公开(公告)号：US4533669A

公开(公告)日：1985-08-06

申请号：US469548

申请日：1983-02-25

申请人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

发明人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

IPC分类号： A61K31/415 ,  A61K31/445 ,  C07D233/54 ,  C07D233/56 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00

CPC分类号： C07D233/64 ,  A61K31/415 ,  A61K31/445 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： An anti-depressant imidazole compound of the formula: ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is hydrogen or lower alkyl, and R.sub.3, R.sub.4 and R.sub.5 are hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di-lower alkylamino, heterocyclic amino, halogen or ##STR2## (in which R.sub.6 is hydrogen, lower alkyl or lower alkylsulfonyl, A is carbonyl or sulfonyl, and R.sub.7 is lower alkyl, halogenated lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylaminoalkyl, unsubstituted phenyl or phenyl having halogen, lower alkyl, lower alkoxy or trifluoromethyl, phenylamino or phenylamino having halogen, lower alkyl, lower alkoxy or trifluoromethyl); and their pharmaceutically acceptable acid addition salts. These compounds are useful as agents for treating depression and depressive states.

摘要翻译： 一种下式的抗抑郁咪唑化合物：其中R1是低级烷基，R2是氢或低级烷基，R3，R4和R5是氢，低级烷基，三氟甲基，氨基，一或二低级烷基氨基， 杂环氨基，卤素或者其中R6是氢，低级烷基或低级烷基磺酰基，A是羰基或磺酰基，R7是低级烷基，卤代低级烷基，一或二低级烷基氨基，单 - 或二 - 低级烷基氨基烷基，未取代的苯基或具有卤素，低级烷基，低级烷氧基或三氟甲基的苯基，苯基氨基或具有卤素，低级烷基，低级烷氧基或三氟甲基的苯基氨基）。 及其药学上可接受的酸加成盐。 这些化合物可用作治疗抑郁和抑郁状态的药剂。

公开(公告)号：US4402966A

公开(公告)日：1983-09-06

申请号：US252674

申请日：1981-04-09

申请人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

发明人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

IPC分类号： A61K31/415 ,  A61K31/445 ,  C07D233/54 ,  C07D233/56 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00

CPC分类号： C07D233/64 ,  A61K31/415 ,  A61K31/445 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： An imidazole compound of the formula: ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is hydrogen or lower alkyl, and R.sub.3, R.sub.4 and R.sub.5 are hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di-lower alkylamino, heterocyclic amino, halogen or ##STR2## (in which R.sub.6 is hydrogen, lower alkyl or lower alkylsulfonyl, A is carbonyl or sulfonyl, and R.sub.7 is lower alkyl, halogenated lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylaminoalkyl, unsubstituted phenyl or phenyl having halogen, lower alkyl, lower alkoxy or trifluoromethyl, phenylamino or phenylamino having halogen, lower alkyl, lower alkoxy or trifluoromethyl); and their pharmaceutically acceptable acid addition salts.The compounds are useful for treating patients suffering from depression.

摘要翻译： 下式的咪唑化合物：其中R1是低级烷基，R2是氢或低级烷基，R3，R4和R5是氢，低级烷基，三氟甲基，氨基，一或二低级烷基氨基，杂环氨基， 卤素或（其中R6是氢，低级烷基或低级烷基磺酰基，A是羰基或磺酰基，R7是低级烷基，卤代低级烷基，一或二低级烷基氨基，一或二低级烷基氨基烷基， 未取代的苯基或具有卤素，低级烷基，低级烷氧基或三氟甲基的苯基，苯基氨基或具有卤素，低级烷基，低级烷氧基或三氟甲基的苯基氨基）; 及其药学上可接受的酸加成盐。 该化合物可用于治疗患有抑郁症的患者。

公开(公告)号：US4602031A

公开(公告)日：1986-07-22

申请号：US741935

申请日：1985-06-06

申请人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

发明人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

IPC分类号： A61K31/415 ,  A61K31/445 ,  C07D233/54 ,  C07D233/56 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00

