150008-24-5Relevant articles and documents
FUSED BICYCLIC RAF INHIBITORS AND METHODS FOR USE THEREOF
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Paragraph 0586-0588, (2022/02/09)
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method o
PROCESSES FOR PREPARING AN S1P-RECEPTOR MODULATOR
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Page/Page column 32, (2021/05/07)
This application relates to processes for preparing an S1P-receptor modulator "Compound 1", which is useful in the treatment of diseases or disorders associated with activity of S1P, including CNS disorders. The process comprises reacting "compound 2" with "compound 3" in the presence of a reducing agent.
sEH Inhibitor or pharmaceutically acceptable composition thereof as well as preparation method and application thereof
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Paragraph 0117-0118, (2021/09/21)
The invention provides sEH inhibitor or a pharmaceutically acceptable composition and a preparation method and application thereof, and belongs to the technical field of medicines. sEH Inhibitor or a pharmaceutically acceptable composition thereof according to the present invention is provided, and the sEH inhibitor has the structure shown I. sEH Inhibitor provided by the invention can stabilize an endogenous substance epoxy fatty acid with wide physiological activity, has a strong inhibition effect on human recombinant sEH, and can be used for regulating the generation of a plurality of pro-inflammatory cytokines. The invention relieves the stress of endoplasmic reticulum, prevents or reverses the dysfunction of endothelial dysfunction, stabilizes mitochondria function multiple action mechanisms to obviously relieve neuropathic pain, and can effectively avoid adverse reactions related to the target spot. Furthermore, the sEH inhibitor structure provided by the invention does not contain free carboxyl groups, can avoid adverse reactions such as gastrointestinal irritation caused by oral administration, and is small in adverse reaction, high in bioavailability, excellent in analgesic effect and small in administration amount.
NOVEL INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 178-179, (2020/11/13)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
NOVEL PHENYL AND PYRIDYL UREAS ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 161, (2020/11/13)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
1, 3, 4, 5-TETRAHYDRO-2H-PYRIDO[4,3-B]INDOLE DERIVATIVES FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES LIKE ALZHEIMER'S DISEASE
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Page/Page column 124, (2019/07/20)
The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00318, (2017/09/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
An efficient catalytic method for the Beckmann rearrangement of ketoximes to amides and aldoximes to nitriles mediated by propylphosphonic anhydride (T3P)
Augustine, John Kallikat,Kumar, Rajesha,Bombrun, Agnes,Mandal, Ashis Baran
experimental part, p. 1074 - 1077 (2011/03/22)
An efficient method for the Beckmann rearrangement of ketoximes to amides mediated by a catalytic amount (15 mol %) of propylphosphonic anhydride (T3P) is described. Aldoximes underwent second order Beckmann rearrangement to provide the corresponding nitriles in excellent yields on reacting with T3P (15 mol %) at room temperature. The main advantages of this environmentally friendly protocol include procedural simplicity, and particularly ease of isolation of the products.
1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia
Anandan, Sampath-Kumar,Webb, Heather Kay,Chen, Dawn,Wang, Yi-Xin,Aavula, Basker R.,Cases, Sylvaine,Cheng, Ying,Do, Zung N.,Mehra, Upasana,Tran, Vinh,Vincelette, Jon,Waszczuk, Joanna,White, Kathy,Wong, Kenneth R.,Zhang, Le-Ning,Jones, Paul D.,Hammock, Bruce D.,Patel, Dinesh V.,Whitcomb, Randall,MacIntyre, D. Euan,Sabry, James,Gless, Richard
scheme or table, p. 983 - 988 (2011/03/20)
1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea 14a (AR9281), a potent and selective soluble epoxide hydrolase inhibitor, was recently tested in a phase 2a clinical setting for its effectiveness in reducing blood pressure and improving insulin resistance in pre-diabetic patients. In a mouse model of diet induced obesity, AR9281 attenuated the enhanced glucose excursion following an intraperitoneal glucose tolerance test. AR9281 also attenuated the increase in blood pressure in angiotensin-II-induced hypertension in rats. These effects were dose-dependent and well correlated with inhibition of the sEH activity in whole blood, consistent with a role of sEH in the observed pharmacology in rodents.
Structure-based rational design, synthesis and antifungal activity of oxime-containing azole derivatives
Xu, Yulan,Sheng, Chunquan,Wang, Wenya,Che, Xiaoying,Cao, Yongbing,Dong, Guoqiang,Wang, Shengzheng,Ji, Haitao,Miao, Zhenyuan,Yao, Jianzhong,Zhang, Wannian
supporting information; experimental part, p. 2942 - 2945 (2010/08/19)
In an attempt to find novel azole antifungal agents with improved activity and broader spectrum, computer modeling was used to design a series of new azoles with piperidin-4-one O-substituted oxime side chains. Molecular docking studies revealed that they formed hydrophobic and hydrogen-bonding interactions with lanosterol 14α-demethylase of Candida albicans (CACYP51). In vitro antifungal assay indicates that most of the synthesized compounds showed good activity against tested fungal pathogens. In comparison with fluconazole, itraconazole and voriconazole, several compounds (such as 10c, 10e, and 10i) show more potent antifungal activity and broader spectrum, suggesting that they are promising leads for the development of novel antifungal agents.