144822-82-2Relevant articles and documents
Imidazo ring PAR4 antagonist and medical applications thereof
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Paragraph 0225; 0227; 0231, (2020/01/12)
The invention relates to an imidazo ring compound represented by formula (I) or formula (II), or a pharmaceutically acceptable salt or ester or solvate thereof. The compound disclosed by the inventioncan be used for preparing medicines for preventing or treating thromboembolic diseases.
Therapeutic diphenyl ether ligands
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Page/Page column 37, (2010/10/20)
This invention is directed to compounds of formula Ia, Ib or Ic and to pharmaceutical compositions thereof: or a prodrug thereof and a pharmaceutically acceptable carrier, wherein the R groups are defined in the specification; and, in which the dashed line represents an optional double bond. The invention is also directed to methods of treating, diagnosing, and preventing disorders of the central nervous system that are associated with 5HT receptors, including obesity, attention deficit disorder, migraine, depression, epilepsy, anxiety, Alzheimer's disease, withdrawal from drug abuse, pain, schizophrenia, stress-related disorders, panic disorder, sleep disorders, phobias, obsessive compulsive disorder, post-traumatic-stress syndrome, immune system depression, stress-induced gastrointestinal dysfunction, stress-induced cardiovascular dysfunction, and sexual dysfunction.
SUBSTITUTED UREA DERIVATIVES AS CELL ADHESION INHIBITORS
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Example 71, (2010/01/30)
Compounds of formula (II) where R 1 is in the para or meta position and is (A); R 2 and R 3 are each independently selected from hydrogen, nitro, C 1-6 alkyl, C 3-6 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-4 alkoxyl, C 1-6 alkylamino, C 1-6 dialkylamino, C 1-6 akylC 1-4 alkoxyl, C 1-6 alkylaminoC 1-6 alkyl, amino, cyano, halogeno, trifluoromethyl, ?CO 2 R 12 and ?CONR 12 R 13 , where R 12 and R 13 are independently selected from hydrogen or C 1-6 alkyl, or R 2 and R 3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R 4 is C 1-4 alkyl; R 5 is selected from hydrogen and C 1-4 alkyl; R 6 is selected from C 1-6 alkyl, C 1-4 alkyl(C 4-6 )cycloalkyl, C 1-6 alkyl(C 1-6 )alkoxyl, C 1-6 alkylS(C 1-6 )alkyl, C 1-4 alkylsulphonyl(C 1-4 )alkyl; (B) where q is an integer from 1 to 6 and R 14 is halogeno; R 7 is selected from C 1-6 alkyl, C 1-8 alkoxylcarbonyl, C 2-6 alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C 1-4 alkoxy, C 1-6 alkyl, cyano, halogeno, and trifluoromethyl; R 8 is aryl, heteroaryl, a bicyclic heteroaryl ring system linked to the nitrogen via a ring carbon or a 9 or 10 membered bicyclic ring system linked to the nitrogen via a ring carbon and each ring is optionally substituted with up to two substituents, which may be the same or different, and are selected from C 1-6 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 1-6 alkylC 1-4 alkoxyl, C 1-6 alkylaminoC 1-6 alkyl, hydroxy, ?CO 2 H, ?(CH 2 ) p OH where p is 1 or 2, cyano, halogeno, and trifluoromethyl; R 9 and R 10 are each independently selected from hydrogen and C 1-4 alkyl or R 8 and R 9 together with the nitrogen to which they are attached form a dihydroindolyl, or a dihidroquinolinyl group; R 11 is selected from carboxyl, tetrazolyl, alkyl sulphonylcarbamyl, sulfo and sulfino; Y is oxygen, sulphur or sulfonyl; m is 0 or 1; and n is 0 or an integer from 1 to 4 with the proviso that when m and n cannot both be 0 and when m is 1, n is 0; or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof. The compounds inhibit the interaction of vascular cell-adhesion molecule-1 and fibronectin with integrin very late antigen 4 (a 4 b 1 ). They have therapeutic applications such as in multiple sclerosis, rheumatoid arthritis, asthma, coronary artery disease and psoriasis
