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    • 12. 发明授权
    • Benzothiophene, benzofuran and indole compounds
    • 苯并噻吩,苯并呋喃和吲哚化合物
    • US06302837B1
    • 2001-10-16
    • US09687308
    • 2000-10-13
    • Guillaume De NanteuilChristine LilaTony VerbeurenAlain Rupin
    • Guillaume De NanteuilChristine LilaTony VerbeurenAlain Rupin
    • A61K314436
    • C07D231/12C07D233/56C07D249/08C07D333/58C07D333/60C07D401/06C07D409/06C07D409/14
    • A compound selected from those of formula (I): wherein: X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description, Y represents oxygen, sulphur, NR3, or may represent single bond in certain cases, T represents nitrogen, carbon, or CH, A represents single bond, alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, or —SO2—R4— wherein R4 is as defined in the description, W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycloalkyloxy or heteroaryloxy, or hydroxyamino, U1 represents hetero, or alkylene wherein one or more of carbon may optionally be replaced by one or more hetero atoms, V1 represents arylene, heteroarylene,or heterocycloalkylene, U2 represents single bond, hetero or alkylene wherein one or more carbon may optionally be replaced by one or more hetero atoms, V2 represents aryl, heteroaryl, or heterocycloalkyl, Ra, Rb, Rc, which may be identical or different, each independently of the others represents a group as defined in the description, R1 represents aryl substituted by from one to five substituents, 1,3-dihydro-2H-indol-2-one, 3,4-dihydro-2(1H)-quinolinone, 1-hydroxy-2(1H)-pyridinone group, or heteroaryl, R2 represents halogen, alkyl, aryl, arylalkyl, cycloalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroarylalkyl, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as inhibitors of PAI-1 in the treatment of thrombosis, pathologies for which the origin is thrombosis, or pathologies causing an increase in risk of thrombosis.
    • 选自式(I)的化合物:其中:X表示氧,硫或NR 3,其中R3如说明书中所定义,Y表示氧,硫,NR 3,或在某些情况下可表示单键,T表示氮 ,碳或CH,A表示单键,亚烷基,亚芳基,亚环烷基,亚杂环亚烷基,亚杂芳基或-SO 2 -R 4 - ,其中R 4如说明书中所定义,W表示羟基,烷氧基,芳氧基,芳基烷氧基,环烷氧基, 杂芳基氧基或羟基氨基,U1表示杂或亚烷基,其中一个或多个碳可以任选被一个或多个杂原子替代,V 1表示亚芳基,亚杂芳基或杂环亚烷基,U 2表示单键,杂或亚烷基,其中一个或多个碳 可任选地被一个或多个杂原子替代,V 2表示芳基,杂芳基或杂环烷基,R a,R b,R c可以相同或不同,各自独立地表示t定义的基团 他描述,R1代表被1至5个取代基取代的芳基,1,3-二氢-2H-吲哚-2-酮,3,4-二氢-2(1H) - 喹啉酮,1-羟基-2(1H) - 吡啶酮基或杂芳基,R 2表示卤素,烷基,芳基,芳基烷基,环烷基,杂环烷基,杂环烷基烷基,杂芳基或杂芳基烷基,其异构体及其药学上可接受的酸或碱加成盐,以及含有它们的药物 作为治疗血栓形成的PAI-1的抑制剂,来自血栓形成的病理学,或导致血栓形成风险增加的病理学。
    • 14. 发明申请
    • Indanyl-piperazine compounds
    • 茚基 - 哌嗪化合物
    • US20060223830A1
    • 2006-10-05
    • US11391916
    • 2006-03-29
    • Guillaume De NanteuilBernard PortevinPhilippe GloanecMark MillanJean-Claude OrtunoClotilde Mannoury La CourAlain Gobert
    • Guillaume De NanteuilBernard PortevinPhilippe GloanecMark MillanJean-Claude OrtunoClotilde Mannoury La CourAlain Gobert
    • A61K31/495C07D241/04
    • C07D213/40C07D295/096C07D295/135C07D295/155C07D333/20
    • A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted,  or R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, n represents 1 or 2, —X— represents a group selected from —(CH2)m—O-Ak-, —(CH2)m—NR4-Ak-, —(CO)—NR4-Ak- and —(CH2)m—NR4-(CO)—,  m represents an integer between 1 and 6 inclusive, Ak represents an optionally substituted alkylene chain, and R4 represents a hydrogen atom or an alkyl group, Ar represents an aryl or heteroaryl group, its enantiomers, diasteroisomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.
