- ION PAIR CATALYSIS OF TUNGSTATE AND MOLYBDATE
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D The present invention relates to ion pair catalysts (I) comprising the cationic bisguanidinium ligand (A) and diperoxomolybdate anion (B). The present invention also relates to ion pair catalysts (III) comprising the cationic bisguanidinium ligand (C) and peroxotungstate anion (D). It further relates to the use of the said catalysts in the manufacture of enantiomerically enriched sulfoxides.
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Page/Page column 35
(2017/10/30)
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- Aromatic sulfone hydroxamates and their use as protease inhibitors
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This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
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- Discovery of Small-Molecule Inhibitors of the ATPase Activity of Human Papillomavirus E1 Helicase
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The Boehringer Ingelheim compound collection was screened for inhibitors of the ATPase activity of human papillomavirus E1 helicase to develop antiviral agents that inhibit human papillomavirus (HPV) DNA replication. This screen led to the discovery of (biphenyl-4-sulfonyl)acetic acid 1, which inhibits the ATPase activity of HPV type 6 E1 helicase with a low micromolar IC50 value. A hit-to-lead exercise rapidly converted 1 into a low nanomolar lead series.
- Faucher, Anne-Marie,White, Peter W.,Brochu, Christian,Grand-Ma?tre, Chantal,Rancourt, Jean,Fazal, Gulrez
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- PYRROLE DERIVATIVE
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A novel pyrrole derivative represented by the following formula (1) and a salt thereof: wherein R1 means substituted alkenyl, etc.; R2 means substituted benzoyl, etc.; and R3 to R5 each means hydrogen, alkyl, halogeno, etc. The derivative and salt have antidiabetic activity.
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- Cinnamamide derivatives and drug compositions containing the same
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The invention relates to cinnamamide derivatives having the following formula wherein R1represents a hydroxyl group, a C1-6-alkoxy group, an arylalkoxy group or a substituted or unsubstituted amino group; R2and R3are same or different, each of which represents a hydrogen atom, a halogen atom or a C1-4-alkyl group; R4represents a hydrogen atom or a C1-6-alkyl group; R5represents a hydrogen atom, a C1-6-alkyl group or an aryl group; R6represents a hydrogen atom, a C1-6-alkyl group, a cyano group or a C1-6-alkoxy-carbonyl group; W represents an oxygen atom, a sulfur atom, an imino group, a methylene group, a hydroxymethylene group or a carbonyl group; X and Y are same or different, each of which represents an oxygen atom or a sulfur atom; m represents an integer of 0 to 2; n represents an integer of 1 to 3; and when m is 0, a group: —C(R2)(R3)—W— may represent a vinylene group; or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the above compound, in particular, an immunomodulatory agent and a prophylactic or therapeutic agent for nephrotic syndrome, circulatory disorders or respiratory diseases.
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- Biphenyl hydroxamate inhibitors of matrix metalloproteinases
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Compounds of formula STR1 or a pharmaceutically acceptable salt thereof inhibit matrix metalloproteinases and TNFα secretion and are useful in the treatment of inflammatory disease states. Also disclosed are matrix metalloproteinases and TNFα secretion inhibiting compositions and a method for inhibiting matrix metalloproteinases and TNFα secretion.
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