- Pyrazolopyridine hydroxamic acid compound as well as preparation method and application thereof
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The invention relates to the technical field of chemical synthesis, in particular to a pyrazolopyridine hydroxamic acid compound as well as a preparation method and application thereof. The pyrazolopyridine hydroxamic acid compound comprises a compound as shown in a formula (1), an isomer thereof, and a hydrate thereof or a pharmaceutically acceptable salt thereof, wherein n is an integer, and R is any one of a substituted or unsubstituted aromatic ring group and a substituted alkyl group. The compound can well inhibit cancer cell proliferation, and then has an excellent treatment effect on tumors.
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- BETA-LACTAMASE INHIBITORS
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Described herein are compounds and compositions that modulate the activity of beta -lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
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Paragraph 0395
(2017/04/08)
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- INDAZOLES
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The invention provides novel substituted indazole compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
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Page/Page column 43
(2016/03/13)
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- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYSNTHESIS FOR BACTERIAL INFECTIONS
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The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections.
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Paragraph 0067; 0070
(2014/09/16)
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- A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway
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Reactivation of the wild-type p53 pathway is one key goal aimed at developing targeted therapeutics in the cancer research field. Although most p53 protein kinases form 'p53-activating' signals, there are few kinases whose action can contribute to the inhibition of p53, as Casein kinase 1 (CK1) and Checkpoint kinase 1 (CHK1). Here we report on a pyrazolo-pyridine analogue showing activity against both CK1 and CHK1 kinases that lead to p53 pathway stabilisation, thus having pharmacological similarities to the p53-activator Nutlin-3. These data demonstrate the emerging potential utility of multivalent kinase inhibitors.
- Huart, Anne-Sophie,Saxty, Barbara,Merritt, Andy,Nekulova, Marta,Lewis, Stephen,Huang, Yide,Vojtesek, Borivoj,Kettleborough, Catherine,Hupp, Ted R.
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p. 5578 - 5585
(2013/10/01)
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- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYNTHESIS FOR BACTERIAL INFECTIONS
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The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial Fab I and can be used for the treatment of Staphylococcal infections.
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Page/Page column 17
(2013/04/10)
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- Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors
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Two series of 3-aminopyrazole compounds including 24 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and 16 pyrazolo[3,4-b]pyridines were synthesized and evaluated against HCT116, A549, and A2780 tumor cell lines. Among them, three compounds were found to have the ideal anti-proliferative activities in vitro. Docking experiments showed that the novel pyrazolo[3,4-b]pyridines share the similar interaction mode with Aurora-A kinase as PHA739358.
- Shi, Jianyou,Xu, Guobin,Zhu, Wei,Ye, Haoyu,Yang, Shengyong,Luo, Youfu,Han, Jing,Yang, Jincheng,Li, Rui,Wei, Yuquan,Chen, Lijuan
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supporting information; experimental part
p. 4273 - 4278
(2010/09/04)
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- HETEROCYCLIC INHIBITORS OF c-MET AND USES THEREOF
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The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders
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Page/Page column 45
(2008/06/13)
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- AZAINDAZOLES USEFUL AS INHIBITORS OF KINASES
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The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. Formula (I):
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Page/Page column 54-55
(2008/06/13)
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- Pyrazolopyridines and pyrazolopyridazines as antidabetics
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The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclyl and the alkyl moieties may each independently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention includes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.
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Page/Page column 17
(2010/02/05)
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- 5-Aryl-pyrazolo[3,4-b]pyridines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)
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A novel series of pyrazolo[3,4-b]pyridines has been identified that are potent inhibitors of glycogen synthase kinase-3 (GSK-3).
- Witherington, Jason,Bordas, Vincent,Garland, Stephen L.,Hickey, Deirdre M. B.,Ife, Robert J.,Liddle, John,Saunders, Martin,Smith, David G.,Ward, Robert W.
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p. 1577 - 1580
(2007/10/03)
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