- ISOINDOLINONE COMPOUNDS
-
Disclosed herein is a compound or pharmaceutically acceptable salts or stereoisomers thereof of of formula I wherein X1 is linear or branched C1-6 alkyl, C3-6 cycloalkyl, -C1-6 alkyl C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, C1-6 alkyl C6-10 aryl, C1-6 alkyl 5-10 membered heteroaryl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, -O-CHF2, -O-(CH2)2-OMe, OCF3, C1-6 alkylamino, -CN, -N(H)C(O)-C1- 6alkyl, -OC(O)-C1-6alkyl, -OC(O)-C1-4alkylamino, -C(O)O-C1-6alkyl, -COOH, - CHO, -C1-6alkylC(O)OH, -C1-6alkylC(O)O-C1-6alkyl, NH2, C1-6 alkoxy or C1-6 alkylhydroxy; X2 is hydrogen, C6-10 aryl, 5-10 membered heteroaryl, -O-(5-10 membered heteroaryl), 4-8 membered heterocycloalkyl, C1-4 alkyl 4-8 membered heterocycloalkyl, -O-(4-8 membered heterocycloalkyl), -O-C1-4 alkyl-(4-8 membered heterocycloalkyl), -OC(O)-C1-4alkyl-4-8 membered heterocycloalkyl or C6 aryloxy, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, NH2, NMe2 or 5-6 membered heterocycloalkyl; n is 0, 1 or 2.
- -
-
Page/Page column 184-185
(2021/04/17)
-
- CARBOXYLATION CATALYSTS
-
The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives.
- -
-
Paragraph 0093
(2013/04/13)
-
- Synthesis and antibacterial activities of pleuromutilin derivatives with thiazole-5-carboxamide and thioether moiety
-
Seven novel pleuromutilin derivatives with thiazole-5-carboxamide and thioether moiety in the C14 side chain were designed and synthesised. The antibacterial activities of the target compounds were tested via agar-well diffusion method in vitro. The results showed that three target compounds still had antibacterial activity against Staphylococcus aureus ATCC26112 and Staphylococcus aureus SC at a low concentration of 0.05 μg mL-1.
- Wang, Liang,Dai, Fu-Ying,Zhu, Jie,Dong, Kui-Kui,Wang, Yu-Liang,Chen, Tian
-
experimental part
p. 313 - 316
(2011/10/05)
-
- Carboxylation of C-H bonds using N -heterocyclic carbene gold(I) complexes
-
A highly efficient [(NHC)AuI]-based (NHC = N-heterocyclic carbene) catalytic system for the carboxylation of aromatic and heteroaromatic C-H bonds was developed. The significant base strength of the Au-OH species is at the origin of the activation process and permits the facile functionalization of C-H bonds without the use of other organometallic reagents.
- Boogaerts, Ine I. F.,Nolan, Steven P.
-
supporting information; experimental part
p. 8858 - 8859
(2010/08/21)
-
- Pharmaceutically active compounds
-
Compounds of formula (I) wherein: R1 and R19 independently represent hydrogen, alkyl C1-6, alkoxy C1-6, alkylthio C1-6, halogen, hydroxyl or amino; R2 represents H or alkyl; R3 represents phenyl, a 6-membered heterocyclic aromatic ring containing one or two nitrogen atoms, or a 5-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from O,N, and S, which phenyl or heterocyclic aromatic ring may be optionally substituted by alkyl C1-6, alkoxy C1-6, haologen, hydroxyl, alkylthio C1-6, cyano, trifluoromethyl, nitro, hydroxymethyl, amino, a group --(CH2)c NHCO2 R10, a group --(CH2)c NR5 R6, or a group --CO2 R11 ; or R3 represents hydrogen or alkyl C1-8, which alkyl group may be optionally substituted by amino or a group --NHCO2 R10 ; R4 represents hydrogen or alkyl C1-6; or R3 and R4 taken together represent a group (CH2)a Z(CH2)b ; c represents an integer 0 to 2; and pharmaceutically acceptable salts thereof, have been found to be useful as a pharmaceuticals. The compounds may especially be used in the treatment of inflammatory disorders.
- -
-
-
- 5-LIPOXYGENASE INHIBITORY THIAZOLES
-
The invention concerns a thiazole of the formula I, wherein Ar1 is optionally substituted aryl of up to 10 carbon atoms; A is a direct link to X, or is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene; X is oxy, thio, sulphinyl, sulphonyl or imino; Ar2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms; R1 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl; R2 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, substituted (1-4C)alkyl or (2-6C)alkanoyl; Q is optionally substituted thiazolyl; or a pharmaceutically-acceptable salt thereof. The invention also concerns processes for the manufacture of a thiazole of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said thiazole
- -
-
-
- Anti-tumour agents
-
A quinazoline of the formula: STR1 wherein R1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy; wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl; wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R3 is such that R3 --NH2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.
- -
-
-
- Thiazole derivatives
-
The invention provides thiazole derivatives of general formula I; STR1 or an acid-addition salt or metal salt complex thereof, in which R represents an optionally substituted aryl group; R1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl or alkynyl group; R2 represents a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, hydroxyl, cyano, nitro, amino, alkylamino, dialkylamino or morpholine group; X represents an oxygen or sulphur atom, a carbonyl group or a group --CR4 R5 -- where R4 and R5 independently represent a hydrogen atom or an alkoxy group; Y represents an oxygen or sulphur atom; n represents an integer from 0 to 6; m is 0 or 1; and Z represents a phenyl group; processes for their preparation; compositions containing such compounds and their use as fungicides.
- -
-
-