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1. 发明授权

US5274116A 1-aminoacetamidopyrroles and 1-aminoacetamido-2-(substituted)pyrroles and related compounds 失效
标题翻译： 1-氨基乙酰胺吡咯和1-氨基乙酰胺基-2-（取代）吡咯及相关化合物
公开(公告)号：US5274116A
公开(公告)日：1993-12-28
申请号：US922291
申请日：1992-07-30
申请人： Lawrence Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
发明人： Lawrence Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
IPC分类号： A61K31/40 , A61K31/00 , A61K31/4025 , A61P25/28 , C07D207/335 , C07D207/34 , C07D207/50 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/06 , C07D409/14 , C07D401/06
CPC分类号： C07D403/04 , C07D207/50 , C07D409/06
摘要： There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)-pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

2. 发明授权

US5605925A 1-aminoacetamidopyrroles and 1-amino acetamido-2-(substituted) pyrroles and related compounds 失效
标题翻译： 1-氨基乙酰胺吡咯和1-氨基乙酰氨基-2-（取代）吡咯及相关化合物
公开(公告)号：US5605925A
公开(公告)日：1997-02-25
申请号：US335238
申请日：1994-11-07
申请人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
发明人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
IPC分类号： A61K31/40 , A61K31/00 , A61K31/4025 , A61P25/28 , C07D207/335 , C07D207/34 , C07D207/50 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/06 , C07D409/14
CPC分类号： C07D403/04 , C07D207/50 , C07D409/06
摘要： There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.
摘要翻译：公开了1-氨基乙酰胺基吡咯啉和1-氨基-2-（取代的）吡咯及其相关化合物，其中所有取代基都在本文中定义，其可用作甘氨酸部分激动剂并用于增强学习和记忆和用于治疗与神经变性疾病相关的记忆功能障碍，因此在治疗阿尔茨海默病和其他老年痴呆症中被指示。

3. 发明授权

US5580987A Process for preparing 1-aminoacetamidopyrroles 失效
标题翻译： 1-氨基乙酰吡啶的制备方法
公开(公告)号：US5580987A
公开(公告)日：1996-12-03
申请号：US335236
申请日：1994-11-07
申请人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
发明人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
IPC分类号： A61K31/40 , A61K31/00 , A61K31/4025 , A61P25/28 , C07D207/335 , C07D207/34 , C07D207/50 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/06 , C07D409/14
CPC分类号： C07D403/04 , C07D207/50 , C07D409/06
摘要： There is disclosed a process for the preparation of 1-aminoacetamidopyrroles and 1-amino-2-(substituted)-pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias which comprises treating a 1-phthalimidopyrrole of the formula ##STR2## with a base to yield a 1-aminopyrrole of the formula ##STR3## which is reacted with a compound of the formula ##STR4## to obtain the compound of Formula (I).
摘要翻译：公开了用于制备本文配制的1-氨基乙酰胺吡咯和1-氨基-2-（取代的） - 吡咯和相关化合物的方法，其可用作甘氨酸部分激动剂并用于增强学习和记忆，以及用于治疗与神经变性疾病相关的记忆功能障碍，因此在治疗阿尔茨海默氏病和其他老年性痴呆症中被指出，其包括用碱处理式“IMAGE”的1-苯二酰亚胺基吡咯，得到下式的1-氨基吡咯：其与式（I）的化合物反应以获得式（I）的化合物。

4. 发明授权

US5576446A 1-amino-2-(substituted)pyrroles and related compounds 失效
标题翻译： 1-氨基-2-（取代）吡咯及相关化合物
公开(公告)号：US5576446A
公开(公告)日：1996-11-19
申请号：US334910
申请日：1994-11-07
申请人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
发明人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
IPC分类号： A61K31/40 , A61K31/00 , A61K31/4025 , A61P25/28 , C07D207/335 , C07D207/34 , C07D207/50 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/06 , C07D409/14 , C07D403/06
CPC分类号： C07D403/04 , C07D207/50 , C07D409/06
摘要： There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.
摘要翻译：公开了1-氨基乙酰胺基吡咯啉和1-氨基-2-（取代的）吡咯及其相关化合物，其中所有取代基均在本文中定义，其可用作甘氨酸部分激动剂并用于增强学习和记忆和用于治疗与神经变性疾病相关的记忆功能障碍，因此在治疗阿尔茨海默病和其他老年性痴呆症中被指出。

