200423-20-7Relevant academic research and scientific papers
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors
Masaki, Hidekazu,Mizuno, Yusuke,Tatui, Akira,Murakami, Akira,Koide, Yuuki,Satoh, Shoji,Takahashi, Atsuo
, p. 4085 - 4088 (2003)
We have identified a new class of chymase inhibitor through a substituent analysis of MWP00965, which we previously discovered by in silico screening. TY-51076 (7) showed high potency (IC50=56 nM) and excellent selectivity for chymase compared to chymotrypsin and cathepsin G (>400-fold). The synthesis and structure-activity relationship of this class are described.
2,3,5 TRISUBSTITUTED ARYL AND HETEROARYL AMINO DERIVATIVES, COMPOSITIONS, AND METHODS OF USE
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Paragraph 0597, (2013/05/09)
Compounds are disclosed that have a formula represented by the following:(I) wherein Cy, L1 R1, R2a, R2b, R3, R4, n, and L2 are as described herein. These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, inflammatory pain, insomnia, ischemia, migraine, migraine with aura, migraine without aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, itch, excessive itch, Pruritis, neuropathic pruritis, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
Benzoylguanidines, a process for their preparation, their use as medicaments and medicaments containing them
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, (2008/06/13)
Benzoylguanidines of the formula I STR1 where R(1) or R(2) is equal to R(6)--S(O)n -- or R(7)R(8)N--O2 S-- and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O)n or R(7)R(8)N-- and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(7) and R(8) are equal to alkyl or phenylakyl or phenyl, and in which R(7) and R(8) may also together be a C4 -C7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system, and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(5) are together an alkylene chain, and where n is equal to zero, 1 or 2 and their pharmaceutically tolerable salts are outstanding antiarrhythmics.
