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公开(公告)号：US20080221107A1
公开(公告)日：2008-09-11
申请号：US11995570
申请日：2006-07-13
IPC分类号： A61K31/53 , C07D513/04 , A61K31/519 , A61K31/5025 , A61P3/10 , A61P3/04 , A61P25/00
CPC分类号： C07D495/04
摘要： Compounds of formula (I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.
摘要翻译： 式（I）化合物，制备这些化合物的方法，它们在治疗肥胖症，精神疾病，认知障碍，记忆障碍，精神分裂症，癫痫和相关病症中的用途，以及神经系统疾病如痴呆，多发性硬化，帕金森病 ，亨廷顿氏舞蹈病和阿尔茨海默病和疼痛相关疾病以及含有它们的药物组合物。
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公开(公告)号：US07723331B2
公开(公告)日：2010-05-25
申请号：US11840382
申请日：2007-08-17
IPC分类号： C07D495/04 , C07D413/14 , A61K31/5355 , A61K31/519 , A61P3/04 , A61P25/18 , A61P25/22 , A61P25/28
CPC分类号： C07D495/04
摘要： The present invention provides compounds of the class of thienopyrimidines, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, type II diabetes, Metabolic syndrome and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, and pain related disorders, and to pharmaceutical compositions containing them.
摘要翻译： 本发明提供噻吩并嘧啶类化合物，制备这些化合物的方法，其用于治疗肥胖症，精神疾病，认知障碍，记忆障碍，精神分裂症，癫痫和相关病症，II型糖尿病，代谢综合征和神经系统疾病 障碍，例如痴呆，多发性硬化，帕金森病，亨廷顿氏舞蹈病，阿尔茨海默病和疼痛相关疾病，以及含有它们的药物组合物。
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公开(公告)号：US20080300232A1
公开(公告)日：2008-12-04
申请号：US10599110
申请日：2005-03-21
申请人： Kay Brickmann , Bryan J. Egner , Fabrizio Giordanetto , Tord Inghardt , Anna Linusson Jonsson , Fritiof Ponten
发明人： Kay Brickmann , Bryan J. Egner , Fabrizio Giordanetto , Tord Inghardt , Anna Linusson Jonsson , Fritiof Ponten
IPC分类号： A61K31/397 , C07D401/02 , A61K31/454 , C07D213/02 , A61P3/04 , A61P3/10 , A61P25/00 , A61K31/4545 , C07D239/24 , A61K31/506
CPC分类号： C07D403/06 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/06 , C07D405/14 , C07D409/14
摘要： Compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.
摘要翻译： 式I化合物，制备这些化合物的方法，它们在治疗肥胖，精神障碍，认知障碍，记忆障碍，精神分裂症，癫痫和相关病症中的用途，以及神经障碍如痴呆，多发性硬化，帕金森病，亨廷顿病 舞蹈病和阿尔茨海默病和疼痛相关疾病以及含有它们的药物组合物。
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公开(公告)号：US20080306055A1
公开(公告)日：2008-12-11
申请号：US11721767
申请日：2005-12-19
申请人： Bryan Egner , Fabrizio Giordanetto , Tord Inghardt
发明人： Bryan Egner , Fabrizio Giordanetto , Tord Inghardt
IPC分类号： A61K31/541 , A61K31/454 , C07D401/02 , A61K31/4545 , A61P25/00 , A61P3/10 , A61P25/18 , C07D401/14 , C07D417/14
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Compounds of formula I depicted below, pharmaceutical compositions containing them, processes for preparing the compounds, and their use in the treatment of obesity, type II diabetes, metabolic syndrome, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy and related conditions, neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease, and pain related disorders. The compounds are melanin concentrating hormone receptor 1 (MCHr1) antagonists.
摘要翻译： 下面描述的式I化合物，含有它们的药物组合物，制备化合物的方法及其在治疗肥胖症，II型糖尿病，代谢综合征，精神病学，认知障碍，记忆障碍，精神分裂症，癫痫和相关病症中的用途， 神经系统疾病如痴呆，多发性硬化，帕金森病，亨廷顿舞蹈病和阿尔茨海默病，以及疼痛相关疾病。 这些化合物是黑色素浓缩激素受体1（MCHr1）拮抗剂。
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公开(公告)号：US20070185079A1
公开(公告)日：2007-08-09
申请号：US10596994
申请日：2005-01-05
IPC分类号： A61K31/554
CPC分类号： C07D215/38 , C07D401/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Compounds of formula(I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders, and pharmaceutical compositions containing them.
摘要翻译： 式（I）化合物，制备这些化合物的方法，它们在治疗肥胖症，精神疾病，认知障碍，记忆障碍，精神分裂症，癫痫和相关病症中的用途，以及神经系统疾病如痴呆，多发性硬化，帕金森病 ，亨廷顿氏舞蹈病和阿尔茨海默病和疼痛相关疾病，以及含有它们的药物组合物。
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公开(公告)号：US20080051405A1
公开(公告)日：2008-02-28
申请号：US11840382
申请日：2007-08-17
IPC分类号： C07D495/04 , A61K31/5025 , A61K31/519 , A61P25/00 , A61P3/00
CPC分类号： C07D495/04
摘要： The present invention provides compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, type II diabetes, Metabolic syndrome and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, and pain related disorders, and to pharmaceutical compositions containing them.
