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    15-Cycloalkyl-prostaglandin derivatives
    1.
    发明授权
    15-Cycloalkyl-prostaglandin derivatives 失效
    15-环烷基 - 前列腺素衍生物

    公开(公告)号：US4180675A

    公开(公告)日：1979-12-25

    申请号：US857341

    申请日：1977-12-05

    申请人： Masaki Hayashi ,  Seiji Kori ,  Isao Ohyama ,  Sadahiko Iguchi ,  Takanori Okada

    发明人： Masaki Hayashi ,  Seiji Kori ,  Isao Ohyama ,  Sadahiko Iguchi ,  Takanori Okada

    IPC分类号： C07C405/00 ,  C07D309/12 ,  C07F9/40 ,  C08B37/00 ,  C07C177/00

    CPC分类号： C08B37/0015 ,  C07C405/00 ,  C07D309/12 ,  C07F9/4006

    摘要： The present invention relates to 15-cycloalkyl-prostaglandins of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 represents a hydrogen atom or a methyl or ethyl group, R.sup.2 represents a straight- or branched-chain alkyl group containing from 2 to 8 carbon atoms or a phenyl group unsubstituted or substituted by an alkyl group containing from 1 to 3 carbon atoms, R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 3 carbon atoms, and n represents 4 or 5 and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, non-toxic salts thereof.These new compounds exhibit characteristic prostaglandin-like activities.

    摘要翻译： 本发明涉及下式的15-环烷基 - 前列腺素：其中A表示下式的基团：W表示亚乙基或反式亚乙烯基，X表示亚乙基或顺式亚乙烯基，Y表示亚乙基或反式亚乙烯基 - 亚乙烯基，R表示氢原子或含有1至12个碳原子的直链或支链烷基，R1表示氢原子或甲基或乙基，R2表示直链或支链烷基， 2至8个碳原子的苯基或未被取代或被含有1至3个碳原子的烷基取代的苯基，R 3表示氢原子或含有1至3个碳原子的直链或支链烷基，n 代表这些酸和酯的4或5和环糊精包合物，当R代表氢原子时，其无毒性盐。 这些新化合物表现出特征性的前列腺素样活性。

    15-Cycloalkyl-prostaglandin derivatives
    2.
    发明授权
    15-Cycloalkyl-prostaglandin derivatives 失效
    15-环烷基 - 前列腺素衍生物

    公开(公告)号：US4087620A

    公开(公告)日：1978-05-02

    申请号：US703158

    申请日：1976-07-07

    申请人： Masaki Hayashi ,  Seiji Kori ,  Isao Ohyama ,  Sadahiko Iguchi ,  Takanori Okada

    发明人： Masaki Hayashi ,  Seiji Kori ,  Isao Ohyama ,  Sadahiko Iguchi ,  Takanori Okada

    IPC分类号： A61K31/557 ,  A61K31/19 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D309/12 ,  C07F9/40 ,  C08B37/00 ,  C07C177/00

    CPC分类号： C07F9/4018 ,  C07C405/00 ,  C07D309/12 ,  C08B37/0015

    摘要： The present invention relates to 15-cycloalkyl-prostaglandins of the formula: ##STR1## WHEREIN A represents a grouping of the formula: ##STR2## W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 represents a hydrogen atom or a methyl or ethyl group, R.sup.2 represents a straight- or branched-chain alkyl group containing from 2 to 8 carbon atoms or a phenyl group unsubstituted or substituted by an alkyl group containing from 1 to 3 carbon atoms, R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 3 carbon atoms, and n represents 4 or 5) and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, non-toxic salts thereof.These new compounds exhibit characteristic prostaglandin-like activities.

