Neurogen Corporation

Novartis Ag

Novartis International Pharmaceutical, Ltd.

H. Lundbeck A/s

Other

Pfizer Corporation

Bristol-myers Squibb Compnay

Jun Yuan

Alan J Hutchison

George D Maynard

Andrew Y Thurkauf

Xi Chen

Frederic Zecri

Pamela Ann Albaugh

Kevin S Currie

Raymond F Horvath

Kyungae Lee

John M Peterson

Manuka Ghosh

Philipp Grosche

Scott A Mitchell

Kenneth Shaw

Jan William Wasley

Guolin Cai

Kayo Yasoshima

George P Luke

Taeyoung Yoon

He Zhao

Linda M Gustavson

Linghong Xie

Bertrand Leo Chenard

Charles A Blum

John Louis Diener

David Juergen Wustrow

Hongbin Li

Spiros Liras

Marlys Hammond

Sarah Williams

Joseph P Yevich

Rajagopal Bakthavatchalam

Ronald J Mattson

David Weninger Barnes

Shari Lynn Caplan

Ken Yamada

Kevin J Hodgetts

Scott Louis Cohen

Richard Louis Elliott

Louise Clare Kirman

Qin Guo

Hongjuan Zhao

Nian Liu

Aimee Richardson Usera

Aaron Kanter

Alexandra Marshall Bruce

Changgang Lou

Guiying Li

Peter Hrnciar

Stanislaw Rachwal

Ling Hong Xie

Jianmin Mao

Martin Patrick Allen

Lawrence Albert Vincent

Zihong Guo

Alan J Hutchinson

Daniel Yohannes

David Barnes-Seeman

Vinod Kumar Singh

Xiaojun Liu

Christian Gampe

James Roache

Amy White

Arthur Nagal

Zhe-Quing Wang

Scott Capitosti

Carla Guimaraes

Derek John Denhart

Frédéric Zecri

David Ihle

Chikwendu Ibebunjo

Arlene S Eison

Eric Peters

Richard L Elliot

Carla Giumaraes

Avirup Bose

Alokesh Duttaroy

Vinod Singh

Xie Ling Hong

The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3:

Fatty acids and their use in conjugation to biomolecules

The disclosure relates to nucleic acids that contain modifications at the 5'-end, 3&#x2032;-end or 5&#x2032;-end and 3&#x2032;-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.

3' end caps, 5&#x2032; end caps and combinations thereof for therapeutic RNA

The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: 

The invention relates to novel compositions comprising modified apelin-13 peptide sequences designed to treat cardiovascular disease in subjects to whom they are administered, and which exhibit greater resistance to degradation, and equivalent or greater bioactivity than their wild type counterparts. The invention also relates to methods of making said compositions and using said compositions as pharmaceutically active agents to treat cardiovascular disease.

Synthetic linear apelin mimetics for the treatment of heart failure

The invention provides a synthetic polypeptide of Formula I (SEQ ID NO: 1):X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13&#x2003;&#x2003;I

Cyclic apelin derivatives for the treatment of heart failure

The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1):X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13&#x2003;&#x2003;I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention or bioconjugates thereof, and their therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Cyclic polypeptides for the treatment of heart failure

The invention provides a synthetic polypeptide of Formula I': X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Disulfide cyclic polypeptides for the treatment of heart failure

The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I' (SEQ ID NO: 1): or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein and a half-life extending moiety wherein the peptide and the half-life extending moiety are covalently linked or fuse, optionally via a linker. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Bioconjugates of synthetic apelin polypeptides

The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1):X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13&#x2003;&#x2003;Ior an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention or bioconjugates thereof, and their therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. 

5-membered heterocyclic amides and related compounds

The invention provides a synthetic polypeptide of Formula I' (SEQ ID NO: 1):X1-X2-X3-R&#x2014;X5-X6-X7-X8-X9-X10-X11-X12-X13&#x2003;&#x2003;I

Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R, R, E, Z, Z, Z, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.

Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds

Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. 

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Guilford, CT, United States of America

Jun Yuan