- DUAL AGONISTS OF FXR AND PPARδ AND THEIR USES
-
The present invention relates to small molecule compounds and their use as agonists of farnesoid X receptor (FXR) and/or peroxisome proliferator activated receptor delta (PPARδ). The present invention also relates to the use of said compounds in the treatment of metabolic diseases and respective methods of treatment.
- -
-
-
- Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis
-
Structure-based drug design was used to guide the optimization of a series of selective BTK inhibitors as potential treatments for Rheumatoid arthritis. Highlights include the introduction of a benzyl alcohol group and a fluorine substitution, each of which resulted in over 10-fold increase in activity. Concurrent optimization of drug-like properties led to compound 1 (RN486) (J. Pharmacol. Exp. Ther. 2012, 341, 90), which was selected for advanced preclinical characterization based on its favorable properties.
- Lou, Yan,Han, Xiaochun,Kuglstatter, Andreas,Kondru, Rama K.,Sweeney, Zachary K.,Soth, Michael,McIntosh, Joel,Litman, Renee,Suh, Judy,Kocer, Buelent,Davis, Dana,Park, Jaehyeon,Frauchiger, Sandra,Dewdney, Nolan,Zecic, Hasim,Taygerly, Joshua P.,Sarma, Keshab,Hong, Junbae,Hill, Ronald J.,Gabriel, Tobias,Goldstein, David M.,Owens, Timothy D.
-
p. 512 - 516
(2015/03/03)
-
- Meta-Oligoazobiphenyls - Synthesis via site-selective Mills reaction and photochemical properties
-
The investigation of multi-photochromic compounds constitutes a great challenge, not only from a synthetic point of view, but also with respect to the analysis of the photochemical properties. In this context we designed a novel strategy to access meta-ol
- Reuter, Raphael,Wegner, Hermann A.
-
supporting information; experimental part
p. 877 - 883
(2012/07/17)
-
- BTK protein kinase inhibitors
-
This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.
- -
-
Page/Page column 52
(2009/05/29)
-
- AMINOQUINAZOLINE CANNABINOID RECEPTOR MODULATORS FOR TREATMENT OF DISEASE
-
The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.
- -
-
-
- QUINAZOLINONES
-
Disclosed are compounds of formula (I), wherein R, R1, R2, R3, R4, R5, R6, R7, R8, Z1, Z2, Z3, k, and Y1 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
- -
-
Page/Page column 97-98
(2008/06/13)
-