- HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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Page/Page column 35; 36
(2019/01/17)
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- NOVEL 5 OR 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
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Disclosed herein are 5 or 8-substituted imidazo[l,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[l,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8- substituted imidazo[l,5-a]pyridines that can be useful for inhibiting indoleamine 2,3- dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.
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Paragraph 0543
(2016/10/31)
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- Highly enantioselective desymmetrizations of meso-anhydrides
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Readily available, low molecular cyclohexane-based organocatalysts promote highly enantioselective desymmetrizations of cyclic meso-anhydrides applying alcohols and benzyl mercaptan as nucleophiles. Both succinic and glutaric anhydrides furnished the corresponding products with up to 96% ee in mostly quantitative yields.
- Schmitt, Ellen,Schiffers, Ingo,Bolm, Carsten
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experimental part
p. 6349 - 6357
(2010/10/03)
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- Pyridine derivatives
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Pyridine compounds of general formula: wherein —R1represents in which R11is hydrogen, C1-6alkyl, halogen, hydroxy, C1-12alkoxy, nitro, amino, C1-6alkylsulfonylamino, C1-6alkoxycarbonyl, C1-6alkylamino, di(C1-6alkyl)amino, C1-6alkanoylamino, phenyl C1-6alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2represents hydrogen or halogen; R3represents hydrogen, —CR31R32R33, or —NR34R35; R4is hydrogen, carbamoyl, CN, carboxyl, etc.; R5is amino, C1-6alkylamino, di C1-6alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
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- Enzymatic desymmetrization of cis-1,3-cyclohexanedicarboxylic acid diesters
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cis-1,3-Cyclohexanedicarboxylic acid (1,3-CHDA) monoesters were prepared in high overall yield and high enantiomeric purity using a three step process from cis/trans-1,3-CHDA. The asymmetry is induced by an enzymatic hydrolytic desymmetrization of a meso
- Boaz, Neil W.
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p. 813 - 816
(2007/10/03)
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- Thiazolidinone compounds and composition for angina pectoris comprising the compounds as an active ingredient
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A thiazolidinone compound represented by general formula (I) or a pharmacoligically acceptable salt thereof, STR1 wherein W represents sulfur or oxygen and X represents --N(R1)--, or alternatively X represents sulfur or oxygen and W represents --N(R1)--, and R1 represents hydrogen, alkyl or substituted alkyl; R2 and R3 are the same or different from each other, and each represents hydrogen, alkyl, substituted alkyl, aryl, or 5- or 6-membered heteroaryl; R4 represents hydrogen, alkyl or substituted C1 -C4 alkyl; R5 represents substituted cycloalkyl which may contain nitrogen, provided the substituents include --B--ONO2 (wherein B represents a single bond or alkylene) as the indispensable member and alkyl groups as optional members; and A represents a single bond or alkylene, has an excellent anti-anginal effect and thus is useful as an angina pectoris remedy or preventive.
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- Reaction Pathways of 3-(3'-Methylenecyclobutyl)propyl and 2-(3'-Methylenecyclobutyl)ethyl Radicals
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Molecular mechanics (MM2) calculations were used to predict the efficacy and regiochemical outcome of radical cyclizations involving the title radicals and others with further substitution at C1 on the ring.The MM2 results were generally ratifi
- Pigou, Paul E.
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p. 4943 - 4950
(2007/10/02)
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