- Facile Palladium-Catalyzed Synthesis of 3-Arylpyrazolo-[1,5-a]pyrimidines
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An efficient palladium-catalyzed synthesis of 3-arylpyrazolo[1,5-a] pyrimidines has been investigated. The key step in the synthesis is a Suzuki biaryl coupling of 3-bromo-2,5-dimethyl-7-aminopyrazolo[1,5-a]pyrimidines with arylboronic acids to provide 3-
- Majo, Vattoly J.,Prabhakaran, Jaya,John Mann,Dileep Kumar
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- SUBSTITUTED BENZAZINONES AS ANTIBACTERIAL COMPOUNDS
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The present invention relates to LpxC antibacterial compounds of Formula (1A), corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions:, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.
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Page/Page column 170
(2017/07/14)
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- ANTI-MALIGNANT TUMOR AGENT COMPOSITION
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To provide a satisfactory anticancer agent composition suppressing the growth of cancer (malignant tumor) reliably and hardly causing side effects, the present invention is directed to an anticancer agent composition including the following agents as active ingredient; a LAT1 inhibitor, and one or more agents selected from the group consisting of an alkylating agent, a platinum-based antineoplastic agent, an anti-metabolite, a topoisomerase inhibitor, an anti-microtubule polymerizing agent, a hormonal agent, an anti-microtubule depolymerizing agent, an anticancer antibiotic, and a molecular targeted agent.
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Paragraph 0087; 0109
(2016/01/25)
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- SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
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Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
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- SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
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Provided are certain pyridopyrazine compounds, pharmaceutical compositions thereof and methods of use therefor.
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- AROMATIC AMINO ACID DERIVATIVES AND MEDICINAL COMPOSITIONS
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An aromatic amino acid derivative represented by the formula ( I ) or its pharmacologically acceptable salt: wherein,R1 is a hydrogen atom or an amino-protecting group,R2 is a halogen atom or an alkyl, aralkyl or aryl group,R3 is 1○ a hydrogen atom, 2○ an aroylamino group, 3○ a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. 4○ a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, 5○ an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, 6○ an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; 1 is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5. This compound can inhibit a transporter (LAT1) of essential amino acid which is one of main nutrition for cancer cells and accordingly cause drain of the essential amino acid on the cancer cells and finally can prohibit the multiplication of cancer cells.
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