摘要:
An industrial microbicide which comprises at least one haloglyoxime derivative of the formula (I):
wherein X is a halogen atom; Y is a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; and Z is a hydrogen atom or an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms; and a known industrial microbicidal ingredient selected from the group consisting of an organonitrogen-sulfur compound, an organohalogen compound, an organonitrogen compound and an organosulfur compound; and optionally a carrier or diluent. Also claimed is: An industrial microbicide which comprises as an effective ingredient at least one haloglyoxime derivative of the formula (I'):
wherein X is a halogen atom; Y is a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; and Z' is a hydrogen atom or an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms; provided that Z' is an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms when Y is a halogen atom, and optionally a carrier or diluent.
wherein R¹ means hydrogen and R² means hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms; Ar means phenyl, a phenyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, amino, nitro and cyano, furyl, a furyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, thienyl, a thienyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, pyrrolyl, a pyrrolyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, pyridyl, or a pyridyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano: Y means a single bond or a straight-chain or branched chain alkylene having 1 to 8 carbon atoms which may have double bond(s) in the chain; W means a group of the formula (i)
(wherein R³ and R⁴ are the same or different and respectively mean hydrogen or a halogen, X means -O- or -S-, Z means a single bond or -O-, A is a straight-chain or branched chain alkylene having 1 to 8 carbon atoms, B means -N(R⁸)(R⁹) (wherein R⁸ and R⁹ are the same or different and respectively mean hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms, or combinedly means a group forming, taken together with the adjacent nitrogen, 1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, piperidino, 1-piperazinyl, a 1-piperazinyl substituted by a straight-chain or branched chain alkyl having 1 to 8 carbon atoms at the 4-position, 1-homopiperazinyl, morpholino and thiomorpholino) or a group of the formula (ii)
(wherein R¹² and R¹³ are the same or different and respectively mean hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms, P is -S- and Q is hexamethylene, heptamethylene, octamethylene, 1-methylpentamethylene, 1-methylhexamethylene, 1-methylheptamethylene, -(CH₂)₂S(CH₂)₃-, -(CH₂)₂S(CH₂)₆-.
or
a pharmaceutically acceptable salt thereof or a hydrate thereof. The compounds exhibit inhibitory activity on prolylendopeptidase. Also disclosed are pharmaceutical compositions containing the novel pyridine compounds.
摘要:
Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula
wherein R 1 is hydrogen, R 2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocar- bonylethyl or alkyl having 6 to 12 carbon atoms, or R 1 and R 2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R 3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R 4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R 5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.
摘要:
This invention relates to an immunosuppressant comprising an effective amount of at least one compound selected from among compounds represented by formula (I), (wherein R represents a hydrogen atom or an acyl group, Y represents a carbonyl or hydroxymethylene group, and symbol ------- represents either a single bond or a double bond) and their lactones and a pharmaceutically acceptable carrier, a method of prophylaxis and treatment of immunorejection or autoimmune diseases comprising administering an effective amount of the above-described compound or its lactone, and a novel compound represented by formula (II) and its lactone.
摘要:
Amino acid derivatives of formula (I), which specifically inhibit prolylendopeptidase activity and are useful for treating or preventing dementia and amnesia, wherein Q represents W-(CH2)m-(A)n-CO-B-, A represents oxygen or imino, B represents (II) or -(CH2)l-, X and Y represent each sulfur or methylene, W represents (III, IV) or (V), wherein Hal represents halogen, R represents hydrogen, formyl, C1 to C5 alkoxycarbonyl, cyano, or -CR1 = N - R2, R1 represents hydrogen, R2 represents hydroxy, C¿1? to C5 alkylcarboxy, phenylcarboxy, C1 to C5 alkoxy, or phenyl(C1 to C5) alkoxy, and n, m and l represent integers of, respectively, 0 or 1, 0 to 3, and 1 to 3, provided that W represents (VI) when R represents hydrogen, formyl or C1 to C5 alkoxycarbonyl.