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31. 发明授权

US06359134B1 Sulfonamide derivatives, their production and use 失效
标题翻译：磺酰胺衍生物，其生产和使用
公开(公告)号：US06359134B1
公开(公告)日：2002-03-19
申请号：US09424892
申请日：1999-11-30
申请人： Hiroyuki Tawada , Fumio Ito , Norihiko Moriya , Zen-ichi Terashita
发明人： Hiroyuki Tawada , Fumio Ito , Norihiko Moriya , Zen-ichi Terashita
IPC分类号： C07D29518
CPC分类号： C07D213/30 , C07D211/34 , C07D213/56 , C07D213/82 , C07D231/12 , C07D233/56 , C07D233/88 , C07D239/26 , C07D239/42 , C07D249/08 , C07D277/56 , C07D295/26 , C07D307/82 , C07D311/58 , C07D401/04 , C07D405/04 , C07D409/04 , C07D417/04 , C07D417/14
摘要： The present invention provides compounds which specifically inhibit FXa, which are effective when orally administered and which are useful as a safe medicine for the prevention or treatment of diseases caused by thrombus or infarction. Compounds of this invention are piperazinones of the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, in addition to being substituted by the group of the formula: and the group of the formula: Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent heterocyclic group; X is a direct bond or an optionally substituted alkylene chain; Z is (1) an amino group substituted with an optionally substituted hydrocarbon group, (2) an optionally substituted imino group or (3) an optionally substituted nitrogen-containing heterocyclic group; provided that when X is a direct bond and Z is an optionally substituted 6-membered nitrogen-containing aromatic heterocyclic group, Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent unsaturated heterocyclic group; or a salt thereof.
摘要翻译：本发明提供特异性抑制FXa的化合物，其在口服给药时是有效的，并且其可用作预防或治疗由血栓或梗塞引起的疾病的安全药物。本发明的化合物是下式的哌嗪酮：其中R1是任选取代的烃基或任选取代的杂环基; 环A是任选取代的二价含氮杂环基，除了被下式所示的基团取代：下式基团：Y是任选取代的二价烃基或任选取代的二价杂环基; X是直接键或任选取代的亚烷基链; Z是（1）被任选取代的烃基取代的氨基，（2）任选取代的亚氨基或（3）任选取代的含氮杂环基; 条件是当X是直接键，Z是任选取代的6元含氮芳族杂环基时，Y是任选取代的二价烃基或任选取代的二价不饱和杂环基; 或其盐。

32. 发明授权

US06169102A Oxazolone derivatives and their use as anti-Helicobacter pylori agent 失效
标题翻译：恶唑酮衍生物及其作为抗幽门螺旋杆菌药物的用途
公开(公告)号：US06169102A
公开(公告)日：2001-01-02
申请号：US09142506
申请日：1998-09-10
申请人： Tsuneo Kanamaru , Masafumi Nakao , Hiroyuki Tawada , Keiji Kamiyama
发明人： Tsuneo Kanamaru , Masafumi Nakao , Hiroyuki Tawada , Keiji Kamiyama
IPC分类号： A61K31422
CPC分类号： C07D413/06 , C07D263/48 , C07D413/14 , C07D471/04 , C12P17/16
摘要： An anti-Helicobacter pylori agent comprising a compound represented by the formula: wherein A represents an aromatic ring group which may be substituted; R1 and R2, whether identical or not, each represent a hydrogen atom or a hydrocarbon group which may be substituted; R3 and R4, whether identical or not, each represent a hydrogen atom, a hydrocarbon group which may be substituted, an acyl group, a carbamoyl group which may be substituted, or a carboxyl group which may be esterified; or a salt thereof.
摘要翻译：一种抗幽门螺杆菌药物，其包含由下式表示的化合物：其中A表示可被取代的芳族环基团; R1和R2各自表示氢原子或可被取代的烃基; R 3和R 4各自表示氢原子，可被取代的烃基，酰基，可被取代的氨基甲酰基或可被酯化的羧基; 或其盐。

33. 发明授权

US5418239A Tricyclic heterocyclic compounds, their production and use 失效
标题翻译：三环杂环化合物，其生产和使用
公开(公告)号：US5418239A
公开(公告)日：1995-05-23
申请号：US117950
申请日：1993-09-08
申请人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： A61K31/365 , A61K31/435 , A61P3/06 , A61P9/08 , A61P9/10 , C07D221/06 , C07D221/08 , C07D221/16 , C07D311/78 , C07D311/92 , C07D311/94 , A61K31/44
CPC分类号： C07D221/16 , C07D221/08 , C07D311/92 , C07D311/94
摘要： Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.
摘要翻译：新颖的通式如下的杂环化合物：其中环A和环B各自表示取代或未取代的苯环; X表示下式的基团：其中R 2为氢，烷基或烷氧基; m为0或1，式为：其中R 3为氢或烷基，或下式：-O-CO-; Y表示键，-NH-，C1或2亚烷基或-CH = CH-; R1表示取代或未取代的烃基; n表示具有优异酰基辅酶A：胆固醇酰基转移酶抑制活性的整数3〜6或其盐，及其制备方法及其用途。

