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：

公开(公告)号：US4024174A

公开(公告)日：1977-05-17

申请号：US534509

申请日：1964-12-19

申请人： Masaki Hayashi ,  Seiji Kori ,  Hirohisa Wakatsuka ,  Yoshitaka Konishi

发明人： Masaki Hayashi ,  Seiji Kori ,  Hirohisa Wakatsuka ,  Yoshitaka Konishi

IPC分类号： C07C405/00 ,  C07D307/20 ,  C07D309/12 ,  C07C177/00

CPC分类号： C07D307/20 ,  C07C405/00 ,  C07D309/12 ,  Y10S514/825

摘要： Trans-.DELTA..sup.2 -prostaglandin compounds are disclosed of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## R.sup.1 represents an alkyl group containing from 1 to 10 carbon atoms, or an alkyl group containing from 1 to 6 carbon atoms carrying a phenyl substituent or a cycloalkyl substituent of 5 to 7 carbon atoms, R.sup.2 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, and R.sup.3.sup.' represents a hydrogen atom or an alkyl group containing from 1 to 12 carbon atoms, the double bonds in the 2- and 5-positions being in the trans- and cis-configurations respectively. These compounds are indicated in the management of conditions such as autoimmune conditions, e.g. rheumatoid arthritis.

摘要翻译： Trans-DELTA 2-前列腺素化合物公开于下列通式：其中A代表下式的基团：其中R 1表示含有1至10个碳原子的烷基，或 含有1〜6个碳原子的烷基，带有苯基取代基或5〜7个碳原子的环烷基取代基，R2表示氢原子或含1〜4个碳原子的烷基，R3'表示氢原子 或含有1至12个碳原子的烷基，2位和5位的双键分别为反式和顺式构型。 这些化合物在诸如自身免疫病症例如自身免疫病症的条件的管理中表示。 类风湿关节炎。

公开(公告)号：US4052512A

公开(公告)日：1977-10-04

申请号：US646316

申请日：1976-01-05

申请人： Masaki Hayashi ,  Seiji Kori ,  Hirohisa Wakatsuka

发明人： Masaki Hayashi ,  Seiji Kori ,  Hirohisa Wakatsuka

IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P13/02 ,  A61P15/00 ,  C07C67/00 ,  C07C391/02 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00 ,  A61K31/19 ,  A61K31/215

CPC分类号： C07C391/02 ,  C07C405/00 ,  C07C405/0025

摘要： New trans-.DELTA..sup.2 -prostaglandins of the formula ##STR1## (wherein R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, R.sup.2 represents a 1,1-dimethyl-pentyl group or a 2-ethylheptyl group, the wavy line indicates attachment of the depicted group in .alpha.-configuration or racemic form consisting of equimolecular mixtures of .alpha.-configuration and .beta.-configuration and the C.sub.2 -C.sub.3 and C.sub.13 -C.sub.14 double bonds are trans), which are useful for the treatment of hypertension, contraception menstrual regulation.

