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

Yam B Poudel

Prasanna Sivaprakasam

Naidu S Chowdari

Liqi He

Heng Cheng

Shoshana L Posy

Qiang Cong

Lesley B Pickford

Matthew H Nieder

Qian Zhang

Ivar M McDonald

Robert Michael Borzilleri

Bilal Sufi

Yong Zhang

Geoffrey T Yarranton

Thomas Jay Lobl

Zhi-Hong Li

Christopher Robert Bebbington

Vincent Guerlavais

Chin Pan

Liang Chen

Howard P Ng

Guoxian Wu

Irina Astafieva

Jimmie L Moore

Tram N Huynh

Andre Trouet

Danny P C McGee

Vincent Dubois

Kyriacos Costa Nicolaou

Oliver L Saunders

Debashis Mandal

Walter Lewis Johnson

Ian Scott Young

Min Lu

Pina M Cardarelli

Kevin M Peese

Christine M Tarby

Christiana I Iwuagwu

Sharon Elaine Boyd

Daniel W Derwin

Ann Marie Fernandez

Evan Lewis

Nils Lonberg

Ashvinikumar V Gavai

Dale L Boger

Lawrence B Snyder

Fukang Yang

David B Passmore

Ashok Vinayak Purandare

Zhihong Li

Gretchen M Schroeder

Honghe Wan

Heidi L Perez

Donna Wei

Matthew Cox

Valeri Martichonok

Vangipuram S Rangan

Matthias Broekema

Robert J Schmidt

Sha Lou

Mei-Chen Sung

Kilian Horgan

Killian Horgan

Oliver L Saunder

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