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1. 发明授权

US07351849B2 Process for producing optically active β-amino acid derivatives 失效
标题翻译：光学活性β-氨基酸衍生物的制备方法
公开(公告)号：US07351849B2
公开(公告)日：2008-04-01
申请号：US10567368
申请日：2004-08-18
申请人： Mikiko Sodeoka , Yoshitaka Hamashima
发明人： Mikiko Sodeoka , Yoshitaka Hamashima
IPC分类号： C07C205/00 , C07C229/00
CPC分类号： C07C269/06 , C07C227/32 , C07C271/20 , C07C271/64
摘要： The present invention is to provide a method for producing the desired optically active β-amino acid derivatives of high optical purities in high yields, without requiring a step of deprotection. More particularly, the present invention relates to a method for producing an optically active β-amino acid derivative or a salt thereof represented by the formula (2): which comprises reacting an α,β-unsaturated carboxylic acid derivative or a salt thereof represented by the formula (1): with an amines or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid.
摘要翻译：本发明提供以高产率生产高光学纯度的所需光学活性β-氨基酸衍生物的方法，而不需要脱保护步骤。更具体地说，本发明涉及由式（2）表示的光学活性β-氨基酸衍生物或其盐的制备方法：其包括使由α，β-不饱和羧酸衍生物或其盐表示的α，β-不饱和羧酸衍生物或其盐式（1）：在手性催化剂的存在下和在存在或不存在酸的情况下，用胺或其盐。

2. 发明授权

US4681951A Bicyclo(3.3.0)octene derivatives 失效
标题翻译：双环（3.3.0）辛烯衍生物
公开(公告)号：US4681951A
公开(公告)日：1987-07-21
申请号：US641587
申请日：1984-08-17
申请人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
发明人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
IPC分类号： C07C405/00 , C07F7/18 , C07D309/10 , C07C47/40
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C405/0083 , Y02P20/55
摘要： There are disclosed bicyclo[3.3.0]octene derivatives having the following formula: ##STR1## wherein R.sup.1 is a straight, branched or cyclic alkyl group or alkenyl group each having 5 to 10 carbon atoms; andR.sup.2 and R.sup.3 are each separately a hydrogen atom or a protective group of a hydroxy group,and process for producing the same. These compounds and the process for producing them are available for producing a 9(0)-methano-.DELTA.6(9.alpha.)-PGI.sub.1.
摘要翻译：公开了具有下式的双环[3.3.0]辛烯衍生物：其中R 1是各自具有5至10个碳原子的直链，支链或环状烷基或烯基; R2和R3各自独立地为氢原子或羟基的保护基，以及其制备方法。这些化合物及其制备方法可用于制备9（0） - 甲 - △DELTA 6（9α）-PGI1。

3. 发明授权

US4777271A Isocarbacyclin derivatives and process for production thereof 失效
标题翻译：异卡环素衍生物及其制备方法
公开(公告)号：US4777271A
公开(公告)日：1988-10-11
申请号：US65218
申请日：1987-05-29
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Toshiaki Mase
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Toshiaki Mase
IPC分类号： C07D319/00 , C07C405/00 , C07D493/08 , C07D319/04
CPC分类号： C07C405/0083 , Y02P20/55
摘要： An isocarbacyclin derivative represented by the general formula ##STR1## wherein R.sup.1 represents a linear, branched or cyclic alkyl, alkenyl or alkynyl group having 5 to 10 carbon atoms, and R.sup.2 and R.sup.3 represent a hydrogen atom or a protective group for the hydroxyl group; and a process for production thereof.

