公开(公告)号：US4563455A

公开(公告)日：1986-01-07

申请号：US587981

申请日：1984-03-09

申请人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano ,  Atsushi Akahane

发明人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano ,  Atsushi Akahane

IPC分类号： A61K31/415 ,  A61P1/04 ,  C07D235/10 ,  C07D235/12 ,  C07D401/06 ,  C07D403/06 ,  C07D417/06 ,  C07D471/04 ,  C07D521/00 ,  A61K31/53

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D235/10 ,  C07D235/12 ,  C07D249/08 ,  C07D401/06 ,  C07D403/06 ,  C07D417/06 ,  C07D471/04

摘要： New fused imidazole compounds of the formula: ##STR1## wherein A is lower alkylene,R.sup.1 is hydrogen, lower alkyl, lower alkoxy or halogen,R.sup.2 is hydrogen, lower alkyl, cyclo(lower)alkyl, pyridyl, ar(lower)alkyl which may be substituted with halogen, or aryl which may be substituted with lower alkyl, lower alkoxy, hydroxy or halogen,R.sup.3 is N-containing unsaturated heterocyclic group which may be substituted with lower alkyl or amino, andY is .dbd.C-- or .dbd.N--,and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and salts thereof are useful as antiulcer agents.

摘要翻译： 其中A为低级亚烷基，R 1为氢，低级烷基，低级烷氧基或卤素，R 2为氢，低级烷基，环（低级）烷基，吡啶基，Ar（低级）烷基， 可以被卤素取代，或可以被低级烷基，低级烷氧基，羟基或卤素取代的芳基，R3是可被低级烷基或氨基取代的含N不饱和杂环基，Y是=或= N - 及其药学上可接受的盐，及其制备方法和包含其的药物组合物。 这些衍生物和其盐可用作抗溃疡剂。

公开(公告)号：US4564621A

公开(公告)日：1986-01-14

申请号：US535298

申请日：1983-09-23

申请人： Ikuo Ueda ,  Masanobu Nagano ,  Atsushi Akahane

发明人： Ikuo Ueda ,  Masanobu Nagano ,  Atsushi Akahane

IPC分类号： C07D401/12 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P1/04 ,  C07D213/56 ,  C07D213/57 ,  C07D213/38

CPC分类号： C07D213/57 ,  C07D213/56

摘要： New .alpha.-aryl-.alpha.-pyridylalkanoic acid derivatives of the formula: ##STR1## wherein R.sup.1 is cyano or carbamoyl,R.sup.2 is hydrogen or halogen,R.sup.3 is hydrogen or lower alkyl,one of R.sup.4 and R.sup.5 is hydrogen and another is lower alkyl,R.sup.6 is hydrogen or lower alkyl, andR.sup.7 is lower alkyl, orR.sup.6 and R.sup.7 are taken together to form an N-containing saturated heterocyclic group with the adjacent nitrogen atom, in which the heterocyclic group may be substituted with lower alkyl or optionally protected hydroxy(lower)alkyl,provided that R.sup.2 is halogen or R.sup.3 is lower alkyl, when R.sup.1 is cyano and R.sup.6 and R.sup.7 are each lower alkyl, and salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and salts thereof are useful as antiulcer agents and spasmolytic agents.

摘要翻译： 新颖的下式的α-芳基-α-吡啶基链烷酸衍生物：其中R 1是氰基或氨基甲酰基，R 2是氢或卤素，R 3是氢或低级烷基，R 4和R 5之一是氢，另一个是低级烷基， R6是氢或低级烷基，R7是低级烷基，或R6和R7一起形成含有相邻氮原子的含氮饱和杂环基，其中杂环基可以被低级烷基或任选被保护的羟基取代 （低级）烷基，条件是当R 1为氰基且R 6和R 7为低级烷基时，R 2为卤素或R 3为低级烷基，及其盐及其制备方法和包含其的药物组合物。 这些衍生物和其盐可用作抗溃疡剂和溶解裂解剂。

