Patent classifications
C07C233/87
PPAR AGONISTS
Provided herein are compounds and compositions useful in increasing PPAR activity. The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
DUAL MODULATORS OF FARNESOID X RECEPTOR AND SOLUBLE EPOXIDE HYDROLASE
The present invention pertains to novel dual modulators of farnesoid X receptor (FXR) and soluble epoxide hydrolase (sEH). The modulators of the invention were designed to provide compounds which harbor a dual activity as agonists of FXR and inhibitors (antagonists) of sEH. The invention also provides methods for treating subjects suffering from diseases associated with FXR and sEH, such as metabolic disorders, in particular non-alcoholic fatty liver or nonalcoholic steatohepatitis (NASH).
DUAL MODULATORS OF FARNESOID X RECEPTOR AND SOLUBLE EPOXIDE HYDROLASE
The present invention pertains to novel dual modulators of farnesoid X receptor (FXR) and soluble epoxide hydrolase (sEH). The modulators of the invention were designed to provide compounds which harbor a dual activity as agonists of FXR and inhibitors (antagonists) of sEH. The invention also provides methods for treating subjects suffering from diseases associated with FXR and sEH, such as metabolic disorders, in particular non-alcoholic fatty liver or nonalcoholic steatohepatitis (NASH).
COMPOUNDS FOR INHIBITION OF ALPHA 4 BETA 7 INTEGRIN
- Peter A. Blomgren ,
- Taryn Campbell ,
- Jayaraman Chandrasekhar ,
- Christopher T. Clark ,
- Julian A. Codelli ,
- Kevin S. Currie ,
- Jeffrey E. Kropf ,
- Yasamin Moazami ,
- Nicole Nava ,
- Leena Patel ,
- Stephane Perreault ,
- Jason K. Perry ,
- Kassandra F. Sedillo ,
- Natalie Seeger ,
- Kirk L. Stevens ,
- Jennifer Anne Treiberg ,
- Suet C. Yeung ,
- Zhongdong Zhao
The present disclosure provides a compound of Formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.
AMINE OR (THIO)AMIDE CONTAINING LXR MODULATORS
The present invention relates to derivatives of formula (I) which bind to the liver X receptor (LXR and/or LXR) and act preferably as inverse agonists of LXR.
##STR00001##
Farnesoid X receptor agonists and uses thereof
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Farnesoid X receptor agonists and uses thereof
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
PPAR agonists
Provided herein are compounds and compositions useful in increasing PPAR activity. The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
PPAR agonists
Provided herein are compounds and compositions useful in increasing PPAR activity. The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
Anti-tumor compound and the medical use thereof
The invention disclose a compound of formula (I), wherein, R.sub.1 is selected from H or C1-C6 hydrocarbon group, NH.sub.2, OH, O(CH.sub.2).sub.nCH.sub.3 (n=0, 1 or 2), N(CH.sub.3).sub.2, or CH.sub.2N(CH.sub.3).sub.2, R.sub.2 is selected from an amino acid ##STR00001##
or an hydroxy acid ##STR00002##
or OH (R.sub.1, R.sub.2 are not CH.sub.3 and OH at the same time), wherein X, Y are ##STR00003##
H, CH.sub.3, CH.sub.2OH, CH(OH)CH.sub.3, CH.sub.2SH, CH(CH.sub.3).sub.2, CH.sub.2CH(CH.sub.3).sub.2, CH(CH.sub.3)CH.sub.2CH.sub.3, CH.sub.2CH.sub.2SCH.sub.3, CH.sub.2COOH, CH.sub.2CONH.sub.2, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2NH.sub.2, or CH.sub.2CH.sub.2CONH.sub.2, R.sub.3-R.sub.5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc. ##STR00004##