CPC分类号： C07D233/64 ,  A61K31/415 ,  A61K31/445 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： An antidepressive imidazole compound of the formula: ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is hydrogen or lower alkyl, and R.sub.3, R.sub.4 and R.sub.5 are hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di-lower alkylamino, heterocyclic amino, halogen or ##STR2## (in which R.sub.6 is hydrogen, lower alkyl or lower alkylsulfonyl, A is carbonyl or sulfonyl, and R.sub.7 is lower alkyl, halogenated lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylaminoalkyl, unsubstituted phenyl or phenyl having halogen, lower alkyl, lower alkoxy or trifluoromethyl, phenylamino or phenylamino having halogen, lower alkyl, lower alkoxy or trifluoromethyl); and their pharmaceutically acceptable acid addition salts.

摘要翻译： 一种下式的抗抑郁咪唑化合物：其中R1是低级烷基，R2是氢或低级烷基，R3，R4和R5是氢，低级烷基，三氟甲基，氨基，一或二低级烷基氨基，杂环氨基 ，卤素或 - - （其中R6是氢，低级烷基或低级烷基磺酰基，A是羰基或磺酰基，R7是低级烷基，卤代低级烷基，一或二低级烷基氨基，一或二 低级烷基，低级烷氧基或三氟甲基，苯基氨基或苯基氨基，具有卤素，低级烷基，低级烷氧基或三氟甲基）; 及其药学上可接受的酸加成盐。

公开(公告)号：US4301169A

公开(公告)日：1981-11-17

申请号：US93469

申请日：1979-11-13

申请人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

发明人： Motosuke Yamanaka ,  Isao Saito ,  Kiyomi Yamatsu ,  Takako Fujimoto

IPC分类号： A61K31/415 ,  A61K31/445 ,  C07D233/54 ,  C07D233/56 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00

CPC分类号： C07D233/64 ,  A61K31/415 ,  A61K31/445 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： An imidazole compound of the formula: ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is hydrogen or lower alkyl, and R.sub.3, R.sub.4 and R.sub.5 are hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di-lower alkylamino, heterocyclic amino, halogen or ##STR2## (in which R.sub.6 is hydrogen, lower alkyl or lower alkylsulfonyl, A is carbonyl or sulfonyl, and R.sub.7 is lower alkyl, halogenated lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylaminoalkyl, unsubstituted phenyl or phenyl having halogen, lower alkyl, lower alkoxy or trifluoromethyl, phenylamino or phenylamino having halogen, lower alkyl, lower alkoxy or trifluoromethyl); and their pharmaceutically acceptable acid addition salts.

摘要翻译： 下式的咪唑化合物：其中R1是低级烷基，R2是氢或低级烷基，R3，R4和R5是氢，低级烷基，三氟甲基，氨基，一或二低级烷基氨基，杂环氨基， 卤素或（其中R6是氢，低级烷基或低级烷基磺酰基，A是羰基或磺酰基，R7是低级烷基，卤代低级烷基，一或二低级烷基氨基，一或二低级烷基氨基烷基， 未取代的苯基或具有卤素，低级烷基，低级烷氧基或三氟甲基的苯基，苯基氨基或具有卤素，低级烷基，低级烷氧基或三氟甲基的苯基氨基）; 及其药学上可接受的酸加成盐。

公开(公告)号：US4661630A

公开(公告)日：1987-04-28

申请号：US803526

申请日：1985-12-02

申请人： Yasuji Harigaya ,  Hiroo Ogura ,  Mitsuo Mihara ,  Motosuke Yamanaka ,  Kiyomi Yamatsu

发明人： Yasuji Harigaya ,  Hiroo Ogura ,  Mitsuo Mihara ,  Motosuke Yamanaka ,  Kiyomi Yamatsu

IPC分类号： A61K31/19 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P1/04 ,  A61P3/06 ,  A61P11/00 ,  A61P25/08 ,  A61P25/20 ,  A61P29/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C233/59 ,  C07C235/82 ,  C07D209/48 ,  C07C103/737

CPC分类号： C07D209/48

摘要： Described herein are novel carboxylic acid amide compounds or carboximide compounds represented by the general formula: ##STR1## wherein Z represents either the monoamido radical of an aromatic or cycloaliphatic ortho dicarboxylic acid or the amide of the corresponding anhydride, and their pharmaceutically acceptable salts; processes for the production thereof; and medicines containing the same. The novel compounds are useful as treating, preventing and improving agents for diseases attended with cerebral dysfunction as well as various symptoms caused by the said diseases.

