21427-62-3Relevant academic research and scientific papers
NOVEL STING AGONISTS
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Paragraph 0507; 0511; 0591; 0592; 0595, (2020/05/14)
The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z1, Z2, R1, R2, R3, R4 and R5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.
AMINO PYRAZOLONE DERIVATIVE HAVING CONDENSED RING STRUCTURE
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Paragraph 0165; 0166; 0167, (2016/10/08)
PROBLEM TO BE SOLVED: To provide a compound that has excellent inhibitory action on ATPase activity of TIP48/TIP49 complex and is therefore useful for the treatment of tumor, or a pharmacologically acceptable salt thereof. SOLUTION: The present invention provides a compound having a structure represented by general formula (I), its pharmacologically acceptable salt, or a pharmaceutical composition comprising the compound (where R3, R4, R5, R6, R7, W, X, Y, and Z are as defined in the specifications). SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
PYRAZOLONE DERIVATIVE HAVING CYCLIC SIDE CHAIN
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Paragraph 0158; 0159, (2016/10/08)
PROBLEM TO BE SOLVED: To provide a compound that has excellent inhibitory action on ATPase activity of TIP48/TIP49 complex and is therefore useful for the treatment of tumor, or a pharmacologically acceptable salt thereof. SOLUTION: The present invention provides a compound having a structure represented by general formula (I), its pharmacologically acceptable salt, or a pharmaceutical composition comprising the compound (where R1, R2, R3, R4, R5, R6, R7, W, and Z are as defined in the specifications). SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
AMINOPYRAZOLONE DERIVATIVE
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Paragraph 0189, (2017/01/05)
The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which has an excellent inhibitory action on the ATPase activity of a TIP48/TIP49 complex and as such, is useful for the treatment of tumors. [Solution] The present invention provides a compound having a structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the present specification.
Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors
Chun, Kwangwoo,Park, Ji-Seon,Lee, Han-Chang,Kim, Young-Ha,Ye, In-Hea,Kim, Kang-Jeon,Ku, Il-Whea,Noh, Min-Young,Cho, Goang-Won,Kim, Heejaung,Kim, Seung Hyun,Kim, Jeongmin
, p. 3983 - 3987 (2013/07/27)
New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC50 = 111 nM, EC50 = 1.78 μM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
PYRIDINYL SULFONAMIDE MODULATORS OF CHEMOKINE RECEPTORS
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Page/Page column 15, (2010/11/27)
The present invention relates to compounds of following formula (I) or pharmaceutically acceptable salts thereof; pharmaceutical compositions containing them, and their use in the treatment of disorders mediated by the CCR-2 receptor.
Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists
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Page/Page column 29, (2010/11/27)
Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(═O)—, —C(═NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.
COMPOUNDS AND METHODS FOR TREATING DYSLIPIDEMIA
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Page/Page column 57-58, (2008/06/13)
The present invention discloses compounds of formula I wherein A, n, m, j, q, K, W, X, K, Z, R1, R2, R3, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and its sequelae.
Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: Synthesis and biological testing
Hussenether, Thomas,Huebner, Harald,Gmeiner, Peter,Troschuetz, Reinhard
, p. 2625 - 2637 (2007/10/03)
Novel 4-arylpiperazin-1-yl-substituted 2,3-dihydro-1H-1,4- and 1H-1,5-benzodiazepines and their aza-analogues were synthesized as debenzoclozapine derivatives for evaluation as potential D4-ligands. While Ki values of some of the title compounds came within the range of clozapine, they showed an impressively greater selectivity over other dopamine receptor subtypes, especially D2. For the most promising compounds, intrinsic activity and binding properties to serotonin 5-HT1A and 5-HT2 were also determined.
Bridged piperazine derivatives
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, (2008/06/13)
A compound of the formula or the pharmaceutically acceptable salt thereof; wherein a, c, d, k, l, m, W, X, Y Z, R1, and R4 are as defined, and useful to treat inflammation and other immune disorders.
