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1. 发明授权

US5652248A Method of preventing peripheral neuropathies induced by anticancer agents 失效
标题翻译：防止由抗癌剂引起的周围神经病变的方法
公开(公告)号：US5652248A
公开(公告)日：1997-07-29
申请号：US327589
申请日：1994-10-24
申请人： Delphine Lekieffre , Jesus Benavides , Bernard Scatton , Pascal George
发明人： Delphine Lekieffre , Jesus Benavides , Bernard Scatton , Pascal George
IPC分类号： C07D211/20 , A61K31/445 , A61P25/02 , A61K31/335 , A61K31/44 , A61K33/24
CPC分类号： A61K31/445
摘要： Eliprodil, or an enantiomer thereof, is indicated for combined administration with anticancer agents in order to prevent peripheral neuropathies induced by administration of the anticancer agents.
摘要翻译： Eliprodil或其对映异构体用于与抗癌剂联合施用以防止通过施用抗癌剂诱导的周围神经病变。

2. 发明授权

US5543421A Method of treatment of peripheral neuropathies and central neurodegenerative diseases 失效
标题翻译：周围神经病变和中枢性神经退行性疾病的治疗方法
公开(公告)号：US5543421A
公开(公告)日：1996-08-06
申请号：US327595
申请日：1994-10-24
申请人： J esus Benavides , Badia Ferzaz , Pascal George , Bernard Scatton
发明人： J esus Benavides , Badia Ferzaz , Pascal George , Bernard Scatton
IPC分类号： C07D211/14 , A61K31/445 , A61P9/10 , A61P25/00 , A61P25/02
CPC分类号： A61K31/445
摘要： Ifenprodil and its enantiomers are disclosed for the preparation of medicines useful for the treatment of peripheral neuropathies and chronic neurodegenerative diseases of the central nervous system.
摘要翻译：公开了伊芬醌及其对映异构体用于制备可用于治疗中枢神经系统的周围神经病和慢性神经变性疾病的药物。

3. 发明授权

US5330985A 2-amino-N- [[4-(aminocarbonyl)pyrimidin-2-yl]amino]-alkyl]pyrimidine-4-carboxamide derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译： 2-氨基-N - [[4-（氨基羰基）嘧啶-2-基]氨基] - 烷基]嘧啶-4-甲酰胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5330985A
公开(公告)日：1994-07-19
申请号：US84493
申请日：1993-07-01
申请人： Pascal George , Benoit Marabout , Jacques Froissant , Jean Pierre Merly
发明人： Pascal George , Benoit Marabout , Jacques Froissant , Jean Pierre Merly
IPC分类号： A61K31/505 , A61K9/08 , A61K9/20 , A61K31/506 , A61P13/02 , A61P13/08 , A61P15/00 , A61P43/00 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/495 , A61K31/50 , C07D403/02 , C07D403/06
CPC分类号： C07D239/42 , C07D401/14
摘要： A compound which is a pyrimidine-4-carboxamide derivative of the general formula (I) ##STR1## in which n is 0 or 1, m is 0 or 1,R.sub.1 represents a methyl group whenR.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), orR.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a 4-phenoxypiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), a phenoxymethylpiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 C.sub.1 -C.sub.4 alkyl groups) or a 4-phenylpiperazin-1-yl group (in which the phenyl group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), and R.sub.3 represents a hydrogen atom or only when n is 1 a hydroxyl group or a methoxy group, or is an addition salt thereof with an acid, is useful as an .alpha.-adrenergic antagonist.
摘要翻译：作为通式（I）的嘧啶-4-甲酰胺衍生物的化合物，其中n为0或1，m为0或1，当R 2表示苯氧基（C 1 -C 4）烷基（其中苯氧基任选地带有1或2个选自卤素原子和甲氧基的取代基），或者R 1和R 2与它们所连接的氮原子一起形成4-苯氧基哌啶-1 （其中苯氧基任选地带有1或2个选自卤素原子和甲氧基的取代基），苯氧基甲基哌啶-1-基（其中苯氧基任选地带有1或2个C 1 -C 4烷基）或 4-苯基哌嗪-1-基（其中苯基任选地带有1或2个选自卤素原子和甲氧基的取代基），并且R 3表示氢原子或仅当n为1时为羟基或甲氧基，或是其与酸的加成盐，可用作α-肾上腺素能拮抗剂。

