854267-89-3Relevant articles and documents
THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS
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Paragraph 0688, (2020/12/11)
Disclosed herein are certain thiadiazolyl derivatives Formula (I): that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.
LYSOPHOSPHATIDIC ACID RECEPTOR 1 (LPAR1) INHIBITOR COMPOUNDS
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Page/Page column 81, (2019/03/17)
A compound of formula (I) or a pharmaceutical salt thereof, use, methods for its preparation are described.
NEW AZIRIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE AS ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 91, (2013/07/05)
The invention relates to new azetidine derivatives of the formula (I) wherein Ar1, Ar2, X, R, T and L are as defined in the description, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
AZETIDINE DERIVATIVES
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Paragraph 0550; 0551; 0552; 0553, (2013/06/28)
Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
SUBSTITUTED 5-,6- AND 7-MEMBERED HETEROCYCLES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, AND THEIR USE
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Page/Page column 66, (2012/01/06)
The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor
Isabel, Elise,Bateman, Kevin P.,Chauret, Nathalie,Cromlish, Wanda,Desmarais, Sylvie,Duong, Le T.,Falgueyret, Jean-Pierre,Gauthier, Jacques Yves,Lamontagne, Sonia,Lau, Cheuk K.,Leger, Serge,LeRiche, Tammy,Levesque, Jean-Francois,Li, Chun Sing,Masse, Frederic,McKay, Daniel J.,Mellon, Christophe,Nicoll-Griffith, Deborah A.,Oballa, Renata M.,Percival, M. David,Riendeau, Denis,Robichaud, Joel,Rodan, Gideon A.,Rodan, Sevgi B.,Seto, Carmai,Therien, Michel,Truong, Vouy Linh,Wesolowski, Gregg,Young, Robert N.,Zamboni, Robert,Black, W. Cameron
scheme or table, p. 887 - 892 (2010/08/22)
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo studies
CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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Page/Page column 44, (2010/02/12)
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Heterocyclic neophane analogs, processes for their preparation and their use as pest-combating agents
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, (2008/06/13)
Compounds of the formula (I) and their stereoisomers STR1 wherein A, B, C' and D independently of one another denote CH or N, in which at least one of the symbols A, B, C' or D must correspond to a nitrogen atom, X denotes CH2 or oxygen, R1 denotes a radical bonded to a carbon atom from the series comprising H, trialkylsilyl, halogen, nitro, cyano, alkenyl, alkynyl, amino, cycloalkyl, phenyl, phenxy, alkoxy, alkenyloxy, alkynyloxy, hydroxycarbonyl, alkylthio, cycloalkyloxy, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxy, halogenoalkylthio, halogenoalkoxyalkyl, alkylthioalkyl, alkoxyalkoxy, halogenoalkoxyalkoxy, alkenyloxyalkoxy, halogenoalkenyloxy, alkoxyalkylthio, alkylthioalkoxy, alkylthioalkylthio, halogenoalkoxycarbonyl, halogenoalkenyloxycarbonyl or dialkylamino or two radicals R1 when they are positioned ortho to one another together denote a methylenedioxy, ethylenedioxy or alkylene radical, R2 and R3 independently of one another denote alkyl, alkenyl or phenyl, or R2 and R3 denote an alkylene chain which--together with the quaternary carbon atom-forms an unsubstituted or fluorinesubstituted ring having three to six ring members, R4 denotes --H, F, --CN, --CCl3, --C CH, (C1 -C4)alkyl, --C--NH2, S R5 denotes pyridyl, furyl or thienyl which can all be substituted, phthalimidyl, dialkylmaleimidyl, thiophthalimidyl, dihydrophthalimidyl, tetrahydrophthalimidyl or substituted phenyl, or R4 and R5 --together with the carbon atom bridging them--denote an optionally substituted indanyl, cyclopentenoyl or cyclopentenyl radical and n denotes 0, 1 or 2, possess advantageous properties for combating pests, in particular insects and acarids. Furthermore, processes for the preparation of compounds of the formula I are described.