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1. 发明授权

US5266591A Ethanolamine benzoate compounds 失效
标题翻译：乙醇胺苯甲酸酯化合物
公开(公告)号：US5266591A
公开(公告)日：1993-11-30
申请号：US979202
申请日：1992-11-20
申请人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Michelle Boulanger , Francoise Lacour
发明人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Michelle Boulanger , Francoise Lacour
IPC分类号： A61K31/24 , A61P3/06 , A61P3/08 , A61P7/00 , A61P9/12 , C07C233/51 , C07C235/34
CPC分类号： C07C233/51 , C07C2103/18
摘要： The compounds are ethanolamine benzoate compounds useful for the treatment of syndrome X, and of hypertension in patients who are insulin resistant or have one or more metabolic anomalies.A compound disclosed is S-1-(m-trifluoromethylphenyl)-2-{.beta.-{4-[2-(N-(3,3-diphenylpropionyl)amino)ethyl] benzoyloxy}ethylamino} propane.
摘要翻译：这些化合物是可用于治疗综合征X的乙醇胺苯甲酸酯化合物，以及患有胰岛素抵抗或具有一种或多种代谢异常的患者的高血压。所公开的化合物是S-1-（间三氟甲基苯基）-2- {β-（4- [2-（N-（3,3-二苯基丙酰基）氨基）乙基]苯甲酰氧基}乙基氨基}丙烷。

2. 发明授权

US5079245A 2-trifluoromethyl-7-substitute-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes 失效
标题翻译： 2-三氟甲基-7-取代基-6,7,8,9-四氢 - （5H） - 苄氧基羰基
公开(公告)号：US5079245A
公开(公告)日：1992-01-07
申请号：US375591
申请日：1989-07-05
申请人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Francoise Lacour
发明人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Francoise Lacour
IPC分类号： A61K31/045 , A61K31/12 , A61K31/135 , A61K31/15 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/275 , A61K31/415 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/10 , C07C29/38 , C07C35/23 , C07C45/00 , C07C49/697 , C07C67/00 , C07C209/00 , C07C209/40 , C07C209/48 , C07C209/50 , C07C209/52 , C07C209/62 , C07C211/30 , C07C211/42 , C07C211/52 , C07C215/08 , C07C215/42 , C07C215/44 , C07C219/14 , C07C223/02 , C07C229/14 , C07C231/06 , C07C231/10 , C07C233/13 , C07C233/14 , C07C233/36 , C07C233/66 , C07C241/00 , C07C251/04 , C07C251/18 , C07C251/20 , C07C251/24 , C07D211/18 , C07D233/04 , C07D295/06 , C07D295/073 , C07D521/00
CPC分类号： C07D295/073 , C07C211/30 , C07C211/42 , C07C215/08 , C07C215/44 , C07C219/14 , C07C229/14 , C07C233/14 , C07C233/36 , C07C251/18 , C07D233/04 , C07C2102/12
摘要： The compounds 2-trifluoromethyl-7-substituted-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes are disclosed and disclosed to be useful in the treatment of metabolic illnesses such as diabetes, obesity, and their complications. A perferred compound is 2-trifluoromethyl-7-amino-6,7,8,9-tetrahydro-[5H-benzocycloheptane.
摘要翻译：公开和公开了化合物2-三氟甲基-7-取代-6,7,8,9-四氢 - [5H] - 苯并环庚烯，可用于治疗代谢疾病如糖尿病，肥胖及其并发症。延迟化合物是2-三氟甲基-7-氨基-6,7,8,9-四氢 - [5H-苯并环庚烷。

3. 发明授权

US5266718A Ethanolamine benzoate compounds 失效
标题翻译：乙醇胺苯甲酸酯化合物
公开(公告)号：US5266718A
公开(公告)日：1993-11-30
申请号：US898916
申请日：1992-06-12
申请人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Francoise Lacour , Michelle Boulanger
发明人： Michel Wierzbicki , Pierre Hugon , Jacques Duhault , Francoise Lacour , Michelle Boulanger
IPC分类号： C07C219/14 , C07C233/51 , C07C235/34 , C07C101/34
CPC分类号： C07C219/14 , C07C233/51 , C07C235/34 , C07C2103/18
摘要： New ethanolamine benzoate compounds which can be used as medicaments and correspond to the formula: ##STR1## wherein R is as defined in the description, in the form of racemic compounds and enantiomers. These new compounds and their physiologically tolerable salts can be used therapeutically for treatment of insulin-resistance states.
摘要翻译：新的可用作药物的乙醇胺苯甲酸酯化合物，其对应于下式：其中R如说明书中所定义，以外消旋化合物和对映体的形式。这些新化合物及其生理上可耐受的盐可用于治疗胰岛素抵抗状态。

