- Fused ring compounds as FGFR4 inhibitors
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The heart toxicity is low. High selectivity as FGFR4 inhibitor fused ring compounds, pharmaceutical compositions containing said compounds, useful intermediates and for preparing said compounds, and methods of treating cell proliferative diseases such as cancer using the compounds of the present invention.
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Paragraph 0465-0470
(2021/10/27)
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- IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
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The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
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Paragraph 0734
(2019/10/17)
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- SOMATOSTATIN MODULATORS AND USES THEREOF
-
Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
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Paragraph 00263
(2018/10/19)
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- ARYL LACTAM KINASE INHIBITORS
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The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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-
-
- Aryl vinyllactam serinekinase inhibitor
-
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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-
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- ARYL ETHER-BASE KINASE INHIBITORS
-
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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Page/Page column 75; 76
(2015/03/28)
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- Aryl Ether-Base Kinase Inhibitors
-
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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Paragraph 0168
(2013/09/26)
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- CYTOMEGALOVIRUS INHIBITOR COMPOUNDS
-
Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
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Page/Page column 25; 26
(2013/10/22)
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- NAPHTHYRIDINONE DERIVATIVES AS INHIBITORS OF CYTOMEGALOVIRUS DNA POLYMERASE
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Compounds of Formula (I) wherein n, m, R1, R2, R3, R4, R5 and R6 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
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Page/Page column 45
(2013/10/22)
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- NOVEL BICYCLIC UREA COMPOUNDS
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The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
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Page/Page column 12
(2012/07/31)
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- Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists
-
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antago
- Blum, Charles A.,Caldwell, Timothy,Zheng, Xiaozhang,Bakthavatchalam, Rajagopal,Capitosti, Scott,Brielmann, Harry,De Lombaert, Stéphane,Kershaw, Mark T.,Matson, David,Krause, James E.,Cortright, Daniel,Crandall, Marci,Martin, William J.,Murphy, Beth Ann,Boyce, Susan,Jones, A. Brian,Mason, Glenn,Rycroft, Wayne,Perrett, Helen,Conley, Rachael,Burnaby-Davies, Nicola,Chenard, Bertrand L.,Hodgetts, Kevin J.
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experimental part
p. 3330 - 3348
(2010/09/07)
-
- Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4- ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the met kinase superfamily
-
Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)- 1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analogue 10 demonstrated complete tumor stasis in a Met- dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials.
- Schroeder, Gretchen M.,An, Yongmi,Cai, Zhen-Wei,Chen, Xiao-Tao,Clark, Cheryl,Cornelius, Lyndon A. M.,Dai, Jun,Gullo-Brown, Johnni,Gupta, Ashok,Henley, Benjamin,Hunt, John T.,Jeyaseelan, Robert,Kamath, Amrita,Kim, Kyoung,Lippy, Jonathan,Lombardo, Louis J.,Manne, Veeraswamy,Oppenheimer, Simone,Sack, John S.,Schmidt, Robert J.,Shen, Guoxiang,Stefanski, Kevin,Tokarski, John S.,Trainor, George L.,Wautlet, Barri S.,Wei, Donna,Williams, David K.,Zhang, Yingru,Zhang, Yueping,Fargnoli, Joseph,Borzilleri, Robert M.
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supporting information; experimental part
p. 1251 - 1254
(2009/12/07)
-
- HETEROARYL SUBSTITUTED QUINOLIN-4-YLAMINE ANALOGUES
-
Heteroaryl substituted quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
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Page/Page column 51
(2008/06/13)
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- SUBSTITUTED QUINOLIN-4-YLAMINE ANALOGUES
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Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor
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Page/Page column 41; 86-87
(2008/06/13)
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