72982-21-9Relevant academic research and scientific papers
Controllable one-pot synthesis for scaffold diversity: Via visible-light photoredox-catalyzed Giese reaction and further transformation
Nam, Su Been,Khatun, Nilufa,Kang, Young Woo,Park, Boyoung Y.,Woo, Sang Kook
, p. 2873 - 2876 (2020/03/19)
This study presents a controllable one-pot synthesis for constructing valuable scaffolds (alcohols, 2,3-dihydrofurans, α-cyano-γ-butyrolactones, and γ-butyrolactones) via a visible-light photoredox-catalyzed Giese reaction and further transformation. This
PHARMACEUTICAL COMPOSITION AND APPLICATION REPLACING QUINOLONE DERIVATIVE, PHARMACEUTICAL ACCEPTABLE SALT, OR STEREOISOMER
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Paragraph 0197; 0198, (2018/07/06)
Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors
Tan, Li,Zhang, Zhang,Gao, Donglin,Luo, Jinfeng,Tu, Zheng-Chao,Li, Zhengqiu,Peng, Lijie,Ren, Xiaomei,Ding, Ke
supporting information, p. 6807 - 6825 (2016/08/05)
Axl is a new potential target for anticancer drug discovery. A series of 4-oxo-1,4-dihydroquinoline-3-carboxamides were designed and synthesized as highly potent Axl kinase inhibitors. One of the most promising compounds, 9im, tightly bound with Axl prote
Novel, Cyclically Substituted Furopyrimidine Derivatives and Use Thereof
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Page/Page column 22, (2011/06/19)
The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor
Coumar, Mohane Selvaraj,Tsai, Ming-Tsung,Chu, Chang-Ying,Uang, Biing-Jiun,Lin, Wen-Hsing,Chang, Chun-Yu,Chang, Teng-Yuan,Leou, Jiun-Shyang,Teng, Chi-Huang,Wu, Jian-Sung,Fang, Ming-Yu,Chen, Chun-Hwa,Hsu, John T.-A.,Wu, Su-Ying,Chao, Yu-Sheng,Hsieh, Hsing-Pang
experimental part, p. 255 - 267 (2010/12/18)
Herein we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compound library to select compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocy
Novel, Acyclically Substituted Furopyrimidine Derivatives and Use Thereof
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Page/Page column 10; 20, (2009/12/28)
The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
FURANOPYRIMIDINES
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Page/Page column 94, (2010/02/15)
The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).
FURANOPYRIMIDINE COMPOUNDS EFFECTIVE AS POTASSIUM CHANNEL INHIBITORS
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Page/Page column 22, (2010/02/15)
A compound of formula (I) wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, -CO2R7, CONR4R5 or halo; R3 is H, NR4R5, NC(O)R8, halo, trifluoromethyl, alkyl, nitrile or alkoxy; R4 and R5 may be the same or different, and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R4 and R5 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; X is O, S or NR6; R6 is H or alkyl; R7 is hydrogen, methyl or ethyl; R8 is methyl or ethyl; Ll is (CH2)n, where n is 1,2 or 3; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; together with pharmaceutically acceptable salts thereof. The use of these compounds as potassium channel inhibitors is also described.
Synthesis of new 2,4-diamino-7H-pyrrolo[2,3-d]pyrimidines via the Taylor ring transformation/ring annulation strategy
Rosowsky,Fu,Queener
, p. 1197 - 1202 (2007/10/03)
Selected examples 2,4-diamino-7H-pyrrolo[2,3-d]pyrimidines with a phenyl or benzyl group at the 5-position were synthesized as inhibitors of dihydrofolate reductase (DHFR) from Pneumocystis carinii and Toxoplasma gondii, two potentially life-threatening opportunistic pathogens associated with AIDS and other disorders of the immune system. Aldol condensation of paraformaldehyde with substituted benzaldehydes or with phenylacetaldehyde afforded α-hydroxyketones with a phenyl or benzyl group at the 4-position. Further reaction of the hydroxyketones with malononitrile afforded 2-aminofuran-3-carbonitriles, which upon heating with guanidine underwent ring transformation/ring annulation to produce 2,4-diamino-7H-pyrrolo[2,3-d]pyrimidines rather than 2,4-diaminofuro[2,3-d]pyrimidines. One of the target compounds obtained in this manner, 2,4-diamino-5-(3,4,5-trimethoxyphenyl)-7H-pyrrolo [2,3 -d]pyrimidine (1d), may be viewed as a conformationally restricted analogue of trimethoprim, an antimicrobial agent widely used in combination with a sulfa drug to treat P. carinii and T. gondii opportunistic infections in patients with AIDS. Compound 1d inhibited P. carinii and T. gondii DHFR with IC50 values of 8.3 and 14 μM, respectively. This potency was somewhat greater than that of trimethoprim. However, because this compound was also more potent than trimethoprim against mammalian (rat liver) DHFR rat liver it lacked species selectivity. The other 2,4-diamino-7H-pyrrolo[2,3-d]pyrimidines synthesized were neither potent nor selective.
Studies on Heterocyclic Enaminonitriles. VI. Synthesis of 2-Amino-3-cyano-4,5-dihydrofurans
Matsuda, Takumi,Yamagata, Kenji,Tomioka, Yukihiko,Yamazaki, Motoyoshi
, p. 937 - 943 (2007/10/02)
Malononitrile reacts with 2-chloroethanol and 1-chloro-2-propanol (or 2-methyloxirane) in the presence of sodium ethoxide to give 2-amino-3-cyano-4,5-dihydrofuran (Ia) and 2-amino-3-cyano-5-methyl-4,5-dihydrofuran (Ib), respectively.The reaction of malono
