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公开(公告)号:US6127396A
公开(公告)日:2000-10-03
申请号:US466716
申请日:1999-12-17
IPC分类号: C07D233/06 , A61K31/4164 , A61P3/04 , A61P15/10 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D233/10 , C07D233/20 , C07D233/22 , C07D401/06 , C07D405/06 , A61K31/415 , C07D233/02 , C07D233/08
CPC分类号: C07D405/06 , C07D233/10 , C07D233/20 , C07D233/22 , Y02P20/55
摘要: The invention relates to a compound of formula (I): ##STR1## wherein: A represents an optionally substituted benzene ring,B represents an imidazoline ring of formula (Ia) or (Ib): ##STR2## X represents CR.sup.6, CR.sup.6 R.sup.7, NR.sup.8, SO or SO.sub.2, or oxygen, nitrogen or sulphur,Y represents a single bond or CH or CH.sub.2,Z represents a carbon atom or CR.sup.4,R.sup.1, R.sup.2, R.sup.3, which may be the same or different, each represent hydrogen or alkyl, it being possible for (R.sup.1 and R.sup.4) or (R.sup.2 and R.sup.4) to form cyclopropane,R.sup.5 represents hydrogen, alkyl or benzyl.
摘要翻译: 本发明涉及式(I)化合物:其中:A表示任选取代的苯环,B表示式(Ia)或(Ib)的咪唑啉环:X表示CR6,CR6R7,NR8,SO或SO2,或 氧,氮或硫,Y表示单键或CH或CH 2,Z表示碳原子或CR 4,可以相同或不同的R 1,R 2,R 3各自表示氢或烷基,可以(R 1 和R 4)或(R 2和R 4)以形成环丙烷,R 5表示氢,烷基或苄基。
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公开(公告)号:US5684020A
公开(公告)日:1997-11-04
申请号:US792179
申请日:1997-01-30
申请人: Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi , Alain Gobert
发明人: Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi , Alain Gobert
IPC分类号: A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00 , C07D307/79 , C07D307/81 , C07D319/18 , C07D321/10 , C07D405/04 , C07D409/12 , C07D407/14
CPC分类号: C07D307/79 , C07D319/18 , C07D321/10 , C07D405/04 , C07D409/12
摘要: A compound selected from those of formula: ##STR1## wherein: A-B, n, D and E are as defined in the specification, their racemic mixtures, and their optical isomers, and also the physiologically tolerable salts thereof with appropriate acids. The products of the invention may be used therapeutically.
摘要翻译: 选自下式的化合物:其中:A-B,n,D和E如说明书中所定义,它们的外消旋混合物及其旋光异构体,以及其与适当的酸的生理上可耐受的盐。 本发明的产品可以在治疗上使用。
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公开(公告)号:US06172097B2
公开(公告)日:2001-01-09
申请号:US09465619
申请日:1999-12-17
IPC分类号: A61K314184
CPC分类号: C07D235/02
摘要: The invention relates to a compound of formula (I): wherein: A represents an optionally substituted benzene ring, B represents an imidazoline ring of formula (Ia) or (Ib): and medicinal products containing the same/are useful in treating or in preventing depression, obesity, panic attacks, anxiety, obsessive-compulsive disorders, cognitive disorders, phobias, impulsive disorders associated with the abuse of drugs and withdrawal therefrom, sexual dysfunctions, and Parkinson's disease.
摘要翻译: 本发明涉及式(I)化合物:其中:A表示任选取代的苯环,B表示式(Ia)或(Ib)的咪唑啉环:和含有该化合物的药物,可用于治疗或 预防抑郁症,肥胖症,惊恐发作,焦虑症,强迫症,认知障碍,恐怖症,与药物滥用相关的冲动性疾病和从其中退出,性功能障碍和帕金森病。
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公开(公告)号:US5753662A
公开(公告)日:1998-05-19
申请号:US655457
申请日:1996-05-30
申请人: Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi , Alain Gobert
发明人: Jean-Louis Peglion , Aimee Dessinges , Bertrand Goument , Mark Millan , Adrian Newman-Tancredi , Alain Gobert
IPC分类号: A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/495 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00 , C07D307/79 , C07D307/81 , C07D319/18 , C07D321/10 , C07D405/04 , C07D409/12 , C07D405/00 , C07D407/00
CPC分类号: C07D307/79 , C07D319/18 , C07D321/10 , C07D405/04 , C07D409/12
摘要: A compound selected from those of formula: ##STR1## wherein: A--B, n, D and E are as defined in the specification, their racemic mixtures, and their optical isomers, and also the physiologically tolerable salts thereof with appropriate acids. The products of the invention may be used therapeutically.
