- Bromine structural domain inhibitor compound and application thereof
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The invention relates to a bromine structural domain inhibitor and provides a compound shown in a general formula I, pharmaceutical salt, an enantiomer, a diastereoisomer, an atropisomer, racemate, apolymorphic substance and solvate of the compound or an isotope labelled compound (including a deuterium substituted compound), a preparation method of the compound, pharmaceutical composition containing the compound and an application of the above components in pharmaceuticals.
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Paragraph 0817-0820
(2019/08/02)
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- Synthesis of benzyl alcohol building blocks bearing an aldehyde, pinacol borane or carboxylic acid motif via lithium-bromide exchange
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A range of useful disubstituted benzyl alcohol building blocks have been synthesised in multigram quantities in a lithium-bromide exchange to give aldehyde, carboxylic acid and pinacol -boranes in high yields. Georg Thieme Verlag Stuttgart · New York.
- Blades, Kevin,Box, Matthew R.,Howe, Nick J.,Kemmitt, Paul D.,Lamont, Gillian M.
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supporting information
p. 123 - 127
(2014/01/06)
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- Synthesis of structurally diverse diarylketones through the diarylmethyl sp3 C-H oxidation
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Under open-flask conditions, an efficient method to assemble a series of diversely functionalized diarylketones in the presence of commercially available NBS has been developed. Yields of up to 99% have been achieved employing diarylmethanes as starting material. Based on 18O-labeled experiment, the addition of stoichiometric water eventually leads to excellent yields in all carbonylation cases.
- He, Chao,Zhang, Xiaohui,Huang, Ruofeng,Pan, Jing,Li, Jiaqiang,Ling, Xuege,Xiong, Yan,Zhu, Xiangming
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supporting information
p. 4458 - 4462
(2014/08/05)
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- TGR5 AGONISTS
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TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
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Page/Page column 158-159
(2011/06/26)
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- METHOD FOR PRODUCING PRECURSORS FOR L-2- [18F] FLUOROPHENYLALANINE AND 6- [18F] FLUORO-L--META-TYROSINE AND THE ALPHA-METHYLATED DERIVATIVES THEREOF, PRECURSOR, AND METHOD FOR PRODUCING L-2- [18F] FLUOROPHENYLALANINE AND 6- [18F] FLUORO-L-META-TYROSINE AN
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Disclosed is a method for producing precursors for 2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the α-methylated derivatives thereof, to the precursor, and to a method for producing 2-[18F]fluorophenyla
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Page/Page column 4
(2010/10/19)
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- TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY
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The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprise
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Page/Page column 147-148
(2012/01/30)
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- 2-Heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl; R1 is 1, 2 or 3 substituents selected from H, alkyl, alkoxy and halo; Z is optionally substituted-aryl, or optionally substituted-heteroaryl; are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.
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Page/Page column 11-12
(2008/06/13)
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- 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 A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.
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Page/Page column 176
(2010/11/27)
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- Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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Page/Page column 20
(2008/06/13)
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- 2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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- Insecticidal ethers
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Insecticidally active compounds of the formula (I): STR1 wherein R4 represents a group selected from those groups represented by R5 in insecticidally active compounds of formula: STR2 R3 is selected from fluoromethyl and difluoromethyl, and either (a) R1 and R2 represent alkyl of one, two, three or four carbon atoms, or (b) R1 and R2 taken together with the adjacent carbon atom form a cycloalkyl ring of four, five or six carbon atoms.
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- Intermediates for preparation of 3-bromo-4-fluoro-benzyl alcohol
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A process for the preparation of 3-bromo-4-fluoro-benzyl alcohol of the formula STR1 comprising reacting 3-bromo-4-fluoro-benzoic acid or a derivative thereof of the formula STR2 in which R is a hydrogen atom, an alkyl radical or an alkoxycarbonyl radical
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