摘要:
This disclosure relates to flavour modification and to compounds of formula (I) wherein X is -(CH 2)m - wherein m is an integer from 7 to 10, or X is C 7 -C 10 alkenyl, and i) n is 1, R 1 and R 3 are hydrogen, and R 2 is the residue of a proteinogenic amino acid; ii) n is 1, R 2 is hydrogen, and R 1 and R 3 together are - CH 2 - CH 2 - CH 2 -; or iii) n is 2 or 3 and R 1 , R 2 and R 3 are hydrogen, modifying flavours.
摘要:
The present invention provides a method for acylating one or more amino groups of a peptide where the acylation reaction is to be performed in an aqueous mixture containing less than 10 %w/w aprotic polar solvent. a) reacting the peptide having at least one free amino group with an acylating agent of the general formula I wherein n, is 0-8 R1is COOR4; R2 is a lipophilic moiety; R3 together with the carboxyl group to which R3 is attached designate a reactive ester or a reactive N-hydroxy imide ester; and R4 is selected from hydrogen, C1-12-alkyl and benzyl, under basic conditions in an aqueous mixture;
摘要:
Novel compounds which are 2,6-di-t-butytphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a group which includes carboxyl, tetrazolyl or N-methyltetrazolyl are useful as inhibitors of leukotriene synthesis and as antiallergic agents. Pharmaceutical compositions containing such compounds and pharmacological methods for use of such compounds are also disclosed.
摘要:
This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要:
A process for producing a compound represented by general formula (I) (E-isomer), wherein R and R are the same or different and each represents hydrogen or alkyl; and R represents hydrogen or alkyl which comprises eliminating the protecting group (P) of the hydroxyl group in the compound represented by general formula (II), wherein R , R and R are as defined above; P represents a protecting group of a hydroxyl group; and SIMILAR represents the configuration of an E- or Z-isomer or a mixture thereof; and an intermediate for the production of compound (I).
摘要:
Intermediate compounds for the preparation of endothelin-receptor antagonist triterpene compounds have the formula
wherein R 2 is hydrogen or -R 3- R 4 wherein R 3 is -SO 3 -, -CH 2 COO-, -COCOO-, or -COR 5 COO- wherein R 5 is C 1 - C 6 alkylene or up to C 6 alkenylene, R 4 is hydrogen, straight or branched C 1 - C 6 alkyl and R 6 is t-butoxycarbonyl or hydrogen, or a pharmaceutically acceptable salt thereof.