37828-19-6Relevant academic research and scientific papers
Synthesis method of arylcyclobutane compound
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Paragraph 0130-0133; 0176-0178, (2022/01/10)
The present invention discloses a method for synthesizing an arylcyclobutane compound to 1eq phenylacetonitrile and 1.1eq 1-bromo-3-chloropropane as raw material, N,N- dimethylacetamide as a solvent, plus 2.5eq sodium hydride, under the protection of iner
Amide compound and derivative thereof, preparation method, pharmaceutical composition and application thereof
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Paragraph 0390; 0391; 0394; 0395, (2021/07/09)
The invention discloses an amide compound and derivative thereof, a preparation method, a pharmaceutical composition and application thereof. The structure of the amide compound is shown as a formula (I). The derivatives of theamide compound relate to a stereoisomer, a tautomer, a metabolite, a metabolic precursor, a prodrug, a solvate, a salt of the solvate, a crystal, a pharmaceutically acceptable salt or a mixture of the above of theamide compound. The amide compound and the derivative thereof have an efficient inhibition effect on indoleamine 2, 3-dioxygenase 1, and can be used for preparing medicines for treating indoleamine 2, 3-dioxygenase 1 mediated immunosuppression related diseases, the prepared medicine can exert the medicine effect at the molecular level and is wide in application, and the synthesis method of the compound is simple, convenient and easy to operate.
Short Synthesis of Oxetane and Azetidine 3-Aryl-3-carboxylic Acid Derivatives by Selective Furan Oxidative Cleavage
Bull, James A.,Choi, Chulho,Dubois, Maryne A. J.,Lee Wei Jie, Alvin,Mousseau, James J.,Smith, Milo A.,White, Andrew J. P.
, p. 5279 - 5283 (2020/08/14)
Four-membered rings remain underexplored motifs despite offering attractive physicochemical properties for medicinal chemistry. Arylacetic acids bearing oxetanes, azetidines, and cyclobutanes are prepared in two steps: a catalytic Friedel-Crafts reaction from four-membered ring alcohol substrates, followed by mild oxidative cleavage. The suitability of the products as building blocks is reflected in their facile purification and amenability to derivatization. Examples include heteroaromatics and aryltriflates, as well as oxetane-derived profen drug analogues and a new endomorphin derivative containing an azetidine amino acid residue.
Iridium-Catalyzed Enantioselective C(sp3)–H Borylation of Cyclobutanes
Chen, Xiang,Chen, Lili,Zhao, Hongliang,Gao, Qian,Shen, Zhenlu,Xu, Senmiao
supporting information, p. 1533 - 1537 (2020/09/09)
We herein report the first example of iridium-catalyzed enantioselective C(sp3)–H borylation of cyclobutanes using benzoxazoline as the directing group. The combination of a chiral bidentate boryl ligand and an iridium precursor has found to effectively catalyze C(sp3)–H borylation to afford a variety of cyclobutylboronates with good to excellent enantioselectivities. We also demonstrate the synthetic utility of the current method by converting the stereogenic C—B bond to other functionalities.
Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO)
He, Wu,Zhou, Bin,Liu, Weijia,Zhang, Meizi,Shen, Zhenhua,Han, Zhifu,Jiang, Qingwei,Yang, Qinghua,Song, Chuanjun,Wang, Ruiyong,Niu, Tianhui,Han, Shengna,Zhang, Lirong,Wu, Jie,Guo, Feima,Zhao, Renbin,Yu, Wenquan,Chai, Jijie,Chang, Junbiao
, p. 7341 - 7348 (2015/10/05)
N-(5-Chloro-2,4-dihydroxyphenyl)-1-phenylcyclobutanecarboxamide (N-CDPCB, 1a) is found to be an inhibitor of the fat mass and obesity associated protein (FTO). The crystal structure of human FTO with 1a reveals a novel binding site for the FTO inhibitor and defines the molecular basis for recognition by FTO of the inhibitor. The identification of the new binding site offers new opportunities for further development of selective and potent inhibitors of FTO, which is expected to provide information concerning novel therapeutic targets for treatment of obesity or obesity-associated diseases.
Cycloalkyl Amine Compounds
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Paragraph 0247; 0249, (2015/03/04)
Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C═O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
PYRAZOLE DERIVATIVES AS MODULATORS OF CALCIUM RELEASE -ACTIVATED CALCIUM CHANNEL
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Page/Page column 71, (2011/04/26)
Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
IL-8 RECEPTOR ANTAGONISTS
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Page/Page column 52, (2008/12/06)
This invention relates to novel compounds, compositions and combinations thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
ACYCLIC HYDRAZIDES AS CANNABINOID RECEPTOR MODULATORS
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Page/Page column 49, (2010/11/08)
The acyclic hydrazides of the invention are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present inventio
Substituted alkanoic acids
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Page 39, (2010/02/05)
The invention is directed to physiologically active compounds of general formula (I): wherein:- represents (i) a saturated 3 to 6 membered carbocycle, optionally substituted by one or more alkyl groups, (ii) indanyl or (iii) a saturated 4 to 6 membered heterocyclic ring; R1 represents R3Z1-Het- or R4N(R5)—C(═O)—NH—Ar1—; L1 represents an —R6—R7— linkage; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; L2 represents an alkylene linkage; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).
