摘要:
Pharmaceutically active salts and esters of 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol and 3-(3-dimethylamino-1-ethyl-1-hydroxy-2-methylpropyl)-phenol, and methods of using the same for treating or inhibiting increased urinary urgency or urinary incontinence and/or pain.
摘要:
A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group, or a pharmaceutically acceptable salt thereof as an active ingredient. The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor against lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.
摘要:
A compound having the formula R--S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.2, wherein R is a phenyl group or a heterocyclic group selected from furyl, thienyl, isoxazolyl, isothiazolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, 1,2,4-oxadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-oxadiazolyl, 1,3,4-thidiazolyl, tetrazolyl, pyridyl, pyridazinyl, pyrazinyl, 1,2,3-triazinyl, 1,3,4-triazinyl, and 1,3,5-triazinyl groups, said phenyl or heterocyclic group being optionally substituted by optionally substituted alkyl, optionally substituted alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, alkoxy, alkenyloxy, alkynyloxy, hydroxyalkyl, alkoxyalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxy, optionally substituted heteroarylalkoxy, optionally substituted heteroaryloxyalkyl, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkenyloxy, haloalkynyloxy, halogen, hydroxy, cyano, nitro, --NR7R8, --NR7COR8, --NR7CSR8, --NR7SO2R8, --N(SO2R7)(SO2R8), --COR7, --CONR7R8, -alkylCONR7R8, --CR7NR8, --COOR7, --OCOR7, --SR7, --SOR7, --SO2R7, -alkylSR7, -alkylSOR7, -alkylSO2R7, --OSO2R7, --SO2NR7R8, --CSNR7R8, --SiR7R8R9, --OCH2CO2R7, --OCH2CH2CO2R7, --CONR7SO2R8, -alkylCONR7SO2R8, --NHCONR7R8, --NHCSNR7R8, or an adjacent pair of R1, R2, R3, R4, R5 and R6 when taken together form a fused 5- or 6-membered carbocyclic or heterocyclic ring; R7, R8 and R9 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, alkynyl, optionally substituted aryl or optionally substituted arylalkyl, haloalkyl, haloalkenyl, haloalkynyl, halogen or hydroxy.
摘要翻译:具有式RS(O)nCH 2 CH 2 CH = CF 2的化合物,其中R是苯基或选自呋喃基,噻吩基,异恶唑基,异噻唑基,恶唑基,噻唑基,咪唑基,吡唑基,1,2,4-恶二唑基,1 2,4,4-噻二唑基,1,3,4-恶二唑基,1,3,4-噻二唑基,四唑基,吡啶基,哒嗪基,吡嗪基,1,2,3-三嗪基,1,3,4-三嗪基和1, 所述苯基或杂环基团任选被任选取代的烷基,任选取代的烯基,炔基,环烷基,烷基环烷基,烷氧基,烯氧基,炔氧基,羟基烷基,烷氧基烷基,任选取代的芳基,任选取代的芳基烷基, 杂芳基,任选取代的杂芳基烷基,任选取代的芳氧基,任选取代的芳基烷氧基,任选取代的芳氧基烷基,任选取代的杂芳氧基,任选取代的杂芳基烷氧基,任选取代的杂芳氧基烷基,卤代烷基,卤代烯基, 卤代炔基,卤代烷氧基,卤代烯氧基,卤代炔氧基,卤素,羟基,氰基,硝基,-NR7R8,-NR7COR8,-NR7CSR8,-NR7SO2R8,-N(SO2R7)(SO2R8),-COR7,-CONR7R8, - 烷基CONR7R8,-CR7NR8, COOR 7,-OCOR 7,-SR 7,-SOR 7,-SO 2 R 7, - 烷基R 7, - 烷基SOR 7, - 烷基SO 2 R 7,-OSO 2 R 7,-SO 2 NR 7 R 8,-CSNR 7 R 8,-SiR 7 R 8 R 9,-OCH 2 CO 2 R 7,-OCH 2 CH 2 CO 2 R 7,-CONR 7 SO 2 R 8, - 烷基CONR 7 SO 2 R 8,-NHCONR 7 R 8, -NHCSNR7R8或R 1,R 2,R 3,R 4,R 5和R 6的相邻对一起形成稠合的5元或6元碳环或杂环; R 7,R 8和R 9各自独立地为氢,任选取代的烷基,任选取代的烯基,炔基,任选取代的芳基或任选取代的芳基烷基,卤代烷基,卤代烯基,卤代炔基,卤素或羟基。
摘要:
The invention describes novel 3-cyano-4-sulfenylated-5-alkoxy-1-arylpyrazoles of general formula(I) ##STR1## wherein typically preferred substituents are: R is C.sub.1 to C.sub.4 alkyl fully substituted by halogen;R.sub.1 is C.sub.1 to C.sub.4 alkyl, C.sub.3 to C.sub.6 alkenyl and alkynyl or aralkyl (each of which may be optionally substituted), dialkylaminocarbonyl or a group --P(.dbd.X)(Oalkyl)(Salkyl) wherein X is oxygen or sulfur;R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are each hydrogen or halogen;R.sub.4 is CF.sub.3, OCF.sub.3, SCF.sub.3, SOCF.sub.3, SO.sub.2 CF.sub.3, OCHF.sub.2, halogen or alkyl; and n is 0, 1 or 2.The invention further relates to intermediates and processes to make the compounds and to compositions thereof and to methods of control of arthopod (especially insect) nematode, helminth, and protozoan pests.
