摘要:
A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough.
摘要:
Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form -CH2-, -CH2CH2-, -O-, -S-, -S(O)-, -S(O)2-, -NR8-, -OCH¿2?-, -SCH2-, -N(R?8)CH¿2-, substituted -CH2- and substituted -CH2CH2-, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR4;X is CR5R6, O, S, NR7 or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C¿1?-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR?9R10, N=CR11R12, OR7, COR13, CO¿2R14 or C1-C6 alkyl substituted by at least one group selected from halogen, C1-C3 alkoxy, CN, NO2, S(O)rR?15, COR13, CO¿2R14 and optionally substituted phenyl; Z is O or S; and R?2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15¿, G, n and r are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling arthropods which involves contacting the arthropods or their environment with an effective amount of a compound of Formula (I).
摘要:
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) lower alkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl -L2-, and (i) heterocyclic -L2-; R2 is selected from (a) formula (1), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) formula (2), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, formula (3), and -P(W)R?R3RR3'; R¿4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylalkyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) -L4-N(R5)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R5)-L5-, (f) -L4-N(R5)-C(W)-L7-L5-, (g) -L4-N(R5)-S(O)p-L7-L5-, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene, (k) a covalent bond, (1) formula (4), and (m) formula (5) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要:
Compounds of formula I wherein R¹ represents a hydrogen or a halogen atom, or a group selected from hydroxy, C₁₋₆ alkyl, C₁₋₆ alkoxy, phenylC₁₋₃alkoxy (in which the phenyl group is unsubstituted or substituted by a halogen atom or a C₁₋₃ alkyl, C₁₋₃ alkoxy or hydroxy group), nitro, trifluoromethyl, cyano, -CO₂R³ (wherein R³ represents a hydrogen atom or a C₁₋₄ alkyl group) and -CONR⁴R⁵ (wherein R⁴ and R⁵ each independently represents a hydrogen atom or a C₁₋₄ alkyl group, or together with the nitrogen atom to which they are attached form a saturated 5- to 7-membered ring, which ring optionally contains one or more atoms selected from an oxygen or a sulphur atom, or a group -NH- or -N(CH₃)-); and R² represents a hydrogen or halogen atom, or a hydroxy, C₁₋₆ alkyl or C₁₋₆ alkoxy group; and salts thereof are inhibitors of the enzyme 5-lipoxygenase. Processes for preparing the compounds of formula (I) and compositions containing them are also described.
摘要:
Neue substituierte N-Amino-1,2,4-triazinone der Formel I worin R₁ Wasserstoff, C₁-C₁₂-Alkyl, C₃-C₆-Cycloalkyl, C₁-C₄-Alkoxy-C₁-C₆-alkyl, C₁-C₂-Halogenalkyl, Phenyl, Benzyl, Phenäthyl, Phenpropyl, Phenbutyl, Phenpentyl oder einen ein- oder zweifach durch Halogen, C₁-C₅-Alkyl, C₁-C₂-Halogenalkyl, Methoxy und/oder Aethoxy substituierten Phenyl-, Benzyl-, Phenäthyl-, Phenpropyl-, Phenbutyl- oder Phenpentylrest, R₂ Wasserstoff, C₁-C₆-Alkyl, C₃-C₆-Cycloalkyl, unsubstituiertes oder durch C₁-C₁₂-Alkyl, Halogen oder C₁-C₁₂-Halogenalkyl substituiertes Phenyl oder R₁ und R₂ zusammen einen gesättigten oder ungesättigten 3- bis 7-gliedrigen Carbocyclus bilden, R₃ Wasserstoff oder C₁-C₆-Alkyl bedeuten und Z für -N=CH- oder -NH-CH₂- steht, sowie ihre Salze mit organischen oder anorganischen Säuren, Verfahren und Zwischenprodukte zu ihrer Herstellung, ihre Verwendung in der Schädlingsbekämpfung und Schädlingsbekämpfungsmittel, welche eine Verbindung der Formel I als Wirkstoff enthalten, werden offenbart. Bevorzugtes Anwendungsgebiet ist die Bekämpfung von Schädlingen an Tieren und Pflanzen.
wherein A is a direct link, or is alkylene of 1 to 4 carbon atoms or alkenylene of 2 to 4 carbon atoms; wherein either X is -CR 1 R 2 - and Y is -0-, -S- or -NR 3 -, wherein R 1 , R 2 and R 3 , which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is-O-,-S- or-NH- and Y is-CR 1 R 2 - wherein R 1 and R 2 have the meanings stated above; and wherein Het is a 5- or 6- membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen or sulphur atoms, which ring may be unsubstituted or may bear one or two substituents as set out in claim 1, provided that when X is -CR 1 R 2 - and A is a direct link, Het is not unsubstituted 2-furyl; and salts thereof where appropriate; processes for their manufacture and pharmaceutical compositions containing them. The compounds possess cardiotonic and/or antihypertensive activity.
摘要:
Novel heterocyclic compounds of the formula:- wherein either X is -CR 1 R 2 - and Y is oxygen, sulphur or -NR 3- , wherein R 1 , R 2 and R 3 , which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is oxygen, sulphur or -NH- and Y is -CH 2 -; wherein R 4 and R 5 , which may be the same or different, each is hydrogen, cyano, nitro, amino or hydroxy, or alkylthio of up to 4 carbon atoms, or has various other meanings defined in i claim 1, provided that R 4 and R 5 are not both hydrogen; or wherein R 4 and R 5 are joined together such that with the benzene ring A they form a benzheterocyclic ring as defined in claim 1; and therein the benzene ring A may optionally bear one or more further substituents; or a salt thereof where appropriate. These compounds possess cardiotonic properties, and some of them possess peripheral vasodilator properties, and they are useful for the treatment of acute or chronic heart failure. Representative of the compounds is N,N-dimethyl-p-(5,6-dihydro-5-oxo-4H-1,3,4-thiadiazin-2-yl)benzamide. Also disclosed are processes for the manufacture of the compounds and pharmaceutical compositions containing them.