University of Missouri

University of Medicine and Dentistry of New Jersey

Other

Rutgers, the State University of New Jersey

Avon Products, Inc.

Philadelphia Health and Education Corporation

William J Welsh

Anil Nair

Seong Jae Yu

Youyi Peng

Ni Ai

Sonia Arora

Qiang Zhang

Susan M Keenan

Xin Wang

Randy J Zauhar

Richard Delarey Wood

John W Lyga

Uma Santhanam

Sandhya Kortagere

Lawrence W Bergman

Raymond B Birge

Akhil Vaidya

Kamlendra Singh

Ching Y Wang

Sean Ekins

Stanley G Kimani

Thomas Walter Comollo

Nina Ching Y Wang

Vladyslav Kholodovych

Raymond Birge

Certain compounds of formula I: I and salts including pharmaceutically acceptable salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using a compound of formula I. 

Aryl and heteroaryl amides for use as anti-proliferative, anti-thrombotic, and anti-viral agents

The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.

Glutamate receptor modulators and therapeutic agents

Substituted triazole compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a pathology linked to a hyperproliferative disorder by administering the substituted triazole compounds to a patient in need thereof.

Anti-mitotic anti-proliferative compounds

Methods for preventing or treating an Apicomplexan parasite infection in a patient administering to a patient in need thereof an effective amount of a compound of Formulas I-IV.

Mechanism-based small-molecule parasite inhibitors

A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and OR; R2 is selected from H, OH, and (C&#x2550;O) (C)alkyl; Ris (C)alkyl or (C&#x2550;O)(C)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.

Estrogen receptor modulators and uses thereof

The disclosure relates to novel topical lightening compositions a skin depigmenting agent and a vehicle. There is provided a topical lightening composition comprising a substituted-4-oxobutanoic acid, ester, or amide tyrosinase inhibitor, and a vehicle. The depigmenting agents of this disclosure can be used as such or as a pharmaceutically acceptable salt including conventional non-toxic salts which include a metal salt or an alkaline earth metal salt, an ammonium salt, or an organic base salt. The depigmenting agents of this disclosure can be incorporated into any cosmetically-, dermatologically-, or cosmeticatically-acceptable vehicle or carrier normally used for topical application. The compositions and methods of the disclosure are effective to lighten skin, hair, lips, and/or nails.

Topical lightening composition and uses thereof

The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds. Diseases and disorders contemplated include, inter alia, diseases and disorders of the central nervous system, the peripheral nervous system, the gastrointestinal system, the circulatory system, skin, retina, brain, heart, and lungs.

Methods related to the generation of shape signatures representing molecular shape, and using shape signatures in both ligand-based and receptor-based molecular design. Ray-tracing is used to explore the volume interior to a ligand, or the space exterior to a receptor site. Shape signatures are then probability distributions derived from the ray-traces. Shape signatures provide condensed descriptors of shape properties readily compared to each other to test for shape similarity or complementarity.

Computer aided ligand-based and receptor-based drug design utilizing molecular shape and electrostatic complementarity

Opioid receptor compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a condition mediated by an opioid receptor by administering an effective amount of the opioid receptor compound to a patient in need thereof.

Opioid receptor subtype-selective agents

A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and OR; R2 is selected from H, OH, and (C&#x2550;O)(C)alkyl; Ris (C)alkyl or (C&#x2550;O)(C)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented. 

The invention provides compounds of formula I: wherein Rto Rand n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.

Opioid receptor active compounds

Novel compounds which selectively bind to the &#x3b4;-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with selectivity for the &#x3b4;-opioid receptor have shown promise in providing enhanced analgesis without the addictive properties, the compounds of the present invention are better than morphine, naltrindole (NTI), spiroindanyloxymorphone (SIOM), and other known &#x3bc;-opioid receptor selectors as analgesics.

Growing community of inventors

New Brunswick, NJ, United States of America

William J Welsh