公开(公告)号：US4730052A

公开(公告)日：1988-03-08

申请号：US753162

申请日：1985-07-09

申请人： Yoshimoto Nakashima ,  Toshihisa Ogawa ,  Atsuro Nakazato ,  Yukinari Kumazawa ,  Kaoru Sota

发明人： Yoshimoto Nakashima ,  Toshihisa Ogawa ,  Atsuro Nakazato ,  Yukinari Kumazawa ,  Kaoru Sota

IPC分类号： C07D211/90

CPC分类号： C07D211/90

摘要： Unsymmetrical 1,4-dihydropyridine-3,5-dicarboxylic acid diesters represented by the general formula ##STR1## wherein R.sup.1 and R.sup.2 are different and represent each a nitratoalkyl having 2 or 3 carbon atoms, are prepared from the corresponding acid monoester in the presence of an organic acid anhydride activating agent. These compounds are useful as therapeutic agents for cardiovascular disorders.

摘要翻译： 由通式“IMAGE”表示的不对称的1,4-二氢吡啶-3,5-二羧酸二酯，其中R 1和R 2不同并表示各自具有2或3个碳原子的硝基烷基，在相应的酸单酯存在下制备 的有机酸酐活化剂。 这些化合物可用作心血管疾病的治疗剂。

公开(公告)号：US4686292A

公开(公告)日：1987-08-11

申请号：US838153

申请日：1986-03-10

申请人： Yoshihiro Migita ,  Tadashi Eguchi ,  Yukinari Kumazawa ,  Jozi Nakagami ,  Takehiro Amano ,  Kaoru Sota ,  Jinsaku Sakakibara

发明人： Yoshihiro Migita ,  Tadashi Eguchi ,  Yukinari Kumazawa ,  Jozi Nakagami ,  Takehiro Amano ,  Kaoru Sota ,  Jinsaku Sakakibara

IPC分类号： A61K31/495 ,  A61P35/00 ,  C07D241/38 ,  C07D241/46 ,  C07D401/06 ,  C07D403/06

CPC分类号： C07D241/38

摘要： Novel benzo[.alpha.]phenazine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, methyl, hydroxyl or alkoxy, R.sup.2 is --COOR.sup.5 (wherein R.sup.5 is hydrogen, straight or branched chain alkyl, cycloalkyl having 3-6 carbon atoms, benzyl or phenyl) or ##STR2## wherein R.sup.6 and R.sup.7 are the same or different and are each hydrogen or lower alkyl, or R.sup.6 and R.sup.7 together with the nitrogen atom to which they are attached form pyrrolidine or piperidine), R.sup.3 and R.sup.4 are the same or different and are each hydrogen or lower alkyl, and n is an integer of 2 or 3, and the salts thereof are disclosed. These compounds have antitumor activity in mammals.

摘要翻译： 式（I）的新的苯并[b]吩嗪衍生物其中R 1是氢，卤素，甲基，羟基或烷氧基，R 2是-COOR 5（其中R 5是氢，直链或支链烷基，具有3-6 碳原子，苄基或苯基）或其中R6和R7相同或不同并且各自为氢或低级烷基，或R6和R7与它们所连接的氮原子一起形成吡咯烷或哌啶），R3和 R4相同或不同，各自为氢或低级烷基，n为2或3的整数，并且其盐被公开。 这些化合物在哺乳动物中具有抗肿瘤活性。

公开(公告)号：US4594197A

公开(公告)日：1986-06-10

申请号：US646230

申请日：1984-08-31

申请人： Kazuyuki Tomisawa ,  Kazuya Kameo ,  Toru Matsunaga ,  Shiuji Saito ,  Yoshimoto Nakashima ,  Kaoru Sota

发明人： Kazuyuki Tomisawa ,  Kazuya Kameo ,  Toru Matsunaga ,  Shiuji Saito ,  Yoshimoto Nakashima ,  Kaoru Sota

IPC分类号： A61K31/195 ,  A61K31/19 ,  A61K31/194 ,  A61K31/215 ,  A61P3/00 ,  A61P29/00 ,  A61P37/04 ,  C07C59/84 ,  C07C59/88 ,  C07C59/90 ,  C07C67/00 ,  C07C313/00 ,  C07C323/56 ,  C07C327/20 ,  C07C327/22 ,  C07C149/40 ,  C07C153/023 ,  C07C157/09

CPC分类号： C07C327/00 ,  C07C323/00 ,  C07C59/84 ,  C07C59/88 ,  C07C59/90

摘要： 3-Benzoyl-2-mercaptopropionic acid derivatives represented by the general formula ##STR1## (wherein, X represents a hydrogen atom, a halogen atom, hydroxy group, a lower alkyl group or a lower alkoxy group, Y represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, Z represents a hydrogen atom or an acyl group, and R represents a hydrogen atom or a lower alkyl group). These compounds have immunomodulative function and are effective for the treatment of diseases caused by abnormal immunofunction.

