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1. 发明授权

US5192775A New aminomethylpiperidine compounds 失效
标题翻译：新的氨基哌啶化合物
公开(公告)号：US5192775A
公开(公告)日：1993-03-09
申请号：US661494
申请日：1991-02-26
申请人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
发明人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
IPC分类号： A61K31/35 , A61K31/34 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/445 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00 , C07D235/30 , C07D263/58 , C07D277/82 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
CPC分类号： C07D401/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention relates to compounds of general formula (I). ##STR1## in which X represents an atom of sulfur or oxygen, or a substituted or unsubstituted amino group;R represents a hydrogen atom or any one of groups A, B, C, D, E, F, or G;R' represents a hydrogen atom, an alkyl group or any one of groups A, B, C, D, E or F, with R'=H when R=G;or R and R' form, with the nitrogen atom to which they are attached, an optionally substituted piperazine ring. Medicaments.
摘要翻译：本发明涉及通式（I）的化合物。（I）其中X表示硫或氧原子，或取代或未取代的氨基; R代表氢原子或A，B，C，D，E，F或G组之一; R'表示氢原子，烷基或基团A，B，C，D，E或F中的任一个，当R = G时，R'= H; 或R和R'与它们所连接的氮原子一起形成任选取代的哌嗪环。药剂

2. 发明授权

US5229399A Aminomethylpiperidine compounds 失效
标题翻译：氨基甲基哌啶化合物
公开(公告)号：US5229399A
公开(公告)日：1993-07-20
申请号：US964423
申请日：1992-10-21
申请人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
发明人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
IPC分类号： A61K31/35 , A61K31/34 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/445 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00 , C07D235/30 , C07D263/58 , C07D277/82 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
CPC分类号： C07D401/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention relates to compounds of general formula (I). ##STR1## in which X represents an atom of sulfur or oxygen, or a substituted or unsubstituted amino group;R represents a hydrogen atom or any one of groups A, B, C, D, E, F or G;R' represents a hydrogen atom, an alkyl group or any one of groups A, B, C, D, E or F, with R'=H when R=G; or R and R' form, with the nitrogen atom to which they are attached, an optionally substituted piperazine ring.Medicaments.
摘要翻译：本发明涉及通式（I）的化合物。（I）其中X表示硫或氧原子，或取代或未取代的氨基; R代表氢原子或A，B，C，D，E，F或G组之一; R'表示氢原子，烷基或基团A，B，C，D，E或F中的任一个，当R = G时，R'= H; 或R和R'与它们所连接的氮原子一起形成任选取代的哌嗪环。药剂

3. 发明授权

US5229398A Aminomethylpiperidine compounds 失效
标题翻译：氨基甲基哌啶化合物
公开(公告)号：US5229398A
公开(公告)日：1993-07-20
申请号：US964416
申请日：1992-10-21
申请人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
发明人： Charles Malen , Guillaume de Nanteuil , Francis Colpaert
IPC分类号： C07D401/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
CPC分类号： C07D401/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The invention relates to compounds of general formula (I). ##STR1## in which X represents an atom of sulfur or oxygen, or a substituted or unsubstituted amino group;R represents a hydrogen atom or any one of groups A, B, C, D, E, F or G;R' represents a hydrogen atom, an alkyl group or any one of groups A, B, C, D, E or F, with R'=H when R=G;or R and R' form, with the nitrogen atom to which they are attached, an optionally substituted piperazine ring.
摘要翻译：本发明涉及通式（I）的化合物。（I）其中X表示硫或氧原子，或取代或未取代的氨基; R代表氢原子或A，B，C，D，E，F或G组之一; R'表示氢原子，烷基或基团A，B，C，D，E或F中的任一个，当R = G时，R'= H; 或R和R'与它们所连接的氮原子一起形成任选取代的哌嗪环。

