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1. 发明授权

US5272271A Pyranobenzoxadiazole derivatives 失效
标题翻译：苯并恶唑衍生物
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.

2. 发明授权

US4900752A Pyranobenzoxadiazole derivatives 失效
标题翻译：苯并恶唑衍生物
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。

3. 发明授权

US5919806A Medicines for cardiac insufficiency 失效
标题翻译：心脏功能不全的药物
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。

4. 发明授权

US4843076A Dihydropyridine-5-phosphonic acid cyclic ester 失效
标题翻译：二氢吡啶-5-膦酸环酯
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。

5. 发明授权

US5177237A Hydrazine derivatives useful as intermediates in the synthesis of hypotensive agents 失效
标题翻译：在合成代谢药物中作为中间体有用的氢INE衍生物
公开(公告)号：US5177237A
公开(公告)日：1993-01-05
申请号：US783103
申请日：1991-10-24
申请人： Hiroo Matsumoto , Kiyotomo Seto , Ryozo Sakoda
发明人： Hiroo Matsumoto , Kiyotomo Seto , Ryozo Sakoda
IPC分类号： C07F9/6574 , C07F9/6571
CPC分类号： C07F9/657181
摘要： A hydrazine derivative having the formula: ##STR1## wherein R is a hydrogen atom or ##STR2##

6. 发明授权

US5319089A Process for the optical resolution of pyranobenzoxadiazole compounds 失效
标题翻译：吡喃并苯并恶二唑化合物的光学拆分方法
公开(公告)号：US5319089A
公开(公告)日：1994-06-07
申请号：US780357
申请日：1991-10-22
申请人： Hiroo Matsumoto , Kiyotomo Seto , Ryozo Sakoda
发明人： Hiroo Matsumoto , Kiyotomo Seto , Ryozo Sakoda
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： A process for the optical resolution of a pyranobenzoxadiazole compound represented by the formula [(.+-.)I]: ##STR1## which comprises reacting the compound [(.+-.)I] with an optically active carboxylic acid represented by the formula [II]: ##STR2## and separating the diastereomeric salt thus formed is disclosed.
摘要翻译：用于光学拆分由式[（+/-）I]表示的吡喃并苯并恶二唑化合物的方法：包括使化合物[（+/-）I]与光学公开了由式[II]表示的活性羧酸：＆lt; IMAGE＆gt;并分离如此形成的非对映体盐。

7. 发明授权

US4879400A Process for producing alpha-(benzylidene)acetonylphosphonates 失效
标题翻译：制备α-（亚苄基）丙酰基膦酸酯的方法
公开(公告)号：US4879400A
公开(公告)日：1989-11-07
申请号：US145042
申请日：1988-01-19
申请人： Kiyotomo Seto , Hiroo Matsumoto , Ryozo Sakoda
发明人： Kiyotomo Seto , Hiroo Matsumoto , Ryozo Sakoda
IPC分类号： C07F9/40 , C07F9/6571
CPC分类号： C07F9/657181 , C07F9/4015
摘要： A process for producing an .alpha.-(benzylidene)acetonylphosphonate of the formula: ##STR1## wherein Ar is phenyl substituted by at least one substituent selected from the group consisting of fluorine, chlorine, bromine, nitro, chloromethyl, dichloromethyl, trichloromethyl, trifluoromethyl, --CO.sub.2 R.sup.7 wherein R.sup.7 is C.sub.1 -C.sub.5 alkyl, --CONR.sup.7 R.sup.8 wherein R.sup.7 is as defined above and R.sup.8 is C.sub.1 -C.sub.5 alkyl, --C(O)R.sup.7 wherein R.sup.7 is as defined above, --OC(O)R.sup.7 wherein R.sup.7 is as defined above, --OSO.sub.3 R.sup.7 wherein R.sup.7 is as defined above, --OCF.sub.3, --S(.dbd.O).sub.2 R.sup.7 wherein R.sup.7 is as defined above, --CN and --SO.sub.3 R.sup.7 wherein R.sup.7 is as defined above, and each of R.sup.1 and R.sup.2 which may be the same or different is a saturated or unsaturated C.sub.1 -C.sub.12 aliphatic group, or R.sup.1 and R.sup.2 together form 1,2-ethylene, 1,3-propylene or 1,4-butylene, which is unsubstituted or substituted by from one to four C.sub.1 -C.sub.3 alkyl groups, which comprises:(a) reacting an aldehyde of the formula:ArCHO (I)wherein Ar is as defined above, with an acetonylphosphonate of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, in the presence of a secondary amine of the formula: ##STR3## wherein each of R.sup.3 and R.sup.4 which may be the same or different is C.sub.1 -C.sub.4 alkyl, or R.sub.3 and R.sub.4 together form 1,4-butylene or 1,5-pentylene, which is unsubstituted or substituted by from one to four C.sub.1 -C.sub.2 alkyl groups, --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 --, and an .alpha.-halogeno fatty acid of the formula: ##STR4## wherein X is fluorine, chlorine, bromine or iodine, and each of R.sup.5 and R.sup.6 which may be the same or different is hydrogen, fluorine, chlorine, bromine, iodine or C.sub.1 -C.sub.4 alkyl; or(b) reacting a compound of the formula ##STR5## wherein Ar, R.sup.1 and R.sup.2 are as defined above, with an acetonylphosphonate of the formula II as defined above, in the presence of an .alpha.-halogeno fatty acid of the formula V as defined above.

