Sleep inducing agent
    31.
    发明授权
    Sleep inducing agent 失效
    睡眠诱导剂

    公开(公告)号:US06395786B1

    公开(公告)日:2002-05-28

    申请号:US09701332

    申请日:2000-11-27

    IPC分类号: A01N3708

    摘要: A sleep-inducing preparation which comprises as an effective ingredient a prostaglandin derivative represented by the formula: wherein X is a halogen atom, Y is a group represented by (CH2)m, a cis-vinylene group or a phenylene group, Z is an ethylene group, a trans-vinylene group, OCH2 or S(O)nCH2, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C4-13 cycloalkylalkyl 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, m is an integer of 1 to 3, and n is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译: 一种睡眠诱导制剂,其包含作为有效成分的由下式表示的前列腺素衍生物:其中X是卤素原子,Y是由(CH 2)m表示的基团,顺式亚乙烯基或亚苯基,Z是 亚乙基,反亚乙烯基,OCH 2或S(O)n CH 2,R 1是C 3-10环烷基,被C 1-4烷基取代的C 3-10环烷基,C 4-13环烷基烷基, C5-10烷基,C5-10烯基,C5-10炔基或桥连环烃基,R2是氢原子,C1-10烷基或C3-10环烷基,m是 1〜3的整数,n为0,1或2,其药学上可接受的盐或其水合物。

    Substituted cyclopentene derivatives and method for preparing the same
    32.
    发明授权
    Substituted cyclopentene derivatives and method for preparing the same 失效
    取代的环戊烯衍生物及其制备方法

    公开(公告)号:US06191291B1

    公开(公告)日:2001-02-20

    申请号:US09456413

    申请日:1999-12-08

    申请人: Fumie Sato

    发明人: Fumie Sato

    IPC分类号: C07D30300

    摘要: A substituted cyclopentene derivative of the formula (VII): wherein R is a hydrogen atom, alkyl radical having 1 to 6 carbon atoms, alkenyl radical having 2 to 6 carbon atoms, alkynyl radical having 2 to 6 carbon atoms, cycloalkyl radical having 3 to 8 carbon atoms, aralkyl radical having 7 to 19 carbon atoms, aryl radical having 6 to 12 carbon atoms, alkoxy radical having 1 to 6 carbon atoms, alkenyloxy radical having 2 to 6 carbon atoms, alkylthio radical having 1 to 6 carbon atoms or alkenylthio radical having 2 to 6 carbon atoms; X1 is (&agr;-OZa, &bgr;-H) or (&agr;-H, &bgr;-OZa), X3 is (&agr;-OZd, &bgr;-H), (&agr;-H, &bgr;-OZd) or oxygen atom, each of Za and Zd, which may be the same or different, is a hydrogen atom or a protective radical for a hydroxyl radical.

    摘要翻译: 式(VII)的取代环戊烯衍生物:其中R是氢原子,具有1-6个碳原子的烷基,具有2-6个碳原子的烯基,具有2-6个碳原子的炔基,具有3-8个碳原子的环烷基 碳原子数为7〜19的芳烷基,碳原子数为6〜12的芳基,碳原子数1〜6的烷氧基,碳原子数2〜6的烯氧基,碳原子数1〜6的烷硫基,烯基硫基 具有2至6个碳原子; X1是(α-OZa,β-H)或(α-H,β-OZa),X3是(α-OZd,β-H),(α-H,β-OZd) 或氧原子,Za和Zd各自可以相同或不同,是氢原子或羟基的保护基。

    Substituted cyclopentene derivatives and method for preparing the same
    33.
    发明授权
    Substituted cyclopentene derivatives and method for preparing the same 失效
    取代的环戊烯衍生物及其制备方法

    公开(公告)号:US5874634A

    公开(公告)日:1999-02-23

    申请号:US894879

    申请日:1997-09-02

    申请人: Fumie Sato

    发明人: Fumie Sato

    摘要: A halogenated substituted cyclopentene derivative of formula (I): ##STR1## wherein R is a hydrogen atom, alkyl radical having 1-6 carbon atoms, alkenyl radical having 2-6 carbon atoms, alkynyl radical having 2-6 carbon atoms, cycloalkyl radical having 3-8 carbon atoms, aralkyl radical having 7-19 carbon atoms, aryl radical having 6-12 carbon atoms, alkoxy radical having 1-6 carbon atoms, alkenyloxy radical having 2-6 carbon atoms, alkylthio radical having 1-6 carbon atoms or alkenylthio radical having 2-6 carbon atoms; X.sup.1 is (.alpha.-OZ.sup.a, .beta.-H) or (.alpha.-H, .beta.-OZ.sup.a), X.sup.3 is (.alpha.-OZ.sup.d, .beta.-H), (.alpha.-H, .beta.-OZ.sup.d) or oxygen atom, each of Z.sup.a and Z.sup.d, which may be the same or different, is a hydrogen atom or a protective radical for a hydroxyl radical; and W is a halogen atom.

