group represented by —(CH2)m, —O(CH2)n— or —S(O)p—(CH2)n— (m is an integer of 0 to 3; n is an integer of 0 to 2; and p is an integer of 0 to 2); R1 is a hydrogen atom, a C1-5 alkyl group or a substituted C1-5 alkyl group; R2 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted by C1-4 alkyl group or C4-15 cycloalkylalkyl group; and R3 is a hydrogen atom, a halogen atom or a C1-5 alkyl group or a substituted C1-5 alkyl group), a pharmaceutically acceptable salt thereof or a hydrate thereof which has an excellent antagonism to prostaglandin DP receptor and, therefore, is useful against diseases such as allergic rhinitis, nasal obstruction, asthma, allergic conjunctivitis, systemic mastocytosis and disorder of systemic mast cell activation.

    摘要翻译： 由式（其中X是卤素原子; Y是亚乙基，亚乙烯基或亚乙基）表示的前列腺素衍生物; Z是由 - （CH 2 CH 2）m表示的基团， （CH 2）n - 或 - （CH 2）n - （CH 2）n - ）n（m为0〜3的整数，n为0〜2的整数，p为0〜2的整数），R 1〜 氢原子，C 1-5烷基或取代的C 1-5烷基; R 2是C 1 -C 6烷基， 3-10个环烷基，被C 1-4烷基取代的C 3-10环烷基或C 1-4 - >环烷基烷基; R 3是氢原子，卤素原子或C 1-5烷基或取代的C 1-5 - >烷基），其药学上可接受的盐或其水合物，其对前列腺素DP受体具有优异的拮抗作用，因此可用于治疗过敏性鼻炎，鼻塞 离子，哮喘，过敏性结膜炎，全身肥大细胞增多症和系统性肥大细胞活化紊乱。

    Prostaglandin E1 derivatives
    10.
    发明授权
    Prostaglandin E1 derivatives 失效
    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。