8. 发明授权

US5097037A Process for the optical resolution of pyranobenzoxadiazole compounds 失效
标题翻译：吡喃并恶唑化合物的光学分解方法
公开(公告)号：US5097037A
公开(公告)日：1992-03-17
申请号：US551795
申请日：1990-07-12
申请人： Hiroo Matsumoto , Kiyotomo Seto , Ryozo Sakoda
发明人： Hiroo Matsumoto , Kiyotomo Seto , Ryozo Sakoda
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： A process for the optical resolution of a pyranobenzoxadiazole compound represented by the formula [(.+-.)I]: ##STR1## which comprises reacting the compound [(.+-.)I] with an optically active carboxylic acid represented by the formula [II]: ##STR2## and separating the diastereomeric salt thus formed is disclosed.

9. 发明授权

US4885284A Dihydropyridine-5-phosphonic acid cyclic propylene ester 失效
标题翻译：二氢吡啶-5-膦酸环丙烯酯
公开(公告)号：US4885284A
公开(公告)日：1989-12-05
申请号：US851158
申请日：1986-04-14
申请人： Kiyotomo Seto , Sakuya Tanaka , Ryozo Sakoda
发明人： Kiyotomo Seto , Sakuya Tanaka , Ryozo Sakoda
IPC分类号： C07F9/6571
CPC分类号： C07F9/657181
摘要： A compound of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 which may be the same or different, is hydrogen or C.sub.1 -C.sub.4 alkyl; one of X.sup.1 and X.sup.2 is nitro, fluroine, chlorine, difluoromethyoxy or trifluoromethyl and the other is hydrogen, or both of X.sup.1 and X.sup.2 are chlorine; and Y is ##STR2## wherein A is C.sub. -C.sub.6 alkylene, each of Ar.sup.1 and Ar.sup.2 which may be the same or different, is phenyl which may be substituted by chlorine, fluorine or C.sub.1 -C.sub.3 alkoxy, and m is an integer of from 0 to 4, or Y is ##STR3## wherein A, Ar.sup.1 and Ar.sup.2 are as defined above when that both X.sup.1 and X.sup.2 are chlorine; or a pharmaceutically acceptable salt thereof.
摘要翻译：下式的化合物：其中R 1，R 2，R 3，R 4，R 5和R 6可以相同或不同的是氢或C 1 -C 4烷基; X1和X2之一是硝基，氟，氯，二氟甲氧基或三氟甲基，另一个是氢，或者X1和X2都是氯; 并且Y为其中A为C-C6亚烷基，Ar1和Ar2可以相同或不同，为可被氯，氟或C1-C3烷氧基取代的苯基，m为 0〜4，或Y为，其中当X1和X2都为氯时，A，Ar1和Ar2如上定义; 或其药学上可接受的盐。

10. 发明授权

US5508403A Phosphorus pyridine compound 失效
标题翻译：磷吡啶化合物
公开(公告)号：US5508403A
公开(公告)日：1996-04-16
申请号：US463511
申请日：1995-06-05
申请人： Shin-ichi Akiyama , Ryozo Sakoda , Kiyotomo Seto , Norimasa Shudo
发明人： Shin-ichi Akiyama , Ryozo Sakoda , Kiyotomo Seto , Norimasa Shudo
IPC分类号： A61K31/675 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/66 , A61K31/665 , A61P35/00 , A61P43/00 , C07D213/80 , C07F9/58 , C07F9/59 , C07F9/6558 , C07F9/6571 , C07F9/6574
CPC分类号： A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/66 , A61K31/665 , A61K31/675 , C07F9/587 , C07F9/597 , C07F9/657181
摘要： An agent for enhancing the drug effects of an antitumor drug, which comprises a compound of the formula I: ##STR1## or a pharmaceutically acceptable salt of the compound.
摘要翻译：一种用于增强抗肿瘤药物的药物作用的药剂，其包含式I化合物或其药学上可接受的盐。

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