38710-60-0Relevant academic research and scientific papers
The liquid crystal aligning agent, liquid crystal alignment film, the liquid crystal display element, phase difference film and method of manufacturing the same, polymer and compound
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Paragraph 0203-0206, (2018/02/04)
The invention provides a liquid crystal alignment agent, a liquid crystal alignment film, a liquid crystal display element, a phase different film, a method of making a phase difference film, a polymer, and a compound. The invention provides the liquid cr
Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors
Illig, Carl R.,Manthey, Carl L.,Meegalla, Sanath K.,Wall, Mark J.,Chen, Jinsheng,Wilson, Kenneth J.,Desjarlais, Renee L.,Ballentine, Shelley K.,Schubert, Carsten,Crysler, Carl S.,Chen, Yanmin,Molloy, Christopher J.,Chaikin, Margery A.,Donatelli, Robert R.,Yurkow, Edward,Zhou, Zhao,Player, Mark R.,Tomczuk, Bruce E.
, p. 6363 - 6369 (2013/11/19)
Structure-activity relationship (SAR) studies on a highly potent series of arylamide FMS inhibitors were carried out with the aim of improving FMS kinase selectivity, particularly over KIT. Potent compound 17r (FMS IC50 0.7 nM, FMS cell IC50 6.1 nM) was discovered that had good PK properties and a greater than fivefold improvement in selectivity for FMS over KIT kinase in a cellular assay relative to the previously reported clinical candidate 4. This improved selectivity was manifested in vivo by no observed decrease in circulating reticulocytes, a measure of bone safety, at the highest studied dose. Compound 17r was highly active in a mouse pharmacodynamic model and demonstrated disease-modifying effects in a dose-dependent manner in a strep cell wall-induced arthritis model of rheumatoid arthritis in rats.
INHIBITORS OF C-FMS KINASE
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Page/Page column 39, (2008/06/13)
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
Medicaments 1,2,3,4-tetrahydrocarbazoles and 5-HT1 agonist use thereof
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, (2008/06/13)
Use of a compound of general formula (I): STR1 wherein R1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C1-6 alkyl, C1-6 alkoxy, arylC1-6 alkoxy, --CO2 R4, --(CH2)n CN, --(CH2)n CONR5 R6, --(CH2)n SO2 NR5 R6, C1-6 alkanoylamino(CH2)n, or C1-6 alkylsulphonylamino(CH2)n ; R4 represents hydrogen, C1-6 alkyl or arylC1-6 alkyl; R5 and R6 each independently represent hydrogen or C1-6 alkyl, or R5 and R6 together with the nitrogen atom to which they are attached form a ring; n represents 0, 1 or 2; and R2 and R3 each independently represent hydrogen, C1-6 alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring; or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT1 -like agonist is indicated, for example migraine. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.
Tetrahydrocarbazole derivatives for the manufacture of a medicament for the treatment of a disease where a 5-HT1-like agonist is indicated
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, (2008/06/13)
Use of a compound of general formula (I): wherein : R1represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C1 6alkyl, C1 6alkoxy, arylC1 6alkoxy, -CO2R4, -(CH2)nCN, -(CH2)nCONR5R6,-(CH2)nSO2NR5R6,C1 6alkanoylamino(CH2)n, or C1 6alkylsulphonylamino (CH2)n; R4represents hydrogen, C1 6alkyl or arylC1 6alkyl; R5 and R6each independently represent hydrogen or C1 6alkyl, or R5 and R6 together with the nitrogen atom to which they are attached form a ring; nrepresents 0, 1 or 2; and R2 and R3each independently represent hydrogen, C1 6alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring; or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT1-like agonist is indicated, for example migraine. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.
Novel N-aralkyl enkephalin amide analogs are provided having analgesic and opioid properties
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, (2008/06/13)
The enkephalin analogs are polypeptide amides including in the chain the series L-tyrosyl-D-alanyl-glycyl, normally followed by L-phenylalanine. The nitrogen substituents are substituted and unsubstituted phenalkylenes or phenalkenylenes, wherein the alky
