Ortho-mcneil Pharmaceutical Corp.

Janssen Pharmaceutica Nv

Ortho Pharmaceutical Corporation

Mcneil Ab

Other

Michael J Costanzo

Bruce E Maryanoff

Stephen C Yabut

William Joel Hoekstra

Philip J Rybczynski

Han-Cheng Zhang

Keith T Demarest

Mona Patel

Brett A Tounge

Min Amy Xiang

Joseph Gunnet

Richard Look

Edward Charles Lawson

Richard P Shank

Bruce E Maryanoef

William J c/o Ortho-Mcneil Pharmaceutical Inc Hoekstra

Min A Xiang

The present invention is directed to a compound of Formula (I): or a form thereof, wherein X, X, X, X, R, Rand Rare as defined herein, useful as tryptase inhibitors.

Spiropiperidines for use as tryptase inhibitors

The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal insufficiency, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

Substituted spiroheterocycles

The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

The invention is directed to novel isonipecotamide derivatives of Formula (I): which are useful in treating integrin-mediated disorders.

Isonipecotamides for the treatment of integrin-mediated disorders

The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

Peptidyl heterocyclic ketones useful as tryptase inhibitors

The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): useful as integrin antagonists and methods for the treatment of integrin-mediated disorders.

Quinazoline and quinazoline-like compounds for the treatment of integrin-mediated disorders

Tricyclic monosaccharide derivatives useful in treating acute ischemia-induced neurodegeneration

This invention relates to methods ands compositions for bringing about changes in skin pigmentation and for treating inflammatory disorders. More particularly, this invention relates to compounds which affect melanogenesis and can be used as depigmenting agents or as agents for darkening skin utilizing the PAR-2 pathway and compounds for the, prevention and treatment of immunomediated inflammatory diseases, particularly those associated with the respiratory tract, such as asthma and allergic rhinitis.

Methods for treating immunomediated inflammatory disorders

Carboxamide derivatives of pyrrolidine, piperidine, and hexahydroazepine of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.

Carboxamide derivatives of piperidine for the treatment of thrombosis

Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.

Peptidyl heterocycles useful in the treatment of thrombin related

Sulfamate derivatives having the following formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as herein defined, have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, the present invention encompasses pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.

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Ivyland, PA, United States of America

Michael J Costanzo