4. 发明授权

US4774341A Bicyclo(3.3.0)octane derivative and preparation thereof 失效
标题翻译：双环（3.3.0）辛烷衍生物及其制备
公开(公告)号：US4774341A
公开(公告)日：1988-09-27
申请号：US912507
申请日：1986-09-29
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa
IPC分类号： C07C405/00 , C07F7/18
CPC分类号： C07C405/0016 , C07C405/0025 , C07C405/0083 , C07F7/1856 , Y02P20/55
摘要： There are disclosed a bicyclo [3.3.0]octane derivative represented by the formula: ##STR1## wherein R.sup.1 is a substituent selected from the group consisting of a hydrogen atom and a protective group of a hydroxy group;R.sup.2 is a substituent selected from the group consisting of --CH.sub.2 OR.sup.5 and ##STR2## where R.sup.5 is a substituent selected from the group consisting of a hydrogen atom and a protective group of a hydroxy group,R.sup.6 is a substituent selected from the group consisting of an alkyl group, an alkenyl group and an alkynyl group, said substituent being straight, branched or cyclic and having 5 to 10 carbon atoms,X is a substituent selected from the group consisting of a vinylene group and an acetylene group, andR.sup.7 is a substituent selected from the group consisting of an alkyl group, an alkenyl group, and an alkynyl group said substituent being straight, branched or cyclic and having 5 to 10 carbon atoms; andR.sup.3 is a substituent represented by the formula --Y--(CH.sub.2).sub.2 --COOR.sup.8 whereR.sup.8 is a hydrogen atom or an alkyl group andY is a vinylene group or an alkylene group; andR.sup.4 is a hydroxy group when the compound is an octane derivative, or a hydrogen atom when the compound is an octene derivative; anddotted line denotes optional presence of a double bond.The compound of this invention and the process for producing the same are available for producing a 9(0)-methano-.DELTA.6(9..alpha.)-PGI.sub.1.
摘要翻译：公开了由下式表示的双环[3.3.0]辛烷衍生物：其中R 1是选自氢原子和羟基保护基的取代基; R2是选自-CH2OR5和R5的取代基，其中R5是选自氢原子和羟基的保护基的取代基，R6是选自下列的取代基：烷基，烯基和炔基，所述取代基是直链，支链或环状的并且具有5至10个碳原子，X是选自亚乙烯基和乙炔基的取代基，并且R 7是取代基选自烷基，烯基和炔基，所述取代基是直链，支链或环状且具有5至10个碳原子; 并且R 3是由式-Y-（CH 2）2 -COOR 8表示的取代基，其中R 8是氢原子或烷基，Y是亚乙烯基或亚烷基; 当化合物为辛烷衍生物时，R4为羟基，当化合物为辛烯衍生物时，为氢原子; 而虚线表示双键的任选存在。本发明的化合物及其制备方法可用于制备9（0） - 甲基-TATA 6（9α）-PGI1。

5. 发明授权

US4699921A Pharmaceuticals containing prostaglandin I.sub.2 失效
标题翻译：含有前列腺素I2的药物
公开(公告)号：US4699921A
公开(公告)日：1987-10-13
申请号：US763618
申请日：1985-08-08
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
IPC分类号： C07C59/46 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/12 , C07C51/00 , C07C67/00 , C07C69/732 , C07C405/00
CPC分类号： C07C405/0083 , A61K31/557 , Y02P20/55
摘要： Disclosed is a pharmaceutical composition having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group, A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or a 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof; the asymmetric center in the substituent represented by A is in the R-configuration or the S-configuration or a mixture thereof.Pharmaceutical compositions containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要翻译：本发明公开了一种具有循环改善作用和抗溃疡效果的药物组合物，其含有下述式表示的前列腺素I 2类似物或其无毒性盐或环糊精包合物作为有效成分：其中R 1表示氢原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基，A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2 1-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1-二甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基 -3-戊炔基或2,6-二甲基-5-庚烯基; 4-和5-位的碳原子之间的双键是E或Z或它们的混合物; 由A表示的取代基中的不对称中心是R构型或S-构型或其混合物。含有本发明的前列腺素I2类似物作为活性成分的药物组合物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

