Chiron Corporation

Novartis Vaccines & Diagnostics, Gmbh

Glaxosmithkline LLC

Rustum S Boyce

Daniel T Chu

David Duhl

Paul A Renhowe

Savithri Ramurthy

Kirk William Johnson

Bryan H Chang

John M Nuss

David B Ring

Keith Bruce Pfister

Aaron Matthew Smith

Allan S Wagman

Stephen David Harrison

Natalia Aurrecoechea

Lynn Seely

Sharadha Subramanian

Manoj C Desai

Dane A Goff

Weibo Wang

Barry Haskell Levine

Annette Olga Walter

Jason Daniel Speake

Xiaohui A Zhou

Sean P Brown

Hong Yang

Mark Knapp

Sabina Pecchi

Hongyan Guo

David C Myles

Paul Andrew Barsanti

Yi Xia

Stephen Andrew Thomson

Kenneth Walter Bair

Zhi-Jie Ni

Tinya Abrams

Eric J Martin

David Lee Musso

Rama Jain

James G Phillips

Michael Joseph Bishop

Ryan N Constantine

Elisa Jazan

Kris Mendenhall

Nathan Brammeier

Elizabeth J Mieuli

Megan C Phillips

Kelly Wayman

Anu Sharma

Kay Huh

Vincent P Le

Christopher R Conlee

Brian D Thompson

Kien S Du

Effie Tozzo

Liana Marie Lagnition

Kris G Mendenhull

Brian A Chauder

William R Swain

Xia Yia

Kevin K Barvian

Judith De Armas Kuntz

Aaron Smith

The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula: 

Substituted imidazole derivates

A variety of low molecular weight, guanidino-containing dihydroisoquinolinoines capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure ID where the values of the variable are defined herein. 

Substituted dihydroisoquinolinone compounds

A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure of Formulas (IA), (IB), or (IC): where the values of the variable are defined herein. 

Substituted pyrido [2,3-d] pyrimidinone compounds

A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein. 

Substituted quinazolinone compounds

The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula: 

Indole and benzimidazole derivatives

Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH, N, NR, C&#x2550;O, C&#x2550;S, S&#x2550;O, SO, S, O, (CRR), C(&#x2550;O)&#x2014;(CRR), and C(&#x2550;S)&#x2014;(CRR), where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S&#x2550;O, SO, C(O), NC(O), NC(S), OC(O), OC(S), C(NR), C(NOR), and a covalent bond. Z, Z, and Zare independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor ('MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.

Guanidino compounds

New pyridine-based compounds of Formula I, compositions, and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3-mediated disorders in vivo are provided. The methods, compounds, and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer. 

Inhibitors of glycogen synthase kinase 3

A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the formula IA and IB. IA and IB have the following structures where Z has the formula shown below and the rest of the variables are defined herein 

Quinazolinone compounds with reduced bioaccumulation

Compounds having the general structure III are provided: where D is N or C; W is selected from Z, Z, and Zare independently selected from CRand N; and the other variables have the values described herein. Compounds of formula III have useful properties for controlling diseases related to MC4-R action in humans including obesity and type II diabetes.

New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.

Compounds of formula IIA and IIB are novel guanidine compoundswhere the variables Rthrough Rhave the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.

Guanidinobenzamides

Compounds having the general structure II are provided:A is selected from the group consisting of C or CH and X and Y are independently selected from the group consisting of CH, N, C&#x2550;O, C&#x2550;S, (CRR), S&#x2550;O, SO, O, NR, S, C(&#x2550;O)&#x2014;(CRR), and C(&#x2550;S)&#x2014;(CRR)where n is 1, 2, or 3. W is selected from the group consisting ofand Z, Z, and Zare independently selected from the group consisting of substituted carbon and nitrogen. L is selected from the group consisting of N, O, S, S&#x2550;O, SO, C(O), NC(O), NC(S), OC(O), OC(S), C(NR), C(NOR), and a covalent bond. Compounds of formula II are agonists of the melanocortin-4 receptor ('MC4-R') and therefore may have useful properties for controlling diseases related to MC4-R action in humans, such as obesity and type II diabetes.

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San Francisco, CA, United States of America

Rustum S Boyce