5. 发明授权

US5428053A 1-aminoacetamidopyrroles and 1-amino acetamido-2-(substituted) pyrroles and related compounds 失效
标题翻译： 1-氨基乙酰胺吡咯和1-氨基乙酰氨基-2-（取代）吡咯及相关化合物
公开(公告)号：US5428053A
公开(公告)日：1995-06-27
申请号：US102181
申请日：1993-09-28
申请人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
发明人： Lawrence L. Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
IPC分类号： A61K31/40 , A61K31/00 , A61K31/4025 , A61P25/28 , C07D207/335 , C07D207/34 , C07D207/50 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/06 , C07D409/14 , C07D403/06
CPC分类号： C07D403/04 , C07D207/50 , C07D409/06
摘要： There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted) pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.
摘要翻译：公开了1-氨基乙酰胺基吡咯啉和1-氨基-2-（取代的）吡咯及其相关化合物，其中所有取代基均在本文中定义，其可用作甘氨酸部分激动剂并用于增强学习和记忆和用于治疗与神经变性疾病相关的记忆功能障碍，因此在治疗阿尔茨海默病和其他老年痴呆症中被指示。

6. 发明授权

US5565579A (1H-indol-1-yl)-2-(amino)acetamides and related (1H-indol-1-yl)-(aminoalkyl)amides 失效
标题翻译：（1H-吲哚-1-基）-2-（氨基）乙酰胺和相关的（1H-吲哚-1-基） - （氨基烷基）酰胺
公开(公告)号：US5565579A
公开(公告)日：1996-10-15
申请号：US218211
申请日：1994-03-25
申请人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
发明人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P25/00 , C07D209/08 , C07D209/12 , C07D209/30
CPC分类号： C07D209/08 , A61K31/40 , C07D209/12 , C07D209/30
摘要： There are disclosed compounds having the formula ##STR1## wherein X, Y, Z and R.sub.1 -R.sub.6 are defined in the specification and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.
摘要翻译：公开了具有式“IMAGE”的化合物，其中X，Y，Z和R 1 -R 6在本说明书及其药学上可接受的加成盐中定义，或适用时，其光学或几何异构体或外消旋混合物，该方法中的中间体用于制备化合物，制备化合物的方法和药物组合物以及用作神经保护剂的方法。

7. 发明授权

US5646300A (1H-indol-1-yl)-2-(amino)acetamides and related (1H-indol-1-yl)-(aminoalkyl)amides, pharmaceutical composition and use 失效
标题翻译：（1H-吲哚-1-基）-2-（氨基）乙酰胺和相关的（1H-吲哚-1-基） - （氨基烷基）酰胺，药物组合物和用途
公开(公告)号：US5646300A
公开(公告)日：1997-07-08
申请号：US457649
申请日：1995-06-01
申请人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
发明人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P25/00 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/10 , C07D493/04
CPC分类号： C07D209/08 , A61K31/40 , C07D209/12 , C07D209/30
摘要： There are disclosed neuroprotective compounds having the formula ##STR1## wherein the moieties are defined in the specification, and processes for making them.
摘要翻译：公开了具有式“IMAGE”的神经保护性化合物，其中部分在说明书中定义，以及制备它们的方法。

8. 发明授权

US5591866A (1H-indol-1-yl)-2-(amino)acetamide derivatives and preparation thereof 失效
标题翻译：（1H-吲哚-1-基）-2-（氨基）乙酰胺衍生物及其制备
公开(公告)号：US5591866A
公开(公告)日：1997-01-07
申请号：US457723
申请日：1995-06-01
申请人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
发明人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P25/00 , C07D209/08 , C07D209/12 , C07D209/30 , C07D403/04
CPC分类号： C07D209/08 , A61K31/40 , C07D209/12 , C07D209/30
摘要： There are disclosed compounds having the formula ##STR1## wherein the variables are defined in the specification, and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.
摘要翻译：公开了具有式“IMAGE”的化合物，其中变量在本说明书中定义，其药学上可接受的加成盐，或适用时，其光学或几何异构体或外消旋混合物，制备该化合物的方法中的中间体制备化合物的方法和药物组合物以及用作神经保护剂的方法。