    • 选自式(I)的化合物的化合物:其中:R 3表示氢原子,R 1和R 2与 带有它们的碳原子形成苯,萘或喹啉环结构,每个环结构任选被取代,或R 1表示氢原子,R 2和R 2 3个与携带它们的碳原子一起形成苯,萘或喹啉环结构,每个环结构可以被取代,n表示1或2,-X-表示选自 - ( CH 2 - (CH 2)n -O - , - (CH 2 CH 2)m -NR 2 -Ak-, - (CO)-NR 4 - 和 - (CH 2)2 -N (CO) - ,m表示1和6之间的整数,包括1和6,Ak表示任选取代的亚烷基链,并且R 4表示氢原子或烷基,Ar 表示芳基或杂芳基,其对映异构体,diastero 异构体及其与药学上可接受的酸的加成盐。 含有该药物的医药产品可用于治疗需要5-羟色胺再摄取抑制剂和/或NK1拮抗剂的病症。
    • 16. 发明授权
    • Alpha-amino acid sulphonyl compounds
    • α-氨基酸磺酰基化合物
    • US06716843B2
    • 2004-04-06
    • US10109407
    • 2002-03-28
    • Guillaume De NanteuilBernard PortevinAlain BenoistNigel LevensOlivier NosjeanBernadette Husson-Robert
    • Guillaume De NanteuilBernard PortevinAlain BenoistNigel LevensOlivier NosjeanBernadette Husson-Robert
    • A61K3140
    • C07D277/04C07D207/16C07D231/04C07D233/06C07D277/06C07D277/10Y02P20/55
    • Compound of formula (I): wherein:  represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or —NR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, Y represents R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as inhibitors of dipeptidyl-peptidase IV.
    • 式(I)化合物:其中:表示任选取代的5元含氮杂环,R 1表示氢,烷基,酰基,脯氨酰基,丙氨酰,组氨酰脯氨酰基或苯丙氨酰脯氨酰基,Ak表示亚烷基或杂亚烷基链,X表示 单键或任选取代的亚苯基,R 2表示任选取代的烷基,(C 3 -C 10)环烷基或-NR 2 a R 2b,其中可以相同或不同的R 2a和R 2b各自代表氢或烷基,或与携带它们的氮原子一起 ,形成含氮杂环,Y表示R 3表示氢或选自烷基,(C 3 -C 7)环烷基和芳基的基团,R 4,R 5和R 6可以相同或不同,各自表示氢或烷基,或R 4 和R6或R5和R6与携带它们的原子一起形成咪唑烷或二氢苯并咪唑环,其光学异构体及其与药学上可接受的酸的加成盐。含有相同的喔 ch可用作二肽基肽酶IV的抑制剂。
    • 20. 发明授权
    • Pyrrolidine and thiazolidine compounds
    • 吡咯烷和噻唑烷化合物
    • US07439263B2
    • 2008-10-21
    • US11131510
    • 2005-05-18
    • Guillaume De NanteuilAlain BenoistMurielle CombettesElizabeth Harley
    • Guillaume De NanteuilAlain BenoistMurielle CombettesElizabeth Harley
    • A61K31/40C07D207/04
    • C07D405/12C07D207/10C07D207/16C07D277/12C07D295/185C07D403/12C07D409/12C07D417/12
    • Compounds of formula (I): wherein: X1 represents an atom or group selected from CR4aR4b, O, S(O)q1 and NR5, wherein R4a, R4b, q1 and R5 are as defined in the description, m1 represents zero or an integer from 1 to 4 inclusive, m2 represents an integer from 1 to 4 inclusive, n1 and n2, which may be identical or different, each represent an integer from 1 to 3 inclusive, R1 represents hydrogen or a group selected from carboxy, alkoxycarbonyl, optionally substituted carbamoyl and optionally substituted alkyl, R2 represents hydrogen or alkyl, Ak represents an optionally substituted alkylene chain, p represents zero, 1 or 2, R3 represents hydrogen or cyano, X2 and X3, which may be identical or different, each represent either S(O)q2, or CR6aR6b, wherein q2, R6a and R6b are as defined in the description, its optical isomers, where they exist, and its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as DPP-IV inhibitors.
    • 式(I)的化合物:其中:X 1表示选自CR 4a R 4a,O,S(O) q1和NR5,其中R 4a 4a,R 4b,q 1和..., R 5如描述中所定义,m 1表示0或1至4的整数,其中m 2表示1的整数, 至4个,其中可以相同或不同的n 1和n 2各自表示1至3的整数,包括1和3的整数,R 1, 表示氢或选自羧基,烷氧基羰基,任选取代的氨基甲酰基和任选取代的烷基的基团,R 2表示氢或烷基,Ak表示任选取代的亚烷基链,p表示0,1或2,R 3或3表示氢或氰基,X 2和X 3可以相同或不同,各自表示S(O) q2,或CR 6a R 6b,其中q2