摘要:
The invention describes novel 3-cyano-4-sulfenylated-5-alkoxy-1-arylpyrazoles of general formula (I) ##STR1## wherein typically preferred substituents are: R is C.sub.1 to C.sub.4 alkyl fully substituted by halogen;R.sub.1 is C.sub.1 to C.sub.4 alkyl, C.sub.3 to C.sub.6 alkenyl and alkynyl or aralkyl (each of which may be optionally substituted), dialkylaminocarbonyl or a group --P(=X)(Oalkyl)(Salkyl) wherein X is oxygen or sulfur;R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are each hydrogen or halogen;R.sub.4 is CF.sub.3, OCF.sub.3, SCF.sub.3, SOCF.sub.3, SO.sub.2 CF.sub.3, OCHF.sub.2, halogen or alkyl; and n is 0, 1 or 2.The invention further relates to intermediates and processes to make the compounds and to compositions thereof and to methods of control of arthopod (especially insect) nematode, helminth, and protozoan pests.
摘要:
1-Aryl-4-.gamma.-arylsulphonyl-3-aminopropoxy-1H-pyrazoles of the formula: ##STR1## and their acid addition salts. Application of these compounds as medicaments useful in particular as hypolipemiant or hypocholesterolemiant agents.
摘要:
Pyrazoles of the formula ##STR1## wherein R is hydrogen, alkyl, aryl, aralkyl, trifluoromethyl or a heterocycle;R.sup.1 is aryl or aralkyl unsubstituted or substituted by halo, trifluoromethyl, alkyl, alkoxy or nitro; or a halo-substituted alkylthio moiety;R.sup.2 is lower alkyl; phenyl; or benzyl;R.sup.3 is aryl unsubstituted or substituted by alkyl, alkenyl, alkoxy, halo, trifluoromethyl, trifluoromethoxy, mono- or di-alkylamino, nitro, cyano, carboxamido, sulphonamido or SO.sub.n -alkyl; phenyl having fused thereto a 5- to 7-membered isocyclic or heterocyclic ring, said heterocyclic ring having 1 or 2 oxygen or sulphur heteroatoms; or pyridyl; andR.sup.4 is unsubstituted or substituted carboacyl or sulphonyl;Are useful for their diuretic, saluretic, antihypertensive and antithrombotic properties.
摘要翻译:其中R为氢,烷基,芳基,芳烷基,三氟甲基或杂环的吡唑类化合物。 R 1为未取代或被卤素,三氟甲基,烷基,烷氧基或硝基取代的芳基或芳烷基; 或卤素取代的烷硫基部分; R2是低级烷基; 苯基; 或苄基; R 3为未取代的或被烷基,烯基,烷氧基,卤素,三氟甲基,三氟甲氧基,单 - 或二 - 烷基氨基,硝基,氰基,甲酰氨基,磺酰氨基或SO-烷基取代的芳基; 与5至7元环或杂环稠合的苯基,所述杂环具有1或2个氧或硫杂原子; 或吡啶基; 并且R 4是未取代的或取代的碳酰基或磺酰基; 有用于他们的DIYTIC,SALURETIC,ANTIHYPERTENSIVE和抗生素属性。
摘要:
Hydrazides of sulphenic acids are inhibitors of premature vulcanization of sulphur curable rubbers. The hydrazides are prepared from sulphenyl chlorides or bromides and the appropriate hydrazine in presence of an acid binding agent. The most effective hydrazides are those from secondary alkyl sulphenyl chlorides or bromides, or those in which the nitrogen atom attached to the sulphenic acid group also carries an acyl group, or in which the other nitrogen atom is attached to an alkylidene or cycloalkylidene group.
摘要:
An aromatic compound represented by formula (1):wherein R1 and R2 each independently represents a halogen atom, a C1-C4 alkyl group, or a C1-C4 haloalkyl group; m and n each independently represents an integer of 0 to 4; R3 and R4 each represents a hydrogen atom; Y represents formula: —OC(═X)ZR5 or —SC(═X)ZR5; R5 represents a C1-C3 alkyl group optionally having one or more halogen atoms; Z represents a sulfur atom, NR8, or a direct bond; R8 represents a C1-C3 alkyl group or a hydrogen atom; Q represents a pyrazolyl group optionally having a substituent; and W and X each independently represents an oxygen atom or a sulfur atom, has excellent control activity against pests.