172270-85-8Relevant academic research and scientific papers
CYCLOALKYLIDENE CARBOXYLIC ACIDS AND DERIVATIVES AS BTK INHIBITORS
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Page/Page column 123-124, (2021/03/05)
The present invention relates to novel cycloalkylidene carboxylic acids and derivatives thereof useful as Bruton tyrosine kinase (BTK) inhibitors. The present disclosure also relates to processes for their preparation, pharmaceutical compositions containing one or more such compounds, and to the use of such compounds and pharmaceutical compositions for the treatment of disorders involving mediation of BTK in humans (Formula I).
Construction of Morphan Derivatives by Nitroso–Ene Cyclization: Mechanistic Insight and Total Synthesis of (±)-Kopsone
Zhai, Li,Tian, Xuechao,Wang, Chao,Cui, Qi,Li, Wenhua,Huang, Sha-Hua,Yu, Zhi-Xiang,Hong, Ran
supporting information, p. 11599 - 11603 (2017/09/11)
A type II nitroso–ene cyclization was developed for the construction of morphan derivatives with good functional-group tolerance. DFT calculations revealed that the nitroso–ene reaction proceeds in a stepwise manner involving diradical or zwitterionic intermediates. The rate-determining step is C?N bond formation, followed by a rapid hydrogen-transfer step with a chair-conformation transition state. The current approach was also successfully applied in the first total synthesis of (±)-kopsone, a highly strained yet simple morphan-type alkaloid isolated from Kopsia macrophylla.
PYRIMIDINE PYRAZOLYL DERIVATIVES
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Page/Page column 130, (2014/02/15)
The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases (I).
NOVEL TETRAHYDROISOQUINOLINE COMPOUNDS
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Page/Page column 10, (2012/07/14)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect and feeding suppressant effect. The present invention provides trans-6-[3-(2,4-difluoro-phenyl)-ureido]-3,4-dihydro-1H-is
NOVEL TETRAHYDROISOQUINOLINE DERIVATIVE
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Page/Page column 25, (2010/12/29)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect and feeding suppressant effect. The present invention provides a compound represented by the general formula (I), or pharmacologically acceptable salt thereof: [wherein, R1 represents a phenylaminocarbonyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group A, a benzoxazol-2-yl group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group A, or the like; R2 independently represents a C1-C6 alkyl group; R3 represents a group represented by the formula -C(=O)-O-R4 or the like; R4 represents a hydrogen atom, a C1-C6 alkyl group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group B, or the like; X represents an oxygen atom, a methylene group, or a group represented by the formula -NH-, or the like; L represents a single bond, a methylene group, or the like;...... represents a single bond or a double bond; m represents 1 or 2; n represents an integer of 0 to 5; Substituent Group A represents a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 alkoxy group, or the like; and Substituent Group B represents a C3-C6 cycloalkyl group, a phenyl group, a carboxyl group, or the like].
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors
Rew, Yosup,McMinn, Dustin L.,Wang, Zhulun,He, Xiao,Hungate, Randall W.,Jaen, Juan C.,Sudom, Athena,Sun, Daqing,Tu, Hua,Ursu, Stefania,Villemure, Elisia,Walker, Nigel P.C.,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
scheme or table, p. 1797 - 1801 (2009/12/07)
Discovery and optimization of a piperidyl benzamide series of 11β-HSD1 inhibitors is described. This series was derived from a cyclohexyl benzamide lead structures to address PXR selectivity, high non-specific protein binding, poor solubility, limited in
SUBSTITUTED BICYCLOLACTAM COMPOUNDS
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Page/Page column 17-18, (2009/03/07)
The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d, Q, A, Z, and R7 /s
DISPIRO TETRAOXANE COMPOUNDS
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Page/Page column 51, (2008/06/13)
A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=-C(O)NR1R2, -NR1R2 or -S(O)2R4, where R1, R2 and R4 are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R1 and R2 are linked so as to form part of a substituted or unsubstituted heterocyclic ring, or X=N and Y=-S(O)2R3 or -C(O)R3, where R3 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.
COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS
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Page/Page column 144; 145, (2008/06/13)
Compounds represented by formula (I) : or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flavivi?dae viral infections Said viral infection is Hepatitis C virus (HCV), bovme viral diarrhea virus (BVDV), hog cholera virus, dengue fever virus, Japanese encephalitis virus or yellow fever virus
Benzamide derivatives and uses related thereto
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Page/Page column 62-63, (2008/06/13)
Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.