公开(公告)号：US4543356A

公开(公告)日：1985-09-24

申请号：US455411

申请日：1983-01-03

申请人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano

发明人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P37/08 ,  C07D239/74 ,  C07D239/80 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D265/26 ,  C07D405/12 ,  C07D487/04 ,  C07D487/14

CPC分类号： C07D265/26 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D487/04

摘要： This invention is directed to new quinazoline derivatives of the following formula having use in the treatment of symptoms associated with allergic manifestations. ##STR1## wherein R.sub.a.sup.1 and R.sub.b.sup.1 are C.sub.2 -C.sub.7 alkoxycarbonyl or R.sub.a.sup.1 and R.sub.b.sup.1 is linked together to form a group of the formula: ##STR2## R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, amino, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylpiperazinyl, C.sub.1 -C.sub.18 alkanoylamino, di(C.sub.1 -C.sub.6)alkanoylamino, C.sub.3 -C.sub.9 alkoxalylamino, C.sub.4 -C.sub.8 cycloalkylcarbonylamino, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkanoylamino, benzamido, phenyl(C.sub.1 -C.sub.6)alkanoylamino, C.sub.1 -C.sub.6 alkylsulfonylamino or di(C.sub.1 -C.sub.6)alkylamino which may be substituted with hydroxy,A.sup.1 is a group of the formula: ##STR3## in which R.sup.4 is hydrogen C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkenyloxy, di(C.sub.1 -C.sub.6)alkylamino or 2,2-di(C.sub.1 -C.sub.6)alkoxycarbonylvinylamino, andR.sup.5 is C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl,or pharmaceutically acceptable salt thereof.

公开(公告)号：US4377580A

公开(公告)日：1983-03-22

申请号：US210340

申请日：1980-11-25

申请人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano

发明人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P37/08 ,  C07D239/74 ,  C07D239/80 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D265/26 ,  C07D405/12 ,  C07D487/04 ,  C07D487/14 ,  C07D471/14

CPC分类号： C07D265/26 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D487/04

摘要： Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.

摘要翻译： 下式的喹唑啉衍生物：其中A 1是A，其中R 1是氢，羧基或酯化的羧基，R 1a和R b1是酯化的羧基，R 2和R 3是氢，烷基，卤素，硝基，氨基， 烷氧基，芳氧基，烷硫基，烷基哌嗪基，酰氨基或可被羟基取代的二烷基氨基，R 4是氢，烷基，羟基，烷氧基，烯氧基，二烷基氨基或2,2-二烷氧基羰基乙烯基氨基R 4a是氢，烷基，羟基，烷氧基，烯氧基或二烷基氨基 R 5为烷基或烯基，R 6为羧基或酯化羧基。

公开(公告)号：US4686227A

公开(公告)日：1987-08-11

申请号：US745638

申请日：1985-06-17

申请人： Ikuo Ueda ,  Youichi Shiokawa ,  Masayuki Kato ,  Nobukiyo Konishi ,  Atsushi Akahane

发明人： Ikuo Ueda ,  Youichi Shiokawa ,  Masayuki Kato ,  Nobukiyo Konishi ,  Atsushi Akahane

IPC分类号： C07D471/04 ,  A61K31/47 ,  A61P1/04 ,  C07D487/04 ,  A61K31/395 ,  C07D405/04

CPC分类号： C07D487/04

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.3 is hydrogen, halogen or ar(lower)alkoxy, andR is lower alkanoyl, nitroso, amino, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, haloformyl, aminomethyleneamino which may be substituted with cyano or lower alkyl, iminomethylamino which may be substituted with cyano or lower alkyl, or a group of the formula: --A--R.sup.2 in whichA is lower alkylene andR.sup.2 is di(lower)alkylamino, cyano, lower alkoxy, N-containing heterocyclic group which may have suitable substituent(s), lower alkynyloxy, lower alkenyloxy, lower alkylthio, amino(lower)alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, hydroxy, lower alkanoyloxy, heterocyclicamino (lower)alkylthio having two oxo groups, hydrogen or a group of the formula: ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are each lower alkyl andX is an acid residue,and pharmaceutically acceptable salts thereof.The compounds are useful as anti ulcer agents.

