公开(公告)号：US5532258A

公开(公告)日：1996-07-02

申请号：US356967

申请日：1994-12-16

申请人： Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue ,  Hisashi Takasugi

发明人： Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue ,  Hisashi Takasugi

IPC分类号： A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P1/00 ,  A61P1/04 ,  A61P43/00 ,  C07D277/20 ,  C07D277/38 ,  C07D277/42 ,  C07D277/48 ,  C07D417/12 ,  C07D417/14 ,  A61K31/125

CPC分类号： C07D277/48

摘要： Thiazole compounds of formula ##STR1## are provided which have antiulcer activity and H.sub.2 -receptor antagonism, wherein R.sup.2 is lower alkyl or lower alkoxy(lower)alkyl, R.sup.3 is hydrogen, A is methylene and R.sup.1 is lower alkyl.

摘要翻译： 提供具有抗溃疡活性和H2受体拮抗作用的式“IMAGE”的噻唑化合物，其中R2是低级烷基或低级烷氧基（低级）烷基，R3是氢，A是亚甲基，R1是低级烷基。

公开(公告)号：US5364871A

公开(公告)日：1994-11-15

申请号：US29359

申请日：1993-03-10

申请人： Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

发明人： Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

IPC分类号： C07D277/48 ,  C07D417/04 ,  C07D417/14 ,  A61K31/44 ,  C07D417/06

CPC分类号： C07D417/04 ,  C07D277/48 ,  C07D417/14

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino, ureido, lower alkanoylamino, lower alkoxycarbonylamino, lower alkylsulfonylamino, lower alkoxy(lower)alkanoylamino, mono or di or trihalo(lower)alkanoylamino, hydroxy(lower)alkanoylamino, protected hydroxy(lower)alkanoylamino, or a group of the formula: ##STR2## in which R.sup.4 is hydrogen or sulfamoyl, R.sup.5 is amino or lower alkoxy, R.sup.2 is hydrogen, lower alkyl, lower alkoxy(lower)alkyl, di(lower)alkylamino(lower)alkyl, (C.sub.3 -C.sub.7)-cycloalkyl, lower alkenyl or mono or di or trihalo(lower)alkyl; R.sup.3 is hydrogen or lower alkyl; or R.sup.2 and R.sup.3 are linked together to form lower alkylene,Y is ##STR3## in which R.sup.6 is hydrogen, A is lower alkylene, and W is NH; or R.sup.2 -W is piperidino or morpholino, or pharmaceutically acceptable salt thereof.

摘要翻译： 下式的化合物，其中R 1是氨基，脲基，低级烷酰基氨基，低级烷氧基羰基氨基，低级烷基磺酰基氨基，低级烷氧基（低级）烷酰基氨基，一或二或三卤代（低级）烷酰基氨基，羟基（低级）烷酰基氨基，被保护的羟基 （低级）烷酰基氨基或下式的基团：其中R 4是氢或氨磺酰基，R 5是氨基或低级烷氧基，R 2是氢，低级烷基，低级烷氧基（低级）烷基，二（低级）烷基氨基 低级烷基，（C 3 -C 7） - 环烷基，低级烯基或一或二或三卤代（低级）烷基; R3是氢或低级烷基; 或R 2和R 3连接在一起形成低级亚烷基，Y是其中R 6是氢，A是低级亚烷基，W是NH; 或R 2 -W是哌啶子基或吗啉代，或其药学上可接受的盐。

公开(公告)号：US5308857A

公开(公告)日：1994-05-03

申请号：US908795

申请日：1992-07-06

申请人： Hisashi Takasugi ,  Yousuke Katsura ,  Yoshikazu Inoue ,  Tetsuo Tomishi

发明人： Hisashi Takasugi ,  Yousuke Katsura ,  Yoshikazu Inoue ,  Tetsuo Tomishi

IPC分类号： C07D417/04 ,  C07D417/14 ,  A61K31/425

CPC分类号： C07D417/14 ,  C07D417/04

摘要： The invention relates to compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and Q are as described, useful in the treatment of ulcers.

