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21. 发明申请

WO1998008834A1 BENZYLAMINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 审中-公开
标题翻译：苯甲酰胺衍生物，其制备及其在治疗中的应用
公开(公告)号：WO1998008834A1
公开(公告)日：1998-03-05
申请号：PCT/FR1997001514
申请日：1997-08-22
申请人： SYNTHELABO , PHILIPPO, Christophe , ORTS, Marie-Claire , CRESPIN, Olivier , BOVY, Philippe
发明人： SYNTHELABO
IPC分类号： C07D307/79
CPC分类号： C07D307/79
摘要： Compounds of general formula (I) in which: A represents either one hydrogen atom, one hydroxyl, one C1-6 hydroxyalkyl group, one thiol, one C1-6 alkylsulphanyl group, one amine group, one C1-6 alkylamine group, one di (C1-6 alkyl) amine group, one C1-6 alkyl hydroxylamine group, one C1-6 alcoxy group, one hydroxylamine group, one C1-6 N, O-dialkyl hydroxylamine group, one azide, one halogen such as fluorine, chlorine or bromine, B represents one hydrogen atom, one C1-6 alkyl, branched or linear, one C2-6 alkenyl group, one C1-6 fluoroalkyl group, one C1-2 perfluoroalkyl group, one C1-6 alcoxy group, one phenyl group, or one oxo group, X represents one oxygen or sulphur atom. The invention is useful in therapeutics.
摘要翻译：通式（I）的化合物，其中：A表示一个氢原子，一个羟基，一个C1-6羟烷基，一个硫醇，一个C1-6烷基硫烷基，一个胺基，一个C1-6烷基胺基，一个二（C 1-6烷基）胺基，一个C 1-6烷基羟胺基，一个C 1-6烷氧基，一个羟胺基，一个C 1-6 N，O-二烷基羟胺基，一个叠氮化物，一个卤素如氟，氯或溴，B表示一个氢原子，一个C 1-6烷基，支链或直链，一个C 2-6烯基，一个C 1-6氟烷基，一个C 1-2全氟烷基，一个C 1-6烷氧基，一个苯基，或一个氧代基，X表示一个氧或硫原子。本发明在治疗中是有用的。

22. 发明申请

WO1997032870A1 2-AMINOETHYL-BENZOFURAN DERIVATIVES, PREPARATION THEREOF AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译： 2-氨基乙基苯并呋喃衍生物，其制备方法及其治疗用途
公开(公告)号：WO1997032870A1
公开(公告)日：1997-09-12
申请号：PCT/FR1997000383
申请日：1997-03-05
申请人： SYNTHELABO , PHILIPPO, Christophe , COURTEMANCHE, Gilles , FETT, Eykmar , ORTS, Marie, Claire , BOVY, Philippe , O'CONNOR, Stephen, Eric , GALZIN, Anne, Marie
发明人： SYNTHELABO
IPC分类号： C07D307/79
CPC分类号： C07D307/79
摘要： Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C1-8 alkyl, C1-8 alkenyl, C1-8 fluoroalkyl or C1-8 perfluoroalkyl group; each of R1, R2 and R5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C1-8 alkyl, C1-8 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C6, C10 or C14 aryl, C1-6 alkoxycarbonyl, C1-6 hydroxyalkyl, C1-6 alkoxyalkyl, C1-6 alkoxy, C1-8 fluoroalkyl or C1-8 perfluoroalkyl group, or R1 and R2 taken together form a C3-8 cycloalkyl, C3-8 cycloalkenyl or C6, C10 or C14 aryl ring, except for compounds in which R1 and R2 are both hydrogen; each of R3 and R4, which are the same or different, is a hydrogen atom or a C1-8 alkyl, C1-8 alkenyl, C3-8 cycloalkyl or C3-8 cycloalkenyl group, or R3 and R4 taken together form a C2-6 cycloalkyl or C3-6 cycloalkenyl ring, e.g. piperidyl, azetidinyl or pyrrolidyl; in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are disclosed. The compounds may be used in therapy.
摘要翻译：式（I）的化合物，其中A是氢原子或羟基; B是氢原子或C 1-8烷基，C 1-8烯基，C 1-8氟烷基或C 1-8全氟烷基; R 1，R 2和R 5各自相同或不同，为氢原子，卤素如氯，溴或氟，C 1-8烷基，C 1-8烯基，C 3-8环烷基，C 3-8环烯基，C 6，C 10或C 14芳基，C 1-6烷氧基羰基，C 1-6羟基烷基，C 1-6烷氧基烷基，C 1-6烷氧基，C 1-8氟代烷基或C 1-8全氟烷基，或者R 1和R 2一起形成C 3-8 环烷基，C3-8环烯基或C6，C10或C14芳基环，其中R1和R2均为氢的化合物; R 3和R 4各自相同或不同，为氢原子或C 1-8烷基，C 1-8烯基，C 3-8环烷基或C 3-8环烯基，或者R 3和R 4一起形成C2- 6环烷基或C 3-6环烯基环，例如哌啶基，氮杂环丁烷基或吡咯烷基; 公开了其对映异构体，非对映异构体或其混合物的形式，包括外消旋混合物，以及其药学上可接受的酸加成盐。该化合物可用于治疗。

