800402-12-4Relevant articles and documents
Organic compound, electroluminescent device containing organic compound and applications of electroluminescent device
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Paragraph 0115-0117, (2020/06/17)
The invention discloses an organic compound with a structure represented by a formula (I), wherein the LUMO energy level of the compound is reduced by linking an aza aromatic ring structure (a structure represented by a formula (II)), so that the electronic conductivity of the material is improved, and the compound is suitable for being used as an electronic material (such as an electron transportmaterial, an electron injection material, a hole blocking material and the like). According to the invention, the organic compound as an electron type material, particularly an electron transmissionmaterial, can be matched with hole type materials (such as a hole transmission material, a hole injection material and an electron blocking material), so that the transmission of electrons and holes is balanced, and the service life of a device is prolonged.
PYRIMIDINE OR PYRIDOPYRIDONE COMPOUND AND APPLICATION THEREOF
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Paragraph 0046; 0069, (2018/11/21)
The present invention discloses a pyrimidine or pyridopyridone compound as shown in formula (I) and an application thereof relating to the technical field of medicament preparation. The compound can selectively suppress cyclin-dependent kinases (Cdks) CDK
Synthesis, molecular docking, antimycobacterial and antimicrobial evaluation of new pyrrolo[3,2-c]pyridine Mannich bases
Jose, Gilish,Suresha Kumara, Tholappanavara H.,Sowmya, Haliwana B.V.,Sriram, Dharmarajan,Guru Row, Tayur N.,Hosamani, Amar A.,More, Sunil S.,Janardhan, Bhavya,Harish,Telkar, Sandeep,Ravikumar, Yalegara Siddappa
, p. 275 - 288 (2017/03/24)
In this report, we describe the synthesis and biological evaluation of a new series of pyrrolo[3,2-c]pyridine Mannich bases (7a-v). The Mannich bases were obtained in good yields by one-pot three component condensation of pyrrolo[3,2-c]pyridine scaffold (6a-c) with secondary amines and excess of formaldehyde solution in AcOH. The chemical structures of the compounds were characterized by 1H NMR, 13C NMR, LC/MS and elemental analysis. Single crystal X-ray diffraction has been recorded for compound 7k ([C23H29ClN4]+2, H2O). The in?vitro antimicrobial activities of the compounds were evaluated against various bacterial and fungal strains using Agar diffusion method and Broth micro dilution method. Compounds 7e, 7f, 7r, 7t, and 7u were showed good Gram-positive antibacterial activity against S.?aureus, B. flexus, C. sporogenes and S. mutans. Furthermore, in?vitro antimycobacterial activity was evaluated against Mycobacterium tuberculosis H37Rv (ATCC 27294) using MABA. Compounds 7r, 7t, and 7u were showed good antitubercular activity against Mtb (MIC ≥6.25?μg/mL). Among the tested compounds, 1-((4-chloro-2-(cyclohexylmethyl)-1H-pyrrolo[3,2-c]pyridin-3-yl)methyl)piperidine-3-carboxamide (7t) was showed excellent antimycobacterial activity against Mtb (MIC >25). Molecular docking of the active compounds against glutamate racemase (MurI) and Mtb glutamine synthetase were explained the structure-activity observed in?vitro.
Pyrimidine or pyridine pyridine ketone compound and its preparation method and application (by machine translation)
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Paragraph 0194, (2016/10/09)
The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)
Osborne, James D.,Matthews, Thomas P.,McHardy, Tatiana,Proisy, Nicolas,Cheung, Kwai-Ming J.,Lainchbury, Michael,Brown, Nathan,Walton, Michael I.,Eve, Paul D.,Boxall, Katherine J.,Hayes, Angela,Henley, Alan T.,Valenti, Melanie R.,De Haven Brandon, Alexis K.,Box, Gary,Jamin, Yann,Robinson, Simon P.,Westwood, Isaac M.,Van Montfort, Rob L. M.,Leonard, Philip M.,Lamers, Marieke B. A. C.,Reader, John C.,Aherne, G. Wynne,Raynaud, Florence I.,Eccles, Suzanne A.,Garrett, Michelle D.,Collins, Ian
supporting information, p. 5221 - 5237 (2016/07/06)
Multiparameter optimization of a series of 5-((4-aminopyridin-2-yl)amino)pyrazine-2-carbonitriles resulted in the identification of a potent and selective oral CHK1 preclinical development candidate with in vivo efficacy as a potentiator of deoxyribonucleic acid (DNA) damaging chemotherapy and as a single agent. Cellular mechanism of action assays were used to give an integrated assessment of compound selectivity during optimization resulting in a highly CHK1 selective adenosine triphosphate (ATP) competitive inhibitor. A single substituent vector directed away from the CHK1 kinase active site was unexpectedly found to drive the selective cellular efficacy of the compounds. Both CHK1 potency and off-target human ether-a-go-go-related gene (hERG) ion channel inhibition were dependent on lipophilicity and basicity in this series. Optimization of CHK1 cellular potency and in vivo pharmacokinetic-pharmacodynamic (PK-PD) properties gave a compound with low predicted doses and exposures in humans which mitigated the residual weak in vitro hERG inhibition.
HETEROARYL SUBSTITUTED AMINOPYRIDINE COMPOUNDS
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Page/Page column 36; 37, (2017/01/09)
Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from imidazo[1,2-b]pyridazinyl and pyrazolo[1,5-a]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, or triazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 0477; 0480; 0481, (2016/09/26)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
HETEROARYL SUBSTITUTED AMINOPYRIDINE COMPOUNDS
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Page/Page column 171-172, (2017/01/09)
Disclosed are compounds of Formula (I) or salts thereof, wherein HET is a heteroaryl selected from pyrrolo[2,3 b]pyridinyl, pyrrolo[2,3 d]pyrimidinyl, pyrazolo[3,4 b]pyridinyl, pyrazolo[3,4 d]pyrimidinyl, imidazolo[4,5 b]pyridinyl, and imidazolo[4,5 d]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a nitrogen ring atom in said heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, triazolyl, isoxazolyl, oxadiazolyl or dihydroisoxazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
Ligand structure includes a new metal complexes
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Paragraph 0318; 0319; 0320, (2016/11/24)
Compounds comprising a metal complex having novel ligands are provided. In particular, the compound is an iridium complex comprising novel aza DBX ligands. The compounds may be used in organic light emitting devices, particularly as emitting dopants, providing improved efficiency, low operating voltage, and long lifetime.
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects
Papillon, Julien P. N.,Lou, Changgang,Singh, Alok K.,Adams, Christopher M.,Ksander, Gary M.,Beil, Michael E.,Chen, Wei,Leung-Chu, Jennifer,Fu, Fumin,Gan, Lu,Hu, Chii-Whei,Jeng, Arco Y.,Lasala, Daniel,Liang, Guiqing,Rigel, Dean F.,Russell, Kerry S.,Vest, John A.,Watson, Catherine
, p. 9382 - 9394 (2015/12/23)
Human clinical studies conducted with LCI699 established aldosterone synthase (CYP11B2) inhibition as a promising novel mechanism to lower arterial blood pressure. However, LCI699's low CYP11B1/CYP11B2 selectivity resulted in blunting of adrenocorticotropic hormone-stimulated cortisol secretion. This property of LCI699 prompted its development in Cushing's disease, but limited more extensive clinical studies in hypertensive populations, and provided an impetus for the search for cortisol-sparing CYP11B2 inhibitors. This paper summarizes the discovery, pharmacokinetics, and pharmacodynamic data in preclinical species and human subjects of the selective CYP11B2 inhibitor 8.