4. 发明授权

US08669250B2 Derivatives of aryl-{4-halogeno-4-[aminomethyl]-piperidin-1-yl}-methanone, their method of preparation and their use as medicinal products 有权
标题翻译：芳基 - {4-卤代-4- [氨基甲基] - 哌啶-1-基} - 甲酮的衍生物，其制备方法及其作为药用物质的用途
公开(公告)号：US08669250B2
公开(公告)日：2014-03-11
申请号：US13376331
申请日：2010-06-03
申请人： Bernard Vacher , Francis Colpaert , Jean-Louis Maurel
发明人： Bernard Vacher , Francis Colpaert , Jean-Louis Maurel
IPC分类号： C07D265/36 , C07D413/12 , A61K31/538
CPC分类号： C07D265/36 , C07D413/12
摘要： The present invention concerns compounds of general formula (1) (I) wherein R1 is: —a hydrogen atom, or a halogen, —a straight or branched C1-C6 alkyl group or a C1-C3 fluoroalkyl group, —a straight or branched C1-C6 alcoxy group, a carbamyl group, N-substituted or not by one or two, straight or branched C1-C3 alkyl groups, or —a cyano group (CN) R2 is: —a hydrogen atom or a straight or branched C1-C6 alkyl group, HaI1, Hal2 and Hal3 are: —a halogen their addition salts and the hydrates of addition salts with pharmaceutically acceptable mineral acids or organic acids, and their enantiomer forms.
摘要翻译：本发明涉及通式（1）（I）的化合物，其中R 1为： - 氢原子或卤素， - 直链或支链C 1 -C 6烷基或C 1 -C 3氟代烷基， - 直链或支链 C1-C6烷氧基，氨基甲酰基，N-取代或不具有一个或两个直链或支链C1-C3烷基或氰基（CN）R2是： - 氢原子或直链或支链C1 -C 1-6烷基，HaI1，Hal2和Hal3是：卤素，它们的加成盐和与药学上可接受的无机酸或有机酸的加成盐的水合物及其对映体形式。

5. 发明授权

US5948806A Treatment of Parkinson's disease with (+)2-(ethyl-2,3-dihydrobenzofuranyl)-2-Imidazoline (dexefaroxan or (+) efaroxan) 失效
标题翻译：用（+）2-（乙基-2,3-二氢苯并呋喃基）-2-咪唑啉（德法洛沙或（+）依法雄）治疗帕金森氏病
公开(公告)号：US5948806A
公开(公告)日：1999-09-07
申请号：US825414
申请日：1997-03-26
申请人： Francis Colpaert , Michael Briley , Thierry Imbert
发明人： Francis Colpaert , Michael Briley , Thierry Imbert
IPC分类号： C07D405/04 , A61K31/415 , A61K31/4178 , A61P25/00 , A61P25/16
CPC分类号： A61K31/415
摘要： The present invention relates to the use of efaroxan and its derivatives for the preparation of a medicinal product intended for the treatment of Parkinson's disease.
摘要翻译：本发明涉及依法鲁昔康及其衍生物在制备用于治疗帕金森病的药物中的应用。

6. 发明授权

US5292761A Piperidine, tetrahydropyridine and pyrrolidine compounds 失效
标题翻译：哌啶，四氢吡啶和吡咯烷化合物
公开(公告)号：US5292761A
公开(公告)日：1994-03-08
申请号：US972120
申请日：1992-11-05
申请人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
发明人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/47 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D207/06 , C07D207/08 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/70 , C07D295/13 , C07D295/185 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06
CPC分类号： C07D295/185 , C07D207/20 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/70 , C07D295/13 , C07D401/04 , C07D405/04
摘要： The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.Ch-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.4 represents a hydrogen atom, a halogen atom, an alkyl radical having 1 to 6 carbon atoms, or an alkoxy radical having 1 to 6 carbon atoms , and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, and medicaments containing the same.
摘要翻译：本发明涉及式I化合物：其中R 1表示萘基，二氢萘基，四氢萘基，喹啉基或1,4-苯并二恶烷基，A表示单键，双键，亚甲基，式z1的基团：-CH =（z1）或式z2的基团：= Ch-（z2）环B表示哌啶基，吡咯烷基或1,2,3,6 并且R 2表示：氢原子，苄基或具有1至6个碳原子的烷基，条件是在这些情况之一中，R 1不同于萘基（y1），二氢萘基（y2）或四氢萘基（y3）基团，B不是哌啶基或具有1-6个碳原子的氨基烷基，具有1至6个碳原子的氰基烷基或式w1的基团：其中其中 n为1-6，R 4表示氢原子，卤素原子，碳原子数1〜6的烷基或烷氧基其具有1至6个碳原子，以及它们与药学上可接受的无机或有机酸的加成盐，以及含有它们的药物。

