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1. 发明授权

US06350759B1 Dihydro- and tetrahydro-quinoline compounds 失效
标题翻译：二氢 - 和四氢 - 喹啉化合物
公开(公告)号：US06350759B1
公开(公告)日：2002-02-26
申请号：US09425267
申请日：1999-10-22
申请人： Patrick Casara , Gilbert Dorey , Pierre Lestage , Brian Lockhart
发明人： Patrick Casara , Gilbert Dorey , Pierre Lestage , Brian Lockhart
IPC分类号： A61K3147
CPC分类号： C07D221/20 , C07D215/20 , C07D401/06 , C07D471/10
摘要： Compound of formula (I): wherein: R1 represents hydrogen or wherein A is as defined in the description, R2 and R3 each independently represents alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl,or optionally substituted aminoalkyl or R2 and R3, together with the carbon atom carrying them, form cycloalkyl or monocyclic heterocyclic group, substituted or unsubstituted, R40 represents hydrogen or a group selected from optionally substituted alkyl, optionally substituted alkenyl and optionally substituted alkynyl or Q or —V—Q wherein V represents alkylene, alkenylene or alkynylene and Q represents optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heterocycloalkyl,or optionally substituted heteroaryl, R41 and R5 together form a bond or each represents hydrogen, R6, R7, R8 and R9 each independently represents hydrogen, halogen, alkyl, (C3-C8)cycloalkyl,or —OW wherein W is as defined in the description, and medicinal products containing the same which are useful as antioxidative agents.
摘要翻译：式（I）化合物：其中：R1表示氢，或者其中A如说明书中所定义，R 2和R 3各自独立地表示烷基，环烷基，杂环烷基，任选取代的芳基，任选取代的杂芳基，环烷基烷基，杂环烷基烷基，任选取代的芳基烷基，取代的杂芳基烷基或任选取代的氨基烷基或R 2和R 3与携带它们的碳原子一起形成取代或未取代的环烷基或单环杂环基，R 40表示氢或选自任选取代的烷基，任选取代的烯基和任选取代的炔基或Q或-VQ，其中V表示亚烷基，亚烯基或亚炔基，Q表示任选取代的环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的杂芳基，R 41和R 5一起形成键或各自表示氢，R6，R7，R8 和R9各自独立地呈现氢，卤素，烷基，（C 3 -C 8）环烷基或-OW，其中W如说明书中所定义，以及含有该化合物的药物，其可用作抗氧化剂。

2. 发明授权

US06638962B2 Cycloheptene compounds 失效
标题翻译：环庚烯化合物
公开(公告)号：US06638962B2
公开(公告)日：2003-10-28
申请号：US10050666
申请日：2002-01-16
申请人： Patrick Casara , Thierry Le Diguarher , Gilbert Dorey , John Hickman , Alain Pierre , Gordon Tucker , Nicolas Guilbaud
发明人： Patrick Casara , Thierry Le Diguarher , Gilbert Dorey , John Hickman , Alain Pierre , Gordon Tucker , Nicolas Guilbaud
IPC分类号： A61K314174
CPC分类号： C07D233/64 , A61K31/4164 , C07D213/38 , C07D401/06
摘要： Compound of formula (I): wherein: X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—, Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, T represents —CH(R5)—, —N(R5)— or —N(R5)CO—, V represents hydrogen or unsubstituted or substituted aryl or heteroaryl, A2 represents [C(R6)(R′6)]p, R7 and R8 are as defined in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as farnesyl transferase inhibitors.
摘要翻译：式（I）的化合物：其中：X表示键或亚烷基，CO，S（O）n，-S（O）n -A1，-CO-A1-，-AS（O）n-A'1 - 或-A1-CO-A'1-，Y表示芳基，杂芳基，环烷基或杂环烷基，每个未取代或取代的，R 1，R 2，R 3和R 4各自独立地表示氢或芳基，杂芳基，环烷基或杂环烷基，每个未取代或取代的或R 1，R 2，R 3和R 4成对取代，一起形成键，或形成稠合苯环或稠合芳族或部分不饱和杂环，T表示-CH（R 5） - ， - N（ R5） - 或-N（R5）CO-，V表示氢或未取代或取代的芳基或杂芳基，A2表示[C（R6）（R'6）] p，R7和R8如说明书中所定义，并且其与药学上可接受的酸或碱的加成盐和含有它们的药物可用作法呢基转移酶抑制剂。

