Bristol-Myers Squibb Compnay

The Scripps Research Institute

William Marsh Rice University

Yam B Poudel

Sanjeev Gangwar

Prasanna Sivaprakasam

Liqi He

Shoshana L Posy

Naidu S Chowdari

Kyriacos Costa Nicolaou

Debashis Mandal

Min Lu

Qian Zhang

Christine M Tarby

Ian Scott Young

Ashvinikumar V Gavai

Ashok Vinayak Purandare

Qiang Cong

Honghe Wan

Matthew Cox

Matthias Broekema

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

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.

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Fremont, CA, United States of America

Yam B Poudel