公开(公告)号：US08044050B2

公开(公告)日：2011-10-25

申请号：US12548641

申请日：2009-08-27

Applicant: Gerhard Zoller ,  Hartmut Strobel ,  David William Will ,  Paulus Wohlfart

Inventor： Gerhard Zoller ,  Hartmut Strobel ,  David William Will ,  Paulus Wohlfart

IPC: A61K31/5025 ,  A61K31/519 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/4188 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519

Abstract: The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Abstract translation: 本发明涉及式I的咪唑并[1,2-a]吖嗪衍生物，其中R，R 1至R 3，X，Y和n具有权利要求中所示的含义，其调节内皮一氧化氮的转录（ NO）合酶，是有价值的药理活性化合物。 具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下使用。 本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及式I化合物用于刺激内皮NO合成酶表达或用于治疗各种疾病，包括心血管疾病 例如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。

公开(公告)号：US20100183712A1

公开(公告)日：2010-07-22

申请号：US12748951

申请日：2010-03-29

Applicant: Hartmut STROBEL ,  Paulus WOHLFART ,  Alena SAFAROVA ,  Armin WALSER ,  Teri SUZUKI ,  Karl SCHÖNAFINGER ,  Ramalinga M. DHARANIPRAGADA

Inventor： Hartmut STROBEL ,  Paulus WOHLFART ,  Alena SAFAROVA ,  Armin WALSER ,  Teri SUZUKI ,  Karl SCHÖNAFINGER ,  Ramalinga M. DHARANIPRAGADA

IPC: A61K9/48 ,  A61K9/36 ,  A61P9/00 ,  A61P9/04 ,  C07C233/01 ,  A61K31/165 ,  C07D241/38 ,  A61K31/498 ,  C07D471/02 ,  A61K31/437

CPC classification number: 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

Abstract: 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.

Abstract translation: 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 。

公开(公告)号：US20100016272A1

公开(公告)日：2010-01-21

申请号：US12486117

申请日：2009-06-17

Applicant: Hartmut STROBEL ,  Paulus WOHLFART ,  Heinz-Werner KLEEMANN ,  Gerhard ZOLLER ,  David William WILL

Inventor： Hartmut STROBEL ,  Paulus WOHLFART ,  Heinz-Werner KLEEMANN ,  Gerhard ZOLLER ,  David William WILL

IPC: A61K31/4709 ,  C07D401/06 ,  C07D267/10 ,  A61K31/496 ,  A61K31/553 ,  A61K31/397 ,  A61P25/00 ,  A61P9/00 ,  A61P3/00

CPC classification number: C07D213/56 ,  C07D213/64 ,  C07D213/73 ,  C07D213/75 ,  C07D215/12 ,  C07D233/64 ,  C07D233/68 ,  C07D239/26 ,  C07D277/30 ,  C07D277/46 ,  C07D333/24 ,  C07D333/60 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

Abstract: The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Abstract translation: 本发明涉及式I的杂芳基丙烯酰胺，其中Het，X，Ra，Rb，R 1，R 2和R 3具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理学 活性化合物。 具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。 本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于 治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

公开(公告)号：US20090239915A1

公开(公告)日：2009-09-24

申请号：US12412481

申请日：2009-03-27

Applicant: Gerhard ZOLLER ,  Hartmut STROBEL ,  David William WILL ,  Paulus WOHLFART

Inventor： Gerhard ZOLLER ,  Hartmut STROBEL ,  David William WILL ,  Paulus WOHLFART

IPC: A61K31/4245 ,  C07D235/18 ,  A61K31/4184 ,  C07D413/10 ,  A61P9/00

CPC classification number: C07D235/18 ,  C07D413/04

Abstract: The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Abstract translation: 本发明涉及式I的2-苯基 - 苯并咪唑的衍生物，其中X，R，R 1至R 3和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录，并且是 有价值的药理活性化合物。 具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。 本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于 治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。

公开(公告)号：US07351703B2

公开(公告)日：2008-04-01

申请号：US10957980

申请日：2004-10-05

Applicant: Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

Inventor： Ursula Schindler ,  Karl Schoenafinger ,  Hartmut Strobel

IPC: A01N43/00 ,  A01N41/06 ,  A01N37/12 ,  A01N37/44 ,  A61K31/55 ,  A61K31/54 ,  A61K31/535 ,  A61K31/4965 ,  A61K31/18 ,  A61K31/195

CPC classification number: C07F9/4056 ,  C07C311/21 ,  C07D207/27 ,  C07D207/325 ,  C07D207/404 ,  C07D209/08 ,  C07D209/48 ,  C07D215/48 ,  C07D217/02 ,  C07D217/24 ,  C07D231/56 ,  C07D235/18 ,  C07D241/20 ,  C07D249/18 ,  C07D295/135 ,  C07D295/192 ,  C07D307/91 ,  C07D311/16 ,  C07D317/60 ,  C07D409/04 ,  C07F9/3882

Abstract: The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular disorders 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. The invention relates to the use of compounds of the formula I for the therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, novel compounds of the formula I, pharmaceutical preparations comprising them and processes for their preparation.