6. 发明授权

US4839388A Prostacyclins and pharmaceuticals containing the same 失效
标题翻译：前列环素和含有相同的药物
公开(公告)号：US4839388A
公开(公告)日：1989-06-13
申请号：US060870
申请日：1987-05-18
申请人： Masakatsu Sibasaki , Mikiko Sodeoka , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Aoki , Yosio Hayasi , Toshiji Kanayama
发明人： Masakatsu Sibasaki , Mikiko Sodeoka , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Aoki , Yosio Hayasi , Toshiji Kanayama
IPC分类号： C07C59/125 , A61K31/557 , A61K31/695 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/12 , C07C51/00 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/64 , C07C59/72 , C07C67/00 , C07C69/03 , C07C69/708 , C07C69/732 , C07C69/734 , C07C231/00 , C07C235/06 , C07C235/30 , C07C235/34 , C07C405/00 , C07D295/18 , C07F7/18
CPC分类号： C07C405/0083
摘要： This invention relates to a novel prostacyclin represented by the formula: ##STR1## [wherein R.sup.1 represents --CO.sub.2 R.sup.5 group or --CONR.sup.6 R.sup.7 group; A is(i) --CH.dbd.CH--CH.sub.2 CH.sub.2 -- or(ii) --CH.sub.2 CH.sub.2 --O--CH.sub.2 --;B represents --C.tbd.C-- group; R.sup.2 represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a phenyl group or a phenoxy group;R.sup.3 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.4 represents a hydrogen atom, an acyl group, a tri(1 to 7 carbon atoms)hydrocarbyl-silyl group or a group forming an acetal bond with an oxygen atom of a hydroxy group; a double bond in the substituent represented by A is E or Z, or a mixture thereof; asymmetric center in the substituent represented by R.sup.2 is an R-configuration or S-configuration, or a mixture thereof];and uses in which they are employed as circulation ameliorating pharmaceuticals for blood flow ameliorating, antithrombus and the like, or antiulcer pharmaceuticals.
摘要翻译： PCT No.PCT / JP86 / 00486 Sec。 371日期1987年5月18日 102（e）日期1987年5月18日PCT提交1986年9月18日PCT公布。公开号WO87 / 01696 日本公开号为1987年3月26日。本发明涉及由下式表示的新型前列环素：其中R1表示-CO2R5基或-CONR6R7基; A是（i）-CH = CH-CH 2 CH 2 - 或（ii）-CH 2 CH 2 -O-CH 2 - ; B表示-C3OND C-基团; R2表示烷基，环烷基，烯基，炔基，苯基或苯氧基; R3表示氢原子，甲基或乙烯基; R 4表示氢原子，酰基，三（1〜7个碳原子）烃基 - 甲硅烷基或与羟基的氧原子形成缩醛键的基团。由A表示的取代基中的双键为E或Z，或其混合物; 由R2表示的取代基中的不对称中心是R构型或S-构型，或其混合物]; 以及它们被用作改善血流改善药物的循环改善剂，抗凝血剂等或抗溃疡药物的用途。

7. 发明授权

US4762936A Bicyclo(3.3.0)Octene derivatives 失效
标题翻译：双环（3.3.0）辛烯衍生物
公开(公告)号：US4762936A
公开(公告)日：1988-08-09
申请号：US940349
申请日：1986-12-11
申请人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
发明人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
IPC分类号： C07C405/00 , C07F7/18 , C07D309/10 , C07C47/40 , C07C35/26
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C405/0083 , Y02P20/55
摘要： There are disclosed a bicyclo[3.3.0]octene derivatives having the following formula: ##STR1## wherein R.sup.1 : a straight, branched or cyclic alkyl group or alkenyl group each having 5 to 10 carbon atoms;R.sup.2 and R.sup.3 : each represent a hydrogen atom or a protective group of a hydroxy group; andR.sup.4 : --CH.dbd.CH--(CH.sub.2).sub.2 --COOR.sup.5 or --CH.sub.2 R.sup.6 ; whereR.sup.5 : a hydrogen atom or an alkyl group; andR.sup.6 : a hydroxy group, an acetyloxy group or a butenyl group,and process for producing the same. These compounds and the process for producing them are available for producing a 9(0)-methano-.DELTA..sup.6 (9.alpha.)-PGI.sub.1.
摘要翻译：公开了具有下式的双环[3.3.0]辛烯衍生物：其中R 1：各自具有5-10个碳原子的直链，支链或环状烷基或烯基; R2和R3各自表示氢原子或羟基的保护基; 和R 4：-CH = CH-（CH 2）2 -COOR 5或-CH 2 R 6; 其中R5为氢原子或烷基; 和R6：羟基，乙酰氧基或丁烯基，及其制备方法。这些化合物及其制备方法可用于制备9（0） - 甲 - △DELTA 6（9α）-PGI1。

