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1. 发明授权

US4699905A Perhydrothiazepine derivatives, their preparation and their therapeutic use 失效
标题翻译：全氟化氮衍生物，其制备及其治疗用途
公开(公告)号：US4699905A
公开(公告)日：1987-10-13
申请号：US721303
申请日：1985-04-09
申请人： Hiroaki Yanagisawa , Sadao Ishihara , Akiko Ando , Takuro Kanazaki , Hiroyuki Koike , Yoshio Tsujita
发明人： Hiroaki Yanagisawa , Sadao Ishihara , Akiko Ando , Takuro Kanazaki , Hiroyuki Koike , Yoshio Tsujita
IPC分类号： C07D281/06 , A61K31/55 , A61K31/554 , A61K38/00 , A61P9/12 , C07D209/48 , C07D307/52 , C07D333/18 , C07D333/20 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/14 , C07K5/02 , C07K5/06
CPC分类号： C07D209/48 , C07D307/52 , C07D333/18 , C07D333/20 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/14 , C07K5/0222 , A61K38/00
摘要： Compounds of formula (I): ##STR1## (wherein: R.sup.1 represents an optionally substituted alkyl, cycloalkyl, aryl, partially hydrogenated aryl or heterocyclic group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen or an optionally substituted alkyl, cycloalkyl, aralkyl, aryl, heterocyclic or heterocyclic-alkyl group or any adjacent pair thereof form a cyclic structure, at least one not being hydrogen; A represents a bond, or a methylene, ethylene, oxymethyl or thiomethyl group; B represents an alkylene, alkylidene, cycloalkylene or cycloalkylidene group; and n is 0, 1 or 2) and salts and esters thereof are hypotensive agents.

2. 发明授权

US5459148A Biphenyl derivatives and their use for the treatment of hypertension and cardiac disease 失效
标题翻译：联苯衍生物及其用于治疗高血压和心脏病的用途
公开(公告)号：US5459148A
公开(公告)日：1995-10-17
申请号：US331356
申请日：1994-10-27
申请人： Hiroaki Yanagisawa , Yoshiya Amemiya , Takuro Kanazaki , Yasuo Shimoji , Hiroyuki Koike , Toshio Sada
发明人： Hiroaki Yanagisawa , Yoshiya Amemiya , Takuro Kanazaki , Yasuo Shimoji , Hiroyuki Koike , Toshio Sada
IPC分类号： A61K31/415 , A61K31/41 , A61K31/4164 , A61K31/4184 , A61K31/4188 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/505 , A61P9/00 , A61P9/12 , A61P43/00 , C07D213/60 , C07D213/80 , C07D233/58 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/88 , C07D233/90 , C07D233/92 , C07D235/04 , C07D235/08 , C07D235/14 , C07D235/26 , C07D239/42 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/12 , C07D471/04
CPC分类号： C07D213/80 , C07D233/90 , C07D235/08 , C07D235/26 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/12 , C07D471/04 , Y02P20/55 , Y02P20/582
摘要： Compounds of formula (I): ##STR1## [wherein: A represents a group (IIa), (IIb) or (IIc): ##STR2## R.sup.1 is alkyl, alkenyl, cycloalkyl or a group of formula R.sup.4 --Y--R.sup.5 --, where: R.sup.4 is hydrogen, alkyl, or cycloalkyl, R.sup.5 is a single bond or alkylene, and Y is oxygen, sulfur or imino group; R.sup.2 is hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted cycloalkyl, hydroxy, amino, alkylamino, dialkylamino, formyl, alkylcarbonyl, alkoxy, alkylthio, cyano or nitro; R.sup.3 is hydrogen, alkyl, carboxy, protected carboxy, carbamoyl or tetrazol-5-yl; X is of formula --CH.dbd., --N.dbd. or --C(COOR.sup.6).dbd., where R.sup.6 is hydrogen or a carboxy-protecting group; Z is a single bond, alkylene or vinylene; and B is carboxy, protected carboxy or tetrazol-5-yl]; and pharmaceutically acceptable salts and esters thereof have the ability to inhibit the action of angiotensin II and thus can be used for the treatment and prophylaxis of hypertension and cardiac diseases.
摘要翻译：（II）化合物：其中：A表示基团（IIa），（IIb）或（IIc）：（IIa）（IIc）（IIc） R1是烷基，烯基，环烷基或式R4-Y-R5-基团，其中：R4是氢，烷基或环烷基，R5是单键或亚烷基，Y是氧，硫或亚氨基; R 2是氢，卤素，任选取代的烷基，任选取代的烯基，任选取代的环烷基，羟基，氨基，烷基氨基，二烷基氨基，甲酰基，烷基羰基，烷氧基，烷硫基，氰基或硝基; R3是氢，烷基，羧基，被保护的羧基，氨基甲酰基或四唑-5-基; X为式-CH =，-N =或-C（COOR 6）=，其中R 6为氢或羧基保护基; Z是单键，亚烷基或亚乙烯基; 和B是羧基，保护的羧基或四唑-5-基]; 其药学上可接受的盐和酯具有抑制血管紧张素II作用的能力，因此可用于治疗和预防高血压和心脏病。

