cas 868171-67-9, 3-Pyridinecarboxylic acid, 1-(4-fluorophenyl)-1,2-dihydro-2-oxo-

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DERIVATIVES OF 2-OXO-N-(4-(PYRIMIDIN-4-YLOXY/THIO)PHENYL)-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE FOR USE AS PROTEIN KINASE INHIBITORS FOR THERAPY
2-oxo-N-(4-(pyrimidin-4-yloxy/thio)phenyl)-1,2-dihydropyridine-3-carboxamide derivatives are disclosed for use in the prevention and/or treatment of proliferative cell diseases and conditions including cancers. The compounds are considered to be capable of inhibiting cell proliferation and cause cancer cell apoptosis by inhibiting the activity of receptor tyrosine kinases (RTKs) such as TYRO3,AXL,MER and/or MET. The compounds have the general structure (I) shown below:
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(2022/02/06)

NAPHTHYRIDINE COMPOUNDS AS INHIBITORS OF MER TYROSINE KINASE AND AXL TYROSINE KINASE
The present invention relates to compounds of Formula (I) that function as inhibitors of MerTK activity, to processes for the preparation of such compounds, to pharmaceutical compositions comprising them and to their use in the treatment of proliferative
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Paragraph 00385

(2021/10/11)

Aromatic ring dioxane quinazoline or quinoline compound, composition and application of aromatic ring dioxane quinazoline or quinoline compound
The invention relates to a novel compound serving as an inhibitor of kinase such as TRK, c-MET, AXL, MER and/or VEGFR2, a composition and application of the novel compound. Specifically, the inventionprovides a compound (as shown in formula (1)) or an isomer, a solvate, a hydrate, a pharmaceutically acceptable salt and a prodrug thereof, and a pharmaceutical composition containing the compound, wherein the compound has the activity of strongly inhibiting kinase such as TRK, c-MET, AXL, MER and/or VEGFR2. The invention further discloses application of the compound or the pharmaceutical composition in preparation of a medicine. The medicine is used for treating autoimmune diseases or cancers.
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(2020/06/09)

THIENOPYRIDINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Since a thienopyridine derivative compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof of the present invention has an excellent effect of inhibiting protein kinase activity, a pharmaceutical composition comprising the same can be usefully used for preventing or treating diseases related to protein kinase activity.COPYRIGHT KIPO 2020
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Paragraph 0171; 0180-0183; 0220-0223

(2019/10/29)

THIENOPYRIDINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
A thienopyridine derivative compound represented by Formula 1 or pharmaceutically acceptable salts thereof have an excellent inhibitory effect on protein kinase activity, and accordingly, pharmaceutical compositions comprising same can be usefully used for the prevention or treatment of a disease associated with the activity of a protein kinase.
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Page/Page column 25-26; 29

(2019/10/15)

PYRIDO-AZAHETERECYDIC COMPOUND AND PREPARATION METHOD AND USE THEREOF
The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.
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(2018/09/21)

Indole-based small molecular C-MET inhibitor
The invention belongs to the technical field of medicines, and provides indole compounds for treating lung cancer, breast cancer, kidney cancer, pancreatic cancer, colorectal cancer, stomach cancer and other cancers.
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(2017/11/18)

PYRROLOTRIAZINE COMPOUNDS AS TAM INHIBITORS
This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
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(2017/10/13)

PROTEIN KINASE INHIBITOR CONTAINING PYRROLOPYRIDAZINE DERIVATIVE
The present invention relates to a pyrrolopyridazine derivative represented by Formula 1 of the detailed description, or a pharmaceutically acceptable salt thereof. The compound according to the present invention and a pharmaceutically acceptable salt the
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(2016/08/17)

Protein kinase inhibitors comprising a pyrrolopyridazine derivative
The present invention relates to a pyrrolopyridazine derivative represented by chemical formula 1, or a pharmaceutically acceptable salt of the same. A compound according to the present invention and a pharmaceutically acceptable salt of the same can be u
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(2016/10/07)

Protein kinase inhibitors comprising a pyrrolopyridazine derivative
The present invention relates to a pyrrolopyridazine derivative represented by Formula 1 of the detailed description, or a pharmaceutically acceptable salt thereof. The compound according to the present invention and a pharmaceutically acceptable salt the
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Paragraph 0186-0188

(2016/11/21)

Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization
Starting from our previously identified novel c-Met kinase inhibitors bearing 1H-imidazo[4,5-h][1,6]naphthyridin-2(3H)-one scaffold, a global structural exploration was conducted to furnish an optimal binding motif for further development, directed by the
An, Xiao-De,Liu, Hongyan,Xu, Zhong-Liang,Jin, Yi,Peng, Xia,Yao, Ying-Ming,Geng, Meiyu,Long, Ya-Qiu
p. 708 - 716
(2015/01/30)

Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor
Bioisosteric replacement of acylureido moiety in 6-acylureido-3- pyrrolylmethylidene-2-oxoindoline derivatives resulted in a series of malonamido derivatives with indolin-2-one scaffold (11-14). Further conformational restrictions of the malonamido moiety led to 2-oxo-1,2-dihydropyridine (21-25) or a 4-oxo-1,4-dihydropyridine derivatives (31-36). 4-Oxo-1,4-dihydropyridine derivatives were more potent Aurora B inhibitors than their 2-oxo-1,2- dihydropyridine counterparts and demonstrated cytotoxicities against A549 and HepG2 cells in the submicromolar range. In A549 cells, 31h decreased phosphorylation of histone H3, triggered polyploidy, induced expression of pro-apoptotic Fas and FasL with subsequent activation of caspase 8, resulting into apoptosis. In a Huh7-xenograft mouse model, 31h demonstrated potent in vivo efficacy with a daily dose of 5 mg/kg.
Wang, Hsiao-Chun,Jagtap, Ajit Dhananjay,Chang, Pei-Teh,Liu, Jia-Rong,Liu, Chih-Peng,Tseng, Hsiang-Wen,Chen, Grace Shiahuy,Chern, Ji-Wang
p. 312 - 334
(2014/08/05)

NOVEL FUSED PYRIDINE DERIVATIVES USEFUL AS c-MET TYROSINE KINASE INHIBITORS
This invention relates to novel fused quinazoline derivatives of Formula I as c-Met inhibitors, their synthesis and uses for treating c-Met mediated disorders.
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(2014/01/17)

Inhibitors of the TAM subfamily of tyrosine kinases: Synthesis and biological evaluation
The TAM subfamily of Receptor Tyrosine Kinases (RTKs) contains three human proteins of therapeutical interest, Axl, Mer, and Tyro3. Our goal was to design a type II inhibitor specific for this family, i.e. able to interact with the allosteric pocket and with the hinge region of the kinase. We report the synthesis of several series of purine analogues of BMS-777607. The structural diversity of the designed inhibitors was expected to modify the interactions formed in the binding site and consequently to modulate their selectivity profiles. The most potent inhibitor 6g exhibits Kds of 39, 42, 65 and 200 nM against Axl, Mer, Met and Tyro3 respectively. Analysis of the affinity of 6g for active and inactive forms of Abl1, an RTK protein that does not belong to the TAM subfamily, together with the binding modes of 6g predicted by docking studies, indicates that 6g displays some selectivity for the TAM family and may act as a type II inhibitor. Crown Copyright
Suarez, Rosa M.,Chevot, Franciane,Cavagnino, Andrea,Saettel, Nicolas,Radvanyi, Francois,Piguel, Sandrine,Bernard-Pierrot, Isabelle,Stoven, Veronique,Legraverend, Michel
p. 2 - 25
(2013/04/23)

INDOLIN-2-ONE DERIVATIVES AS PROTEIN KINASE INHIBITORS
A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.
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(2013/11/05)

New aminopyrimidine derivatives as inhibitors of the TAM family
In this study, we describe the synthesis of new pyrimidine analogs of BMS-777607, a potent and selective inhibitor of Met kinase. Inhibition of Met and Axl remained high whereas inhibition of Tyro3 and Mer decreased to some extend. The preferential modera
Traoré, Ténin,Cavagnino, Andrea,Saettel, Nicolas,Radvanyi, Fran?ois,Piguel, Sandrine,Bernard-Pierrot, Isabelle,Stoven, Véronique,Legraverend, Michel
p. 789 - 801
(2013/12/04)

