- N-(3-(2-(4-CHLOROPHENOXY)ACETAMIDO)BICYCLO[1.1.1]PENTAN-1-YL)-2-CYCLOBUTANE-1-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ATF4 INHIBITORS FOR TREATING CANCER AND OTHER DISEASES
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The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein X, a, b, C, D, L2,L3, Y1, Y2, R2, R4, R5, R6, z2, z4, z5, and z6 are 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 N-(3-(2-(4-chlorophenoxy) acetamido)bicyclo[1.1.1]pentan-l-yl)-2-cyclobutane-l-carboxamide derivatives and related compounds.
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Page/Page column 96; 97
(2019/01/21)
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- TRIAZOLE-ISOXAZOLE COMPOUND AND MEDICAL USE THEREOF
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A compound represented by Formula [I]: or pharmaceutically acceptable salt thereof, wherein each symbol is as defined in the description.
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Paragraph 3415
(2016/06/06)
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- Larvicidal activity and click synthesis of 2-alkoxyl-2-(1,2,3-triazole-1- yl)acetamide library
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Heterogeneous copper-in-charcoal-catalyzed click synthesis in 96-well polypropylene filter plates is an efficient method for the rapid generation of sufficient pure 2-alkoxyl-2-(1,2,3-triazole-1-yl) acetamide derivatives library by simple filtration, which directly assay the products for larvicidal activity against mosquitoes. In this procedure, copper nanoparticles on charcoal were arrayed into each well on a 96-well plate, reagents were delivered using a pipette gun, and a constant temperature shaker bath was used to complete the click reaction in 24-72 hours under temperature-controlled conditions. The results of bioassays indicated that the target compounds possessed excellent larvacidal activities against mosquitoes. In particular, the larvacidal activities against mosquitoes of compounds 8[2,3] and 8[7,1] at 2g.mL-1 were 100% and 73%, respectively.
- Su, Na-Na,Xiong, Li-Xia,Yu, Shu-Jing,Zhang, Xiao,Cui, Can,Li, Zheng-Ming,Zhao, Wei-Guang
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p. 484 - 493
(2013/07/28)
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- Novel Pyrimidine- And Triazine-Hepcidine Antagonists
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The present invention relates to new hepcidin antagonists, pharmaceutical compositions containing them and the use thereof as a drug, in particular for the treatment of iron metabolism disorders such as, in particular, iron deficiency diseases and anaemia, in particular anaemia associated with chronic inflammatory disease (ACD: anaemia of chronic disease and AI: anaemia of inflammation).
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- Asymmetric hydrogenation of α- Or β-acyloxy α,β- unsaturated phosphonates catalyzed by a Rh(i) complex of monodentate phosphoramidite
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The Rh(i) complex of a monodentate phosphoramidite bearing a primary amine moiety (DpenPhos) has been disclosed to be highly efficient for the asymmetric hydrogenation of a variety of α- or β-acyloxy α,β- unsaturated phosphonates, providing the corresponding biologically important chiral α- or β-hydroxy phosphonic acid derivatives with excellent enantioselectivities (90->99% ee).
- Zhang, Jinzhu,Dong, Kaiwu,Wang, Zheng,Ding, Kuiling
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supporting information; scheme or table
p. 1598 - 1601
(2012/03/22)
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- 2-Arylbenzoxazoles as CETP inhibitors: Substitution and modification of the α-alkoxyamide moiety
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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.
- 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.
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scheme or table
p. 1019 - 1022
(2010/06/14)
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- SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
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Page/Page column 111
(2009/01/20)
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- SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I or Formula II wherein RIa, RIb, RIc, B, R3, R4, R5 and W of Formula I, and RIa, RIb, RIc, R2, R2a, R3, R4, R5, R6, Al, A2, A3, A4, W, X, Z, m and n of Formula II are defined herein.
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Page/Page column 146
(2009/01/20)
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- Lewis base activation of Lewis acids: Catalytic, enantioselective addition of glycolate-derived silyl ketene acetals to aldehydes
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(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
- Denmark, Scott E.,Chung, Won-Jin
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p. 4582 - 4595
(2008/09/21)
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- PYRROLOPYRIDAZINE DERIVATIVES
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The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.
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- An improved and practical synthesis of 5,5-dimethyl-3-(2-propoxy)-4-(4-methanesulfonylphenyl)-2-(5H)-furanone (DFP - A selective inhibitor of cyclooxygenase-2)
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DFP, a highly selective and potent COX-2 inhibitor, has been synthesized by a modified approach. Three modifications of the existing method enabled us to prepare DFP in good quantity.
- Padakanti, Srinivas,Pal, Manojit,Yeleswarapu, Koteswar Rao
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p. 7915 - 7920
(2007/10/03)
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- Pyrimidine derivatives
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The present invention relates to trisubstituted pyrimidines of formula (I) 1wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
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- Process for making phenyl heterocycles useful as COX-2 inhibitors
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The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
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- Quinazoline derivatives
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The invention concerns quinazoline derivatives of formula wherein n is 1, 2 or 3 and each R2 is independently halogeno; and R1 is 1-4C)alkoxy-(2-4C)alkylamino; or pharmaceutically-acceptable salts thereof; processes for their prepara
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- SAR in the alkoxy lactone series: The discovery of DFP, a potent and orally active COX-2 inhibitor
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Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4- methanesulfonylphenyl)-2(5H)-furanone), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied.
- Leblanc,Roy,Boyce,Brideau,Chan,Charleson,Gordon,Grimm,Guay,Leger,Li,Riendeau,Visco,Wang,Webb,Xu,Prasit
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p. 2207 - 2212
(2007/10/03)
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- Sulfinyl imidazole derivatives and antiulcer agents containing the same
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Disclosed are novel imidazole derivatives having the formula: STR1 wherein R1 is hydrogen or an alkyl group having 1-6 carbon atoms, R2 is an alkyl group having 2-6 carbon atoms substituted with an alkoxy group having 1-4 carbon atom
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- 1-carboalkoxyalkyl-3-alkoxy-4-(2'-carboxyphenyl)-azet-2-ones as plant growth regulators and selective herbicides
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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.
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- Photolysis of Alkoxyacetic Acids in the presence of Mercury(II) Oxide and Iodine
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Homolytic decarboxylation of a series of alkoxyacetic acids has furnished alkoxyalkyl alkoxyacetates when no substituents were present at the 2-position.Electron donating and withdrawing 2-substituents, with the exception of trichloromethyl, afforded products due to fragmentation of the alkoxyacetic acids.The reaction pathway is rationalised on the basis of the reactivity of the alkoxyalkyl iodide intermediates.
- Glover, Stephen A.,Golding, Stephen L.,Goosen, Andre,McCleland, Cedric W.
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p. 2479 - 2483
(2007/10/02)
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