3. 发明授权

US4734410A Lactam derivatives and their use as hypotensive agents 失效
标题翻译：内酰胺衍生物及其作为降血压剂的用途
公开(公告)号：US4734410A
公开(公告)日：1988-03-29
申请号：US917041
申请日：1986-10-09
申请人： Hiroaki Yanagisawa , Sadao Ishihara , Akiko Ando , Takuro Kanazaki , Hiroyuki Koike , Yasuteru Iijima
发明人： Hiroaki Yanagisawa , Sadao Ishihara , Akiko Ando , Takuro Kanazaki , Hiroyuki Koike , Yasuteru Iijima
IPC分类号： C07D317/00 , A61K31/395 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/55 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C67/00 , C07C227/00 , C07C227/06 , C07C227/18 , C07C239/00 , C07C253/00 , C07C255/41 , C07C271/22 , C07D211/76 , C07D223/10 , C07D223/12 , C07D225/02 , C07D227/087 , C07D227/10 , C07D333/00 , C07D405/04 , C07D405/06 , C07D409/04 , C07K5/02 , C07K5/06 , C07K5/12 , C07K14/81 , C12N9/99
CPC分类号： C07K5/0222 , C07D223/12 , A61K38/00 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## (wherein R.sup.1 and R.sup.3 are organic groups, A is a direct bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CO--CH.sub.2, --O--CH.sub.2 -- or --S--CH.sub.2 --, B is lower alkylene and n is 1-3) are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group at the 3-position.
摘要翻译：式（I）化合物：其中R 1和R 3是有机基团，A是直接键，-CH 2 - ， - CH 2 CH 2 - ， - CO-CH 2，-O-CH 2 - 或-S- CH2-，B是低级亚烷基，n是1-3）是有价值的降压剂，其可以通过相应的具有3-位氨基的化合物的缩合反应来制备。

4. 发明授权

US5646171A Angiotensin II antagonist 1-biphenylmethylimidazole compounds and their therapeutic use 失效
标题翻译：血管紧张素II拮抗剂1-联苯甲基咪唑化合物及其治疗用途
公开(公告)号：US5646171A
公开(公告)日：1997-07-08
申请号：US465369
申请日：1995-06-05
申请人： Hiroaki Yanagisawa , Yoshiya Amemiya , Yasuo Shimoji , Takuro Kanazaki , Hiroyuki Koike , Toshio Sada
发明人： Hiroaki Yanagisawa , Yoshiya Amemiya , Yasuo Shimoji , Takuro Kanazaki , Hiroyuki Koike , Toshio Sada
IPC分类号： C07D233/90 , C07D403/10 , C07D405/12 , C07D405/14 , C07F7/18 , C07D405/08 , C07D257/04 , A61K31/415 , A61K31/41
CPC分类号： C07D403/10 , C07D233/90 , C07D405/12 , C07D405/14 , C07F7/1856
摘要： An angiotensin II antagonist of the formula: ##STR1## in which: R.sub.p.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.1 -C.sub.6 alkanoyl; R.sub.p.sup.2 represents a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.1 -C.sub.4 alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; R.sub.p.sup.5 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, benzyl, diphenylmethyl, naphthylmethyl, alkanoyloxyalkyl, cycloalkanecarbonyloxyalkyl, alkoxycarbonyloxyalkyl, cycloalkyloxycarbonyloxyalkyl, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl, (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl or phthalaidyl; R.sub.p.sup.6 represents a carboxy or a tetrazol-5-yl; and X.sub.p represents an oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds have hypotensive activity and can thus be used for the treatment and prophylaxis of hypertension.
摘要翻译：一种下式的血管紧张素II拮抗剂：其中：Rp1表示氢，C1-C6烷基，C3-C6环烷基或C1-C6烷酰基; Rp2表示单键，C1-C4亚烷基或C1-C4亚烷基; Rp3和Rp4独立地选自氢和C1-C6烷基; R 5表示氢，C 1 -C 4烷基，苯基，萘基，苄基，二苯基甲基，萘基甲基，烷酰氧基烷基，环烷基羰氧基烷基，烷氧基羰氧基烷基，环烷氧基羰基氧基烷基，（5-苯基-2-氧代-1,3-二氧杂环戊烯-4-基） - 烷基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基或邻苯二甲酰基; Rp6表示羧基或四唑-5-基; Xp表示氧或硫，以及其药学上可接受的盐。这些化合物具有降血压活性，因此可用于治疗和预防高血压。

