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1. 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.

2. 发明授权

US5117037A Cis-bicyclo[4,3.0]non-2-end derivatives 失效
标题翻译： CIS-BICYCLO（4,3.0）非2-D衍生物
公开(公告)号：US5117037A
公开(公告)日：1992-05-26
申请号：US622471
申请日：1990-12-05
申请人： Masakatsu Shibasaki , Takahashi Atsuo , Tuyoshi Aoki , Hiroyasu Sato , Shin-ichi Yamada , Michiko Kudo , Takaji Yamaguchi , Kentaro Kogi , Sen-ichi Narita
发明人： Masakatsu Shibasaki , Takahashi Atsuo , Tuyoshi Aoki , Hiroyasu Sato , Shin-ichi Yamada , Michiko Kudo , Takaji Yamaguchi , Kentaro Kogi , Sen-ichi Narita
IPC分类号： C07C59/46 , C07C59/62 , C07C69/712 , C07C69/732 , C07C69/738 , C07C405/00
CPC分类号： C07C69/738 , C07C405/0083 , C07C59/46 , C07C59/62 , C07C69/712 , C07C69/732 , Y02P20/55
摘要： A cis-bicyclo[4.3.0]non-2-ene derivative of the formula: ##STR1## wherein R is a hydrogen atom, or a protecting group for a hydroxyl group, R.sup.1 is a hydrogen atom, A C.sub.1 -C.sub.12 straight or branched chain alkyl group, a substituted or unsubstituted phenyl group, a C.sub.6 -C.sub.12 aralkyl group containing a condensed aromatic ring or an aromatic hetero ring, or 1 equivalent of a cation, A is --CH.dbd.CH--CH.sub.2 --, or --CH.sub.2 --CH.sub.2 --O--, R.sup.2 is a C.sub.3 -C.sub.10 straight or branched chain alkyl group, a C.sub.1 -C.sub.3 alkyl group substituted by an aryloxy group which may be substituted, a C.sub.3 -C.sub.12 straight or branched chain alkenyl group, a C.sub.3 -C.sub.8 straight or branched chain alkynyl group, a C.sub.1 -C.sub.3 alkyl group substituted by a phenyl or phenoxy group which may be substituted, by a C.sub.1 -C.sub.6 alkoxy group or by a C.sub.5 -C.sub.8 cycloalkyl group, R.sup.3 is a hydrogen atom, a methyl group, or a vinyl group, and X is a halogen atom.

3. 发明申请

US20050148801A1 Optically active nitro alcohol derivatives, optically active amino alcohol derivatives, and process for producing thereof 有权
标题翻译：光学活性硝基醇衍生物，光学活性氨基醇衍生物及其制备方法
公开(公告)号：US20050148801A1
公开(公告)日：2005-07-07
申请号：US11044223
申请日：2005-01-28
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
IPC分类号： C07C201/12 , C07C205/16 , C07C205/17 , C07C205/37 , C07C205/42 , C07C213/02 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07D319/08 , C07F7/18 , C07C25/16
CPC分类号： C07D319/08 , B01J31/223 , B01J2231/342 , B01J2531/0266 , B01J2531/37 , B01J2531/38 , C07B2200/07 , C07C205/16 , C07C205/17 , C07C205/35 , C07C205/37 , C07C205/40 , C07C205/42 , C07C213/02 , C07C215/60 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07F7/1804 , C07F7/1892
摘要： Optically active 1-substituted phenyl-2-nitro alcohol derivatives having the formula (1) and the process for producing thereof, and 1-substituted phenyl-2-amino alcohol derivatives having the formula (2) and the process for producing thereof from the optically active 1-substituted phenyl-2-nitro alcohol derivatives. From these nitro alcohols, pharmaceuticals such as (R)-albutamin and (R)-sarmeterol useful as a bronchodilator is obtained via optically active amino alcohols which are useful pharmaceutical intermediates.
摘要翻译：具有式（1）的光学活性1-取代苯基-2-硝基醇衍生物及其制备方法和具有式（2）的1-取代苯基-2-氨基醇衍生物及其制备方法光学活性的1-取代苯基-2-硝基醇衍生物。通过这些硝基醇，可以通过作为有用的药物中间体的光学活性氨基醇获得用作支气管扩张剂的（R） - 丁二胺和（R） - 三异胺的药物。

