公开(公告)号：US4493846A

公开(公告)日：1985-01-15

申请号：US243570

申请日：1981-03-13

申请人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Shunsuke Sami ,  Atsuyuki Kojima ,  Junki Katsube

发明人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Shunsuke Sami ,  Atsuyuki Kojima ,  Junki Katsube

IPC分类号： C07C69/708 ,  A61K31/557 ,  C07C29/09 ,  C07C29/128 ,  C07C35/32 ,  C07C43/196 ,  C07C47/198 ,  C07C47/277 ,  C07C51/00 ,  C07C51/08 ,  C07C59/125 ,  C07C59/13 ,  C07C59/31 ,  C07C59/46 ,  C07C59/62 ,  C07C67/00 ,  C07C67/08 ,  C07C69/734 ,  C07C405/00 ,  C07D211/32 ,  C07D295/08 ,  C07D295/18 ,  C07C69/608 ,  C07C61/13 ,  C07C61/28 ,  C07C69/616

CPC分类号： C07C255/00 ,  C07C29/095 ,  C07C29/1285 ,  C07C35/32 ,  C07C405/0083 ,  C07C43/196 ,  C07D211/32 ,  C07B2200/07 ,  C07B2200/09 ,  C07C2102/24 ,  Y10S514/925

摘要： A compound of the formula ##STR1## wherein X.sup.1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7-membered saturated heterocyclic group) or a group of the formula: ##STR3## (R.sup.a and R.sup.b are each as defined above), Y is an ethylene group or a vinylene group, R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sub.1 and R.sub.2, when taken together, means a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.3 -C.sub.8 alkynyl group, a C.sub.1 -C.sub.8 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group or a group of the formula: --(CH.sub.2).sub.n --B (n is 1 or 2 and B is a C.sub.1 -C.sub.4 alkoxyl group, a C.sub.3 -C.sub.7 cycloalkyl group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group or a C.sub.1 -C.sub.4 alkoxyl group), A is a group of either one of the formulae: ##STR4## (R.sup.6 and R.sup.7 are each independently a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and ##STR5## m.sub.1 is 1 or 2 and m.sub.2 is 0, 1 or 2, and the non-toxic pharmaceutically acceptable salts threreof. Said compounds have strong anti-ulcerogenic activity and are useful in treatment of gastraintestinal ulcer.

摘要翻译： 下式的化合物其中X1是游离或酯化的羧基，羟甲基，氰基，下式的基团：（R a和R b各自独立地是氢原子，C 1 -C 4 烷基，C3-C7环烷基，苄基，苯基，被卤素原子或C1-C4烷基取代的苯基，或者当与它们所连接的相邻氮原子一起时， 它们表示5至7元饱和杂环基）或下式的基团：（R a和R b各自如上所定义），Y是亚乙基或亚乙烯基，R 1是氢原子， 羟基或受保护的羟基，R2是氢原子或R1和R2，当它们一起表示在它们连接的碳原子之间形成双键的单键，R3是羟基或被保护的羟基 R4是氢原子或C1-C4烷基，R5是氢原子，C3-C8链烯基，C3-C8烷基 正丁基，C 1 -C 8烷基，C 3 -C 7环烷基或下式基团： - （CH 2）n B（n为1或2，B为C 1 -C 4烷氧基，C 3 -C 7环烷基 或任选被卤素原子取代的苯基或苯氧基，C 1 -C 4烷基，三氟甲基或C 1 -C 4烷氧基），A是以下基团之一： R 7各自独立地为氢原子或C 1 -C 4烷基），并且M 1为1或2，m 2为0,1或2，以及无毒的药学上可接受的盐。 所述化合物具有强的抗溃疡活性，可用于治疗胃肠溃疡。