Abstract translation: 本发明涉及式Ⅰ化合物，其中A 1，A 2，R 2，R 3和R 3 >具有权利要求书中所示的含义，其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，心脏功能不全，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。 本发明涉及式I化合物用于治疗和预防指定疾病状态及其制备药物的用途，式I化合物，包含它们的药物制剂及其制备方法。

公开(公告)号：US20080021029A1

公开(公告)日：2008-01-24

申请号：US11627515

申请日：2007-01-26

Applicant: Hartmut Strobel ,  Sven Ruf ,  Dominique Lesuisse ,  Conception Nemecek ,  Youssef El-Ahmad ,  Jacques Mauger ,  Stefan Guessregen ,  Kurt Ritter ,  Jean-Luc Malleron

Inventor： Hartmut Strobel ,  Sven Ruf ,  Dominique Lesuisse ,  Conception Nemecek ,  Youssef El-Ahmad ,  Jacques Mauger ,  Stefan Guessregen ,  Kurt Ritter ,  Jean-Luc Malleron

IPC: A61K31/506 ,  A61K31/4709 ,  A61K31/5377 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00 ,  A61P25/00 ,  A61P3/00 ,  A61P3/10 ,  A61P35/00 ,  A61P37/08 ,  A61P7/00 ,  C07D215/58 ,  C07D401/02 ,  C07D413/14 ,  C12N9/99

CPC classification number: C07D401/06 ,  C07D409/14

Abstract: The disclosure relates to the novel compounds of formula (I): wherein R1, R2, R2′, R3, R3′, p, A, B, Y, Y1, and Y2 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.

Abstract translation: 本公开涉及新的式（I）化合物：其中R 1，R 2，R 2，R 3，R 3， p，A，B，Y，Y 1和Y 2具有本说明书中给出的含义及其盐，包含所述化合物的药物组合物及其用途为 蛋白激酶抑制剂。

公开(公告)号：US20070082897A1

公开(公告)日：2007-04-12

申请号：US11548501

申请日：2006-10-11

Applicant: Hartmut STROBEL ,  Paulus WOHLFART ,  Alena SAFAROVA ,  Armin WALSER ,  Teri SUZUKI ,  Karl SCHONAFINGER ,  Ramalinga DHARANIPRAGADA

Inventor： Hartmut STROBEL ,  Paulus WOHLFART ,  Alena SAFAROVA ,  Armin WALSER ,  Teri SUZUKI ,  Karl SCHONAFINGER ,  Ramalinga DHARANIPRAGADA

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/517 ,  A61K31/498 ,  A61K31/497 ,  A61K31/4709 ,  A61K31/428 ,  A61K31/423 ,  C07D417/02 ,  C07D413/02

CPC classification number: 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

Abstract: 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.

Abstract translation: 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 。

公开(公告)号：US07202278B2

公开(公告)日：2007-04-10

申请号：US10920395

申请日：2004-08-18

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

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

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

CPC classification number: C07C233/65 ,  A61K31/166 ,  C07C2602/08

Abstract: 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.

Abstract translation: 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，

公开(公告)号：US06913898B2

公开(公告)日：2005-07-05

申请号：US10268533

申请日：2002-10-10

Applicant: Ursula Schindler ,  Hartmut Strobel ,  Peter Schindler ,  Alexander Muelsch

Inventor： Ursula Schindler ,  Hartmut Strobel ,  Peter Schindler ,  Alexander Muelsch

IPC: G01N33/50 ,  C12Q1/32 ,  C12Q1/527 ,  C12Q1/66 ,  G01N21/78

CPC classification number: C12Q1/527 ,  G01N2333/795 ,  G01N2500/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06844347B1

公开(公告)日：2005-01-18

申请号：US09762893

申请日：1999-08-04

Applicant: Ursula Schnidler ,  Karl Schoenafinger ,  Hartmut Strobel

Inventor： Ursula Schnidler ,  Karl Schoenafinger ,  Hartmut Strobel

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/16 ,  A61P3/08 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D239/30 ,  C07D239/36 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D521/00 ,  A61K31/50

CPC classification number: C07D239/30 ,  C07D231/12 ,  C07D233/56 ,  C07D239/36 ,  C07D239/42 ,  C07D249/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/04 ,  C07D417/04

Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.

Abstract translation: 本发明涉及式I化合物，其中R 1，R 2，R 3和R 4具有权利要求中给出的含义。 所述化合物是用于治疗和预防疾病的有价值的活性成分，例如高血压，心绞痛，心力衰竭，血栓形成或动脉粥样硬化等心血管疾病。 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cGMP平衡受损相关的疾病。 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。