    摘要翻译： 本发明涉及下式的15-环烷基 - 前列腺素：其中A表示下式的基团：W表示亚乙基或反 - 亚乙烯基，X表示亚乙基或顺式 - 亚乙烯基，Y表示亚乙基或反式 - 亚乙烯基，R表示氢原子或含有1至12个碳原子的直链或支链烷基，R1表示氢原子或甲基或乙基，R2表示直链或支链烷基， 2至8个碳原子的苯基或未被取代或被含有1至3个碳原子的烷基取代的苯基，R 3表示氢原子或含有1至3个碳原子的直链或支链烷基，n 代表4或5）和这些酸和酯的环糊精包合物，当R代表氢原子时，其无毒性盐。

    .DELTA..sup.3 -Prostaglandin analogs
    5.
    发明授权
    .DELTA..sup.3 -Prostaglandin analogs 失效
    {66 {HU 3 {B-前列腺素类似物

    公开(公告)号：US4165437A

    公开(公告)日：1979-08-21

    申请号：US934444

    申请日：1978-08-17

    申请人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

    发明人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

    IPC分类号： C07C405/00 ,  C07D309/12 ,  C08B37/00 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07D309/12 ,  C08B37/0015

    摘要： The present invention relates to prostaglandin analogues of the general formula: ##STR1## [wherein X represents cis or trans-vinylene or ethylene, R represents ##STR2## R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents a hydrogen atom or a methyl group, R.sup.3 represents a straight- or branched-chain alkylene group containing from 1 to 7 carbon atoms and R.sup.4 represents a cycloalkyl group containing from 5 to 7 carbon atoms, a grouping of the formula: ##STR3## (wherein R.sup.5 and R.sup.6, which may be the same or different, each represent a hydrogen atom or halogen atom, a trifluoromethyl group or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms), or a grouping of the formula: ##STR4## (wherein R.sup.5 and R.sup.6 are as hereinbefore defined), or R.sup.3 and R.sup.4 together represent a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, and (1) the double bond between C.sub.3 -C.sub.4 is trans or cis, or trans and cis, when X is cis-vinylene or ethylene, and (2) the double bond between C.sub.3 -C.sub.4 is trans, when X is trans-vinylene, and the double bond between C.sub.13 -C.sub.14 is trans] and cyclodextrin clathrates of such acids and esters, and when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, which exhibit characteristic prostaglandin-like activities.

    摘要翻译： 本发明涉及以下通式的前列腺素类似物：其中X表示顺式或反式亚乙烯基或亚乙基，R表示R 1表示氢原子或含有1个直链或支链烷基的直链或支链烷基 至12个碳原子，R 2表示氢原子或甲基，R 3表示含有1至7个碳原子的直链或支链亚烷基，R 4表示含有5至7个碳原子的环烷基， 式（其中R5和R6可以相同或不同，分别表示氢原子或卤原子，三氟甲基或含有1至4个碳原子的直链或支链烷基） ，或下式的分组：其中R 5和R 6如上所定义，或者R 3和R 4一起表示含有1至10个碳原子的直链或支链烷基，和（1） C3-C4之间的双键是反式或顺式，或 反式和顺式，当X为顺式 - 亚乙烯基或亚乙基时，和（2）当X为反式亚乙烯基时，C 3 -C 4之间的双键为反式，C13-C14之间的双键为反式]和环糊精包合物 酸和酯，当R1代表氢原子时，其无毒性盐显示出特征性的前列腺素样活性。

    .DELTA..sup.3 -Prostaglandin analogs
    6.
    发明授权
    .DELTA..sup.3 -Prostaglandin analogs 失效
    {66 {HU 3 {B-前列腺素类似物

    公开(公告)号：US4145555A

    公开(公告)日：1979-03-20

    申请号：US774828

    申请日：1977-03-07

    申请人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

    发明人： Masaki Hayashi ,  Seiji Kori ,  Yoshinobu Arai ,  Takanori Okada ,  Yoshitaka Konishi

    IPC分类号： A61K31/23 ,  A61K9/48 ,  A61K31/557 ,  A61K31/5575 ,  A61K31/70 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D309/12 ,  C08B37/00 ,  C08B37/16 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07D309/12 ,  C08B37/0015

