13211-32-0Relevant articles and documents
2-(4-CHLOROPHENOXY)-N-((1 -(2-(4-CHLOROPHENOXY)ETHYNAZETIDIN-3-YL)METHYL)ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ATF4 INHIBITORS FOR TREATING CANCER AND OTHER DISEASES
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Page/Page column 76, (2019/01/21)
The invention is directed to substituted azetidine derivatives. Specifically, the invention is directed to compounds according Formula I: (I) wherein C, D, L1,L2,L3,R1, R2, R4, R5, R6, z2, z4, z5, and z6are as defined herein; and salts thereof. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to compounds for use in methods of inhibiting the ATF4 (activating transcription factor 4) pathway and treatment of disorders associated therewith, such as e.g. cancer, neurodegenerative diseases and many other diseases, using a compound of the invention or a pharmaceutical composition comprising a compound of the invention. Preferred compounds of the invention are 2-(4-chlorophenoxy)-N-((l- (2-(4-chlorophenoxy)ethynazetidin-3-yl)methyl)acetamide derivatives and related compounds.
METHODS OF PREPARING CARBOCYCLIC NUCLEOSIDES
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Page/Page column 24, (2017/12/18)
The present disclosure provides methods of preparing carbocyclic nucleosides, in particular, Prurisol? ((-) cis-[4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-hydroxymethyl acetate).
PROCESS FOR THE PREPARATION OF A GLUCOKINASE ACTIVATOR COMPOUND
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Page/Page column 8, (2011/04/14)
The present invention relates to a process for the preparation of a compound of formula I, wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen. (R)-2-phenyl propionic acid derivatives of formula I are key intermediates in the synthesis of 5-substituted-pyrazine or pyridine glucokinase activators of the formula Xa, which have the potential to be useful for the treatment and/or prophylaxis of type II diabetes.
PROCESS FOR THE PREPARATION OF A GLUCOKINASE ACTIVATOR COMPOUND
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Page/Page column 17, (2011/04/14)
The present invention related to a process for the preparation of formula (I), wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen. (R)-2-phenyl propionic acid derivatives of the formula (I) are key intermediates in the synthesis of 5-substituted -pyra
2-Arylbenzoxazoles as CETP inhibitors: Substitution and modification of the α-alkoxyamide moiety
Hunt, Julianne A.,Gonzalez, Silvia,Kallashi, Florida,Hammond, Milton L.,Pivnichny, James V.,Tong, Xinchun,Xu, Suoyu S.,Anderson, Matt S.,Chen, Ying,Eveland, Suzanne S.,Guo, Qiu,Hyland, Sheryl A.,Milot, Denise P.,Sparrow, Carl P.,Wright, Samuel D.,Sinclair, Peter J.
scheme or table, p. 1019 - 1022 (2010/06/14)
The development of a series of 2-arylbenzoxazole α-alkoxyamide and β-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated α-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole β-alkoxyamine 4 showed a desirable combination of in vitro potency (IC50 = 151 nM) and oral bioavailability in the mouse.
Lewis base activation of Lewis acids: Catalytic, enantioselective addition of glycolate-derived silyl ketene acetals to aldehydes
Denmark, Scott E.,Chung, Won-Jin
, p. 4582 - 4595 (2008/09/21)
(Chemical Equation Presented) A catalytic system involving silicon tetrachloride and a chiral, Lewis basic bisphosphoramide catalyst is effective for the addition of glycolate-derived silyl ketene acetals to aldehydes. It was found that the sense of diast
Evaluation of copper chelation agents as anti-angiogenic therapy
Camphausen, Kevin,Sproull, Mary,Tantama, Steve,Sankineni, Sandeep,Scott, Tamalee,Menard, Cynthia,Coleman, C.Norman,Brechbiel, Martin W.
, p. 4287 - 4293 (2007/10/03)
The design, synthesis and evaluation of N,N′,N″-tris(2-pyridylmethyl)-cis,cis-1,3,5,-triaminocyclohexane (tachpyr, 1) derivatives as novel anti-angiogenic agents were performed in an in vitro endothelial cell proliferation assay to assess their cytotoxicity and selectivity. The selective nature of the anti-angiogenic agents for human umbilical vein endothelial cells (Huvec) was compared to a normal fibroblast cell line and a human Glioma cell line to evaluate these compounds. N,N′,N″-tris(2-mercaptoethyl)-cis,cis-1,3,5-triaminocyclohexane trihydrochloride (3b) was superior to tachpyr in terms of selectivity of its inhibitory activity toward the proliferation of Huvec compared to the fibroblast and human Glioma cell lines.
Synthesis of chiral and achiral pyranenamine derivatives. Potent agents with topical ocular antiallergic activity
Gluchowski,Bischoff,Garst,Kaplan,Dietrich,Aswad,Gaffney,Aoki,Garcia,Wheeler
, p. 392 - 397 (2007/10/02)
The SS, RR and meso stereoisomers of pyranenamine SK and F 84210 (2) were synthesized stereospecifically starting from commercially available (R)-(-)- or (S)-(+)-2,2-dimethyl-1,3-dioxolane-4-methanol (3). In addition, two achiral pyranenamines 19 and 26 w
1-carboalkoxyalkyl-3-alkoxy-4-(2'-carboxyphenyl)-azet-2-ones as plant growth regulators and selective herbicides
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, (2008/06/13)
Compounds of the formula: STR1 wherein R1 is lower alkyl of 1 to 6 carbon atoms lower alkenyl of 2 to 6 carbon atoms or benzyl; R2 is lower alkoxy of 1 to 6 carbon atoms, benzyloxy or the group STR2 where R4 is lower alkoxy of 1 to 4 carbon atoms; and R3 is hydrogen, lower alkyl of 1 to 6 carbon atoms, lower alkyl of 1 to 6 carbon atoms substituted with 1 to 3 trihalomethyl groups, lower haloalkyl of 1 to 6 carbon atoms substituted with 1 to 6 halogen atoms, lower alkenyl of 2 to 6 carbon atoms, arylalkyl of 7 to 12 carbon atoms, lower alkoxyalkyl of 2 to 6 carbon atoms, lower alkylthioalkyl of 2 to 6 carbon atoms, or lower cycloalkyl of 3 to 8 carbon atoms are active as plant growth regulators. Certain of these compounds also show activity as selective herbicides.
2H-pyran-2,6-(3H)-dione derivatives with anti-allergic activity
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, (2008/06/13)
Achiral compounds of a 2H-pyran-2,6(3H)-dione derivative of the formula STR1 or a pharmaceutically acceptable salt thereof, where R is --(CH2)m OH or --CH((CH2)n CH2 OH)2 where m is 1-5 and n is 0-4. These compounds are useful in the treatment of allergic conditions.