4. 发明授权

US4711885A N-(N'-phenylpiperazine)-alkyl triazole compounds having anxiolytic and analgesic properties 失效
标题翻译：具有抗焦虑和止痛特性的N-（N'-苯基哌嗪） - 烷基三唑化合物
公开(公告)号：US4711885A
公开(公告)日：1987-12-08
申请号：US846911
申请日：1986-04-01
申请人： Michel Wierzbicki , Pierre Hugon , Jean-Claude Poignant
发明人： Michel Wierzbicki , Pierre Hugon , Jean-Claude Poignant
IPC分类号： A61K31/495 , A61K31/55 , A61P25/04 , A61P25/20 , C07D209/52 , C07D215/22 , C07D217/24 , C07D221/04 , C07D295/14 , C07D317/66 , C07D453/00 , C07D453/06 , C07D471/04 , C07D471/18 , C07D487/04 , C07D401/14 , C07D403/14
CPC分类号： C07D471/04 , C07D487/04
摘要： Triazole compounds of the formula: ##STR1## in which: X and X', which are the same or different, each represents hydrogen, halogen, trifluoromethyl, C.sub.1 -.sub.5 alkyl, or C.sub.1 -.sub.5 alkoxy, orX and X' together represent methylenedioxy,n is an integer of from 1 to 6,a is 0, 1 or 2;b is 0, 1, 2 or 3;c is 0, 1 or 2 andd is 2, 3, 4 or 5 such that a+b+c+d is equal to 4, 5, 6 or 7.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of pain and anxiety.
摘要翻译：下式的三唑化合物：其中：X和X'相同或不同，表示氢，卤素，三氟甲基，C 1-5烷基或C 1-5烷氧基，或X和X'一起代表亚甲二氧基 n为1〜6的整数，a为0,1或2， b为0,1,2或3; c为0,1或2，d为2,3,4或5，使得+ b + c + d等于4,5,6或7.这些化合物及其生理上可耐受的酸加成盐可用作药物特别是治疗疼痛和焦虑症。

5. 发明授权

US06465660B1 Isoindoloindolone compounds 失效
标题翻译：异吲哚啉酮化合物
公开(公告)号：US06465660B1
公开(公告)日：2002-10-15
申请号：US10083074
申请日：2002-02-26
申请人： Michel Wierzbicki , Marie-Françoise Boussard , Anne Rousseau , Jean Albert Boutin , Philippe Delagrange
发明人： Michel Wierzbicki , Marie-Françoise Boussard , Anne Rousseau , Jean Albert Boutin , Philippe Delagrange
IPC分类号： C07D20958
CPC分类号： C07D487/04
摘要： Compound of formula (I): wherein: R1, R2, R3, R4, R5, R6 and R8, which may be identical or different, each represents hydrogen, alkyl, arylalkyl, hydroxy, alkoxy, arylalkoxy, acyloxy, arylcarbonyloxy, carboxyalkyl or carboxy, R7 represents hydrogen, hydroxy, alkoxy, arylalkoxy, acyloxy or arylcarbonyloxy group, or one of R1 to R8, together with another of R1 to R8 adjacent to it, forms an alkylenedioxy, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
摘要翻译：式（I）化合物：其中：R 1，R 2，R 3，R 4，R 5，R 6和R 8可以相同或不同，各自表示氢，烷基，芳基烷基，羟基，烷氧基，芳基烷氧基，酰氧基，芳基羰基氧基，羧基烷基或羧基，R 7表示氢，羟基，烷氧基，芳基烷氧基，酰氧基或芳基羰基氧基，或R 1至R 8中的一个与R 1至R 8中的另一个一起形成亚烷基二氧基，其光学异构体及其加成盐与药学上可接受的酸或碱。

