- NOVEL STING AGONISTS
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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.
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Paragraph 0507; 0511; 0591; 0592; 0595
(2020/05/14)
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- AMINO PYRAZOLONE DERIVATIVE HAVING CONDENSED RING STRUCTURE
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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
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Paragraph 0165; 0166; 0167
(2016/10/08)
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- PYRAZOLONE DERIVATIVE HAVING CYCLIC SIDE CHAIN
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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
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Paragraph 0158; 0159
(2016/10/08)
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- AMINOPYRAZOLONE DERIVATIVE
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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.
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Paragraph 0189
(2017/01/05)
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- 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
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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.
- 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
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p. 3983 - 3987
(2013/07/27)
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- PYRIDINYL SULFONAMIDE MODULATORS OF CHEMOKINE RECEPTORS
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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.
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Page/Page column 15
(2010/11/27)
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- Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists
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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.
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Page/Page column 29
(2010/11/27)
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- COMPOUNDS AND METHODS FOR TREATING DYSLIPIDEMIA
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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.
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Page/Page column 57-58
(2008/06/13)
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- Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: Synthesis and biological testing
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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.
- Hussenether, Thomas,Huebner, Harald,Gmeiner, Peter,Troschuetz, Reinhard
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p. 2625 - 2637
(2007/10/03)
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- Bridged piperazine derivatives
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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.
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- New Process for the Synthesis of Imidazopyridine Derivatives as Potent Orally Active Thromboxane A2 Receptor Antagonists
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A new synthetic route to prepare the 4-pyridin-2-yl>-3,3-dimethylbutanoic acid (UP 116-77) is described.UP 116-77 is a potent orally active TXA2/PGH2 receptor antagonist currently under pharmacological investigation.Its development needed a suitable synthesis for industrial processing.The cyclization of 3-amino-5-chloro-2-(4-chlorophenyl)methylaminopyridine 4 with 3,3-dimethylglutaric anhydride in refluxing acetic acid affords a new efficient and simple way to UP 116-77 and subsequently to various 2-substituted imidazopyridine derivatives.
- Nikolai, E.,Claude, S.,Teulon, J. M.
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- Process for the preparation of (3-fluoropyridin-2-yloxy)phenoxypropionic acids
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(3-Fluoropyridin-2-yloxy)phenoxypropionic acids of formula I STR1 wherein X is hydrogen, fluoro, chloro, bromo or trifluoromethyl and Y is hydrogen, sodium or potassium, are prepared by reacting a compound of formula II STR2 wherein X and Y are as defined for formula I, in an anhydrous mixture of hydrogen fluoride, dimethylsulfoxide and a diazotising agent under normal pressure, and converting the diazonium fluoride so produced by thermal decomposition into the (3-fluoropyridin-2-yloxy)phenoxypropionic acid of formula I.
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- REACTIVITIES OF HETEROCYCLIC COMPOUNDS IN NITRATION. 5. KINETICS OF NITRATION OF 5-SUBSTITUTED 2-PICRYLAMINOPYRIDINES
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The kinetics of nitration of 5-bromo-, 5-chloro-, and 5-nitro-2-picrylaminopyridines in 80-96percent sulfuric acid were studied by a spectrophotometric method.The kinetic parameters of nitration were calculated.The UV spectra of the neutral and protonated forms in aqueous sulfuric acid solutions were identified.It was established that the indicated compounds are nitrated in the protonated form.The relative (as compared with benzene) rates of nitration were calculated.
- Sharnin, G. P.,Falyakhov, I. F.,Khairutdinov, F. G.
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p. 1234 - 1238
(2007/10/02)
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