- AZETIDIN-3-YLMETHANOL DERIVATIVES AS CCR6 RECEPTOR MODULATORS
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The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.
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Page/Page column 178
(2021/11/06)
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- CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT
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PROBLEM TO BE SOLVED: To provide a cyclic amine compound that has insecticidal activity and/or acaricidal activity, has excellent safety, and can be synthesized in an industrially advantageous manner, and a pest control agent containing the same as an active ingredient. SOLUTION: The present invention provides a compound represented by formula (I), or a salt thereof. (Q is halogeno or the like; R1 is cyano or the like; R2 is H, halogeno or the like; R3 is halogeno, C1-6 alkyl or the like; A is O or S; p1 and p2 are 0 or 1; X1 is halogeno, C1-6 alkoxy or the like; m is an integer of 0-4; X2 is H, a halogeno group or the like; Y is C6-10 aryl or the like; X1 and X2 may form oxymethylene oxy groups). SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0126; 0137; 0138
(2019/07/03)
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- CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT
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A compound represented by a formula (I), or a salt thereof: wherein Ar1 is a substituted or unsubstituted C6-10 aryl group, or the like; the number of X1 groups that can be substituted on Ar1 is 5 or less; Xsup
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Paragraph 0450-0453
(2019/07/10)
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- Histone deacetylase inhibitor and preparation method and application thereof
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The invention provides a compound shown in a formula (A) or a conformational isomer of the compound or an optical isomer of the compound or a pharmaceutically acceptable salt of the compound. Throughan experiment, it is proved that the compound shown in the formula (A) can effectively inhibit the activity of histone deacetylase (HDAC), in addition, the compound, especially the compounds II-1-II-4, the compounds II-6-II-7, the compound II-13, the compound II-15, the compound II-18, the compounds II-25-II-26, the compounds III-1-III-4 and the compounds III-12-III-13, has a significant inhibiting effect on the proliferative activity of multiple kinds of tumor cells, and the inhibiting effect of the compound is superior to that of a known reference compound SAHA. Therefore, the compound has great potential in preparation of histone deacetylase inhibitors and antitumor medicines.
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Paragraph 0132-0134
(2019/07/08)
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- COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES
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The present disclosure relates to compounds according to Formula (I), treating diseases.
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Paragraph 00357-00358
(2019/03/12)
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- Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy
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In this study, a series of novel HDAC inhibitors, using 1,2,4-oxadiazole-containing as the cap group, were synthesized and evaluated in vitro. Compound 14b, N-hydroxy-2-(methyl((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide, displayed the most potent histone deacetylase (HDAC) inhibition, especially against HDAC1, 2, and 3 with IC50 values of 1.8, 3.6 and 3.0 nM, respectively. In vitro antiproliferative studies confirmed that 14b was more potent than SAHA, with IC50 values against 12 types of cancer cell lines ranging from 9.8 to 44.9 nM. The results of Western blot assays showed that compound 14b can significantly up-regulate the acetylation of the biomarker his-H3 and molecular docking analyses revealed the mode of action of compound 14b against HDAC1. The results of flow-cytometry analysis suggested that compound 14b induces cell cycle arrest at the G1 phase and has apoptotic effects. Further investigation of the activity of 14b on the primary cells of three patients, showed IC50 values of 21.3, 61.1, and 77.4 nM. More importantly, an oral bioavailability of up to 53.52% was observed for 14b. An in vivo pharmacodynamic evaluation demonstrated that compound 14b can significantly inhibit tumor growth in a Daudi Burkitt's lymphoma xenograft model, with tumor inhibition rates of 53.8 and 46.1% observed at 20 and 10 mg/kg when administered p.o. and i.v., respectively. These results indicate that compound 14b may be a suitable lead for further evaluation and development as an HDAC inhibitor and a potent anticancer agent.
- Yang, Zhuang,Shen, Mingsheng,Tang, Minghai,Zhang, Wanhua,Cui, Xue,Zhang, Zihao,Pei, Heying,Li, Yong,Hu, Mengshi,Bai, Peng,Chen, Lijuan
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p. 116 - 130
(2019/06/11)
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- OXYMETHYLENE ARYL COMPOUNDS FOR TREATING INFLAMMATORY GASTROINTESTINAL DISEASES OR GASTROINTESTINAL CONDITIONS
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Use of oxymethylene aryl GPRl 19 agonists, and optionally DPP IV inhibitors and optionally metformin, for the treatment of inflammatory gastrointestinal diseases or gastrointestinal conditions involving malabsorption of nutrients and/or fluids are provide
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Paragraph 0436; 0437
(2018/03/28)
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- COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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Page/Page column 131
(2018/05/17)
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- Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques
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USP7 is a deubiquitinase implicated in destabilizing the tumor suppressor p53, and for this reason it has gained increasing attention as a potential oncology target for small molecule inhibitors. Herein we describe the biophysical, biochemical, and comput
- Di Lello, Paola,Pastor, Richard,Murray, Jeremy M.,Blake, Robert A.,Cohen, Frederick,Crawford, Terry D.,Drobnick, Joy,Drummond, Jason,Kategaya, Lorna,Kleinheinz, Tracy,Maurer, Till,Rougé, Lionel,Zhao, Xianrui,Wertz, Ingrid,Ndubaku, Chudi,Tsui, Vickie
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p. 10056 - 10070
(2018/01/10)
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- INDAZOLONES AS MODULATORS OF TNF SIGNALING
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The disclosure provides indazolone compounds, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the disclosure may be useful for treating immunological and oncological conditions.
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Page/Page column 116
(2016/11/02)
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- NOVEL TRIAZOLONE DERIVATIVES OR SALTS THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention provides a triazolone derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The triazolone derivative or its pharmaceutically acceptable salt can effectively activate GPR119; and therefore be usefully applied for preventing or treating diabetes mellitus.
