Bristol-myers Squibb Compnay

Medarex Inc.

The Scripps Research Institute

William Marsh Rice University

E. R. Squibb Sons, Inc.

Bristol Meyers Squibb Company

Coulter Pharmaceutical, Inc.

Sanjeev Gangwar

Naidu S Chowdari

Liqi He

Heng Cheng

Shoshana L Posy

Qiang Cong

Lesley B Pickford

Matthew H Nieder

Robert Michael Borzilleri

Yong Zhang

Howard P Ng

Kyriacos Costa Nicolaou

Nils Lonberg

Qian Zhang

Ashvinikumar V Gavai

David J King

Yam B Poudel

Prasanna Sivaprakasam

Ivar M McDonald

Bilal Sufi

Geoffrey T Yarranton

Thomas Jay Lobl

Zhi-Hong Li

Christopher Robert Bebbington

Vincent Guerlavais

Chin Pan

Liang Chen

Guoxian Wu

Irina Astafieva

Jimmie L Moore

Tram N Huynh

Andre Trouet

Danny P C McGee

Vincent Dubois

Oliver L Saunders

Debashis Mandal

Walter Lewis Johnson

Ian Scott Young

Pina M Cardarelli

Min Lu

Kevin M Peese

Christiana I Iwuagwu

Sharon Elaine Boyd

Ann Marie Fernandez

Daniel W Derwin

Evan Lewis

Dale L Boger

Lawrence B Snyder

Fukang Yang

David B Passmore

Christine M Tarby

Ashok Vinayak Purandare

Zhihong Li

Gretchen M Schroeder

Honghe Wan

Donna Wei

Matthew Cox

Valeri Martichonok

Heidi L Perez

Vangipuram S Rangan

Robert J Schmidt

Matthias Broekema

Ivar M Mcdonald

Sha Lou

André Trouet

Mei-Chen Sung

Killian Horgan

Kilian Horgan

Oliver L Saunder

Danny P Mcgee

Geoffrey Thomas Yarranton

Donna D Wei

Sharon Boyd

Thomas J Lobl

Peter Viski

Anne-Marie Fernandez

Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

1-pyrazolo[4,3-]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists

Compounds represented by formula (I) can be used to make antibody-drug conjugates. The conjugates so made are stable in both human and mouse serum, enabling the performance of pre-clinical studies using a mouse model.

Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making

1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor

Compounds having a structure according to formula are modulators of TLR7 activity and can be used to treat conditions amenable to treatment by the modulation of TLR7 activity. 

Macrocyclic toll-like receptor 7 (TLR7) agonists

Compounds according to formula II are useful as agonists of Toll-like receptor 7 (TLR7).  Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

2H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor

In antibody-drug conjugates having tubulysin analog as the warhead, according to formula (III) the acetate group in the Tuv subunit (dotted box) demonstrates improved stability against hydrolytic cleavage.

Antibody-drug conjugate with a tubulysin analog warhead having a stabilized acetate group in the TUV subunit

Compounds having a structure according to formula (I), (II), or (III) where R, R, R, RX, X, and Xare as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Toll-like receptor 7 (TLR7) agonists having a tricyclic moiety, conjugates thereof, and methods and uses therefor

Compounds having a structure according to formula (I) where R, R, and Rare as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor

Compounds having a structure according to formula (I) or (II) where R, R, and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Toll-like receptor 7 (TLR7) agonists having a heterobiaryl moiety, conjugates thereof, and methods and uses therefor

Compounds having a structure according to formula (I) where Rand Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Toll-like receptor 7 (TLR7) agonists having a pyridine or pyrazine moiety, conjugates thereof, and methods and uses therefor

Compounds having a structure according to formula (I) or (II) where R, R, R, R, Ar and Xare as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor

In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.

Derivatives of uncialamycin, methods of synthesis and their use as antitumor agents

A compound capable of inhibiting cell proliferation, having a structure according to formula (I) wherein the variables in formula (I) are as defined in the specification. Such compounds are useful as anti-cancer agents, especially in antibody-drug conjugates.

Antiproliferative compounds and conjugates made therefrom

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Foster City, CA, United States of America

Sanjeev Gangwar