摘要翻译： 本发明涉及下式的化合物：其中R1，R2，R3，R4，A和Q如上所述，可用于治疗溃疡。

公开(公告)号：US4675324A

公开(公告)日：1987-06-23

申请号：US780582

申请日：1985-09-26

申请人： Ikuo Ueda ,  Youichi Shiokawa ,  Takashi Manabe ,  Yousuke Katsura

发明人： Ikuo Ueda ,  Youichi Shiokawa ,  Takashi Manabe ,  Yousuke Katsura

IPC分类号： C07D311/22 ,  A61K31/415 ,  A61K31/4162 ,  A61K31/435 ,  A61K31/47 ,  A61K31/4745 ,  A61P7/10 ,  A61P9/02 ,  A61P9/08 ,  A61P9/12 ,  A61P19/06 ,  C07D215/22 ,  C07D215/233 ,  C07D215/38 ,  C07D311/56 ,  C07D471/04 ,  C07D491/04 ,  C07D491/052 ,  A61K31/395

CPC分类号： C07D215/233 ,  C07D311/56 ,  C07D471/04 ,  C07D491/04

摘要： This invention provides a benezene-fused heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is halogen, nitro, amino, hydroxy, lower alkyl, lower alkoxy substituted by carboxy or protected carboxy, acylamino which may have lower alkyl on the amino moiety, or aryloxy which may have halogen,R.sup.2 is hydrogen or halogen,X is --O-- or ##STR2## in which R.sup.3 is hydrogen, lower alkyl or acyl and A is a group of the formula: ##STR3## in which R.sup.4 is hydrogen, lower alkenyl, lower alkynyl or alkyl which may have suitable substituent(s) selected from the groups consisting of hydroxy, acyl, lower alkoxy, di(lower)alkylamino, carboxy, protected carboxy and aryl; orR.sup.1 is hydrogen or lower alkoxy,R.sup.2 is hydrogen,X is ##STR4## in which R.sub.a.sup.3 is lower alkanoyl and A is a group of the formula: ##STR5## and pharmaceutically acceptable salts thereof. This compound possesses diuretic activity, uricosuric activity and vasodilative activity and are useful as a diuretic agent, uricosuric agent and anti-hypertensive agent. The invention further relates to processes for the preparation of this compound and pharmaceutical composition comprising compound of the above formula.

摘要翻译： 本发明提供了下式的有益稠合的杂环化合物：其中R 1是卤素，硝基，氨基，羟基，低级烷基，被羧基或被保护的羧基取代的低级烷氧基，在氨基部分上可以具有低级烷基的酰基氨基， 或可具有卤素的芳氧基，R 2是氢或卤素，X是-O-或者其中R 3是氢，低级烷基或酰基，和A是下式的基团：其中R 4是氢， 低级烯基，低级炔基或烷基，其可以具有选自羟基，酰基，低级烷氧基，二（低级）烷基氨基，羧基，保护的羧基和芳基的合适取代基。 或R 1为氢或低级烷氧基，R 2为氢，X为R a为低级烷酰基，A为下式基团：及其药学上可接受的盐。 该化合物具有利尿活性，尿酸活性和血管舒张活性，可用作利尿剂，尿酸血症药和抗高血压药。 本发明还涉及制备该化合物的方法和包含上式化合物的药物组合物。

公开(公告)号：US5371097A

公开(公告)日：1994-12-06

申请号：US80051

申请日：1993-06-22

申请人： Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

发明人： Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P1/04 ,  A61P43/00 ,  C07D277/48 ,  C07D417/04 ,  C07D417/14 ,  C07D521/00

