公开(公告)号：US5817828A

公开(公告)日：1998-10-06

申请号：US999493

申请日：1997-12-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

公开(公告)号：US4843076A

公开(公告)日：1989-06-27

申请号：US77220

申请日：1987-07-24

申请人： Kiyotomo Seto ,  Ryozo Sakoda ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Sakuya Tanaka

发明人： Kiyotomo Seto ,  Ryozo Sakoda ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Sakuya Tanaka

IPC分类号： C07F9/38 ,  A61K31/675 ,  A61P9/08 ,  C07F9/40 ,  C07F9/6571 ,  C07F9/6574

CPC分类号： C07F9/657181

摘要： An optical isomer of a compound having the formula: ##STR1## wherein the two methyl groups at 4- and 6-positions of the dioxaphosphorinane ring assume trans configurations to each other, which has a levo-rotatory angle of optical rotation attributable to the asymmetric carbon atom at 4-position of the dihydropyridine ring, and a pharmaceutically acceptable salt thereof.

摘要翻译： 具有下式的化合物的光学异构体：其中二氧杂磷杂环戊烷环的4位和6位上的两个甲基呈现相互构型，其具有归因于旋光的左旋旋角 到二氢吡啶环的4-位的不对称碳原子及其药学上可接受的盐。

公开(公告)号：US5272271A

公开(公告)日：1993-12-21

申请号：US726897

申请日：1991-07-08

申请人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Keisuke Ohdoi ,  Ryozo Sakoda ,  Yukinori Masuda

发明人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Keisuke Ohdoi ,  Ryozo Sakoda ,  Yukinori Masuda

IPC分类号： A61K31/41 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  C07D498/04 ,  C07F7/18 ,  C07D403/04 ,  C07D271/12

CPC分类号： C07D498/04 ,  C07F7/1856

摘要： A compound of the formula (I): ##STR1## wherein X.sup.1 and X.sup.2 do not exist or represent oxygen atom; A represents OH or acyloxy group having 1 to 4 carbon atoms; B represents hydrogen atom; A and B together represent a bond; R.sup.1 and R.sup.2 represent hydrogen atom or alkyl group having 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 together represent 1,2-ethylene, 1,3-propylene, 1,4-butylene or 1,5-pentylene, and these alkylene groups may be substituted by alkyl group having 1 to 4 carbon atoms; R.sup.3 represents amido group of the formula: ##STR2## wherein n, R.sup.4, R.sup.5, R.sup.6, R.sup.7. R.sup.8. R.sup.9, R.sup.10 and R.sup.11 represent specific groups, and the pharmacological acceptable salts of the compounds which can form salts have strong activity for lowering blood pressure, and process therefor and pharmaceutical use of the compounds.

公开(公告)号：US4900752A

公开(公告)日：1990-02-13

申请号：US304641

申请日：1989-02-01

申请人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Kyoko Nakayama ,  Ryozo Sakoda ,  Yukinori Masuda

发明人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Kyoko Nakayama ,  Ryozo Sakoda ,  Yukinori Masuda

IPC分类号： C07D491/052 ,  A61K31/352 ,  A61K31/41 ,  A61K31/4245 ,  A61P9/02 ,  A61P9/12 ,  A61P11/06 ,  C07D20060101 ,  C07D498/04

CPC分类号： C07D498/04

摘要： A compounds of the formula (I): ##STR1## wherein A represents OH or OC(O)CH.sub.3-n X.sub.n, B represents hydrogen atom, or A and B together represent a bond; R.sup.1 represents hydrogen atom, R.sup.2 represents hydrogen atom, C(Z)CH.sub.3-n X.sub.n or C(Z)NHCH.sub.3-n X.sub.n or R.sup.1 and R.sup.2 together represents (CH.sub.2).sub.m, (CH.sub.2).sub.m-1 C(Z), N(R.sup.3)(CH.sub.2).sub.2 C(Z), (CH.sub.2).sub.m-2 NHC(Z) or (CH.sub.2).sub.m-2 OC(Z) in which X represents fluorine atom, chlorine atom, bromine atom, a methyl group or a methoxy group and n represents 0 or an integer of 1 to 3, Z represents oxygem atom or sulfur atom, m represents an integer of 4 or 5 and R.sup.3 represents hydrogen atom or a methyl group, and pharmacological acceptable salts of the compounds which can form salts, processes therefor and pharmaceutical use of the compounds.

