专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1997013768A1 OXAZOLIDIN-2-ONE DERIVATIVES, PREPARATION METHOD THEREFOR AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译：氧杂环丁二烯-2-酮衍生物，其制备方法及其治疗用途
公开(公告)号：WO1997013768A1
公开(公告)日：1997-04-17
申请号：PCT/FR1996001511
申请日：1996-10-08
申请人： SYNTHELABO , JEGHAM, Samir , PUECH, Frédéric , BURNIER, Philippe , BERTHON, Danielle , LECLERC, Odile
发明人： SYNTHELABO
IPC分类号： C07D413/04
CPC分类号： C07D413/04
摘要： Oxazolidin-2-one derivatives of general formula (I), wherein R1 is a hydrogen atom, an alkyl, hydroxyalkyl, fluoroalkyl, hydroxyfluoroalkyl, cyanoalkyl, optionally substituted phenyl or optionally substituted phenylmethyl group, or a group R3A- where R3 is a cycloalkyl or cyclooxyalkyl group optionally substituted by a hydroxy group, and A is a -CH2 or -CH2-CH2 radical, R2 is a hydrogen atom or a methyl group, X is an oxygen or sulphur atom or a group NR4 where R4 is an alkyl group, and Z is an oxygen atom or a group -CH=CH or -CH2-CH2, a method for preparing said derivatives, and the therapeutical uses thereof, are disclosed.
摘要翻译：通式（I）的恶唑烷-2-酮衍生物，其中R 1是氢原子，烷基，羟基烷基，氟代烷基，羟基氟烷基，氰基烷基，任选取代的苯基或任选取代的苯基甲基，或基团R 3 -A，其中R 3是环烷基或任选被羟基取代的环氧烷基，A是-CH 2或-CH 2 -CH 2基，R 2是氢原子或甲基，X是氧或硫原子或基团R 4，其中R 4是烷基，Z为氧原子或-CH = CH或-CH 2 -CH 2基，制备所述衍生物的方法及其治疗用途。

2. 发明申请

WO1997017347A1 COMPOUNDS DERIVED FROM OXAZOLIDIN-2-ONE AND PREPARATION AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译：衍生自奥沙星2-ONE的化合物及其制备及其治疗用途
公开(公告)号：WO1997017347A1
公开(公告)日：1997-05-15
申请号：PCT/FR1996001732
申请日：1996-11-05
申请人： SYNTHELABO , JEGHAM, Samir , PUECH, Frédéric , BURNIER, Philippe , BERTHON, Danielle
发明人： SYNTHELABO
IPC分类号： C07D413/04
CPC分类号： C07D413/04
摘要： Oxazolidin-2-one derivatives of general formula (I), wherein n is 0 or 1, R1 is a cyano, alkyl or fluoroalkyl group, R2 is a hydrogen atom or a hydroxyl group, and R3 is a hydrogen atom or a methyl group, and the therapeutical use thereof, are disclosed.
摘要翻译：通式（I）的恶唑烷-2-酮衍生物，其中n为0或1，R1为氰基，烷基或氟代烷基，R2为氢原子或羟基，R3为氢原子或甲基，及其治疗用途。

3. 发明申请

WO1997017346A1 COMPOUNDS DERIVED FROM 3-(BENZOFURAN-5-YL)OXAZOLIDIN-2-ONE, PREPARATION METHOD THEREFOR AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译：衍生自3-（苯并呋喃-5-基）氧杂环丁烷-2-酮的化合物，其制备方法及其治疗用途
公开(公告)号：WO1997017346A1
公开(公告)日：1997-05-15
申请号：PCT/FR1996001731
申请日：1996-11-05
申请人： SYNTHELABO , JEGHAM, Samir , PUECH, Frédéric , BURNIER, Philippe , BERTHON, Danielle
发明人： SYNTHELABO
IPC分类号： C07D413/04
CPC分类号： C07D413/04
摘要： Compounds derived from 3-(benzofuran-5-yl)oxazolidin-2-one, having general formula (I), wherein R1 is a phenyl, phenylmethyl, alkyl or fluoroalkyl group and R2 is a hydrogen atom or a methyl group, and the therapeutical use thereof, are disclosed.
摘要翻译：衍生自具有通式（I）的3-（苯并呋喃-5-基）恶唑烷-2-酮的化合物，其中R 1是苯基，苯基甲基，烷基或氟烷基，R 2是氢原子或甲基，公开了其治疗用途。