    摘要： The present invention relates to prostaglandin analogues of the general formula: ##STR1## �wherein X represents cis or trans-vinylene or ethylene, Z represents ##STR2## R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents a hydrogen atom or a methyl group, R.sup.3 represents a straight- or branched-chain alkylene group containing from 1 to 7 carbon atoms and R.sup.4 represents a cycloalkyl group containing from 5 to 7 carbon atoms, a grouping of the formula: ##STR3## (wherein R.sup.5 and R.sup.6, which may be the same or different, each represent a hydrogen atom or halogen atom, a trifluoromethyl group or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms), or a grouping of the formula: ##STR4## (wherein R.sup.5 and R.sup.6 are as hereinbefore defined), or R.sup.3 and R.sup.4 together represent a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, and (1) the double bond between C.sub.3 -C.sub.4 is trans or cis, or trans and cis, when X is cis-vinylene or ethylene, and (2) the double bond between C.sub.3 -C.sub.4 is trans, when X is trans-vinylene, and the double bond between C.sub.13 -C.sub.14 is trans! and cyclodextrin clathrates of such acids and esters, and when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, which exhibit characteristic prostaglandin-like activities.

    摘要翻译： 本发明涉及以下通式的前列腺素类似物：其中X表示顺式或反式亚乙烯基或亚乙基，Z表示R 1表示氢原子或含有1个或更多个的直链或支链烷基 至12个碳原子，R 2表示氢原子或甲基，R 3表示含有1至7个碳原子的直链或支链亚烷基，R 4表示含有5至7个碳原子的环烷基， 式（其中R5和R6可以相同或不同，分别表示氢原子或卤原子，三氟甲基或含有1至4个碳原子的直链或支链烷基） ，或下式的分组：其中R 5和R 6如上所定义，或者R 3和R 4一起表示含有1至10个碳原子的直链或支链烷基，和（1） C3-C4之间的双键是反式或顺式，或 反式和顺式，当X为顺式 - 亚乙烯基或亚乙基时，和（2）当X为反式亚乙烯基时，C 3 -C 4之间的双键为反式，C13-C14之间的双键为反式]和环糊精包合物 酸和酯，当R1代表氢原子时，其无毒性盐显示出特征性的前列腺素样活性。

    16-Phenoxy and phenylthio prostaglandin derivatives
    7.
    发明授权
    16-Phenoxy and phenylthio prostaglandin derivatives 失效
    16-苯氧基和苯硫基前列腺素衍生物

    公开(公告)号：US4065632A

    公开(公告)日：1977-12-27

    申请号：US713941

    申请日：1976-08-12

    申请人： Masaki Hayashi ,  Seiji Kori ,  Hajimu Miyake ,  Takanori Okada

    发明人： Masaki Hayashi ,  Seiji Kori ,  Hajimu Miyake ,  Takanori Okada

    IPC分类号： A61K31/12 ,  A61K31/19 ,  A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07F9/40 ,  C07C69/76

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0016 ,  C07C405/0025 ,  C07C405/0033 ,  C07D309/12 ,  C07F9/4006 ,  Y10S514/822 ,  Y10S514/826 ,  Y10S514/869 ,  Y10S514/927

    摘要： The present invention relates to compounds of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## B represents an oxygen or sulphur atom, R.sup.1 and R.sup.2, which may be the same or different, each represent a hydrogen or halogen atom, a trifluoromethyl group, or a straight- or branched-chain alkyl or alkoxy group containing from 1 to 4 carbon atoms, R represents a group of the formula --COOR.sup.3, in which R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, or a group of the formula --CH.sub.2 OR.sup.4, in which R.sup.4 represents a hydrogen atom or an alkylcarbonyl group containing from 2 to 5 carbon atoms and the double bonds depicted in positions C.sub.2 -C.sub.3, C.sub.5 -C.sub.6 and C.sub.13 -C.sub.14 are trans, cis and trans respectively, the cyclodextrin clathrates thereof and, when R.sup.3 in the group --COOR.sup.3 represents a hydrogen atom, non-toxic salts thereof. These compounds exhibit characteristics of prostaglandin-like activity.