公开(公告)号：US4313954A

公开(公告)日：1982-02-02

申请号：US122704

申请日：1980-02-19

申请人： Hirohisa Wakatsuka ,  Masaki Hayashi ,  Yoshitaka Konishi

发明人： Hirohisa Wakatsuka ,  Masaki Hayashi ,  Yoshitaka Konishi

IPC分类号： A61K31/557 ,  A61P7/02 ,  A61P43/00 ,  C07C405/00 ,  C07D209/52 ,  A61K31/40

CPC分类号： C07C405/0041 ,  C07C405/00 ,  C07D209/52

摘要： Prostaglandin I.sub.2 analogues of the general formula ##STR1## [wherein R.sup.1 represents a hydrogen atom, an alkyl group containing from 1 to 12 carbon atoms, an aralkyl group containing from 7 to 13 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, a phenyl group unsubstituted or substituted by at least one halogen atom, trifluoromethyl or phenyl group, or by at least one alkyl, alkoxy or alkylthio group containing from 1 to 4 carbon atoms, or represents a group --C.sub.m H.sub.2m COOR.sup.6, --C.sub.n H.sub.2n OR.sup.7 or ##STR2## in which m represents an integer of 1 to 12, n represents an integer of 2 to 12, R.sup.6, R.sup.8 and R.sup.9, which may be the same or different, each represent an alkyl group containing from 1 to 4 carbon atoms, and R.sup.7 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents an alkyl group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.5 represents an alkyl group containing from 1 to 10 carbon atoms, Y represents ethylene or trans-vinylene, the hydroxy group attached to the C-11 carbon atom is in .alpha.-configuration, and the wavy line attached to the C-15 carbon atom is in .alpha.- or .beta.-configuration or a mixture thereof] and non-toxic acid addition salts thereof and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof are new compounds possessing pharmacological properties typical of the prostaglandins.

摘要翻译： 具有通式的前列腺素I2类似物[其中R1表示氢原子，含有1至12个碳原子的烷基，含有7至13个碳原子的芳烷基，含有4至7个碳原子的环烷基 未取代或被至少一个含有1至4个碳原子的烷基取代的苯基，未被取代或被至少一个卤素原子取代的苯基，三氟甲基或苯基，或至少一个含有1至4个碳原子的烷基，烷氧基或烷硫基 4个碳原子，或表示基团-C m H 2 mCOOR 6，-C n H 2n OR 7或其中m表示1至12的整数，n表示2至12的整数，R 6，R 8和R 9可以相同或不同 各自表示含有1至4个碳原子的烷基，R 7表示氢原子或含有1至4个碳原子的烷基，R 2表示氢原子或甲基或乙基，R 3表示含有 从1 至4个碳原子，R 4表示氢原子或含有1至4个碳原子的烷基，R 5表示含有1至10个碳原子的烷基，Y表示亚乙基或反式亚乙烯基， C-11碳原子为α-构型，连接至C-15碳原子的波浪线为α-或β-构型或其混合物）及其无毒的酸加成盐，当R1表示 氢原子，其无毒盐是具有典型的前列腺素的药理学性质的新化合物。

公开(公告)号：US4367237A

公开(公告)日：1983-01-04

申请号：US097675

申请日：1979-11-27

申请人： Hirohisa Wakatsuka ,  Katsuichi Shimoji ,  Sadahiko Iguchi ,  Yoshitaka Konishi ,  Hisashi Suga ,  Yasuyuki Miyata ,  Yoichi Iguchi ,  Hajimu Miyake ,  Masaki Hayashi

发明人： Hirohisa Wakatsuka ,  Katsuichi Shimoji ,  Sadahiko Iguchi ,  Yoshitaka Konishi ,  Hisashi Suga ,  Yasuyuki Miyata ,  Yoichi Iguchi ,  Hajimu Miyake ,  Masaki Hayashi

