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公开(公告)号：US06913898B2
公开(公告)日：2005-07-05
申请号：US10268533
申请日：2002-10-10
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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![Substituted 4-amino-2-aryl-cyclopenta[d]pyrimidines, their production and use and pharmaceutical preparations containing same](/abs-image/US/2003/09/30/US06627628B1/abs.jpg.150x150.jpg)
22.发明授权Substituted 4-amino-2-aryl-cyclopenta[d]pyrimidines, their production and use and pharmaceutical preparations containing same 有权取代的4-氨基-2-芳基 - 环戊二烯并[d]嘧啶，其制备和用途以及含有它们的药物制剂公开(公告)号：US06627628B1
公开(公告)日：2003-09-30
申请号：US09856069
申请日：2001-05-17
IPC分类号： C07D23970
CPC分类号： C07D401/12 , C07D239/70
摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).
摘要翻译： 本发明涉及其中R 1，R 2和R 3具有权利要求中给出的含义的式（I）化合物。 所述化合物是药物中有价值的活性剂，用于治疗和预防疾病，例如高血压，心绞痛，心力衰竭，血栓形成和动脉粥样硬化等心血管疾病。 式（I）化合物能够调节人体自身产生的环鸟苷酸（cGMP），并且通常适用于与受损的cGMP平衡相关的疾病的治疗和预防。 本发明还涉及制备式（I）化合物的方法，用于治疗和预防上述疾病以及用于制备这些疾病的药物，以及含有式（I）化合物的药物制剂。
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23.发明授权Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments 有权取代的2-芳基-4-氨基 - 噻唑啉酮，其生产和使用方法作为药物公开(公告)号：US06613772B1
公开(公告)日：2003-09-02
申请号：US09581763
申请日：2000-06-16
IPC分类号： C07D23994
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/12 , C07D403/12
摘要： Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.
摘要翻译： R1，R2，R3和Ar具有权利要求中所示含义的式Iin化合物适用于制备药物，例如预防和治疗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的化合物具有调节环鸟苷酸（cGMP）的内源性产生的能力，并且通常适用于治疗和预防与受干扰的cGMP平衡相关的疾病状态。
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24.发明授权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：US06335334B1
公开(公告)日：2002-01-01
申请号：US09349933
申请日：1999-07-08
IPC分类号： A61K315375
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A1，A2，R1，R2，R3，X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价值的药物活性化合物，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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25.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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26.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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27.发明申请Pharmaceutical composition comprising a sodium hydrogen exchange inhibitor and an angiotensin converting enzyme inhibitor 失效包含钠氢交换抑制剂和血管紧张素转化酶抑制剂的药物组合物公开(公告)号：US20050009899A1
公开(公告)日：2005-01-13
申请号：US10910912
申请日：2004-08-04
申请人： Wolfgang Linz , Ursula Schindler
发明人： Wolfgang Linz , Ursula Schindler
IPC分类号： A61K31/155 , A61K31/403 , A61K31/401
CPC分类号： A61K31/155 , A61K31/403 , A61K2300/00
摘要： This invention is directed to a pharmaceutical composition comprising the sodium-hydrogen exchanger (NHE) inhibitor cariporide and an angiotensin converting enzyme (ACE) inhibitor which exhibits unexpectedly efficacious properties for preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life, and to methods of preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life comprising administering pharmaceutically effective amounts of the sodium-hydrogen exchange inhibitor cariporide and an ACE inhibitor.
摘要翻译： 本发明涉及一种药物组合物，其包含钠 - 氢交换剂（NHE）抑制剂卡立劳和血管紧张素转换酶（ACE）抑制剂，其显示出意想不到的有效性质用于预防心力衰竭和其他与年龄有关的器官功能障碍，年龄相关疾病和 用于延长寿命，以及预防心力衰竭和其他与年龄有关的器官功能障碍，年龄相关疾病和延长寿命的方法，包括给予药学有效量的钠 - 氢交换抑制剂卡立劳和ACE抑制剂。
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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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29.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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