Bristol-myers Squibb Compnay

Bristol Meyers Squibb Company

Pfizer Ireland Pharmaceuticals

Gene Michael Dubowchik

John E Macor

Xiaojun Han

Guanglin Luo

Ling Chen

Prasad V Chaturvedula

R Michael Lawrence

Dasa Lipovsek

Prasanna Sivaprakasam

Claudio Mapelli

Graham S Poindexter

Paul E Morin

Andrew P Degnan

Vivekananda M Vrudhula

Michael C Myers

Olafur S Gudmundsson

Cort S Madsen

George O Tora

Bireshwar Dasgupta

Xiang Jun J Jiang

Rita Civiello

Swanee E Jacutin-Porte

Dolatrai M Vyas

Raymond A Firestone

Richard A Hartz

Stephen E Mercer

Vijay T Ahuja

Jonathan L Ditta

George N Karageorge

Dmitry S Zuev

David Paul Provencal

Allen B Reitz

Stephen R Bertenshaw

Jeffrey Claude Pelletier

Dalton King

Haiquan Fang

Derek John Denhart

Senliang Pan

Shikha Vig

Charles M Conway

Charles Mark Conway

The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

Methods of treating kidney failure, and/or improving or stablizing renal function using modified relaxin polypeptides

Treatment of fibrosis, cardiovascular disease and heart failure with modified relaxin polypeptides

Disclosed are prodrugs of CGRP antagonists, methods of treating CGRP related disorders, e.g., migraine, by administering to a patient in need thereof the prodrugs, pharmaceutical compositions comprising prodrugs and kits including the pharmaceutical compositions and instructions for use.

Prodrugs of CGRP antagonists

Modified relaxin polypeptides comprising a pharmacokinetic enhancer and pharmaceutical compositions thereof

Method of treating cardiovascular disease and heart failure with modified relaxin polypeptides

The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3. 

Pyrimidine carboxamides as GSK-3 inhibitors

The disclosure generally relates to compounds of formula (I), including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3. 

GSK-3 inhibitors

Modified relaxin polypeptides comprising a pharmacokinetic enhancer and uses thereof

The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system. 

Substituted pyridine derivatives useful as GSK-3 inhibitors

The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD). 

CGRP receptor antagonists

The disclosure generally relates to the compound of formula I, (R)&#x2014;N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)piperazin-1-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide, including pharmaceutically acceptable salts, which is a CGRP-receptor antagonist. The disclosure also relates to pharmaceutical compositions and methods for using the compound in the treatment of CGRP related disorders including migraine headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and cancer. 

CGRP receptor antagonist

The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors ('CGRP-receptor'), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

Anti-migraine spirocycles

Growing community of inventors

Middlefield, CT, United States of America

Gene Michael Dubowchik