    摘要翻译： 本发明涉及下式的化合物：其中A表示下式的基团：IV B表示氧或硫原子，R 1和R 2可以是 相同或不同，各自表示氢或卤素原子，三氟甲基或含有1至4个碳原子的直链或支链烷基或烷氧基，R表示式-COOR 3的基团，其中R 3 表示氢原子或含有1至12个碳原子的直链或支链烷基，或式-CH 2OR 4基团，其中R 4表示氢原子或含有2至5个碳原子的烷基羰基， 位置C2-C3，C5-C6和C13-C14中所示的双键分别是反式，顺式和反式，环糊精包合，当-COOR3基团中的R3表示氢原子时，其无毒盐。 这些化合物表现出前列腺素样活性的特征。

    20-Hydroxy-prostaglandins
    8.
    发明授权
    20-Hydroxy-prostaglandins 失效
    20-羟基 - 前列腺素

    公开(公告)号：US4140712A

    公开(公告)日：1979-02-20

    申请号：US547293

    申请日：1975-02-05

    申请人： Masaki Hayashi ,  Seiji Kori ,  Hajimu Miyake

    发明人： Masaki Hayashi ,  Seiji Kori ,  Hajimu Miyake

    IPC分类号： C07D317/72 ,  B01J31/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07F9/40 ,  C07C177/00

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07D309/12 ,  C07F9/4006 ,  Y10S514/826 ,  Y10S514/929 ,  Y10S514/957 ,  Y10S514/962

    摘要： The present invention relates to 20-hydroxy prostaglandins of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## and X represents ethylene or cis-vinylene and Y represents trans-vinylene, or X and Y each represent ethylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 , R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or a methyl or ethyl group, and n represents zero or an integer from 1 to 3 inclusive, and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, the non-toxic salts thereof.These compounds exhibit characteristic prostaglandin activity.

    摘要翻译： 本发明涉及下式的20-羟基前列腺素：其中A代表下式的组：其中X表示亚乙基或顺式 - 亚乙烯基，Y表示反式亚乙烯基，或X和Y各自表示 乙烯，R表示氢原子或含有1至12个碳原子的直链或支链烷基，可以相同或不同的R 1，R 2，R 3，R 4和R 5各自表示氢原子或 甲基或乙基，n表示0或1〜3的整数，以及这些酸和酯的环糊精包合物，当R表示氢原子时，为无毒性盐。

    Dithio prostaglandin derivatives
    9.
    发明授权
    Dithio prostaglandin derivatives 失效
    Dithio前列腺素衍生物

    公开(公告)号：US4110341A

    公开(公告)日：1978-08-29

    申请号：US765580

    申请日：1977-02-04

    申请人： Masaki Hayashi ,  Seiji Kori ,  Hajimu Miyake

    发明人： Masaki Hayashi ,  Seiji Kori ,  Hajimu Miyake

    IPC分类号： A61K31/23 ,  A61K31/215 ,  A61K31/385 ,  A61K31/70 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07D339/04 ,  C08B37/16

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0033 ,  C07D309/12 ,  C07D339/04

    摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R.sup.1 represents a straight- or branched-chain alkyl group containing from 4 to 10 carbon atoms, and R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms and cyclodextrin clathrates of such acids and esters and, when R.sup.2 represents a hydrogen atom, non-toxic salts thereof, the bonds attaching the epidithio radical to the carbon atoms in the 9- and 11-positions in the grouping of formula VA being either botn in .alpha.-configuration or both in .beta.-configuration are disclosed.These compounds exhibit characteristic prostaglandin properties.