9. 发明授权

US5319096A (1H-indol-1-yl)-2-(amino) acetamides and related (1H-indol-1-yl)-(aminoalkyl)amides, pharmaceutical composition and use 失效
标题翻译：（1H-吲哚-1-基）-2-（氨基）乙酰胺和相关的（1H-吲哚-1-基） - （氨基烷基）酰胺，药物组合物和用途
公开(公告)号：US5319096A
公开(公告)日：1994-06-07
申请号：US863273
申请日：1992-04-03
申请人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
发明人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P25/00 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/04 , C07D493/02
CPC分类号： C07D209/08 , A61K31/40 , C07D209/12 , C07D209/30
摘要： There are disclosed compounds having the formula ##STR1## wherein X is hydrogen, chloro, bromo, fluoro, hydroxy, loweralkoxy, arylloweralkoxy, acyloxy, loweralkylaminocarbonyloxy, diloweralkylaminocarbonyloxy, amino, loweralkylamino, diloweralkylamino, acylamino, loweralkyl or trifluoromethyl;Y is hydrogen, loweralkyl, chloro or bromo;Z is hydrogen, loweralkyl, loweralkoxy or halogen; or X and Z taken together can form a methylenedioxy group;R.sup.1 is hydrogen, loweralkyl, arylloweralkyl, carboxyloweralkyl, arylloweralkoxycarbonylloweralkyl or loweralkoxycarbonylloweralkyl;R.sup.2 is hydrogen, loweralkyl or hydroxyloweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 together with the carbon to which they are attached form (C.sub.3 -C.sub.7)cycloalkyl;R.sup.4 is hydrogen or loweralkyl;R.sup.5 is hydrogen, loweralkyl, aryl, arylloweralkyl, acyl, arylloweralkoxycarbonyl, loweralkoxycarbonyl or aryloxycarbonyl;R.sup.6 is hydrogen, chloro, bromo, arylcarbonyl, loweralkylcarbonyl, aryl(hydroxy)loweralkyl or hydroxyloweralkyl; andm and n are independently 0 to 5 with the proviso that the sum of m plus n is not greater than 5;and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.
摘要翻译：公开了具有下式的化合物：卤代，羟基，低级烷氧基，芳基低级烷氧基，酰氧基，低级烷基氨基羰基氧基，二低烷基氨基羰基氧基，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，低级烷基或三氟甲基。 Y是氢，低级烷基，氯或溴; Z是氢，低级烷基，低级烷氧基或卤素; 或X和Z一起可以形成亚甲二氧基; R 1是氢，低级烷基，芳基低级烷基，羧基低级烷基，芳基低级烷氧基羰基低级烷基或低级烷氧基羰基低级烷基; R2是氢，低级烷基或羟基低级烷基; R3是氢或低级烷基; 或R 2和R 3与它们所连接的碳一起形成（C 3 -C 7）环烷基; R4是氢或低级烷基; R5是氢，低级烷基，芳基，芳基低级烷基，酰基，芳基低级烷氧羰基，低级烷氧羰基或芳氧基羰基; R6是氢，氯，溴，芳基羰基，低级烷基羰基，芳基（羟基）低级烷基或羟基低级烷基; 并且m和n独立地为0至5，条件是m + n的总和不大于5; 或其药学上可接受的加成盐，或适用时，其光学或几何异构体或外消旋混合物，制备该化合物的方法中的中间体，制备该化合物的方法和药物组合物以及用作神经保护剂的方法。

10. 发明授权

US08642603B2 Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof 有权
标题翻译：取代的二氢和四氢恶唑啉嘧啶酮，其制备和应用
公开(公告)号：US08642603B2
公开(公告)日：2014-02-04
申请号：US12554129
申请日：2009-09-04
申请人： Bin Cao , Vieroslava Gurunian , Sathapana Kongsamut , Raymond W. Kosley, Jr. , Rosy Sher , Ryan E. Hartung
发明人： Bin Cao , Vieroslava Gurunian , Sathapana Kongsamut , Raymond W. Kosley, Jr. , Rosy Sher , Ryan E. Hartung
IPC分类号： C07D491/04 , A61K31/519 , A61P25/28 , A61P25/22 , A61P25/18 , A61P25/06 , A61P25/02
CPC分类号： C07D498/04
摘要： The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
摘要翻译：本发明涉及一系列取代的二氢和四氢恶唑啉嘧啶酮，特别涉及一系列2-取代-2,3-二氢 - 恶唑并[3,2-a]嘧啶-7-酮和2-取代-2,2-二氧杂唑并[ （I）的3,5,6-四氢恶唑并[3,2-a]嘧啶-7-酮：其中p，n，X，Y，R1，R2，R3，R4，R5，R6， R7和R8如本文所定义。本发明还涉及制备这些化合物的方法，包括新型中间体。本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，抽搐，焦虑，抑郁症，偏头痛，疼痛，睡眠障碍和呕吐。

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