Discovery of 3H-Imidazo[4,5-b]pyridines as Potent c-Met Kinase Inhibitors: Design, Synthesis, and Biological Evaluation
To identify novel c-Met inhibitors, sequences and crystal structures of the human kinome were analyzed to find interesting hinge binders that have been underexplored within the tyrosine kinase subfamily. Through this study, the imidazolopyridine ring was selected as a novel c-Met hinge-binding inhibitor scaffold. A series of derivatives was prepared, and the structure-activity relationships were studied. Among these, one compound in particular showed excellent activities in enzymatic and cellular assays, good invitro metabolic stability, and favorable pharmacokinetic parameters. When administered orally, the compound inhibited tumor growth in an NIH-3T3/TPR-Met xenograft model and did not show adverse effects on body weight. The present work not only conceptually demonstrates a new route for designing novel kinase inhibitors by using known structural information of ligand-hinge interactions but also provides a series of imidazolopyridine derivatives as potent c-Met inhibitors.
Chen, Danqi,Wang, Ying,Ma, Yuchi,Xiong, Bing,Ai, Jing,Chen, Yi,Geng, Meiyu,Shen, Jingkang
p. 1057 - 1070
(2012/07/31)

PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITES
Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
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(2011/11/30)

AMIDOPHENOXYINDAZOLES USEFUL AS INHIBITORS OF C-MET
The present invention provides amidophenoxyindazole compounds useful in the treatment of cancer.
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Page/Page column 17

(2010/02/17)

Discovery of pyrrolopyridine-pyridone based inhibitors of met kinase: Synthesis, X-ray crystallographic analysis, and biological activities
Conformationally constrained 2-pyridone analogue 2 is a potent Met kinase inhibitor with an IC50 value of 1.8 nM. Further SAR of the 2-pyridone based inhibitors of Met kinase led to potent 4-pyridone and pyridine N-oxide inhibitors such as 3 and 4. The X-ray crystallographic data of the inhibitor 2 bound to the ATP binding site of Met kinase protein provided insight into the binding modes of these inhibitors, and the SAR of this series of analogues was rationalized. Many of these analogues showed potent antiproliferative activities against the Met dependent GTL-16 gastric carcinoma cell line. Compound 2 also inhibited Flt-3 and VEGFR-2 kinases with IC50 values of 4 and 27 nM, respectively. It possesses a favorable pharmacokinetic profile in mice and demonstrates significant in vivo antitumor activity in the GTL-16 human gastric carcinoma xenograft model.
Kyoung, Soon Kim,Zhang, Liping,Schmidt, Robert,Cai, Zhen-Wei,Wei, Donna,Williams, David K.,Lombardo, Louis J.,Trainor, George L.,Xie, Dianlin,Zhang, Yaquan,An, Yongmi,Sack, John S.,Tokarski, John S.,Darienzo, Celia,Kamath, Amrita,Marathe, Punit,Zhang, Yueping,Lippy, Jonathan,Jeyaseelan Sr., Robert,Wautlet, Barri,Henley, Benjamin,Gullo-Brown, Johnni,Manne, Veeraswamy,Hunt, John T.,Fargnoli, Joseph,Borzilleri, Robert M.
experimental part
p. 5330 - 5341
(2009/07/01)

PYRIDONECARBOXAMIDE DERIVATIVES USEFUL IN TREATING HYPER-PROLIFERATIVE AND ANGIOGENESIS DISORDERS
Pyridonecarboxamide derivatives, pharmaceutical compositions which contain the same and methods for treating hyper-proliferative disorders and angiogenesis disorders using the same.
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Page/Page column 53-54

(2008/12/05)

Pyrrolotriazine kinase inhibitors
In general, the instant invention comprises compounds having Formulae I and II: including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and ot
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Page/Page column 16

(2008/06/13)

Met kinase inhibitors
The present invention is directed to compounds that are useful for treating cancer having one of the following Formulas:
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Page/Page column 15

(2010/11/26)

Fused heterocyclic compounds useful as kinase modulators
Compounds having the formula (1), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are usefuil as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, Z is N or CR3, and R1, R2, R3, X and Y are as defined herein.
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Page/Page column 62-63

(2010/11/26)

QUINOLINE COMPOUNDS AND METHODS OF USE
Compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. [ Formula I]
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Page/Page column 142

(2008/06/13)

Bicyclic heterocycles as kinase inhibitors
The compounds of the instant invention can be used as anticancer agents. More specifically, the invention comprises a compound having Formula I or II,
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Page/Page column 16

(2008/06/13)