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1. 发明授权

US08163751B2 Acylated indanyl amines and their use as pharmaceuticals 有权
标题翻译：酰化茚满胺及其作为药物的用途
公开(公告)号：US08163751B2
公开(公告)日：2012-04-24
申请号：US12748951
申请日：2010-03-29
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger , Ramalinga M. Dharanipragada
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger , Ramalinga M. Dharanipragada
IPC分类号： A61K31/495 , A61K31/44 , C07D241/36 , C07D513/02
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译：本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有在描述中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B是CH 2或CH- （C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征，心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药。

2. 发明授权

US06617359B2 4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
标题翻译： 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。

3. 发明授权

US07713963B2 Acylated indanyl amines and their use as pharmaceuticals 有权
标题翻译：酰化茚满胺及其作为药物的用途
公开(公告)号：US07713963B2
公开(公告)日：2010-05-11
申请号：US11548501
申请日：2006-10-11
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schoenafinger , Ramalinga M. Dharanipragada
IPC分类号： A61K31/541 , A61K31/5377 , C07D417/02 , C07D413/02
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译：本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有在描述中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B是CH 2或CH- （C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征，心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药。

4. 发明授权

US07202278B2 4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
标题翻译： 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，

5. 发明授权

US06812253B2 4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
标题翻译： 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。

6. 发明授权

US07179839B2 Acylated indanyl amines and their use as pharmaceuticals 有权
标题翻译：酰化茚满胺及其作为药物的用途
公开(公告)号：US07179839B2
公开(公告)日：2007-02-20
申请号：US10073160
申请日：2002-02-13
申请人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger
发明人： Hartmut Strobel , Paulus Wohlfart , Alena Safarova , Armin Walser , Teri Suzuki , Karl Schönafinger
IPC分类号： A61K31/357 , C07D317/46
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1–R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1–C3-alkyl), B is CH2 or CH—(C1–C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
摘要翻译：本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有说明书中给出的含义，A是CH CH 2或CH-（C 1 -C 3 - 烷基），B是CH 2或CH-（C（C 1 -C 3） C 1 -C 3烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征，心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常，糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药。

7. 发明申请

US20050054729A1 4-Fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
标题翻译： 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。

8. 发明授权

US07393849B2 Substituted sulfonamides and ureas useful for inhibiting kinase activity 失效
标题翻译：可用于抑制激酶活性的取代磺酰胺和脲
公开(公告)号：US07393849B2
公开(公告)日：2008-07-01
申请号：US11738733
申请日：2007-04-23
申请人： Pavel Safar , Armin Walser , Stephen James Shimshock
发明人： Pavel Safar , Armin Walser , Stephen James Shimshock
IPC分类号： A61K31/496 , A61K31/4545 , C07D211/06 , C07D241/04 , C07D401/04
CPC分类号： C07C257/18 , A61K38/00 , C07D209/42 , C07D211/62 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07K5/0207 , C07K5/021
摘要： Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:
摘要翻译：具有对Src激酶具有抑制作用的磺酰胺和脲化合物，包括其对映体，立体异构体和互变异构体，以及所述化合物的药学上可接受的盐或溶剂合物，所述化合物具有式II所示的一般结构，

9. 发明授权

US07223763B2 Substituted sulfonamides and ureas useful for inhibiting kinase activity 失效
标题翻译：可用于抑制激酶活性的取代磺酰胺和脲
公开(公告)号：US07223763B2
公开(公告)日：2007-05-29
申请号：US10835630
申请日：2004-04-30
申请人： Pavel Safar , Armin Walser , Stephen James Shimshock
发明人： Pavel Safar , Armin Walser , Stephen James Shimshock
IPC分类号： A61K31/496 , A61K31/4545 , C07D241/04 , C07D401/04 , C07D211/06
CPC分类号： C07C257/18 , A61K38/00 , C07D209/42 , C07D211/62 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07K5/0207 , C07K5/021
摘要： Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:
摘要翻译：具有对Src激酶具有抑制作用的磺酰胺和脲化合物，包括其对映体，立体异构体和互变异构体，以及所述化合物的药学上可接受的盐或溶剂合物，所述化合物具有式II所示的一般结构，

10. 发明授权

US06794365B2 Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them 有权
标题翻译：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。

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