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公开(公告)号:US06998403B2
公开(公告)日:2006-02-14
申请号:US10925712
申请日:2004-08-25
IPC分类号: A61K31/496 , C07D403/12
CPC分类号: C07D209/60
摘要: A compound of formula (I): wherein: R1 and R2 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, and R3 and R4 represent hydrogen, or R1 and R4 represent hydrogen and R2 and R3 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, or R1 and R2 represent hydrogen and R3 and R4 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, addition salts thereof with a pharmaceutically acceptable acid or base, and methods of treating conditions susceptible to α2-AR/5-HT2C antagonists.
摘要翻译: 式(I)化合物:化学式id =“CHEM-US-00001”num =“000
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公开(公告)号:US5472979A
公开(公告)日:1995-12-05
申请号:US323508
申请日:1994-10-14
申请人: Gilbert Lavielle , Thierry Dubuffet , Olivier Muller , Michel Laubie , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
发明人: Gilbert Lavielle , Thierry Dubuffet , Olivier Muller , Michel Laubie , Tony Verbeuren , Serge Simonet , Jean-Jacques Descombes
IPC分类号: A61K31/18 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61P7/02 , A61P9/00 , A61P43/00 , C07C311/02 , C07C311/14 , C07C311/20 , C07C311/29 , C07D213/55 , C07D311/58 , C07D335/06 , A61K31/14
CPC分类号: C07D335/06 , C07C311/20 , C07D213/55 , C07D311/58
摘要: R.sub.1 and R.sub.2 form, with the carbon atoms to which they are attached, cyclopentane or cyclohexane,R.sub.3 represents hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or unsubstituted or substituted amino,R.sub.4 represents alkyl, unsubstituted or substituted phenyl, naphthyl, pyridyl or thienyl, X represents methylene or oxygen or sulfur,its enantiomers and its addition salts with a pharmaceutically acceptable base, and medicinal products containing the same are useful as anti-thrombotic.
摘要翻译: 其中:R 1和R 2可以相同或不同,表示氢或卤素,烷基,取代或未取代的苯基,苄基,吡啶基甲基或咪唑基甲基或噻唑基甲基,吡啶基,咪唑基或噻唑基,或者R1 和R 2与它们所连接的碳原子形成环戊烷或环己烷,R 3表示羟基,直链或支链(C 1 -C 6)烷氧基或未取代或取代的氨基,R 4表示烷基,未取代或取代的苯基,萘基,吡啶基或 噻吩基,X表示亚甲基或氧或硫,其对映体及其与药学上可接受的碱的加成盐,以及含有它们的药物可用作抗血栓形成。
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公开(公告)号:US5723484A
公开(公告)日:1998-03-03
申请号:US786504
申请日:1997-01-21
IPC分类号: A61K31/40 , A61K31/435 , A61P9/00 , A61P13/02 , A61P15/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/30 , A61P43/00 , C07D491/04 , C07D491/052 , C07D491/52
CPC分类号: C07D491/04
摘要: Compounds of formula (I): ##STR1## in which: n represents 1 or 2, R.sub.1 represents hydrogen or alkyl, benzyl, acetyl, benzoyl, allyl, pyridinecarbonyl, pyridinemethyl, acylaminoalkyl (optionally substituted), pyridineaminocarbonyl, phthalimidoalkyl, thiochromanyloxyalkyl or (benzodioxanyloxy)alkyl, R.sub.2, R.sub.3 or R.sub.4, which may be identical or different, represent hydrogen or halogen or alkyl, alkoxy, hydroxyl, acetyl, aminocarbonyl, aminomethyl, cyano, nitro, amino, phenyl (which may or may not be substituted), furyl, pyridinyl, thienyl or pyridyl, or alternatively, when they are located on adjacent carbons, R.sub.2 and R.sub.3 form, with the carbon atoms which bear them, a furan or phenyl ring, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same are useful for the treatment of diseases requiring a ligand to the 5-HT.sub.2C receptors.
