cas 105391-70-6, 5-BROMO-6-FLUORO-1H-INDAZOLE

Articles about 105391-70-6Total 18 be found

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Compounds and their use in treatment on hepatitis B
The invention provides compounds, a pharmaceutical composition containing the compounds and an application of the compounds. The compound is a compound shown in a formula (I) or a stereoisomer, a tautomer, nitric oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compound shown in the formula (I). The compound provided by the invention can interfere with the shell assembly process of hepatitis B virus, thereby inhibiting hepatitis B virus replication. Moreover, the compound has good absorption, relatively high biological activity and availability and low toxicity, particularly has relatively strong stability in vivo, is not easy to decompose and has long drug effect time, so that an effect of treating hepatitis B is achieved and the compound has a goodapplication prospect.
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(2020/07/15)

3-(1H-PYRROLO[2,3-B]PYRIDIN-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
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(2017/02/28)

3-(1H-PYRROLO[2,3-C]PYRIDIN-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
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(2017/03/08)

3-(1H-PYRROLO[3,2-C]PYRIDIN-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
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(2017/02/28)

3-(1H-INDOL-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
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(2017/02/28)

2-(1H-INDAZOL-3-YL)-1H-IMIDAZO[4,5-C]PYRIDINE AND THERAPEUTIC USES THEREOF
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
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(2016/04/09)

2-(1H-INDAZOL-3-YL)-3H-IMIDAZO[4,5-B]PYRIDINE AND THERAPEUTIC USES THEREOF
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
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(2016/04/22)

TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
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(2016/12/22)

Optimization of potency and pharmacokinetics of tricyclic indole derived inhibitors of HCV NS5B polymerase. Identification of ester prodrugs with improved oral pharmacokinetics
HCV infections are the leading causes for hepatocellular carcinoma and liver transplantation in the United States. Recent advances in drug discovery have identified direct acting antivirals which have significantly improved cure rates in patients. Current
Venkatraman, Srikanth,Velazquez, Francisco,Gavalas, Stephen,Wu, Wanli,Chen, Kevin X.,Nair, Anilkumar G.,Bennett, Frank,Huang, Yuhua,Pinto, Patrick,Jiang, Yueheng,Selyutin, Oleg,Vibulbhan, Bancha,Zeng, Qingbei,Lesburg, Charles,Duca, Jose,Heimark, Larry,Huang, Hsueh-Cheng,Agrawal, Sony,Jiang, Chuan-Kui,Ferrari, Eric,Li, Cheng,Kozlowski, Joseph,Rosenblum, Stuart,Shih, Neng-Yang,George Njoroge
p. 447 - 458
(2014/01/17)

Discovery, optimization, and biological evaluation of 5-(2- (trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists
A high throughput screening campaign identified 5-(2-chlorophenyl)indazole compound 4 as an antagonist of the transient receptor potential A1 (TRPA1) ion channel with IC50 = 1.23 μM. Hit to lead medicinal chemistry optimization established the SAR around the indazole ring system, demonstrating that a trifluoromethyl group at the 2-position of the phenyl ring in combination with various substituents at the 6-position of the indazole ring greatly contributed to improvements in vitro activity. Further lead optimization resulted in the identification of compound 31, a potent and selective antagonist of TRPA1 in vitro (IC50 = 0.015 μM), which has moderate oral bioavailability in rodents and demonstrates robust activity in vivo in several rodent models of inflammatory pain.
Rooney, Lisa,Vidal, Agnès,D'Souza, Anne-Marie,Devereux, Nick,Masick, Brian,Boissel, Valerie,West, Ryan,Head, Victoria,Stringer, Rowan,Lao, Jianmin,Petrus, Matt J.,Patapoutian, Ardem,Nash, Mark,Stoakley, Natalie,Panesar, Moh,Verkuyl, J. Martin,Schumacher, Andrew M.,Petrassi, H. Michael,Tully, David C.
supporting information
p. 5129 - 5140
(2014/07/08)

OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
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Page/Page column 23

(2012/11/13)

BICYCLIC HETEROARYL COMPOUNDS AS GPR119 RECEPTOR AGONISTS
The present invention provides a new class of bicyclic heteroaryl compounds represented by Formula (I), pharmaceutical compositions containing these compounds, and their use for modulating the activity of GPR119 in the treatment of metabolic disorders and complications thereof, as well as methods for the treatment of the metabolic disorders and complications thereof.
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Page/Page column 55

(2012/08/27)

OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptor are disclosed.
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Page/Page column 17; 39

(2011/07/07)

TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF
The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
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Page/Page column 179-180

(2009/04/25)

2,3-SUBSTITUTED AZAINDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS
The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3-Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted Azaindole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
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Page/Page column 119

(2009/04/25)

SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF
The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
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Page/Page column 194

(2009/04/25)

TRICYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF
The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient
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Page/Page column 103

(2010/01/07)

THIADIAZOLE COMPOUNDS AND METHODS OF USE
The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated
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Page/Page column 37-38

(2010/11/08)