Patent classifications
A61K31/5545
DIACYLGLYCEROL KINASE MODULATING COMPOUNDS
- Masaaki SAWA ,
- Mai ARAI ,
- Ryoko NAKAI ,
- Hirokazu MATSUMOTO ,
- Catherine Pugh ,
- Eric Hu ,
- Juan Guerrero ,
- Jesse Jacobsen ,
- Jonathan William Medley ,
- Jie Xu ,
- Latesh Lad ,
- Leena Patel ,
- Michael Graupe ,
- Qingming Zhu ,
- Stephen Holmbo ,
- Tetsuya Kobayashi ,
- Will Watkins ,
- Yasamin Moazami ,
- Suet C. Yeung ,
- Julian A. Codelli ,
- Heath A. Weaver
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
ANTI-FOLATE RECEPTOR ANTIBODY CONJUGATES, COMPOSITIONS COMPRISING ANTI-FOLATE RECEPTOR ANTIBODY CONJUGATES, AND METHODS OF MAKING AND USING ANTI-FOLATE RECEPTOR ANTIBODY CONJUGATES
The present disclosure relates to antibody conjugates with binding specificity for folate receptor alpha (FOLR1) and its isoforms and homologs, and compositions comprising the antibody conjugates, including pharmaceutical compositions. Also provided are methods of producing the antibody conjugates and compositions as well as methods of using the antibody conjugates and compositions, such as in therapeutic and diagnostic methods.
Compounds for treating myelin related disorders
Disclosed is a pharmaceutical composition comprising a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a myelin related disorder in a subject, the method comprising administering to the subject an effective amount of a compound of Structural Formula (I) or a pharmaceutical composition comprising the compound of Structural Formula (I). The variables of Structural Formula (I) are described herein. ##STR00001##
HETEROCYCLIC TRPML1 AGONISTS AND USES THEREOF
Described herein are TRPML1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of TRPML1-mediated disorders or diseases.
CENICRIVIROC COMBINATION THERAPY FOR THE TREATMENT OF FIBROSIS
Cenicriviroc (CVC) is an orally active antagonist of ligand binding to CC chemokine receptor type 5 (CCR5) and CC chemokine receptor type 2 (CCR2). CVC blocks the binding of RANTES, MIP-1, and MIP-1 to CCR5, and of MCP-1/CCL2 to CCR2. Methods of treating fibrosis and related conditions comprising co-administration of CVC with chemokine antagonists, FXR agonists, high dose vitamin E (>400 iU/d), a peroxisome proliferator-activated receptor alpha (PPAR-) agonist, PPAR- agonist, and/or PPAR- agonist are provided herein.
Anti-folate receptor alpha antibody conjugated with hemiasterlins
The present disclosure relates to antibody conjugates with binding specificity for folate receptor alpha (FOLR1) and its isoforms and homologs, and compositions comprising the antibody conjugates, including pharmaceutical compositions. The variable light chains are those of trastuzumab. Also provided are methods of producing the antibody conjugates and compositions as well as methods of using the antibody conjugates and compositions, such as in therapeutic and diagnostic methods. The antibody conjugates comprise a non-natural amino acid at a site selected from the group consisting of HC-F404, HC-K121, HC-Y180, HC-F241, HC-221, LC-T22, LC-S7, LC-N152, LC-K42, LC-E161, LC-D170, HC-S136, HC-S25, HC-A40, HC-S119, HC-S190, HC-K222, HC-R19, HC-Y52, or HC-S70, according to the Kabat, Chothia, or EU numbering scheme.
SUPPRESSION OF COVID-19 REPLICATION BY COVID-19 ENTRY INHIBITORS
The present invention relates to compounds, compositions, and methods, for treating viral infections. In particular, entry inhibitor compounds are disclosed for treatment of coronavirus infections, including SARS-COV-1 and SARS-COV-2 infections. The compounds bind to the interface of a SARS-COV-2 spike protein receptor binding domain (RBD) and a host cell ACE-2 receptor. The entry inhibitor compounds show antiviral activity, favorable kinetics, and temporally act at the entry of SARS-COV-2 infection. In embodiments, the compounds are used as medicaments for the inhibition of viral replication including SARS-COV-1 and/or SARS-COV-2 replication, for the treatment or prophylaxis of viral infections including SARS-COV-1 and SARS-COV-2 infections, and/or for the treatment or prophylaxis of an illness due to SARS-COV-1 and SARS-COV-2 infections.
INHIBITORS OF NLRP3
- XIAOYAN ZHANG ,
- TIANYI ZHENG ,
- SCOTT j BARRAZA ,
- LAUREN BEJCEK ,
- BRADLEY B GILBERT ,
- HUA GONG ,
- HANDOKO HANDOKO ,
- SEYEDMORTEZA HOSSEYNI ,
- EDUARDO HUARTE ,
- WOOHYUNG JEON ,
- JING LI ,
- YAO LIU ,
- KYLE NIEDERER ,
- MEENU PILLAI ,
- ERICA N PARKER ,
- ETTORE RASTELLI ,
- NADIYA SYDORENKO ,
- ANTHONY TURPOFF ,
- MATTHEW G WOLL ,
- NANJING ZHANG ,
- YAN ZHANG ,
- RAUFUL ALAM
The present invention relates to novel compounds of Formulae I-XI: wherein each A, A, Q, Q, W, Rw, Y, and Z, and -- are as defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.
##STR00001##
Diacylglycerol kinase modulating compounds
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
METHODS OF TREATING OVARIAN CANCER WITH HEMP EXTRACT
Methods for treating ovarian cancer comprising: administering to a patient and effective amount of a cannabis extract comprising CBD wherein preferably the cannabis extract is administered via a mucosal formulation.