7. 发明授权

US5166156A Naphthyl piperazines useful as 5-HT.sub.1A receptor ligands 失效
标题翻译：可用作5-HT1A受体配体的萘基哌嗪
公开(公告)号：US5166156A
公开(公告)日：1992-11-24
申请号：US752065
申请日：1991-08-29
申请人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
发明人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
IPC分类号： C07D209/48 , C07D213/82 , C07D221/20 , C07D295/13 , C07D333/38 , C07D487/04
CPC分类号： C07D209/48 , C07D213/82 , C07D221/20 , C07D295/13 , C07D333/38 , C07D487/04
摘要： Compounds of formula I: ##STR1## in which: n=1-4,R represents hydrogen, halogen, alkyl, hydroxyl or alkoxy, R.sub.1 represents a radical --NHCOR2 (A.sub.1); (in which R.sub.2 represents alkyl, cycloalkyl, phenyl optionally substituted, -O-alkyl, 3-pyridyl, 2-pyrrolyl, quinolyl, 1-isoquinolyl, 2-thienyl or 3-indolyl); a radical of -NHSO2R3 (A.sub.2) (in which R.sub.3 represents alkyl, cycloalkyl or phenyl optionally substituted); a radical --NHCONHR4 (A.sub.3) (in which R.sub.4 represents alkyl or phenyl-optionally substituted); a phthalimido radical (A.sub.4); an o-sulfobenzoic imido radical (A.sub.5); a di(benzoyl)amino radical (A.sub.6) optionally substituted; a radical of formula A.sub.7 : ##STR2## (in which R.sub.5 represents carbamoyl, cyano, carboxy or alkoxycarbonyl); or a radical of formula A.sub.8 : ##STR3## their stereoisomers and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, are disolosed to be useful as 5-HT.sub.1A receptor ligands and accordingly as the active principle in medicinal products containing the same.
摘要翻译：式I化合物：其中：n = 1-4，R表示氢，卤素，烷基，羟基或烷氧基，R 1表示基团-NHCOR 2（A1）; （其中R2代表烷基，环烷基，任选取代的苯基，-O-烷基，3-吡啶基，2-吡咯基，喹啉基，1-异喹啉基，2-噻吩基或3-吲哚基）。 -NHSO 2 R 3（A2）（其中R 3表示烷基，环烷基或任选取代的苯基）的基团; 基团-NHCONHR 4（A3）（其中R 4表示烷基或苯基 - 任选取代的）; 苯二甲酰亚胺基（A4）; 邻磺基苯甲酰亚胺基（A5）; 任选取代的二（苯甲酰基）氨基（A6）（A7）（其中R5表示氨基甲酰基，氰基，羧基或烷氧基羰基）的式A7的基团：或式A8的基团：其具有药学上可接受的无机酸或有机酸的立体异构体及其加成盐与式（A8）化合物被解离，可用作5-HT 1A受体配体，因此作为含有一样。

8. 发明授权

US5143916A Naphthylpiperazines useful as 5-HT.sub.1A receptor ligands 失效
标题翻译：萘普生可用作5-HT1A受体配体
公开(公告)号：US5143916A
公开(公告)日：1992-09-01
申请号：US629824
申请日：1990-12-19
申请人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
发明人： Gilbert Lavielle , Michel Laubie , Francis Colpaert
IPC分类号： A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4406 , A61K31/495 , A61K31/505 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/24 , A61P25/26 , C07D209/48 , C07D213/82 , C07D221/20 , C07D295/08 , C07D295/13 , C07D333/38 , C07D487/04
CPC分类号： C07D209/48 , C07D213/82 , C07D221/20 , C07D295/13 , C07D333/38 , C07D487/04
摘要： Compounds of the formula I: ##STR1## in which: n=1-4,R represents hydrogen, halogen, alkyl, hydroxyl or alkoxy, R.sub.1 represents a radical --NHCOR2 (A.sub.1); (in which R.sub.2 represents alkyl, cycloalkyl, phenyl optionally substituted-, --O-alkyl, 3-pyridyl, 2-pyrrolyl, quinolyl, 1-isoquinolyl, 2-thienyl or 3-indolyl); a radical of --NHS02R3 (A.sub.2) (in which R.sub.3 represents alkyl, cycloalkyl or phenyl optionally substituted); a radical --NHCONHR4 (A.sub.3) (in which R.sub.4 represents alkyl or phenyl-optionally substituted); a phthalimido radical (A.sub.4); an o-sulfobenzoic imido radical (A.sub.5); a di(benzoyl)amino radical (A.sub.6) optionally substituted; a radical of formula A.sub.7 : ##STR2## (in which R.sub.5 represents carbamoyl, cyano, carboxy or alkoxycarbonyl); or a radical of formula A.sub.8 : ##STR3## their stereoisomers and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, are disclosed to be useful as 5-HT.sub.1A receptor ligands and accordingly as the active principle in medicinal products containing the same.
摘要翻译：式I化合物：其中：n = 1-4，R表示氢，卤素，烷基，羟基或烷氧基，R1表示基团-NHCOR2（A1）; （其中R 2表示烷基，环烷基，任选取代的 - ， - O-烷基，3-吡啶基，2-吡咯基，喹啉基，1-异喹啉基，2-噻吩基或3-吲哚基）。 -NHSO 2 R 3（A2）的基团（其中R 3表示烷基，环烷基或任选取代的苯基）; 基团-NHCONHR 4（A3）（其中R 4表示烷基或苯基 - 任选取代的）; 苯二甲酰亚胺基（A4）; 邻磺基苯甲酰亚胺基（A5）; 任选取代的二（苯甲酰基）氨基（A6）（A7）（其中R5表示氨基甲酰基，氰基，羧基或烷氧基羰基）的式A7的基团：或式A8的基团：其具有药学上可接受的无机酸或有机酸的立体异构体及其加成盐的式（A8）可用作5-HT 1A受体配体，因此作为含有一样。