4. 发明授权

US5244901A 4-pyrimidinecarboxamide derivatives, their preparation and their application in therapy 失效
标题翻译： 4-PYRIMIDINECARBOXAMIDE衍生物，其制备及其在治疗中的应用
公开(公告)号：US5244901A
公开(公告)日：1993-09-14
申请号：US903705
申请日：1992-06-26
申请人： Pascal George , Jacques Froissant , Arlette Tixidre
发明人： Pascal George , Jacques Froissant , Arlette Tixidre
IPC分类号： A61K31/505 , A61K31/506 , A61P13/00 , A61P13/02 , A61P13/08 , A61P15/00 , C07D231/42 , C07D239/42 , C07D295/08 , C07D403/12
CPC分类号： C07D239/42
摘要： The present invention provides a compound which is a 4-pyrimidinecarboxamide derivative of general formula (I) ##STR1## in which X represents one or more substituents independently chosen from fluorine, chlorine, methoxy and cyclopropyl,R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, andR.sub.2 represents a hydrogen atom or a methyl group, or a pharmaceutically acceptable acid addition salt thereof; their preparation and their application in therapy.
摘要翻译：本发明提供了一种化合物，其是通式（I）的4-嘧啶甲酰胺衍生物，其中X表示一个或多个独立地选自氟，氯，甲氧基和环丙基的取代基，R 1表示氢原子或 C1-C3烷基，R2表示氢原子或甲基，或其药学上可接受的酸加成盐; 其准备及其在治疗中的应用。

5. 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。

6. 发明授权

US4990506A 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivatives and their application in therapy 失效
标题翻译： 3-（酰氨基甲基）咪唑并[1,2-a]吡啶衍生物及其在治疗中的应用
公开(公告)号：US4990506A
公开(公告)日：1991-02-05
申请号：US425870
申请日：1989-10-24
申请人： Pascal George , Claudie Giron , Jacques Froissant
发明人： Pascal George , Claudie Giron , Jacques Froissant
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl;R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl:or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.5 denotes C.sub.2 -C.sub.6 alkyl; or dialkylamino of formula --NR.sub.6 R.sub.7 in which R.sub.6 and R.sub.7 independently denote C.sub.2 -C.sub.6 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--: and Y denotes hydrogen; halogen; methyl; trifluoromethyl; optionally esterified carboxy of formula --COOR.sub.8 in which R.sub.8 denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.9 R.sub.10 in which R.sub.9 and R.sub.10 independently hydrogen or C.sub.1 -C.sub.4 alkyl; or optionally mono- or dialkylated amino of formula --NR.sub.11 R.sub.12 in which R.sub.11 and R.sub.12 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl: with the exclusion of compounds in which X denotes halogen; alkyl; or methylthio and Y denotes hydrogen; halogen; or methyl:or a pharmacologically acceptable acid addition salt is useful in therapy.
摘要翻译：化合物，其是式（I）的3-（酰氨基甲基）咪唑并[1,2-a]吡啶衍生物，其中R1表示氢; 直链或支链C 1 -C 4烷基; 或苄基; R2表示直链或支链C 1 -C 6烷基; 环己基三氯甲基 1-丙烯基; 烯丙基苯基; 4-氯苯基; 或苄基：或R 1和R 2一起表示C 3 -C 5脂族链：X表示卤素; C1-C3烷基; 甲硫基三氟甲基任选的式-COOR的酯化羧基，其中R表示氢或C 1 -C 6烷基; 氰基; 任选的式-CONR 3 R 4的单或二烷基化氨基羰基，其中R 3和R 4独立地表示氢或C 1 -C 4烷基或一起表示式 - （CH 2）2 -Z-（CH 2）2 - 的链，其中Z表示直接键，氧，硫或式-CH 2 - ， - NH-或-N（C 1 -C 4烷基） - 的二价基团。式NHR5的烷基氨基，其中R 5表示C 2 -C 6烷基; 或式-NR6R7的二烷基氨基，其中R6和R7独立地表示C2-C6烷基或一起表示式 - （CH2）2-Z-（CH2）2-的链，其中Z表示直接键，氧，硫或式为-CH 2 - ， - NH-或-N（C 1 -C 4烷基） - 的二价基团，Y表示氢; 卤素; 甲基; 三氟甲基任选的式-COOR 8的酯化羧基，其中R 8表示氢或C 1 -C 6烷基; 氰基; 任选的式-CONR 9 R 10的单或二烷基化氨基羰基，其中R 9和R 10独立地是氢或C 1 -C 4烷基; 或任选的式-NR 11 R 12的单或二烷基化氨基，其中R 11和R 12独立地表示氢或C 1 -C 4烷基：排除其中X表示卤素的化合物; 烷基; 或甲硫基，Y表示氢; 卤素; 或甲基：或药理学上可接受的酸加成盐可用于治疗。

