摘要:
The present invention relates to acylamino-substituted heteroaromatic compounds of the formula (I), in which R1, R2, R3, R4 and R5 and X have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmaceutically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要:
The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines of the formula I, (I) in which A, R1, R2, R3, R4, R5 and n have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要:
The invention relates to compounds of formula (I), wherein A?1, A2, R2 and R3¿ have the meanings cited in the claims. Said compounds are valuable pharmaceutical active substances for the treatment and prophylaxis of diseases, e.g. cardiovascular diseases such a hypertension, angina pectoris, heart failures, thrombosis or atherosclerosis. The compounds of formula (I) have the ability of modulating endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for treatment and prophylaxis of pathological states associated with cGMP metabolic disorders. The invention also relates to the use of compounds of formula (I) for treatment and prophylaxis of the above-mentioned pathological states and for producing corresponding medicaments, to pharmaceutical preparations containing said compounds and to a method of production.
摘要:
The present invention relates to acylated arylcycloalkylamines of the formula I, in which R1, R2 and n have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要:
The present invention relates to compounds of formula (I) wherein R?1, 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:
The present invention relates to acylated indanyl amines according to the general formula (I) where R1-R4 have the meanings given in the description, A is CH¿2? CHOH or CH-(C1-C3-alkyl), B is CH2 or CH-(C1-C3-alkyl), and R?5¿ 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, Prinymetal angina, actue coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothel 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:
The invention relates to substituted isoindolon derivatives of formula (I), wherein R?1, R2, R3, R4, R5, R6 and R7¿ have the meanings cited in the description. Said derivatives represent valuable active substances in medicaments for the therapy and prophylaxis of diseases, e.g. cardiovascular diseases such a hypertension, angina pectoris, heart failures, thrombosis or atherosclerosis. The compounds of formula (I) are capable of modulating endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of pathological states associated with disorders of the cGMP metabolism. The invention also relates to a method for the production of compounds of formula (I), their use in the therapy and prophylaxis of the above-mentioned pathological states and in the production of medicaments for such states. The invention further relates to pharmaceutical preparations containing the compounds of formula (I).
摘要:
The invention relates to a method for the detection of a soluble guanylate cyclase, whose haem iron is present in a trivalent oxidation state and a method for detecting chemical substances which stimulate the activity of soluble guanylate cyclase when said haem iron present in soluble guanylate cyclase is at least in part trivalently oxidized. Said invention also relates to a diagnostic agent for detecting a soluble guanylate cyclase containing trivalent haem iron.
摘要:
The invention relates to inventive compounds of formula (I), wherein R?1, R2, R3¿ and Ar have the meanings cited in the claims. The inventive compounds are suitable for use in the production of medicaments, e.g. for prophylaxis and therapy of cardiovasular diseases such as hypertension, angina pectoris, heart failure, thromboses or arteriosclerosis. The compounds of formula (I) have a capacity for modulating endogenic production of cyclic guanosine monophosphate (cGMP) and are generally suitable for therapy and prophylaxis of pathological conditions linked to cGMP metabolism disorders.