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1. 发明授权

US5001132A Phenyloxypropanolamine derivatives and their application in therapeutics 失效
标题翻译：苯氧基丙醇胺衍生物及其在治疗中的应用
公开(公告)号：US5001132A
公开(公告)日：1991-03-19
申请号：US432686
申请日：1989-11-07
申请人： Philippe Manoury , Jean Binet , Gerard Defosse
发明人： Philippe Manoury , Jean Binet , Gerard Defosse
IPC分类号： A61K31/435 , A61P27/02 , A61P27/06 , C07D471/04
CPC分类号： C07D471/04
摘要： Phenyloxypropanolamine derivatives in the form of racemates or enantiometers, of formula (I) ##STR1## in which R is H or CH3, and their pharmaceutically acceptable salts.
摘要翻译：式（I）其中R为H或CH 3的式（I）的消旋体或对映体形式的苯氧基丙醇胺衍生物及其药学上可接受的盐。

2. 发明授权

US4885296A 1-piperazinylpyrimidine derivatives and application thereof in therapeutics and cosmetics 失效
标题翻译： 1-哌嗪基嘧啶衍生物及其在治疗和化妆品中的应用
公开(公告)号：US4885296A
公开(公告)日：1989-12-05
申请号：US126799
申请日：1987-12-01
申请人： Philippe Manoury , Jean F. Grollier
发明人： Philippe Manoury , Jean F. Grollier
IPC分类号： C07D239/48 , A61K8/00 , A61K8/49 , A61K8/73 , A61K31/505 , A61P43/00 , A61Q5/00 , A61Q7/00 , C07D239/50 , C07D403/04 , C07D403/12 , C07D405/12
CPC分类号： C07D239/50 , A61K8/4953 , A61Q7/00 , C07D405/12 , Y10S514/88
摘要： New compounds derived from 1-piperazinylpyrimidine derivatives, and their application in therapeutics and cosmetics, corresponding to the general formula: ##STR1## in which R represents an alkoxycarbonyl group containing from 1 to 3 carbon atoms in the alkoxy chain or alternatively a furoyl group, n being 0 or 1, and their addition salts with cosmetically or pharmaceutically acceptable acids.
摘要翻译：衍生自1-哌嗪基嘧啶衍生物的新化合物及其在治疗和化妆品中的应用，其通式如下：其中R表示在烷氧基链中含有1至3个碳原子的烷氧基羰基，或者替代地，糠酰基，n为0或1，以及它们与化妆品或药学上可接受的酸的加成盐。

3. 发明授权

US5929078A 1-�2-(2,3-Dihydro-1H-inden-1-yl)ethyl!-4-(naphthalen-1-yl) piperazine, derivatives, preparation thereof and therapeutical use thereof 失效
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，其制备及其治疗用途
公开(公告)号：US5929078A
公开(公告)日：1999-07-27
申请号：US11807
申请日：1998-02-03
申请人： Pascal George , Mireille Sevrin , Philippe Manoury , Michel Peynot , Daniele De Peretti , Jean Fran.cedilla.ois Gibert , Arlette Tixidre , David Machnik
发明人： Pascal George , Mireille Sevrin , Philippe Manoury , Michel Peynot , Daniele De Peretti , Jean Fran.cedilla.ois Gibert , Arlette Tixidre , David Machnik
IPC分类号： C07D295/02 , A61K31/00 , A61K31/495 , A61P9/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30 , C07D295/033 , C07D295/08 , C07D295/096
CPC分类号： C07D295/033 , C07D295/096
摘要： Compounds corresponding to the general formula (I): ##STR1## in which X represents a hydrogen atom, a hydroxyl group, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom, a hydroxyl group or a methoxy group and salts and bases thereof. The compounds may exists in the form of a pure enantiomer or as a mixture of enantiomers. Additionally, the compounds of formula (I) are useful for the treatment of diseases associated with serotoninergic receptors, particularly anxiety and/or depression.
摘要翻译： PCT No.PCT / FR96 / 01216 Sec。 371日期：1998年4月15日 102（e）日期1998年4月15日PCT提交1996年8月1日PCT公布。公开号WO97 / 06155 日期1997年2月20日对应于通式（I）的化合物：其中X表示氢原子，羟基，C1-C3烷氧基或环丙基甲氧基，Y表示氢原子，羟基或甲氧基基团及其盐和碱。化合物可以以纯对映异构体的形式存在或作为对映异构体的混合物存在。此外，式（I）化合物可用于治疗与血清素能受体有关的疾病，特别是焦虑和/或抑郁症。

