Novartis Vaccines & Diagnostics, Gmbh

Chiron Corporation

Bryan H Chang

Daniel T Chu

Rustum S Boyce

Aaron Matthew Smith

Natalia Aurrecoechea

David Duhl

Aaron Smith

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

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

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.

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Concord, CA, United States of America

Bryan H Chang