摘要翻译： 下式的化合物，其中R 1为低级烷基，R 3为氢，卤素或芳（低级）烷氧基，R为低级烷酰基，亚硝基，氨基，羧基，酯化羧基，氨基甲酰基，羟基氨基甲酰基，卤代甲酰基，氨基亚甲基氨基 可以被氰基或低级烷基取代，可以被氰基或低级烷基取代的亚氨基甲基氨基，或下列基团：其中A是低级亚烷基，R2是二（低级）烷基氨基，氰基，低级烷氧基 ，可具有适当取代基的含N杂环基，低级炔氧基，低级烯氧基，低级烷硫基，氨基（低级）烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，羧基，酯化羧基，氨基甲酰基，羟基氨基甲酰基，羟基，低级烷酰氧基， 具有两个氧代基的杂环氨基（低级）烷硫基，氢或下式的基团：其中R 4，R 5和R 6各自为低级烷基，X为酸残基，及其药学上可接受的盐。 该化合物可用作抗溃疡剂。

公开(公告)号：US4429126A

公开(公告)日：1984-01-31

申请号：US384998

申请日：1982-06-04

申请人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano

发明人： Ikuo Ueda ,  Masayuki Kato ,  Masanobu Nagano

IPC分类号： C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D265/26 ,  C07D487/04 ,  A61K31/505 ,  C07D239/80 ,  C07D471/14

CPC分类号： C07D487/04 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D265/26

摘要： Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.

摘要翻译： 喹啉衍生物，其结构式如下：其中A1是甲基，R1是氢，羧基或酯化的羧基，Ra1和Rb1是酯化的羧基，R2和R3是氢，烷基，卤素，硝基 ，可以被羟基取代的氨基，烷氧基，芳氧基，烷硫基，烷基哌嗪基，酰基氨基或二烷基氨基，R 4是氢，烷基，羟基，烷氧基，烯氧基，二烷基氨基或2,2-二烷氧基羰基乙烯基氨基R 4a是氢，烷基，羟基，烷氧基， 烯氧基或二烷基氨基，R 5是烷基或烯基，R 6是羧基或酯化的羧基。

公开(公告)号：US4738967A

公开(公告)日：1988-04-19

申请号：US945788

申请日：1986-12-23

申请人： Ikuo Ueda ,  Youichi Shiokawa ,  Masayuki Kato ,  Nobukiyo Konishi ,  Atsushi Akahane

发明人： Ikuo Ueda ,  Youichi Shiokawa ,  Masayuki Kato ,  Nobukiyo Konishi ,  Atsushi Akahane

IPC分类号： C07D471/04 ,  A61K31/47 ,  A61P1/04 ,  C07D487/04 ,  A61K31/40

CPC分类号： C07D487/04

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.3 is hydrogen, halogen or ar(lower)alkoxy, andR is lower alkanoyl, nitroso, amino, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, haloformyl, aminomethyleneamino which may be substituted with cyano or lower alkyl, iminomethylamino which may be substituted with cyano or lower alkyl, or a group of the formula: --A--R.sup.2 in which A is lower alkylene andR.sup.2 is di(lower) alkylamino, cyano, lower alkoxy, N-containing heterocyclic group which may have suitable substituent(s), lower alkynyloxy, lower alkenyloxy, lower alkylthio, amino(lower)alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, hydroxy, lower alkanoyloxy, heterocyclicamino(lower)alkylthio having two oxo groups, hydrogen or a group of the formula: ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are each lower alkyl andX is an acid residue,and pharmaceutically acceptable salts thereof. pa The compounds are useful as anti ulcer agents.