IPC分类号： C07C405/00 ,  C07D333/78 ,  C07D335/04 ,  A61K31/38

CPC分类号： C07C405/0033 ,  C07C405/00 ,  C07D333/78 ,  C07D335/04

摘要： Prostaglandin analogues of the general formula: ##STR1## [wherein the ring A represents: ##STR2## the ring B represents: ##STR3## (wherein R.sup.6 represents hydrogen, methyl or ethyl, and r is zero, one or two), Y represents ethylene, cis- or trans-vinylene or ethynylene, Z represents a grouping of the formula: --(CH.sub.2).sub.m --, --(CH.sub.2).sub.3 --CHR.sup.7 --, --(CH.sub.2).sub.2 --CHR.sup.7 --CH.sub.2 --, --CH.sub.2 --CHR.sup.7 --(CH.sub.2).sub.2 --, --CHR.sup.7 --(CH.sub.2).sub.3 --, or trans--(CH.sub.2).sub.2 --CH.dbd.CH-- (wherein m is 3, 4 or 5, and R.sup.7 represents methyl or ethyl), R.sup.1 represents a grouping of the formula: --COOR.sup.8, ##STR4## or --CH.sub.2 OR.sup.11 (wherein R.sup.8 represents hydrogen, alkyl, aralkyl, cycloalkyl which is unsubstituted or substituted by at least one alkyl group, or R.sup.8 represents phenyl which is unsubstituted or substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkylthio or phenyl, or represents naphthyl, 2,3- or 1,3-dihydroxypropyl, 2,3- or 1,3-bisalkanoyloxypropyl, a grouping of the formula: -D.sub.1 --COOR.sup.12, ##STR5## -D.sub.2 -R.sup.15 or -D.sub.3 -R.sup.16, wherein D.sub.1 represents alkylene, D.sub.2 represents alkylene, D.sub.3 represents a single bond or alkylene, R.sup.12, R.sup.13 and R.sup.14, each represent alkyl, R.sup.15 represents hydroxy, alkoxy or alkylthio and R.sup.16 represents a heterocyclic ring, or R.sup.8 represents a grouping of the formula: ##STR6## R.sup.9 and R.sup.10, each represent hydrogen, alkyl, alkylsulphonyl, alkanoyl or ##STR7## represents a heterocyclic ring, and R.sup.11 represents hydrogen or alkanoyl, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond or alkylene, R.sup.4 represents hydrogen, alkyl, alkoxy, cycloalkyl or cycloalkyloxy unsubstituted or substituted by alkyl, or represents phenyl or phenoxy unsubstituted or substituted by halogen, trifluoromethyl or alkyl with the proviso that, when R.sup.3 represents a single bond, R.sup.4 does not represent alkoxy, cycloalkyloxy or phenoxy, R.sup.5 represents hydrogen, methyl or ethyl and with the proviso that, when one of the groups R.sup.5, R.sup.6 and R.sup.7 represents methyl or ethyl the other two groups are hydrogen atoms] and cyclodextrin clathrates, non-toxic salts and non-toxic acid addition salts thereof, possess selective strong stimulatory activity on uterine contraction in female mammals.

公开(公告)号：US4399147A

公开(公告)日：1983-08-16

申请号：US872635

申请日：1978-01-26

申请人： Masaki Hayashi ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hirohisa Wakatsuka ,  Hiroyuki Ito

发明人： Masaki Hayashi ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hirohisa Wakatsuka ,  Hiroyuki Ito

IPC分类号： C07D307/935 ,  A61K31/34 ,  A61K31/343 ,  A61P43/00 ,  C07C405/00 ,  C07D307/937 ,  A61K31/557

CPC分类号： C07D307/937 ,  C07C405/00

摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein X represents trans-vinylene or an ethylene group unsubstituted or substituted by a bromine atom at the C-5 position, Y represents trans-vinylene or ethylene, R.sup.1 represents hydrogen or an alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents hydrogen or methyl or ethyl, R.sup.3 represents a single bond or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents hydrogen, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or a phenyl or phenoxy group unsubstituted or carrying at least one substituent selected from halogen atoms, the trifluoromethyl group and alkyl groups containing from 1 to 3 carbon atoms, and the wavy line attached to the carbon atoms in positions 6, 11 and 15 depicted in the formula represents .alpha.- or .beta.-configuration or mixtures thereof] are new compounds possessing pharmacological properties typical of prostaglandins, for example PGI.sub.2, and are more stable than PGI.sub.2.

摘要翻译： 前列腺素I2类似物，具有下式：其中X表示反式亚乙烯基或未被取代或被C-5位上的溴原子取代的亚乙基，Y表示反式亚乙烯基或亚乙基，R 1表示氢或烷基 含有1至12个碳原子，R 2表示氢或甲基或乙基，R 3表示单键或含有1至4个碳原子的亚烷基，R 4表示氢，含有1至8个碳原子的烷基，环烷基 含有未取代或被至少一个含有1至8个碳原子的烷基取代的4至7个碳原子的基团，或未取代或携带至少一个选自卤素原子的取代基的苯基或苯氧基，三氟甲基和含有 1至3个碳原子，并且连接在式中描述的6,11和15位的碳原子上的波浪线代表α-或β-构型或其混合物] 是具有典型的前列腺素的药理学性质的新化合物，例如PGI 2，并且比PGI2更稳定。

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。

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。

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。

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。