- MATRIX METALLOPROTEINASE (MMP) INHIBITORS AND METHODS OF USE THEREOF
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Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.
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Paragraph 0532-0533
(2019/12/02)
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- Microwave-assisted N-debenzylation of amides with triflic acid
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A new and facile microwave-assisted protocol for the debenzylation of N-benzylamides with triflic acid has been developed. Both secondary and tertiary aliphatic or aromatic amides are obtained in moderate to good yields.
- Rombouts, Frederik,Franken, Dennis,Martínez-Lamenca, Carolina,Braeken, Mirielle,Zavattaro, Chiara,Chen, Jinsheng,Trabanco, Andrés A.
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experimental part
p. 4815 - 4818
(2010/10/02)
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- Azetidine derivatives, their preparation and medicaments containing them
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The invention concerns compounds of formula (1) wherein: R represents a chain (A) or (B); R1 is methyl or ethyl; R2 is either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R3 and R4, identical or different, are either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R′ represents a hydrogen atom or a —CO—alk radical, their optical isomers, their salts, their preparation and medicines containing them.
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- Synthesis of 3-substituted benzamides and 5-substituted isoquinolin-1(2H)-ones and preliminary evaluation as inhibitors of poly(ADP-ribose)polymerase (PARP)
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Inhibitors of poly(ADP-ribose)polymerase (PARP) inhibit repair of damaged DNA and thus potentiate radiotherapy and chemotherapy of cancer. 3-Substituted benzamides and 5-substituted isoquinolin-1-ones have been synthesised and evaluated for inhibition of PARP. Reduction of 3-(bromoacetyl)benzamide, followed by treatment with base, gave RS-3-oxiranylbenzamide. Reduction of 3-(hydroxyacetyl)benzonitrile with bakers' yeast gave the R-diol which was converted to R-3-(1,2-dihydroxyethyl)benzamide. Similar reduction of 3-(acetoxyacetyl)benzonitrile led towards the S-diol which was converted to its cyclic acetonide. E-2-(2,6-Dicyanophenyl)-N,N-dimethylethenamine was formed by condensation of 2,6-dicyanotoluene with dimethylformamide dimethyl acetal (DMFDMA); cyclisation under acidic conditions afforded 5-cyanoisoquinolin-1-one. Heck coupling of 5-iodoisoquinolin-1-one with propenoic acid formed E-3-(1-oxoisoquinolin-5-yl)propenoic acid. 3-Oxiranylbenzamide, 5-bromoisoquinolin-1-one and 5-iodoisoquinolin-1-one were among the most potent inhibitors of PARP activity in a preliminary screen in vitro. Copyright (C) 1998 Elsevier Science Ltd.
- Watson, Corrine Y.,Whish, William J. D.,Threadgill, Michael D.
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p. 721 - 734
(2007/10/03)
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- IMIDAZOLIDINE ANTIPSYCHOTIC AGENTS
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Compounds of the general formula I STR1 are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I.
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- SYNTHESIS OF SOME NOVEL α,β-ETHYLENIC SULFONES
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Novel unsaturated sulfones E-alkoxy/carbamoyl benzyl styryl sulfones (VI) and E-4(N-benzylcarbamoyl)benzyl styryl sulfones (IX) have been prepared by the Knoevenagel condensation of alkoxy/carbamoyl benzylsulfonylacetic acid (V) and 4-carboxybenzylsulfonylacetic acid (VIII) with araldehydes.The E-geometry of these compounds has been assigned based on IR and 1H NMR spectral data. Key words: Configuration, Knoevenagel condensation, sulfonylacetic acids, unsaturated sulfones.
- Reddy, M. V. Ramana,Vijayalakshmi, S.,Reddy, D. Bhaskar,Reddy, P. V. Ramana
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p. 209 - 214
(2007/10/02)
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