The present invention relates to compounds represented by the formula [I] and salts thereof, wherein R.sup.1 and R.sup.5 each represents carboxyl, phosphonic or a derivative thereof; R.sup.2 represents hydrogen, lower alkyl, (substituted) phenyl lower alkyl, lower alkoxy or (substituted) phenyl lower alkoxy; R.sup.3 represents lower alkyl or (substituted) phenyl lower alkyl; and R.sup.4 represents a group represented by the formula [XI], [XII] or [XIII]. The compounds of the present invention have endopeptidase 24.11 inhibitory activity and are useful for treating cardiovascular diseases such as heart failure and hypertension, renal diseases such as renal failure, gastroenteric disorders such as diarrhea and hyperchlorhydria, endocrine and metabolic diseases such as obesity, and autoimmune diseases such as rheumatic disease, and for mitigating myosalgia, migraine, etc.

Santen Pharmaceutical Co., Ltd.

1,3-dialkylurea derivative

A method of treating, preventing or inhibiting a disorder selected from the group consisting of cardiovascular or heart related diseases such as stroke, hypertension, tachycardia, and congestive heart failure, osteoporosis, premature birth, psychosocial dwarfism, stress-induced fever, ulcer, diarrhea, post-operative ileus, and colonic hypersensitivity associated with psychopathological disturbance and stress, comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of the formula ##STR1##or a pharmaceutically acceptable salt thereof, wherein A, B, D, E, Y, Z, R.sub.3, R.sub.4, and R.sub.5 are as defined herein.

Pfizer Inc

Corticotropin releasing factor antagonists

Disclosed are novel methods of antagonizing the A.sub.1 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the formula: ##STR00001## wherein R.sup.1 is optionally substituted C.sub.1-14 alkyl; Y is C.sub.1-14 alkylene; and Z is phenyl that is optionally substituted with halo, hydroxy, amino, cyano, or optionally substituted C.sub.1-4 alkyl or a pharmaceutically acceptable salt, ester, or prodrug thereof. The A.sub.1 adenosine receptors are antagonized in order to treat a disease state is chosen from renal failure, renal dysfunction, nephritis, hypertension, edema, Alzheimers disease, stress, depression, cardiac arrhythmia, restoration of cardiac function, congestive heart failure, diabetes, asthma, respiratory disorders, ischemia-induced injury of the brain, heart and kidney, and diarrhea.

CV Therapeutics, Inc.

A1 adenosine receptor antagonists

Compounds of the formula ##STR1## wherein Y is O or NH and X is ##STR2## will inhibit the action of neutral endopeptidase. As a result, such compounds produce diuresis, natriuresis, and lower blood pressure as well as being useful in the treatment of congestive heart failure, relieving pain, and diarrhea when administered to a mammalian host.

E. R. Squibb &amp; Sons, Inc.

Phosphonate and phosphonamide endopeptidase inhibitors

The present invention related to compounds represented by the following formula (I) and salts thereof, ##STR1## wherein R.sup.1 and R.sup.4 each represents a carboxyl or a carboxyl which is converted into an ester, an amide or hydroxamic acid; R.sup.2 represents a lower alkyl or a phenyl-lower alkyl; R.sup.3 represents a hydrogen atom, a lower alkyl, an amino-lower alkyl, a lower alkylamino-lower alkyl, a hydroxy-lower alkyl, a mercapto-lower alkyl, a carboxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an imidazolyl-lower alkyl, an indolyl-lower alkyl, a (substituted) phenyl group, a (substituted) phenyl-lower alkyl group, a (substituted) naphthyl group, or a (substituted) naphtyl-lower group. The compounds of the present invention have inhibitory effects on endopeptidase 24.11 and are useful as therapeutic agents for cardiovascular disease such as heart failure and hypertension, renal disease such as renal failure, gastroenteric disorder, such as diarrhea and hyperchlorhydria, endocrine and metabolic disease such as obesity, and autoimmune disease such as rheumatism, and as an analgesics for myosalgia and migraine.

heart failure/diarrhea

1,3-dialkylurea derivative

Corticotropin releasing factor antagonists

A1 adenosine receptor antagonists

Phosphonate and phosphonamide endopeptidase inhibitors

1,3-dialkylurea derivatives having a hydroxyl group

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