cas 79456-34-1, 2-Amino-5-bromo-3-(trifluoromethyl)pyridine

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Transition metal-free direct C–H trifluoromethyltion of (hetero)arenes with Togni's reagent
A new transition-metal-free direct C–H trifluoromethylation reaction of (hetero)arenes with Togni's reagent was developed. This transformation proceeded smoothly under mild conditions and exhibited good tolerance of many synthetically relevant functional groups. It provided an alternative approach for the synthesis of trifluoromethylated (hetero)arenes.
Chen, Xiaoyu,Ding, Licheng,Li, Linlin,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
supporting information

(2019/12/30)

Synthesis method and applications of polysubstituted 2-aminopyridine derivative
The invention belongs to the field of organic synthetic chemistry, and relates to a synthetic method and applications of a polysubstituted 2-aminopyridine derivative. According to the method, a 1,2,3-triazine compound and a cyanomethyl compound are used as substrates and are subjected to a one-step cycloaddition reaction under an alkaline condition to obtain a polysubstituted 2-aminopyridine derivative, wherein the reaction does not involve in danger and control reagents and medicines, and a simple, safe, efficient and environment-friendly strategy is provided for synthesizing the polysubstituted 2-aminopyridine derivative. According to the present invention, the obtained product is subjected to further derivatization, such that the active molecule or the drug molecule containing the 2-aminopyridine structure can be synthesized, such as active molecule SC-53606, drug molecule apatinib and nevirapine.
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Paragraph 0060-0062; 0063; 0064

(2020/04/22)

Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834
A practical fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834 (1) was developed. The key C[sbnd]C bond was constructed via a Suzuki–Miyaura cross-coupling of iodopyrazole 2 and pyridine boronic ester 3 to afford ketone 12. Su
Angelaud, Rémy,Beaudry, Danial,Carrera, Diane E.,Gosselin, Francis,Huestis, Malcolm P.,Liu, Wendy,Siu, Michael,Xu, Jie
(2020/10/02)

HETEROCYCLIC COMPOUNDS AND THEIR USE FOR TREATMENT OF HELMINTHIC INFECTIONS AND DISEASES
Provided herein are Heterocyclic compounds of formula (I): and pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein W, X, Y, R1, R2, and RN are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound, and methods for treating or preventing animal and human filarial worm infections and diseases.
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Paragraph 00249

(2020/11/03)

SUBSTITUTED THIAZOLO-PYRIDINE COMPOUNDS AS MALT1 INHIBITORS
Disclosed are compounds of the general formula (I), wherein R1-R3 are as defined herein, for use as MALT1 inhibitors in the treatment of autoimmune and inflammatory diseases or disorders. Methods of synthesizing the compounds are also disclosed. Also disc
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Page/Page column 314-315

(2018/02/28)

2-MORPHOLIN-4,6-DISUBSTITUTED PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
Disclosed is a 2-morpholin-4,6-disubstituted pyrimidine derivative as shown in formula (I) below, and a pharmaceutically acceptable salt, solvate, stereoisomer or prodrug thereof, and a pharmaceutical composition thereof and a use thereof, wherein the definition of each group is as shown in the description. The compound has a PI3K kinase inhibition activity, and has a relatively high inhibitive ability and a low cytotoxicity against PIK3CA mutant breast cancer cell strains T47D and MCF-7.
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Paragraph 0092; 0109

(2017/11/11)

As the NS4B inhibitor benzofuran analogs (by machine translation)
The present invention discloses a kind of as NS4B benzofuran analogue inhibitors, in particular to the formula (I) below or a pharmaceutically acceptable salt thereof. (by machine translation)
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Paragraph 0364; 0366; 0367; 0368; 0369

(2016/10/31)

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19
The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putative oncogene. Here we report the discovery of 109 (CCT251921), a potent, selective, and orally bioavailable inhibitor of CDK8 with equipotent affinity for CDK19. We describe a structure-based design approach leading to the discovery of a 3,4,5-trisubstituted-2-aminopyridine series and present the application of physicochemical property analyses to successfully reduce in vivo metabolic clearance, minimize transporter-mediated biliary elimination while maintaining acceptable aqueous solubility. Compound 109 affords the optimal compromise of in vitro biochemical, pharmacokinetic, and physicochemical properties and is suitable for progression to animal models of cancer.
Mallinger, Aurélie,Schiemann, Kai,Rink, Christian,Stieber, Frank,Calderini, Michel,Crumpler, Simon,Stubbs, Mark,Adeniji-Popoola, Olajumoke,Poeschke, Oliver,Busch, Michael,Czodrowski, Paul,Musil, Djordje,Schwarz, Daniel,Ortiz-Ruiz, Maria-Jesus,Schneider, Richard,Thai, Ching,Valenti, Melanie,De Haven Brandon, Alexis,Burke, Rosemary,Workman, Paul,Dale, Trevor,Wienke, Dirk,Clarke, Paul A.,Esdar, Christina,Raynaud, Florence I.,Eccles, Suzanne A.,Rohdich, Felix,Blagg, Julian
p. 1078 - 1101
(2016/02/23)

multi-links class PI3K inhibitors (by machine translation)
The invention belongs to the field of medical technology, in particular of formula (I) shown in multi-links class of PI3K inhibitors, its stereoisomers or its pharmaceutically acceptable salt thereof, wherein the R 1, R 2, R 3, R 4 or R 5 as defined in the specification; the invention also relates to methods of preparing such compounds, pharmaceutical compositions of these compounds in the preparation and treatment and/or prevention of proliferative diseases of the use of the medicament. (by machine translation)
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Paragraph 0454; 0455; 0456