摘要翻译： 本发明提供了式I化合物，其制备方法，用于治疗肥胖症，精神疾病，认知障碍，记忆障碍，精神分裂症，癫痫和相关病症，II型糖尿病，代谢综合征和神经障碍 作为痴呆，多发性硬化，帕金森病，亨廷顿氏舞蹈病，阿尔茨海默病和疼痛相关疾病，以及含有它们的药物组合物。
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公开(公告)号：US07241757B2
公开(公告)日：2007-07-10
申请号：US10815954
申请日：2004-04-02
IPC分类号： A61K31/397 , A61K31/445 , C07D207/00
CPC分类号： C07D205/04 , C07D207/16 , C07D405/06
摘要： There is provided compounds of formula I wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
摘要翻译： 提供式I化合物，其中R 1，R x，Y，R y，n和B具有在描述中给出的含义 可用作胰蛋白酶样蛋白酶（例如凝血酶）的竞争性抑制剂，特别是用于治疗需要凝血酶抑制（例如血栓形成）或作为抗凝剂的条件。
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公开(公告)号：US07056907B2
公开(公告)日：2006-06-06
申请号：US10487805
申请日：2002-08-30
申请人： Tord Inghardt , Anders Johansson , Arne Svensson
发明人： Tord Inghardt , Anders Johansson , Arne Svensson
IPC分类号： C07D205/04 , A61K31/397
CPC分类号： C07D401/12 , C07C45/004 , C07C45/29 , C07C45/516 , C07C45/673 , C07C45/71 , C07C47/575 , C07C59/56 , C07C59/64 , C07C69/732 , C07C69/734 , C07C69/738 , C07C205/59 , C07D205/04 , C07D207/16 , C07D403/12 , C07C49/84 , C07C47/565
摘要： There is provided a compound of formula (1) and pharmaceutically-acceptable derivatives (including prodrugs) thereof. Which compound and derivatives are useful as, or are as useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
摘要翻译： 提供式（1）的化合物和其药学上可接受的衍生物（包括前药）。 哪种化合物和衍生物可用作胰蛋白酶样蛋白酶的竞争性抑制剂例如凝血酶，因此特别是用于治疗需要凝血酶抑制（例如血栓形成）或作为 抗凝剂
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公开(公告)号：US20060014734A1
公开(公告)日：2006-01-19
申请号：US10516423
申请日：2003-05-27
IPC分类号： A61K31/397 , A61K9/20
CPC分类号： A61K31/397 , A61K9/0019 , A61K9/0095 , A61K9/08 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/40
摘要： According to the present invention there is provided an immediate release pharmaceutical formulation comprising, as active ingredient, a compound of formula (I): wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy; and n represents 0, 1 or 2; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable diluent or carrier; provided that when the active ingredient is other than in the form of a salt the formulation does not solely contain: a solution of one active ingredient and water, a solution of one active ingredient and dimethylsulphoxide; or a solution of one active ingredient in a mixture of ethanol:PEG 660 12-hydroxy stearate:water 5:5:90; such formulations being of use for the treatment of a cardiovascular disorder.
摘要翻译： 根据本发明，提供了一种立即释放药物制剂，其包含作为活性成分的式（I）化合物：其中R 1表示C 1-12烷基 被一个或多个氟取代基取代; R 2表示氢，羟基，甲氧基或乙氧基; n表示0,1或2; 或其药学上可接受的盐; 和药学上可接受的稀释剂或载体; 条件是当活性成分不是盐形式时，制剂不仅包含：一种活性成分和水的溶液，一种活性成分和二甲基亚砜的溶液; 或一种活性成分在乙醇：PEG 660 12-羟基硬脂酸酯：水5:5:90的混合物中的溶液; 这样的制剂可用于治疗心血管疾病。
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公开(公告)号：US20050234035A1
公开(公告)日：2005-10-20
申请号：US10516422
申请日：2003-05-27
IPC分类号： C07D205/04 , A61K20060101 , A61K31/396 , A61K31/397 , A61P7/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P43/00 , C07D20060101 , C07D25/02
CPC分类号： C07D205/04
摘要： There is provided pharmaceutically-acceptable acid addition salts of compounds of formula I, wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents C1-2 alkyl; and n represents 0, 1 or 2, which salts are useful as prodrugs of competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
摘要翻译： 提供式I化合物的药学上可接受的酸加成盐，其中R 1表示被一个或多个氟取代基取代的C 1-12烷基; R 2表示C 1-12烷基; 和n表示0,1或2，这些盐可用作胰蛋白酶样蛋白酶如凝血酶的竞争性抑制剂的前药，因此特别是在需要抑制凝血酶的条件（例如血栓形成）或 作为抗凝剂。
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