    摘要翻译： （IV）的前列腺素类似物：其中A表示下式的基团：（VI）或（IMA）（VB）X表示亚乙基或顺式亚乙烯基，Y表示亚乙基或反式亚乙烯基， R1表示含有4至10个碳原子的直链或支链烷基，R2表示氢原子或含有1至12个碳原子的直链或支链烷基和这些酸和酯的环糊精包合物 并且当R2表示氢原子时，其无毒盐，附加硫代自由基与式VA组中9-和11位中的碳原子的键或者是以α-构型或两者均为β - 配置。

    Trans-.DELTA..sup.2 -prostaglandins
    10.
    发明授权
    Trans-.DELTA..sup.2 -prostaglandins 失效
    Trans- {66 {hu 2 {b-前列腺素

    公开(公告)号：US3931296A

    公开(公告)日：1976-01-06

    申请号：US427403

    申请日：1973-12-21

    申请人： Masaki Hayashi ,  Hirohisa Wakatsuka ,  Seiji Kori

    发明人： Masaki Hayashi ,  Hirohisa Wakatsuka ,  Seiji Kori

    IPC分类号： C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07F9/40 ,  C07F9/54 ,  C07C61/38 ,  C07C69/74

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0025 ,  C07D309/12 ,  C07F9/4006 ,  C07F9/5407 ,  Y10S514/927

    摘要： New process for the preparation of trans-.DELTA..sup.2 -prostaglandins of the formula ##SPC1##(wherein A represents a grouping of the PGE, PGF or PGA type, X represents --CH.sub.2 CH.sub.2 -- or trans --CH=CH--, R.sub.1 represents an alkyl radical of 1 to 10 carbon atoms or an alkyl radical of 1 to 6 carbon atoms carrying a phenyl substituent or a cycloalkyl substituent of 5 to 7 carbon atoms, R.sub.2 represents a hydrogen atom or an alkyl radical of 1 to 4 carbon atoms) and alkyl esters thereof having 1 to 10 carbon atoms in the chain, which comprises reacting a cyclopentane derivative of the formula: ##SPC2##(where R.sub.3 represents a 2-tetrahydropyranyl group unsubstituted or substituted by at least one alkyl radical, or a 1-ethoxyethyl group) with an alkyl phosphonate of the general formula: ##EQU1## (wherein R.sub.4 represents a methyl or ethyl radical, and R.sub.5 represents an alkyl radical of 1 to 10 carbon atoms), optionally hydrolyzing the resulting trans-.DELTA..sup.2 -prostaglandin ester of the general formula: ##SPC3##To the corresponding acid, optionally converting the 9.alpha.-hydroxy radical in the ester or acid product to an oxo group, and hydrolyzing the tetrahydropyranyloxy or ethoxyethoxy groups in the resulting trans-.DELTA..sup.2 -prostaglandin compound of the formula: ##SPC4##(wherein R.sub.6 represents a hydrogen atom or an alkyl radical of 1 to 10 carbon atoms, Z represents ##EQU2## or C=O) to hydroxy radicals to obtain a trans-.DELTA..sup.2 -PGF or trans-.DELTA..sup.2 -PGE compound of the formula: ##SPC5##And, if desired, converting the PGE alicyclic ring (Z represents C=O) into that of a PGA compound.The trans-.DELTA..sup.2 -prostaglandin products, which are new compounds except for trans-.DELTA..sup.2 -PGE.sub.1, possess typical pharmacological properties of the `natural` prostaglandins.

    摘要翻译： 用于制备下式的转DELTA 2-前列腺素的新方法（WHEREIN A代表PGE，PGF或PGA类型的一组，X表示-CH 2 CH 2 - 或反-CH = CH-，R 1表示1的烷基 至10个碳原子或1至6个碳原子的烷基，带有苯基取代基或5至7个碳原子的环烷基取代基，R2表示氢原子或1至4个碳原子的烷基）及其烷基酯，其具有 1至10个碳原子的链，其包括使下式的环戊烷衍生物：