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    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    1.
    发明申请
    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
    4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途

    公开(公告)号：US20050054729A1

    公开(公告)日：2005-03-10

    申请号：US10920395

    申请日：2004-08-18

    申请人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    发明人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    IPC分类号： A61K31/00 ,  A61K31/166 ,  A61K31/66 ,  A61P1/16 ,  A61P5/48 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P15/10 ,  A61P19/10 ,  A61P25/28 ,  A61P27/06 ,  A61P43/00 ,  C07C233/65 ,  A61K31/165

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： The present invention relates to the method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan-2-yl benzamide according to the formula (I) to the said mammal. The compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.

    摘要翻译： 本发明涉及刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括将生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺给予 哺乳动物说 化合物（I）可用于治疗和预防心血管疾病如稳定和不稳定型心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗死，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化 ，PTCA后再狭窄，内皮损伤，原发性高血压，肺动脉高压，继发性高血压，肾血管性慢性肾小球肾炎，勃起功能障碍，室性心律失常，绝经后妇女心血管危险降低或避孕药物摄入后，糖尿病和糖尿病的治疗和预防 并发症（肾病，视网膜病变），血管生成，哮喘支气管炎，慢性肾功能衰竭，肝硬化，限制性记忆能力或受限的学习能力。

    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    3.
    发明授权
    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
    4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途

    公开(公告)号：US06617359B2

    公开(公告)日：2003-09-09

    申请号：US10073330

    申请日：2002-02-13

    申请人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    发明人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    IPC分类号： A61K3165

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： The present invention relates to the method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan-2-yl benzamide according to the formula (I) to the said mammal. The compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.

    摘要翻译： 本发明涉及刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括将生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺给予 哺乳动物说 化合物（I）可用于治疗和预防心血管疾病如稳定和不稳定型心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗死，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化 ，PTCA后再狭窄，内皮损伤，原发性高血压，肺动脉高压，继发性高血压，肾血管性慢性肾小球肾炎，勃起功能障碍，室性心律失常，绝经后妇女心血管危险降低或避孕药物摄入后，糖尿病和糖尿病的治疗和预防 并发症（肾病，视网膜病变），血管生成，哮喘支气管炎，慢性肾功能衰竭，肝硬化，限制性记忆能力或受限的学习能力。

    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    6.
    发明授权
    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
    4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途

    公开(公告)号：US07202278B2

    公开(公告)日：2007-04-10

    申请号：US10920395

    申请日：2004-08-18

    申请人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    发明人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    IPC分类号： A61K31/165 ,  A61K31/495 ,  A61K31/44 ,  A61K31/195

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： A method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan- 2-yl benzamide according to the formula (I) to the said mammal. Compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.

    摘要翻译： 一种刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括给予生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺，

    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    7.
    发明授权
    4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
    4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途

    公开(公告)号：US06812253B2

    公开(公告)日：2004-11-02

    申请号：US10623775

    申请日：2003-07-22

    申请人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    发明人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    IPC分类号： A61K31165

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： The present invention relates to the method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan-2-yl benzamide according to the formula (I) to the said mammal. Compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.

    摘要翻译： 本发明涉及刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括将生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺给予 哺乳动物说 化合物（I）可用于治疗和预防心血管疾病如稳定和不稳定性心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化， PTCA后的再狭窄，内皮损伤，原发性高血压，肺动脉高压，继发性高血压，肾血管性慢性肾小球肾炎，勃起功能障碍，室性心律失常，以及降低绝经后妇女心血管危险或摄入避孕药后，治疗和预防糖尿病和糖尿病并发症 （肾病，视网膜病变），血管发生，支气管哮喘，慢性肾功能衰竭，肝硬化，受限的记忆力或受限的学习能力。

    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them
    10.
    发明授权
    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，其用途和含有它们的药物组合物

    公开(公告)号：US06794365B2

    公开(公告)日：2004-09-21

    申请号：US09790641

    申请日：2001-02-23

    申请人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： C07K506

    CPC分类号： C07D213/56 ,  A61K38/00 ,  C07C257/18 ,  C07C279/14 ,  C07C2601/14 ,  C07K5/0202 ,  C07K5/06026 ,  C07K5/06034

    摘要： The present invention relates to new malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula I, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

    摘要翻译： 本发明涉及式I的新型丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和R（6） 索赔。 式I化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，使用式I化合物治疗和预防可治疗的疾病 或通过抑制诸如血栓栓塞性疾病的因子Xa活性来防止，以及式I化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式I化合物的组合物，其与惰性载体混合或以其它方式结合，特别是含有式I化合物与药学上可接受的载体物质和辅助物质的药物组合物。