摘要:
The crystalline dihydrochloride of a specific cephalosporin derivative is stable to heat and retains its antibacterial activity even after storage over long periods at high temperature. The crystalline dihydrochloride can be obtained by removing protective groups from the cephalosporin derivative wherein the amino group and carboxy groups are protected and then crystallizing the cephalosporin derivative from a hydrochloric acid aqueous solution. The crystalline dihydrochloride is useful for pharmaceutical preparations.
摘要:
Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereon. The compounds are useful as antiallergic agents and exhibit excellent bioavailability. wherein R1 represents hydrogen, OH, alkyl or phenyl alkyl, R2, R3, R4, and R5 represent hydrogen, halogen, optionally protected hydroxyl, formyl, optionally substituted alkyl, alkenyl, alkoxy or the like, and Q represents a group selected from the following groups (i) to (iv), halogen, or alkoxy:
摘要:
A process for preparing a compound represented by formula (IIa′) wherein Q represents group (i) as defined in the specification and R2 to R5, R31, R32, and R52 are as defined in the specification, by (1) reacting a compound represented by formula (V) wherein R2 to R5 and R52 are as defined in the specification. with a compound represented by R31R32C═O wherein R31 and R32 are as defined in the specification; (2) reacting the compound prepared in (1) with a compound represented by R71—C(═O)—R72 wherein R71 and R72 each independently represent a chlorine atom, 4-nitrophenyl, or 1-imidazolyl; and (3) reacting the compound prepared in (2) with a compound represented by R33OH wherein R33 is as defined in the specification.
摘要:
Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereon. The compounds are useful as antiallergic agents and exhibit excellent bioavailability. wherein R1 represents hydrogen, OH, alkyl or phenyl alkyl, R2, R3, R4, and R5 represent hydrogen, halogen, optionally protected hydroxyl, formyl, optionally substituted alkyl, alkenyl, alkoxy or the like, and Q represents a group selected from the following groups (i) to (iv), halogen, or alkoxy:
摘要:
Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds are useful as antiallergic agents and exhibit excellent bioavailability. wherein R1 represents hydrogen, OH, alkyl or phenyl alkyl, R2, R3, R4, and R5 represent hydrogen, halogen, optionally protected hydroxyl, formyl, optionally substituted alkyl, alkenyl, alkoxy or the like, and Q represents a group selected from the following groups (i) to (iv), halogen, or alkoxy:
摘要:
Desalaninebenanomicin A has been synthesized by chemical conversion of benanomicin A. Amino acid derivatives of desalaninebenanomicin A having the general formula (Ia): ##STR1## where R.sup.a represents a hyhrogen atom, a C.sub.1-5 alkyl group, a C.sub.1-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group have been synthesized by condensing the 2-carboxyl group of desalaninebenanomicin A with a variety of amino acids. Among the derivatives of the formula (Ia) having antifungal activities, such desalaninebenanomicin A derivatives in which R.sup.a is a C.sub.2-5 alkyl group, a C.sub.2-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group are novel semi-synthetic antibiotics having antifungal activities.
摘要:
The present invention relates to a compound of formula (1), wherein R1, R2, R3, n, and X are as defined in the specification, and a process for producing the same. This compound is useful as an intermediate for the synthesis of compounds useful as pharmaceuticals or agricultural chemicals.
摘要:
The present invention relates to a compound of formula (1), wherein R1, R2, R3, n, and X are as defined in the specification, and a process for producing the same. This compound is useful as an intermediate for the synthesis of compounds useful as pharmaceuticals or agricultural chemicals.
摘要:
Tricyclic benzazepine compounds represented by the following formula (I) and pharmacologically acceptable salts thereof are disclosed. These compounds have antiallergic activity and are useful for treatment and prevention of bronchial asthma, eczema, hives, allergic gastrointestinal troubles, allergic rhinitis, allergic conjunctivitis, etc. wherein R represents a hydrogen atom, substituted C.sub.1-6 alkyl or a protective group and R.sup.1, R.sup.2, R.sup.3, and R.sup.4 represent a hydrogen atom, a hydroxyl group, substituted C.sub.1-4 alkyl, substituted C.sub.2-12 alkenyl, substituted C.sub.1-12 alkoxy, or substituted amino.