Emory University

Neurop, Inc.

Altiris Therapeutics, Inc.

Janssen Pharmaceutica Nv

Lawrence J Wilson

Dennis C Liotta

Yesim Altas Tahirovic

Michael G Natchus

John Wiseman

James P Snyder

Florence Fevrier Wagner

Michael P Clark

Stephen F Traynelis

Raymond J Dingledine

Mark A Lockwood

Edgars Jecs

Scott James Myers

Tricia L Johnson

Cara Mosley

Brandon C Doroh

Jason W Skudlarek

Yue-Mei Zhang

Shyh-Ming Yang

Kenneth Rhodes

Robert Scannevin

Paul F Jackson

Bangping Xiang

Xiaodong Fan

Bryan D Cox

Prabha Saba Karnachi

Stephen Pelly

Julie Wurster

Jianying Wang

Anthony Prosser

Davraj Chakravarty

Robert James Wilson

Huy Hoang Nguyen

Michelle Bora Kim

Valarie Truax

Eric James Miller

This disclosure relates to compounds according to Formula (I), salts, prodrugs and pharmaceutical formulation comprising the compound are provided herein for the treatment of CXCR4 and CCR5 related conditions. The conditions may include viral infections, abnormal cellular proliferation, retinal degeneration and inflammatory diseases, or the compounds may be used as immunostimulants or immunosuppressants. Furthermore, the compounds may be used in combination with another active ingredient selected from an antiviral agent or chemotherapeutic agent. 

Pan-tropic entry inhibitors

The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. The receptor modulators can be formulated to form pharmaceutical compositions comprising the disclosed compounds or pharmaceutically acceptable salts or prodrugs thereof. The compositions may be used for managing CXCR4 related conditions, typically prevention or treatment of viral infections abnormal cellular proliferation, retinal degeneration, inflammatory diseases, or as an immunostimulant or immunosuppressant or for managing cancer and may be administered with another active ingredient such as an antiviral agent or chemotherapeutic agent.

Chemokine CXCR4 receptor modulators and uses related thereto

The disclosure relates to chemokine receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing chemokine related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.

Chemokine CXCR4 and CCR5 receptor modulators and uses related thereto

The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing CXCR4 related conditions, typically prevention or treatment of viral infections such as HIV or for managing cancer.

The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof. These compounds, and pharmaceutical composition comprising such compounds are useful treating or preventing HIV infections, and in treating proliferative disorders such as inhibiting the metastasis of various cancers.

Chemokine receptor modulators

Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein:

NMDA receptor antagonists for neuroprotection

Chemokine CXCR4 receptor modulators and used related thereto

Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein:each (L)-Aris a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NRor O and each Rand Ris independently H, alkyl, alkenyl or aralkyl or Rand Rtaken together form a 5-8 membered ring; RRare selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO, CH, NH, N(alkyl), or NHC(&#x2550;O); and Z is OH, NRR, NRSO(alkyl), NRC(O)NRR, NRC(O)O(alkyl), NR-dihydrothiazole, or NR-dihydroimidazole or wherein Z can fuse with Arto form selected heterocycles.

This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

Heterocyclic derived metalloprotease inhibitors

A process for the preparation of 2',3' dideoxynucleosides, 2'-deoxynucleosides, and 2',3'-dideoxy-2',3'-didehydronucleosides is provided that includes the synchronous addition of a stereoselecting moiety (a directing group) and a protected purine or pyrimidine base to 5-(S)-6-(protected-oxy)-4,5-dihydrofuran in the presence of a Lewis acid. This one vessel reaction eliminates the need to separately prepare and purify a 2'-substituted ribose derivative that in a second step is condensed with a purine or pyrimidine base. The process can be easily modified to increase the stereoselectivity of formation of the .beta.-anomeric nucleoside as necessary.

One vessel stereoselective glycosylation of purines and pyrimidines

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Atlanta, GA, United States of America

Lawrence J Wilson