摘要:
The invention relates to urethane-protected amino acid-N-carboxyanhydride and N-thiocarboxyanhydride compounds which are useful in peptide, polypeptide and protein synthesis. Disclosed herein is the preparation and use of these novel compounds.
摘要:
A novel optically active diamide derivative represented by the following general formula is provided, which is useful as a starting material for asymmetric synthesis of optically active compounds, ##STR1## wherein R.sup.1 is an acyclic or cyclic, divalent atomic group containing at least one carbon atom which will, upon substitution of one of the heterocyclic groups in the formula with a nucleophilic reagent, stand as an asymmetric center in the substitution product; R.sup.2 is a substituent which has such a configuration and a molecular size that the regioselectivity in the substitution reaction of the heterocyclic group with the nucleophilic reagent can be determined by a stereo-chemical interaction thereof with the substituent R.sup.1, the steric configuration of the two asymmetric carbon atoms to which the R.sup.2 substituents are attached being identical; X is a sulfur atom or an oxygen atom; and n is an integer which is 1 or 2. Such a diamide derivative can be prepared by subjecting the corresponding dicarboxylic acid or an anhydride thereof to a condensation reaction with the corresponding heterocyclic compound in the presence of a condensation agent. The optically-active diamide derivative can be used in the reaction with a nucleophilic reagent to obtain an optically-active compound. The resulting compound can be further modified by subjecting it to reaction with another nucleophilic reagent or to hydrolysis.
摘要:
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.
摘要:
The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group;R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group;R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group;R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group;R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group;R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group;m is 0 or 1; andn is 1 or 2,with the proviso that R.sup.2 means hydrogen when m is 0.The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g. the senile dementia, Alzheimer's disease or disturbances of the cognitive function.
摘要:
An indandione pigment having high tinting strength and good weatherability and light fastness of the formula ##STR1## WHEREIN A is a phenylene or naphthylene group optionally substituted by a halogen atom, a lower alkyl group, a lower alkoxy group or a nitro group; n is 2 or 1; and B represents a direct bond or an n valont aromatic radical.The pigment mentioned above can be prepared by reacting an indandione derivative of the formula ##STR2## (E is an alkoxy group with 1 to 3 carbon atoms, or an amino group; and G is an oxygen atom, or ##STR3## in which Q is a lower alkyl group, and Q.sub.2 is a lower alkyl group or a phenyl group) with an amino compound of the formula H.sub.2 N--B--NH.sub.2 ]n-1.
摘要:
Chemical compounds of the class of carbamate esters of 2oxyimino-3-keto-1,4-diheterocyclics, such as 2methylcarbamoyloxyimino-4-methyl-3-thiomorpholinone useful in controlling pests such as insects and nematodes.
摘要:
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
摘要:
Azolyloxy-carboxylic acid N-oxy-amide compound of the formula ##STR1## wherein R is a five-membered hetero-aromatic monocyclic radical which contains an oxygen atom or a sulphur atom and in addition 1 to 3 nitrogen atoms and which is optionally substituted by halogen, cyano, nitro, amino, alkylamino, arylamino, dialkylamino, alkylcarbonylamino, alkylcarbonyl, carboxyl, alkoxycarbonyl, carbamoyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl (which is optionally substituted by halogen, nitro or alkyl), aryl (which is optionally substituted by halogen, cyano, nitro, alkyl or alkoxy), by a radical which is optionally substituted by halogen and is selected from aralkyl, alkoxy, alkenoxy, alkynoxy, alkoxycarbonylalkoxy, aralkoxy, aryloxy, alkylthio, alkenylthio, alkoxycarbonylalkylthio, aralkylthio, arylthio, alkylsulphinyl, alkylsulphonyl, alkyl, alkenyl, alkynyl, alkoxyalkyl, aralkoxyalkyl, aryloxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, arylthioalkyl, arylsulphinylalkyl, arylsulphonylalkyl, carboxyalkyl, and alkoxycarbonylalkyl, or by optionally substituted aminocarbonylalkyl, cyanoalkyl or cycloalkyl, or which is optionally benzo-fused, the benzo radical optionally being substituted by halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino, dialkylamino, nitro, cyano, alkoxycarbonyl or optionally halogen-substituted alkylenedioxy,R.sup.1 is hydrogen or alkyl, andR.sup.2 and R.sup.3 are individually selected from optionally substituted radicals selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, aryl orR.sup.2 and R.sup.3 taken together represent alkyleneare effective herbicides.
摘要:
2-Substituted-5-trifluoromethyl-1,3,4-thiadiazoles of the formula ##STR1## in which R is substituted alkyl, phenyl monosubstituted in the o- or m- position, polysubstituted phenyl, substituted phenylalkyl, phenylalkenyl, substituted phenylalkenyl, an optionally substituted 5-membered or 6-membered heterocyclic radical with 1 to 4 hetero-atoms selected from N and S atoms, optionally substituted benzimidazolyl or benzthiazolyl, optionally substituted naphthyl, quinolyl, cyano or one of the groups ##STR2## wherein R.sup.1 and R.sup.2 conjointly are a trimethylene, tetramethylene or pentamethylene group, X is oxygen or sulfur, R' and R" each independently is alkyl or, together with the nitrogen atom and optionally further hetero-atoms selected from O and N atoms, form an optionally substituted 6-membered or 7-membered ring, and N is 0, 1 or 2, Which possess fungicidal, bactericidal, arthropodicidal and insecticidal properties.
摘要翻译:2-取代的5-三氟甲基-1,3,4-噻二唑,其中R是取代的烷基,在邻位或间位单取代的苯基,多取代的苯基,取代的苯基烷基,苯基烯基, 取代的苯基烯基,任选取代的具有1至4个选自N和S原子的杂原子的5元或6元杂环基,任选取代的苯并咪唑基或苯并噻唑基,任选取代的萘基,喹啉基,氰基或基团之一。 其中R1和R2共同是三亚甲基,四亚甲基或五亚甲基,X是氧或硫,R'和R“各自独立地是烷基,或者与氮原子和任选的另外的选自O和N原子的杂原子一起, 形成任选取代的6元或7元环,以及N IS 0,1或2,其具有杀真菌剂,杀真菌剂,抗坏血酸和杀虫剂性质。
摘要:
CHEMICAL COMPOUNDS OF THE CLASS OF CARBAMATE ESTERS OF 2-OXYIMINO-3-KETO-1,4-DIHETEROCYCLICS, SUCH AS 2METHYLCARBAMOYLOXYIMINO-4METHYL -3 - THIOMORPHOLINONE USEFUL IN CONTROLLING PESTS SUCH AS INSECTS AND NEMATODES.