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1.发明申请公开(公告)号：US20050176799A1
公开(公告)日：2005-08-11
申请号：US11104556
申请日：2005-04-13
IPC分类号： A61K31/415 , A61K31/00 , A61K31/34 , A61P1/00 , A61P1/16 , A61P3/00 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/12 , A61P25/28 , A61P43/00 , C07D231/56 , C07D307/34 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , A61K31/416 , C07D43/04 , C07D45/04 , C07D49/04
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
摘要翻译： 本发明涉及式I的吡唑衍生物及其制备及其在药物中的用途：其中X，R 1，R 1a，R 2， R 3，R 4，R 4和n如权利要求中所定义，它们是用于治疗和预防疾病的有用的药物活性化合物，例如心血管 疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。 式I的化合物能够调节身体产生的环鸟苷酸“cGMP”，通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 本发明还涉及用于制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于该目的的药物，还涉及包含式I化合物的药物制剂。
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2.发明申请Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them 有权硫取代磺酰氨基羧酸N-芳基酰胺，其制备方法及其应用和包含它们的药物制剂公开(公告)号：US20080096936A1
公开(公告)日：2008-04-24
申请号：US12000844
申请日：2007-12-18
IPC分类号： A61K31/44 , C07D213/02 , A61P9/00 , C07D231/02 , A61K31/415
CPC分类号： C07C311/21 , C07C311/46 , C07C311/51 , C07C311/58 , C07C317/40 , C07C323/42 , C07C323/52 , C07C323/60 , C07C331/12 , C07C2601/02 , C07C2601/14 , C07C2602/04 , C07C2602/08 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/48 , C07D209/10 , C07D209/14 , C07D211/46 , C07D211/54 , C07D211/62 , C07D211/96 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/82 , C07D215/36 , C07D221/20 , C07D231/18 , C07D231/38 , C07D231/42 , C07D233/84 , C07D235/18 , C07D239/06 , C07D239/26 , C07D239/42 , C07D243/08 , C07D261/10 , C07D261/16 , C07D265/30 , C07D277/04 , C07D277/36 , C07D277/46 , C07D277/52 , C07D277/54 , C07D277/64 , C07D279/12 , C07D295/26 , C07D333/34 , C07D333/38 , C07D333/40 , C07D401/12 , C07D413/12 , C07D491/10
摘要： The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
摘要翻译： 本发明涉及式I化合物，其中A 1，A 2，R 1，R 2， R 3，X和n如权利要求中所定义，其是用于治疗和预防疾病的有价值的药学活性化合物，例如心血管疾病如高血压，心绞痛，心功能不全， 血栓形成或动脉粥样硬化。 式I的化合物能够调节身体的环鸟苷酸（cGMP）的产生，并且通常适用于治疗和预防与扰乱的cGMP平衡相关的疾病。 本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于此目的的药物以及包含式I化合物的药物制剂。
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3.发明授权
公开(公告)号：US6162819A
公开(公告)日：2000-12-19
申请号：US166283
申请日：1998-10-05
IPC分类号： A61K31/415 , A61K31/00 , A61K31/34 , A61P1/00 , A61P1/16 , A61P3/00 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/12 , A61P25/28 , A61P43/00 , C07D231/56 , C07D307/34 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , A61K31/4155 , A61K31/416
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: ##STR1## in which X, R.sup.1, R.sup.1a, R.sup.2, R.sup.3, R.sup.4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate "cGMP" and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula 1, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
摘要翻译： 本发明涉及式I的吡唑衍生物及其制备及其在药物中的用途：其中X，R 1，R 1a，R 2，R 3，R 4和n如权利要求中所定义，其是用于 治疗和预防疾病，例如心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。 式I的化合物能够调节身体产生的环鸟苷酸“cGMP”，通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 本发明还涉及制备式1化合物的方法，用于治疗和预防上述疾病和用于制备用于该目的的药物，以及用于包含式I化合物的药物制剂。
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4.发明授权公开(公告)号：US07300950B2