23. 发明申请

WO1997020836A1 5-NAPHTHALEN-1-YL-1,3-DIOXANE DERIVATIVES, PREPARATION AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译： 5-萘-1-基-1,3-二氧化物衍生物，其制备及其治疗用途
公开(公告)号：WO1997020836A1
公开(公告)日：1997-06-12
申请号：PCT/FR1996001926
申请日：1996-12-04
申请人： SYNTHELABO , DARGAZANLI, Gihad , EVANNO, Yannick , FROST, Jonathan , LARDENOIS, Patrick , SEVRIN, Mireille , GEORGE, Pascal
发明人： SYNTHELABO
IPC分类号： C07D319/06
CPC分类号： C07D319/06
摘要： Compounds of general formula (I), wherein R1 is a hydrogen atom or a (C1-4) alkyl, (C3-6) cycloalkylméthyl or phenyl (C1-3) alkyl group optionally substituted on the phenyl ring by one or more atoms or groups selected from halogens and methyl, trifluoromethyl, methoxy and cyano groups, R2 is a hydroxy or alkoxy group or a group of general formula NR3R4 where each of R3 and R4 is a hydrogen atom, an alkyl group, a cycloalkyl group, a cycloalkylmethyl group, a phenyl group, a phenylmethyl group or a pyridinyl group, or R3 and R4, taken together with the nitrogen atom, form a pyrrolidine or piperidine ring, and n is 1, 2 or 3. The compounds are for therapeutical use.
摘要翻译：通式（I）的化合物，其中R 1为氢原子或（C 1-4）烷基，（C 3-6）环烷基乙基或苯基（C 1-3）烷基，其任意在苯环上被一个或多个原子取代或选自卤素和甲基，三氟甲基，甲氧基和氰基的基团，R2是羟基或烷氧基或通式为NR3R4的基团，其中R3和R4各自为氢原子，烷基，环烷基，环烷基甲基苯基，苯甲基或吡啶基，或者R3和R4与氮原子一起形成吡咯烷或哌啶环，n为1,2或3。这些化合物用于治疗用途。

24. 发明申请

WO1997006155A1 1-[2-(2,3-DIHYDRO-1H-INDEN-1-YL)ETHYL]-4-(NAPHTHALEN-1-YL)PIPERAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译： 1- [2-（2,3-二氢-1H-茚-1-基）乙基] -4-（萘-1-基）哌嗪衍生物，其制备方法及其治疗用途
公开(公告)号：WO1997006155A1
公开(公告)日：1997-02-20
申请号：PCT/FR1996001216
申请日：1996-08-01
申请人： SYNTHELABO , GEORGE, Pascal , SEVRIN, Mireille , MANOURY, Philippe , PEYNOT, Michel , DE PERETTI, Danièle , GIBERT, Jean, François , TIXIDRE, Arlette , MACHNIK, David
发明人： SYNTHELABO
IPC分类号： C07D295/08
CPC分类号： C07D295/033 , C07D295/096
摘要： Compounds of general formula (I), wherein X is a hydrogen atom, a hydroxy group, a C1-3 alkoxy group or a cyclopropylmethoxy group, and Y is a hydrogen atom, a hydroxy group or a methoxy group, are provided for therapeutical use.
摘要翻译：通式（I）的化合物，其中X为氢原子，羟基，C 1-3烷氧基或环丙基甲氧基，Y为氢原子，羟基或甲氧基，用于治疗用途。

25. 发明申请

WO1997002823A1 USE OF POLYAMINE ANTAGONISTS FOR THE TREATMENT OF GLAUCOMA 审中-公开
标题翻译：使用聚酰胺拮抗剂治疗葡萄球菌
公开(公告)号：WO1997002823A1
公开(公告)日：1997-01-30
申请号：PCT/US1995008150
申请日：1995-07-12
申请人： SYNTHELABO
发明人： SYNTHELABO , KAPIN, Michael, A. , DeSANTIS, Louis, Jr. , LANGER, Salomon
IPC分类号： A61K31/445
CPC分类号： A61K31/445 , A61K31/00 , Y10S514/913
摘要： Polyamine antagonists are found to be effective in preventing or reducing visual field loss associated with glaucoma. Especially preferred are certain 1-phenyl-2-piperidinoalkanol derivatives, such as eliprodil and ifenprodil.
摘要翻译：发现多胺拮抗剂有效预防或减少与青光眼有关的视野丧失。特别优选的是1-苯基-2-哌啶子基链烷醇衍生物，例如厄洛替丁和伊芬醌。

26. 发明公开

EP0728000A1 THE USE OF ALFUZOSIN OR TERAZOSIN IN THE TREATMENT OF PREMATURE EJACULATION 失效
标题翻译：或阿夫唑嗪特拉唑嗪在治疗早泄USE
公开(公告)号：EP0728000A1
公开(公告)日：1996-08-28
申请号：EP94931582.0
申请日：1994-11-08
申请人： SYNTHELABO
发明人： SYNTHELABO
IPC分类号： C07D405 , A61K31 , A61K45 , A61P13 , A61P15 , A61P43
CPC分类号： A61K31/517 , A61K31/505
摘要： The use of the a1-blockers drugs, alfuzosin and terazosin in the treatment of premature ejaculation is disclosed.