公开(公告)号：US4297282A

公开(公告)日：1981-10-27

申请号：US90857

申请日：1979-11-02

申请人： Naohito Ohashi ,  Shoji Nagata ,  Junki Katsube

发明人： Naohito Ohashi ,  Shoji Nagata ,  Junki Katsube

IPC分类号： C07C327/00 ,  C07D207/16 ,  C07C153/017

CPC分类号： C07C327/00 ,  C07D207/16

摘要： This invention relates to a process for the optical resolution of DL-.alpha.-methyl-.beta.-acylthiopropionic acids of the formula [I], ##STR1## wherein R is a lower alkyl group having 1-4 carbon atoms, phenyl or substituted phenyl bearing methyl or chloro radical; a method for the racemization of an optically active .alpha.-methyl-.beta.-acylthiopropionic acid of the formula [Ia], ##STR2## wherein R is as defined above; and a process for the synthesis of captopril of the formula [II], ##STR3## using the D-acid [Ia] as an intermediate. The optically active .alpha.-methyl-.beta.-acylthiopropionic acids are useful as intermediates for the production of medicines, for example, captopril or its congeners.

摘要翻译： 本发明涉及一种用于光学拆分式[I]，其中R是具有1-4个碳原子的低级烷基的式[I]，其中R 1是苯基或 取代的含甲基或氯基的苯基; 式[Ia]的光学活性α-甲基-β-酰基硫代丙酸外消旋化的方法，其中R如上定义; 以及使用D-酸[Ia]作为中间体合成式[II]，IMAGE [II]的卡托普利的方法。 光学活性α-甲基-β-酰基硫代丙酸可用作生产药物的中间体，例如卡托普利或其同系物。

公开(公告)号：US4292432A

公开(公告)日：1981-09-29

申请号：US117981

申请日：1980-02-04

申请人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Junki Katsube

发明人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Junki Katsube

IPC分类号： C07C45/00 ,  C07C45/28 ,  C07C45/30 ,  C07C45/40 ,  C07C45/59 ,  C07C45/67 ,  C07C49/523 ,  C07C62/32 ,  C07C67/00 ,  C07C405/00 ,  C07D317/72 ,  C07D319/08 ,  C07D317/12 ,  C07D339/06

CPC分类号： C07D317/72 ,  C07C405/0083 ,  C07C45/28 ,  C07C45/30 ,  C07C45/40 ,  C07C45/59 ,  C07C45/67 ,  C07C49/523 ,  C07C62/32 ,  Y02P20/55

摘要： A process for producing novel aldol derivatives of the formula, ##STR1## wherein C=W is a carbonyl group or a protected carbonyl group which comprises reacting a compound of the formula: ##STR2## wherein C=W is as defined above in the presence of an acid or a base at a temperature ranging from -70.degree. C. to room temperature. The novel aldol derivatives of the above formula are useful as intermediate for producing methanoprostacyclin derivatives which are useful medicines for prevention of thrombosis.

摘要翻译： 一种制备下式的新型醛醇衍生物的方法，其中C = W是羰基或被保护的羰基，其包括使下式化合物：其中C = W如上所定义， 的酸或碱在-70℃至室温的温度下进行。 上述式的新型醛醇衍生物可用作生产甲基前列腺素衍生物的中间体，其是预防血栓形成的有用药物。

公开(公告)号：US4230706A

公开(公告)日：1980-10-28

申请号：US021776

申请日：1979-03-19

申请人： Isamu Maruyama ,  Shunji Aono ,  Junki Katsube

发明人： Isamu Maruyama ,  Shunji Aono ,  Junki Katsube

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P9/12 ,  C07D239/95

CPC分类号： C07D239/95

摘要： Quinazoline compounds of the formula: ##STR1## wherein A is ##STR2## wherein n is an integer of 1 or 2, or ##STR3## wherein X is O or CH.sub.2, and n and m are independently an integer of 1 or 2, and its non-toxic pharmaceutically acceptable salts, having an excellent antihypertensive activity without causing adverse effects such as orthostatic hypotension.