3. 发明授权

US5595976A Tetrahydropyran compounds 失效
标题翻译：四氢吡喃化合物
公开(公告)号：US5595976A
公开(公告)日：1997-01-21
申请号：US521189
申请日：1995-08-30
申请人： David Billington , Gilbert Dorey , Pascale Leon , Ghanem Atassi , Alain Pierre , Michael Burbridge , Nicolas Guilbaud
发明人： David Billington , Gilbert Dorey , Pascale Leon , Ghanem Atassi , Alain Pierre , Michael Burbridge , Nicolas Guilbaud
IPC分类号： C07H9/02 , A61K31/70 , A61K31/7028 , A61P9/00 , A61P29/00 , A61P35/00 , C07H9/04 , C07H15/04 , C07H15/10 , C07H15/18 , C07H15/26 , A61K37/00 , C07H3/00
CPC分类号： C07H9/04 , C07H15/04 , C07H15/10 , C07H15/26
摘要： A compound selected from those of formula (I): ##STR1## in which: A either represents --OR.sub.6, and B represents --CH.sub.2 --X,or, together with B and the carbon atom carrying them, forms an oxygen-containing heterocycle selected from oxirane, 2,2-dimethyl[1,3]dioxolane and [1,3]dioxolan-2-one,and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and X are as defined in the description.
摘要翻译：选自式（I）的化合物：其中：A表示-OR6，B表示-CH2-X，或者与B和携带它们的碳原子一起形成氧 - 含有杂环的环氧乙烷，2,2-二甲基[1,3]二氧戊环和[1,3]二氧戊环-2-酮，R1，R2，R3，R4，R5，R6和X如说明书中所定义。

4. 发明授权

US5258385A .beta.-Carboline-derived compounds, lamchart benzodiazepine-receptor ligands, having an inverse agonist and antagonist effect on benzodiazepines, and drugs containing them 失效
标题翻译：具有对苯并二氮杂类药物的反向激动剂和拮抗剂作用的β-α-胆甾醇衍生化合物，lamchart苯并二氮杂受体配体和含有它们的药物
公开(公告)号：US5258385A
公开(公告)日：1993-11-02
申请号：US834399
申请日：1992-02-12
申请人： Robert Dodd , Pierre Potier , Jean Rossier , Gilbert Dorey , Laurent Dubois , Lia Prado de Carvalho
发明人： Robert Dodd , Pierre Potier , Jean Rossier , Gilbert Dorey , Laurent Dubois , Lia Prado de Carvalho
IPC分类号： A61K31/435 , A61K31/55 , A61P25/20 , C07D405/04 , C07D471/14 , C07D491/14 , C07D491/147 , C07D495/14 , C07D213/81
CPC分类号： C07D405/04 , C07D471/14 , C07D491/14
摘要： The invention relates to novel .beta.-carboline-derived compounds which are benzodiazepine-receptor ligands having an inverse agonist and antagonist effect on benzodiazepines. These compounds are of the formulae: ##STR1## in which: X is O, S, ##STR2## or alternatively, ##STR3## represents the radical --N(R.sub.6)--C(=O)--CH.sub.2 --X, R.sub.1 is a hydroxyl, alkoxy or alkyl radical substituted by a hydroxyl or alkoxy radical,R.sub.2 is a hydrogen atom or an alkyl, hydroxyl, alkoxy, acyloxy or benzyloxy radical, it being possible for said radicals to be optionally substituted,R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are chosen from a hydrogen atom or an alkyl radical optionally substituted by a hydroxyl, alkoxy or alkoxycarbonylmethyl radical,as well as the corresponding tetrahydro derivatives of .beta.-carboline and the quaternary ammonium salts or derivatives of these pharmaceutically acceptable compounds.
摘要翻译：本发明涉及新的β-咔啉衍生化合物，它们是对苯并二氮杂类具有反向激动剂和拮抗作用的苯并二氮杂受体配体。这些化合物具有下列结构式：其中：X是O，S，，或者，IMA图表示基团-N（R 6）-C（= O）-CH 2 - X，R 1是被羟基或烷氧基取代的羟基，烷氧基或烷基，R 2是氢原子或烷基，羟基，烷氧基，酰氧基或苄氧基，所述基团可以任选被取代， R4，R5和R6选自氢原子或任选被羟基，烷氧基或烷氧基羰基甲基取代的烷基，以及相应的β-咔啉四氢衍生物和这些药学上可接受的化合物的季铵盐或衍生物。

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