6. 发明授权

US5061704A Thiophene compounds, compositions and use 失效
标题翻译：噻吩化合物，组成和用途
公开(公告)号：US5061704A
公开(公告)日：1991-10-29
申请号：US617501
申请日：1990-11-23
申请人： Michel Wierzbicki , Frederic Sauveur , Jacqueline Bonnet , Martine Brisset , Charles Tordjman
发明人： Michel Wierzbicki , Frederic Sauveur , Jacqueline Bonnet , Martine Brisset , Charles Tordjman
IPC分类号： A61K31/38 , A61K31/381 , A61K31/495 , A61K31/535 , A61K31/54 , A61P3/00 , A61P43/00 , C07D333/20 , C07D333/24
CPC分类号： C07D333/24 , C07D333/20
摘要： 1. New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.2. As new intermediate products used in the synthesis of the compounds I above defined, the amides of the formula: ##STR2## in which: X, n, a, b, c, R.sub.1, R.sub.2, R and R' are as above defined.
摘要翻译： 1.下式的新噻吩化合物：其中：X表示氢，卤素，C 1 -C 5烷基或烷氧基或二烷基氨基; n表示1或2; a表示2〜6的整数， b表示2或3; c表示1或2，并且b + c = 4; R1和R2表示氢或（C1-C5）烷基，或与它们所键合的碳原子一起形成含有3至6个碳原子的烃环; 并且R和R'表示氢或（C1-C5）烷基，或与它们所键合的氮原子一起形成任选地含有氧原子的五价或六价杂环或本身可被取代的第二氮原子; 及其生理上可耐受的盐。本发明的产品可以治疗特别用于治疗以组织损失为特征的病理学。 2.作为合成上述化合物I的新中间体产物，下式的酰胺如下：其中：X，n，a，b，c，R1，R2，R和R'如上所述定义

7. 发明授权

US4567196A Thieno [2,3-b] pyrrole compounds and their use in alleviating pain 失效
标题翻译：噻吩并[2,3-b]吡咯化合物及其在缓解疼痛中的应用
公开(公告)号：US4567196A
公开(公告)日：1986-01-28
申请号：US667909
申请日：1984-11-02
申请人： Michel Wierzbicki
发明人： Michel Wierzbicki
IPC分类号： A61K31/40 , A61P25/04 , A61P29/00 , C07D495/04 , C07D495/06 , A61K31/38
CPC分类号： C07D495/04
摘要： New thieno [2,3-b] pyrrole compounds of the formula: ##STR1## in which: R is hydrogen, (C.sub.1 -C.sub.5) alkyl, alkali or alkaline earth metals ammnonium or mono- di- or tri-(C.sub.1 -C.sub.5) alkylammnonium;R.sub.1 is hydrogen, or (C.sub.1 -C.sub.5) alkyl;R.sub.2 is hydrogen, (C.sub.1 -C.sub.5) alkyl, phenyl or phenyl-(C.sub.1 -C.sub.5) alkyl;R.sub.3 and R.sub.4, the same or different are each hydrogen, halogen, (C.sub.1 -C.sub.5) alkyl, (C.sub.1 -C.sub.5) alkoxy, orR.sub.3 and R.sub.4 together represent: --CH.dbd.CH--CH.dbd.CH--.These new compounds may be used as medicines especially in the treatment of acute or chronic pain.
摘要翻译：新型噻吩并[2,3-b]吡咯化合物，其结构式如下：其中：R为氢，（C1-C5）烷基，碱金属或碱土金属铵或单 - 或三 - （C1-C5 ）烷基铵; R1是氢或（C1-C5）烷基; R2是氢，（C1-C5）烷基，苯基或苯基 - （C1-C5）烷基; R 3和R 4相同或不同，各自为氢，卤素，（C 1 -C 5）烷基，（C 1 -C 5）烷氧基，或者R 3和R 4一起表示：-CH = CH-CH = CH-。这些新化合物可以用作药物，特别是用于治疗急性或慢性疼痛。

8. 发明授权

US08404742B2 Diosmetin compounds, a process for their preparation and pharmaceutical compositions containing them 有权
标题翻译： Diosmetin化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US08404742B2
公开(公告)日：2013-03-26
申请号：US13372811
申请日：2012-02-14
申请人： Michel Wierzbicki , Marie-Francoise Boussard , Tony Verbeuren , Patricia Sansilvestri-Morel , Alain Rupin , Jérôme Paysant , François Lefoulon
发明人： Michel Wierzbicki , Marie-Francoise Boussard , Tony Verbeuren , Patricia Sansilvestri-Morel , Alain Rupin , Jérôme Paysant , François Lefoulon
IPC分类号： A01N43/16 , A61K31/35
CPC分类号： C07D311/30 , C07D407/12 , C07H15/203 , C07H17/07
摘要： Compounds of formula (I): wherein R1, R2 and R3, which may be the same or different, each represent a hydrogen atom or the group of formula (A): Medicinal products containing the same which are useful in the prevention and/or treatment of venous diseases and other conditions.
摘要翻译：式（I）化合物：其中可以相同或不同的R 1，R 2和R 3各自表示氢原子或式（A）的基团：含有其的药物，其可用于预防和/或治疗静脉疾病等病症。