摘要翻译： 本发明包括式（I）的化合物：其中A表示OH或OC（O）CH 3 -n Xn，B表示氢原子，或A和B一起表示键; R 1表示氢原子，R 2表示氢原子，C（Z）CH 3 -n Xn或C（Z）NHCH 3 -n X n或R 1和R 2一起表示（CH 2）m， ）m-1C（Z），N（R 3）（CH 2）2 C（Z），（CH 2）m -NHHC（Z）或（CH 2）m -OOC（Z） 原子，溴原子，甲基或甲氧基，n表示0或1〜3的整数，Z表示氧原子或硫原子，m表示4或5的整数，R 3表示氢原子或 甲基和可以形成盐的化合物的药理学可接受的盐，其制备方法，化合物的药物用途和包含该化合物的组合物。

公开(公告)号：US6114369A

公开(公告)日：2000-09-05

申请号：US403763

申请日：1999-11-01

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Mitsuaki Hirotsuka ,  Takehisa Iwama ,  Akiko Yamamoto ,  Yoichiro Fujita

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Mitsuaki Hirotsuka ,  Takehisa Iwama ,  Akiko Yamamoto ,  Yoichiro Fujita

IPC分类号： A61K31/4184 ,  A61P37/08 ,  C07D235/10 ,  C07D235/14 ,  C07D235/30

CPC分类号： C07D235/14 ,  C07D235/30

摘要： A benzimidazole derivative of the formula (I) or its salt: wherein A is a single bond or a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), R.sup.6 is a C.sub.1-4 alkyl group (this alkyl group may optionally be substituted by a phenyl group), B is a C.sub.2-3 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), X is an oxygen atom, a sulfur atom or NR.sup.7 (wherein R.sup.7 is a nitro group, a cyano group or a C.sub.1-4 alkoxy group), each of R.sup.1 and R.sup.2 which are independent of each other, is a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, E is a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), R.sup.3 is a phenyl group (this phenyl group may optionally be substituted by a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group), a C.sub.1-4 alkoxy group or a benzyloxy group, each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group (this alkyl group may optionally be substituted by a phenyl group), D is a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), and Ar is a phenyl group.

摘要翻译： PCT No.PCT / JP98 / 01986 Sec。 371日期：1999年11月1日 102（e）1999年11月1日PCT 1998年4月30日PCT PCT。 WO98 / 50368 PCT出版物 日期：1998年11月12日一种式（I）的苯并咪唑衍生物或其盐：其中A为单键或C1-2亚烷基（该亚烷基可任选被C 1-4烷基取代），R 6为 C 1-4烷基（该烷基可以任选被苯基取代），B是C2-3亚烷基（该亚烷基可以任选被C 1-4烷基取代），X是氧原子 ，硫原子或NR 7（其中R 7为硝基，氰基或C 1-4烷氧基），R 1和R 2各自独立地为氢原子，卤素原子，C1- 4烷基或C 1-4烷氧基，E是C1-2亚烷基（该亚烷基可以任选被C 1-4烷基取代），R 3是苯基（该苯基可以任选地被 卤素原子，C 1-4烷基或C 1-4烷氧基），C 1-4烷氧基或苄氧基，R 4和R 5各自独立地为C 1-4烷基（ t 其烷基可任选被苯基取代），D为C1-2亚烷基（该亚烷基可任选被C 1-4烷基取代），Ar为苯基。