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Paragraph 771; 772; 773
(2014/11/13)
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- AMINOPYRIMIDINONES AS INTERLEUKIN RECEPTOR-ASSOCIATED KINASE INHIBITORS
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This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
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Page/Page column 149
(2013/05/22)
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- CHEMOKING RECEPTOR ANTAGONISTS
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Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
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Page/Page column 100
(2013/03/26)
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- Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors
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Mycobacterial transcriptional repressor EthR controls the expression of EthA, the bacterial monooxygenase activating ethionamide, and is thus largely responsible for the low sensitivity of the human pathogen Mycobacterium tuberculosis to this antibiotic.
- Flipo, Marion,Desroses, Matthieu,Lecat-Guillet, Nathalie,Villemagne, Baptiste,Blondiaux, Nicolas,Leroux, Florence,Piveteau, Catherine,Mathys, Vanessa,Flament, Marie-Pierre,Siepmann, Juergen,Villeret, Vincent,Wohlk?nig, Alexandre,Wintjens, René,Soror, Sameh H.,Christophe, Thierry,Jeon, Hee Kyoung,Locht, Camille,Brodin, Priscille,Déprez, Benoit,Baulard, Alain R.,Willand, Nicolas
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experimental part
p. 68 - 83
(2012/03/10)
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- PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora.
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Page/Page column 46
(2011/11/30)
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- TRIAZOLE OXADIAZOLES DERIVATIVES
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The invention relates to compounds of formula (I), wherein R1, R2, Ra, Rb, X have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
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Page/Page column 122
(2009/07/25)
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- PTSA-ZnCl2: An efficient catalyst for the synthesis of 1,2,4-oxadiazoles from amidoximes and organic nitriles
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(Chemical Equation Presented) PTSA-ZnCl2 has been proved to be an efficient and mild catalyst for the synthesis of 3,5-disubstituted-1,2,4- oxadiazoles from amidoximes and organic nitriles.
- Augustine, John Kallikat,Akabote, Vani,Hegde, Shrivatsa Ganapati,Alagarsamy, Padma
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supporting information; experimental part
p. 5640 - 5643
(2009/12/08)
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- CYCLIC AMINOALKYLCARBOXAMIDE DERIVATIVE
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The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or -C(R6)(R7)-, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.
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Page/Page column 22
(2009/06/27)
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- NOVEL HETEROCYCLIC METHYLENE PIPERIDINE DERIVATIVES AND THEIR USE
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The present invention is directed to compounds of formula (I) compositions comprising them and their use.
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Page/Page column 97
(2009/03/07)
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- P70 S6 KINASE INHIBITORS
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The present invention provides p70 S6 kinase inhibitors of the formula: pharmaceutical formulations comprising them, and methods for their use.
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Page/Page column 24
(2009/01/20)
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- HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
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Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.
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Page/Page column 102-103
(2008/12/07)
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- AMIDE COMPOUNDS
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The present invention provides compounds represented by the formula (Ie) and the formula (If) wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT
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Page/Page column 153-154
(2008/06/13)
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- Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
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The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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Page/Page column 33
(2008/06/13)
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- Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors
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Human immunodeficiency virus type-1 (HIV-1) integrase, one of the three constitutive viral enzymes required for replication, is a rational target for chemotherapeutic intervention in the treatment of AIDS that has also recently been confirmed in the clinical setting. We report here on the design and synthesis of N-benzyl-5,6-dihydroxypyrimidine-4-carboxamides as a class of agents which exhibits potent inhibition of the HIV-integrase-catalyzed strand transfer process. In the current study, structural modifications on these molecules were made in order to examine effects on HIV-integrase inhibitory potencies. One of the most interesting compounds for this series is 2-[1-(dimethylamino)-1-methylethyl]-N-(4-fluorobenzyl)-5,6-dihydroxypyrimidine- 4-carboxamide 38, with a CIC95 of 78 nM in the cell-based assay in the presence of serum proteins. The compound has favorable pharmacokinetic properties in preclinical species (rats, dogs, and monkeys) and shows no liabilities in several counterscreening assays, highlighting its potential as a clinically useful antiviral agent.
- Pace, Paola,Di Francesco, M. Emilia,Gardelli, Cristina,Harper, Steven,Muraglia, Ester,Nizi, Emanuela,Orvieto, Federica,Petrocchi, Alessia,Poma, Marco,Rowley, Michael,Scarpelli, Rita,Laufer, Ralph,Paz, Odalys Gonzalez,Monteagudo, Edith,Bonelli, Fabio,Hazuda, Daria,Stillmock, Kara A.,Summa, Vincenzo
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p. 2225 - 2239
(2007/10/03)
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- BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS
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Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
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- Substituted homopiperidine, piperidine or pyrrolidine derivatives
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A novel class of substituted homopiperidine, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the compounds possess histamine H3 receptor antagonistic activity and are thus useful in the treatment of disorders in which a histamine H3 receptor blockade is beneficial.
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Page/Page column 32-33
(2010/02/11)
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- HETEROARYLPIPERIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to compounds of the formula (I): (wherein R>12345610 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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- SUBSTITUTED HOMOPIPERIDINE, PIPERIDINE OR PYRROLIDINE DERIVATIVES
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A novel class of substituted homopiperidin, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the compounds possess histamine H3 receptor antagonistic activity and are useful in the treatment of disorders in which a histamine H3 receptor blockade is beneficial.
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- HETEROCYCLIC CYCLOPENTYL TETRAHYDROISOQUINOLINE AND TETRAHYDROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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- BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS
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Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula (I): which are used to modulate the CCR-
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