7. 发明授权

US4885302A 2-((4-Piperidyl)methyl)-1,2,3,4-tetrahydroisoquinoline derivatives, their preparation and their application in therapy 失效
标题翻译： 2 - （（4-哌啶基）甲基）-1,2,3,4-四氢异喹啉衍生物，其制备及其在治疗中的应用
公开(公告)号：US4885302A
公开(公告)日：1989-12-05
申请号：US228748
申请日：1988-08-05
申请人： Pascal George , Mireille Sevrin , Christian Maloizel
发明人： Pascal George , Mireille Sevrin , Christian Maloizel
IPC分类号： A61K31/47 , A61K31/475 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A compound of formula (I) ##STR1## in which R is (a) a hydrogen atom;(b) a linear or branched (C.sub.1 -C.sub.6) alkyl group; an allyl group; a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a phenylmethyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, amino, dimethylamino, cyano, aminocarbonyl, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 2-phenylethyl group; a 3-phenylpropyl group; a 3-phenyl-2-propenyl group; a phenylcarbonylmethyl group; a naphthylmethyl group; a pyridylmethyl group; a furylmethyl group; or a thienylmethyl group; or(c) a linear or branched (C.sub.2 -C.sub.6) alkanoyl group; a cycloalkylcarbonyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a trifluoroacetyl group; a phenyl-carbonyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 1-oxo-3-phenyl-2-propenyl group; a naphthylcarbonyl group; a pyridylcarbonyl group; a furylcarbonyl group; a thienylcarbonyl group; a (2-indolyl)-carbonyl group; or a (5-indolyl)carbonyl group; or a pharmacologically acceptable acid addition salt thereof.
摘要翻译：式（I）化合物其中R为（a）氢原子; （b）直链或支链（C1-C6）烷基; 烯丙基; 环烷基甲基，其中环烷基部分具有3至6个碳原子; 未取代或被一至三个选自卤素原子和三氟甲基，硝基，氨基，二甲基氨基，氰基，氨基羰基，直链或支链（C 1 -C 3）烷基，直链或支链（C 1 -C 3）烷氧基和直链或支链支链（C1-C3）烷硫基; 2-苯基乙基; 3-苯基丙基; 3-苯基-2-丙烯基; 苯基羰基甲基; 萘基甲基; 吡啶基甲基; 呋喃甲基; 或噻吩甲基; 或（c）直链或支链（C 2 -C 6）烷酰基; 环烷基部分具有3至6个碳原子的环烷基羰基; 三氟乙酰基; 直链或支链（C1-C3）烷基，直链或支链（C1-C3）烷氧基和直链或支链的（C1-C3）烷基，烷硫基; 1-氧代-3-苯基-2-丙烯基; 萘基羰基; 吡啶基羰基; 呋喃基羰基; 噻吩基羰基; （2-吲哚基） - 羰基; 或（5-吲哚基）羰基; 或其药理学上可接受的酸加成盐。