摘要翻译: 乙酰基,苯甲酰基,烯丙基,吡啶羰基,吡啶甲基,酰氨基烷基(任意取代的),吡啶氨基羰基,苯二甲酰亚氨基烷基, 可以相同或不同的二氢苯并二氢吡喃基氧基烷基或(苯并二氧代氧基)烷基,R2,R3或R4代表氢或卤素或烷基,烷氧基,羟基,乙酰基,氨基羰基,氨基甲基,氰基,硝基,氨基,苯基(可以或不可以 或呋喃基,吡啶基,噻吩基或吡啶基,或者当它们位于相邻的碳上时,R2和R3与它们携带的碳原子一起形成呋喃或苯环,其异构体及其加成盐 与药学上可接受的酸和含有该药物的药物可用于治疗需要5-HT 2C受体配体的疾病。
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公开(公告)号:US6020336A
公开(公告)日:2000-02-01
申请号:US146009
申请日:1998-09-02
申请人: Gilbert Lavielle , Olivier Muller , Christine Vayssettes-Courchay , Jean-Jacques Descombes , Tony Verbeuren
发明人: Gilbert Lavielle , Olivier Muller , Christine Vayssettes-Courchay , Jean-Jacques Descombes , Tony Verbeuren
IPC分类号: C07D401/14 , A61K31/41 , A61K31/415 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/505 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/06 , A61P43/00 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D521/00 , A61K31/425 , C07D403/10
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08
摘要: Compound of formula (I): ##STR1## wherein: n is 0 or 1,A represents a .sigma. bond or alkylene or alkenylene,X represents nitrogen or C--R.sub.2,R.sub.1 represents hydrogen or alkyl, andG.sub.1 represents any one of the groups defined in the description and medicaments containing the same.
摘要翻译: 式(I)化合物:其中:n为0或1,A表示σ键或亚烷基或亚烯基,X表示氮或C-R2,R1表示氢或烷基,G1表示 描述和含有相同的药物。
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公开(公告)号:US5348968A
公开(公告)日:1994-09-20
申请号:US189798
申请日:1994-02-01
申请人: Gilbert Lavielle , Philippe Maillos , Olivier Muller , Michel Laubie , Tony Verbeuren , Jean-Jacques Descombes
发明人: Gilbert Lavielle , Philippe Maillos , Olivier Muller , Michel Laubie , Tony Verbeuren , Jean-Jacques Descombes
IPC分类号: A61K31/40 , A61K31/415 , A61P25/04 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D419/14 , A61K31/41 , C07D209/08 , C07D231/56
CPC分类号: C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D419/14
摘要: The invention relates to a compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or halogen, alkyl, alkoxy, cyano or aminocarbonyl or any one of the following: ##STR2## in which: m is equal to 1, 2 or 3,n is equal to 0, 1 or 2,T represents a CO or SO.sub.2,R.sub.4 or R.sub.5, which are identical or different, represent hydrogen or alkyl or phenyl,R.sub.2 represents hydrogen or alkyl, phenyl or acyl,R.sub.3 represents hydrogen, alkyl (optionally substituted by hydroxyl or phenyl) or alkoxycarbonyl,--X--Y.dbd. represents --N--C.dbd., --N--N.dbd.or else ##STR3## represents --O--N.dbd.; to its enantiomers, diastereoisomers and epimers and to its addition salts with a pharmaceutically acceptable acid.
