262450-65-7Relevant academic research and scientific papers
NOVEL MACROCYCLIC DERIVATIVES, PROCESS FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
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Paragraph 0138-0140; 0479-0481, (2020/08/25)
Compound of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, X, Y and G are as defined in the description, and their use in the manufacture of medicaments.
DIHYDROBENZOFURAN AND INDEN ANALOGS AS CARDIAC SARCOMERE INHIBITORS
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Paragraph 0412, (2019/08/08)
Provided are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A, Z, B, R1, R2, R3, G1, G2, and G3 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt, thereof for use in methods of treatment heart diseases through cardiac sarcomere inhibtion.
Design and synthesis of novel meta-linked phenylglycine macrocyclic FVIIa inhibitors
Richter, Jeremy M.,Cheney, Daniel L.,Bates, J. Alex,Wei, Anzhi,Luettgen, Joseph M.,Rendina, Alan R.,Harper, Timothy M.,Narayanan, Rangaraj,Wong, Pancras C.,Seiffert, Dietmar,Wexler, Ruth R.,Priestley, E. Scott
supporting information, p. 67 - 72 (2017/12/12)
Two novel series of meta-linked phenylglycine-based macrocyclic FVIIa inhibitors have been designed to improve the rodent metabolic stability and PK observed with the precursor para-linked phenylglycine macrocycles. Through iterative structure-based design and optimization, the TF/ FVIIa Ki was improved to subnanomolar levels with good clotting activity, metabolic stability, and permeability.
CYCLIC AMINES AS BROMODOMAIN INHIBITORS
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Paragraph 0512, (2014/05/25)
The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
MACROCYCLIC FACTOR VIIA INHIBITORS
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Paragraph 00295, (2015/01/09)
The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Page/Page column 23, (2009/07/17)
Compounds of formula I, wherein R1, R2, R3, X1, X2 and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 16, (2009/01/20)
Compounds of formula I, wherein R1, R2, R3, R4, Ra, X, X1, and Y are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 21, (2008/12/08)
Compounds of formula I, wherein R1, R2, R3, R4, R5, X, Y, and Ar are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
Structure-based approach to the development of potent and selective inhibitors of dihydrofolate reductase from Cryptosporidium
Bolstad, David B.,Bolstad, Erin S. D.,Frey, Kathleen M.,Wright, Dennis L.,Anderson, Amy C.
experimental part, p. 6839 - 6852 (2009/11/30)
Cryptosporidiosis is an emerging infectious disease that can be life-threatening in an immune-compromised individual and causes gastrointestinal distress lasting up to 2 weeks in an immune-competent individual. There are few therapeutics available for eff
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 19, (2008/06/13)
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, X1 and X2 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