4. 发明授权

US5244894A 2-aminopyrimidine-4-carboxamide derivatives, their preparation and their use in therapeutics 失效
标题翻译： 2-氨基嘧啶-4-羧酰胺衍生物，其制备及其在治疗中的应用
公开(公告)号：US5244894A
公开(公告)日：1993-09-14
申请号：US904060
申请日：1992-06-26
申请人： Pascal George , Philippe Manoury , Benoit Marabout , Jacques Froissant , Jean-Pierre Merly
发明人： Pascal George , Philippe Manoury , Benoit Marabout , Jacques Froissant , Jean-Pierre Merly
IPC分类号： A61K31/505 , A61K31/506 , A61P13/00 , A61P13/02 , A61P13/08 , A61P15/00 , C07D239/42 , C07D239/46 , C07D295/13 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12
CPC分类号： C07D239/42 , C07D239/47 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Compounds corresponding to the general formula (I) ##STR1## in which n=2 or 3, X=H, F, Cl or OCH.sub.3, R=H or CH.sub.3, R.sub.1 =H or CH.sub.3, R.sub.2 =alkyl, hydroxyalkyl, (hydroxy)(methoxy)alkyl, dimethoxyalkyl, 2-(aminosulphonyl)ethyl, 2-(methylsulphonyl)ethyl, 2-(methylsulphonylamino)ethyl, aminocarbonylmethyl which is optionally substituted by nitrogen, phenylethyl which is optionally substituted, pyrimidinylaminoalkyl or arylcaronylaminoalkyl, or else R.sub.1 and R.sub.2 form, with the nitrogen which carries them, a piperidine, morpholine, thiomorpholine or piperazine ring, optionally substituted by nitrogen. Use in therapeutics.
摘要翻译：对应于通式（I）的化合物其中n = 2或3，X = H，F，Cl或OCH 3，R = H或CH 3，R 1 = H或CH 3，R 2 =烷基，羟基烷基，（羟基）（甲氧基）烷基，二甲氧基烷基，2-（氨基磺酰基）乙基，2-（甲基磺酰基）乙基，2-（甲基磺酰基氨基）乙基，任选被氮取代的氨基羰基甲基，任选取代的苯基乙基，嘧啶基氨基烷基或芳基羰基氨基烷基，或者R1和R2与携带它们的氮形成任选被氮取代的哌啶，吗啉，硫代吗啉或哌嗪环。用于治疗。

5. 发明授权

US4891376A 1-((2-Pyrimidinyl)aminoalkyl)piperidines, their preparation and their application in therapy 失效
标题翻译： 1 - （（2-嘧啶基）氨基烷基）哌啶，其制备及其在治疗中的应用
公开(公告)号：US4891376A
公开(公告)日：1990-01-02
申请号：US242430
申请日：1988-09-08
申请人： Philippe Manoury , Alfred Saarmets
发明人： Philippe Manoury , Alfred Saarmets
IPC分类号： A61K31/505 , A61P7/04 , A61P9/12 , A61P11/00 , A61P23/00 , A61P25/00 , A61P25/28 , A61P37/08 , C07D401/12 , C07D409/14
CPC分类号： C07D409/14 , C07D401/12
摘要： A compound which is a pyrimidinylamino derivative of piperidine of formula (I) ##STR1## in which: X is a (CH.sub.2).sub.2, CH.dbd.CH or CH.sub.2 --CO group;Y is a CH.dbd.CH gruop or sulphur;n is 2, 3 or 4;R.sub.1 is hydrogen or a halogen;R.sub.2 is hydrogen or a (C.sub.1-4) alkyl group; andR.sub.3 is hydrogen or a hydroxy group;or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：式（I）哌啶的嘧啶基氨基衍生物的化合物其中：X为（CH 2）2，CH = CH或CH 2 -CO基; Y是CH = CH 3或硫; n为2,3或4; R1是氢或卤素; R2是氢或（C1-4）烷基; 并且R 3是氢或羟基; 或其药学上可接受的酸加成盐。