4. 发明授权

US06677461B2 Ligands and asymmetric catalysts made by using the same 失效
标题翻译：配体和不对称催化剂通过使用它们制备
公开(公告)号：US06677461B2
公开(公告)日：2004-01-13
申请号：US10070724
申请日：2002-07-30
申请人： Masakatsu Shibasaki , Motomu Kanai , Yoshitaka Hamashima
发明人： Masakatsu Shibasaki , Motomu Kanai , Yoshitaka Hamashima
IPC分类号： C07D30910
CPC分类号： C07F9/74 , B01J31/1875 , B01J31/2226 , B01J31/223 , B01J2231/341 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/32 , B01J2531/38 , C07F7/003 , C07F9/6552 , C07F9/6596
摘要： A ligand expressed by a general formula (1) in claim 1, wherein R1, R2 and R3 denote substituting groups on aromatic rings, X is P or As, and n is 1 to 3.
摘要翻译：由权利要求1的通式（1）表示的配体，其中R 1，R 2和R 3表示芳环上的取代基，X为P或As，n为1至3。

5. 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。

6. 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。

7. 发明授权

US07820862B2 Ligand, method for producing the same, and catalyst using the ligand 失效
标题翻译：配体，其制备方法和使用配体的催化剂
公开(公告)号：US07820862B2
公开(公告)日：2010-10-26
申请号：US12281361
申请日：2007-03-02
申请人： Masakatsu Shibasaki , Motomu Kanai , Ikuo Fujimori , Kenzo Yamatsugu , Shin Kamijo
发明人： Masakatsu Shibasaki , Motomu Kanai , Ikuo Fujimori , Kenzo Yamatsugu , Shin Kamijo
IPC分类号： C07C9/02 , B01J31/00
CPC分类号： B01J31/223 , B01J31/0212 , B01J31/18 , B01J31/1875 , B01J2231/32 , B01J2531/0258 , B01J2531/25 , B01J2531/31 , B01J2531/38 , B01J2531/46 , B01J2531/48 , B01J2540/22 , C07B2200/07 , C07C67/347 , C07C2601/04 , C07C2601/16 , C07D207/325 , C07F9/5325 , C07C69/757
摘要： Disclosed is a novel asymmetric ligand which can be synthesized by a short process at low cost and is capable of exhibiting higher catalytic activity and enantioselectivity than the conventional ligands derived from sugars. Also disclosed are a method for producing such an asymmetric ligand, and a catalyst using such an asymmetric ligand. Specifically disclosed is a ligand represented by the general formula I below or the like. (In the formula, R1 and R2 independently represent 0-5 substituents; X represents P, As or N; m represents an integer of 0-7; n represents an integer of 0-3; A1-A4 independently represent hydrogen, fluorine, chlorine, bromine, benzoyl or acetyl, or alternatively A2 and A3 combine together to form a ring.)
摘要翻译：公开了一种新型的不对称配体，其可以通过短时间的方法以低成本合成，并且能够表现出比来自糖的常规配体更高的催化活性和对映选择性。还公开了制备这种不对称配体的方法和使用这种不对称配体的催化剂。具体公开了由下述通式I表示的配体等。（式中，R 1和R 2独立地表示0〜5个取代基，X表示P，As或N; m表示0〜7的整数，n表示0〜3的整数，A 1〜A 4独立地表示氢，氟，氯，溴，苯甲酰基或乙酰基，或者A2和A3组合在一起形成环。）