公开(公告)号：US4354022A

公开(公告)日：1982-10-12

申请号：US270876

申请日：1981-06-05

申请人： Takao Takaya ,  Takashi Masugi ,  Toshiyuki Chiba ,  Akiteru Yoshioka ,  Masayuki Kato ,  Ikuo Ueda ,  Masakazu Kobayashi

发明人： Takao Takaya ,  Takashi Masugi ,  Toshiyuki Chiba ,  Akiteru Yoshioka ,  Masayuki Kato ,  Ikuo Ueda ,  Masakazu Kobayashi

IPC分类号： C07D501/04

CPC分类号： C07D501/04

摘要： A new process for preparing 3-methylenecepham compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group, andR.sup.2 is a carboxy or a protected carboxy group,or a salt thereof,which comprises reducing a compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, andR.sup.3 is halogen or heterocyclicthio which may have suitable sutstituent, or a salt thereof, with a combination of a metal selected from the group consisting of zinc, tin and iron, and an ammonium salt of an acid selected from the group consisting of ammonium halide, ammonium carbonate and ammonium acetate, said 3-methylenecepham compounds being useful as intermediates for preparing antimicrobially active 3-cephem compounds.

摘要翻译： 一种制备下式的3-亚甲基头孢烯化合物的新方法：其中R1为氨基或被保护的氨基，R2为羧基或被保护的羧基，或其盐，其包括将式 ：其中R 1和R 2各自如上所定义，并且R 3是可以具有合适取代基的卤素或杂环硫基，或其盐与选自锌，锡和铁的金属的组合，和 选自卤化铵，碳酸铵和乙酸铵的酸的铵盐，所述3-亚甲基头孢烯化合物可用作制备抗微生物活性3-头孢烯化合物的中间体。

公开(公告)号：US4563453A

公开(公告)日：1986-01-07

申请号：US658683

申请日：1984-10-09

申请人： Ikuo Ueda ,  Masayuki Kato ,  Yosiharu Kasai

发明人： Ikuo Ueda ,  Masayuki Kato ,  Yosiharu Kasai

IPC分类号： C07D513/04 ,  A61K31/54 ,  C07D513/14

CPC分类号： C07D513/04

摘要： New thiazine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen or acyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkyl or lower alkoxy,Z is taken together with the adjacent carbon atoms to form an unsaturated heterocyclic ring which may be substituted with phenyl, halogen, acyl or lower alkyl, andthe heavy solid line means single or double bond,and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and salts thereof are useful as antiinflammatory, analgesic and antirheumatic agents.

摘要翻译： 下式的新的噻嗪衍生物：其中R 1是氢或酰基，R 2是氢或低级烷基，R 3是氢，羟基，卤素，低级烷基或低级烷氧基，Z与相邻碳原子一起形成 可被苯基，卤素，酰基或低级烷基取代的不饱和杂环，重实线表示单键或双键，及其药学上可接受的盐，及其制备方法和包含其的药物组合物。 这些衍生物和盐可​​用作抗炎，镇痛和抗风湿剂。

公开(公告)号：US4443443A

公开(公告)日：1984-04-17

申请号：US213232

申请日：1980-12-05

申请人： Ikuo Ueda ,  Masaaki Matsuo ,  Kiyoshi Tsuji ,  Masayuki Kato

发明人： Ikuo Ueda ,  Masaaki Matsuo ,  Kiyoshi Tsuji ,  Masayuki Kato

IPC分类号： C07D209/48 ,  C07D257/04 ,  C07D277/20 ,  C07D295/13 ,  C07D295/205 ,  C07D501/36 ,  A61K31/545

CPC分类号： C07D209/48 ,  C07D257/04 ,  C07D277/587 ,  C07D295/13 ,  C07D295/205 ,  Y02P20/55

摘要： This invention relates to novel cephem compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is carboxy or a protected carboxy group;A is lower alkylene which may have an oxo group;R.sup.3 is carboxy, a protected carboxy group, lower alkyl, lower alkenyl, hydroxy (lower) alkyl, phenyl (lower) alkyl, phenyl, tolyl, xylyl, cumenyl, or naphthyl; andR.sup.4 is hydrogen or lower alkoxy, and pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及高抗微生物活性的新型头孢烯化合物，其具有下式：其中R 1是氨基或被保护的氨基; R2是羧基或被保护的羧基; A是可以具有氧代基的低级亚烷基; R3是羧基，被保护的羧基，低级烷基，低级烯基，羟基（低级）烷基，苯基（低级）烷基，苯基，甲苯基，二甲苯基，枯烯基或萘基; 和R4是氢或低级烷氧基，及其药学上可接受的盐。