6. 发明授权

US4820710A Benzimidazole derivatives and pharmaceutical compositions containing them 失效
标题翻译：苯并咪唑衍生物和含有它们的药物组合物
公开(公告)号：US4820710A
公开(公告)日：1989-04-11
申请号：US906279
申请日：1986-09-10
申请人： Philippe Manoury , Jean Binet , Gerard Defosse
发明人： Philippe Manoury , Jean Binet , Gerard Defosse
IPC分类号： A61K31/415 , A61K31/44 , A61K31/505 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D239/04
CPC分类号： C07D401/14
摘要： Benzimidazole derivatives corresponding to the formula (1) ##STR1## in which X is CH or N,R.sub.1 is either a hydrogen atom, or a benzyl radical which can bear 1 to 3 substituents chosen from halogen atoms and trifluoromethyl, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, cyano, methylthio, methylsulphinyl and methylsulphonyl radicals, or a methyl radical bearing a heterocyclic substituent in which the heterocyclic system can be a pyridyl, thienyl or furyl radical and can bear one or more substituents, R.sub.2 is a hydrogen atom or a (C.sub.1-4)alkyl radical, R.sub.3 is a hydrogen atom or a hydroxy radical, and R.sub.4 is a hydrogen atom or a (C.sub.1-4)alkyl radical, where appropriate, in tautomeric form when R.sub.3 is OH.The compounds may be used in treating allergy and histamine-induced inflammation.
摘要翻译：对应于式（1）的苯并咪唑衍生物其中X是CH或N，R 1是氢原子或可以带有1-3个选自卤素原子和三氟甲基的取代基的苄基，（C1 -4）烷基，（C 1-4）烷氧基，氰基，甲硫基，甲基亚磺酰基和甲基磺酰基，或具有杂环取代基的甲基，其中杂环体系可以是吡啶基，噻吩基或呋喃基，并且可以具有一个或多个取代基，R 2为氢原子或（C 1-4）烷基，R 3为氢原子或羟基，R 4为氢原子或（C 1-4）烷基，当R 3为是OH。该化合物可用于治疗过敏和组胺诱导的炎症。

7. 发明授权

US4711892A Certain 5-nitro-2-furyl derivatives of pyridylpropenoic acid hydrazides which are useful in treating bacterial, fungal, protozoal, parasitic and intestinal infections 失效
标题翻译：可用于治疗细菌，真菌，原生动物，寄生虫和肠道感染的吡啶丙酸酰肼的某些5-硝基-2-呋喃基衍生物
公开(公告)号：US4711892A
公开(公告)日：1987-12-08
申请号：US851113
申请日：1986-04-10
申请人： Philippe Manoury , Daniel Obitz , Michel Peynot
发明人： Philippe Manoury , Daniel Obitz , Michel Peynot
IPC分类号： A61K31/44 , A61K31/443 , A61P31/04 , A61P33/02 , C07D405/12
CPC分类号： C07D405/12
摘要： Nitrofuran derivatives corresponding to the formula (I). ##STR1## in which m is 0 or 1R is H or (C.sub.1-4)alkoxy are useful in treating bacterial, fungal, parasitic or protozan infections.
摘要翻译：对应于式（I）的硝基呋喃衍生物。其中m为0或1，R为H或（C1-4）烷氧基，可用于治疗细菌，真菌，寄生虫或原生动物感染。

8. 发明授权

US4267328A 1-Phenylpiperazines 失效
标题翻译： 1-苯基哌嗪
公开(公告)号：US4267328A
公开(公告)日：1981-05-12
申请号：US61245
申请日：1979-07-27
申请人： Henry Najer , Philippe Manoury
发明人： Henry Najer , Philippe Manoury
IPC分类号： C07D295/088 , C07D295/096 , C07D461/00 , C07D471/14 , C07D295/06 , A01N43/60
CPC分类号： C07D295/096 , C07D295/088 , C07D461/00 , C07D471/14
摘要： Phenylpiperazine derivatives having the general formula (I) ##STR1## in which R.sub.1 represents a radical S(O).sub.m R.sub.3, S(O).sub.n CF.sub.3 or ##STR2## in which radicals m is 0, 1 or 2, n is 1 or 2, R.sub.3 is an alkyl radical having 1 to 10 carbon atoms and R.sub.4 and R.sub.5 independently represent a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms, or the N atom, R.sub.4 and R.sub.5 together form a heterocyclic ring, which can contain another hetero-atom, and R.sub.2 represents a hydrogen atom, the radical CH.sub.2 --CH.sub.2 --OH or a radical of formula CH.sub.2 --CH.sub.2 --O--COR.sub.6, CH.sub.2 --CH.sub.2 --O--CONHR.sub.6 or CH.sub.2 --CH.sub.2 --O--R.sub.6 in which radicals R.sub.6 being an alkyl radical having 1 to 6 carbon atoms and their pharmaceutically acceptable acid addition salts are useful psychotropic agents and analgesics. Compounds in which R.sub.1 is --SCH.sub.3 and simultaneously R.sub.2 is H are not part of the invention. These derivatives can be prepared by reacting an aniline derivative of formula ##STR3## with a compound of formula ##STR4## in which X represents a halogen atom or OH, alkyl--SO.sub.3 or aryl--SO.sub.3 group or the two X symbols together represent a divalent oxygen atom, thereby completing a morpholine ring.
摘要翻译：具有通式（I）的化合物（I）其中R 1表示基团S（O）m R 3，S（O）n CF 3或者其中基团m为0,1或2的基团，n为1 或2，R3是具有1-10个碳原子的烷基，R4和R5独立地表示氢原子或具有1至4个碳原子的烷基，或者N原子，R4和R5一起形成杂环，其可以含有另一个杂原子，R 2表示氢原子，基团CH 2 -CH 2 -OH或式CH 2 -CH 2 -O-COR 6，CH 2 -CH 2 -O-CONHR 6或CH 2 -CH 2 -O-R 6的基团，其中基团R6是具有1至6个碳原子的烷基，其药学上可接受的酸加成盐是有用的精神药物和镇痛药。其中R 1为-SCH 3且同时为R 2的化合物不是本发明的一部分。这些衍生物可以通过使式（I）的苯胺衍生物与其中X表示卤素原子或OH，烷基-SO 3或芳基-SO 3基团的式（III）化合物或式 X符号一起表示二价氧原子，从而完成吗啉环。

