- HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
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Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
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Paragraph 0459; 0609
(2021/01/23)
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- Functionalized Dialdehydes as Promising Scaffolds for Access to Heterocycles and β-Amino Acids: Synthesis of Fluorinated Piperidine and Azepane Derivatives
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Functionalized dialdehydes are considered important substrates that can be transformed into various substituted heterocyclic, alicyclic, and polysubstituted compounds. Here, we report a robust stereocontrolled procedure for the synthesis of novel functionalized trifluoromethyl-containing piperidine and azepane derivatives, based on oxidative ring cleavage of the C=C bond of diversely substituted cycloalkenes, followed by reductive ring closure of the diformyl intermediates in the presence of fluorine-containing amines.
- ábrahámi, Renáta A.,Kiss, Loránd,Fustero, Santos,Fül?p, Ferenc
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p. 1206 - 1213
(2017/03/11)
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- Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 0486-0487
(2016/08/17)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
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Page/Page column 151
(2015/02/02)
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- Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 0485; 0486
(2015/06/17)
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- NOVEL INDAZOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION
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The invention provides novel compounds having the general formula: formula (I) wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 98
(2014/02/15)
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- THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHOD OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
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Page/Page column 207
(2012/02/02)
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- New route to 4-aminocyclopent-2-en-1-ols: Synthesis and enantioselective rearrangement of 4-amino-substituted cyclopentene oxides
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A new route for the asymmetric synthesis of 4-aminocyclopent-2-en-1-ols (90% ee) for carbocyclic nucleoside analogue synthesis is described. The approach involves the stereoselective preparation of cis 4-amino-substituted cyclopentene oxides and subsequent chiral base-mediated rearrangement to the corresponding allylic alcohols. Full details on the synthesis and stereoselectivity of epoxidation of 4-amino-substituted cyclopentenes are presented. (C) 2000 Elsevier Science Ltd.
- Barrett, Stephen,O'Brien, Peter,Steffens, H.Christian,Towers, Timothy D,Voith, Matthias
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p. 9633 - 9640
(2007/10/03)
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- 2-amino-5,6-dichlorobenzimidazole derivatives having antiviral activity
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The present invention relates to benzimidazole derivatives of formula (I) wherein: R1 represents H, C1-4 alkyl, C3-5 cycloalkyl; R2 represents H, C1-4 alkyl; or R1 and R2 together form with the nitrogen a 4 or 5 membered heterocyclic ring; R3 represents BR4 or R4 wherein B represents a bridging group --C(O)NH--, --C(O)NC1-4 alkyl-, or C(O)O-- and R4 represents H, C1-4 alkyl, C2-6 alkenyl or halo (preferably fluoro); and each n is an integer independently selected from 0, 1, or 2 (preferably 0 or 1); and geometric isomers or mixtures thereof; and physiologically functional derivatives thereof, and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to their preparation and pharmaceutical formulations containing them.
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- Synthesis and enantioselective rearrangement of 4-amino-substituted cyclopentene oxides
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Several N-mono- and diprotected alkenes have been prepared and the stereoselectivity of their epoxidation has been investigated: N-monoprotected alkenes give cis epoxides preferentially (due to hydrogen bonding directed epoxidations) whereas N-diprotected alkenes produce trans epoxides exclusively (due to steric effects). Chiral lithium amide base-mediated rearrangement of a cis-monoprotected epoxide generated the corresponding amino-cyclopentenol in good yield and with an enantiomeric excess of 60%.
- O'Brien, Peter,Towers, Timothy D.,Voith, Matthias
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p. 8175 - 8178
(2007/10/03)
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- Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety
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Balanol is a potent protein kinase C (PKC) inhibitor that is structurally composed of a benzophenone diacid, a 4-hydroxybenzamide, and a perhydroazepine ring. A number of balanol analogs in which the perhydroazepine moiety is replaced have been synthesized and their biological activities evaluated against both PKC and cAMP-dependent kinase (PKA). The results suggested that the activity and the isozyme/kinase selectivity of these compounds are largely related to the conformation about this nonaromatic structural element of the molecules.
- Lai, Yen-Shi,Mendoza, José S.,Jagdmann Jr., G. Erik,Menaldino, David S.,Biggers, Christopher K.,Heerding, Julia M.,Wilson, Joseph W.,Hall, Steven E.,Jiang, Jack B.,Janzen, William P.,Ballas, Lawrence M.
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p. 226 - 235
(2007/10/03)
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