    摘要翻译: PCT No.PCT / JP96 / 00422 Sec。 371日期:1997年9月2日 102(e)1997年9月2日PCT PCT 1996年2月23日PCT公布。 WO96 / 26891 PCT出版物 日本1996年9月6日一种式(I)的卤代取代环戊烯衍生物:其中R是氢原子,具有1-6个碳原子的烷基,具有2-6个碳原子的烯基, 2-6个碳原子,具有3-8个碳原子的环烷基,具有7-19个碳原子的芳烷基,具有6-12个碳原子的芳基,具有1-6个碳原子的烷氧基,具有2-6个碳原子的烯氧基 具有1-6个碳原子的烷硫基或具有2-6个碳原子的烯基硫基; X1是(α-Za,β-H)或(α-H,β-OZa),X3是(α-Zd,β-H),(α-H,β-OZd)或氧原子 和Zd可以相同或不同,是氢原子或羟基的保护基; W是卤素原子。

    Prostaglandin E.sub.1 analogues
    34.
    发明授权
    Prostaglandin E.sub.1 analogues 失效
    前列腺素E1类似物

    公开(公告)号:US5583158A

    公开(公告)日:1996-12-10

    申请号:US416871

    申请日:1995-04-19

    IPC分类号: A61K31/557 C07C405/00

    CPC分类号: C07C405/0025 C07C405/0033

    摘要: A prostaglandin E.sub.1 analogue represented by formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; and X is an oxygen atom and R.sup.2 represents ##STR2## or X is a sulfur atom and R.sup.2 represents ##STR3## The compound has a strong and prolonged inhibitory action for platelet aggregation and is useful for treatment of various thrombotic diseases including peripheral circulatory disturbance.

    摘要翻译: PCT No.PCT / JP93 / 01510 Sec。 371日期1995年04月19日 102(e)日期1995年4月19日PCT提交1993年10月20日PCT公布。 公开号WO94 / 08961 日本1994年4月28日由式表示的前列腺素E1类似物,其中R1表示氢原子或C1-C6烷基; X是氧原子,R2表示或X是硫原子,R2代表血小板聚集的作用,可用于治疗各种血栓形成疾病,包括外周循环障碍。

    Optically active alcohols, process for producing the same, and process
for resolving the same
    36.
    发明授权
    Optically active alcohols, process for producing the same, and process for resolving the same 失效
    光学活性醇,其制备方法及其分离方法

    公开(公告)号:US5037855A

    公开(公告)日:1991-08-06

    申请号:US437886

    申请日:1989-11-17

    申请人: Fumie Sato

    发明人: Fumie Sato

    摘要: Provided herein is an optically active alcohol having a silyl group, stannyl group, or halogen atom at the .gamma.-position, selected from compounds represented by the general formula [I], ##STR1## the general formula [II], ##STR2## the general formula [III], ##STR3## and the general formula [IV], ##STR4## (where, R denotes a C.sub.1 -C.sub.10 substituted or unsubstituted alkyl group or substituted or unsubstituted phenyl group; A denotes a silyl group represented by ##STR5## a stannyl group represented by ##STR6## or a halogen atom. R.sup.1, R.sup.2, and R.sup.3 are substituted or unsubstituted C.sub.1 -C.sub.10 alkyl groups or substituted or unsubstituted phenyl group, which may be the same or different, provided that this does not apply in the case where A represents a stannyl group or halogen atom in the general formulas [III] and [IV].); a process for producing the same, and a process for resolving the optically active alcohol into isomers of high optical purity.

