17309-13-6Relevant academic research and scientific papers
HETEROARYL-SUBSTITUTED SULFONAMIDE COMPOUNDS AND THEIR USE AS SODIUM CHANNEL INHIBITORS
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Paragraph 0808-0810, (2020/03/23)
This invention is directed to heteroaryl-substituted sulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.
Synthesis, X-ray analysis, biological evaluation and molecular docking study of new thiazoline derivatives
Mabkhot, Yahia N.,Algarni,Alsayari, Abdulrhman,Muhsinah, Abdullatif Bin,Kheder, Nabila A.,Almarhoon, Zainab M.,Al-Aizari, Faiz A.
, (2019/05/24)
A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing1H-NMR,13C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.
Process for Preparing Ethyl-4-methyl-5-thiazolecarboxyate
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Paragraph 0031; 0051; 0052, (2017/07/25)
Provided is a method for preparing ethyl-4-methyl-5-thiazolecarboxylate, used as an intermediate for manufacturing Febuxostat, an arthrifuge, in an efficient and economical manner and environmentally friendly conditions. The method comprises the following steps: (i) reacting ethyl 2-chloroacetoacetate and ammonium dithiocarbamate and obtaining ethyl-4-methyl-2-thioxo-2,3-dihydro-1,3-thiazole-5-carboxylate; and (ii) desulfurizing ethyl-4-methyl-2-thioxo-2,3-dihydro-1,3-thiazole-5-carboxylate.COPYRIGHT KIPO 2017
Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors
Kameda, Minoru,Ando, Makoto,Nakama, Chisato,Kobayashi, Kensuke,Kawamoto, Hiroshi,Ito, Sayaka,Suzuki, Tomoki,Tani, Takeshi,Ozaki, Satoshi,Tokita, Shigeru,Sato, Nagaaki
scheme or table, p. 5124 - 5127 (2010/03/24)
A series of 2,4-diaminopyridine derivatives was synthesized and evaluated as potential candidates for neuropeptide Y (NPY) Y1 receptor positron emission tomography (PET) tracers. Derivatives bearing substitutions allowing reliable access to radiolabeling
MORPHOLINE COMPOUND
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Page/Page column 51, (2010/11/27)
A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is hydrogen atom and the like or a pharmaceutically acceptable salt thereof, and a hydrate or solvate thereof have affinity for CCR3, and can be pharmaceutical products for the treatment and/or prophylaxis of immune or inflammatory diseases.
3- (1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
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Page/Page column 48, (2008/06/13)
The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein " G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; " p is an integer ranging from 0 to 5; " R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5, or corresponds to a group R5; " each R2 is independently hydrogen, fluorine or C1-4alkyl; " n is 2, 3, 4, or 5; " R3 is C1-4alkyl; " R4 is hydrogen, or a C1-4alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5;or R4 is a -SR6 group; " R5 is selected from a group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; " R6 is C1-4alkyl or -CH2C3-4cycloalkyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
