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1. 发明授权

US5348967A Diaminotrifluoromethylpyridine derivatives, process for their production and phospholipase A.sub.2 inhibitor containing them 失效
标题翻译：二氨基三氟甲基吡啶衍生物，其制备方法和含有它们的磷脂酶A2抑制剂
公开(公告)号：US5348967A
公开(公告)日：1994-09-20
申请号：US35622
申请日：1993-03-23
申请人： Takahiro Haga , Hideo Sugi , Itaru Shigehara , Shinji Odawara , Syuichi Yotsuya , Hirohiko Kimura , Kazuhiro Yamamoto
发明人： Takahiro Haga , Hideo Sugi , Itaru Shigehara , Shinji Odawara , Syuichi Yotsuya , Hirohiko Kimura , Kazuhiro Yamamoto
IPC分类号： A61K31/4427 , A61P5/48 , A61P29/00 , C07D213/75 , C07D213/76 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D495/04 , A61K31/44
CPC分类号： C07D213/75 , C07D213/76 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D453/02 , C07D495/04
摘要： A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1)W.sup.2 R.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N(R.sup.11)R.sup.12, as defined herein.
摘要翻译：式（I）的二氨基三氟甲基吡啶衍生物或其盐：其中X为-CW1R1，-COCOR2，-CW1NHCOR2，-C（= W1）W2R3或-CW1N（R4）R5，Y为烷基，-CW 3 R 6，-COCOR 7，-NHCOR 7，-C（= W 3）W 4 R 8， - （NH）m SO 2 R 9， - （NH）m SO 2 OR 10或 - （NH）m SO 2 N（R 11）R 12。

2. 发明授权

US5260320A Diaminotrifluoromethylpyridine compounds and phospholipase A.sub.2 inhibitor containing them 失效
标题翻译：二氨基三氟甲基吡啶化合物和含有它们的磷脂酶A2抑制剂
公开(公告)号：US5260320A
公开(公告)日：1993-11-09
申请号：US921083
申请日：1992-07-29
申请人： Takahiro Haga , Hideo Sugi , Itaru Shigehara , Shinji Odawara , Syuichi Yotsuya , Hirohiko Kimura , Kazuhiro Yamamoto
发明人： Takahiro Haga , Hideo Sugi , Itaru Shigehara , Shinji Odawara , Syuichi Yotsuya , Hirohiko Kimura , Kazuhiro Yamamoto
IPC分类号： C07D213/75 , C07D213/76 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D495/04 , A61K31/44
CPC分类号： C07D213/75 , C07D213/76 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D417/12 , C07D453/02 , C07D495/04
摘要： A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1)W.sup.2 R.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N(R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted, each of R.sup.2 and R.sup.7, which are independent from each other, is alkyl which may be substituted, alkoxy which may be substituted, phenyl which may be substituted or phenoxy which may be substituted, each of R.sup.3, R.sup.8 and R.sup.10, which are independent from one another, is alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted or benzyl which may be substituted, each of R.sup.4, R.sup.5, R.sup.11 and R.sup.12, which are independent from one another, is alkyl which may be substituted, each of W.sup.1, W.sup.2, W.sup.3 and W.sup.4, which are independent from one another, is an oxygen atom or a sulfur atom, and m is 0 or 1, provided that a combination wherein one of X and Y is --COCF.sub.2 X.sup.1 wherein X.sup.1 is a hydrogen atom, a halogen atom, alkyl or haloalkyl, and the other is --COCF.sub.2 X.sup.2 wherein X.sup.2 is a hydrogen atom, a halogen atom, alkyl, haloalkyl or alkylcarbonyl, or --COOX.sup.3 wherein X.sup.3 is alkyl which may be substituted or phenyl which may be substituted, is excluded.
摘要翻译：式（I）的二氨基三氟甲基吡啶衍生物或其盐：其中X为-CW1R1，-COCOR2，-CW1NHCOR2，-C（= W1）W2R3或-CW1N（R4）R5，Y为烷基，-CW 3 R 6，-COCOR 7，-NHCOR 7，-C（= W3）W 4 R 8， - （NH）m SO 2 R 9， - （NH）m SO 2 OR 10或 - （NH）m SO 2 N（R 11）R 12，其中R 1，R 6和R 9各自彼此独立，可以被取代的链状烃基，可以被取代的单环烃基，可以被取代的多环烃基，可以被取代的单环杂环基或可以被取代的多环杂环基取代的，R 2和R 7各自独立地为可以被取代的烷基，可以被取代的烷氧基，可以被取代的苯基或可被取代的苯氧基，R 3，R 8和R 10各自为彼此独立地是可以被取代的烷基，可以被取代的链烯基，可被取代的炔基，其中的环烷基可被取代的苯基或可被取代的苄基，R 4，R 5，R 11和R 12各自彼此独立地是可以被取代的烷基，各自为W1，W2，W3和W4，其彼此独立的是氧原子或硫原子，并且m为0或1，条件是其中X和Y之一是-COCF 2 X 1的组合，其中X 1是氢原子，卤素原子，烷基或卤代烷基另一个是-COCF 2 X 2，其中X 2是氢原子，卤原子，烷基，卤代烷基或烷基羰基，或-COOX 3，其中X 3是可被取代的烷基或可被取代的苯基。

