16618-68-1Relevant academic research and scientific papers
TEAD INHIBITORS AND USES THEREOF
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Paragraph 00465; 00551, (2020/12/11)
The present invention provides compounds, compositions thereof, and methods of using the same.
M-di-substituted phenol compound as well as preparation method thereof and application of tubercle bacillus resistance
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Paragraph 0152, (2018/05/16)
The invention provides an m-di-substituted phenol compound with a general formula (I) as well as a preparation method and application thereof. The m-di-substituted phenol compound provided by the invention has a novel tubercle bacillus resistance drug parent nucleus structure and excellent tubercle bacillus resistance activity and especially has very strong inhibition activity on a drug-resistantvariant tubercle bacillus strain. The invention further provides the preparation method of the m-di-substituted phenol compound; the preparation method has the advantages that raw materials are cheapand easy to obtain, a high-toxicity and high-pollution reagent are not needed, reaction steps are simple and industrialized production can be realized; the m-di-substituted phenol compound has a goodmedicinal prospect.
Synthesis of 1,5-bifunctional organolithium reagents by a double directed ortho-metalation: Direct transformation of esters into 1,8-dimethoxy-acridinium salts
Fischer, Christian,Sparr, Christof
, p. 5486 - 5493 (2018/05/29)
The impact of electronic and steric factors on the selectivity of the electrophilic aromatic substitution amounts to several limitations in accessing specific substitution patterns. Nucleophiles generated by directed metalation represent an effective alte
Indole and quinoline derivatives and its preparation method and application
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Paragraph 0074; 0075, (2017/02/28)
The invention provides an indoloquinoline derivative, a preparation method and application thereof in preparing antitumor drugs and antiviral drugs. The chemical structure of the indoloquinoline derivative is shown as a formula I. Experiments show that a partly-boric-acid-modified indoloquinoline derivative and a non-boric-acid-modified indoloquinoline derivative have strong inhibition effect on various tumor cell strains, thereby being capable of being used for preparation of the antitumor drugs, and have strong antiviral activity, thereby being capable of being used for preparation of the antiviral drugs.
Metal-Free Reduction of Aromatic Nitro Compounds to Aromatic Amines with B2pin2 in Isopropanol
Lu, Hongtao,Geng, Zhiyue,Li, Jingya,Zou, Dapeng,Wu, Yusheng,Wu, Yangjie
supporting information, p. 2774 - 2776 (2016/06/15)
A metal-free reduction of aromatic nitro compounds to the corresponding amines has been achieved by a combination of B2pin2 and KOtBu in isopropanol. A series of nitro compounds containing various reducible functional groups were chemoselectively reduced in good to excellent yields.
PROTEIN KINASE INHIBITORS
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Paragraph 0788, (2015/02/18)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against mycobacterium tuberculosis
Hameed P, Shahul,Patil, Vikas,Solapure, Suresh,Sharma, Umender,Madhavapeddi, Prashanti,Raichurkar, Anandkumar,Chinnapattu, Murugan,Manjrekar, Praveena,Shanbhag, Gajanan,Puttur, Jayashree,Shinde, Vikas,Menasinakai, Sreenivasaiah,Rudrapatana, Suresh,Achar, Vijayashree,Awasthy, Disha,Nandishaiah, Radha,Humnabadkar, Vaishali,Ghosh, Anirban,Narayan, Chandan,Ramya,Kaur, Parvinder,Sharma, Sreevalli,Werngren, Jim,Hoffner, Sven,Panduga, Vijender,Kumar, C. N. Naveen,Reddy, Jitendar,Kumar Kn, Mahesh,Ganguly, Samit,Bharath, Sowmya,Bheemarao, Ugarkar,Mukherjee, Kakoli,Arora, Uma,Gaonkar, Sheshagiri,Coulson, Michelle,Waterson, David,Sambandamurthy, Vasan K.,De Sousa, Sunita M.
supporting information, p. 4889 - 4905 (2014/07/07)
DNA gyrase is a clinically validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clinical value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase activity. The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown by their ability to inhibit the growth of fluoroquinolone-resistant Mtb. Biochemical studies demonstrated this class to exert its action via single-strand cleavage rather than double-strand cleavage, as seen with fluoroquinolones. The compounds are highly bactericidal against extracellular as well as intracellular Mtb. Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability. Compounds from this series are efficacious in various murine models of tuberculosis.
3-Amino-1-arylpropyl indoles and aza-substituted indoles and uses thereof
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Page/Page column 79, (2008/06/13)
The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
