Patent classifications
C07D491/08
QUINOLINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
The present invention relates to compounds of formula (I), (I), wherein R.sup.1, R.sup.2 and R.sup.3 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
##STR00001##
QUINOLINE DERIVATIVES
- 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.
SUBSTITUTED INDOLE COMPOUNDS
- Alaric J. Dyckman ,
- Dharmpal S. Dodd ,
- Christopher P. Mussari ,
- Trevor C. Sherwood ,
- John L. Gilmore ,
- Tsair Shamsul Haque ,
- Brian K. Whiteley ,
- David R. Tortolani ,
- Shoshana L. Posy ,
- John E. Macor ,
- Louis J. Lombardo ,
- Ramesh Kumar Sistla ,
- Anupama Kandhi Ramachandra Reddy ,
- Subramanya Hegde ,
- Laxman Pasunoori ,
- Sreekantha Ratna Kumar
Disclosed are compounds of Formula (I)
##STR00001##
or salts thereof, wherein Ring Het, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
Inhibitors of histone deacetylase
The present invention relates to compounds of formula (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
Inhibitors of histone deacetylase
The present invention relates to compounds of formula (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
TRNA SYNTHETASE INHIBITORS
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.
IRAK DEGRADERS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
Bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and use thereof
Bifunctional chimeric heterocyclic compounds of formula (I) is effective for targeted degradation of androgen receptors and use thereof. The compound of formula (I) also has an isotopic compound, an optical isomer, a tautomer, pharmacologically acceptable salt, a prodrug thereof, or a solvate. In formula (I), ARB is an androgen receptor recognition/binding part, L is a link part, and U is a ubiquitin protease recognition/binding part; and the three parts are connected by means of chemical bonds. The compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors.
##STR00001##
Bifunctional chimeric heterocyclic compounds for targeted degradation of androgen receptors and use thereof
Bifunctional chimeric heterocyclic compounds of formula (I) is effective for targeted degradation of androgen receptors and use thereof. The compound of formula (I) also has an isotopic compound, an optical isomer, a tautomer, pharmacologically acceptable salt, a prodrug thereof, or a solvate. In formula (I), ARB is an androgen receptor recognition/binding part, L is a link part, and U is a ubiquitin protease recognition/binding part; and the three parts are connected by means of chemical bonds. The compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors.
##STR00001##
P38ALPHA MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS
Disclosed herein are p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38α mitogen-activated protein kinase inhibitors.