公开(公告)日：2007-11-27
申请号：US11104556
申请日：2005-04-13
IPC分类号： C07D403/04 , A61K31/416 , C07D405/04 , A61K31/4155
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
摘要翻译： 本发明涉及式I的吡唑衍生物及其制备及其在药物中的用途：其中X，R 1，R 1a，R 2， R 3，R 4，R 4和n如权利要求中所定义，它们是用于治疗和预防疾病的有用的药物活性化合物，例如心血管 疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。 式I的化合物能够调节身体产生的环鸟苷酸“cGMP”，通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 本发明还涉及用于制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于该目的的药物，还涉及包含式I化合物的药物制剂。
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公开(公告)号：US06897232B2
公开(公告)日：2005-05-24
申请号：US10252825
申请日：2002-09-24
IPC分类号： A61K31/415 , A61K31/00 , A61K31/34 , A61P1/00 , A61P1/16 , A61P3/00 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/12 , A61P25/28 , A61P43/00 , C07D231/56 , C07D307/34 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , A61K31/4155
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
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6.发明授权Method for screening for activators of soluble guanylate cyclase having oxidized heme iron 失效用于筛选具有氧化血红素铁的可溶性鸟苷酸环化酶活化剂的方法公开(公告)号：US07309579B2
公开(公告)日：2007-12-18
申请号：US11144265
申请日：2005-06-03
IPC分类号： C12Q1/48
CPC分类号： C12Q1/527 , G01N2333/795 , G01N2500/00
摘要： The invention relates to methods for detecting a soluble guanylate cyclase whose heme iron is in the trivalent oxidation state, and to methods for finding chemical substances which stimulate the activity of a soluble guanylate cyclase when the heme iron of at least part of this soluble guanylate cyclase is oxidized to the trivalent state and also to diagnostic aids or kits for detecting a soluble guanylate cyclase with trivalent heme iron. Further, the invention relates methods for detecting a soluble guanylate cyclase lacking a heme group, and to methods for finding chemical substances which stimulate the activity of a soluble guanylate cyclase lacking a heme group.
摘要翻译： 本发明涉及用于检测其血红素铁处于三价氧化状态的可溶性鸟苷酸环化酶的方法，以及当该可溶性鸟苷酸环化酶的至少一部分的血红素铁时，发现刺激可溶性鸟苷酸环化酶活性的化学物质的方法 被氧化成三价状态，也用于用三价血红素铁检测可溶性鸟苷酸环化酶的诊断辅助剂或试剂盒。 此外，本发明涉及用于检测缺少血红素基团的可溶性鸟苷酸环化酶的方法，以及用于发现刺激缺少血红素基团的可溶性鸟苷酸环化酶的活性的化学物质的方法。
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7.发明申请Method for detecting oxidized forms of soluble guanylate cyclase and a method for screening for activators of soluble guanylate cyclase having oxidized heme iron 失效用于检测可溶性鸟苷酸环化酶的氧化形式的方法和用于筛选具有氧化血红素铁的可溶性鸟苷酸环化酶活化剂的方法公开(公告)号：US20050227308A1
公开(公告)日：2005-10-13
申请号：US11144265
申请日：2005-06-03
CPC分类号： C12Q1/527 , G01N2333/795 , G01N2500/00
摘要： The invention relates to methods for detecting a soluble guanylate cyclase whose heme iron is in the trivalent oxidation state, and to methods for finding chemical substances which stimulate the activity of a soluble guanylate cyclase when the heme iron of at least part of this soluble guanylate cyclase is oxidized to the trivalent state and also to diagnostic aids or kits for detecting a soluble guanylate cyclase with trivalent heme iron. Further, the invention relates methods for detecting a soluble guanylate cyclase lacking a heme group, and to methods for finding chemical substances which stimulate the activity of a soluble guanylate cyclase lacking a heme group.