3. 发明授权

US5229403A Diaminotrifluoromethylpyridine derivatives and phospholipase A.sub.2 inhibitor containing them 失效
标题翻译：含有它们的二氨基三氟甲基吡啶衍生物和磷脂酶A2抑制剂
公开(公告)号：US5229403A
公开(公告)日：1993-07-20
申请号：US723377
申请日：1991-06-28
申请人： Takahiro Haga , Hideo Sugi , Itaru Shigehara , Shinji Odawara , Syuichi Yotsuya , Hirohiko Kimura , Kazuhiro Yamamoto
发明人： Takahiro Haga , Hideo Sugi , Itaru Shigehara , Shinji Odawara , Syuichi Yotsuya , Hirohiko Kimura , Kazuhiro Yamamoto
IPC分类号： A61K31/4427 , A61P5/48 , A61P29/00 , C07D213/75 , C07D213/76 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D495/04
CPC分类号： C07D213/75 , C07D213/76 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D453/02 , C07D495/04
摘要： A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1 (W.sup.2 W.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted, each of R.sup.2 and R.sup.7, which are independent from each other, is alkyl which may be substituted, alkoxy which may be substituted, phenyl which may be substituted or phenoxy which may be substituted, each of R.sup.3, R.sup.8 and R.sup.10, which are independent from one another, is alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted or benzyl which may be substituted, each of R.sup.4, R.sup.5, R.sup.11 and R.sup.12, which are independent from one another, is alkyl which may be substituted, each of W.sup.1, W.sup.2, W.sup.3 and W.sup.4, which are independent from one another, is an oxygen atom or a sulfur atom, and m is 0 or 1, provided that a combination wherein one of X and Y is --COCF.sub.2 X.sup.1 wherein X.sup.1 is a hydrogen atom, a halogen atom, alkyl or haloalkyl, and the other is --COCF.sub.2 X.sup.2 wherein X.sub.2 is a hydrogen atom, a halogen atom, alkyl, haloalkyl or alkylcarbonyl, or --COOX.sup.3 wherein X.sup.3 is alkyl which may be substituted or phenyl which may be substituted, is excluded.
摘要翻译：式（I）的二氨基三氟甲基吡啶衍生物或其盐：其中X为-CW1R1，-COCOR2，-CW1NHCOR2，-C（= W1（W2W3或-CW1N（R4）R5，Y为烷基，-CW 3 R 6，-COCOR 7，-NHCOR 7，-C（= W 3）W 4 R 8， - （NH）m SO 2 R 9， - （NH）m SO 2 OR 10或 - （NH）m SO 2 N R 11）R 12，其中R 1，R 6和R 9 彼此独立地是可以被取代的链状烃基，可以被取代的单环烃基，可以被取代的多环烃基，可以被取代的单环杂环基或可以被取代的多环杂环基相互独立的R 2和R 7各自为可被取代的烷基，可被取代的烷氧基，可被取代的烷氧基，可被取代的苯基或可被取代的苯氧基，R 3，R 8和R 10各自独立地可以是可以被取代的烷基，可以被取代的链烯基，可被取代的炔基，其中的环烷基可被取代的苯基或可被取代的苄基，R 4，R 5，R 11和R 12各自彼此独立地是可以被取代的烷基，各自为W1，W2，W3和W4，其彼此独立的是氧原子或硫原子，并且m为0或1，条件是其中X和Y之一是-COCF 2 X 1的组合，其中X 1是氢原子，卤素原子，烷基或卤代烷基另一个是-COCF 2 X 2，其中X 2是氢原子，卤原子，烷基，卤代烷基或烷基羰基，或-COOX 3，其中X 3是可被取代的烷基或可被取代的苯基。

