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The present invention relates to compounds of formula (I) that are metallo-beta-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with beta-lactam antibiotics for overcoming resistance.

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The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma

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A compound selected from those of formula (I): wherein:W represents optionally substituted naphthyl,n represents an integer from 2 to 3 inclusive,Z represents a single bond,A represents nitrogen,Q represents nitrogen,M, together with the carbon of pyridyl to which it is bonded, represents thieno, furo, pyrrolo or oxopyrrolo,Its optical isomers and pharmaceutically-acceptable acid or base additional salts thereof, andMedicinal products containing the same which are useful in the treatment of CNS disorders.It being understood that “aryl” is phenyl, naphthyl, dihydronaphthyl, or tetrahydronaphthyl. ”

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The present work highlights unprecedented Ni-catalyzed reductive coupling of unactivated alkyl iodides with aryl acid chlorides to efficiently generate alkyl aryl ketones under mild conditions.

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Selective catalytic synthesis of Z-olefins has been challenging. Here we describe a method to produce 1,2-disubstituted olefins in high Z selectivity via reductive cross-coupling of alkyl halides with terminal arylalkynes. The method employs inexpensive and nontoxic catalyst (iron(II) bromide) and reductant (zinc). The substrate scope encompasses primary, secondary, and tertiary alkyl halides, and the reaction tolerates a large number of functional groups. The utility of the method is demonstrated in the synthesis of several pharmaceutically relevant molecules. Mechanistic study suggests that the reaction proceeds through an iron-catalyzed anti-selective carbozincation pathway.

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A cobalt-catalyzed cross-coupling of diarylmanganese reagents with secondary alkyl iodides using the THF-soluble salt CoCl2·2LiCl, which leads to the cross-coupling products in up to 92% yield, is reported. High diastereoselectivities can be reached in these cross-couplings (dr up to 99:1). Remarkably, rearrangement of secondary alkyl iodides to unbranched products was not observed in these C-C forming reactions.

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Compounds of general formula (I): or a stereoisomer, tautomer, polymorph, hydrate, solvate, or a pharmaceutically acceptable salt thereof, wherein R is as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as proliferative diseases, e.g. cancers, viral and fungal infections, neurodegenerative or inflammatory diseases or conditions. The invention also relates to the preparation of these compounds as well as to pharmaceutical compositions comprising them.

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New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.

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Extracurricular laboratory:new discovery of tert-Butyl 4-iodopiperidine-1-carboxylate

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The present invention provides a process for preparing benzimidazole thiophene compounds of formula I. Intermediates used in the process are also claimed.

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HETEROARYL COMPOUNDS FOR TREATING HUNTINGTON’S DISEASE

The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington’s disease. In particular, the present description relates to substituted benzothiazole compounds of Formula (I) or (II), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington’s disease.

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