5. 发明授权

US5616599A Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their therapeutic use 失效
标题翻译：血管紧张素II拮抗剂1-联苯甲基咪唑化合物及其治疗用途
公开(公告)号：US5616599A
公开(公告)日：1997-04-01
申请号：US378650
申请日：1995-01-26
申请人： Hiroaki Yanagisawa , Koichi Fujimoto , Yoshiya Amemiya , Yasuo Shimoji , Takuro Kanazaki , Hiroyuki Koike , Toshio Sada
发明人： Hiroaki Yanagisawa , Koichi Fujimoto , Yoshiya Amemiya , Yasuo Shimoji , Takuro Kanazaki , Hiroyuki Koike , Toshio Sada
IPC分类号： C07D233/90 , C07D403/10 , C07D405/12 , C07D405/14 , C07F7/18 , C07D257/04 , A61K31/41 , A61K31/415
CPC分类号： C07D403/10 , C07D233/90 , C07D405/12 , C07D405/14 , C07F7/1856
摘要： Compounds of the following formula (I) or the formula (I).sub.p : ##STR1## wherein R.sup.1 is alkyl or alkenyl; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R.sup.4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula --SiR.sup.a R.sup.b R.sup.c, in which R.sup.a, R.sup.b and R.sup.c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R.sup.5 is carboxy or --CONR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 hydrogens or alkyl, or R.sup.8 and R.sup.9 together form alkylene; R.sup.6 is hydrogen, alkyl, alkoxy or halogen; R.sup.7 is carboxy or tetrazol-5-yl; R.sub.p.sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R.sub.p.sup.2 is a single bond, alkylene or alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are each hydrogen or alkyl; R.sub.p.sup.6 is carboxy or tetrazol-5-yl; and X.sub.p is oxygen or sulfur; and pharmaceutically acceptable salts and esters thereof. The compounds are AII receptor antagonists and thus have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. The compounds may be prepared by reacting a biphenylmethyl compound with an imidazole compound.
摘要翻译：下式（I）或式（I）的化合物p：其中R 1是烷基或链烯基; R2和R3是与环烷基稠合的氢，烷基，烯基，环烷基，芳烷基，芳基或芳基; R4是氢，烷基，烷酰基，烯酰基，芳基羰基，烷氧基羰基，四氢吡喃基，四氢噻喃基，四氢噻吩基，四氢呋喃基，式-SiRaRbRc的基团，其中R a，R b和R c是烷基或芳基，烷氧基甲基，（烷氧基烷氧基）甲基，卤代烷氧基甲基，芳烷基，芳基或烷酰氧基甲氧基羰基; R5是羧基或-CONR8R9，其中R8和R9的氢或烷基，或R8和R9一起形成亚烷基; R6是氢，烷基，烷氧基或卤素; R7是羧基或四唑-5-基; Rp1为氢，烷基，环烷基或烷酰基; Rp2是单键，亚烷基或亚烷基; Rp3和Rp4各自为氢或烷基; Rp6是羧基或四唑-5-基; Xp为氧或硫; 及其药学上可接受的盐和酯。化合物是AII受体拮抗剂，因此具有低血压活性，可用于治疗和预防高血压。该化合物可以通过使联苯甲基化合物与咪唑化合物反应来制备。

6. 发明授权

US5002942A 1,5-benzothiazepine derivatives, their preparation and their use in the treatment of cardiovascular disorders 失效
标题翻译： 1,5-苯并硫氮因衍生物，其制备及其在治疗心血管疾病中的应用
公开(公告)号：US5002942A
公开(公告)日：1991-03-26
申请号：US384261
申请日：1989-07-21
申请人： Hiroaki Yanagisawa , Koichi Fujimoto , Yasuo Shimoji , Takuro Kanazaki , Hiroyuki Koike , Hiroshi Nishino
发明人： Hiroaki Yanagisawa , Koichi Fujimoto , Yasuo Shimoji , Takuro Kanazaki , Hiroyuki Koike , Hiroshi Nishino
IPC分类号： C07D281/10 , C07D417/04 , C07D417/06
CPC分类号： C07D417/04 , C07D281/10 , C07D417/06
摘要： Compounds of formula (I): ##STR1## in which: R.sup.1 is aryl or aromatic heterocyclic; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkoxy, halogen, phenyl, phenoxy, C.sub.1 -C.sub.6 alkylthio, phenylthio, C.sub.1 -C.sub.6 haloalkyl, cyano or nitro, or together are alkylene optionally containing oxygen; R.sup.4 is hydrogen, aliphatic acyl, cycloalkylcarbonyl, cycloalkoxycarbonyl, aromatic acyl, alkoxycarbonyl or benzyloxycarbonyl; R.sup.5 and R.sup.6 are alkyl; and X is oxygen, sulfur or methylene, have calcium channel blocking activity and can serve for the treatment or prophylaxis of cardiovascular diseases and disorders. They may be prepared by reacting a corresponding compound where R.sup.4 is hydrogen and the aminoethyl group is replaced by hydrogen with a compound providing the aminoethyl group and the, if required, acylating the product.

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