University of Michigan

G.d. Searle & Company

Henry Mosberg

Donald W Hansen, Jr

Nizal S Chandrakumar

Sofya Tsymbalov

Karen B Peterson

Roger K Sunahara

Joseph Holoshitz

Aaron M Bender

Alvin H Schmaier

Yafei Jin

John Hilfinger

Song Ling

Richard Neubig

Deanna Montgomery

Sean Henry

Aubrie Harland

Katarzyna Sobczyk-Kojiro

Donna L Hammond

Anthony Nastase

Fernanda F Marques

Hauiling Zhong

Disclosed herein are compounds useful for modulating the mu-opioid receptor ('MOR') and/or delta-opioid receptor ('DOR'), and methods of using these compounds to treat diseases and conditions, such as pain. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: wherein the substituents are as described.

Peptidomimetics and methods of using the same

The present disclosure relates to methods and compositions for treating disease related to disorders of bone remodeling. In particular, the present disclosure relates to cyclic peptide compositions and methods for treating rheumatoid arthritis.

Methods and compositions for the treatment of arthritis

The invention provides a compound of formula (I), wherein Ris H, C(NH)NH, an amino acid, or a peptide; X is OH, NH, NHR, NRR, an amino acid, or a peptide; Rand Rare selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each Rand Ris independently H or CH; Z is 2-amino-2,3-dihydro-1H-indene-2-carboxylic acid; 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; or octahydro-1H-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that X is not NHwhen Ris H, Ris H, Ris CH, Z is Aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided. 

Compound and method for modulating opioid receptor activity

The invention relates to synthetic peptide analogs of D-Arg-Oic-Pro-Gly-Phe and methods of their use to inhibit human platelet aggregation, thrombosis and cell activation mediated by PAR1 and PAR4.

Synthetic peptide inhibitors of thrombin and thrombin activation of protease activated receptors 1 and 4

The present invention relates to novel inhibitors of G-protein signaling. In particular, the present invention provides peptide inhibitors of G protein signaling proteins and methods of using such inhibitors to modulate physiological effects of G protein signaling. The present invention thus provides novel drug targets for a variety of pathologies mediated by defects in G-protein signaling.

Inhibitors of RGS proteins

The present invention provides substituted cyclic tetrapeptide compounds of Formula I: ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, which are useful for treating pain in animals, pharmaceutical compositions which comprises a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Substituted cyclic tetrapeptides

The present invention provides substituted cyclic pentapeptide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable slats, esters and amides thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Substituted cyclic pentapeptides

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Ann Arbor, MI, United States of America

Henry Mosberg