34. 发明授权

US5264454A Certain 2-oxo-tetrahydro-cycloalkyl-benzopyran-3yl ureas having acyl-CoA-cholesterol acyl transferase inhibitory activity 失效
标题翻译：具有酰基-CoA-胆固醇酰基转移酶抑制活性的某些2-氧代 - 四氢 - 环烷基 - 苯并吡喃-3-基脲
公开(公告)号：US5264454A
公开(公告)日：1993-11-23
申请号：US765182
申请日：1991-09-25
申请人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： A61K31/365 , A61K31/435 , A61P3/06 , A61P9/08 , A61P9/10 , C07D221/06 , C07D221/08 , C07D221/16 , C07D311/78 , C07D311/92 , C07D311/94 , A61K31/35
CPC分类号： C07D221/16 , C07D221/08 , C07D311/92 , C07D311/94
摘要： Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen, an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.

35. 发明授权

US5256782A Thienopyridine derivatives which are intermediates 失效
标题翻译：作为中间体的噻吩并吡啶衍生物
公开(公告)号：US5256782A
公开(公告)日：1993-10-26
申请号：US886081
申请日：1992-05-20
申请人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： C07D495/04 , C07D495/02 , C07D495/14
CPC分类号： C07D495/04
摘要： Thienopyridine derivatives of the formula (I): ##STR1## wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: ##STR2## (wherein R.sup.1 is hydrogen, alkyl or alkoxy; and n is 0 or 1) or a group of the formula: ##STR3## (wherein R.sup.2 is hydrogen or alkyl); Y is a single bond, --NH--, alkylene having 1 or 2 carbon atoms or --CH.dbd.CH--; and R.sup.3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.
摘要翻译：式（I）的噻吩并吡啶衍生物：其中环A是任选取代的苯环; 环B是任选取代的噻吩环：X是下式的基团：其中R 1是氢，烷基或烷氧基，n是0或1）或下式的基团：其中 R2是氢或烷基）; Y是单键，-NH-，具有1或2个碳原子的亚烷基或-CH = CH-; 并且R 3是任选取代的烃基，或其盐。他们表现出强烈的ACAT抑制活性。

36. 发明授权

US5143919A Thienopyridine derivatives and their pharmaceutical use 失效
标题翻译：噻吩吡啶衍生物及其药物用途
公开(公告)号：US5143919A
公开(公告)日：1992-09-01
申请号：US744492
申请日：1991-08-13
申请人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Thienopyridine derivatives of the formula (I): ##STR1## wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: ##STR2## (wherein R.sup.1 is hydrogen, alkyl or alkoxy; and n is 0 or 1) or a group of the formula: ##STR3## (wherein R.sup.2 is hydrogen or alkyl); Y is a single bond, --NH--, alkylene having 1 or 2 carbon atoms or --CH.dbd.CH--; and R.sup.3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.

37. 发明授权

US4349547A Suppressing obesity and over-secretion of insulin with 2-(.alpha.-hydroxy-m-trifluoromethylbenzyl)azetidine 失效
标题翻译：用2-（α-羟基 - 间 - 三氟甲基苄基）氮杂环丁烷抑制胰岛素的肥胖和过度分泌
公开(公告)号：US4349547A
公开(公告)日：1982-09-14
申请号：US178951
申请日：1980-08-18
申请人： Kanji Meguro , Hiroyuki Tawada , Takao Matsuo
发明人： Kanji Meguro , Hiroyuki Tawada , Takao Matsuo
IPC分类号： A61K31/395 , A61K31/397 , A61P3/04 , C07D205/04
CPC分类号： C07D205/04 , Y10S514/884 , Y10S514/91
摘要： 2-(.alpha.-hydroxy-m-trifluoromethylbenzyl)azetidine and its physiologically acceptable acid addition salts have antiobesity action as well as suppressive action against oversecretion of insulin.
摘要翻译： 2-（α-羟基 - 间 - 三氟甲基苄基）氮杂环丁烷及其生理上可接受的酸加成盐具有抗肥胖作用以及抑制胰岛素过分分泌的作用。

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