144464-66-4Relevant articles and documents
Asymmetric synthesis of tricyclic tetralin derivatives via an intramolecular photoreaction
Yang, Chao,Xia, Wu Jiong,Scheffer, John R.
, p. 6791 - 6795 (2007)
An intramolecular photoreaction for the synthesis of tricyclic tetralin derivatives through a Norrish/Yang type cyclization is described. Asymmetric studies on this reaction using ionic chiral auxiliaries gave enantiomeric excesses of up to 99% at conversions?of?80%, and the reaction mechanism was mapped out by a single crystal-to-single crystal reaction.
Farnesoid X receptor (FXR) stimulant
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Paragraph 0235; 0240; 0241; 0242, (2019/02/25)
The invention belongs to the technical field of medicines, and particularly relates to a compound as shown in the formula (I), and pharmaceutically acceptable salt and ester or a stereisomer thereof.R1, R2, R3, M1, M2, m, n, Q, L, ring A, ring B and ring
Design, synthesis, and biological evaluation of Cyclobentinib (CB1107) as a potential anti-CML agent
Zhou, Zijun,Wang, Yang,Li, Jun,Hu, Baichun,Lin, Xiaolin,Chen, Ye,Wang, Rui,Liu, Ju,Liu, Hongsheng
, p. 1863 - 1875 (2018/06/20)
Cyclobentinib was designed and synthesized as a novel anti-CML agent, its in vitro activity against K562 cells was evaluated by MTT assay. CB1107 showed remarkable cytotoxicity against K562 cell line with an IC50 of 0.037 ± 0.028 μmol/L, and thus it was 17-fold more potent than the reference drug Imatinib. Inducing cell apoptosis and affecting cell cycling of this compound in K562 cells were estimated by using flow cytometry and Acridine Orange/Ethidium Bromide (AO/EB) staining. The results showed that CB1107 was capable of arresting cell cycle at G0/G1 phase as well as inducing cell apoptosis significantly. Molecular mechanism of CB1107 was detected by the protein expression of Bcr-AblP210 using western blotting analysis. Downregulation of expression of Bcr-AblP210 was obviously revealed in the treatment of this tetralin amide compound. Of note, the results of these investigations suggested that CB1107 is more potent than the reference drug Imatinib against K562 cells. Additionally, in vivo results indicated that CB1107 significantly decreased tumor growth in K562 tumor-bearing Non-obese Diabetic/Severe Combined Immunodeficiency (NOD/SCID) mice. Histopathological investigation revealed that CB1107 without notable toxicity in a given dose range. These findings collectively demonstrate CB1107 is a promising candidate as a novel anti-CML agent.
A DOR receptor antagonist compound as
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Paragraph 0183; 0184; 0185, (2017/08/19)
The invention provides a compound used as a DOR receptor antagonist. The structural formula of the compound is as shown in the specification. In comparison with the prior art, the invention expounds a pharmaceutical composition and a preparation containin
F- Nucleophilic-Addition-Induced Allylic Alkylation
Tian, Panpan,Wang, Cheng-Qiang,Cai, Sai-Hu,Song, Shengjin,Ye, Lu,Feng, Chao,Loh, Teck-Peng
supporting information, p. 15869 - 15872 (2016/12/23)
Herein we present a novel strategy based on palladium-catalyzed allylic alkylation by taking advantage of the nucleophilic addition of external fluoride onto gem-difluoroalkenes as the initiation step. The merit of this protocol is highly appealing, as it enables a formal allylation of trifluoroethylarene derivatives through the in situ generation of β-trifluorocarbanions, which otherwise are deemed to be problematic in deprotonative allylation. Furthermore, this strategy distinguishes itself by high modularity, operational simplicity, and wide substrate scope with respect to allyl carbonates, giving rise to a broad array of homoallyltrifluoromethane derivatives, which otherwise would not be easily obtained using existing synthetic methods.
THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
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Paragraph 00199, (2015/07/07)
The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
AMINO-PYRIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS
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Paragraph 00200, (2014/05/24)
The invention provides certain amino-pyridine-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R3, R4, R5, R6, and the subscript n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
One-pot formal synthesis of biorenewable terephthalic acid from methyl coumalate and methyl pyruvate
Lee, Jennifer J.,Kraus, George A.
supporting information, p. 2111 - 2116 (2014/04/17)
Diverse functionalized aromatic compounds are constructed from captodative dienophiles with exclusive regioselectivity. 100% biorenewable dimethyl terephthalate (DMT) from methyl coumalate and methyl pyruvate is achieved in a one-pot, Diels-Alder/decarboxylation/elimination sequence in nearly quantitative yield. The DMT system is solvent-free and purification is accomplished through recrystallization. DMT hydrolysis reveals the co-monomer terephthalic acid (TPA) as a bio-based drop-in replacement for the polymer industry, avoiding harsh oxidation and petrochemicals. the Partner Organisations 2014.
THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
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Paragraph 00224, (2014/11/13)
The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
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Page/Page column 62, (2012/02/01)
This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.