8. 发明申请

US20070060656A1 Optically active nitro alcohol derivatives, optically active amino alcohol derivatives, and process for producing thereof 审中-公开
标题翻译：光学活性硝基醇衍生物，光学活性氨基醇衍生物及其制备方法
公开(公告)号：US20070060656A1
公开(公告)日：2007-03-15
申请号：US11595987
申请日：2006-11-13
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
IPC分类号： A61K31/138 , C07C205/16
CPC分类号： C07D319/08 , B01J31/223 , B01J2231/342 , B01J2531/0266 , B01J2531/37 , B01J2531/38 , C07B2200/07 , C07C205/16 , C07C205/17 , C07C205/35 , C07C205/37 , C07C205/40 , C07C205/42 , C07C213/02 , C07C215/60 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07F7/1804 , C07F7/1892
摘要： Optically active 1-substituted phenyl-2-nitro alcohol derivatives having the formula (1) and the process for producing thereof, and 1-substituted phenyl-2-amino alcohol derivatives having the formula (2) and the process for producing thereof from the optically active 1-substituted phenyl-2-nitro alcohol derivatives. From these nitro alcohols, pharmaceuticals such as (R)-albutamin and (R)-sarmeterol useful as a bronchodilator is obtained via optically active amino alcohols which are useful pharmaceutical intermediates.
摘要翻译：具有式（1）的光学活性1-取代苯基-2-硝基醇衍生物及其制备方法和具有式（2）的1-取代苯基-2-氨基醇衍生物及其制备方法光学活性的1-取代苯基-2-硝基醇衍生物。通过这些硝基醇，可以通过作为有用的药物中间体的光学活性氨基醇获得用作支气管扩张剂的（R） - 丁二胺和（R） - 三异胺的药物。

9. 发明申请

US20050004388A1 Method of manufacturing cyano compounds 有权
标题翻译：制备氰基化合物的方法
公开(公告)号：US20050004388A1
公开(公告)日：2005-01-06
申请号：US10882337
申请日：2004-07-02
申请人： Masakatsu Shibasaki , Motomu Kanai , Yutaka Suto
发明人： Masakatsu Shibasaki , Motomu Kanai , Yutaka Suto
IPC分类号： C07C253/30 , C07C255/12 , C07C253/08
CPC分类号： C07C253/30 , C07B2200/07 , C07C2601/14 , C07C255/12
摘要： A method of manufacturing a cyano compound by reacting a carbonyl compound with a nitrile compound having at least one α-hydrogen atom in the presence of a ligand and a metal compound of formula (III), MX (III) wherein M is a copper atom or a silver atom, and X is an alkoxy group, an alkyl group, an aryl group or an anionic residue.
摘要翻译：在配体和式（III）的金属化合物，MX（III）的存在下，使羰基化合物与具有至少一个α氢原子的腈化合物反应制备氰基化合物的方法，其中M是铜原子或银原子，X为烷氧基，烷基，芳基或阴离子残基。

10. 发明授权

US06809059B2 Catalyst 失效
标题翻译：催化剂
公开(公告)号：US06809059B2
公开(公告)日：2004-10-26
申请号：US09912319
申请日：2001-07-26
申请人： Masakatsu Shibasaki
发明人： Masakatsu Shibasaki
IPC分类号： B01J3100
CPC分类号： B01J31/223 , B01J23/10 , B01J2231/348 , B01J2531/0238 , B01J2531/0266 , B01J2531/37 , C07B53/00 , C07B2200/07 , C07C67/347 , C07C2601/14 , C07C69/716 , C07C69/738
摘要： A catalyst and method for performing a Michael addition reaction between a &bgr;-dicarbonyl compound with a cyclic or acyclic enone, where the catalyst comprises a substituted or unsubstituted lanthanum-linked BINOL complex, e.g. a (R,R)-La-linked-BINOL complex (I), are described. The catalyst is stable in air, is readily separated from the reaction mixtures and may be reused if desired.
摘要翻译：一种用于在β-二羰基化合物与环状或无环烯酮之间进行迈克尔加成反应的催化剂和方法，其中催化剂包含取代或未取代的镧连接的BINOL络合物，例如。描述了（R，R）-La-连接的BINOL络合物（I）。催化剂在空气中是稳定的，容易与反应混合物分离，并且如果需要可以重复使用。

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