9. 发明授权

US5100902A 1,2-benzisoxazole compounds 失效
标题翻译： 1,2-苯并噻唑化合物
公开(公告)号：US5100902A
公开(公告)日：1992-03-31
申请号：US604789
申请日：1990-10-26
申请人： Jean L. Peglion , Francis Colpaert
发明人： Jean L. Peglion , Francis Colpaert
IPC分类号： A61K31/44 , A61K31/445 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D413/04 , C07D413/06 , C07D413/14 , C07D471/04 , C07D493/04
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , C07D493/04
摘要： Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.2, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, an alkyl radical, an alkoxy radical, a hydroxyl radical, a hydroxyalkyl radical or an alkylthio radical, or together form a methylenedioxy radical or an ethylenedioxy radical, and R.sub.3 represents a hydrogen atom or a linear or branched alkyl radical having 1 to 6 carbon atoms),or a radical of formula C: ##STR3## (in which R.sub.4, R.sub.5 and R.sub.6, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, a hydroxyl radical, an alkyl radical, an alkoxy radical or an alkylthio radical,their optical isomers and their addition salts with a pharmaceutically acceptable organic or inorganic acid.
摘要翻译：式I的化合物（I）其中m表示0至5的整数，n表示1至2的整数，p等于0,1或2，X，Y和Z可以相同或不同的，各自表示氢原子，卤素原子，直链或支链烷基，三氟甲基，烷氧基，烷硫基或羟基，R表示2-苯并呋喃基或2,3-二氢 - 2-苯并呋喃基（每个可以在苯环上取代），2,3,6,7-四氢苯并[1,2-b：4,5-b']二呋喃-2-基， 4-氧代-4H-色烯-2-基（在苯环上任选取代），式A的苯并环丁烯基或式B的茚满基基团：（A）（B）（B）其中R 1和R 2可以相同或不同，各自表示氢原子，卤素原子，三氟甲基，烷基，烷氧基，羟基，羟基烷基或烷硫基，或一起用于（C）（其中R 4，R 5和R 6）的基团，其中R 1，R 2，R 3，R 4，R 5，R 6和R 6独立地选自氢原子或具有1至6个碳原子的直链或支链烷基）其可以相同或不同，各自表示氢原子，卤素原子，三氟甲基，羟基，烷基，烷氧基或烷硫基，它们的光学异构体及其与药学上可接受的有机物的加成盐或无机酸。

10. 发明申请

US20060264471A1 3-(cyclopenten-1-yl)-benzyl-or 3-(cyclopenten-1-yl)-heteroarylmethyl-amine derviatives and use thereof as medicines for treating schizophrenia 有权
标题翻译： 3-（环戊烯-1-基） - 苄基 - 或3-（环戊烯-1-基） - 杂芳基甲基胺的用途及其用作治疗精神分裂症的药物
公开(公告)号：US20060264471A1
公开(公告)日：2006-11-23
申请号：US11494697
申请日：2006-07-28
申请人： Bernard Vacher , Stephane Cuisiat , Wouter Koek , Francis Colpaert
发明人： Bernard Vacher , Stephane Cuisiat , Wouter Koek , Francis Colpaert
IPC分类号： A61K31/4433 , C07D407/02
CPC分类号： C07D405/12 , C07C45/298 , C07C47/548 , C07C47/55 , C07D213/48 , C07D307/86 , C07D307/94
摘要： The invention provides compounds of the formula wherein (a) is a single or double bond; W is CH, CH2, CHCH3, C(CH3)2, C(CH2)2 or C(CH2)3; X is N; and Y is H or F, and salts, hydrates, tautomers, pure enantiomers, and enantiomeric mixtures; and a method of treating schizophrenia comprising administering same.
摘要翻译：本发明提供下式的化合物，其中（a）是单键或双键; W是CH，CH 2，CHCH 3，C（CH 3）2，C（CH

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