- JAK inhibitor compound and application thereof
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The invention relates to a JAK inhibitor compound and application thereof. Specifically, the invention discloses a compound shown as a formula (G), or an isotope labeled compound, or an optical isomer, a geometrical isomer, a tautomer or an isomer mixture of the compound, or a pharmaceutically acceptable salt of the compound, or a prodrug of the compound, or a metabolite of the compound. The invention also relates to the medical application of the compound.
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Paragraph 0508; 0511; 0519-0521
(2020/09/12)
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- 2-AZABICYCLO HEXANE JAK INHIBITOR COMPOUND
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The invention provides a compound of formula 1 or a pharmaceutically-acceptable salt thereof, that is useful as a JAK inhibitor. The invention also provides pharmaceutical compositions comprising the compound, methods of using the compound to treat diseas
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Paragraph 0183
(2020/05/14)
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- 3-formyl-1H-substituted indazole and preparation method thereof
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The embodiment of the invention discloses 3-formyl-1H-substituted indazole and a preparation method thereof. The method comprises the step of taking 2-nitro-substituted toluene as a raw material to prepare a compound in a formula (VI). The method takes the 2-nitro-substituted toluene as the raw material to prepare the 3-formyl-1H-substituted indazole. The raw material used by the preparation method is cheap and easy to get; a product with relatively high purity can be obtained without column chromatography separation and purification; the method can be well applied to practical production andapplication. Further, reaction conditions required by a whole preparation process are mild; the use of reagents with strong reducibility or strong oxidability is not involved; the method is suitable for industrial production.
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Paragraph 0069-0074
(2019/10/01)
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- An optimized procedure for direct access to 1: H -indazole-3-carboxaldehyde derivatives by nitrosation of indoles
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Indazole derivatives are currently drawing more and more attention in medicinal chemistry as kinase inhibitors. 1H-indazole-3-carboxaldehydes are key intermediates to access to a variety of polyfunctionalized 3-substituted indazoles. We report here a general access to this motif, based on the nitrosation of indoles in a slightly acidic environment. These very mild conditions allow the conversion of both electron-rich and electron-deficient indoles into 1H-indazole-3-carboxaldehydes.
- Chevalier, Arnaud,Ouahrouch, Abdelaaziz,Arnaud, Alexandre,Gallavardin, Thibault,Franck, Xavier
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p. 13121 - 13128
(2018/04/23)
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- JAK KINASE INHIBITOR COMPOUNDS FOR TREATMENT OF RESPIRATORY DISEASE
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The invention provides compounds of formula (I): wherein X is (I) and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
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Page/Page column 35
(2017/06/01)
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- HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
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Paragraph 000263
(2016/05/02)
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- An indazole compound derivatives and its preparation method
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The invention relates to an indazole compound derivative and a preparation method thereof. The indazole compound derivative is 6-bromine-3-acetyl indazole. The preparation method comprises the following steps: (1) a compound 1, namely 6-bromine-indole, reacts with sodium nitrite and hydrochloric acid to generate a compound 2; (2) the compound 2 reacts with di-tert-butyl dicarbonate ester to generate a compound 3 (Boc-protected indazole carboxaldehyde); (3) the compound 3 is reduced with sodium boro-hydride to generate a compound 4; (4) the indazole hydroxy of the compound 4 is oxidized into indazole acetyl by manganese dioxide to obtain the end product, namely the compound 5. The end product has a wide application prospect in the aspects such as curing of inflammation related diseases.
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Paragraph 0023; 0024; 0029
(2016/11/21)
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- AROMATIC HETEROCYCLIC COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS
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Provided herein are novel aromatic heterocyclic compounds or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and methods for using such compounds or pharmaceutical compositions thereof to treat Alzheimer's disease.
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Paragraph 00347; 00357
(2015/07/07)
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- COMPOSITION FOR PREVENTION OR TREATMENT OF HEART FAILURE
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Provided are a composition for preventing or treating heart failure and a method for screening an agent for treating heart failure. The present disclosure demonstrates for the first time that administration of PKC zeta inhibitor provides inotropic effect
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- 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC-ζ inhibitor
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The inhibition of PKC-ζ has been proposed to be a potential drug target for immune and inflammatory diseases. A series of 2-(6-phenyl-1H indazol-3-yl)-1H-benzo[d]imidazoles with initial high crossover to CDK-2 has been optimized to afford potent and selec
- Trujillo, John I.,Kiefer, James R.,Huang, Wei,Thorarensen, Atli,Xing, Li,Caspers, Nicole L.,Day, Jacqueline E.,Mathis, Karl J.,Kretzmer, Kuniko K.,Reitz, Beverley A.,Weinberg, Robin A.,Stegeman, Roderick A.,Wrightstone, Ann,Christine, Lori,Compton, Robert,Li, Xiong
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scheme or table
p. 908 - 911
(2009/09/06)
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