CPC分类号： C07D417/04 ,  C07D277/48 ,  C07D417/14

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino, acylamino, cyclo(lower)alkenylamino having amino and oxo, imido, triazolylamino, benzoisothiazolylamino, wherein each of said heterocyclicamino groups may be substituted by one or more substituent(s) selected from the group consisting of lower alkyl, amino and oxo, 2-cyano-3-lower alkylguanidino, 2-acyl-3-lower alkylguanidino, 2-acylguanidino, (1-lower alkylamino-2-nitrovinyl)amino, hydroxy, halogen, cyano, acyl, benzimidazolylthio, triazolyl substituted with amino, or a group of the formula: ##STR2## in which R.sup.4 is hydrogen, cyano, or acyl, andR.sup.5 is amino or lower alkoxy,R.sup.2 and R.sup.3 are each hydrogen, acyl or lower alkyl which may have halogen; orR.sup.2 and R.sup.3 are linked together to form lower alkylene,Y is ##STR3## in which R.sup.6 is hydrogen or halogen, andA is lower alkylene, or pharmaceutically acceptable salt thereof.

摘要翻译： 下式的化合物，其中R 1是氨基，酰氨基，具有氨基和氧代的环（低级）烯基氨基，亚氨基，三唑基氨基，苯并异噻唑基氨基，其中每个所述杂环氨基可以被一个或多个被选择的取代基取代 由2-烷基氨基和氧代低级烷基，2-氰基-3-低级烷基胍基，2-酰基-3-低级烷基胍基，2-酰基胍基，（1-低级烷基氨基-2-硝基乙烯基）氨基，羟基，卤素， 氰基，酰基，苯并咪唑硫基，被氨基取代的三唑基或下式的基团：其中R 4是氢，氰基或酰基，R 5是氨基或低级烷氧基，R 2和R 3各自是氢，酰基或更低级 可以具有卤素的烷基; 或R 2和R 3连接在一起形成低级亚烷基，Y是其中R 6是氢或卤素，A是低级亚烷基或其药学上可接受的盐。

公开(公告)号：US4692444A

公开(公告)日：1987-09-08

申请号：US836402

申请日：1986-03-05

申请人： Ikuo Ueda ,  Youichi Shiokawa ,  Takashi Manabe ,  Yousuke Katsura

发明人： Ikuo Ueda ,  Youichi Shiokawa ,  Takashi Manabe ,  Yousuke Katsura

IPC分类号： A61K31/415 ,  A61P7/10 ,  A61P9/12 ,  A61P19/06 ,  C07D495/04

CPC分类号： C07D495/04

摘要： This invention provides a benzene-fused heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is halogen, nitro, amino, hydroxy, lower alkyl, lower alkoxy or acylamino,X is --S--, ##STR2## n is an integer of 1 or 2 and A is a group of the formula: ##STR3## in which R.sup.2 is hydrogen, lower alkyl, lower alkynyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl, or pharmaceutically acceptable salts thereof. This compound possesses diuretic, uricosuric, and vasodilative activities and therefore is useful as a diuretic agent, uricosuric agent and anti-hypertensive agent. This invention further provides processes for the preparation of this compound and pharmaceutical composition comprising compound of the above formula.

摘要翻译： 本发明提供下式的苯稠稠杂环化合物：其中R1是卤素，硝基，氨基，羟基，低级烷基，低级烷氧基或酰基氨基，X是-S-，n是 其中R 2为氢，低级烷基，低级炔基，羧基（低级）烷基或被保护的羧基（低级）烷基）或其药学上可接受的盐。 该化合物具有利尿，尿酸和血管扩张活性，因此可用作利尿剂，尿酸血症药和抗高血压药。 本发明还提供了制备该化合物的方法和包含上式化合物的药物组合物。

