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1. 发明授权

US5494934A Guanidine compounds 失效
标题翻译：胍化合物
公开(公告)号：US5494934A
公开(公告)日：1996-02-27
申请号：US787374
申请日：1991-11-04
申请人： Charles Malen , Jean-Michel Lacoste , Guillaume de Nanteuil
发明人： Charles Malen , Jean-Michel Lacoste , Guillaume de Nanteuil
IPC分类号： A61K31/155 , A61K31/415 , A61K31/495 , A61P3/04 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P11/00 , A61P25/24 , A61P25/26 , C07C279/06 , C07C279/08 , C07C281/16 , C07C281/18 , C07D233/48 , C07D233/50 , C07D233/52 , C07D239/14 , C07D239/18
CPC分类号： C07C281/18 , C07C281/16 , C07D233/48 , C07D233/52 , C07C2101/02
摘要： A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Medicine products.
摘要翻译：式（I）化合物：其中：R 1表示取代或未取代的苯基或（C 3 -C 7）环烷基，R 2表示三氟甲基或（C 3 -C 4）环烷基，A表示-CH 2 - ， - CH = N，= N-或-NH-，R 3和R 4可以相同或不同，表示氢或直链或支链（C1-C6）烷基，或与它们相连的氮原子形成5 - 或6-元杂环，当A = -CH 2 - ， - CH = N-或-NH-的情况下，R表示氢，或者当后者等于= N-时A基团的键，其对映异构体和差向异构体以及其与药学上可接受的酸的加成盐。医药产品。

2. 发明授权

US5254590A Acylaminophenol compounds 失效
标题翻译：酰氨基苯酚化合物
公开(公告)号：US5254590A
公开(公告)日：1993-10-19
申请号：US847599
申请日：1992-03-05
申请人： Charles Malen , Jean-Michel Lacoste , Jean-Paul Vilaine , Albert Lenaers
发明人： Charles Malen , Jean-Michel Lacoste , Jean-Paul Vilaine , Albert Lenaers
IPC分类号： A61K31/165 , A61P3/06 , A61P9/10 , C07C231/14 , C07C233/25 , C07C233/26 , C07C233/27 , C07C233/60 , A01N37/22 , A01N37/18
CPC分类号： C07C233/26 , C07C233/25 , C07C233/27 , C07C2101/08
摘要： The invention relates to the compounds of formula (I): ##STR1## in which R represents higher alkyl, 1-(higher alkyl)lower cycloalkyl-1-yl or higher alkenyl comprising one or more double bonds, and eitherR.sub.3 represents hydroxyl,R.sub.1 and R.sub.2, which are different, represent hydrogen or lower alkyl,R.sub.4 and R.sub.5, which are identical or different, represent lower alkyl or alkoxy, orR.sub.1 and R.sub.4 represent hydroxyl andR.sub.2, R.sub.3 and R.sub.5, which are identical or different, represent lower alkyl or alkoxy,their isomers as well as their salts, and a method for treating an animal or human living body afflicted with dylipidemias or atherosclerosis.
摘要翻译：本发明涉及式（I）化合物：其中R表示高级烷基，1-（高级烷基）低级环烷基-1-基或含有一个或多个双键的更高级链烯基，R3或R3 表示羟基，不同的R 1和R 2表示氢或低级烷基，R 4和R 5相同或不同，表示低级烷基或烷氧基，或者R 1和R 4表示羟基，R 2，R 3和R 5是相同或不同的，代表低级烷基或烷氧基，它们的异构体及其盐，以及用于治疗患有血脂异常或动脉粥样硬化的动物或人类活体的方法。

3. 发明申请

US20110034460A1 Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them 有权
标题翻译：二氢吲哚酮化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US20110034460A1
公开(公告)日：2011-02-10
申请号：US12806045
申请日：2010-08-04
申请人： Jean-Claude Ortuno , Alexis Cordi , Jean-Michel Lacoste , Vincent Lacoste , Pauline Lacoste , Imre Fejes , Michael Burbridge , John Hickman , Alain Pierre
发明人： Jean-Claude Ortuno , Alexis Cordi , Jean-Michel Lacoste , Vincent Lacoste , Pauline Lacoste , Imre Fejes , Michael Burbridge , John Hickman , Alain Pierre
IPC分类号： A61K31/5377 , C07D413/14 , A61K31/422 , A61K31/496 , A61K31/454 , A61P35/00
CPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14
摘要： Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.
摘要翻译：式（I）化合物：其中：m和n表示1或2，A表示吡咯基，X表示C（O），S（O）或SO 2基团，R 1和R 2表示烷基，与它们携带的氮原子一起形成杂环基，R3和R4与携带它们的原子一起形成杂环基，R 5表示氢原子或烷基，R 6表示氢原子或卤素原子。含有该药物的药物可用于治疗癌症。

