- BICYCLIC IMIDAZOLE DERIVATIES USEFUL FOR THE TREATMENT OF RENAL DISEASE, CARDIOVASCULAR DISEASES AND FIBROTIC DISORDERS
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The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 39-40; 42
(2018/02/03)
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- NOVEL PROCESS FOR PREPARATION OF SPIRO[2.5]OCTANE-5,7-DIONE AND SPIRO[3.5]NONANE-6,8-DIONE
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This invention relates to methods for the synthesis of spiro[2.5]octane-5, 7-dione and spiro[3.5]nonane-6, 8-dione which are useful as intermediates in the manufacture of pharmaceutically active ingredients.
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- Short and tandem syntheses of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione via diethyl acetonedicarboxylate
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A general synthetic route to spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione that involves cyclization of the related acrylates and diethyl acetonedicarboxylate, followed by decarboxylation, has been developed. Compared with previous synthetic methods, the developed protocol avoids the use of column chromatography in each of the synthetic steps. Therefore, it can be readily scaled-up. The use of diethyl acetonedicarboxylate under mild conditions to build the skeleton of 1,3-cyclohexanedione has proved to be very efficient.
- Jin, Xiangle,Xu, Wei,Yang, Jinsong,Lu, Jun,Fu, Yan,Xie, Le,Zhu, Qian,Dong, Weitong
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p. 6287 - 6289
(2015/10/20)
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- Process for preparing spiro[2.5]octane-5,7-dione
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Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.
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- PROCESS FOR PREPARING SPIRO[2.5]OCTANE-5,7-DIONE
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Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.
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- METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
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The invention relates to heterocyclic derivatives of formula (I) as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders wherein Y, W, R1, R2 and R3 are as defined in claim 1.
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Page/Page column 49
(2012/05/05)
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- METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
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The invention relates to heterocyclic derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorder
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Page/Page column 60
(2012/07/13)
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- (5S) -3-[(S)-FLUORO (4-TRIFLUOROMETHYLPHENYL) METHYL]-5,6,7,8-TETRAHYDROQUINOLINE-5-OL DERIVATIVES AND USE THEREOF AS CETP INHIBITORS
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The invention relates to novel tetrahydroquinoline derivatives of formula (I), wherein R1 represents cyclohexyl or cyclopentyl, R2 and R3 each represent methyl or jointly form a cyclobutane, and R4 represents cyclopentyl or isopropyl, the salts and solvates thereof, and the solvates of said salts. Also disclosed are a method for the production thereof, the use thereof on its own or in combinations for the treatment and/or prevention of diseases, and the use thereof for producing medicaments, particularly as a cholesterol ester transfer protein (CETP) inhibitor in order to treat and/or prevent cardiovascular diseases, especially hypolipoproteinemia, dyslipidemia, hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, and arteriosclerosis.
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Page/Page column 11; 12; 26; 27; 42; 43
(2008/06/13)
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