4. 发明申请

WO1996038444A1 OXAZOLIDINONE DERIVATIVES, THEIR PREPARATION AND THERAPEUTICAL USE 审中-公开
标题翻译：奥沙利汀衍生物，其制备和治疗用途
公开(公告)号：WO1996038444A1
公开(公告)日：1996-12-05
申请号：PCT/FR1996000792
申请日：1996-05-28
申请人： SYNTHELABO , JEGHAM, Samir , PUECH, Frédéric , BURNIER, Philippe
发明人： SYNTHELABO
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D417/04
摘要： The disclosed 5-(hydroxymethyl)oxazolidin-2-one derivatives are 3-substituted by an indazol, benzisoxazol or benzisothiazol ring and have the general formula (I), in which X stands for an oxygen atom, a sulphur atom or a NR group, R being a hydrogen atom or a linear or branched C1-C4 alkyl chain; R1 stands for a hydrogen atom or a methyl group; and R2 stands for either (i) a R3O group in which R3 stands for a hydrogen atom or a benzyl group optionally substituted by a halogen atom or by a nitro or methylene dioxy group, or for a methoxyethyl, butyl, 4,4,4-trifluorobutyl, 4,4,4-trifluoro-3-hydroxybutyl or 4,4,4-trifluorobut-2-enyl group; or for (ii) a -CH=CH-R or -CH2-CH2-R4 group in which R4 stands for a hydrogen atom or a phenyl, 3,3,3-trifluoropropyl or 3,3,3-trifluoro-2-hydroxypropyl group. Also disclosed are their process of preparation and their therapeutical applications.
摘要翻译：所公开的5-（羟甲基）恶唑烷-2-酮衍生物被吲唑，苯并异恶唑或苯并异噻唑环3-取代，具有通式（I），其中X代表氧原子，硫原子或NR基团 R为氢原子或直链或支链C 1 -C 4烷基链; R1代表氢原子或甲基; R2表示（i）R3代表氢原子或任选被卤素原子取代的苄基或硝基或亚甲基二氧基的R3O基，或甲氧基乙基，丁基，4,4,4 四氟丁基，4,4,4-三氟-3-羟基丁基或4,4,4-三氟丁-2-烯基; 或者（ⅱ）-CH = CH-R或-CH2-CH2-R4基，其中R4代表氢原子或苯基，3,3,3-三氟丙基或3,3,3-三氟-2- 羟丙基。还公开了它们的制备方法及其治疗应用。

5. 发明申请

WO1998024790A1 1,4-DIAZABICYCLO [2.2.2] OCT-2-YLMETHYL DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC APPLICATION 审中-公开
标题翻译： 1,4-二氮杂双环[2.2.2] OCT-2-甲基衍生物，其制备和治疗应用
公开(公告)号：WO1998024790A1
公开(公告)日：1998-06-11
申请号：PCT/FR1997002174
申请日：1997-12-02
申请人： SYNTHELABO , LOCHEAD, Alistair , JEGHAM, Samir , NEDELEC, Alain , SOLIGNAC, Axelle
发明人： SYNTHELABO
IPC分类号： C07D487/08
CPC分类号： C07D487/08
摘要： The invention concerns compounds of general formula (I) in which R1 represents a methyl group, X1 represents a hydrogen atom, or OR1 and X1 together form a group of formula -O(CH2)2-, -O(CH2)3-, -O(CH2)2O-, or -O(CH2)3O-, X2 represents a hydrogen atom or an amino group, and X3 represents a halogen atom. The compounds are ligands of serotoninergic receptors of the 5-HT3 and/or 5-HT4 types, and act as 5-HT4 agonists and/or 5-HT3 antagonists.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1表示甲基，X 1表示氢原子，或OR 1和X 1一起形成式-O（CH 2）2 - ， - O（CH 2）3 - -O（CH 2）2 O-或-O（CH 2）3 O-，X 2表示氢原子或氨基，X 3表示卤素原子。这些化合物是5-HT3和/或5-HT4类型的5-羟色胺能受体的配体，并且作为5-HT4激动剂和/或5-HT3拮抗剂。

6. 发明申请

WO1997017345A1 5-PHENYL-3-(PIPERIDIN-4-YL)-1,3,4-OXADIAZOL-2(3H)-ONE DERIVATIVES FOR USE AS 5-HT4 OR H3 RECEPTOR LIGANDS 审中-公开
标题翻译：用作5-HT4或H3受体配体的5-苯基-3-（哌啶-4-基）-1,3,4-氧杂双唑-2（3H） - 酮衍生物
公开(公告)号：WO1997017345A1
公开(公告)日：1997-05-15
申请号：PCT/FR1996001730
申请日：1996-11-05
申请人： SYNTHELABO , JEGHAM, Samir , LOCHEAD, Alistair , GALLI, Frédéric , NEDELEC, Alain , SOLIGNAC, Axelle , DE CRUZ, Laurence
发明人： SYNTHELABO
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： Compounds of general formula (I), wherein R1 is a (C1-4) alkyl or (C3-7) cycloalkylmethyl group, X1 is a hydrogen or halogen atom or a (C1-4) alkoxy group, or OR1 and X1 together form a group of formula -OCH2O-, -O(CH2)2-, -O(CH2)3-, -O(CH2)2O- or -O(CH2)3O-, X2 is a hydrogen atom or an amino group, X3 is a hydrogen or halogen atom, and R2 is a hydrogen atom, an optionally substituted (C1-6) alkyl group, a phenyl (C1-4) alkyl group optionally substituted on the phenyl ring, a phenyl (C2-3) alkenyl group, a phenoxy (C2-4) alkyl group, a cyclo (C3-7) alkylmethyl group, a 2,3-dihydro-1H-inden-1-yl or 2,3-dihydro-1H-inden-2-yl group, or a group having general formula -(CH2)nCO-Z, wherein n is a number from 1 to 6 and Z is a piperidin-1-yl or 4-(dimethylamino)piperidin-1-yl group, are disclosed. Said compounds may be used for treating and preventing disorders in which 5-HT4 and/or H3 receptors are involved, particularly in the central nervous system, the gastro-intestinal system, the lower urinary organs or the cardiovascular system.
摘要翻译：通式（I）的化合物，其中R 1是（C 1-4）烷基或（C 3-7）环烷基甲基，X 1是氢或卤素原子或（C 1-4）烷氧基，或OR 1和X 1一起形成式-OCH 2 O-，-O（CH 2）2 - ， - O（CH 2）3 - ， - O（CH 2）2 O-或-O（CH 2）3 O-的基团，X 2是氢原子或氨基， X 3为氢或卤原子，R 2为氢原子，任意取代的（C 1-6）烷基，苯基（C 1-4）烷基，苯基（C 2-3）烯基基团，苯氧基（C 2-4）烷基，环（C 3-7）烷基甲基，2,3-二氢-1H-茚-1-基或2,3-二氢-1H-茚-2-基基团或具有通式 - （CH 2）n CO-Z的基团，其中n为1至6的数，Z为哌啶-1-基或4-（二甲基氨基）哌啶-1-基。所述化合物可用于治疗和预防其中涉及5-HT4和/或H3受体的疾病，特别是在中枢神经系统，胃肠系统，下泌尿器官或心血管系统中。