摘要翻译： 本文描述的是由以下通式表示的新颖的羧酸酰胺化合物或羧甲酰化合物：其中Z表示芳族或脂环族邻二羧酸的单酰氨基或相应酸酐的酰胺及其药学上可接受的盐; 生产过程; 和含有它的药物。 该新化合物可用作治疗，预防和改善患有脑功能障碍的疾病以及由所述疾病引起的各种症状。

公开(公告)号：US4596826A

公开(公告)日：1986-06-24

申请号：US620050

申请日：1984-06-12

申请人： Yasuji Harigaya ,  Hiroo Ogura ,  Mitsuo Mihara ,  Motosuke Yamanaka ,  Kiyomi Yamatsu

发明人： Yasuji Harigaya ,  Hiroo Ogura ,  Mitsuo Mihara ,  Motosuke Yamanaka ,  Kiyomi Yamatsu

IPC分类号： A61K31/19 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P25/08 ,  A61P25/20 ,  C07C67/00 ,  C07C231/00 ,  C07C231/12 ,  C07C233/58 ,  C07C233/59 ,  C07C233/60 ,  C07C235/82 ,  C07D209/48 ,  C07C101/453 ,  A61K31/195

CPC分类号： C07D209/48

摘要： Described herein are novel carboxylic acid amide compounds or carboximide compounds represented by the general formula: ##STR1## wherein Z represents a group of the formula (1) or (2): ##STR2## wherein R.sup.1 and R.sup.2 are hydrogen atom or methyl group, respectively; Xs, which may be the same or different, are hydrogen atom, a lower alkyl, lower alkoxy, halo, or alkyl halide group, respectively, and n represents an integer of 0 to 2, and their pharmaceutically acceptable salts; process for the production thereof; and medicines containing the same. The novel compounds are useful as treating, preventing and improving agents for diseases attended with cerebral dysfunction as well as various symptoms caused by the said diseases. Further, the compounds are useful for the improvement of neurosis of the stomach; and treatment and prevention for various constipation.

摘要翻译： 本文描述的是由以下通式表示的新颖的羧酸酰胺化合物或羧甲酰化合物：其中Z代表式（1）或（2）的基团：其中 R1和R2分别是氢原子或甲基; 分别为氢原子，低级烷基，低级烷氧基，卤素或卤代烷基，n表示0〜2的整数，以及它们的药学上可接受的盐，其可以相同或不同。 生产过程; 和含有它的药物。 该新化合物可用作治疗，预防和改善患有脑功能障碍的疾病以及由所述疾病引起的各种症状。 此外，该化合物可用于改善胃的神经症; 治疗和预防各种便秘。

公开(公告)号：US4285939A

公开(公告)日：1981-08-25

申请号：US137753

申请日：1980-04-07

申请人： Yoshimasa Machida ,  Isao Saito ,  Motosuke Yamanaka ,  Seiichiro Nomoto ,  Shigeto Negi ,  Kyosuke Kitoh ,  Kanemasa Katsu ,  Yukio Ohya ,  Takeshi Suzuki ,  Kyoko Koizumi

发明人： Yoshimasa Machida ,  Isao Saito ,  Motosuke Yamanaka ,  Seiichiro Nomoto ,  Shigeto Negi ,  Kyosuke Kitoh ,  Kanemasa Katsu ,  Yukio Ohya ,  Takeshi Suzuki ,  Kyoko Koizumi

IPC分类号： C07D501/22 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D311/22 ,  C07D501/34 ,  C07D501/20

CPC分类号： C07D311/22

摘要： New cephalosporin derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 each represents hydroxy, acyloxy, and hydrogen provided that two or three of R.sub.1, R.sub.2, and R.sub.3 are not hydrogen at the same time, and their salts, and processes for the preparation thereof. The cephalosporin derivatives of the present invention are useful as antibacterial drugs.

