389890-42-0Relevant articles and documents
Novel CDK inhibitory compounds, preparation method thereof, pharmaceutical composition for use in preventing or treating CDK relating diseases containing the same as an active ingredient
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, (2018/10/24)
The present invention relates to a novel CDK inhibitory compound, a method for manufacturing the same, and a pharmaceutical composition for preventing or treating a CDK-related disease containing the compound as an active ingredient. The novel CDK inhibit
ISOXAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF PULMONARY DISEASES AND DISORDERS
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, (2017/03/21)
The present disclosure features disclosed method of treating disorders such as COPD, bronchitis and/or asthma using disclosed compounds, optionally together with one or more additional active agents. Contemplated methods include administrating orally or by inhalation to a patient one or more disclosed compounds.
INHIBITORS OF THE TEC KINASE ENZYME FAMILY
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Page/Page column 56, (2016/12/22)
The present invention relates to a novel family of kinases inhibitors. Compounds of this class have been found to have inhibitory activity against members of the TEC kinase family, particularly BTK. The present invention is directed to a compound of Formula I or pharmaceutically acceptable salt, solvate, solvate of salt, stereoisomer, tautomer, isotope, prodrug, complex or biologically active metabolite thereof, for use in therapy.
DERIVATIVES OF 3-HETEROARYLISOXAZOL-5-CARBOXYLIC AMIDE USEFUL FOR THE TREATMENT OF INTER ALIA CYSTIC FIBROSIS
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, (2016/07/27)
The present disclosure is based, in part, on the discovery that disclosed compounds can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY
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, (2016/11/07)
The present disclosure features compounds such as those having the Formulae (Ila), (lIb), (lIc), (Ild), (IlIa), and (Illb), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (Ila), (lIb), (lIc), (lId), (IlIa), or (Illb).
Highly potent HCV NS4B inhibitors with activity against multiple genotypes
Phillips, Barton,Cai, Ruby,Delaney, William,Du, Zhimin,Ji, Mingzhe,Jin, Haolun,Lee, Johnny,Li, Jiayao,Niedziela-Majka, Anita,Mish, Michael,Pyun, Hyung-Jung,Saugier, Joe,Tirunagari, Neeraj,Wang, Jianhong,Yang, Huiling,Wu, Qiaoyin,Sheng, Chris,Zonte, Catalin
supporting information, p. 2161 - 2166 (2014/04/03)
The exploration of novel inhibitors of the HCV NS4B protein that are based on a 2-oxadiazoloquinoline scaffold is described. Optimization to incorporate activity across genotypes led to a potent new series with broad activity, of which inhibitor 1 displayed the following EC50 values: 1a, 0.08 nM; 1b, 0.10 nM; 2a, 3 nM; 2b, 0.6 nM, 3a, 3.7 nM; 4a, 0.9 nM; 6a, 3.1 nM.
Cyclobutane-derived diamines: Synthesis and molecular structure
Radchenko, Dmytro S.,Pavlenko, Sergiy O.,Grygorenko, Oleksandr O.,Volochnyuk, Dmitriy M.,Shishkina, Svitlana V.,Shishkin, Oleg V.,Komarov, Igor V.
experimental part, p. 5941 - 5952 (2010/11/04)
Cyclobutane diamines (i.e., cis- and trans-1,3-diaminocyclobutane, 6-amino-3-azaspiro[3.3]heptane, and 3,6-diaminospiro[3.3]heptane) are considered as promising sterically constrained diamine building blocks for drug discovery. An approach to the syntheses of their Boc-monoprotected derivatives has been developed aimed at the preparation of multigram amounts of the compounds. These novel synthetic schemes exploit classical malonate alkylation chemistry for the construction of cyclobutane rings. The conformational preferences of the cyclobutane diamine derivatives have been evaluated by X-ray diffraction and compared with the literature data on sterically constrained diamines, which are among the constituents of commercially available drugs.
NEW PLEUROMUTILIN DERIVATIVE AND ITS USE
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Page/Page column 13, (2010/11/27)
The invention is directed to the L-tartrate salt of trans-3-aminocyclobutyl (lS,2R,3S,4S:,6R,7R,8R-,14R)-4-ethenyl-3-hydroxy-2,4,7, 14-tetramethyl-9- oxotricyclo[5.4.3.01,8]tetradec-6-yl imidodicarbonate (Compound IA.) Compound IA is useful for the treatment of a variety of diseases and conditions, such as respiratory tract and skin and skin structure infections. Accordingly, the invention is further directed to pharmaceutical compositions comprising Compound IA. The invention is still further directed to methods of treating respiratory tract and skin and skin structure infections using Compound IA or a pharmaceutical composition comprising Compound IA.