(2016/10/09)

HETEROARYL SUBSTITUTED HETEROCYCLYL SULFONES
The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 87; 88

(2015/11/09)

PROCESS FOR THE PREPARATION OF SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE COMPOUNDS, INTERMEDIATES AND POLYMORPHS THEREOF
The present invention relates to a process for preparation of substituted imidazo[4,5- c]quinoline compounds (the compounds of formula I as described) and intermediates thereof. The present invention also relates to polymorphs of a compound encompassed in the compound of formula I and their use in the treatment of proliferative disorders, particularly cancers.
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Page/Page column 36-37

(2015/12/08)

Design, synthesis, and biological evaluation of novel imidazo[1,2-a]pyridine derivatives as potent c-met inhibitors
A series of imidazo[1,2-a]pyridine derivatives against c-Met was designed by means of bioisosteric replacement. In this study, a selective, potent c-Met inhibitor, 22e was identified, with IC50 values of 3.9 nM against c-Met kinase and 45.0 nM
Li, Chunpu,Ai, Jing,Zhang, Dengyou,Peng, Xia,Chen, Xi,Gao, Zhiwei,Su, Yi,Zhu, Wei,Ji, Yinchun,Chen, Xiaoyan,Geng, Meiyu,Liu, Hong
supporting information
p. 507 - 512
(2015/05/27)

Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K
PI3 kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration and differentiation. The PI3 Kinase pathway is often de-regulated in cancer through PI3Kα overexpression, gene amplification, mutations and PTEN p
Pecchi, Sabina,Ni, Zhi-Jie,Han, Wooseok,Smith, Aaron,Lan, Jiong,Burger, Matthew,Merritt, Hanne,Wiesmann, Marion,Chan, John,Kaufman, Susan,Knapp, Mark S.,Janssen, Johanna,Huh, Kay,Voliva, Charles F.
supporting information
p. 4652 - 4656
(2013/08/23)

OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION FOR COMBINATION THERAPY
The present invention relates to combination therapy using compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein and an additional pharmaceutically active agent. The invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations in the treatment of various diseases and disorders.
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Paragraph 0278; 0279

(2013/08/14)

SUBSTITUTED IMIDAZOQUINOLINE DERIVATIVES AS KINASE INHIBITORS
The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R1 R2, R3, R4, R5, R6 and R7 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of formula (I), and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammatory diseases and angiogenesis related disorders.
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Page/Page column 49

(2012/02/02)

OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 135

(2012/03/11)

BIARYL COMPOUNDS AND METHODS OF USE THEREOF
Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
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Page/Page column 214

(2011/04/13)

PIPERAZINYL ANTIVIRAL AGENTS
Provided are compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).
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Page/Page column 142

(2011/04/25)

PI3K/M TOR INHIBITORS
The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula (I): wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; meth
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Page/Page column 147

(2010/04/03)

PIPERIDINYL CYCLIC AMIDO ANTIVIRAL AGENTS
Provided are compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).
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Page/Page column 79

(2010/08/18)

1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES
The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c] quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H- imidazo[4,5-c] quinofinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c] quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H- imidazo[4,5-c] quinolinone derivatives; and a process for the preparation of the novel 1H- imidazo[4,5-c] quinolinone derivatives.
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Page/Page column 135

(2010/12/29)

1H-IMIDAZO[4, 5-c]QUINOLINONE COMPOUNDS, USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
The invention relates to the use of 1 H-imidazo[4,5-c]quinolinone compounds and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1 H-imidazo[4,5-c]quinolinone compounds for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1 H-imidazo[4,5-c]quinolinone compounds to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1 H-imidazo[4,5-c]quinolinone compounds, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H-imidazo[4,5-c]quinolinone compounds; and a process for the preparation of the novel 1 H-imidazo[4,5-c]quinolinone compounds.
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Page/Page column 102

(2010/12/29)

CERTAIN NITROGEN CONTAINING BICYCLIC CHEMICAL ENTITIES FOR TREATING VIRAL INFECTIONS
Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).
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Page/Page column 196-197

(2009/04/25)

2,4-SUBSTITUTED QUINAZOLINES AS LIPID KINASE INHIBITORS
The invention relates to compounds of the formula (I), which are appropriate for the treatment of kinase, e.g. PI3K-related, diseases, such as proliferative diseases, inflammatory diseases, obstructive airways disorders and transplantation related disease
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Page/Page column 69

(2008/06/13)

SUBSTITUTED IMIDAZOPYRIDAZINES AND PYRROLOPYRIMIDINES AS LIPID KINASE INHIBITORS
The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.
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Page/Page column 85

(2009/01/20)

SUBSTITUTED IMIDAZOPYRIDAZINES AS PI3K LIPID KINASE INHIBITORS
The invention relates to novel compounds of formula (I), as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.
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Page/Page column 89

(2009/01/20)

Novel compounds as metabotropic glutamate receptor antagonists
The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.
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Page/Page column 18

(2008/06/13)

PYRAZOLO [3, 4-D] PYRIMIDINE DERIVATIVES USEFUL TO TREAT RESPIRATORY DISORDERS
The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R1-R3 and Y are defined in the description, and its use in the treatment of disorders in which pi3 kinase is imp
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Page/Page column 68

(2008/06/13)