摘要翻译： 由以下通式表示的新型头孢菌素衍生物：其中R 1，R 2和R 3各自表示羟基，酰氧基和氢，条件是R 1，R 2和R 3中的两个或三个不同时为氢， ，及其制备方法。 本发明的头孢菌素衍生物可用作抗菌药物。

公开(公告)号：US5559225A

公开(公告)日：1996-09-24

申请号：US209484

申请日：1994-03-14

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

摘要翻译： 由下式（1）表示的7-酰基-3-取代氨基甲酰氧基头孢烯化合物：其中A表示-CH =或-N =基团; R1表示羟基，低级烷氧基或被保护的羟基; R2和R3相同或不同，分别表示低级烷基，羟基取代的低级烷基，氨基甲酰取代的低级烷基或氰基取代的低级烷基，R2是氢原子，R3是低级烷氧基或烷基 任选地被一个或多个卤素原子取代，或者“IMAGE”是指含有一个氮原子或吗啉基的4-6元杂环基，所述杂环基或吗啉基任选被一个或多个低级烷基 ，羟基和/或羟基取代的低级烷基; R4表示羧基或被保护的羧基; 或其药学上可接受的盐; 及其制备方法; 以及含有上述头孢烯化合物的抗菌组合物。

公开(公告)号：US5179095A

公开(公告)日：1993-01-12

申请号：US798963

申请日：1991-11-26

申请人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

发明人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

IPC分类号： C07D211/28 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/10

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/10

摘要： A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sup.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, CH.sup.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## 1 being 1 or 2, --A--B, A being --(CH.sub.2).sub.n --, n being an integer of 1 to 5,a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkene having a double bond formed between carbon atoms adjacent to each other by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,--(CH.sub.2)k--S--, k being an integer of 2 to 5, --(CH.sub.2)p--CO--, p being an integer of 1 to 4, B being cyano, --NR.sub.4 R.sub.5, a heterocyclic ring or a condensed aromatic ring.

摘要翻译： 新的哌啶化合物在治疗心律失常方面是药理学有效的，并由下式定义：其中R1是低级烷基或甲苯基，R2是氢，羟基，低级烷氧基或低级烷基，R3是氢 低级烷基，低级烯基，环烷基或环烷基烷基，X为-CO-，-CH 2 - 或-CHOH-，g为1〜3的整数，h为1〜3的整数，Y为氢 ，低级烷基，低级烯基，氰基，CH 2 COOR，R为氢或低级烷基，环烷基，环烷基烷基，A为1或2，-AB，A为 - （CH 2）n - ，n为 1至5的整数，具有1至5个碳原子的直链亚烷基，其是衍生自直接与一个或多个碳原子键合的低级烷基，苯基或羟基的直链烷烃的二价基团 通过除去与位于其两端的每个碳原子键合的氢原子构成所述烷烃，具有1至5个碳原子的直链亚烷基，其是 通过除去与位于其两端的每个碳原子键合的氢原子，通过除去彼此相邻的碳原子之间形成的双键的直链烯烃的二价基团， - （CH 2）k S - ，k为 2〜5的整数， - （CH 2）p -CO-，p为1〜4的整数，B为氰基，-NR 4 R 5，杂环或稠合芳环。

公开(公告)号：US4803276A

公开(公告)日：1989-02-07

申请号：US107473

申请日：1987-10-09

申请人： Motosuke Yamanaka ,  Kazutoshi Miyake ,  Shinji Suda ,  Hideto Ohhara ,  Toshiaki Ogawa

发明人： Motosuke Yamanaka ,  Kazutoshi Miyake ,  Shinji Suda ,  Hideto Ohhara ,  Toshiaki Ogawa

IPC分类号： C07D213/64 ,  A61K31/435 ,  A61K31/437 ,  A61K31/44 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  C07D213/78 ,  C07D471/04

CPC分类号： C07D471/04

摘要： Novel 1-(imidazo[1,2-a]pyridin-6-yl)-2-alkanone derivatives and (imidazo [1,2-a]pyridin-6-yl) acetaldehyde derivatives are provided. The novel derivatives are intermediates for the production of 5-(6-imidazo[1,2-a]pyridyl)pyridine derivatives which are useful as cardiotonics.