摘要翻译: 选自下式的化合物:其中:A-B,n,D和E如说明书中所定义,它们的外消旋混合物及其旋光异构体,以及其与适当的酸的生理上可耐受的盐。 本发明的产品可以在治疗上使用。
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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。
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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。
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公开(公告)号:US5648374A
公开(公告)日:1997-07-15
申请号:US420064
申请日:1995-04-11
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。
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公开(公告)号:US5919784A
公开(公告)日:1999-07-06
申请号:US966040
申请日:1997-11-07
申请人: Daniel Lesieur , Pascal Carato , Jean-Paul Bonte , Patrick Depreux , Daniel-Henri Caignard , Mark Millan , Adrian Newman-Tancredi , Pierre Renard , Marie-Claire Rettori
发明人: Daniel Lesieur , Pascal Carato , Jean-Paul Bonte , Patrick Depreux , Daniel-Henri Caignard , Mark Millan , Adrian Newman-Tancredi , Pierre Renard , Marie-Claire Rettori
IPC分类号: A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/536 , A61K31/5377 , A61K31/538 , A61P25/00 , A61P25/18 , C07D263/58 , C07D265/36 , C07D277/68 , C07D279/16 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , A61K413/10 , A61K417/10 , C07D31/495 , C07D31/535
CPC分类号: C07D263/58 , C07D265/36 , C07D277/68 , C07D279/16
摘要: A compound of general formula (I): ##STR1## where A, X, R.sub.1, Y, n and Ar are defined in the description. Medicinal products containing the same are useful as D.sub.4 receptor Ligands.
摘要翻译: 通式(I)的化合物:其中A,X,R 1,Y,n和Ar在说明书中定义。 含有它们的药物可用作D4受体配体。
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公开(公告)号:US6107345A
公开(公告)日:2000-08-22
申请号:US261803
申请日:1999-03-03
申请人: Jean-Louis Peglion , Aimee Dessinges , Jean-Christophe Harmange , Mark Millan , Adrian Newman-Tancredi , Mauricette Brocco
发明人: Jean-Louis Peglion , Aimee Dessinges , Jean-Christophe Harmange , Mark Millan , Adrian Newman-Tancredi , Mauricette Brocco
IPC分类号: C07D233/50 , A61K31/00 , A61K31/135 , A61K31/33 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P1/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/30 , A61P43/00 , C07C215/42 , C07C217/58 , C07C217/74 , C07D211/44 , C07D233/48 , C07D263/28 , C07D309/10 , C07D335/02 , C07D345/00 , A61K31/133
CPC分类号: C07D309/10 , C07C215/42 , C07C217/74 , C07D233/48 , C07D263/28 , C07D335/02
摘要: A compound of formula (I): ##STR1## wherein: Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, which may be identical or different, represent a group as defined in the description,X represents oxygen, S(O).sub.p, --(CH.sub.2).sub.n -- or --CH.sub.2 --Y--CH.sub.2 -- wherein p, n and Y are as defined in the description,A represents ##STR2## wherein m, R.sub.1, R.sub.2 and G are as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid, and medicinal products containing the same are useful in the treatment of diseases like depression, panic attacks, obsessive compulsive disorders, phobias, impulsive disorders, drug abuse or anxiety.
摘要翻译: 式(I)的化合物:其中:可以相同或不同的Z 1,Z 2,Z 3,Z 4表示如说明书中所定义的基团,X表示氧,S(O)p, - (CH 2)n - 或-CH 2 -Y-CH 2 - ,其中p,n和Y如说明书中所定义,A表示其中m,R 1,R 2和G如说明书中所定义,其异构体和加成盐与药学上可接受的酸 和含有它们的药用产品可用于治疗抑郁症,恐慌发作,强迫症,恐惧症,冲动性疾病,药物滥用或焦虑症等疾病。
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公开(公告)号:US5958927A
公开(公告)日:1999-09-28
申请号:US165844
申请日:1998-10-02
IPC分类号: A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P25/00 , A61P25/04 , A61P43/00 , C07D311/18 , C07D319/18 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , A61K31/495 , C07D405/10 , C07D409/10 , C07D411/10
CPC分类号: C07D405/04 , C07D311/18 , C07D319/18 , C07D405/14 , C07D409/04
摘要: A compound of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X-Y, A, Z and Z' are as defined in the description, in the form of the cis or trans isomers each in racemic or optically active form, and acid addition salts thereof, and medicinal products containing the same are useful in the treatment of diseases of the central nervous system or of manifestations of pain.
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