摘要翻译： 由通式“IMAGE”表示的3-苯甲酰基-2-巯基丙酸衍生物（其中，X表示氢原子，卤素原子，羟基，低级烷基或低级烷氧基，Y表示氢原子， 卤素原子，低级烷基或低级烷氧基，Z表示氢原子或酰基，R表示氢原子或低级烷基）。 这些化合物具有免疫调节功能，对于治疗异常免疫功能引起的疾病有效。

公开(公告)号：US4803266A

公开(公告)日：1989-02-07

申请号：US104152

申请日：1987-10-05

申请人： Yutaka Kawashima ,  Masakazu Satoh ,  Yuichi Hatada ,  Fumiko Hazato ,  Yoshimoto Nakashima ,  Kaoru Sota

发明人： Yutaka Kawashima ,  Masakazu Satoh ,  Yuichi Hatada ,  Fumiko Hazato ,  Yoshimoto Nakashima ,  Kaoru Sota

IPC分类号： C07D205/08 ,  A61K31/395 ,  A61K31/397 ,  A61P7/02 ,  C07D205/10 ,  C07D405/04

CPC分类号： C07D205/10

摘要： 2-Azetidione derivatives represented by the following formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group or a cyano group, l is 1 or 2, R.sup.1 is a lower alkyl group, a cycloalkyl group, a 1-naphthylmethyl group, an optionally substituted phenethyl group, an optionally substituted phenyl group, an optionally substituted benzyl group or a bis(alkoxycarbonyl)ethyl group, and R.sup.2 is a lower alkyl group, a lower alkoxy group, an amino group, an adamantyl group, a lower alkoxycarbonylmethyl group or an optionally substituted phenyl group, are disclosed. These compounds are useful as blood platelet aggregation inhibiting agents.

公开(公告)号：US4150240A

公开(公告)日：1979-04-17

申请号：US813989

申请日：1977-07-08

申请人： Kaoru Sota ,  Toshihisa Ogawa ,  Jiro Sawada

发明人： Kaoru Sota ,  Toshihisa Ogawa ,  Jiro Sawada

IPC分类号： C07C319/02 ,  C07C67/00 ,  C07C313/00 ,  C07C323/58 ,  C07C99/00

摘要： D-Penicillamine and salts thereof may be prepared by reacting certain aryl amines with 4-thiazolidinecarboxylic acid compounds obtained by splitting the .beta.-lactam ring of penicillin derivatives such as benzylpenicillin or phenoxymethylpenicillin.

摘要翻译： D-青霉胺及其盐可以通过使某些芳基胺与通过分解青霉素衍生物例如苄青霉素或苯氧基甲基青霉素的β-内酰胺环获得的4-噻唑烷羧酸化合物反应来制备。

公开(公告)号：US4885367A

公开(公告)日：1989-12-05

申请号：US271641

申请日：1988-11-16

申请人： Kensei Yoshikawa ,  Yutaka Ohuchi ,  Kazuto Sekiuchi ,  Shiuji Saito ,  Katsuo Hatayama ,  Kaoru Sota

发明人： Kensei Yoshikawa ,  Yutaka Ohuchi ,  Kazuto Sekiuchi ,  Shiuji Saito ,  Katsuo Hatayama ,  Kaoru Sota

IPC分类号： C07C311/08 ,  C07C311/09 ,  C07C317/40 ,  C07C323/35 ,  C07D211/46 ,  C07D309/12 ,  C07D335/02

CPC分类号： C07D211/46 ,  C07C311/08 ,  C07C311/09 ,  C07C317/40 ,  C07C323/35 ,  C07D309/12 ,  C07D335/02 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2101/18 ,  C07C2102/42

摘要： Sulfonanilide compounds represented by the formula ##STR1## wherein R.sup.1 is a lower alkyl group or a trifluoromethyl group, R.sup.2 is a cycloalkylidenemethyl group, a group of the formula --A--R.sup.3 (wherein A is an oxygen atom, a sulfur atom, a sulfynyl group or a sulfinyl group and R.sup.3 is a cycloalkyl group having 5-8 carbon atoms; a cycloalkyl group having 5-8 carbon atoms substituted by one or two of a lower alkyl group, an oxo group, a hydroxyl group or a methanesulfonyloxy group, a tetrahydropyranyl group; a tetrahydrothiopyranyl group; or a 1-methyl-piperidyl group) or a group of the formula --B--R.sup.4 (wherein B is a carbonyl group, a hydroxymethylene group or a methylene group, R.sup.4 is a cycloalkyl group having 5-8 carbon atoms) and the pharmaceutically acceptable salts thereof have anti-inflammatory activity.