9. 发明授权

US06844445B2 Indenoindolone compounds 失效
标题翻译：茚并吲哚酮化合物
公开(公告)号：US06844445B2
公开(公告)日：2005-01-18
申请号：US10100784
申请日：2002-03-19
申请人： Michel Wierzbicki , Marie-Françoise Boussard , Anne Rousseau , Jean Albert Boutin , Philippe Delagrange
发明人： Michel Wierzbicki , Marie-Françoise Boussard , Anne Rousseau , Jean Albert Boutin , Philippe Delagrange
IPC分类号： C07D491/056 , A61K31/40 , A61K31/403 , A61K31/407 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P5/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/28 , A61P35/00 , A61P43/00 , C07D209/80 , C07D209/94 , C07D207/323 , C07D207/36
CPC分类号： C07D209/80 , A61K31/40
摘要： Compound of formula (I): wherein: R represents hydrogen or a group selected from alkenyl and optionally substituted alkyl, each of R1 to R8, which may be identical or different, represents hydrogen or a group selected from alkyl, alkenyl, hydroxy, alkoxy, alkenyloxy, arylalkyl, arylalkoxy, carboxy, acyloxy and arylcarbonyloxy, or one of R1 to R8 forms with an adjacent one R1 to R8 an alkylenedioxy group, its optical isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid or base, with the proviso that: when R does not represent hydrogen, then at least one of R1 to R8 represents hydroxy or acyloxy, and the compounds of formula (I) are other than indeno[1,2-b]indol-10(5H)-one and medicinal products containing the same which are useful for treatment of disorders of the melatoninergic system.
摘要翻译：式（I）的化合物：其中：R表示氢或选自烯基和任选取代的烷基的基团，R 1至R 8可以相同或不同，表示氢或选自烷基，烯基，羟基，烷氧基的基团，烯氧基，芳基烷基，芳基烷氧基，羧基，酰氧基和芳基羰基氧基，或者R 1至R 8中的一个与相邻的一个R 1至R 8为亚烷基二氧基，其旋光异构体及其药学上可接受的酸或碱的加成盐，条件是：当R不表示氢时，R 1至R 8中的至少一个表示羟基或酰氧基，式（I）化合物不是茚并[1,2-b]吲哚-10（5H） - 和含有该药物的药物，其可用于治疗褪黑激素系统的病症。

10. 发明授权

US5705525A Thiophene compounds 失效
标题翻译：噻吩化合物
公开(公告)号：US5705525A
公开(公告)日：1998-01-06
申请号：US605537
申请日：1996-02-22
申请人： Michel Wierzbicki , Frederic Sauveur , Jacqueline Bonnet , Charles Tordjman
发明人： Michel Wierzbicki , Frederic Sauveur , Jacqueline Bonnet , Charles Tordjman
IPC分类号： A61K31/38 , A61K31/381 , A61P1/00 , A61P17/00 , A61P29/00 , C07D333/24 , C07D333/16 , C07D333/20
CPC分类号： C07D333/24
摘要： The invention relates to thiophene compounds of formula: ##STR1## wherein: X.sub.1, X.sub.2, Y.sub.1 and Y.sub.2, which are identical or different, each represents hydrogen or halogen, (C.sub.1 -C.sub.5)-alkyl or alkoxy, or trifluoromethyl, R.sub.1 represents hydrogen or (C.sub.1 -C.sub.5)-alkyl, A represents a straight (C.sub.1 -C.sub.5)-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C.sub.1 -C.sub.5)-alkyl, and R.sub.2 represents hydrogen, (C.sub.1 -C.sub.6)-alkyl, cyclohexyl or benzyl; and their physiologically tolerable salts. The products of the invention may be used as anti-inflammatory agents.
摘要翻译：本发明涉及下式的噻吩化合物：其中：X 1，X 2，Y 1和Y 2相同或不同，各自表示氢或卤素，（C 1 -C 5） - 烷基或烷氧基或三氟甲基，R 1表示氢或（C 1 -C 5） - 烷基，A表示直链（C 1 -C 5） - 烃链，其中每个碳原子任选被（C 1 -C 5） - 烷基单取代或二取代，并且R 2表示氢，（ C 1 -C 6） - 烷基，环己基或苄基; 及其生理上可耐受的盐。本发明的产品可以用作抗炎剂。

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