公开(公告)号：US5846991A

公开(公告)日：1998-12-08

申请号：US998671

申请日：1997-12-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415 ,  A61K31/44

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

公开(公告)号：US5721264A

公开(公告)日：1998-02-24

申请号：US525555

申请日：1995-09-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

摘要翻译： PCT No.PCT / JP94 / 00587第 371 1995年9月29日第 102（e）1995年9月29日PCT PCT 1994年4月7日PCT公布。 公开号WO94 / 22838 日期：1994年10月13日式[1]吡唑化合物及其互变异构体和盐：其中R1是烷基等; R2是羧基等; R3是卤素原子， 烷基，苯基等; R4，R5和R6各自为氢原子，卤素原子等; R7为羧基，5-四唑基等; X为氮原子， Y和Z各自为CH，氮原子等; A和E各自为亚甲基等; D为苯基等; G为共价键等）。 本发明化合物对血管紧张素II具有拮抗作用，可用于预防和治疗高血压，充血性心功能不全，慢性肾功能不全，醛固酮增多症，超眼压等。

公开(公告)号：US5919806A

公开(公告)日：1999-07-06

申请号：US530252

申请日：1995-09-29

申请人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Toru Yamashita ,  Yukinori Masuda

发明人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Toru Yamashita ,  Yukinori Masuda

IPC分类号： A61K31/41 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61P9/04 ,  C07D491/04 ,  C07D491/052 ,  C07D498/04 ,  C07D513/04 ,  A61K31/37

CPC分类号： C07D491/04 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  C07D513/04

摘要： Disclosed are cardiotonic medicines containing, as the active ingredient, at least one of compounds of formula (I) and their pharmacologically acceptable salts when they form salts. ##STR1## wherein X.sup.1 and X.sup.2 do not exist or represents an oxygen atom; A represents OH or a C.sub.1 -C.sub.4 acyloxy group; B represents a hydrogen atom or may form a chemical bond along with A; X is an oxygen atom, nitrogen, sulfur, etc.; R.sup.1 and R.sup.2 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc.; R.sup.3 and R.sup.4 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc., or they may together form a 1,4-butylene or 1,5-pentylene group. The compounds have a strong activity of reinforcing the contraction of cardiac muscles and a strong activity of reducing the rate of heart beats. As they are not toxic, they are useful as cardiotonic medicines.

摘要翻译： PCT No.PCT / JP94 / 00544 Sec。 371 1995年9月29日第 102（e）1995年9月29日PCT PCT 1994年4月1日PCT公布。 第WO94 / 22442号公报 日期1994年10月13日被公开是强心药，当它们形成盐时，含有作为活性成分的至少一种式（I）化合物及其药理学上可接受的盐。 其中X1和X2不存在或表示氧原子; A表示OH或C1-C4酰氧基; B代表氢原子或与A形成化学键; X是氧原子，氮，硫等; R1和R2各自表示氢原子，C1-C4烷基等; R3和R4各自表示氢原子，C1-C4烷基等，或者它们可以一起形成1,4-亚丁基或1,5-亚戊基。 这些化合物具有强化心肌收缩的强烈活性和降低心脏搏动速率的强烈活性。 因为它们没有毒性，它们可用作强心药物。

公开(公告)号：US5840909A

公开(公告)日：1998-11-24

申请号：US998669

申请日：1997-12-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

摘要翻译： 式[1]的吡唑化合物及其互变异构体和盐：其中R1是烷基等; R2是羧基等; R3是卤素原子，烷基， 苯基等; R4，R5和R6分别是氢原子，卤素原子等; R7是羧基，5-四唑基等; X是氮原子等; Y和 Z各自为CH，氮原子等; A和E各自为亚甲基等; D为苯基等; G为共价键等）。 本发明化合物对血管紧张素II具有拮抗作用，可用于预防和治疗高血压，充血性心功能不全，慢性肾功能不全，醛固酮增多症，超眼压等。