摘要翻译： 本发明涉及用于检测其血红素铁处于三价氧化状态的可溶性鸟苷酸环化酶的方法，以及当该可溶性鸟苷酸环化酶的至少一部分的血红素铁时，发现刺激可溶性鸟苷酸环化酶活性的化学物质的方法 被氧化成三价状态，也用于用三价血红素铁检测可溶性鸟苷酸环化酶的诊断辅助剂或试剂盒。 此外，本发明涉及用于检测缺少血红素基团的可溶性鸟苷酸环化酶的方法，以及用于发现刺激缺少血红素基团的可溶性鸟苷酸环化酶的活性的化学物质的方法。
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公开(公告)号：US06500631B1
公开(公告)日：2002-12-31
申请号：US09661915
申请日：2000-09-14
IPC分类号： C12Q148
CPC分类号： C12Q1/527 , G01N2333/795 , G01N2500/00
摘要： The invention relates to methods for detecting a soluble guanylate cyclase whose heme iron is in the trivalent oxidation state, and to methods for finding chemical substances which stimulate the activity of a soluble guanylate cyclase when the heme iron of at least part of this soluble guanylate cyclase is oxidized to the trivalent state and also to diagnostic aids or kits for detecting a soluble guanylate cyclase with trivalent heme iron. Further, the invention relates methods for detecting a soluble guanylate cyclase lacking a heme group, and to methods for finding chemical substances which stimulate the activity of a soluble guanylate cyclase lacking a heme group.
摘要翻译： 本发明涉及用于检测其血红素铁处于三价氧化状态的可溶性鸟苷酸环化酶的方法，以及当该可溶性鸟苷酸环化酶的至少一部分的血红素铁时，发现刺激可溶性鸟苷酸环化酶活性的化学物质的方法 被氧化成三价状态，也用于用三价血红素铁检测可溶性鸟苷酸环化酶的诊断辅助剂或试剂盒。 此外，本发明涉及用于检测缺少血红素基团的可溶性鸟苷酸环化酶的方法，以及用于发现刺激缺少血红素基团的可溶性鸟苷酸环化酶的活性的化学物质的方法。
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9.发明授权Substituted isoindolones and their use as cyclic GMP modulators in medicaments 有权取代的异吲哚啉酮及其作为药物中循环GMP调节剂的用途公开(公告)号：US06344468B1
公开(公告)日：2002-02-05
申请号：US09622691
申请日：2000-10-06
IPC分类号： A61K314035
CPC分类号： C07D209/48 , C07D401/04 , C07D409/04
摘要： The present invention relates to substituted isoindolone derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for these, and also pharmaceutical preparations which comprise compounds of the formula I.
摘要翻译： 本发明涉及式I的取代的异吲哚酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如权利要求中所定义，其是用于治疗和预防疾病的有用的药物活性化合物， 例如心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。 式I的化合物能够调节人体产生的环鸟苷酸（cGMP），并且通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备这些疾病的药物，以及包含式I化合物的药物制剂。
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公开(公告)号：US08541410B2
公开(公告)日：2013-09-24
申请号：US13345223
申请日：2012-01-06
IPC分类号： A61K31/535 , C07C303/00
CPC分类号： C07C311/21 , C07C311/46 , C07C311/51 , C07C311/58 , C07C317/40 , C07C323/42 , C07C323/52 , C07C323/60 , C07C331/12 , C07C2601/02 , C07C2601/14 , C07C2602/04 , C07C2602/08 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/48 , C07D209/10 , C07D209/14 , C07D211/46 , C07D211/54 , C07D211/62 , C07D211/96 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/82 , C07D215/36 , C07D221/20 , C07D231/18 , C07D231/38 , C07D231/42 , C07D233/84 , C07D235/18 , C07D239/06 , C07D239/26 , C07D239/42 , C07D243/08 , C07D261/10 , C07D261/16 , C07D265/30 , C07D277/04 , C07D277/36 , C07D277/46 , C07D277/52 , C07D277/54 , C07D277/64 , C07D279/12 , C07D295/26 , C07D333/34 , C07D333/38 , C07D333/40 , C07D401/12 , C07D413/12 , C07D491/10
摘要： The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
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