8. 发明授权

US4810711A 1-(acylaminomethyl)imidazo(1,2-A)quinoline derivatives, their preparation and their application in therapy 失效
标题翻译： 1-（酰氨基甲基）咪唑（1,2-A）喹啉衍生物，其制备及其在治疗中的应用
公开(公告)号：US4810711A
公开(公告)日：1989-03-07
申请号：US5823
申请日：1987-01-21
申请人： Pascal George , Daniele De Peretti
发明人： Pascal George , Daniele De Peretti
IPC分类号： A61K31/47 , A61P1/04 , A61P25/04 , A61P25/08 , A61P25/20 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： A compound which is a 1-acylaminomethylimidazo[1,2-a]quinoline of formula (I) ##STR1## in which A and B both denote hydrogen or together denote a direct carbon-carbon bond,X denotes hydrogen or a halogen or a (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.1-4)alkylthio, methylsulphonyl, amino, (C.sub.1-4)alkylamino, di(C.sub.1-4)alkylamino, nitro or trifluormethyl group,Y denotes hydrogen or a halogen or a methyl group and is attached to the aryl ring at position 6, 7 or 8,R.sub.1 denotes hydrogen or a (C.sub.1-4)alkyl group, andR.sub.2 denotes a (C.sub.1-6)alkyl group, or a pharmaceutically acceptable acid addition salt thereof is useful in therapy.
摘要翻译：化合物，其为A和B均表示氢或一起表示直接碳 - 碳键的式（I）的1-酰基氨基甲基咪唑并[1,2-a]喹啉，X表示氢或卤素或（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷硫基，甲基磺酰基，氨基，（C 1-4）烷基氨基，二（C 1-4）烷基氨基，硝基或三氟甲基，Y表示氢或卤素或甲基，并且在6,7或8位连接到芳环，R 1表示氢或（C 1-4）烷基，R 2表示（C 1-6）烷基，或其药学上可接受的酸加成盐可用于治疗。

9. 发明授权

US4460592A 6-Methyl-2-(4-methylthiophenyl)-i midazo[1,2-a]-pyridine-3-N,N-dimethylacetamide 失效
标题翻译： 6-甲基-2-（4-甲硫基苯基） - 咪唑并[1,2-a] - 吡啶-3-N，N-二甲基乙酰胺
公开(公告)号：US4460592A
公开(公告)日：1984-07-17
申请号：US465605
申请日：1983-02-10
申请人： Jean-Pierre Kaplan , Pascal George
发明人： Jean-Pierre Kaplan , Pascal George
IPC分类号： A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P9/00 , A61P25/08 , A61P25/20 , A61P25/28 , C07D471/04 , C07D487/02
CPC分类号： C07D471/04
摘要： 6-Methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylacetamide is provided, preferably in the form of a pharmaceutically acceptable salt, for example, 6-methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylacetamide methylsulfate. Also provided is a method of providing a patient with a hypnotic effect which comprises administering to said patient a hynotically effective amount of the compound 6-methyl-2-(4-methylthiophenyl)-imidazo[1,2-a]-pyridine-3-N,N-dimethylacetamide or a pharmaceutically acceptable salt thereof.
摘要翻译：提供6-甲基-2-（4-甲硫基苯基） - 咪唑并[1,2-a] - 吡啶-3-N，N-二甲基乙酰胺，优选为药学上可接受的盐，例如6-甲基 -2-（4-甲硫基苯基） - 咪唑并[1,2-a] - 吡啶-3-N，N-二甲基乙酰胺甲基硫酸盐。还提供了向患者提供催眠作用的方法，其包括向所述患者施用有机体有效量的化合物6-甲基-2-（4-甲硫基苯基） - 咪唑并[1,2-a] - 吡啶-3 -N，N-二甲基乙酰胺或其药学上可接受的盐。

10. 发明授权

US07294632B2 Substituted 8′-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one and 8′-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one derivatives 失效
标题翻译：取代的8'-吡啶基 - 二氢螺 - [环烷基] - 嘧啶并[1,2-a]嘧啶-6-酮和8'-嘧啶基 - 二氢螺 - [环烷基] - 嘧啶并[1,2-a]嘧啶-6-酮衍生品
公开(公告)号：US07294632B2
公开(公告)日：2007-11-13
申请号：US11220999
申请日：2005-09-07
申请人： Pascal George , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
发明人： Pascal George , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
IPC分类号： A61P25/28 , C07D243/04 , C07D487/20
CPC分类号： C07D487/10
摘要： The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
摘要翻译：本发明涉及由式（I）表示的二氢螺环 - [环烷基] - 嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，m，n，p和q如本文所述。本发明还涉及包含所述衍生物或其盐作为活性成分的药物，所述活性成分用于预防和/或治疗由GSK3β如阿尔茨海默病异常活动引起的神经变性疾病。

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