912846-63-0Relevant academic research and scientific papers
2,4-disubstituted pyrimidine derivative as well as preparation method and application thereof
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Paragraph 0173-0178, (2021/01/11)
The invention belongs to the field of chemical medicines, and particularly relates to a 2,4-disubstituted pyrimidine derivative as well as a preparation method and application thereof. The invention provides the 2,4-disubstituted pyrimidine derivative, wh
TRIAZOLOPHTHALAZINE COMPOUNDS, USE AS ANTI-HUMAN IMMUNODEFICIENCY VIRUS INHIBITORS OF HIV VIF-DEPENDENT DEGRADATION OF APOBEC3
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Paragraph 00448, (2019/07/17)
The present disclosure is concerned with triazolophthalazine compounds that are capable of inhibiting infection by the Human Immunodeficiency Virus (HIV) by inhibiting HIV Vif-dependent degradation of the APOBEC3 innate immune system. The present disclosu
ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0329; 0330; 0331, (2017/04/18)
An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.
Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
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Paragraph 0171; 0172; 0173, (2016/10/08)
The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs
Watson, Nigel S.,Adams, Carl,Belton, David,Brown, David,Burns-Kurtis, Cynthia L.,Chaudry, Laiq,Chan, Chuen,Convery, Máire A.,Davies, David E.,Exall, Anne M.,Harling, John D.,Irvine, Stephanie,Irving, Wendy R.,Kleanthous, Savvas,McLay, Iain M.,Pateman, Anthony J.,Patikis, Angela N.,Roethke, Theresa J.,Senger, Stefan,Stelman, Gary J.,Toomey, John R.,West, Robert I.,Whittaker, Caroline,Zhou, Ping,Young, Robert J.
scheme or table, p. 1588 - 1592 (2011/05/05)
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the form
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5- tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity
Smith, Brian M.,Smith, Jeffrey M.,Tsai, James H.,Schultz, Jeffrey A.,Gilson, Charles A.,Estrada, Scott A.,Chen, Rita R.,Park, Douglas M.,Prieto, Emily B.,Gallardo, Charlemagne S.,Sengupta, Dipanjan,Dosa, Peter I.,Covel, Jon A.,Ren, Albert,Webb, Robert R.,Beeley, Nigel R. A.,Martin, Michael,Morgan, Michael,Espitia, Stephen,Saldana, Hazel R.,Bjenning, Christina,Whelan, Kevin T.,Grottick, Andrew J.,Menzaghi, Frederique,Thomsen, William J.
, p. 305 - 313 (2008/09/19)
The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [3H]phosphoinositol turnover: 5-HT 2C = 8.1; 5-HT2A = 6.8; 5-HT2B = 6.1) and was potent in an acute in vivo rat food intake model upon oral administration (ED50 at 6 h = 18 mg/kg). Lorcaserin was further characterized in a single-dose pharmacokinetic study in rat (t1/2 = 3.7 h; F = 86%) and a 28-day model of weight gain in growing Sprague-Dawley rat (8.5% decrease in weight gain observed at 36 mg/kg b.i.d.). Lorcaserin was selected for further evaluation in clinical trials for the treatment of obesity.
3-SULFONYLAMINO-PYRROLIDINE-2-ONE DERIVATIVES AS FACTOR XA INHIBITORS
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Page/Page column 49, (2008/06/13)
The present invention provides at least one chemical entity chosen from compounds of formula (I) wherein: R1 represents a group selected from formula (II), (III), (IV), (V), (VI), (VII), each ring of which optionally contains a further heteroatom N, Z represents an optional substituent halogen, -C1-3alkyl or -NRaRb, alk represents alkylene or alkenylene, T represents S, O or NH; Ra and Rb independently represent hydrogen or -C1-3alkyl; R2 represents a group selected from formula (VIII), (IX), W, X and Y independently represent CH, C-R5 or N; R5 represents halogen or C1-3alkyl; V represents NR3, S or O; R3 represents hydrogen or C1-3alkyl; one of A1 and A2 represents N and the other represents CH; Each R4, R6, R7, R8, R9 independently represents hydrogen or C1-3alkyl; R10 represents hydrogen, -C1-6alkyl, -C1-3alkylCONRaRb, -C1-3alkylCO2C1-4alkyl, -CO2C1-4alkyl or -C1-3alkylCO2H; and pharmaceutically acceptable derivative(s) thereof. The invention also relates to processes for the preparation of compound(s) of formula (I), pharmaceutical compositions containing compound(s) of formula (I) and to the use of compound(s) of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
