- 2-ARYLSULFONAMIDO-N-ARYLACETAMIDE DERIVATIZED STAT3 INHIBITORS
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The present disclosure provides pharmaceutical compositions comprising 2-arylsulfonamido-N-arylacetamide derivatized Stat3 inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use.
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Paragraph 00351
(2018/08/20)
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- Methods for producing N-protected-azetidine-2-carboxylic acids
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There is disclosed a method for producing an essentially enantiomerically pure N-protected-azetidine-2-carboxylic acid of formula (1): which method is characterized by: subjecting a crude enantiomerically excess N-protected-azetidine-2-carboxylic acid comprising said enantiomer represented by formula (1) in excess to the other enantiomer thereof to crystallization in an organic solvent selected from aromatic hydrocarbon, aliphatic ether, aliphatic alcohol, aliphatic ketone, aliphatic nitrile, aliphatic amide, aliphatic sulfoxide, aliphatic ester and a mixed solvent thereof, wherein R is: an optionally substituted alkyl, alicyclic or alicyclicalkyl group, an optionally substituted alkenyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, or a dialkylamino group, and absolute configuration of the asterisked asymmetric carbon atom is S or R.
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- Novel arginine, glycine, aspartic acid derivatives as platelet-aggregation inhibitors
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Disclosed are novel amino acid derivatives of the formula: STR1 wherein X is H, amidino or STR2 Y is H, amino or STR3 Z is STR4 OR1 or a naturally occurring L-amino acid, bounded to the carbon atom at the α-amino position; R is alkyl, aryl or aralkyl; R1 and R2 are independently H, alkyl, aryl, aralkyl or allyl; m is 1 through 5; n is 0 through 4; and pharmaceutically acceptable salts thereof, that inhibit platelet aggregation and thrombus formation in mammalian blood.
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- Anti-thrombotic peptide and pseudopeptide derivatives
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Disclosed are novel peptide and pseudopeptide derivatives and phrmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
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