Abstract: Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.

Abstract: Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.

Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.

Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Abstract: The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.

Abstract: The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.

Abstract: The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.

Abstract: The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.

Abstract: Steroids are well known, medicinal relevant, chemical entities. There are numerous steroids which have fully or partially reduced ‘A’ rings. These fully or partially reduced ‘A’ rings have been reduced in the past through Birch and other dissolving metal reductions. Novel reducing conditions for steroid substrates are described which utilizes stabilized alkali metal-silica gel materials. The invention relates to a method for reducing a double bond within a steroid by contacting an unsaturated steroid having a phenyl ring with a Stage 0 or Stage I alkali metal-silica gel material in the presence of a proton source under reaction conditions sufficient to form a reduced steroid having a diene structure.

Abstract: 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.

Abstract: 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.

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

Abstract: The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.

Abstract: The present invention is directed to a compound of Formula (I) or a form thereof: wherein U, V, W and Ring A are as defined herein, useful as vasopressin receptor antagonists.

Abstract: 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.

Abstract: 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.

Abstract: The invention is directed to novel isonipecotamide derivatives of Formula (I): 1

Abstract: The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): 1

Abstract: 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.

Abstract: Anticonvulsant compounds of the general formula I: where X, R1, R2, R3, R4, R5, and R6 are as herein defined; are useful in treating acute ischemia-induced neurodegeneration, such as occurs during and after stroke, head trauma, spinal injury, non-fatal cardiac arrest, or major surgical procedures. Furthermore, pharmaceutical compositions containing a compound of formula I as well as methods for their use are disclosed.