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Patent

1-aryltriazolin(ethi)ones

TL;DR: In this article, a new 1-aryltriazolin(ethi)ones of the general formula (I) are described, where R 1 represents nitro or represents a radical, R 2 represents hydrogen, amino or cyano, or represents one of the radicals.
Abstract: The invention relates to new 1-aryltriazolin(ethi)ones of the general formula (I) ##STR1## in which R 1 represents nitro or represents a radical --NR 8 R 9 , R 2 represents hydrogen, amino or cyano, or represents one of the radicals --R 10 , --O--R 10 , --S--R 10 , --NR 10 R 11 , --N(R 11 )--CO--R 10 or --N═CR 10 R 11 , R 3 , R 6 and R 7 independently of one another each represent hydrogen, halogen or nitro, R 4 represents hydrogen, halogen, cyano or nitro, or represents one of the radicals --R 12 , --O--R 12 , --S--R 12 , --S(O)--R 12 , --SO 2 --R 12 , --SO--OR 12 , --SO--NR 11 R 12 , --CO--OR 12 , --CO--NR 11 R 12 , --O--SO 2 --R 12 , --N(R 11 )--SO 2 --R 12 , --NR 11 R 12 , --NH--P(O)(R 11 )(OR 12 ) or --NH--P(O)(OR 11 )(OR 12 ), R 5 represents nitro, cyano, halogen or halogenoalkyl, and X represents oxygen or sulphur, where R 8 and R 9 independently of one another each represent hydrogen or represent in each case optionally substituted alkyl, alkenyl, alkinyl, alkoxy, cycloalkyl, aryl or heterocyclyl, or represent, together with the nitrogen atom to which they are attached, an optionally substituted heterocycle, R 10 represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aryl, arylalkyl or heterocyclyl, R 11 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, arylalkyl or aryl, and R 12 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aryl or heterocyclyl, to a number of processes for their preparation, to a number of new intermediates, and to their use as herbicides.
Citations
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Patent
25 May 2007
TL;DR: In this paper, the authors proposed methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof, by administering to the subject a substituted triazole compound or a composition comprising such a compound.
Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

149 citations

Patent
27 Sep 2000
TL;DR: In this article, the present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts and exhibits activity as serotonin, norepinephrine, and dopanine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.
Abstract: The present invention relates to compounds of formula (I) and to their pharmaceutically acceptable salts. Compounds of formula (I) exhibit activity as serotonin, norepinephrine, and dopanine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.

78 citations

Patent
19 Mar 2003
TL;DR: Substituted phenylacetic acids, phenylethanols and related compounds are provided that are useful in treating or controlling a number of diseases associated with glucose metabolism, lipid metabolism and insulin secretion as mentioned in this paper.
Abstract: Substituted phenylacetic acids, phenylethanols and related compounds are provided that are useful in treating or controlling a number of diseases associated with glucose metabolism, lipid metabolism and insulin secretion.

36 citations

Patent
14 Nov 2012
TL;DR: A pharmaceutical combination comprising a BRAF inhibitor, and an Hsp90 inhibitor according to the following formulae (I): or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables are defined therein this article.
Abstract: A pharmaceutical combination comprising a BRAF inhibitor, and an Hsp90 inhibitor according to the following formulae (I): or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables are defined therein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.

26 citations

Patent
01 Nov 2012
TL;DR: A pharmaceutical combination comprising a topoisomerase I inhibitor, and an Hsp90 inhibitor according to the following formulae (I) (la) a tautomer, or a pharmaceutically acceptable salt thereof, is defined in this article.
Abstract: A pharmaceutical combination comprising a topoisomerase I inhibitor, and an Hsp90 inhibitor according to the following formulae (I) (la) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.

24 citations

References
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Journal ArticleDOI
TL;DR: In this article, the Nitrierung of 1.4.2.4-triazolone-(5) is found to be auser in 3-Stellung des 3-Nitro-verbindungen.
Abstract: Die Nitrierung von 1.2.4-Triazolonen-(5) ergibt die 3-Nitroverbindungen, wahrend sich die entsprechenden 1.2.4-Triazolone-(3) wie die 5-Alkoxy-1.2.4-triazole nicht nitrieren lassen. Sowohl bei N- wie bei C-phenyl- oder -benzylsubstituierten 1.2.4-Triazolonen-(5) findet die Nitrierung auser in 3-Stellung des 1.2.4-Triazolonringes auch in p-Stellung des Phenylkerns, im 1-Phenyl- bzw. 1-Benzyl-1.2.4-triazolon-(3) nur in p-Stellung statt. – Die Bromierung fuhrt nur bei N-monosubstituierten 1.2.4-Triazolonen-(5) zu den entsprechenden, 3-Brom-1.2.4-triazolonen-(5). Die gleichen, und auch auf diesem Wege nicht zugangliche, 3-Halogen-1.2.4-triazolone-(5) konnen durch saurekatalysierten nucleophilen Austausch aus den entsprechenden 3-Nitro-1.2.4-triazolonen-(5) mit Hilfe der Halogenwasserstoffsauren gewonnen werden. – Auserdem wird die Reduktion der Nitrogruppe, die Methylierung, der Austausch von Brom gegen Chlor und von Halogen gegen die Aminogruppe an einzelnen der dargestellten Verbindungen beschrieben.

28 citations

Patent
29 May 1992
TL;DR: Heterocyclic substituted 2-acylamino-5-thiazoles, their preparation and pharmaceutical compositions containing them, are discussed in this paper, where a 2-Acylaminothiazole of formula: ##STR1## is defined.
Abstract: Heterocyclic substituted 2-acylamino-5-thiazoles, their preparation and pharmaceutical compositions containing them. A 2-Acylaminothiazole of formula: ##STR1## in which R 1 is H, an alkyl or a substituted alkyl; R IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R IV and R V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).

27 citations

Journal ArticleDOI
TL;DR: In this paper, a mixture of a monopicryl and a dipricryl derivative of 1 in a ratio of 2:1, regardless of the initial concentrations of 1 and PkF, were identified as 5-nitro-2-picryl-2,4-dihydro-3H-1,2-4-triazol-3-one (2) by X-ray crystallography.

19 citations

Patent
13 Sep 1990
TL;DR: In this paper, a process for preparing optically active 3-phenylglycidic acid ester compound is described, which comprises permitting a culture broth, cells or treated cells of a microorganism having the ability of stereoselectively hydrolyzing a (2R, 3S)-3-PNE compound to act on a racemic 3-PNEster compound which may also have a substituent on the phenyl group.
Abstract: There is disclosed a process for preparing optically active 3-phenylglycidic acid ester compound, which comprises permitting a culture broth, cells or treated cells of a microorganism having an ability of stereoselectively hydrolyzing a (2R, 3S)-3-phenylglycidic acid ester compound to act on a racemic 3-phenylglycidic acid ester compound which may also have a substituent on the phenyl group, thereby hydrolyzing the (2R, 3S) optically active isomer and separating and collecting the (2S, 3R) antipode from the reaction mixture.

13 citations

Patent
18 Dec 1981
TL;DR: A compound of the formula: wherein R is a C 1-C 4 alkyl group, a C 3-C4 alkenyl group, X is a chlorine or bromine atom and Y is a hydrogen atom or a c 1 -C 4 alkoxy group, which is useful as a herbicide as discussed by the authors.
Abstract: A compound of the formula: wherein R is a C1-C4 alkyl group, a C3-C4 alkenyl group or a C3-C4 cycloalkyl group, X is a chlorine or bromine atom and Y is a hydrogen atom or a C1-C4 alkoxy group, which is useful as a herbicide

5 citations