Showing papers by "William N. Washburn published in 2005"

2-amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors

Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R 1 , R 2 , X, Y and Z are defined herein.

Addition of Benzylic and Allylic Organozinc and Grignard Reagents to Resin-Bound Imines To Provide α-Branched Secondary Amines Bearing a Wide Variety of Functional Groups. Utility in the Synthesis of β-3 Adrenergic Receptor Agonists

Abstract: Benzylic and allylic organozinc and Grignard reagents have been added to resin-bound imines to provide α-branched secondary amines. Many functional groups, including electrophilic groups, were compatible with this methodology. Three modulesa resin-bound primary amine, an aromatic aldehyde, and the organometallicwere independently varied to produce a combinatorial library of α-branched secondary amines designed as β-3 adrenergic receptor agonists.

2-Amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors

Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure [INSERT CHEMICAL STRUCTURE HERE] I or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X and Z are defined herein.

2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors

Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure [PLEASE INSERT CHEMICAL STRUCTURE HERE] I or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1 and R2 are defined herein.