摘要:
A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.
摘要翻译:由通式[I]表示的3,4-二卤代异噻唑衍生物(其中R1是卤素原子; A是氧原子或硫原子; R是C1-C6烷基,C2-C5烯基, C 2 -C 5炔基,C 3 -C 6环烷基,苯基或含有氧原子,硫原子和氮原子中的至少一个的5元至10元杂环基)或其盐。
摘要:
The invention relates to compounds of the following formula that may be used to inhibits kinases, as well as compositions of matter and kits comprising these compounds. The present invention also relates to methods for inhibiting kinases, as well as treatment methods using compounds according to the present invention.
摘要:
Organic compounds having the structure I are provided where the variables have the values described herein. Pharmaceutical formulations and medicaments include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compound or a pharmaceutically acceptable salt of the organic compound with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation or medicament according to the invention to a patient in need thereof.
摘要:
The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: 1 in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.
摘要:
The present invention relates to novel heterocyclic compounds having the general formula (1) ##STR1## geometric and optical isomers and racemates thereof where such isomers exist, as well as pharmaceutically acceptable acid addition salts thereof and solvates thereof;having therapeutic activity, processes and intermediates for their preparation, pharmaceutical formulations containing said compounds and the medicinal use of said compounds.
摘要:
Rolipram-based PDE IV inhibitors containing phenyl- or benzyl-substituted moieties of the formula: ##STR1## wherein X.sub.1 and X.sub.2 may be the same or different and each is O or S;R.sub.1 is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C.sub.2-12 alkyl groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety;R.sub.2 =R.sub.1 or --CH.sub.3 ;R.sub.3 is hydrogen, halogen, or a saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl group, a cycloalkyl or cycloalkyl-alkyl groups containing from 3 to 7 carbon atoms in the cycloalkyl moiety;Z is a linkage selected from --CH.sub.2 CONH-- or --CH.sub.2 NHCO--, andR.sub.4 is a phenyl or benzyl which may be unsubstituted or substituted with one or more halogen atoms, alkyl groups, hydroxyl groups, cyano groups, carboxyl groups, alkoxy groups, alkoxycarbonyl, amido, carboxamido, substituted or unsubstituted amino groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety, aryl or aralkyl groups preferably containing from about 6 to about 10 carbon atoms, or heterocyclic groups containing nitrogen, oxygen or sulfur in the ring; the alkyl, alkoxy, cycloalkyl, cycloalkylalkyl, aryl, and aryl-alkyl groups being saturated or unsaturated, unsubstituted or substituted by halogen atoms, hydroxyl groups, cyano groups, carboxyl groups, alkoxy groups, alkoxycarbonyl, carboxamido or substituted or unsubstituted amino groups, or one or more lower alkyl groups having from 1 to 3 carbon atoms;provided that R.sub.4 cannot be substituted with more than one methoxy group. compared to theophylline or rolipram as well as with improved selectivity with regard to PDE III inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.
摘要:
Compounds of formula (I): (A)m·(B)n (I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.
摘要:
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要:
Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds have the formula: ##STR1## wherein: R.sub.1 and R.sub.2 may be the same or different and each is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety;R.sub.3 is hydrogen, halogen, or a saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl group, a cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 7 carbon atoms in the cycloalkyl moiety;R.sub.4 is a phenyl or benzyl or a 6-membered heteroaryl which may be unsubstituted or substituted with one or more halogen atoms, alkyl groups, nitro groups, hydroxyl groups, cyano groups, carboxyl groups, alkoxy group, alkoxycarbonyl, amido, carboxamido, substituted or unsubstituted amino groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety, aryl or aralkyl groups preferably containing from about 6 to about 10 carbon atoms, or heterocyclic groups containing nitrogen, oxygen or sulfur in the ring; said alkyl, cycloalkyl, cycloalkyl-alkyl, aryl, and arylalkyl groups being unsubstituted or substituted by halogen atoms, hydroxyl groups, cyano groups, carboxyl groups, alkoxy groups, alkoxycarbonyl, carboxamido or substituted or unsubstituted amino groups, or one or more lower alkyl groups having from 1 to 3 carbon atoms;Z is selected from the group consisting of --CH.sub.2 CO--, --NHCH.sub.2 --, --CH.sub.2 NH--, --CH.sub.2 CONH--, --CH.sub.2 NHCO--, --CH.sub.2 COCH.sub.2 --, --COCH.sub.2 --, --C(.dbd.NOC(.dbd.O)NHQ)--, and --C(.dbd.NQ)NH--;X.sub.1 and X.sub.2 may be the same or different and each is O or S;wherein Q is R.sub.4 or hydrogen except that when Z.dbd.C(.dbd.NOCONHQ)--, R.sub.4 is not benzyl and R.sub.1 and R.sub.2 are both not hydrogen.
摘要:
A method of inhibiting the growth or replication of viruses of the HIV group is disclosed. Also disclosed are compounds useful in the method and pharmaceutical formulations incorporating such compounds. The method involves the use of compounds having the general formula: ##STR1## wherein the substituent groups are as defined in the specification.