503552-68-9Relevant academic research and scientific papers
Discovery of 1-pyrimidinyl-2-aryl-4,6-dihydropyrrolo [3,4-d]imidazole-5(1H)-carboxamide as a novel JNK inhibitor
Cho, Hyunwook,Hah, Jung-Mi,Im, Daseul,Jang, Miyoung,Moon, Hyungwoo,Oh, Youri,Yang, Songyi
, (2020/03/13)
We designed and synthesized 1-pyrimidinyl-2-aryl-4, 6-dihydropyrrolo [3,4-d] imidazole-5(1H)-carboxamide derivatives as selective inhibitors of c-Jun-N-terminal Kinase 3 (JNK3), a target for the treatment of neurodegenerative diseases. Based on the compounds found in previous studies, a novel scaffold was designed to improve pharmacokinetic characters and activity, and compound 18a, (R)-1-(2-((1-(cyclopropanecarbonyl)pyrrolidin-3-yl)amino)pyrimidin-4-yl)-2-(3,4-dichlorophenyl)-4,6-dihydro pyrrolo [3,4-d]imidazole-5(1H)-carboxamide, showed the highest IC50 value of 2.69 nM. Kinase profiling results also showed high selectivity for JNK3 among 38 kinases, having mild activity against JNK2, RIPK3, and GSK3β, which also known to involve in neuronal apoptosis.
JAK inhibitor compound and application thereof
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, (2020/09/12)
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.
FGFR4 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0422-0424, (2019/10/10)
Provided are a class of compounds as shown in formula (I) as FGFR4 inhibitors, and pharmaceutically acceptable salts thereof, preparation methods therefor and the use thereof in the preparation of drugs for treating FGFR4-related diseases.
Compound JK-03M having higher protein kinase G inhibitory activity or pharmaceutically acceptable salt thereof and preparation method thereof
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Paragraph 0093; 0118; 0150-0151, (2018/11/03)
The invention discloses a compound which has higher protein kinase G inhibitory activity and is shown in a formula I or pharmaceutically acceptable salt thereof and a preparation method thereof. The compound JK-03M having the higher protein kinase G inhibitory activity comprises a pharmaceutical composition of a new compound and application of the new compound in treatment of pain, in particular to chronic pain. The formula (1) is shown in the description.
Pyrrole imidazole ring derivative and medical use thereof wherein the compound represented by the general formula (I) has excellent inhibitory effect on and selectivity of dipeptidyl peptidase IV(DPP-IV)
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Page/Page column 64, (2017/08/02)
The present invention relates to a pyrrole imidazole ring derivative and medical use thereof, more particularly a pyrrole imidazole ring derivative represented by the general formula (I) or stereoisomers thereof, pharmaceutically acceptable salts thereof, prodrugs, pharmaceutical compositions containing the derivative, and pharmaceutical applications for the preparation of dipeptidyl peptidase IV(DPP-IV) inhibitors, wherein the definitions of all substitution groups in general formula (I) are the same as those defined in the specification.
Compounds with higher PKG (protein kinase G) inhibitory activity and preparation method of compounds
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Paragraph 0178; 0179; 0180; 0181; 0182; 0183, (2016/10/08)
The invention discloses compounds which have higher PKG (protein kinase G) inhibitory activity and are represented as a formula I, pharmaceutically acceptable salts, pharmaceutical composition containing the novel compounds, as well as an application of the novel compounds in treatment of pain, especially chronic pain. The invention further discloses a preparation method of the compounds and new intermediates. R1 and R2 are the same or different and are selected from a group comprising halogen (such as F or Cl), C1-C6 alkoxy, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl; R3 is a terminal group and is selected from a group comprising H, halogen, alkyl, naphthenic base, alkenyl, alkynyl, aryl and heteroaryl; n is the number of repetitive units and is an integer in a range from 1 to 15.
COMPOUND HAVING HIGHER INHIBITION OF PROTEIN KINASE G ACTIVITY AND PREPARATION METHOD THEREFOR
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Paragraph 0081; 0082, (2016/12/12)
Disclosed are a compound of Formula I having higher inhibition of protein kinase G (PKG) activity and pharmaceutically acceptable salts thereof. In Formula I, R1 and R2 are the same or different, each being independently chosen from the halogens, the C1-C6 alkoxyl group, the C1-C6 alkyl group, the C2-C6 alkenyl group, and the C2-C6 alkynyl group; R3 is chosen from H, the halogens, the substituted or unsubstituted C1-C6 alkyl group, C3-C6 cycloalkyl group, C2-C6 alkenyl group, and C2-C6 alkynyl group, aryl group, and heteroaryl group; and n is an integer between 0 and 15. Also disclosed is a pharmaceutical composition comprising said compound, the use of the compound in treating pains, in particular chronic pain, a preparation method for the compound, and a new intermediate.
THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
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, (2010/01/12)
A series of thieno[2,3-6]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fus
Structure-guided design of C2-symmetric HIV-1 protease inhibitors based on a pyrrolidine scaffold
Blum, Andreas,B?ttcher, Jark,Heine, Andreas,Klebe, Gerhard,Diederich, Wibke E.
, p. 2078 - 2087 (2008/12/22)
Infections with the human immunodeficiency virus, which inevitably lead to the development of AIDS, are still among the most serious global health problems causing more than 2.5 million deaths per year. In the pathophysiological processes of this pandemic
AMINOCYCLOHEXANES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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Page/Page column 39, (2008/06/13)
The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
