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![6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof](/abs-image/US/2013/01/15/US08354405B2/abs.jpg.150x150.jpg)
1.发明授权6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof 有权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。
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![6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof](/abs-image/US/2014/09/30/US08846676B2/abs.jpg.150x150.jpg)
2.发明授权6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof 有权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。
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3.发明申请ALKYL-, ALKENYL- AND ALKYNYLCARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 审中-公开阿尔茨基，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
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。
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4.发明授权Alkyl-, alkenyl- and alkynylcarbamate derivatives, their preparation and their application in therapeutics 失效烷基，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
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。
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5.发明授权2-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydoimidazo{1,2-a}pyrimidin-5(1H)one derivatives 失效2-吡啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-吡啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1H）公开(公告)号：US06974819B2
公开(公告)日：2005-12-13
申请号：US10362850
申请日：2001-08-31
申请人： Antonio Almario Garcia , Thierry Gallet , Adrien Tak Li , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
发明人： Antonio Almario Garcia , Thierry Gallet , Adrien Tak Li , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
IPC分类号： A61K31/519 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/14 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/06 , A61P35/00 , A61P35/02 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： Imidazo[1,2-α]pyrimidinones and pyrimido[1,2-α]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3β activity.
摘要翻译： 咪唑并[1,2-α]嘧啶酮和嘧啶并[1,2-α]嘧啶酮，用于预防和/或治疗由异常GSK3β活性引起的神经变性疾病，如阿尔茨海默病。
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![2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a] pyrimidin-5(1H)one derivatives](/abs-image/US/2009/07/28/US07566720B2/abs.jpg.150x150.jpg)
6.发明授权2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a] pyrimidin-5(1H)one derivatives 失效2-吡啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-吡啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1H）公开(公告)号：US07566720B2
公开(公告)日：2009-07-28
申请号：US11841285
申请日：2007-08-20
申请人： Antonio Almario Garcia , Thierry Gallet , Adrien Tak Li , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
发明人： Antonio Almario Garcia , Thierry Gallet , Adrien Tak Li , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Philippe Yaiche
IPC分类号： A61P25/00 , A61P25/28 , A61P3/04 , C07D471/04 , C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to therapeutic uses of a pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, Y, R1, R2, m and n are as defined herein. Specifically, a medicament comprising the said derivative or a salt thereof as an active ingredient is used for preventive and/or therapeutic treatment of a neurodegenerative diseases caused by abnormal activity of GSK3β such as Alzheimer's disease.
摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐的治疗用途：其中X，Y，R 1，R 2，m和n如本文所定义。 具体地说，包含所述衍生物或其盐作为活性成分的药物用于预防和/或治疗由诸如阿尔茨海默病的GSK3β的异常活性引起的神经变性疾病。
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7.发明授权2-amino-3-(alkyl)-pyrimidone derivatives as GSK3.β.inhibitors 失效2-氨基-3-（烷基） - 嘧啶酮衍生物作为GSK3.beta.抑制剂公开(公告)号：US06844335B2
公开(公告)日：2005-01-18
申请号：US10221598
申请日：2001-03-22
申请人： Antonio Almario Garcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Tak Li , Aya Shoda , Jonathan Reid Frost , Kazutoshi Watanabe
发明人： Antonio Almario Garcia , Ryoichi Ando , Keiichi Arimoto , Fumiaki Uehara , Adrien Tak Li , Aya Shoda , Jonathan Reid Frost , Kazutoshi Watanabe
IPC分类号： A61K31/505 , A61K31/506 , A61P3/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P11/00 , A61P15/00 , A61P17/02 , A61P17/14 , A61P19/00 , A61P25/00 , A61P25/02 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P27/06 , A61P31/12 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/04 , C07D401/14 , C07D409/14
CPC分类号： A61K31/505 , C07D401/04 , C07D401/14 , C07D409/14
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted. And 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's disease.
摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐：其中：R1表示氢原子或可被C6,10芳基取代的C1-6烷基; R2表示可以被C 1-6烷基取代的C 1-10烷基， 可被取代的C2-6烯基，可被取代的C3-6炔基，可被取代的C3-6环烷基或可被取代的C6-10ArYL基;或R1 并且R 2一起形成可被取代的C 2-6亚烷基;或者R 1和R 2一起形成式 - （CH 2）2 -X-（CH 2）2 - 或 - （CH 2）2 -X-（CH 2） 3-其中X表示氧原子，硫原子或可被取代的氮原子; R 3表示任选被C 1-4烷基，C 1-4烷氧基或卤素取代的2,3或4-吡啶基 原子; R 4表示可以被羟基任选取代的C 1-10烷基，可以被取代的氨基，C 1-6单烷基氨基，C 2-12二烷基氨基或C 6〜10芳基。并且包含所述衍生物或其盐 作为用于预防和/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的活性成分。
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8.发明授权Derivatives of 1-piperazine- and 1-homopiperazine-carboxylates, preparation method thereof and use of same as inhibitors of the FAAH enzyme 有权1-哌嗪和1-高哌嗪羧酸酯的衍生物及其制备方法和作为FAAH酶抑制剂的用途公开(公告)号：US08114866B2
公开(公告)日：2012-02-14
申请号：US12701897
申请日：2010-02-08
IPC分类号： A61P1/08 , A61P9/00 , A61K31/55 , C07D243/08
CPC分类号： C07D295/185 , C07D213/74 , C07D215/46 , C07D231/38 , C07D239/42 , C07D295/205 , C07D311/04 , C07D317/58 , C07D495/04
摘要： The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.
摘要翻译： 本发明涉及具有通式（I）的化合物：其中m，R 1和R 2如本文所定义。 本发明还涉及该化合物在治疗中的用途。 更具体地说，本发明的化合物是FAAH酶的抑制剂，因此可用于治疗与FAAH酶相关的各种疾病，其包括非限制性的疼痛，进食障碍，神经和精神病理学 ，其他疾病。
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9.发明申请DERIVATIVES OF 1-PIPERAZINE- AND 1-HOMOPIPERAZINE-CARBOXYLATES, PREPARATION METHOD THEREOF AND USE OF SAME AS INHIBITORS OF THE FAAH ENZYME 有权1-哌啶酮和1-庚酮 - 羧酸酯的衍生物，其制备方法及其作为FAAH酶的抑制剂的用途公开(公告)号：US20100137329A1
公开(公告)日：2010-06-03
申请号：US12701897
申请日：2010-02-08
IPC分类号： A61K31/496 , A61K31/501 , A61K31/506 , A61K31/4965 , C07D403/04 , C07D401/04 , C07D495/04 , C07D413/04 , C07D405/10 , C07D295/033 , A61P9/10 , A61P25/00 , A61P1/00
CPC分类号： C07D295/185 , C07D213/74 , C07D215/46 , C07D231/38 , C07D239/42 , C07D295/205 , C07D311/04 , C07D317/58 , C07D495/04
摘要： The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.
摘要翻译： 本发明涉及具有通式（I）的化合物：其中m，R 1和R 2如本文所定义。 本发明还涉及该化合物在治疗中的用途。 更具体地说，本发明的化合物是FAAH酶的抑制剂，因此可用于治疗与FAAH酶相关的各种疾病，其包括非限制性的疼痛，进食障碍，神经和精神病理学 ，其他疾病。
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10.发明授权Derivatives of 1-piperazine-and 1-homopiperazine-carboxylates, preparation method thereof and use of same as inhibitors of the FAAH enzyme 有权1-哌嗪和1-高哌嗪羧酸酯的衍生物及其制备方法及其作为FAAH酶抑制剂的用途公开(公告)号：US07687503B2
公开(公告)日：2010-03-30
申请号：US11473284
申请日：2006-06-22
IPC分类号： A61P1/08 , A61P9/00 , A61K31/501 , A61K31/497 , A61K31/4965 , C07D295/185 , C07D401/00 , C07D403/02 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/02 , C07D417/02
CPC分类号： C07D295/185 , C07D213/74 , C07D215/46 , C07D231/38 , C07D239/42 , C07D295/205 , C07D311/04 , C07D317/58 , C07D495/04
摘要： The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.
摘要翻译： 本发明涉及具有通式（I）的化合物：其中m，R 1和R 2如本文所定义。 本发明还涉及该化合物在治疗中的用途。 更具体地说，本发明的化合物是FAAH酶的抑制剂，因此可用于治疗与FAAH酶相关的各种疾病，其包括非限制性的疼痛，进食障碍，神经和精神病理学 ，其他疾病。
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