Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Sirna Therapeutics, Inc.

Other

Merck Sharp & Dohme LLC

Sima Therapeutics, Inc.

Anthony W Shaw

Daniel Vincent Paone

S Jane deSolms

Christopher S Burgey

Steven L Colletti

Thomas Joseph Tucker

David M Tellers

Yu Yuan

Theresa M Williams

Diem N Nguyen

Samuel L Graham

Weimin Wang

Vadim Y Dudkin

Rubina G Parmar

Zhengwu James Deng

Lu Tian

Kathleen B Calati

Terrence M Ciccarone

William C Lumma, Jr

Gerald E Stokker

Hongbiao Liao

Byeong Moon Kim

John Howard Hutchinson

Joseph P Vacca

Harold G Selnick

Ian M Bell

Neville J Anthony

Vasant R Jadhav

Craig A Stump

John S Wai

Ling Tong

Francis Gosselin

Marina Busuek

Robert A Kowtoniuk

Rachel Anne Storr

Jeffrey Aaronson

Aaron Momose

Craig M Potteiger

Suzanne C MacTough

Tao Pei

Lijun Wang

Man Zhu

Craig Parish

Steven D Young

Cheng Wang

Robert P Gomez

William D Shipe

Anthony T Ginnetti

Brendan M Crowley

John T Sisko

Antonella Converso

Debra S Perlow

Ashley Forster

Stanley F Barnett

Daniel Zewge

Abdellatif El Marrouni

Yunlong Zhang

Quang Truong

Norihiro Ikemoto

Lekhanh O Tran

Jeffrey G Aaronson

David N Hunter

Michelle Sparks Kuo

Anthony J Roecker

Anthony Ginetti

Deping Wang

Vadim Dudkin

Michael Aaron Plotkin

Aaron A Momose

René Bartz

Zhengwu J Deng

Daniel V Paone

Christopher Douglas Cox

Richard Thaddeus Berger

Rene Bartz

Jason W Skudlarek

Deyou Sha

The present disclosure is directed to tetrahydroquinazoline derivatives of Formula (I) and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naive cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

Tetrahydroquinazoline derivatives as selective cytotoxic agents

Disclosed herein is a modular composition comprising 1) an oligonucleotide; 2) one or more tetraGalNAc ligands of Formula (I), which may be the same or different; optionally, 3) one or more linkers, which may be the same or different; 4) one or more peptides independently selected from Table 3, which may be the same or different; and optionally, 5) one or more targeting ligands, solubilizing agents, pharmacokinetics enhancing agents, lipids, and/or masking agents.

Tetragalnac and peptide containing conjugates and methods for delivery of oligonucleotides

The present disclosure is directed to tetrahydroquinazoline derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV na&#xef;ve cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

Disclosed herein is a modular composition comprising 1) an oligonucleotide; 2) one or more tetraGalNAc ligands of Formula (I), which may be the same or different; optionally, 3) one or more linkers, which may be the same or different; and optionally, 4) one or more targeting ligands, solubilizing agents, pharmacokinetics enhancing agents, lipids, and/or masking agents.

Tetragalnac containing conjugates and methods for delivery of oligonucleotides

In an embodiment the instant invention discloses a modular composition comprising 1) an oligonucleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at any 3' and/or 5&#x2032; end; 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.

Single chemical entities and methods for delivery of oligonucleotides

The subject invention relates to novel P2Xreceptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2Xreceptor subunit modulator.

P2X3, receptor antagonists for treatment of pain

Compounds of Formula (I): and Formula (II): (where variables R, R, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. 

CGRP receptor antagonists

Compounds of Formula I: (where variables R, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

The present invention is directed to compounds of Formula I: and Formula II: (where variables R, R, R, R, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Growing community of inventors

Harleysville, PA, United States of America

Anthony W Shaw