摘要翻译： 喹唑啉化合物，其结构式如下：其中A是其中n是1或2的整数，或者其中X是O或CH 2，n和m独立地是1或2的整数， 其无毒的药学上可接受的盐，具有优异的抗高血压活性而不引起诸如直立性低血压的不利影响。

公开(公告)号：US4210669A

公开(公告)日：1980-07-01

申请号：US911039

申请日：1978-05-30

申请人： Hiromi Shimomura ,  Akihiko Sugie ,  Junki Katsube

发明人： Hiromi Shimomura ,  Akihiko Sugie ,  Junki Katsube

IPC分类号： C07C405/00 ,  C07D307/935 ,  C07C177/00 ,  A61K31/19 ,  A61K31/215

CPC分类号： C07D307/935 ,  C07C405/00 ,  Y10S514/925

摘要： Prostanoic acid derivatives of the formula, ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, R.sub.2 is C.sub.4-8 alkyl and >C.dbd.Z is >C.dbd.0 or ##STR2## are prepared by reacting a cyclopentane of the formula, ##STR3## wherein R.sub.2 is defined above and R is hydrogen or tetrahydropyranyl, with Wittig reagent of the formula,(R.sub.3).sub.3 P.dbd.CH(CH.sub.2).sub.3 COOMwherein R.sub.3 is aryl and M is alkali metal and, if necessary, hydrolyzing, or by oxidizing a compound of the formula, ##STR4## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.9 is tetrahydropyranyl group, with an oxidizing agent. The compounds (I) are useful as anti-ulcer agent.

摘要翻译： 其中R 1为氢或C 1-4烷基，R 2为C 4-8烷基且C = Z的式I的前列腺酸衍生物为：C = 0或，通过使 其中R 2如上所定义，R是氢或四氢吡喃基，与下式的维t希试剂（R 3）3 P = CH（CH 2）3 COOM，其中R 3是芳基，M是碱金属，如果需要，水解 或通过将氧化剂氧化下式的化合物，其中R 1和R 2如上定义，R 9为四氢吡喃基。 化合物（I）可用作抗溃疡剂。

公开(公告)号：US4125731A

公开(公告)日：1978-11-14

申请号：US748539

申请日：1976-12-08

申请人： Akihiko Sugie ,  Hiromi Shimomura ,  Junki Katsube ,  Hisao Yamamoto

发明人： Akihiko Sugie ,  Hiromi Shimomura ,  Junki Katsube ,  Hisao Yamamoto

IPC分类号： C07C17/32 ,  C07C33/38 ,  C07C405/00 ,  C07D307/93 ,  C07D309/12 ,  C07C69/76

CPC分类号： C07D309/12 ,  C07C17/32 ,  C07C33/38 ,  C07C405/00 ,  C07D307/93 ,  C07C2102/08 ,  Y10S514/927

摘要： Novel indan compounds of the formula ##STR1## wherein A and X are each ethylene or vinylene; B is C.sub.2-4 alkylene; R and R.sub.2 are each hydrogen or C.sub.1-4 alkyl; R.sub.1 is C.sub.1-8 alkyl;

摘要翻译： 式IMA的新型茚满化合物，其中A和X各自为亚乙烯基或亚乙烯基; B是C 2-4亚烷基; R和R 2各自为氢或C 1-4烷基; R1是C1-8烷基; 及其无毒盐，其可用作抗溃疡剂，胃分泌物抑制剂和假体。

公开(公告)号：US4110376A

公开(公告)日：1978-08-29

申请号：US605012

申请日：1975-08-15

申请人： Atsuyuki Kojima ,  Junki Katsube ,  Yoshito Kameno ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Atsuyuki Kojima ,  Junki Katsube ,  Yoshito Kameno ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： A61K31/135 ,  A61K31/13 ,  C07C20060101 ,  C07C67/00 ,  C07C209/00 ,  C07C209/50 ,  C07C211/26 ,  C07C87/32

CPC分类号： C07D401/12

摘要： Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.

