87600-97-3Relevant articles and documents
CDPK1 INHIBITORS, COMPOSITIONS, AND METHODS RELATED THERETO
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Paragraph 0516; 0525-0526, (2021/11/13)
The invention relates to inhibitors of calcium-dependent protein kinase 1 (CDPK1) and pharmaceutical preparations thereof. The invention further relates to methods of treatment of parasitic infections, such as T. gondii, P. falciparum, C. hominis, or C. parvum infections, using the novel inhibitors of the invention.
Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators
Miyazaki, Tohru,Kawasaki, Masanori,Suzuki, Atsushi,Ito, Yuki,Imanishi, Akio,Maru, Takamitsu,Kawamoto, Tomohiro,Koike, Tatsuki
, p. 815 - 820 (2019/01/30)
The voltage-gated sodium channel, Nav1.1, is predominantly expressed in parvalbumin-positive fast spiking interneurons and has been genetically linked to Dravet syndrome. Starting from a high throughput screening hit isoxazole derivative 5, mod
HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 1366-1367, (2018/04/26)
The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.
Substituted aminopyrimidine compounds and their method and use thereof
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Paragraph 0622; 0623, (2017/12/28)
The invention relates to a new aminopyrimidine compound and an application thereof as a drug for treating disorder or diseases related to PI3-kinase abnormity in a free form or a pharmaceutically acceptable salt and preparation form. The invention also relates to a pharmaceutical composition which contains the new aminopyrimidine compound and an application of the pharmaceutical composition in treating mammal disorder or diseases and especially treating human disorder or diseases related to the PI3-kinase abnormity, such as treatment of immunity and inflammatory diseases of PI3-kinase regulation which plays a leading role in a leucocyte function and treatment of proliferative diseases which are related to PI3-kinase activity and include but not limited to leukaemia and solid tumor.
SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE
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Paragraph 369, (2016/10/04)
The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
Substituted aminopyrimidine compound and usage method and application thereof
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Paragraph 0705; 0706, (2017/07/20)
The present invention relates to a substituted aminopyrimidine compound and a usage method and application thereof, and in particular to application of the novel aminopyrimidine compound and free-form salts or pharmaceutically acceptable salts and preparations thereof as the medicaments for the treatment of PI3-kinase abnormality-related disorder or diseases. The invention also relates to the pharmaceutical compositions comprising the compound, and application of the pharmaceutical compositions to the treatment of mammals, particularly for the treatment of PI3-kinase abnormality-related human disorder or diseases, such as treatment of PI3-kinase regulated immune and inflammatory diseases, wherein PI3-kinase plays a major role in leukocyte function, and the treatment of of PI3- kinase-related proliferative diseases including but not limited to leukemia and solid tumors.
SYNTHESIS OF SUBSTITUTED 1H-PYRAZOLO[3,4-D]PYRIMIDINES
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Page/Page column 18-19, (2016/05/19)
The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H- pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-l-yl)prop-2-en-l-one(ibrutinib) and its synthesis intermediates.
Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors
Zou, Yi,Xiao, Jianhu,Tu, Zhengchao,Zhang, Yingyi,Yao, Kun,Luo, Minghao,Ding, Ke,Zhang, Yihua,Lai, Yisheng
supporting information, p. 3052 - 3059 (2016/06/13)
A series of novel 4,5,6-trisubstituted pyrimidines were designed as potent covalent Bruton's tyrosine kinase (BTK) inhibitors based on the structure of ibrutinib by using a ring-opening strategy. Among these derivatives, compound I1 exhibited the most potent inhibitory activity with an IC50 value of 0.07 μM. The preliminary structure-activity relationship was discussed and the primary amino group at the C-4 position of pyrimidine was crucial for maintaining BTK activity. Furthermore, molecular dynamics simulations and binding free energy calculations were performed for three inhibitor-BTK complexes to determine the probable binding model, which provided a comprehensive guide for further structural modification and optimization.
ANTIVIRAL COMPOUNDS
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Paragraph 1107, (2015/03/13)
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
NOVEL COMPOUND AS A DIACYLGLYCEROL ACYLTRANSFERASE INHIBITOR
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Page/Page column 14; 15, (2015/04/22)
This invention relates to a novel compound which is an inhibitor of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT1), to pharmaceutical compositions containing it, to processes for its preparation, and to its use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy, for the prevention or treatment of diseases related to DGAT1 dysfunction or where modulation of DGAT1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia- related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.