- ROR[gamma] inhibitors, preparation method thereof and application of the ROR[gamma] inhibitors in medicine
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The present specification provides compounds of formula (I) shown in the specification: or a pharmaceutically acceptable salt thereof, a deuterated compound, a tautomer, a cis-trans-isomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or a mixtu
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Paragraph 0330-0331; 0336-0339
(2021/05/26)
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- INHIBITORS OF CYCLIN-DEPENDENT KINASES
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Provided herein are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
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Paragraph 00365
(2019/11/19)
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- NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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The present invention discloses compounds according to Formula (I), wherein R1, R3, R4, R5, L1, and Cy are as defined herein. The present invention also provides compounds, methods for the production of said compounds of the invention, pharmaceutical compositions comprising the same and their use in allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 and/or interferons. The present invention also methods for the prevention and/or treatment of the aforementioned diseases by administering a compound of the invention.
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Paragraph 0649
(2017/02/09)
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- 1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors with a Novel Monodentate Binding Interaction
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Herein we describe the identification of 4-{[1,2,4]triazolo[1,5-a]pyridin-5-yl}benzonitrile-based inhibitors of the hypoxia-inducible factor prolylhydroxylase domain-1 (PHD-1) enzyme. These inhibitors were shown to possess a novel binding mode by X-ray crystallography, in which the triazolo N1 atom coordinates in a hitherto unreported monodentate interaction with the active site Fe2+ ion, while the benzonitrile group accepts a hydrogen-bonding interaction from the side chain residue of Asn315. Further optimization led to potent PHD-1 inhibitors with good physicochemical and pharmacokinetic properties.
- Ahmed, Saleh,Ayscough, Andrew,Barker, Greg R.,Canning, Hannah E.,Davenport, Richard,Downham, Robert,Harrison, David,Jenkins, Kerry,Kinsella, Natasha,Livermore, David G.,Wright, Susanne,Ivetac, Anthony D.,Skene, Robert,Wilkens, Steven J.,Webster, Natalie A.,Hendrick, Alan G.
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supporting information
p. 5663 - 5672
(2017/07/22)
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- 2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors
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New non-nucleoside reverse transcriptase inhibitors (NNRTI), which are similar in structure to earlier described di(arylamino)pyrimidines but featuring a 2,6-di(arylamino)-3-fluoropyridine, 2,4-di(arylamino)-5-fluoropyrimidine, or 1,3-di(arylamino)-4-fluorobenzene moiety instead of a 2,4-disubstituted pyrimidine moiety, are reported. The short and practical synthesis of novel NNRTI relies on two sequential Pd-catalyzed aminations as the key steps. It is demonstrated through direct comparison with reference compounds that the presence of a fluorine atom increases the in vitro anti-HIV activity, both against the wild type virus and drug-resistant mutant strains.
- Sergeyev, Sergey,Yadav, Ashok Kumar,Franck, Philippe,Michiels, Johan,Lewi, Paul,Heeres, Jan,Vanham, Guido,Ari?n, Kevin K.,Vande Velde, Christophe M. L.,De Winter, Hans,Maes, Bert U. W.
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p. 1854 - 1868
(2016/03/22)
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- Efficient three-component synthesis of diversely substituted tetrahydro-1H-cyclopenta[c]quinolines
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The synthesis of highly functionalized substituted tetrahydro-1H-cyclopenta[c]quinoline (I) and its reduced derivatives hexahydro-1H-cyclopenta[c]quinolines (II) via Povarov reaction in high diastereoselectivity and high to moderate yields is described he
- Ni?o, Patricia,Caba, Marta,Aguilar, Nuria,Terricabras, Emma,Albericio, Fernando,Fernàndez, Joan-Carles
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p. 854 - 881
(2017/01/18)
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- Compound for treatment or prevention of breast cancer
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The invention discloses a compound for treatment or prevention of breast cancer, specifically a 2-phenyl benzoselenazole compound, its pharmaceutically acceptable salt and easily hydrolysable prodrug. The invention further discloses a pharmaceutical composition containing the compounds and use of the compound in preparation of drugs for treatment or prevention of breast cancer in mammals. The compound involved in the invention can effectively inhibit or reduce mammalian breast cancer cell growth or proliferation, at the same time, the compound has no inhibiting effect on the growth of partial test cells except for breast cancer cells and has good selectivity. The compound shows more obvious efficacy, high selectivity, low toxicity and small side effect. (formula of the compound).
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EPl receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EPl receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EPl receptor as well as to pharmaceutical compositions comprising them.
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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