1003-85-6Relevant articles and documents
NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
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Paragraph 0474, (2013/10/07)
The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACID DERIVATIVES AND THEIR USE AS GPR40 RECEPTOR AGONISTS
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Page/Page column 85, (2013/10/21)
The present invention relates to compounds of general formula I, (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACID DERIVATIVES AND THEIR USE AS GPR40 RECEPTOR AGONISTS
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Page/Page column 137, (2013/10/21)
The present invention relates to compounds of general formula (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7- tetrahydropyridinoazole templates
Sund, Christian,Belda, Oscar,Borkakoti, Neera,Lindberg, Jimmy,Derbyshire, Dean,Vrang, Lotta,Hamelink, Elizabeth,Hgren, Cathrine,Woestenenk, Esmeralda,Wikstroem, Kristina,Eneroth, Anders,Lindstroem, Erik,Kalayanov, Genadiy
, p. 6721 - 6727,7 (2012/12/12)
A set of low molecular weight compounds containing a hydroxyethylamine (HEA) core structure with different prime side alkyl substituted 4,5,6,7-tetrahydrobenzazoles and one 4,5,6,7-tetrahydropyridinoazole was synthesized. Striking differences were observed on potencies in the BACE-1 enzymatic and cellular assays depending on the nature of the heteroatoms in the bicyclic ring, from the low active compound 4 to inhibitor 6, displaying BACE-1 IC50 values of 44 nM (enzyme assay) and 65 nM (cell-based assay).
Investigations on cytotoxicity and anti-inflammatory potency of licofelone derivatives
Liu, Wukun,Zhou, Jinpei,Bensdorf, Kerstin,Zhang, Huibin,Liu, Haoran,Wang, Yubin,Qian, Hai,Zhang, Yanchun,Wellner, Anja,Rubner, Gerhard,Huang, Wenlong,Guo, Cancheng,Gust, Ronald
scheme or table, p. 907 - 913 (2011/04/19)
A series of C5-substituted licofelone ([2,2-dimethyl-6-(4-chlorophenyl)-7- phenyl-2,3-dihydro-1H-pyrrolizin-5-yl]acetic acid) derivatives were developed by a parallel synthesis approach and investigated for cytotoxicity against MCF-7 and MDA-MB-231 cells as well as for anti-inflammatory potency in vitro and in vivo. Dependent on the C5-substituent, the compounds showed high selectivity for MCF-7 cells. Especially 2-oxoethyl benzoate derivatives were inactive at the MDA-MB-231 cell line and as active as 5-FU at MCF-7 cells. C5-acetyl (8a), -2-oxoethyl formiate (8e), -2-oxoethyl acetate (8f) and -2-oxoethyl propionate (8g) derivatives showed growth inhibition at both cell lines, comparable with cisplatin. Modifications significantly reduced the inhibitory potency at COX-1 and COX-2 in vitro and in the xylene-induced ear swelling assay in mice. Only compound 8a was equipotent to licofelone, ibuprofen and celecoxibe in vivo.
Method for Chlorinating Alcohols
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Page/Page column 4-5, (2008/12/07)
A process for preparing organic chlorides in which the chlorine atom is bonded to a CH2 group by reacting the corresponding alcohols with thionyl chloride in the presence of a triaylphosphine oxide at a temperature of from 20 to 200° C. and a pressure of from 0.01 to 10 MPa abs, which comprises using the triarylphosphine oxide in a molar ratio to the amount of OH groups to be chlorinated of from 0.0001 to 0.5.
Preparation of cyclic sulfites by transesterification of diols and diisopropyl sulfite
King, Steven A.,Pipik, Brenda,Conlon, David A.,Bhupathy
, p. 701 - 707 (2007/10/03)
Cyclic sulfites of 1,2-, 1,3- and 1,4-diols can be prepared in high yield by acid or base catalyzed transesterification with diisopropyl sulfite.
Process for the production of cyclopropanenitrile derivatives
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, (2008/06/13)
A process for the production of cyclopropanenitrile derivatives. A diol of the formula: STR1 wherein R1 and R2 are the same or different and each is a hydrogen atom, a C1 -C6 alkyl group, branched or unbranched,
Acceleration of the 4-exo radical cyclization to a synthetically useful rate. Cyclization of the 2,2-dimethyl-5-cyano-4-pentenyl radical
Park,Varick,Newcomb
, p. 2975 - 2978 (2007/10/02)
The title radical, formed in the reaction of the corresponding bromide with Bu3SnH, cyclizes in a 4-exo fashion to give the (3,3-dimethylcyclobutyl)cyanomethyl radical. At 50°C, the rate constant for cyclization is 1.9 x 104s-1.
Process for producing intermediate furanones from diol derivative and thionyl chloride
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, (2008/06/13)
A novel process for the manufacture of the furanone of the formula STR1 is described. In this process, a diol is firstly reacted with thionyl chloride, then the sulphite formed, optionally after oxidation to the corresponding sulphate, is treated with sodium cyanide and the resulting hydroxynitrile is hydrolyzed. The furanone of formula I can be used as a starting material for the manufacture of R-(-)-pantolactone.