公开(公告)号：US5512588A

公开(公告)日：1996-04-30

申请号：US182119

申请日：1994-01-28

申请人： Hisashi Takasugi ,  Yousuke Katsura ,  Yoshikazu Inoue ,  Tetsuo Tomishi

发明人： Hisashi Takasugi ,  Yousuke Katsura ,  Yoshikazu Inoue ,  Tetsuo Tomishi

IPC分类号： A61K31/425 ,  A61K31/44 ,  A61P1/04 ,  A61P31/04 ,  C07D417/04 ,  C07D417/14

CPC分类号： C07D417/04 ,  C07D417/14

摘要： This invention relates to furylthiazole derivatives represented by the following formula: ##STR1## wherein each symbol is as defined in the specification and pharmaceutically acceptable salts thereof which have antiulcer activity, H.sub.2 -receptor antagonism and antimicrobial activity, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of ulcer and infectious diseases in human being or animals.

摘要翻译： PCT No.PCT / JP92 / 00986 Sec。 371日期1994年1月28日 102（e）日期1994年1月28日PCT提交1992年8月3日PCT公布。 出版物WO93 / 0302800 日本特开1993年2月18日。本发明涉及由下式表示的呋喃基噻唑衍生物：其中每个符号如说明书中所定义，其药学上可接受的盐具有抗溃疡活性，H2-受体拮抗作用和抗微生物活性， 制备方法，包含其的药物组合物和治疗人或动物中的溃疡和感染性疾病的方法。

公开(公告)号：US5047411A

公开(公告)日：1991-09-10

申请号：US397669

申请日：1989-08-23

申请人： Hisashi Takasugi ,  Yousuke Katsura ,  Yoshikazu Inoue ,  Shigetaka Nishino ,  Takao Takaya

发明人： Hisashi Takasugi ,  Yousuke Katsura ,  Yoshikazu Inoue ,  Shigetaka Nishino ,  Takao Takaya

IPC分类号： C07D277/68 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/423 ,  A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/496 ,  A61K31/505 ,  A61P1/04 ,  A61P43/00 ,  C07D213/38 ,  C07D213/40 ,  C07D235/08 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D263/56 ,  C07D263/58 ,  C07D277/70 ,  C07D277/82 ,  C07D307/38 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/00 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D263/58 ,  C07D277/82 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

摘要： The benzazole compounds of this invention can be represented by the following formula [I]: ##STR1## wherein R.sup.1 is aryl or a heterocyclic group, each of which may have suitable substitutent(s),R.sup.2 is hydroxy, mercapto, lower alkylthio, sulfo, lower alkyl, amino or substituted amino,R.sup.3 is hydrogen, halogen or lower alkoxy,A is lower alkenylene, lower alkylene optionally substituted with hydroxy, or a group of the formula:--A'--Q--A"--, in which A' is lower alkylene, A" is lower alkylene or a single bond, and Q is O or S, andX is O, S, NH or N--R.sup.4, in which R.sup.4 is lower alkyl,More particularly, it relates to benzazole compounds and pharmaceutically acceptable salts thereof which have antiulcer activity and H.sub.2 -receptor antagonism, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of ulcers in human being or animals.

公开(公告)号：US4767780A

公开(公告)日：1988-08-30

申请号：US42299

申请日：1987-04-24

申请人： Ikuo Ueda ,  Youichi Shiokawa ,  Takashi Manabe ,  Yousuke Katsura

发明人： Ikuo Ueda ,  Youichi Shiokawa ,  Takashi Manabe ,  Yousuke Katsura

IPC分类号： C07D311/22 ,  A61K31/415 ,  A61K31/4162 ,  A61K31/435 ,  A61K31/47 ,  A61K31/4745 ,  A61P7/10 ,  A61P9/02 ,  A61P9/08 ,  A61P9/12 ,  A61P19/06 ,  C07D215/22 ,  C07D215/233 ,  C07D215/38 ,  C07D311/56 ,  C07D471/04 ,  C07D491/04 ,  C07D491/052 ,  A61K31/35 ,  C07D487/04

