73387-52-7Relevant academic research and scientific papers
2-AMINO-BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS 5-LIPOXYGENASE AND/OR PROSTAGLANDIN E SYNTHASE INHIBITORS
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Page/Page column 52, (2016/03/12)
The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X1 and X2 are independently, at each occurrence, CR5 or N; Y is C1-C6 alkylene, wherein alkylene is optionally substituted with one to two C1-C3 alkyl groups; R1 is selected from the group consisting of hydrogen, halogen, C1-C6 alkoxy, -NH2, -NHR6, -NR7R8 and -NH-(R9)n-R10, n being 0 or 1; R2 is selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, -NH2, -NHR6, - NR7R8 and -NH-(R9)n-R10; R3 is selected from the group consisting of hydrogen, hydroxyl, OR11, -NR7R8, C1-C6 alkoxy, C1-C6 alkyl, C3-C10 cycloalkyl, C1-C3 haloalkyl, -C(O)NHR11, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four Ra groups; and R4 is selected from the group consisting of -NH2, -N(R12)(V)pR13, - NH(V)p-OR14, -NHC(O)R15, and groups of formula la shown below, and their use in the treatment of diseases, in particular inflammatory diseases, cancer, stroke and/or Alzheimer's disease.
1,2,3,4-TETRAHYDROISOQUINOLINE COMPOUNDS AND COMPOSITIONS AS SELECTIVE ESTROGEN RECEPTOR ANTAGONISTS AND DEGRADERS
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Paragraph 00258, (2015/07/07)
The present invention relates to compounds of formula (I) in which n, R1, R2, R3, R4and R5 are as defined in the claims; capable of being both potent antagonists and degraders of estrogen receptors. Also described is a process for the preparation of compounds of the invention, and the invention further provides pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
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, (2014/06/11)
The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Y1 and Y2 are adjacent atoms in Het1, which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—Ra as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N—Ra as ring members; Het2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—R1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het1 and inter alia-halogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C1-C6-fluoroalkyl, C1-C6-fluoroalkoxy, C3-C6-cycloalkyl etc.
Development an efficient route to the 5-lipoxygenase inhibitor PF-04191834
De Koning, Pieter D.,Murtagh, Lorraine,Lawson, Jon P.,Vonder Embse, Richard A.,Kunda, Sastry A.,Kong, Wei
experimental part, p. 1046 - 1051 (2012/01/04)
A convergent six-step process for the synthesis of PF-04191834 (1), a potent and selective 5-lipoxygenase inhibitor, has been developed and used to deliver over 20 kg of API. The process uses the same bond-forming steps as the initial medicinal chemistry
PYRAZOLE DERIVATIVES AS 5-LO INHIBITORS
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Page/Page column 67-68, (2009/07/03)
The invention relates to compounds of formula (I) processes for their preparation, their use as 5-lipoxygenase inhibitors and pharmaceutical compositions containing the same.
Pyrazole Analogs
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Page/Page column 14; 16, (2008/12/05)
The invention relates to the compounds of formula (I): or a pharmaceutically acceptable salt and solvate thereof, wherein R1 is F or H and to processes for the preparation of, intermediates used in the preparation of, compositions containing th
Thermolyses of 1,1-dimethyl-2-pyrazolinium fluoborates - Evidence for spiro--1-aza-1,4,6-octatrienyl cation
Subramaniam, Girija,Fishel, Derry L
, p. 172 - 176 (2007/10/02)
Thermolyses of 3-aryl-1,1-dimethyl-2-pyrazolinium fluoborates give an isomeric mixture of 3-aryl-1-methylpyrazole and 5-aryl-1-methylpyrazole as major products in complete contrast to the corresponding acyclic analogs. 2,6-Diaryl-3-methylpyridines were isolated only in trace quantities.The probable reasons for this unique behaviour was explored using semi-empirical calculations, non-kinetic methods and radiolabelling experiments.A pathway was proposed.