    Optically active alcohols and process for producing the same
    37.
    发明授权
    Optically active alcohols and process for producing the same 失效
    光学活性醇及其制备方法

    公开(公告)号:US4987236A

    公开(公告)日:1991-01-22

    申请号:US437885

    申请日:1989-11-17

    申请人: Fumie Sato

    发明人: Fumie Sato

    摘要: Provided herein is an optically active alcohol having a silyl group, stannyl group, or halogen atom at the .gamma.-position, selected from compounds represented by the general formula [I], ##STR1## the general formula [II], ##STR2## the general formula [III], ##STR3## and the general formula [IV], ##STR4## (where, R denotes a C.sub.1 -C.sub.10 substituted or unsubstituted alkyl group or substituted or unsubstituted phenyl group; A denotes a silyl group represented by ##STR5## a stannyl group represented by ##STR6## or a halogen atom, R.sup.1, R.sup.2, and R.sup.3 are substituted or unsubstituted C.sub.1 -C.sub.10 alkyl groups or substituted or unsubstituted phenyl group, which may be the same or different, provided that this does not apply in the case where A represents a stannyl group or halogen atom in the general formulas [III] and [IV].); a process for producing the same, and a process for resolving the optically active alcohol into isomers of high optical purity.

    Antipruritic agent
    40.
    发明申请
    Antipruritic agent 失效
    止痒剂

    公开(公告)号:US20050009917A1

    公开(公告)日:2005-01-13

    申请号:US10493693

    申请日:2003-08-07

    摘要: A pharmaceutical preparation for preventing or treating pruritic symptoms which contains as an effective ingredient a prostaglandin derivative represented by formula [1] wherein X1 and X2 which are different from each other represent a hydrogen atom, a halogen atom or a hydroxyl group; Y is an ethylene group, a vinylene group or an ethynylene group; Z is the formula (CH2)kA(CH2)hB(CH2)q, (CH2)kA(CH2)rA′(CH2)t (CH2)kB(CH2)hB′(CH2)q or (CH2)k-1B′(CH2)q-1A′wherein k is an integer of 1 to 4, h is an integer of 0 to 4, q is an integer 1 to 4, r is an integer of 0 to 4, and t is an integer of 0 to 2; A and A′ which may be the same or different represent an ethylene group, a vinylene group or an ethynylene group; B and B′ which may be the same or different represent an oxygen atom or a group represented by the formula S(O)u wherein u is an integer of 0 to 2; W1 is a hydroxyl group, a C1-10 alkyloxy group, a C3-10 cycloalkyloxy group, an aryloxy group or an arylalkyloxy group; W2 is a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, a C3-10 cycloalkyl group, a C1-5 alkyl group substituted by C3-10 cycloalkyl group(s), or a group represented by the formula wherein W4 is a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group or a C1-5 alkyl group substituted by C3-10 cycloalkyl group(s); v is an integer of 0 to 4; W3 is a hydrogen atom or a methyl group, or W3 when taken together with W2 and the adjacent carbon atom forms a C3-10 cycloalkyl group; m is 0 or 1, a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译: 用于预防或治疗瘙痒症状的药物制剂,其含有作为有效成分的由式[1]表示的前列腺素衍生物,其中X 1和X 2彼此不同,表示氢原子,卤素原子或 羟基; Y是亚乙基,亚乙烯基或亚乙炔基; Z是式(CH2)kA(CH2)hB(CH2)q,(CH2)kA(CH2)rA'(CH2)t(CH2)kB(CH2)hB'(CH2)q或(CH2) '(CH 2)q-1A'其中k为1〜4的整数,h为0〜4的整数,q为1〜4的整数,r为0〜4的整数,t为 0〜2; A和A'可以相同或不同,表示亚乙基,亚乙烯基或亚乙炔基; B和B'可以相同或不同,表示氧原子或由式S(O)u表示的基团,其中u为0-2的整数; W 1是羟基,C 1-10烷氧基,C 3-10环烷氧基,芳氧基或芳基烷氧基; W 2是C 1-10烷基,C 2-10烯基,C 2-10炔基,C 3-10环烷基,被C 3-10环烷基取代的C 1-5烷基, 或由下式表示的基团,其中W 4是C 1-10烷基,C 2-10烯基,C 2-10炔基或被C 3-10环烷基取代的C 1-5烷基, ; v为0〜4的整数; W 3为氢原子或甲基时,W 3与W 2一起形成,相邻碳原子形成C3-10环烷基; m为0或1,其药学上可接受的盐或其水合物。