公开(公告)号：US4812562A

公开(公告)日：1989-03-14

申请号：US887941

申请日：1986-07-22

申请人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Kaoru Sota

发明人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Kaoru Sota

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/36 ,  C07D501/59

CPC分类号： C07D501/59 ,  Y02P20/55

摘要： Cephalosporin derivatives represented by the general formula ##STR1## wherein X represents a halogen atom, a hydroxyl group, a cyano group, a trifluoromethyl group, an amino group, a lower alkylcarbonylamino group, a lower alkoxy group, a lower alkylthio group, a lower alkoxycarbonyl group, a carbamoyl group, a substituted carbamoyl group, a carbamoyloxy group, a lower alkylcarbonyl group, a lower alkenyl group, an ethynyl group, a thiocyanate group, an .alpha.-carboxyaminomethyl group, a phenyl group, a pyridinyl group or an aminothiazolyl group, and n is an integer of 1 to 3, and the non-toxic salts thereof, are disclosed. These compounds are useful as antibacterial agents.

摘要翻译： 由通式表示的头孢菌素衍生物，其中X表示卤素原子，羟基，氰基，三氟甲基，氨基，低级烷基羰基氨基，低级烷氧基，低级烷硫基，低级 烷氧基羰基，氨基甲酰基，取代氨基甲酰基，氨基甲酰氧基，低级烷基羰基，低级烯基，乙炔基，硫氰酸酯基，α-羧基氨基甲基，苯基，吡啶基或氨基噻唑基 基，n为1〜3的整数，并且其无毒盐被公开。 这些化合物可用作抗菌剂。

公开(公告)号：US4680386A

公开(公告)日：1987-07-14

申请号：US789771

申请日：1985-10-21

申请人： Shigeo Morimoto ,  Takashi Adachi ,  Toshifumi Asaka ,  Yoshiaki Watanabe ,  Kaoru Sota

发明人： Shigeo Morimoto ,  Takashi Adachi ,  Toshifumi Asaka ,  Yoshiaki Watanabe ,  Kaoru Sota

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08

摘要： A novel 6-O-methylerythromycin A derivative represented by the formula ##STR1## and the salts thereof are disclosed. These compounds are useful as intermediates for preparation of 6-O-methylerythromycin A and useful as antibiotics.

摘要翻译： 公开了由式“IMAGE”表示的新型6-O-甲基红霉素A衍生物及其盐。 这些化合物可用作制备6-O-甲基红霉素A并用作抗生素的中间体。

公开(公告)号：US4990602A

公开(公告)日：1991-02-05

申请号：US283387

申请日：1988-12-12

申请人： Shigeo Morimoto ,  Takashi Adachi ,  Tohru Matsunaga ,  Masato Kashimura ,  Toshifumi Asaka ,  Yoshiaki Watanabe ,  Kaoru Sota ,  Kazuto Sekiuchi

发明人： Shigeo Morimoto ,  Takashi Adachi ,  Tohru Matsunaga ,  Masato Kashimura ,  Toshifumi Asaka ,  Yoshiaki Watanabe ,  Kaoru Sota ,  Kazuto Sekiuchi

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： Erthromycin A derivatives represented by the general formula ##STR1## wherein R.sup.1 is a group of the formula R.sup.7 CH.sub.2 -- (wherein R.sup.7 is a hydrogen group or a lower alkyl group) or a group of the formula R.sup.8 O-- (wherein R.sup.8 is a lower alkyl group), R.sup.2 is R.sup.8, a cycloalkyl group, a phenyl group or an aralkyl group.), or R.sup.2 and R.sup.7 together form an alkylene group, R.sup.3 is a hydrogen atom, a lower alkyl group, a phenyl group or an aralkyl group, or R.sup.3 and R.sup.7 together form an alkylene group, or R.sup.2 and R.sup.3 together form an alkylene group, R.sup.4 is a lower alkyl group, R.sup.5 is a substituted silyl group, and R.sup.6 is a hydrogen atom or R.sup.5, are disclosed. These compounds are useful as intermediates for the synthesis of antibacterial agents.

公开(公告)号：US4841044A

公开(公告)日：1989-06-20

申请号：US943037

申请日：1986-12-18

申请人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Minoru Taguchi ,  Kaoru Sota

发明人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Minoru Taguchi ,  Kaoru Sota

IPC分类号： A61K31/545 ,  C07D501/36 ,  C07D501/59

CPC分类号： C07D501/59

摘要： Cephalosporin derivatives represented by the general formula ##STR1## wherein R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R' is a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, or R and R' together with the nitrogen atom to which they are attached form a tetrahydropyridinyl group, a morpholinyl group or pyrroridinyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.

摘要翻译： 其中R为氢原子或碳原子数为1〜4的低级烷基，R'为氢原子，碳原子数1〜4的低级烷基， ，具有5或6个碳原子的环烷基或苄基，或R和R'与它们所连接的氮原子一起形成四氢吡啶基，吗啉基或吡咯烷基，其无毒盐是 披露 这些化合物可用作抗菌剂。