8. 发明授权

US4632997A Method for preparing cis-bicyclo[3.3.0]octylidene derivative 失效
标题翻译：顺式 - 双环[3.3.0]亚辛基衍生物的制备方法
公开(公告)号：US4632997A
公开(公告)日：1986-12-30
申请号：US700003
申请日：1985-02-08
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa
IPC分类号： C07C405/00 , C07F7/18 , C07C51/36 , C07C67/303 , C07D309/10
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C405/0083 , Y02P20/55
摘要： A method for preparing a cis-bicyclo[3.3.0]octylidene derivative represented by the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group; R.sup.2 is a hydrogen atom or a protective group for hydroxyl group; and Y is ##STR2## where R.sup.3 is a hydrogen atom or a protective group for hydroxyl group; R.sup.4 is a hydrogen atom or a straight, branched or cyclic alkyl group, alkenyl group or alkynyl group; and X is a group represented by CH.dbd.CH or C.tbd.C,comprises carrying out the catalytic hydrogenation reaction of a (1-alkenyl)-cis-bicyclo[3.3.0]octene derivative represented by the formula: ##STR3## wherein R.sup.1, R.sup.2 and Y have the same meanings as defined above, in the presence of a metal carbonyl compound or its complex represented by the formula:Mw(CO)x(H)y(R)zwherein M is a metal element of the group VIB; R is a .pi. ligand or a phosphine ligand; w is 1 or 2; x is an integer of 3 to 6; y is 0 or 1; and z is 0 or an integer of 1 to 3.
摘要翻译：一种制备由下式表示的顺式 - 双环[3.3.0]亚辛基衍生物的方法：其中R1是氢原子或烷基; R2是氢原子或羟基的保护基; Y为，其中R3为氢原子或羟基保护基; R4是氢原子或直链，支链或环状烷基，烯基或炔基; X为由CH = CH或C 3 B C表示的基团，包括进行由下式表示的（1-烯基） - 双 - 二环[3.3.0]辛烯衍生物的催化氢化反应：其中R1 在其中M是该基团的金属元素的情况下，在由式（M）（CO）x（H）y（R）z表示的金属羰基化合物或其络合物的存在下，R2和Y具有与上述相同的含义： VIB; R是π配体或膦配体; w为1或2; x为3〜6的整数， y为0或1; z为0或1〜3的整数。

9. 发明授权

US06589977B1 Pyrrole derivatives and cell death inhibitors 失效
标题翻译：吡咯衍生物和细胞死亡抑制剂
公开(公告)号：US06589977B1
公开(公告)日：2003-07-08
申请号：US09890827
申请日：2001-08-06
申请人： Mikiko Sodeoka , Miho Katoh , Mikako Fujita , Rei Asakai
发明人： Mikiko Sodeoka , Miho Katoh , Mikako Fujita , Rei Asakai
IPC分类号： A61K31404
CPC分类号： C07D403/14
摘要： Bisindolylpyrrole derivatives represented by general formula [I] which are useful in inhibiting cell death and expected as being useful as preventives and remedies for the progress of various diseases in the progress and worsening of which cell death participates; and cell death inhibitors, drugs and cell/tissue/organ preservatives containing as the active ingredient these derivatives or pharmaceutically acceptable salts thereof.
摘要翻译：由通式[I]表示的双吲哚基吡咯衍生物，其可用于抑制细胞死亡并且预期作为预防药物和用于在进行中的各种疾病的进展以及哪种细胞死亡参与恶化的补救措施; 和细胞死亡抑制剂，药物和细胞/组织/器官防腐剂，其含有这些衍生物或其药学上可接受的盐。

10. 发明授权

US5053526A Pharmaceuticals containing prostaglandin I.sub.2 失效
标题翻译：含有前列腺素I2的药物
公开(公告)号：US5053526A
公开(公告)日：1991-10-01
申请号：US511945
申请日：1990-04-16
申请人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
发明人： Masakatsu Shibasaki , Mikiko Sodeoka , Yuji Ogawa , Toshiaki Mase , Akira Ishibashi , Daijiro Horii , Toshiji Kanayama , Katsuhiko Iseki , Masaki Shinoda , Chiyoko Ishiyama , Yoshio Hayashi
IPC分类号： A61K31/557 , C07C405/00
CPC分类号： C07C405/0083 , A61K31/557
摘要： Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要翻译：本发明公开了一种具有循环改善作用和抗溃疡效果的药物，其含有下述式表示的前列腺素I2类似物或其盐的无毒性盐或其环糊精包合物作为有效成分：其中R1表示氢原子，碳原子数1〜12的烷基，碳原子数4〜7的环烷基或苯基; A表示戊基，环戊基，环己基，1-甲基-3-己炔基，2-甲基-3-己炔基，1-甲基己基，2-苯乙基，1,1 2-甲基戊基，2-甲基戊基，1-环己基乙基，2-甲基己基，1-甲基-3-戊炔基或1,6-二甲基-5-庚烯基; 在4-和5-位碳原子之间的双键是E或Z或其混合物，由A表示的取代基中的不对称中心是R-构型或S-构型或其混合物。含有本发明的前列腺素I2类似物作为活性成分的药物具有有效的血小板聚集抑制作用，降血压作用，血管扩张作用和抗溃疡作用，毒性也低。

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