4. 发明授权

US5677325A 4-imidazolidinone compound 失效
标题翻译： 4-咪唑烷酮化合物
公开(公告)号：US5677325A
公开(公告)日：1997-10-14
申请号：US770290
申请日：1996-12-20
申请人： Alex Cordi , Jean-Michel Lacoste , Mark Millan , Valerie Audinot
发明人： Alex Cordi , Jean-Michel Lacoste , Mark Millan , Valerie Audinot
IPC分类号： C07D233/38 , A61K31/415 , A61K31/4166 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D233/32 , C07D233/06
CPC分类号： C07D233/32
摘要： Compound of formula (I): ##STR1## and its addition salts with a pharmaceutically acceptable acid or base, a medicinal products containing the same are useful as partial agonist of the glycine B site.
摘要翻译：式（I）的化合物：其中药学上可接受的酸或碱的加成盐及其加成盐可用作甘氨酸B位点的部分激动剂。

5. 发明授权

US5266565A Vanadium complexes 失效
标题翻译：钒配合物
公开(公告)号：US5266565A
公开(公告)日：1993-11-30
申请号：US909107
申请日：1992-07-02
申请人： Jean-Michel Lacoste , Jacques Duhault , Denis Ravel
发明人： Jean-Michel Lacoste , Jacques Duhault , Denis Ravel
IPC分类号： A61K31/28 , A61K31/66 , A61P3/04 , A61P3/08 , A61P3/10 , C07F9/00 , C07F9/09 , C07F9/58 , A61K31/555 , C07F11/00
CPC分类号： C07F9/005
摘要： Compounds of formula (I): ##STR1## in which: R.sub.1 or R.sub.4, which are identical or different, represent hydrogen or alkyl,R.sub.2 represents hydrogenm or alkyl, hydroxymethyl, --CH.sub.2 OPO(OH).sub.2 or --CH.sub.2 OPO(ONa).sub.2,R.sub.3 represents hydrogen, alkyl or hydroxyl or any one of the following groups: ##STR2## in which: T represents oxygen or sulfur,n represents an integer between 1 and 4,R.sub.5 represents hydrogen or alkyl,X represents nitrogen, CH or CR'.sub.3 (in which R'.sub.3 has the same meaning as R.sub.3 except in the case where R.sub.3 represents hydroxyl),A represents alkylene of formula --(CH.sub.2).sub.p -in which p represents an integer between 2 and 4, optionally substituted by one or more linear or branched (C.sub.1 -C.sub.4) alkyl, or any one of the following radicals: ##STR3## Y and Z together form oxygen or simultaneously represent two hydroxyl and in this case, the compound of formula (I) is positively charged,their isomers as well as their addition salts with a pharmaceutically acceptable acid or base.
摘要翻译：式（I）化合物：其中：R 1或R 4相同或不同，表示氢或烷基，R 2表示氢或烷基，羟甲基，-CH 2 OPO（OH）2或-CH 2 OPO（ONa ）2，R 3表示氢，烷基或羟基或以下基团中的任何一个：其中：T表示氧或硫，n表示1至4的整数，R 5表示氢或烷基，X表示氮，CH或CR'3（其中R 3具有与R 3相同的含义，除了在R3表示羟基的情况下），A表示式 - （CH 2）p - 的亚烷基，其中p表示2至4的整数任选地被一个或多个直链或支链（C 1 -C 4）烷基或任何一个以下基团取代：Y和Z一起形成氧或同时代表两个羟基，在这种情况下，式（I ）带正电荷，它们的异构体以及它们与药学上可接受的酸或碱的加成盐。

6. 发明申请

US20120046287A1 Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them 有权
公开(公告)号：US20120046287A1
公开(公告)日：2012-02-23
申请号：US13373016
申请日：2011-11-02
申请人： Jean-Claude Ortuno , Alexis Cordi , Jean-Michel Lacoste , Vincent Lacoste , Pauline Lacoste , Imre Fejes
发明人： Jean-Claude Ortuno , Alexis Cordi , Jean-Michel Lacoste , Vincent Lacoste , Pauline Lacoste , Imre Fejes
IPC分类号： A61K31/5377 , A61K31/445 , A61P35/04 , A61K31/404
CPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14
摘要： Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.

