- Synthesis method of Brigatinib intermediate
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The invention discloses a synthesis method of a Brigatinib intermediate. The Brigatinib intermediate is 2-methoxy-4-(4-(4-methyl piperazine-1-yl) piperidine-1-yl) aniline (I). The synthesis method comprises the following steps: taking 5-fluoro-2-nitroanis
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Paragraph 0034-0038; 0044-0051
(2021/06/26)
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- Substituted diaminopyrimidine compound
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The present invention provides a substituted diaminopyrimidine compound represented by a formula (I), or a pharmaceutically acceptable salt, a crystal form, a prodrug, a metabolite, a hydrate, a solvate, a stereoisomer or an isotope derivative thereof, as well as a pharmaceutical composition and uses thereof. The compound provided by the invention can be used for treating ALK-mediated related diseases, such as non-small cell lung cancer, breast cancer, neural tumor, esophageal cancer, soft tissue cancer, lymphoma and leukemia.
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Paragraph 0229-0234
(2019/07/04)
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- Preparation method and crystal form of deuterated diphenyl amino pyrimidine compound
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The present invention discloses a preparation method and a crystal form of a compound shown in the formula (A) and also discloses a pharmaceutical composition comprising the crystal form of the compound shown in the formula (A) and a method for treating A
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Paragraph 0340-0344
(2019/04/27)
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- DEUTERIUM-MODIFIED BRIGATINIB DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND USE THEREOF
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The present invention relates to the field of pharmaceutical chemistry, and relates to a deuterium-modified Brigatinib derivative, preparation method thereof, pharmaceutical composition containing the same and the uses of the deuterium-modified Brigatinib derivative and the pharmaceutical composition thereof in preparing a medicament for treating the disease mediated by anaplastic lymphoma kinase. The deuterium-modified Brigatinib derivative of the present invention has an excellent inhibitory activity on anaplastic lymphoma kinase and has better pharmacodynamic or pharmacokinetic properties relative to Brigatinib.
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- 2,4-dibasic miazines compound
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The invention belongs to the field of medical chemistry, relates to a 2,4-dibasic miazines compound and specifically relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof, a drug compound thereof and an application thereof in treating EGFR or/and ALK mediated diseases.
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- Diaminopyrimidine compound and composition containing same
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The invention provides a diaminopyrimidine compound and a composition containing the same and discloses the diaminopyrimidine compound shown as in a formula (I) and a drug combination containing the compound or salt thereof acceptable in crystal form and
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Paragraph 0112-0119
(2017/06/02)
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- METHOD FOR PRODUCING DI(ARYLAMINO)ARYL COMPOUND, AND SYNTHETIC INTERMEDIATE THEREFOR
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Provided is a method for producing a di(arylamino)aryl compound that has superior inhibitory activity against the kinase activities of EML4-ALK fusion protein and mutant EGFR protein and is useful as an active ingredient in pharmaceutical compositions for cancer treatment. The production method includes no purification step using silica gel column chromatography or no step possibly producing a mutagenic mesylate ester as a by-product, greatly improves overall yield, and is high yield and low cost and suitable for the industrial production of pharmaceutical products. Also provided is a synthetic intermediate that is useful in the production method.
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Paragraph 0040
(2014/01/07)
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- CHEMICAL COMPOUNDS
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The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the tr
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- THIAZOLE SULFONAMIDE AND OXAZOLE SULFONAMIDE KINASE INHIBITORS
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The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents
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Page/Page column 144
(2010/10/03)
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- COMPOUNDS AND THERAPEUTIC USES THEREOF
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The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
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Page/Page column 130-131
(2010/11/03)
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- Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)
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The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimi
- Emmitte, Kyle A.,Wilson, Brian J.,Baum, Erich W.,Emerson, Holly K.,Kuntz, Kevin W.,Nailor, Kristen E.,Salovich, James M.,Smith, Stephon C.,Cheung, Mui,Gerding, Roseanne M.,Stevens, Kirk L.,Uehling, David E.,Mook Jr., Robert A.,Moorthy, Ganesh S.,Dickerson, Scott H.,Hassell, Anne M.,Anthony Leesnitzer,Shewchuk, Lisa M.,Groy, Arthur,Rowand, Jason L.,Anderson, Kelly,Atkins, Charity L.,Yang, Jingsong,Sabbatini, Peter,Kumar, Rakesh
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scheme or table
p. 1004 - 1008
(2009/10/15)
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- 2- [ (2-{PHENYLAMINO}-1H-PYRROLO [2, 3-D] PYRIMIDIN-4-YL) AMINO] BENZAMIDE DERIVATIVES AS IGF-1R INHIBITORS FOR THE TREATMENT OF CANCER
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Novel pyrrolopyrimidines as shown in formula (I) and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.
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Page/Page column 97-98
(2009/04/25)
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- Imidazopyridine Kinase Inhibitors
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The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 72
(2009/01/20)
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- 2, 4- DI (PHENYLAMINO) PYRIMIDINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS
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Novel pyrimidine derivatives of formula (I), to processes for their production, their use as pharmaceuticals in the treatment of neoplastic diseases, inflammatory and immune system disorders and to pharmaceutical compositions comprising them.
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Page 131-132
(2010/02/08)
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