- FGFR INHIBITOR AND APPLICATION THEREOF
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An azatricyclic compound (as represented by formula I) which acts as an inhibitor of fibroblast growth factor receptors (FGFR), as well as a pharmaceutical composition thereof, a preparation method, and a use therefor in the treatment of FGFR-mediated diseases. The azatricyclic compound exerts an effect by means of participating in the regulation of a plurality of processes such as cell proliferation, apoptosis, migration, neovascularization, and the like. AA%%%Formula (I).
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Paragraph 0118-0119
(2020/01/22)
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- Pyrido[2,3-d]pyrimidin-7(8H)-one derivatives and Composition for skin whitening and Pharmaceutical composition for use in preventing or treating disorders of Melanin Hyperpigmentation containing the same as an active ingredient
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The present invention relates to a pyrido[2,3-d]pyrimidin-7(8H)-one derivative, and to a composition for skin whitening comprising the same as an active ingredient. Since the derivative exhibits an effect of inhibiting the production of melanin even when
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Paragraph 0196; 0210-0212
(2020/11/03)
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- Pyridopyrimidinone derivatives as potent and selective c-jun N-terminal kinase (JNK) inhibitors
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A novel series of 2-aminopyridopyrimidinone based JNK (c-jun N-terminal kinase) inhibitors were discovered and developed. Structure-activity relationships (SARs) were systematically developed utilizing biochemical and cell based assays and in vitro and in vivo drug metabolism and pharmacokinetic (DMPK) studies. Through the optimization of lead compound 1, several potent and selective JNK inhibitors with high oral bioavailability were developed. Inhibitor 13 was a potent JNK3 inhibitor (IC50 = 15 nM), had high selectivity against p38 (IC50 > 10 μM), had high potency in functional cell based assays, and had high stability in human liver microsome (t1/2 = 76 min), a clean CYP-450 inhibition profile, and excellent oral bioavailability (%F = 87). Moreover, cocrystal structures of compounds 13 and 22 in JNK3 were solved at 2.0 ?. These structures elucidated the binding mode (Type-I binding) and can pave the way for further inhibitor design of this pyridopyrimidinone scaffold for JNK inhibition.
- Zheng, Ke,Park, Chul Min,Iqbal, Sarah,Hernandez, Pamela,Park, Hajeung,Lograsso, Philip V.,Feng, Yangbo
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supporting information
p. 413 - 418
(2015/04/27)
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- Pyridopyrimidinone derivatives for treatment of neurodegenerative disease
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This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferatives disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2 (amino and thio)pyrido[2,3-d]pyrimidines and 2,4-di
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- Pyrido[2,3-d]pyrimidine-2,7-diamine kinase inhibitors
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Disclosed are compounds of the formula (I) wherein: R2, R7, RI3, R14 and R15 are independently hydrogen, or (un)substituted lower alkyl, (un)substitued lower alkenyl, (un)substituted lower alkynyl, or (un)substituted —(CH2)nR12; R5 is halogen, cyano, nitro, —R9, —NR9R10, or —OR9; R6 is halogen, cyano, nitro, —R9, —NR9R10, —OR9, —Co2R9, —COR9, —CONR9R10, —NR9COR10, (un)substiuted lower alkenyl, or (un)substituted lower alkynyl; R8 is —CO2R13, —COR13, —CONR13R14, —CSNR13R14, —C(NR13)NR14R15, —SO3R13, —SO2R13, —SO2NR13R14, —PO3R13R14, —POR13R14, —PO(NR13R14)2; R9 and R10 are independently hydrogen or (un)substituted lower alkyl; R11 is a heteroaryl or a heterocyclic group; R12 is a cycloalkyl, a heterocyclic, an aryl, or a heteroaryl group; and n is 0,1,2, or 3. These compounds and their pharmaceutical compositions are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cdks and growth factor-mediated kinases.
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- Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
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This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 2,4-dia
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