7. 发明授权

US5486532A Benzospiroalkenes 失效
标题翻译：苯并噻唑烯
公开(公告)号：US5486532A
公开(公告)日：1996-01-23
申请号：US276910
申请日：1994-07-19
申请人： Alex Cordi , Jean-Michel Lacoste , Michel Laubie , Tony Verbeuren , Jean-Jacques Descombes , Mark Millan
发明人： Alex Cordi , Jean-Michel Lacoste , Michel Laubie , Tony Verbeuren , Jean-Jacques Descombes , Mark Millan
IPC分类号： C07D277/60 , A61K31/415 , A61K31/4162 , A61K31/4184 , A61K31/4188 , A61K31/42 , A61K31/423 , A61K31/424 , A61K31/425 , A61K31/428 , A61K31/429 , A61P9/00 , A61P9/04 , A61P9/12 , A61P9/14 , A61P23/00 , A61P23/02 , A61P25/02 , A61P25/04 , A61P25/20 , A61P25/30 , A61P43/00 , C07D235/02 , C07D263/52 , C07D491/107 , C07D493/10 , C07D495/10 , C07D498/10 , C07D513/10 , C07D263/28
CPC分类号： C07D235/02 , C07D263/52
摘要： Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.5 --,R.sub.1 represents halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl or linear or branched (C.sub.1 -C.sub.6) alkoxy,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (unsubstituted or substituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.4 represents hydrogen or amino (unsubstituted or substituted)R.sub.5 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl,or alternativelyR.sub.1 and R.sub.2 form, together with the carbon atoms which bear them, a benzenic ring, on condition that, in this case, X represents --CH.sub.2 -- or --(CH.sub.2).sub.2 --, their isomers and their addition salts with a pharmaceutically acceptable acid, and medicinal product containing the same are useful as .alpha.2-adrenergic agonist.
摘要翻译：式（I）化合物：其中：X表示-CH 2 - ， - （CH 2）2 - ， - CH = CH - ， - O-CH 2 - ， - S-CH 2 - ，-SO- CH 2 - 或-SO 2 -CH 2 - ，Y表示氧或硫或-NR 5 - ，R 1表示卤素，直链或支链（C 1 -C 6）烷基（未取代或取代的），羟基或直链或支链（C 1 -C 6）烷氧基，直链或支链（C1-C6）烷基（未取代或取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R3代表氢或卤素，或支链（C1-C6）烷基（未取代或取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R4代表氢或氨基（未取代或取代的）直链或支链（C1-C6）烷基，或者R1和R2与带有它们的碳原子一起形成苯环，条件是在这种情况下，X表示-CH 2 - 或 - （CH 2）2 - ，它们的异构体及其加成盐一种药学上可接受的酸，以及含有该酸的药物可用作α2-肾上腺素能激动剂。

