Abstract: Novel acylated amino acids which are antagonists of endothelin are described. Methods for their preparation and pharmaceutical compositions containing them are also included. The compounds are expected to be useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, diabetes, head injury, and stroke.

Abstract: The invention concerns novel renin-inhibitory compounds which contain an amino-substituted heterocycle at the P.sub.2 position. These are useful for treating renin-associated hypertension, congestive heart failure, glaucoma, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the compounds, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.

Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.

Abstract: The invention concerns novel renin-inhibitory compounds which contain an amino-substituted heterocycle at the P.sub.2 position. These are useful for treating renin-associated hypertension, congestive heart failure, glaucoma, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the compounds, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.

Abstract: The invention concerns novel renin-inhibitory compounds which contain a tetrahydroisoquinoline or similar heterocycle at the P.sub.3 position. These are useful for treating hypertension, congestive heart failure, glaucoma, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I, -II and -III. Processes for preparing the compounds, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.

Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.

Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma, and diseases caused by retroviruses including HTLV-I, -II, -III. Processes for preparing the peptides, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.

Abstract: Novel substituted derivatives of 3-amino-2-hydroxypropionic acid are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as renin inhibitors and thus useful in controlling hypertension, hyperaldosteronism and congestive heart failure as well as diagnostic agents.

Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.

Abstract: Novel N.sup.6 -substituted-5'-oxidized adenosine analogs, and pharmaceutical compositions, methods of use or processes to make therefor. The novel adenosines have utility for the treatment of hypertension, coronary insufficiency, psychosis, pain, angina, and heart failure.

Abstract: Novel N.sup.6 -substituted adenosines having desirable ratio of affinities at A1 or A2 receptors and highly desirable central nervous system and cardiovascular activities, such as analgesic, antipsychotic, sedative, or antihypertensive as well as immunoinflammatory activity.

Abstract: The present invention is various novel diallyl analogs of xanthine. Additionally, the invention is pharmaceutical compositions having as the active compound diallyl analogs of xanthines and methods of use therefor. Processes of preparation of diallyl analogs of xanthine are also the invention. The use of the analogs relates particularly to a desirable affinity at adenosine receptors, particularly the A.sub.1 receptor. The analogs are adenosine receptor antagonists. The analogs, thus, for example provide activity for use as a CNS stimultant cognition activator, antifibrillatory agent, and bronchodilator.

Abstract: Method for treating congestive heart failure by administration of N.sup.6 -[(1,2-dihydro-1-acenaphthylenyl)-methyl]adenosine or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is a novel disubstituted derivative of xanthine, pharmaceutical composition and method of use therefor. Activity of the novel xanthine includes particularly cognition activation.

Abstract: The present inventions are novel N.sup.6 -substituted adenosines wherein the N substituent is ##STR1## wherein Ar is an unsubstituted or substituted (1) phenyl, (2) 1- or 2-naphthalenyl, (3) 2- or 3-thienyl, (4) 2- or 3-furanyl, (5) 2-, 4-, or 5-thiazyl, (6) 2-, 3-, or 4-pyridyl, or (7) 2-pyrimidyl wherein the substituents include at least one of lower alkyl, halo, trifluoromethyl, hydroxy, lower alkoxy, lower acyloxyamino, N-lower monoalkyl or N,N-lower dialkylamino, lower thioalkyl, lower alkylsulfonyl, or nitro and R' is hydrogen or alkyl, A is ##STR2## wherein q, q', or q" are one to four, n and m are independently zero to three provided if A is a bond then n and m is at least 2 and if A is other than a bond then n and m is at least one. These novel adenosines have highly desirable central nervous system and cardiovascular activities and therefore the present invention also includes pharmaceutical compositions and methods of use therefor.

Abstract: Novel N.sup.6 -substituted-5'-oxidized adenosine analogs, and pharmaceutical compositions, methods of use or processes to make therefore. The novel adenosines have utility for the treatment of hypertension, coronary insufficiency, psychosis, pain, angina, and heart failure.

Abstract: N.sup.6 -Acenaphthyl adenosines and analogs thereof and pharmaceutically acceptable acid addition salts having highly desirable blood pressure lowering properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.

Abstract: The present invention relates to novel 5-substituted pyrazolo[4,3-d]pyrimidine-7-one compounds, and compositions, methods of use and processes to make therefor. The novel compounds are useful in the treatment of cardiovascular disorders, such as heart failure or cardiac insufficiency. The novel compounds bind adenosine receptors and selectively inhibit phosphodiesterase.

Abstract: Various novel analogs of pyrazolo[4,3d]pyrimidine-5,7-(4H,6H)diones and also 5-thione-7-ones, novel methods of synthesis therefor, compositions and uses are the present invention. For example, the novel 5,7-diones and 5-thione-7-ones are useful for stimulating the central nervous system reversing bronchoconstriction, and as cardiac stimulants cardiotonic agents.

Abstract: N.sup.6 -Dihydroxypropyladenosines and pharmaceutically acceptable acid addition salts having highly desirable central nervous system properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.