9. 发明授权

US5229392A 2-aminopyrimidine-4-carboxamide derivatives, their preparaton and their application in therapy 失效
标题翻译： 2-氨基嘧啶-4-羧酰胺衍生物及其制剂及其在治疗中的应用
公开(公告)号：US5229392A
公开(公告)日：1993-07-20
申请号：US872028
申请日：1992-04-23
申请人： Pascal George , Philippe Manoury , Michel Mangane , Jean-Pierre Merly
发明人： Pascal George , Philippe Manoury , Michel Mangane , Jean-Pierre Merly
IPC分类号： A61K31/505 , A61P13/02 , A61P15/00 , A61P43/00 , C07D239/42
CPC分类号： C07D239/42
摘要： A compound which is a 2-aminopyrimidine-4-carboxamide derivative represented by general formula (I) ##STR1## in which m represents 2 or 3,n represents 2 or 3,R.sub.1 represents hydrogen or methyl, andX represents a substituent selected from the group consisting of hydrogen, fluorine, chlorine, methoxy, ethoxy, methyl and 1-methylethyl, with the proviso that more than one substituent X may be present in which case each X may be the same or different, or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：作为通式（I）表示的2-氨基嘧啶-4-甲酰胺衍生物的化合物，其中m表示2或3，n表示2或3，R 1表示氢或甲基，X表示选自氢，氟，氯，甲氧基，乙氧基，甲基和1-甲基乙基的取代基，条件是可以存在多于一个取代基X，在这种情况下，每个X可以相同或不同，或药学上其可接受的酸加成盐。

10. 发明授权

US5010079A Indolone derivatives, their preparation and their application in therapy 失效
标题翻译：吲哚酮衍生物，其制备及其在治疗中的应用
公开(公告)号：US5010079A
公开(公告)日：1991-04-23
申请号：US388373
申请日：1989-08-02
申请人： Philippe Manoury , Jean Binet , Daniel Obitz , Gerard Defosse , Elisabeth Dewitte , Corinne Veronique
发明人： Philippe Manoury , Jean Binet , Daniel Obitz , Gerard Defosse , Elisabeth Dewitte , Corinne Veronique
IPC分类号： A61K31/495 , A61P43/00 , C07D209/34 , C07D401/12
CPC分类号： C07D401/12 , C07D209/34
摘要： An indolone derivative is useful for the treatment of anxiety, depression and schizophrenia and is a 5HT.sub.1A agonist and 5HT.sub.2 antagonist, which is a compound of formula (I): ##STR1## in which R.sub.1 is a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical,R.sub.2 is a hydrogen atom or a (C.sub.1-4)alkyl radical,R.sub.3 is a hydrogen atom, a (C.sub.1-4)alkyl radical or an S-(C.sub.1-4) alkyl radical; andR.sub.4 is a phenyl, chlorophenyl, naphthyl, 7-methoxy-1-naphthyl, 6-methoxy-1-indanyl, 2-methoxy-6-pyridyl, 3-methoxy-2-pyridyl, isoquinolyl, 7-methoxy-1-isoquinolyl, 7-methoxy-1,2,3,4-tetrahydro-1-naphthyl or 7-fluoro-1-naphthyl radical;or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：吲哚酮衍生物可用于治疗焦虑，抑郁和精神分裂症，并且是5HT1A激动剂和5HT2拮抗剂，其为式（I）的化合物：其中R 1为氢或卤素原子或（C1- 4）烷基，R 2是氢原子或（C 1-4）烷基，R 3是氢原子，（C 1-4）烷基或S-（C 1-4）烷基; 并且R 4是苯基，氯苯基，萘基，7-甲氧基-1-萘基，6-甲氧基-1-二氢化茚基，2-甲氧基-6-吡啶基，3-甲氧基-2-吡啶基，异喹啉基，7-甲氧基-1- 异喹啉基，7-甲氧基-1,2,3,4-四氢-1-萘基或7-氟-1-萘基; 或其药学上可接受的酸加成盐。

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