摘要翻译： 下式的新型环丙基甲胺化合物：其中R 1和R 2各自为氢或卤素，R 3为氢或甲基，及其无毒盐，其具有各种有用的药理活性，可通过还原相应化合物 其中R 1，R 2和R 3各自如上所定义，或其无毒盐，或通过下式的相应化合物的缩合：其中R 1和R 2各自如上所定义，X为 常规的可互换基团如卤素或磺酰氧基与甲胺或二甲胺。

公开(公告)号：US4085210A

公开(公告)日：1978-04-18

申请号：US646908

申请日：1976-01-06

申请人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

发明人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

IPC分类号： C07D265/30 ,  C07D267/10 ,  C07D409/06 ,  A61K31/535 ,  C07D405/06

CPC分类号： C07D265/30 ,  C07D267/10

摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

摘要翻译： 式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> D-E-代表选自下组的三价基团：CH -CH 2 - 和> C = CH-且C 1和C 2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基，它们的无毒 盐，其可用作抗抑郁药并且可以通过各种方法制备。

公开(公告)号：US4017621A

公开(公告)日：1977-04-12

申请号：US635355

申请日：1975-11-26

申请人： Yoshinori Takashima ,  Isamu Maruyama ,  Junki Katsube

发明人： Yoshinori Takashima ,  Isamu Maruyama ,  Junki Katsube

IPC分类号： A61K20060101 ,  A61K31/535 ,  A61K31/55 ,  C07D20060101 ,  C07D223/14 ,  C07D223/22 ,  C07D223/24 ,  C07D233/14 ,  C07D265/30 ,  C07D413/06

摘要： Novel tricyclic compounds of the formula: ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH=CH-- or ##STR2## X is hydrogen, halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.3 -C.sub.6 cycloalkyl (C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl, polyhalo(C.sub.1 -C.sub.2)alkyl, C.sub.1 -C.sub.4 alkoxy(C.sub.1 -C.sub.3)alkyl or hydroxy(C.sub.1 -C.sub.3)alkyl, and non-toxic salts thereof which are useful as antidepressants and can be prepared by reduction of a compound of the formula: ##STR3## wherein A, X, R.sub.1, R.sub.2 and R.sub.3 are each as defined above.

摘要翻译： 新颖的下式的三环化合物：其中A是-CH 2 -CH 2 - ， - CH = CH-或X是氢，卤素，硝基，三氟甲基，C 1 -C 3烷基或C 1 -C 3烷氧基，R 1和 R 2各自为氢或C 1 -C 4烷基，R 3为氢，C 1 -C 4烷基，C 3 -C 5烯基，C 3 -C 5炔基，C 3 -C 6环烷基（C 1 -C 3）烷基，芳（C 1 -C 3）烷基，多卤代（ C1-C2）烷基，C1-C4烷氧基（C1-C3）烷基或羟基（C1-C3）烷基，及其无毒盐，可用作抗抑郁剂，可通过还原下式化合物来制备： IMAGE>其中A，X，R 1，R 2和R 3各自如上所定义。

公开(公告)号：US4482573A

公开(公告)日：1984-11-13

申请号：US550583

申请日：1983-11-10

申请人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

发明人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

IPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  C07C93/08

CPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  Y10S514/929

摘要： Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4) alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylamino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.4) alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in addition to the said nitrogen atom and, in case of having the additional nitrogen atom, bearing a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, and ar(C.sub.1 -C.sub.4)alkyl group or a phenyl group thereon), ##STR3## is a group of the formula: ##STR4## or the formula: ##STR5## A.sup.1 is a C.sub.2 -C.sub.6 alkylene group and A.sup.2 is a C.sub.2 -C.sub.4 alkylene group, and non-toxic, pharmaceutically acceptable acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.