摘要翻译: 本发明涉及式(I)化合物:其中:R 1表示氢或卤素,烷基,烷氧基,氰基或氨基羰基或下列任何一种:(CH 2) mNHCONHR4,
(CH2)mSO2NHR4,CHCHSO2NHR4, 其中:m等于1,2或3,n等于0,1或2,T表示CO或SO2 ,R 4或R 5相同或不同,表示氢或烷基或苯基,R 2表示氢或烷基,苯基或酰基,R 3表示氢,烷基(任选被羟基或苯基取代)或烷氧基羰基,-XY =表示-NC =,-NN =否则 表示-ON =; 其对映异构体,非对映异构体和差向异构体及其与药学上可接受的酸的加成盐。 -
公开(公告)号:US6046205A
公开(公告)日:2000-04-04
申请号:US299314
申请日:1999-04-26
申请人: Gilbert Lavielle , Olivier Muller , Christine Vayssettes-Courchay , Jean-Jacques Descombes , Tony Verbeuren
发明人: Gilbert Lavielle , Olivier Muller , Christine Vayssettes-Courchay , Jean-Jacques Descombes , Tony Verbeuren
IPC分类号: C07D401/14 , A61K31/41 , A61K31/415 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/505 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/06 , A61P43/00 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D521/00
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08
摘要: Compound of formula (I): ##STR1## wherein: n is 0 or 1,A represents a .sigma. bond or alkylene or alkenylene,X represents nitrogen or C--R.sub.2,R.sub.1 represents hydrogen or alkyl,G.sub.1 represents any one of the groups defined in the description.These compounds are useful for treating a living body afflicted with venous insufficiency, and/or migraine, and/or migraine associated with vascular diseases.
摘要翻译: 式(I)化合物:其中:n为0或1,A表示σ键或亚烷基或亚烯基,X表示氮或C-R2,R1表示氢或烷基,G1表示说明书中定义的任何一个基团 。 这些化合物可用于治疗患有静脉功能不全的活体,和/或偏头痛,和/或与血管疾病相关的偏头痛。
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17.
公开(公告)号:US5407946A
公开(公告)日:1995-04-18
申请号:US259697
申请日:1994-06-14
IPC分类号: A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/47 , A61P7/02 , A61P9/00 , A61P9/10 , A61P43/00 , C07D207/08 , C07D207/22 , C07D207/48 , C07D401/04 , C07D401/06 , C07D401/12
CPC分类号: C07D401/06 , C07D207/22 , C07D207/48 , C07D401/12
摘要: Components of formula (I): ##STR1## in which: R.sub.1 represents optionally substituted phenylsulfonyl, naphthylsulfonyl, quinolyl, or isoquinolyl,R.sub.2 represents hydrogen, optionally substituted phenyl, or optionally substituted 3-pyridyl or 2-pyridyl,R.sub.3 represents ##STR2## in which m is equal to 2, 3, or 4; n is equal to 4, 5, 6, or 7; and R represents hydrogen or alkyl, as thromboxane A.sub.2 receptor inhibitors or thromboxane A.sub.2 -synthase inhibitors, and pharmaceutical compositions containing the same.
摘要翻译: 式(I)的组分:其中:R 1表示任选取代的苯磺酰基,萘磺酰基,喹啉基或异喹啉基,R 2表示氢,任选取代的苯基或任选取代的3-吡啶基或2-吡啶基,R 3表示 或者(CH2)nCO2R,其中m等于2,3或4; n等于4,5,6或7; 和R表示氢或烷基,作为凝血恶烷A2受体抑制剂或血栓烷A2-合成酶抑制剂,以及含有它们的药物组合物。
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公开(公告)号:US06365605B1
公开(公告)日:2002-04-02
申请号:US09480038
申请日:2000-01-10
IPC分类号: A61K3144
CPC分类号: C07D491/04
摘要: Compounds of formula (I): wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≦m+n≦3, p is 1 to 6 inclusive, X represents cyano or —CO—NR4R5, R4 and R5 being selected from hydrogen, linear or branched (C1-C6)-alkyl, (C3-C7)-cycloalkyl, and aryl, R1 and R2 each independently represent hydrogen or linear or branched (C1-C6)-alkyl, R3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A′-Cy, A′ and Cy being as defined in the description, and medicinal products containing the same which are useful as D3 receptor ligands.
