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    • 7. 发明申请
      WO2002094176A3 USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY ON THE PREPARATION OF MEDICAMENTS 审中-公开
    • USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY ON THE PREPARATION OF MEDICAMENTS
    • WO2002094176A3
    • 2002-11-28
    • PCT/EP2002/005259
    • 2002-05-14
    • SOLVAY PHARMACEUTICALS GMBH , BERGER, Claudia , FISCHER, Yvan , HÖLTJE, Dagmar , WALDECK, Harald , WESKE, Michael , ZIEGLER, Dieter
    • BERGER, Claudia , FISCHER, Yvan , HÖLTJE, Dagmar , WALDECK, Harald , WESKE, Michael , ZIEGLER, Dieter
    • A61K31/55
    • This invention relates to the use of a compound having combined, in particular concurrent, inhibitorz activity on neutral endopeptidase (NEP) and on a novel metalloprotease designated IGS5, or of a pharmaceutically acceptable salt or solvate or biolabile ester thereof, for the manufacture of a medicament (pharmaceutical composition) for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition which can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. In a particular aspect the present invention pertains to the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where bit-ET-l levels are elevated and which disease or condition can be alleviated or prevented by cobined or concurrent inhibition of NEP and IGS5. In a further particular aspect the present invention pertainsto the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where ET-1 is significantly upregulated and which disease or condition can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. In the present invention said compounds with combined or concurrent NEP/IGS5-inhibitory activity preferably are used for the treatment and/or prophylaxis of hypertension, including secondary forms of hypertension such as renal or pulmonary hypertension, heart failure, angina pectoris, arrhythmias, myorcadial infarction, cardiac hypertrophy, cerebral ischemia, peripheral vascular disease, subarachnoidal hemorrhage, chronic obstructive pulmonary disease (COPD), asthma, renal disease, atherosclerosis, and pain in colorectal cancer or prostate cancer, in mammals, preferably in humans, and more preferably in a patient sub-population suffering from or being susceptible to a disease or condition which can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. Furthermore, it may be beneficial to additionally combine the said compounds showing combined or concurrent NEP/IGS5 inhibitory activity with other individual and/or combined metalloprotease inhibitors than the NEP/IGS5 inhibitors, e.g. with separate ACE- and/or NEP-inhibitors and/or mixed inhibitors of these metalloproteases.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      WO2002094176A2 USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY IN THE PREPARATION OF MEDICAMENTS 审中-公开
    • USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY IN THE PREPARATION OF MEDICAMENTS
    • 在制剂中使用具有组合NEP / MP-抑制活性的化合物
    • WO2002094176A2
    • 2002-11-28
    • PCT/EP2002/005259
    • 2002-05-14
    • SOLVAY PHARMACEUTICALS GMBH , BERGER, Claudia , FISCHER, Yvan , HÖLTJE, Dagmar , WALDECK, Harald , WESKE, Michael , ZIEGLER, Dieter
    • BERGER, Claudia , FISCHER, Yvan , HÖLTJE, Dagmar , WALDECK, Harald , WESKE, Michael , ZIEGLER, Dieter
    • A61K
    • A61K31/55 , A61K31/00
    • This invention relates to the use of a compound having combined, in particular concurrent, inhibitorz activity on neutral endopeptidase (NEP) and on a novel metalloprotease designated IGS5, or of a pharmaceutically acceptable salt or solvate or biolabile ester thereof, for the manufacture of a medicament (pharmaceutical composition) for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition which can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. In a particular aspect the present invention pertains to the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where bit-ET-l levels are elevated and which disease or condition can be alleviated or prevented by cobined or concurrent inhibition of NEP and IGS5. In a further particular aspect the present invention pertainsto the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where ET-1 is significantly upregulated and which disease or condition can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. In the present invention said compounds with combined or concurrent NEP/IGS5-inhibitory activity preferably are used for the treatment and/or prophylaxis of hypertension, including secondary forms of hypertension such as renal or pulmonary hypertension, heart failure, angina pectoris, arrhythmias, myorcadial infarction, cardiac hypertrophy, cerebral ischemia, peripheral vascular disease, subarachnoidal hemorrhage, chronic obstructive pulmonary disease (COPD), asthma, renal disease, atherosclerosis, and pain in colorectal cancer or prostate cancer, in mammals, preferably in humans, and more preferably in a patient sub-population suffering from or being susceptible to a disease or condition which can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5. Furthermore, it may be beneficial to additionally combine the said compounds showing combined or concurrent NEP/IGS5 inhibitory activity with other individual and/or combined metalloprotease inhibitors than the NEP/IGS5 inhibitors, e.g. with separate ACE- and/or NEP-inhibitors and/or mixed inhibitors of these metalloproteases.
    • 本发明涉及在中性肽链内切酶（NEP）和指定为IGS5的新型金属蛋白酶或其药学上可接受的盐或溶剂合物或生物不稳定酯上具有特别并用的抑制剂活性的化合物的用途，用于制备 用于治疗患有或易患有疾病或病症的较大哺乳动物，优选人类的药物（药物组合物），其可通过组合或同时抑制NEP和IGS5而减轻或预防。 在一个特定方面，本发明涉及具有组合或并用NEP / IGS5抑制活性的所述化合物在治疗患有或易于患有bit-ET-1水平的疾病或病症的较大哺乳动物，优选人的用途 升高，哪些疾病或病症可以通过核苷或同时抑制NEP和IGS5来缓解或预防。 在另一个特定方面，本发明涉及具有组合或并发NEP / IGS5抑制活性的所述化合物在治疗患有或易于患有ET-1显着上调的疾病或病症的较大哺乳动物，优选人的情况下的用途 通过NEP和IGS5的组合或同时抑制可以减轻或预防哪种疾病或病症。 在本发明中，具有组合或并发NEP / IGS5抑制活性的所述化合物优选用于治疗和/或预防高血压，包括高血压的次要形式如肾或肺动脉高压，心力衰竭，心绞痛，心律失常，肌筋膜 动脉粥样硬化，大肠癌，前列腺癌疼痛，脑梗塞，心脏肥大，脑缺血，外周血管疾病，蛛网膜下腔出血，慢性阻塞性肺疾病（COPD），哮喘，肾脏疾病，动脉粥样硬化， 患有或易患疾病或病症的患者亚群可以通过NEP和IGS5的组合或同时抑制而减轻或预防。 此外，与NEP / IGS5抑制剂例如NEP / IGS5抑制剂相比，另外组合显示组合或并发NEP / IGS5抑制活性的其它单独和/或组合的金属蛋白酶抑制剂的所述化合物可能是有益的。 与这些金属蛋白酶的单独的ACE-和/或NEP-抑制剂和/或混合抑制剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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