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1. 发明授权

US08846676B2 6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof 有权
标题翻译： 6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物及其治疗用途
公开(公告)号：US08846676B2
公开(公告)日：2014-09-30
申请号：US13617678
申请日：2012-09-14
申请人： Antonio Almario Garcia , Mathieu Barrague , Philippe Burnier , Cecile Enguehard-Gueiffier , Zhongli Gao , Pascal George , Alain Gueiffier , Adrien Tak Li , Frederic Peuch , Roy Vaz , Qiuxia Zhao
发明人： Antonio Almario Garcia , Mathieu Barrague , Philippe Burnier , Cecile Enguehard-Gueiffier , Zhongli Gao , Pascal George , Alain Gueiffier , Adrien Tak Li , Frederic Peuch , Roy Vaz , Qiuxia Zhao
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.
摘要翻译：本发明涉及对应于通式（I）的6-环氨基-3-（吡啶-4-基）咪唑并[ⅰ，2-b]哒嗪衍生物：其中R2，R3，R7，R8，A，L和B 如本文所定义。还公开了其制备方法及其治疗用途。

2. 发明授权

US08354405B2 6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof 有权
标题翻译： 6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物及其治疗用途
公开(公告)号：US08354405B2
公开(公告)日：2013-01-15
申请号：US12647059
申请日：2009-12-24
申请人： Antonio Almario Garcia , Matthieu Barrague , Philippe Burnier , Cécile Enguehard , Zhongli Gao , Pascal George , Alain Gueiffier , Adrien Tak Li , Frédéric Puech , Roy Vaz , Qiuxia Zhao
发明人： Antonio Almario Garcia , Matthieu Barrague , Philippe Burnier , Cécile Enguehard , Zhongli Gao , Pascal George , Alain Gueiffier , Adrien Tak Li , Frédéric Puech , Roy Vaz , Qiuxia Zhao
IPC分类号： C07D487/04 , C07D237/00 , C07D413/14 , A61K31/5025 , A61K31/5355 , A61P25/30 , A61P25/00
CPC分类号： C07D487/04
摘要： The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.
摘要翻译：本发明涉及对应于通式（I）的6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物：其中R2，R3，R7，R8，A，L和B 如本文所定义。还公开了其制备方法及其治疗用途。

3. 发明申请

US20130190314A1 DERIVATIVES OF 6-CYCLOAMINO-2-THIENYL-3-(PYRIDIN-4-YL)IMIDAZO[1,2-b]-PYRIDAZINE AND 6-CYCLOAMINO-2-FURANYL-3-(PYRIDIN-4-YL)IMIDAZO[1,2-b]-PYRIDAZINE, PREPARATION AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译： 6-环丙氨基-2-苯基-3-（吡啶-4-基）咪唑并[1,2-b] - 吡啶和6-环丙氨基-2-呋喃-3-基（吡啶-4-基）咪唑并[1 ，2-b] - 吡啶，其制备及其治疗用途
公开(公告)号：US20130190314A1
公开(公告)日：2013-07-25
申请号：US13141006
申请日：2009-12-17
申请人： Yulin Chiang , Cecile Enguehard-Gueiffier , Pascal George , Alaim Gueiffier , Frederic Puech , Mireille Sevrin , Qiuxia Zhao
发明人： Yulin Chiang , Cecile Enguehard-Gueiffier , Pascal George , Alaim Gueiffier , Frederic Puech , Mireille Sevrin , Qiuxia Zhao
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to derivatives of 6-cycloamino-2-thienyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine and 6-cycloamino-2-furanyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine with general formula (I). The invention also relates to a method for the preparation and therapeutic application thereof, in the treatment or prevention of illnesses involving casein kinase 1 epsilon and/or casein kinase 1 delta.
摘要翻译：本发明涉及6-环氨基-2-噻吩基-3-（吡啶-4-基）咪唑并[1,2-b] - 哒嗪和6-环氨基-2-呋喃基-3-（吡啶-4-基））具有通式（I）的咪唑并[1,2-b]哒嗪。本发明还涉及其在治疗或预防涉及酪蛋白激酶1ε和/或酪蛋白激酶1δ的疾病中的制备和治疗应用的方法。

4. 发明申请

US20090088470A1 ALKYL-, ALKENYL- AND ALKYNYLCARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 审中-公开
标题翻译：阿尔茨基，亚苄基和烷基氨基甲酸酯衍生物，其制备及其在治疗中的应用
公开(公告)号：US20090088470A1
公开(公告)日：2009-04-02
申请号：US12328386
申请日：2008-12-04
申请人： Antonio ALMARIO-GARCIA , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
发明人： Antonio ALMARIO-GARCIA , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
IPC分类号： A61K31/27 , A61P25/24 , A61P25/22 , A61P25/28 , A61P25/08 , A61P25/14 , A61P25/16
CPC分类号： C07C271/12 , C07C271/24 , C07C2601/18
摘要： The invention relates to a compound of formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to methods of preparation of compounds of formula (I) as well as to their therapeutic application.
摘要翻译：本发明涉及式（I）化合物：其中R1，R2，R3和R4如本文所定义。本发明还涉及式（I）化合物的制备方法及其治疗应用。

5. 发明授权

US07476756B2 Alkyl-, alkenyl- and alkynylcarbamate derivatives, their preparation and their application in therapeutics 失效
标题翻译：烷基，链烯基和炔基氨基甲酸酯衍生物，其制备及其在治疗中的应用
公开(公告)号：US07476756B2
公开(公告)日：2009-01-13
申请号：US11874959
申请日：2007-10-19
申请人： Antonio Almario-Garcia , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
发明人： Antonio Almario-Garcia , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
IPC分类号： C07C269/04 , C07C271/08 , A61K31/27
CPC分类号： C07C271/12 , C07C271/24 , C07C2601/18
摘要： The invention relates to a compound of formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to methods of preparation of compounds of formula (I) as well as to their therapeutic application.
摘要翻译：本发明涉及式（I）化合物：其中R1，R2，R3和R4如本文所定义。本发明还涉及式（I）化合物的制备方法及其治疗应用。

6. 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。

7. 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。

8. 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。

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

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。

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