27. 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。

28. 发明申请

WO1998011112A1 TRICYCLIC INDAZOLE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION THEREOF 审中-公开
标题翻译：三唑吲哚衍生物，其制备和治疗应用
公开(公告)号：WO1998011112A1
公开(公告)日：1998-03-19
申请号：PCT/FR1997001581
申请日：1997-09-09
申请人： SYNTHELABO , EVEN, Luc , ALETRU, Michel
发明人： SYNTHELABO
IPC分类号： C07D498/06
CPC分类号： C07D471/06
摘要： The invention concerns compounds of general formula (I) in which: X represents one oxygen atom or one methene group, R1 represents one hydrogen atom, one halogen such as bromine, chlorine or fluorine, one C1-4 oxyalkylate group, or one hydroxyl or amino group; R2, R3, and R4, identical or different, represent either one hydrogen atom, or one C1-4 alkyl group, linear or branched, one phenyl group or one benzyl group, and R5 represents one hydrogen atom, one hydroxyl group, one amino group or one C1-4 alkyl group, in the form of enantiomer, of diastereoisomer, including racemic mixture as well as their additive salt to pharmaceutically acceptable acids. The compounds of formula I are antagonists of 5-HT3 and 5-HT4 serotoninergic receptors.
摘要翻译：本发明涉及通式（I）的化合物，其中：X表示一个氧原子或一个元素基团，R1表示一个氢原子，一个卤素如溴，氯或氟，一个C1-4烷氧基化物或一个羟基或氨基; R2，R3和R4相同或不同，表示一个氢原子或一个C 1-4烷基，直链或支链，一个苯基或一个苄基，R5表示一个氢原子，一个羟基，一个氨基基团或一个C1-4烷基，以对映异构体的形式，包括外消旋混合物以及它们的添加盐与药学上可接受的酸形成非对映异构体。式I的化合物是5-HT3和5-HT4血清素能受体的拮抗剂。

29. 发明申请

WO1998000423A1 1-OXO-1,2-DIHYDROISOQUINOLINE-4-PROPANAMIDE DERIVATIVES AND THEIR APPLICATION IN THERAPEUTICS 审中-公开
标题翻译： 1-氧代-1,2-二氢吲哚啉-4-丙酰胺衍生物及其在治疗中的应用
公开(公告)号：WO1998000423A1
公开(公告)日：1998-01-08
申请号：PCT/FR1997001126
申请日：1997-06-25
申请人： SYNTHELABO , MARABOUT, Benoit , SEVRIN, Mireille , FROISSANT, Jacques
发明人： SYNTHELABO
IPC分类号： C07D409/04
CPC分类号： C07D217/24
摘要： The invention discloses compounds of general formula (I) in which X represents an atom of hydrogen or of chlorine or of a methyl group, trifluoromethyl or methoxy; R1 represents a methyl group; R2 and R3 each represent an atom of hydrogen or an alkyl group, or form, with the nitrogen atom, a pyrrolidinyl ring; and R4 represents a furan-2-yl, thien-2-yl, thien-3 yl or 5-methyl-thien-3-yl. It is applicable in therapeutics.
摘要翻译：本发明公开了通式（I）的化合物，其中X表示氢或氯或甲基或三氟甲基或甲氧基的原子; R1表示甲基; R2和R3各自表示氢原子或烷基，或与氮原子形成吡咯烷基环; R 4代表呋喃-2-基，噻吩-2-基，噻吩-3-基或5-甲基噻吩-3-基。适用于治疗。

30. 发明申请

WO1997033582A1 POLYAMINE SITE ANTAGONIST COMPOSITIONS 审中-公开
标题翻译：聚氨基甲酸丁酯组合物
公开(公告)号：WO1997033582A1
公开(公告)日：1997-09-18
申请号：PCT/FR1997000447
申请日：1997-03-13
申请人： SYNTHELABO
发明人： SYNTHELABO , KAPIN, Michael, A. , GOODE, Stephen, M. , SCATTON, Bernard , LANGER, Salomon
IPC分类号： A61K31/445
CPC分类号： A61K31/445
摘要： (NMDA) polyamine site antagonist compositions for treating optical neuritis, and specifically the use of eliprodil or ifenprodil for treating said disease, are disclosed.
摘要翻译：（NMDA）多胺位点拮抗剂组合物用于治疗光学神经炎，并且具体地使用厄洛替丁或伊芬生药物治疗所述疾病。

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