7. 发明申请

WO1998004546A1 BENZIMIDAZOLE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTICAL USES THEREOF 审中-公开
标题翻译：苯并咪唑衍生物，其制备方法及其治疗用途
公开(公告)号：WO1998004546A1
公开(公告)日：1998-02-05
申请号：PCT/FR1997001364
申请日：1997-07-23
申请人： SYNTHELABO , COURTEMANCHE, Gilles , EVEN, Luc , DEFOSSE, Gérard , BERTIN, Jean , BOVY, Philippe
发明人： SYNTHELABO
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D471/04
摘要： Compounds of formula (I), wherein A is a nitrogen atom or a CH group; B is a C4-8 cycloalkyl group, a naphthyl group or a group of formula (Y), where n is 0 or 1; X is an oxygen or sulphur atom; Z is a nitrogen atom or a CH group; R2 is a hydrogen atom, a C1-4 alkyl group or a phenyl group; R3 is a C3-6 cycloalkyl group, a phenyl group, benzyl, a furyl group, thienyl, pyrrolyl, pyrazolyl, isoxazolyl, thioazolyl, pyridyl, imidazolyl or benzimidazolyl; and R7 is a hydrogen atom or a straight or branched C1-4 alkyl group; and the therapeutical uses thereof, are disclosed.
摘要翻译：式（I）的化合物，其中A是氮原子或CH基团; B是C 4-8环烷基，萘基或式（Y）的基团，其中n是0或1; X是氧或硫原子; Z是氮原子或CH基团; R2是氢原子，C1-4烷基或苯基; R3是C3-6环烷基，苯基，苄基，呋喃基，噻吩基，吡咯基，吡唑基，异恶唑基，硫代唑基，吡啶基，咪唑基或苯并咪唑基; 且R 7为氢原子或直链或支链C 1-4烷基; 及其治疗用途。

8. 发明申请

WO1997009310A1 1-PHENYL-3-4-[BENZYLPIPERIDINYL-1]-PROPANOL-1 DERIVATIVES, PREPARATION THEREOF AND THERAPEUTICAL APPLICATION THEREOF 审中-公开
标题翻译： 1-苯基-3,4- - [苄基]吡啶-2-基] - 丙醇1衍生物，其制备方法及其应用
公开(公告)号：WO1997009310A1
公开(公告)日：1997-03-13
申请号：PCT/FR1996001361
申请日：1996-09-05
申请人： SYNTHELABO , FROST, Jonathan , GAUDILLIERE, Bernard , ROUSSEAU, Jean
发明人： SYNTHELABO
IPC分类号： C07D211/14
CPC分类号： C07D211/18 , C07D211/14
摘要： Compounds of general formula (I), wherein R1 is a hydrogen or halogen atom or a methyl or methoxy group, R2 is a hydrogen atom or a methyl group, and R3 is a hydrogen or halogen atom, are useful for therapeutical applications.
摘要翻译：通式（I）的化合物，其中R 1为氢或卤素原子或甲基或甲氧基，R 2为氢原子或甲基，R 3为氢或卤素原子，可用于治疗用途。

