Patent classifications
C07D207/08
SYNTHETIC PROCESSES AND INTERMEDIATES
The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.
SYNTHETIC PROCESSES AND INTERMEDIATES
The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.
NOVEL SUBSTITUTED SULFOXIMINE DERIVATIVES
The present invention relates to novel heterocyclic compounds of general formula (I) their tautomers, stereoisomers, enantiomers, pharmaceutically acceptable salts and pharmaceutical composition. The compounds of general formula (I) belongs to the family of NOD like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators and use of these novel inhibitor compounds in the treatment of disease or conditions as well as treatment of disease states mediated by NLRP3 as well as treatment of diseases or conditions in which interleukin 1β activity and interleukin-18 (IL-18) is implicated.
NOVEL SUBSTITUTED SULFOXIMINE DERIVATIVES
The present invention relates to novel heterocyclic compounds of general formula (I) their tautomers, stereoisomers, enantiomers, pharmaceutically acceptable salts and pharmaceutical composition. The compounds of general formula (I) belongs to the family of NOD like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators and use of these novel inhibitor compounds in the treatment of disease or conditions as well as treatment of disease states mediated by NLRP3 as well as treatment of diseases or conditions in which interleukin 1β activity and interleukin-18 (IL-18) is implicated.
Cytotoxic and anti-mitotic compounds, and methods of using the same
Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.
Cytotoxic and anti-mitotic compounds, and methods of using the same
Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.
SUBSTITUTED STRAIGHT CHAIN SPIRO DERIVATIVES
- Wei Cai ,
- Xuedong Dai ,
- Oliver Alexis Georges QUEROLLE ,
- Johannes Wilhelmus John F. Thuring ,
- Yingtao Liu ,
- Lianzhu LIU ,
- Yanping XU ,
- Liqiang Fu ,
- Ming Li ,
- Lichao FANG ,
- Xianguin DENG ,
- Qiwu ZHAO ,
- Kangying LI ,
- Alicia Tee Fuay NG ,
- Nicolas Freddy J. DARVILLE ,
- Edward CLEATOR ,
- Gregor Thomas URBANIETZ ,
- William Marc MATON ,
- Vineet PANDA
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, including but not limited to leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasms (MPN); and diabetes.
SUBSTITUTED STRAIGHT CHAIN SPIRO DERIVATIVES
- Wei Cai ,
- Xuedong Dai ,
- Oliver Alexis Georges QUEROLLE ,
- Johannes Wilhelmus John F. Thuring ,
- Yingtao Liu ,
- Lianzhu LIU ,
- Yanping XU ,
- Liqiang Fu ,
- Ming Li ,
- Lichao FANG ,
- Xianguin DENG ,
- Qiwu ZHAO ,
- Kangying LI ,
- Alicia Tee Fuay NG ,
- Nicolas Freddy J. DARVILLE ,
- Edward CLEATOR ,
- Gregor Thomas URBANIETZ ,
- William Marc MATON ,
- Vineet PANDA
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, including but not limited to leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasms (MPN); and diabetes.
3-DIARYLMETHYLENES AND USES THEREOF
3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
3-DIARYLMETHYLENES AND USES THEREOF
3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.