358780-13-9Relevant academic research and scientific papers
3-Substituted Quinolines as RORγt Inverse Agonists
Tanis, Virginia M.,Venkatesan, Hariharan,Cummings, Maxwell D.,Albers, Michael,Kent Barbay,Herman, Krystal,Kummer, David A.,Milligan, Cynthia,Nelen, Marina I.,Nishimura, Rachel,Schlueter, Thomas,Scott, Brian,Spurlino, John,Wolin, Ronald,Woods, Craig,Xue, Xiaohua,Edwards, James P.,Fourie, Anne M.,Leonard, Kristi
, p. 1463 - 1470 (2019)
We have previously reported the syntheses of a series of 3,6-disubstituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). These molecules are potent binders but are high molecular weight and they exhibited poor solubility at pH 2 and pH 7. This manuscript details our efforts at improving physical chemical properties for this series of compounds by increasing the diversity at the 3-position (i.e. introducing heteroatoms and lowering the molecular weight). These efforts have led to molecules which are potent binders with improved solubility.
Cross-Electrophile Coupling of Unactivated Alkyl Chlorides
Sakai, Holt A.,Liu, Wei,Le, Chi,MacMillan, David W. C.
, p. 11691 - 11697 (2020)
Alkyl chlorides are bench-stable chemical feedstocks that remain among the most underutilized electrophile classes in transition metal catalysis. Overcoming intrinsic limitations of C(sp3)-Cl bond activation, we report the development of a novel organosilane reagent that can participate in chlorine atom abstraction under mild photocatalytic conditions. In particular, we describe the application of this mechanism to a dual nickel/photoredox catalytic protocol that enables the first cross-electrophile coupling of unactivated alkyl chlorides and aryl chlorides. Employing these low-toxicity, abundant, and commercially available organochloride building blocks, this methodology allows access to a broad array of highly functionalized C(sp2)-C(sp3) coupled adducts, including numerous drug analogues.
Nickel-Catalyzed Addition of C–C Bonds of Amides to Strained Alkenes: The 1,2-Carboaminocarbonylation Reaction
Ito, Yuri,Kodama, Takuya,Nakatani, Syun,Shiraki, Ryota,Tobisu, Mamoru
supporting information, p. 662 - 666 (2022/02/05)
C(aryl)–C(═O) bonds of aryl amides can be activated and added across alkenes with the aid of a nickel catalyst. This 1,2-carboaminocarbonylation reaction enables the dicarbofunctionalization of alkenes with an atom economy of 100%.
Biocatalytic Strategy for the Highly Stereoselective Synthesis of CHF2-Containing Trisubstituted Cyclopropanes
Carminati, Daniela M.,Decaens, Jonathan,Couve-Bonnaire, Samuel,Jubault, Philippe,Fasan, Rudi
supporting information, p. 7072 - 7076 (2021/02/27)
The difluoromethyl (CHF2) group has attracted significant attention in drug discovery and development efforts, owing to its ability to serve as fluorinated bioisostere of methyl, hydroxyl, and thiol groups. Herein, we report an efficient biocat
Novel Inhibitors of an Insect Pest Chitinase: Design and Optimization of 9-O-Aromatic and Heterocyclic Esters of Berberine
Chen, Lei,Cheng, Jiagao,Qian, Xuhong,Shao, Xusheng,Yang, Qing,Zhu, Ling
, p. 7526 - 7533 (2021/07/26)
OfChi-h, a lepidopteran-exclusive glycoside hydrolase family 18 (GH18) chitinase from the agricultural insect pest Ostrinia furnacalis, is a promising molecular target candidate for pest control and management. Berberine (BER), a traditional Chinese medic
NOVEL NUCLEOSIDE OR NUCLEOTIDE DERIVATIVES, AND USES THEREOF
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Paragraph 0063; 0090, (2020/12/10)
The present disclosure relates to a novel nucleoside or nucleotide derivative, a racemate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating viral infection-associated diseases, containing the same as an active ingredient.
PROLONGED ECTOPARASITE-CONTROLLING AGENT FOR ANIMAL
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Paragraph 0161; 0168, (2019/04/16)
A compound represented by Formula (1) can be used as a prolonged ectoparasite-controlling agent for an animal. A preparation for systemic application for use in prolonged control of an ectoparasite in an animal include the compound. A method for prolonged
HETEROARYL COMPOUNDS AS KINASE INHIBITOR
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Page/Page column 77-78, (2019/10/04)
Provided herein are heteroaryl compounds of formula (I) having activity on a receptor protein tyrosine kinase, wherein R 1, R 2, R 3, A, Q, Z, X and W are set forth in the description, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof.
HETEROARYL LINKED QUINOLINYL MODULATORS OF RORγT
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Paragraph 0189-0192, (2016/11/21)
The present invention comprises compounds of Formula I wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification, The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndro
PHENYL LINKED QUINOLINYL MODULATORS OF RORyt
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Paragraph 0195, (2015/04/21)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also