4. 发明授权

US5098907A Powdery pharmaceutical composition containing benzoyl urea, a dispersant and silicic acid 失效
标题翻译：含有苯甲酸尿素，分散剂和硅酸的粉末药物组合物
公开(公告)号：US5098907A
公开(公告)日：1992-03-24
申请号：US469054
申请日：1990-01-23
申请人： Nobuo Kondo , Masahiro Kikuchi , Tsunetaka Nakajima , Masahiro Watanabe , Kouichi Yamauchi , Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi
发明人： Nobuo Kondo , Masahiro Kikuchi , Tsunetaka Nakajima , Masahiro Watanabe , Kouichi Yamauchi , Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi
IPC分类号： A61K9/14 , A61K31/44 , A61K31/505 , A61K47/14 , A61K47/26 , A61P35/00
CPC分类号： A61K9/14 , A61K31/44 , A61K31/505 , A61K47/14 , A61K47/26 , Y10S514/975
摘要： A powdery pharmaceutical composition comprising a benzoyl urea compound of the formula: ##STR1## wherein X is a halogen atom or a nitro group, Y is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group, Z.sub.1 is a halogen atom or a trifluoromethyl group, Z.sub.2 is a hydrogen atom or a halogen atom, and A is CH or a nitrogen atom, as an active ingredient, a nonionic surfactant as a dispersant, at least one member selected from the group consisting of sugar, sugar-alcohol and a nonionic surfactant as a disintegrant, and anhydrous silicic acid as a fluidizer.

5. 发明授权

US4973700A Method of purifying a microbicide 失效
标题翻译：净化杀微生物剂的方法
公开(公告)号：US4973700A
公开(公告)日：1990-11-27
申请号：US295628
申请日：1989-01-10
申请人： Ayako Sekikawa , Hideo Sugi , Ryoichi Takahashi
发明人： Ayako Sekikawa , Hideo Sugi , Ryoichi Takahashi
IPC分类号： A01N25/22 , A01N43/80 , A01N59/00 , A01N61/00 , C07D275/02 , C07D275/03
CPC分类号： C07D275/03 , A01N43/80 , A01N59/00 , A01N61/00
摘要： A clathrate compound is produced if a powdery host compound which reacts with a microbicide to form the clathrate compound is added into an aqueous solution of the microbicide. If the microbicide is separated from the clathrate compound, a microbicide of high purity can be obtained.

6. 发明授权

US4927919A Chartreusin derivatives and salts thereof 失效
标题翻译： Chartreusin衍生物及其盐
公开(公告)号：US4927919A
公开(公告)日：1990-05-22
申请号：US922433
申请日：1986-10-23
申请人： Nobutoshi Yamada , Hideo Sugi , Kenji Kon
发明人： Nobutoshi Yamada , Hideo Sugi , Kenji Kon
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P35/00 , C07H17/04
CPC分类号： C07H17/04
摘要： This invention relates to a novel chartreusin derivative of the general formula (I): ##STR1## and a salt thereof. This chartreusin derivative and a salt thereof have an excellent antitumor activity, which is exhibited even when the site of cancer inoculation and the site of drug administration are different. This invention further relates to a antitumorous composition containing the above-mentioned compound as active ingredient. This invention furthermore relates to a process for producing the above-mentioned chartreusin derivative or salt thereof.
摘要翻译：本发明涉及通式（I）的新颖的甲状腺素衍生物：其中（Ⅰ）及其盐。这种沙盘菌素衍生物及其盐具有优异的抗肿瘤活性，即使在癌症接种部位和药物给药部位不同的情况下也能够显示出来。本发明还涉及含有上述化合物作为活性成分的抗肿瘤组合物。本发明还涉及一种制备上述的沙特罗林衍生物或其盐的方法。