CPC分类号： C07D215/233 ,  C07D311/56 ,  C07D471/04 ,  C07D491/04

摘要： This invention provides a benezene-fused heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is halogen, nitro, amino, hydroxy, lower alkyl, lower alkoxy substituted by carboxy or protected carboxy, acylamino which may have lower alkyl on the amino moiety, or aryloxy which may have halogen,R.sup.2 is hydrogen or halogen,X is --O-- or ##STR2## in which R.sup.3 is hydrogen, lower alkyl or acyl and A is a group of the formula: ##STR3## in which R.sup.4 is hydrogen, lower, alkenyl, lower alkynyl or alkyl which may have suitable substituent(s) selected from the groups consisting of hydroxy, acyl, lower alkoxy, di(lower)alkylamino, carboxy, protected carboxy and aryl; orR.sup.1 is hydrogen or lower alkoxy,R.sup.2 is hydrogen,X is ##STR4## in which R.sub.a.sup.3 is lower alkanoyl and A is a group of the formula: ##STR5## and pharmaceutically acceptable salts thereof. This compound possesses diuretic activity, uricosuric activity and vasodilative activity and are useful as a diuretic agent, uricosuric agent and anti-hypertensive agent. The invention further relates to processes for the preparation of this compound and pharmaceutical composition comprising compound of the above formula.

公开(公告)号：US4764514A

公开(公告)日：1988-08-16

申请号：US855904

申请日：1986-04-24

申请人： Ikuo Ueda ,  Yousuke Katsura

发明人： Ikuo Ueda ,  Yousuke Katsura

IPC分类号： A61K31/425 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/55 ,  A61P25/00 ,  A61P25/28 ,  C07D243/00 ,  C07D277/14 ,  C07D333/00 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D521/00

CPC分类号： C07D417/06 ,  C07D277/14 ,  C07D417/12 ,  C07D417/14

摘要： This invention provides a oxothiazolidine compound of the formula: ##STR1## wherein R.sup.1 is acyl;di(lower)alkylamino(lower)alkylcarbamoyl(lower)alkyl; arylcarbamoyl(lower)alkyl;ar(lower)alkylcarbamoyl(lower)alkyl;heterocyclic carbamoyl(lower)alkyl;heterocyclic(lower)alkylcarbamoyl(lower)alkyl;thiazolidinylcarbonyl(lower)alkyl;morpholinylcarbonyl(lower)alkyl or a group of the formula: ##STR2## in which A is lower alkylene;n is an integer of 0 or 1;m is an integer of 2 or 3;X is --N--, ##STR3## or --CH-- and R.sup.2 is hydroxy;lower alkyl which may have hydroxy;ar(lower)alkyl which may have halogen;arylthio which may have halogen;acyl or heterocyclic group andY is --S--, ##STR4## or pharmaceutically acceptable salt thereof. This compound is useful as cognition activator. This invention further provides processes for the preparation of this compound and pharmaceutical composition comprising compound of the above formula.

摘要翻译： 本发明提供下式的氧代噻唑烷化合物：其中R 1是酰基; 二（低级）烷基氨基（低级）烷基氨基甲酰基（低级）烷基; 芳基氨基甲酰基（低级）烷基; 芳（低级）烷基氨基甲酰基（低级）烷基; 杂环氨基甲酰基（低级）烷基; （低级）烷基氨基甲酰基（低级）烷基; 噻唑烷基羰基（低级）烷基; 吗啉基羰基（低级）烷基或下式的基团：其中A是低级亚烷基; n为0或1的整数; m为2或3的整数; X是-N-，或-CH-，R 2是羟基; 可具有羟基的低级烷基; 可以具有卤素的芳基（低级）烷基; 可以具有卤素的芳硫基; 酰基或杂环基，Y是-S-，其中或其药学上可接受的盐。 该化合物可用作认知激活剂。 本发明还提供了制备该化合物的方法和包含上式化合物的药物组合物。