摘要翻译: 式(I)的化合物:其中:m为0〜3,n为0〜3,2 <= m + n <= 3,p为1〜6,X表示氰基或-CO-NR 4 R 5, R 5选自氢,直链或支链(C 1 -C 6) - 烷基,(C 3 -C 7) - 环烷基和芳基,R 1和R 2各自独立地表示氢或直链或支链(C 1 -C 6) - 烷基,R 3表示氢 ,任选取代的苯基,萘基或杂芳基,或芳氧基或芳硫基,或被A'-Cy,A'和Cy取代的芳基或杂芳基如说明书中所定义,和含有它们的可用作D3受体配体的医药产品。
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公开(公告)号:US06326377B1
公开(公告)日:2001-12-04
申请号:US09480037
申请日:2000-01-10
IPC分类号: A61K3144
CPC分类号: C07D491/04
摘要: Compounds of formula (I): wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≦m+n≦3, p is 1 to 6 inclusive, X represents cyano or —CO—NR4R5, R4 and R5 being selected from hydrogen, linear or branched (C1-C6)-alkyl, (C3-C7)-cycloalkyl,and aryl, R1 and R2 each independently represent hydrogen or linear or branched (C1-C6)-alkyl, R3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A′—Cy, A′ and Cy being as defined in the description, and medicinal products containing the same which are useful as D3 receptor ligands.
摘要翻译: 式(I)的化合物:其中:m为0〜3,n为0〜3,2 <= m + n <= 3,p为1〜6,X表示氰基或-CO-NR 4 R 5, R 5选自氢,直链或支链(C 1 -C 6) - 烷基,(C 3 -C 7) - 环烷基和芳基,R 1和R 2各自独立地表示氢或直链或支链(C 1 -C 6) - 烷基,R 3表示氢 ,任选取代的苯基,萘基或杂芳基,或芳氧基或芳硫基,或被A'-Cy,A'和Cy取代的芳基或杂芳基如说明书中所定义,和含有它们的可用作D3受体配体的医药产品。
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公开(公告)号:US6090837A
公开(公告)日:2000-07-18
申请号:US103304
申请日:1998-06-23
申请人: Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Fran.cedilla.oise Lejeune , Mark Millan
发明人: Gilbert Lavielle , Thierry Dubuffet , Patrick Hautefaye , Fran.cedilla.oise Lejeune , Mark Millan
IPC分类号: A61K31/40 , A61K31/435 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07B53/00 , C07D491/04 , C07D491/052 , A61K31/407 , A61K31/436 , C07D491/02
CPC分类号: C07D491/04
摘要: Compounds of formula (I): ##STR1## wherein: m is 0 to 3 inclusive,n is 0 to 3 and 2.ltoreq.m+n.ltoreq.3,p is 1 to 6 inclusive,X represents cyano or --CO--NR.sub.4 R.sub.5, R.sub.4 and R.sub.5 being selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)-alkyl, (C.sub.3 -C.sub.7)-cycloalkyl, and aryl,R.sub.1 and R.sub.2 each independently represent hydrogen or linear or branched (C.sub.1 -C.sub.6)-alkyl,R.sub.3 represents hydrogen, optionally substituted phenyl, naphthyl or heteroaryl, or aryloxy or arylthio, or aryl or heteroaryl substituted by A'-Cy, A' and Cy being as defined in the description, andmedicinal products containing the same which are useful as D.sub.3 receptor ligands.
摘要翻译: 式(I)的化合物:其中:m为0〜3,n为0〜3,m为2〜3,p为1〜6,X为氰基或-CO-NR 4 R 5, R 4和R 5选自氢,直链或支链(C 1 -C 6) - 烷基,(C 3 -C 7) - 环烷基和芳基,R 1和R 2各自独立地表示氢或直链或支链(C 1 -C 6) - 烷基,R 3 表示氢,任选取代的苯基,萘基或杂芳基,或芳氧基或芳硫基,或被A'-Cy,A'和Cy取代的芳基或杂芳基如说明书中所定义,和含有它们的药物,可用作D3受体 配体。
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