742100-75-0Relevant academic research and scientific papers
SULFONAMIDE COMPOUNDS HAVING TNAP INHIBITORY ACTIVITY
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Page/Page column 112; 230; 231; 232, (2018/07/29)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
CERTAIN PROTEIN KINASE INHIBITORS
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Paragraph 155; 156, (2017/12/27)
Provided are certain CDK4/6 inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
NOVEL PYRAZOLO PYRIMIDINE DERIVATIVES AND THEIR USE AS MALT1 INHIBITORS
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Page/Page column 76, (2015/12/31)
The present invention describes new pyrazolo-pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein, R1 is halogen, cyano, or C1-C3alkyl optionally substituted by halogen; R2 is C1-C6alkyl optionally substituted one or more times by C1-C6alkyl, C2-C6alkenyl, hydroxyl, N,N-di-C1-C6alkyl amino, N-mono-C1-C6alkyl amino, O-Rg, Rg, phenyl, or by C1-C6alkoxy wherein said alkoxy again may optionally be substituted by C1-C6alkoxy, N,N-di-C1-C6alkyl amino, Rg or phenyl; C3-C6cycloalkyl optionally substituted by C1-C6alkyl, N,N-di-C1-C6alkyl amino or C1-C6alkoxy-C1-C6alkyl, and/or two of said optional substituents together with the atoms to which they are bound may form an annulated or spirocyclic 4 - 6 membered saturated heterocyclic ring comprising 1 - 2 O atoms; phenyl optionally substituted by C1-C6alkoxy; a 5 - 6 membered heteroaryl ring having 1 to 3 heteroatoms selected from N and O said ring being optionally substituted by C1-C6alkyl which may be optionally substituted by amino or hydroxy; Rg; or N,N-di-C1-C6alkyl amino carbonyl; and R is phenyl independently substituted two or more times by Ra, 2-pyridyl independently substituted one or more times by Rb, 3-pyridyl independently substituted one or more times by Rc, or 4-pyridyl independently substituted one or more times by Rd; which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
SPIRO CONDENSED BARBITURIC ACID DERIVATIVES FOR USE AS ANTIBACTERIAL
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Page/Page column 70, (2009/03/07)
In one aspect, the present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to method for their preparation.
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors
Letavic, Michael A.,Keith, John M.,Ly, Kiev S.,Barbier, Ann J.,Boggs, Jamin D.,Wilson, Sandy J.,Lord, Brian,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 2566 - 2569 (2008/02/01)
A series of novel tetrahydronaphthyridine-based histamine H3 ligands that have serotonin reuptake transporter inhibitor activity is described. The 1,2,3,4-tetrahydro-2,6-naphthyridine scaffold is assembled via the addition of a nitrostyrene to a metalated pyridine followed by reduction and cyclization to form the naphthyridine. In vitro biological data for these novel compounds are discussed.
NAPHTHYRIDINE COMPOUNDS
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Page/Page column 26, (2010/11/25)
Certain naphthyridine compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
ACRYLAMIDE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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Page/Page column 98, (2010/02/14)
A compound represented by the formula: wherein R1 is a 5- or 6-membered ring; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; R7 and R8 are each a hydrogen atom or a lower alkyl group; Z1 is another 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W1-Z2b- [wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group or a bond, and W1 is an alkylene chain]; X is CR (wherein R is a hydrogen atom, a lower alkyl group, a lower alkoxy group, an acyl group, or R and adjacent R4 may form a 5- or 6-membered alicyclic heterocyclic group) or N; R4 is NR5R6 (wherein R5 and R6 are each a hydrogen atom, a hydrocarbon group, a heterocyclic group or an acyl group), or R5 and R6 are bonded to each other to form a heterocyclic group of NR5R6; and R2 is (1) an amino group which may be a quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or the like; or a salt thereof. The compound has excellent CCR5 antagonistic activity and thus is useful as a prophylactic and/or therapeutic medicine for HIV infection into human peripheral blood monocyte, especially for AIDS.
