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31. 发明授权

US06833442B2 Complex and method for producing epoxides by using the complex 失效
标题翻译：通过使用络合物制备环氧化物的复合物和方法
公开(公告)号：US06833442B2
公开(公告)日：2004-12-21
申请号：US10211548
申请日：2002-08-05
申请人： Masakatsu Shibasaki , Takashi Ohshima , Tetsuhiro Nemoto
发明人： Masakatsu Shibasaki , Takashi Ohshima , Tetsuhiro Nemoto
IPC分类号： C07F500
CPC分类号： C07F9/70 , Y10S526/906 , Y10S526/915
摘要： There is provided a complex having a specified chemical structure and an asymmetric catalyst using such a complex. Further, an epoxidation of amine or ketone is enantioselectively conducted by using such an asymmetric catalyst.
摘要翻译：提供具有特定化学结构的复合物和使用这种络合物的不对称催化剂。此外，通过使用这种不对称催化剂对胺选择性地进行胺或酮的环氧化。

32. 发明授权

US06248918B1 Optically active binaphthyl compound and method for producing an optically active cyanohydrin compound employing the binaphthyl compound 有权
标题翻译：光学活性联萘化合物和使用联萘化合物制备光学活性羟腈化合物的方法
公开(公告)号：US06248918B1
公开(公告)日：2001-06-19
申请号：US09410747
申请日：1999-10-01
申请人： Masakatsu Shibasaki , Motomu Kanai , Yoshitaka Hamashima
发明人： Masakatsu Shibasaki , Motomu Kanai , Yoshitaka Hamashima
IPC分类号： C07C25300
CPC分类号： C07C253/00 , C07B2200/07 , C07F9/5329 , C07F9/6596 , C07C255/15 , C07C255/16 , C07C255/36
摘要： An optically active binaphthyl compound of the formula (1): wherein R1 is a C1-6 alkyl group, an aryl group or an aryl C1-6 alkyl group, X is an oxygen atom or a sulfur atom, R2 is a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group or a halogen atom, each of L1 and L2 is a hydrogen atom, or L1 and L2 together form MY wherein M is a rare earth element or a Group 13 element, and Y is a C1-6 alkoxy group, a C1-6 alkylcarbonyloxy group or a halogen atom, and m is an integer of from 1 to 3.
摘要翻译：式（1）的光学活性联萘化合物：其中R1是C1-6烷基，芳基或芳基C1-6烷基，X是氧原子或硫原子，R2是氢原子， C 1-6烷基，C 2-6烯基，C 2-6炔基或卤素原子，L1和L2各自为氢原子，或L1和L2一起形成MY，其中M为稀土元素或第13族元素，Y为C 1-6烷氧基，C 1-6烷基羰基氧基或卤素原子，m为1〜3的整数。

33. 发明授权

US5081238A .beta.methyl azetidinone derivatives and stereoselective process for preparing the same 失效
标题翻译：（BETA）甲基亚肼酮衍生物和用于制备其的立体选择性方法
公开(公告)号：US5081238A
公开(公告)日：1992-01-14
申请号：US535223
申请日：1990-06-08
申请人： Masakatsu Shibasaki , Takamasa Iimori
发明人： Masakatsu Shibasaki , Takamasa Iimori
IPC分类号： B01J23/00 , B01J23/40 , C07B61/00 , C07D205/08 , C07F7/18
CPC分类号： C07F7/186 , C07D205/08 , Y02P20/55
摘要： An azetidinone derivative having the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen atom or a protective group and R.sup.3 is an alkyl group or hydrogen atom, a process for preparing the same, and a process for preparing an azetidinone derivative having the general formula (II): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as above. The azetidinone derivative (I) of the present invention can be converted into an important intermediate of 1.beta.-methylcarbapenem antibiotics of a selective reduction of the double bond.
摘要翻译：具有通式（I）的氮杂环丁酮衍生物：其中R1和R2是氢原子或保护基，R3是烷基或氢原子，其制备方法和制备方法具有通式（II）的氮杂环丁酮衍生物：其中R1，R2和R3如上所述。本发明的氮杂环丁酮衍生物（I）可以转化为选择性还原双键的1β-甲基碳青霉烯类抗生素的重要中间体。

34. 发明授权

US4837342A Prostacyclin analogue, and blood circulation improving agent and anti-ulcer composition containing it as active ingredient 失效
公开(公告)号：US4837342A
公开(公告)日：1989-06-06
申请号：US14591
申请日：1987-02-13
申请人： Masakatsu Shibasaki , Atsuo Takahashi , Tuyoshi Aoki , Kentaro Kogi , Yozo Nishimiya , Takeshi Nara , Takashi Yamaguchi
发明人： Masakatsu Shibasaki , Atsuo Takahashi , Tuyoshi Aoki , Kentaro Kogi , Yozo Nishimiya , Takeshi Nara , Takashi Yamaguchi
IPC分类号： C07C405/00
CPC分类号： C07C405/0083
摘要： A prostacyclin analogue having the formula: ##STR1## wherein R.sup.1 is --CO.sub.2 R.sup.5 (wherein R.sup.5 is a hydrogen atom, a straight chain or branched alkyl group having from 1 to 12 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted phenyl group, or one equivalent of a cation), or --CONR.sup.6 R.sup.7 (wherein each of R.sup.6 and R.sup.7 is a hydrogen atom or an alkyl group having from 1 to 10 carbon atoms, or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom, form a 5- or 6-membered substituted or unsubstituted hetero ring which may contain a hetero atom other than said nitrogen atom); A is --CH.sub.2 CH.sub.2 CH.sub.2 --, CH.sub.2 --O--CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 --O--CH.sub.2 -- or --CH.dbd.CHCH.sub.2 CH.sub. 2 --; B is trans --CH.dbd.CH-- or --C.tbd.C--; R.sup.2 is a straight chain or branched alkyl group having from 3 to 10 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a straight chain or branched alkenyl group having from 3 to 12 carbon atoms, a straight chain or branched alkynyl group having from 3 to 8 carbon atoms, or an alkyl group having from 1 to 3 carbon atoms substituted by a substituted or unsubstituted phenyl or phenoxy group, by an alkoxy group having from 1 to 6 carbon atoms or by a cycloalkyl group having from 5 to 8 carbon atoms; R.sup.3 is a hydrogen atom, a methyl group or a vinyl group; and R.sup.4 is a hydrogen atom, an acyl group having from 1 to 7 carbon atoms, a tri-C.sub.1 -C.sub.7 hydrocarbon-silyl group or a group capable of forming an acetal bond together with the oxygen atom of a hydroxyl group; provided that the double bond in a substituent for A is E or Z, or a mixture thereof; the asymmetric center in a substituent for R.sup.2 assumes a R-conformation or a S-conformation, or a mixture thereof; and the bonds shown by dotted lines at the 2-3 and 3-4 positions mean that either one of them is a double bond.

35. 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.

36. 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。

37. 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。

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