7. 发明授权

US4863924A N-benzoyl urea compounds, antitumorous compositions containing them 失效
标题翻译： N-苯甲酰脲化合物，含有它们的抗肿瘤组合物
公开(公告)号：US4863924A
公开(公告)日：1989-09-05
申请号：US939025
申请日：1986-12-08
申请人： Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi , Hiroshi Okada
发明人： Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi , Hiroshi Okada
IPC分类号： C07D213/64 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/50 , A61K31/505 , A61P35/00 , C07D213/643 , C07D237/14 , C07D239/34
CPC分类号： C07D213/643 , C07D237/14 , C07D239/34
摘要： An N-benzoyl urea compound having the formula: ##STR1## wherein X is a hydrogen atom, a halogen atom or a nitro group, n is an integer of from 1 to 3, and Q is ##STR2## wherein Y.sub.1 is an unsubstituted or substituted alkyl group, or an alkoxy or alkoxycarbonyl group with its alkyl moiety unsubstituted or substituted, Y.sub.2 is a hydrogen atom, a halogen atom, a nitro group, an unsubstituted or substituted alkyl group, or an alkoxy or alkoxycarbonyl group with its alkyl moiety unsubstituted or substituted, Z is a hydrogen atom, a halogen atom, a trifluoromethyl group or a nitro group, and each of A and B is .dbd.CH-- or a nitrogen atom, provided that one of A and B is .dbd.CH-- and the other is a nitrogen atom, with the provisos (1) that when Q is ##STR3## where when X is a hydrogen atom and Y.sub.1 is an alkyl group, Z is not a hydrogen atom, a halogen atom nor a trifluoromethyl group, and (2) that when Q is ##STR4## wherein A is a nitrogen atom and Y.sub.1 is a trifluoromethyl group, Y.sub.2 is other than a hydrogen atom.
摘要翻译：具有下式的N-苯甲酰脲化合物：其中X是氢原子，卤素原子或硝基，n是1至3的整数，Q是＆lt; IMAGE＆gt; 其中Y1是未取代或取代的烷基，或其烷基部分被未取代或取代的烷氧基或烷氧基羰基，Y2是氢原子，卤素原子，硝基，未取代或取代的烷基或烷氧基或其烷基部分为未取代或取代的烷氧基羰基，Z为氢原子，卤素原子，三氟甲基或硝基，A和B各自为= CH-或氮原子，条件是A和 B是= CH-，另一个是氮原子，条件是（1）当Q是 + TR 时，当X是氢原子且Y1是烷基时，Z是不是氢原子，卤素原子或三氟甲基，和（2）当Q是氮时，其中A是氮原子，Y 1是三氟甲基堆，Y2不是氢原子。

8. 发明授权

US4845093A N-benzoyl-N'-pyridazinyloxyphenyl urea compounds, and antitumorous compositions containing them, and process for their preparation 失效
标题翻译： N-苯甲酰基-N'-哒嗪氧基苯基脲化合物和含有它们的抗肿瘤组合物及其制备方法
公开(公告)号：US4845093A
公开(公告)日：1989-07-04
申请号：US111080
申请日：1987-10-19
申请人： Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi , hiroshi Okada
发明人： Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi , hiroshi Okada
IPC分类号： A61K31/50 , A61P35/00 , C07D237/14
CPC分类号： C07D237/14 , A61K31/50
摘要： An N-benzoyl-N'-pyridazinyloxyphenyl urea compound having the formula: ##STR1## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a nitro group, Y is a hydrogen atom, a halogen atom or a methyl group which may be substituted by fluorine, and Z is a hydrogen atom, a halogen atom or a trifluoromethyl group, provided that when X.sub.1 is a hydrogen atom and X.sub.2 is a hydrogen atom or a halogen atom, Y is a methyl group which may be substituted by fluorine and/or Z is a hydrogen atom or a trifluoromethyl group. The compound is useful as an active ingredient for an antitumorous composition.
摘要翻译：具有下式的N-苯甲酰基-N'-哒嗪氧基苯基脲化合物：其中X1和X2各自为氢原子，卤素原子或硝基，Y为氢原子，卤素原子或可以被氟取代的甲基，Z是氢原子，卤素原子或三氟甲基，条件是当X1为氢原子，X2为氢原子或卤素原子时，Y为甲基，可以被氟取代，和/或Z是氢原子或三氟甲基。该化合物可用作抗肿瘤组合物的活性成分。

