- Anthranilic acid amide compound and its preparation and use
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The invention belongs to the field of drug synthesis and relates to an anthranilamide compound with the general formula (I), in particular to an anthranilamide compound containing piperidine or piperazine, and pyridine analogues, a preparation method and medical application of the anthranilamide compound and the pyridine analogues. According to the compound, through a target gene Gli inhibitory activity test in an in-vitro Hedgehog signal pathway, a result shows that the compound has good Hedgehog signal pathway inhibitory activity, and a new antitumor drug can further be prepared. (Please see the formula in the specification).
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Paragraph 0027; 0028
(2018/03/24)
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- A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor
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A novel series of P2Y12 antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure-activity relationships (SAR) are described. Several compounds
- Bach, Peter,Bostr?m, Jonas,Brickmann, Kay,Van Giezen,Hovland, Ragnar,Petersson, Annika U.,Ray, Asim,Zetterberg, Fredrik
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supporting information; experimental part
p. 2877 - 2881
(2011/06/24)
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- PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
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The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
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- NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND BENAMIDE COMPOUNDS AND DRUGS CONTAINING THE SAME
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Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases. In formula (I), R1 and R2 represent alkyl, alkoxy, cycloalkyl, phenyl, alkenyl, alkynyl, or a five- or six-membered saturated or unsaturated heterocyclic ring, or R1 and R2, together with a nitrogen atom to which R1 and R2 are attached, may form a ring; R3 and R4 represent a hydrogen atom, alkyl, a halogen atom, hydroxyl, nitrile, alkoxycarbonyl, alkoxy, or carboxyl; or R2 and R3 may be attached to each other to form -(CH2)m-, -N=CH-, -CH=N-, or -(C1-6 alkyl)C=N-; A, D, E, and G each represent a carbon atom, or any one of A, D, E, and G represents a nitrogen atom with the other three each representing a carbon atom; Q represents a nitrogen atom or a carbon atom; Y represents a group represented by formula (II) wherein X represents a hydrogen atom, group -C(=O)N(R5)R6 or group -C(=O)OR7, R8 is absent or represents a bond, an oxygen atom, a sulfur atom, -SO2-, -SO-, -CH2-CH2-, or - CH=CH-, and R9 and R10 represent a hydrogen atom, alkyl, alkoxy, a halogen atom, or hydroxyl; and Z represents - (CH2)n-, -O-(CH2)i-, or -C(=O)NH-(CH2)i-.
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