9. 发明申请

WO1998022443A1 N-(IMIDAZOLYLBUTYL) BENZENESULPHONAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC APPLICATION 审中-公开
标题翻译： N-（咪唑啉基）苯并噻吩衍生物及其制备和治疗应用
公开(公告)号：WO1998022443A1
公开(公告)日：1998-05-28
申请号：PCT/FR1997002079
申请日：1997-11-19
申请人： SYNTHELABO , ALTENBURGER, Jean-Michel , LASSALLE, Gilbert , MARTIN, Valérie , GALTIER, Daniel
发明人： SYNTHELABO
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07D233/68 , C07D401/06 , C07D401/12 , C07D409/12 , C07D409/14
摘要： The invention concerns compounds of formula (I) in which R1 and R'1 represent hydrogen, halogen or (C1-C4) alkyl, R2 represents a piperidin-1-yl group, 1, 2, 3, 6-tetrahydropyridin-1-yl optionally substituted, hexahydro-1H-azepin-1-yl, heptahydroazocin-1-yl, octahydro-1H-azonin-1-yl, (a) (A-B = -CONR", m = 1 to 2 and p = 1 to 2), (b) (Q = carbon or nitrogen, D = (C1-C4) alkyl or -CH2CF3, and r = 1 to 3, R3 represents (C1-C5) alkyl, -COR5 [R5 being (C1-C4) alkyl, -(CH2)nOCH3, -CH2O(C2H4O)nCH3, -(CH2)nCF3, -(CH2)nOH (n = 1 to 4)], -SO2R6, -CONHR6, -SO2N(R6)2 (R6 being (C1-C4) alkyl), R4 represents hydrogen or halogen and A represents phenyl or heterocycle optionally substituted or cyclo (C5-C8) alkyl. The invention is applicable in therapeutics.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 1表示氢，卤素或（C 1 -C 4）烷基，R 2表示哌啶-1-基，1,2,3,6-六氢吡啶-1-基，（a）（AB = -CONR“，m = 1〜2，p = 1〜2， 2），（b）（Q =碳或氮，D =（C 1 -C 4）烷基或-CH 2 CF 3，r = 1至3，R 3表示（C 1 -C 5）烷基，-COR 5 [ ）（CH 2）n CF 3， - （CH 2）n OH（n = 1-4）]，-SO 2 R 6，-CONHR 6，-SO 2 N（R 6）2 （C 1 -C 4）烷基），R 4表示氢或卤素，A代表苯基或任选取代的杂环或环（C 5 -C 8）烷基。

10. 发明申请

WO1997038998A1 3-[(1,2,3,4-TETRAHYDROISOQUINOLINE-2-YL)METHYL]-8-AZABICYCLO[3.2.1]OCTANE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 审中-公开
标题翻译： 3 - [（1,2,3,4-四氢喹啉-2-基）甲基] -8-亚氨基] [3.2.1]月桂衍生物，其制备及其在治疗中的应用
公开(公告)号：WO1997038998A1
公开(公告)日：1997-10-23
申请号：PCT/FR1997000634
申请日：1997-04-10
申请人： SYNTHELABO , SEVRIN, Mireille , MARABOUT, Benoit , GEORGE, Pascal , MERLY, Jean-Pierre
发明人： SYNTHELABO
IPC分类号： C07D451/02
CPC分类号： C07D451/02
摘要： Compounds of general formula (I) in which each of R1, R2 and R3 represents a hydrogen or halogen atom or a hydroxy, alkyl or alkoxy group, R4 represents a hydrogen or halogen atom or an alkyl, 2-methoxyethoxy, alkoxy, cycloalkylmethoxy or phenylmethoxy group, or R3 and R4 together form a methylenedioxy group, Z represents oxygen or two hydrogen atoms and R represents an ethoxy group when Z represents oxygen, or represents a phenyl group optionally substituted by one or more halogen atoms or alkyl, alkoxy or amino groups. The compounds have a strong affinity for dopamine receptors of D2 and D3 type and for serotonin receptors of 5-HT1A and 5-HT2 type and are mixed ligands. Other compounds have a strong affinity for the dopamine receptors of D3 type and a weak affinity for the dopamine receptors of D2 type and serotonin receptors of 5-HT1A and 5-HT2 and are therefore selective and specific ligands.
摘要翻译： R 1，R 2和R 3各自表示氢或卤素原子或羟基，烷基或烷氧基的通式（I）的化合物，R 4表示氢或卤素原子或烷基，2-甲氧基乙氧基，烷氧基，环烷基甲氧基或苯基甲氧基或R3和R4一起形成亚甲二氧基，Z表示氧或两个氢原子，当Z表示氧时R表示乙氧基，或表示任选被一个或多个卤素原子取代的苯基或烷基，烷氧基或氨基组。这些化合物对D2和D3型的多巴胺受体和5-HT1A和5-HT2型的血清素受体具有强烈的亲合力，并且是混合配体。其他化合物对D3型多巴胺受体具有强亲和力，对5型HT1A和5-HT2的D2型和5-羟色胺受体的多巴胺受体具有弱亲和性，因此是选择性和特异性配体。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式