8. 发明授权

US5436261A Benzospiroalkene heterocyclic compounds 失效
标题翻译：苯并四氢烯烃杂环化合物
公开(公告)号：US5436261A
公开(公告)日：1995-07-25
申请号：US276918
申请日：1994-07-19
申请人： Alex Cordi , Jean-Michel Lacoste , Michel Laubie , Tony Verbeuren , Jean-Jacques Descombes
发明人： Alex Cordi , Jean-Michel Lacoste , Michel Laubie , Tony Verbeuren , Jean-Jacques Descombes
IPC分类号： A61K31/415 , A61K31/4162 , A61K31/4184 , A61K31/4188 , A61K31/42 , A61K31/423 , A61K31/424 , A61K31/425 , A61K31/429 , A61P25/02 , A61P25/04 , A61P25/06 , A61P43/00 , C07D235/02 , C07D263/52 , C07D491/10 , C07D491/107 , C07D495/10 , C07D498/10 , C07D513/10
CPC分类号： C07D235/02 , C07D263/52 , C07D491/10 , C07D495/10
摘要： Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.6 --,R.sub.1 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl, (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6)alkylthio,R.sub.4 represents hydrogen (on condition that, in this case, R.sub.1 represents hydrogen), halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted) or hydroxyl, or alternativelyR.sub.1 and R.sub.2, R.sub.2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and X, together with the carbon atoms which bear them, form a benzene ring, on condition that, in the case where R.sub.1 and R.sub.2 form a benzene ring, X is other than --CH.sub.2 -- or --(CH.sub.2).sub.2 --,R.sub.5 represents hydrogen or amino (substituted or unsubstituted),R.sub.6 has the same meaning as R.sub.1,their isomers and also their. addition salts with a pharmaceutically acceptable acid and medicinal product containing the sarne are useful as partial .alpha..sub.1 and .alpha..sub.2 adrenergic agonist in the treatment of venous disease and migraine.
摘要翻译：式（I）化合物：其中：X表示-CH 2 - ， - （CH 2）2 - ， - CH = CH - ， - O-CH 2 - ， - S-CH 2 - ，-SO- CH2-或-SO2-CH2-，Y表示氧或硫或-NR6-，R1表示氢或直链或支链（C1-C6）烷基，R2表示氢或卤素，直链或支链（C1-C6）烷基，（取代或未取代的），羟基，直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R3表示氢或卤素，直链或支链（C1-C6）烷基（取代或未取代的）直链或支链（C1-C6）烷氧基或直链或支链（C1-C6）烷硫基，R4代表氢（在这种情况下，R1表示氢），卤素，直链或支链（C1-C6）烷基或未取代的）或羟基，或者R1和R2，R2和R3，R3和R4或R4和X与它们携带的碳原子一起形成苯环，条件是在R1和R2形成苯环，X不是-CH 2 - 或 - （CH 2）2 - ， R5代表氢或氨基（取代或未取代的），R6具有与R1相同的含义，它们的异构体以及它们的含义。与药学上可接受的酸和含有缬氨酸的药物的加成盐可用作治疗静脉疾病和偏头痛的部分α1和α2肾上腺素能激动剂。

9. 发明授权

US5385920A Diacylglycerol nicotinates 失效
标题翻译：二酰基甘油烟酸酯
公开(公告)号：US5385920A
公开(公告)日：1995-01-31
申请号：US73894
申请日：1993-06-09
申请人： Alex Cordi , Jean-Michel Lacoste , Jacques Duhault , Joseph Espinal , Michelle Boulanger
发明人： Alex Cordi , Jean-Michel Lacoste , Jacques Duhault , Joseph Espinal , Michelle Boulanger
IPC分类号： A61K31/44 , A61K31/4406 , A61K31/495 , A61K31/50 , A61P9/10 , C07D213/80 , C07D241/24 , C07D213/02
CPC分类号： C07D213/80
摘要： Compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent a higher alkyl or higher alkenyl radical,R.sub.3 represents a pyridyl or pyrazinyl radical,their isomers and their addition salts with a pharmaceutically acceptable acid and medicaments for the reduction of plasma lipids containing the same.
摘要翻译：式（I）化合物：其中：R1和R2相同或不同，代表高级烷基或更高级的烯基，R3代表吡啶基或吡嗪基，它们的异构体及其加成盐与用于还原含有其的血浆脂质的药学上可接受的酸和药物。

10. 发明授权

US5296498A Guanidine compounds 失效
标题翻译：胍化合物
公开(公告)号：US5296498A
公开(公告)日：1994-03-22
申请号：US5653
申请日：1993-01-19
申请人： Charles Malen , Jean-Michel Lacoste , Guillaume de Nanteuil
发明人： Charles Malen , Jean-Michel Lacoste , Guillaume de Nanteuil
IPC分类号： A61K31/155 , A61K31/415 , A61K31/495 , A61P3/04 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P11/00 , A61P25/24 , A61P25/26 , C07C279/06 , C07C279/08 , C07C281/16 , C07C281/18 , C07D233/48 , C07D233/50 , C07D233/52 , C07D239/14 , C07D239/18
CPC分类号： C07C281/18 , C07C281/16 , C07D233/48 , C07D233/52 , C07C2101/02
摘要： A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.
摘要翻译：式（I）化合物：其中：R 1表示取代或未取代的苯基或（C 3 -C 7）环烷基，R 2表示三氟甲基或（C 3 -C 4）环烷基，A表示-CH 2 - ， - CH = N，= N-或-NH-，R 3和R 4可以相同或不同，表示氢或直链或支链（C1-C6）烷基，或与它们相连的氮原子形成5 - 或6-元杂环，当A = -CH 2 - ， - CH = N-或-NH-的情况下，R表示氢，或者当后者等于= N-时A基团的键，其对映异构体和差向异构体以及其与药学上可接受的酸的加成盐。

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