1332487-79-2Relevant articles and documents
Potent cholesteryl ester transfer protein inhibitors of reduced lipophilicity: 1,1′-spiro-substituted hexahydrofuroquinoline derivatives
Trieselmann, Thomas,Wagner, Holger,Fuchs, Klaus,Hamprecht, Dieter,Berta, Daniela,Cremonesi, Paolo,Streicher, Rüdiger,Luippold, Gerd,Volz, Astrid,Markert, Michael,Nar, Herbert
, p. 8766 - 8776 (2015/03/14)
A series of 1,1′-spiro-substituted hexahydrofuroquinoline derivatives exhibiting potent cholesteryl ester transfer protein (CETP) inhibition at reduced lipophilicity was identified. A focused structure-activity relationship (SAR) exploration led to the potent and comparatively polar CETP inhibitor 26 showing robust high density lipoprotein-cholesterol (HDL-C) elevation and low density lipoprotein-cholesterol (LDL-C) reduction in transgenic hCETP/hApoB-100 mice. Compound 26 was also shown to positively differentiate from highly lipophilic CETP inhibitors in its complete elimination from fat tissue in hCETP transgenic mice as evident within 21 days after cessation of treatment. In addition, compound 26 showed no significant effects on aldosterone secretion from H295R cells, as well as no significant effects on blood pressure and electrocardiogram parameters in telemetrized cynomolgus monkeys.
Crystalline forms of a hexahydrofuro[3,4-c]quinoline derivative
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, (2013/08/28)
The present invention relates to crystalline forms of (3R,9S)-4-isopropyl-7,7-dimethyl-3-(4-(trifluoromethyl)phenyl)-2′,3′,5′,6,6′,7,8,9-octahydro-3H-spiro[furo[3,4-c]quinoline-1,4′-pyran]-9-ol and its hydrochloride or hydrobromide salts, to a process for the manufacture thereof, and to the use thereof in pharmaceutical compositions.
CRYSTALLINE FORMS OF OCTAHYDRO-3H-SPIRO [FURO [3, 4-C] QUINOLINE -1, 4 '-PYRAN] -9-OL
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, (2013/03/26)
The present invention relates to crystalline forms of the compound of formula (I) as shown in the description and its hydrochloride or hydrobromide salts, to a process for the manufacture thereof, and to the use thereof in pharmaceutical compositions.
Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation
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Paragraph 1083; 1084; 1085; 1086, (2013/03/26)
The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION
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Page/Page column 166; 173-174, (2012/09/10)
The present invention relates to compounds defined by formula (I), wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol
TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION
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Page/Page column 87, (2012/03/10)
The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION
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Page/Page column 166; 173-174, (2011/09/19)
The present invention relates to compounds defined by formula (I) wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol
