Chiron Corporation

Novartis Ag

Novartis Vaccines & Diagnostics, Gmbh

David Duhl

Paul A Renhowe

Paul Andrew Barsanti

Annette Olga Walter

Rustum S Boyce

Tinya Abrams

Kris Mendenhall

Daniel T Chu

Weibo Wang

Savithri Ramurthy

Sharadha Subramanian

Ryan N Constantine

Nathan Brammeier

Megan C Phillips

Hong Yang

Mark Knapp

Sabina Pecchi

Yi Xia

Kenneth Walter Bair

Eric J Martin

Rama Jain

Liana Marie Lagniton

Elisa Jazan

Elizabeth J Mieuli

Rustum Boyce

Anu Sharma

Kelly Wayman

Vincent P Le

Kay Huh

Bryan H Chang

Michel Faure

Yia Xia

Kirk William Johnson

David C Myles

Cheng Hu

Zhi-Jie Ni

Wooseok Han

Yue Pan

Yu Ding

Song Leng

Juliet Welch

Val Sheffield

Liana Marie Lagnition

Susan W Gorman

Choi Ying Chiu

Arwen E Adams

Xia Yia

Effie Tozzo

Kris G Mendenhall

Annette O Walter

Tinya J Abrams

Nathan M Brammeier

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

The invention provides novel compounds having a substituted imidazole ring, and methods of using such compounds for the treatment of certain disorders such as hematological cancers and solid tumors. The compounds of the invention are tri-substituted imidazole derivatives that inhibit KSP. These compounds are also useful for the treatment of drug resistant tumors, such as solid tumors that express elevated levels of P-glycoprotein.

Kinesin inhibitors as cancer therapeutics

The present invention provides triazole compounds of Formula I: 

Triazole compounds as KSP inhibitors

Substituted imidazole derivatives

Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof: 

Substituted pyrazole and triazole compounds as KSP inhibitors

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

Substituted imidazole compounds as KSP inhibitors

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

The present invention is a novel nucleic acid sequence which hybridizes to SEQ ID NO:6 or fragments thereof under stringent conditions, or fragments thereof. The invention also includes diagnostic assays, expression vectors, control sequences, antisense molecules, ribozymes, and host cells to express the polypeptide encoded by the nucleic acid sequence. The present invention also includes claims to the polypeptide sequence coded by the nucleic acid sequences.

Polynucleotides that hybridize to DP-75 and their use

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.

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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Oakland, CA, United States of America

David Duhl