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Hydrosilyl ethers, generated in situ by the dehydrogenative silylation of cyclopropylmethanols with diethylsilane, undergo asymmetric, intramolecular silylation of cyclopropyl C?H bonds in high yields and with high enantiomeric excesses in the presence of a rhodium catalyst derived from a rhodium precursor and the bisphosphine (S)-DTBM-SEGPHOS. The resulting enantioenriched oxasilolanes are suitable substrates for the Tamao?Fleming oxidation to form cyclopropanols with conservation of the ee value from the C?H silylation. Preliminary mechanistic data suggest that C?H cleavage is likely to be the turnover-limiting and enantioselectivity-determining step.

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The present invention relates to the NSAID derivatives of omega-3 fatty acids as gamma secretase modulators and their use in treating Alzheimer’s disease, hypertriglyceridemia, and cardiovascular disease by reducing triglycerides, and for use as anti-inflammatory agents.

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The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

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A monoprotected aminoethyl amine chiral ligand based on an ethylenediamine backbone was developed to achieve Pd-catalyzed enantioselective C(sp3)-H arylation of cyclopropanecarboxylic and 2-aminoisobutyric acids without using exogenous directing groups. This new chiral catalyst affords new disconnection for preparing diverse chiral carboxylic acids from simple starting materials that are complementary to the various ring forming approaches.

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The present invention relates to tetrazole containing compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease syndrome, condition, or symptoms, in particular related to chronic pain and inflammation, as a sole agent or in combination with other active ingredients.

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The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.

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The present disclosure describes carbamate analogs of mibefradil, as well as their compositions and methods of use. The compounds block the activity of one or more isoforms of voltage-gated calcium channels and are useful in the treatment of diseases including, e.g., cancer.

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The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

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This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.

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Disclosed is a dehydrohalogenation method in which a halogen atom on a carbon atom in an organic compound is removed by substituting the halogen atom by a hydrogen atom. Also disclosed is a process for production of a dehalogenated compound. The dehydrohalogenation method comprises the step of treating an organic compound having a halogen atom on a carbon atom therein with a compound represented by the formula (2-1): M2BHpR1 q (2-1) or the formula (2-2): M3(BHpR1 q)2 (2-2) wherein M2 represents an alkali metal atom; M3 represents a alkali earth metal atom or a zinc atom; R1 represents a hydrogen atom, a cyano group, an acyloxy group having 2 to 13 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; p represents an integer of 1 to 4; and q represents an integer of 0 to 3, provided that the sum total of p and q is 4 in a solvent in the presence of a complex of a metal belonging to Group VIII represented by the formula (1): M1XmLn (1) wherein M1 represents a metal belonging to Group VIII; X represents a halogen atom; L represents a neutral ligand; m represents an integer of 1 to 2; and n represents an integer of 2 to 3, provided that the sum total of m and n is 4.

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