- Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2- yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist
-
High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified t
- Swanson, Devin M.,Dubin, Adrienne E.,Shah, Chandra,Nasser, Nadia,Chang, Leon,Dax, Scott L.,Jetter, Michele,Breitenbucher, J. Guy,Liu, Changlu,Mazur, Curt,Lord, Brian,Gonzales, Lisa,Hoey, Kenway,Rizzolio, Michele,Bogenstaetter, Michael,Codd, Ellen E.,Lee, Doo H.,Zhang, Sui-Po,Chaplan, Sandra R.,Carruthers, Nicholas I.
-
-
Read Online
- INHIBITORS FOR SOLUBLE EPOXIDE HYDROLASE (SEH) AND FATTY ACID AMIDE HYDROLASE (FAAH)
-
The present invention provides compounds that are dual inhibitors of soluble epoxide hydrolase and fatty acid amide hydrolase. The present invention also provides methods of using the compounds to inhibit soluble epoxide hydrolase and fatty acid amide hydrolase, and to treat cancer.
- -
-
Paragraph 0174
(2017/10/11)
-
- SUBSTANCE FOR INHIBITION OF GLYCINE TRANSPORTER
-
PROBLEM TO BE SOLVED: To provide a new compound or its pharmaceutically acceptable salt useful for preventing or treating diseases such as integrated dystonia, Alzheimer disease, cognitive dysfunction, dementia, anxiety disorder(such as global anxiety disorder, panic disorder, obsessive compulsive disorder, social anxiety disorder, post traumatic stress disorder, particular phobia, acute stress disorder), depression, drug dependence, convulsion, trembling, ache, Parkinson disease, attention-deficit/hyperactivity disorder, bipolar disorder, eating disorder or sleep disorder, based on inhibitory effect on glycine uptake. SOLUTION: There are provided a compound represented by the formula [I] or its pharmaceutically acceptable salt. COPYRIGHT: (C)2015,JPOandINPIT
- -
-
Paragraph 0091-0093
(2020/04/21)
-
- GLYCINE TRANSPORTER-INHIBITING SUBSTANCES
-
The present invention relates to novel compounds of formula [I] or pharmaceutically acceptable salts thereof: The compounds of the present invention are useful in the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.
- -
-
Paragraph 0193; 0194
(2014/01/08)
-