专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US3931296A Trans-.DELTA..sup.2 -prostaglandins 失效
标题翻译： 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：

2. 发明授权

US4024174A Tranes-delta 2-prostaglandins 失效
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。

3. 发明授权

US4052512A Prostaglandin analogues 失效
标题翻译： PROSTAGLANDIN ANALOGUES
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.

4. 发明授权

US3966792A Prostaglandin compounds 失效
标题翻译：前列腺素化合物
公开(公告)号：US3966792A
公开(公告)日：1976-06-29
申请号：US446241
申请日：1974-02-27
申请人： Masaki Hayashi , Seiji Kori , Isao Ohyama , Hirofumi Endo
发明人： Masaki Hayashi , Seiji Kori , Isao Ohyama , Hirofumi Endo
IPC分类号： C07C67/00 , C07C401/00 , C07C405/00 , C07C61/38 , C07C69/74
CPC分类号： C07C405/0016 , C07C405/00 , Y10S514/822 , Y10S514/824 , Y10S514/826 , Y10S514/869 , Y10S514/926 , Y10S514/927
摘要： New prostaglandin analogues having therapeutic utility of the formula: ##SPC1##(wherein B is a grouping of the formula: ##SPC2##X is --CH.sub.2 CH.sub.2 -- or cis --CH=CH--, Y is trans --CH=CH-- or, when X is --CH.sub.2 CH.sub.2 --, Y is additionally --CH.sub.2 CH.sub.2 --, A is alkyl of 1 through 3 carbon atoms, n is 4 or 5, and indicates attachment of the hydroxy radical to the carbon atom in alpha or beta configuration), and alkyl esters thereof, and cyclodextrin clathrates of such acids and esters, and non-toxic salts of such acids.
摘要翻译：具有下列治疗效用的新型前列腺素类似物：

5. 发明授权

US4140712A 20-Hydroxy-prostaglandins 失效
标题翻译： 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。

6. 发明授权

US4110341A Dithio prostaglandin derivatives 失效
标题翻译： 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。

7. 发明授权

US4195182A Trans-.DELTA..sup.2 -prostaglandin analogues 失效
标题翻译：经DELTA 2前列腺素类似物
公开(公告)号：US4195182A
公开(公告)日：1980-03-25
申请号：US824384
申请日：1977-08-12
申请人： Masaki Hayashi , Seiji Kori , Takanori Okada
发明人： Masaki Hayashi , Seiji Kori , Takanori Okada
IPC分类号： C08B37/16 , A61K31/19 , A61K31/715 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0033
摘要： This invention relates to prostaglandin analogues of the formula: ##STR1## (wherein R represents a hydrogen atom or a methyl group, and the double bonds between C.sub.2 -C.sub.3 and C.sub.13 -C.sub.14 are trans) and cyclodextrin clathrates of such compounds and, when R represents a hydrogen atom, non-toxic salts thereof, which possess characteristic prostaglandin-like activity.
摘要翻译：本发明涉及下式的前列腺素类似物：其中R表示氢原子或甲基，C2-C3和C13-C14之间的双键为反式）和这些化合物的环糊精包合物， R表示具有特征性前列腺素样活性的氢原子，无毒性盐。

8. 发明授权

US4165437A .DELTA..sup.3 -Prostaglandin analogs 失效
标题翻译： {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。

9. 发明授权

US4128720A Prostaglandin analogues 失效
标题翻译：前列腺素类似物
公开(公告)号：US4128720A
公开(公告)日：1978-12-05
申请号：US657125
申请日：1976-02-11
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
IPC分类号： A61K31/23 , A61K31/557 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F1/00 , C07F1/02 , C08B37/16 , C07C177/00
CPC分类号： C07D307/935 , C07C321/00 , C07C405/00 , C07C405/0033 , C07F1/00 , C07F1/02
摘要： Prostaglandins 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 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 straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, R.sup.2 represents a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms, or a grouping of the formula: ##STR3## wherein R.sup.4 and R.sup.5 each represents a hydrogen or halogen atom, a trifluoromethyl group or an alkyl group containing from 1 to 3 carbon atoms, or R.sup.2 and R.sup.3 together represent an ethylene or trimethylene group and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, non-toxic salts of such acids, are disclosed.These compounds exhibit characteristic prostaglandin activity, in particular, inhibitory activity on gastric secretion, luteolytic activity and so on.
摘要翻译：下式的前列腺素：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表示亚乙基或反式亚乙烯基，R表示氢原子或直链，或含有1至12个碳原子的支链烷基，R 1表示氢原子或含有1至10个碳原子的直链或支链烷基，R 2表示直链或支链烷基， 1至4个碳原子，R 3表示含有1至4个碳原子的直链或支链烷基，含有4至7个碳原子的环烷基，或下式的组：其中R 4和 R5各自表示氢或卤素原子，三氟甲基或含有1至3个碳原子的烷基，或者R 2和R 3一起表示这些酸和酯的乙烯或三亚甲基和环糊精包合物，当R表示氢原子公开了这种酸的有毒盐。

10. 发明授权

US4069387A 16-Chloro-substituted prostaglandins and derivatives thereof 失效
标题翻译： 16-氯取代的前列腺素及其衍生物
公开(公告)号：US4069387A
公开(公告)日：1978-01-17
申请号：US709847
申请日：1976-07-29
申请人： Masaki Hayashi , Seiji Kori , Katsuichi Shimoji
发明人： Masaki Hayashi , Seiji Kori , Katsuichi Shimoji
IPC分类号： A61K31/12 , A61K31/19 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P3/04 , A61P3/06 , A61P7/02 , A61P7/10 , A61P9/12 , A61P11/08 , A61P15/00 , A61P15/04 , B01J31/00 , C07B61/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0025 , C07F9/4006
摘要： The present invention relates to compounds of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## B represents a single bond or a straight- or branched-chain alkylene group containing from 1 to 9 carbon atoms, W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydroxymethyl group or a grouping of the formula --COOR.sup.4, in which R.sup.4 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 hydrogen atom or a methyl or ethyl group and R.sup.3 represents a hydrogen or chlorine atom or a hydroxy group and cyclodextrin clathrates of such alcohols, acids and esters and, when R.sup.4 in the formula --COOR.sup.4 represents a hydrogen atom, non-toxic salts thereof, and intermediates therefor. These compounds exhibit characteristic 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：B表示单键或含有1至9个碳原子的直链或支链亚烷基 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，R表示羟甲基或式-COOR4的基团，其中R4表示氢原子或直链，或含有1至12个碳原子的支链烷基，R1表示氢原子或甲基或乙基，R2表示氢原子或甲基或乙基，R3表示氢或氯原子或羟基，这些醇，酸和酯的环糊精包合物，以及当式-COOR 4中的R 4表示氢原子时，其无毒盐及其中间体。这些化合物表现出特征性的前列腺素样活性。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式