9. 发明授权

US4818771A Diphenic acid bis(dicyclohexylamide) for clothrate compound, process for producing the same 失效
标题翻译：二苯甲酸双（二环己基酰胺）用于布料化合物，其制备方法
公开(公告)号：US4818771A
公开(公告)日：1989-04-04
申请号：US941004
申请日：1986-12-12
申请人： Fumio Toda , Ayako Sekikawa , Hideo Sugi , Kenji Tahara
发明人： Fumio Toda , Ayako Sekikawa , Hideo Sugi , Kenji Tahara
IPC分类号： A01N37/18 , A01N25/08 , A61K47/48 , C07C67/00 , C07C231/00 , C07C233/65 , A61L3/00 , C02B1/18 , C07C103/24
CPC分类号： C07C233/65 , A01N25/08 , A61K47/48023 , C07C2101/14
摘要： Diphenic acid bis(dicyclohexylamide) represented by the following formula: ##STR1## A process for producing diphenic acid bis(dicyclohexylamide) represented by the above formula, which comprises dimerizing a diazonium salt of o-aminobenzoic acid in the presence of a reducing agent, followed by acidification to give 2,6'-dicarboxylbiphenyl; converting this dicarboxylic acid to 2,6'-dichloroformylbiphenyl by chlorination; and reacting this acid chloride with dicyclohexylamine.Sustained release antimicrobial compositions comprising a clathrate compound consisting of a microbial agent and diphenic acid bis(dicyclohexylamide) represented by the above formula.
摘要翻译：由下式表示的二苯酸双（二环己基酰胺）：由上式表示的二苯酸双（二环己基酰胺）的制造方法，其包括在还原剂存在下使邻氨基苯甲酸的重氮盐二聚，然后酸化得到2,6-二羧基联苯; 通过氯化将该二羧酸转化为2,6-二氯甲酰基联苯; 并使该酰氯与二环己基胺反应。包含由上式表示的微生物剂和二苯酸双（二环己基酰胺）组成的包合物的缓释抗微生物组合物。

10. 发明授权

US4387218A Anthracycline antibiotics FA-1180 B and B.sub.1, or salts thereof 失效
标题翻译：蒽环类抗生素FA-1180B和B1或其盐
公开(公告)号：US4387218A
公开(公告)日：1983-06-07
申请号：US299259
申请日：1981-09-03
申请人： Hiroyuki Mori , Yasuo Ogawa , Hideo Sugi , Noboru Fujikawa , Kiyoshi Tamai
发明人： Hiroyuki Mori , Yasuo Ogawa , Hideo Sugi , Noboru Fujikawa , Kiyoshi Tamai
IPC分类号： C07G11/00 , A61K35/74 , A61P31/04 , A61P35/00 , C07H15/252 , C12P1/06 , C12P19/56 , C12R1/01 , C12R1/03 , C07H15/24
CPC分类号： C07H15/252 , C12P19/56 , C12R1/03
摘要： An anthracycline antibiotic FA-1180 A, A.sub.1, B or B.sub.1, or salts thereof, said antibiotic having the formula (I): ##STR1## wherein R represents an acetyl group or a 1-hydroxyethyl group.
摘要翻译：蒽环类抗生素FA-1180A，A1，B或B1或其盐，所述具有式（I）的抗生素：其中R表示乙酰基或1-羟乙基。

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