148430-81-3Relevant articles and documents
Mild C–C Bond Formation via Lewis Acid Catalyzed Oxetane Ring Opening with Soft Carbon Nucleophiles
Huang, Hai,Zhang, Tianyu,Sun, Jianwei
supporting information, p. 2668 - 2673 (2020/12/07)
Mild oxetane opening by soft carbon nucleophiles has been developed for efficient C?C bond formation. In the presence of LiNTf2 or TBSNTf2 as catalyst, silyl ketene acetals were found to be effective nucleophiles to generate a wide range of highly oxygenated molecules, which are key substructure in natural products like polyketides. Furthermore, intramolecular oxetane opening by a styrene-based carbon nucleophile via a Prins-type process was also achieved with Sc(OTf)3 as catalyst, leading to efficient formation of the useful 2,3-dihydrobenzo[b]oxepine skeleton.
A GAP Replacement: Improved Synthesis of 3-Azidooxetane and Its Homopolymer Based on Sulfonic Acid Esters of Oxetan-3-ol
Born, Max,Karaghiosoff, Konstantin,Klap?tke, Thomas M.
supporting information, p. 12607 - 12614 (2021/09/18)
In the field of energetic binders, only hydroxy-terminated glycidyl azide polymer (GAP) has found widespread application and prevailed in the market. However, oxiranes such as glycidyl azide (GA) allow two ring-opening modes during polymerization and thus
N-(AZAARYL)CYCLOLACTAM-1-CARBOXAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
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Paragraph 0143; 0162; 0163, (2020/03/23)
An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.
Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis
Janetka, James W.,Hopper, Allen T.,Yang, Ziping,Barks, Jennifer,Dhason, Mary Savari,Wang, Qiuling,Sibley, L. David
supporting information, p. 6144 - 6163 (2020/07/10)
Calcium dependent protein kinase 1 (CDPK1) is an essential Ser/Thr kinase that controls invasion and egress by the protozoan parasite Toxoplasma gondii. The Gly gatekeeper of CDPK1 makes it exquisitely sensitive to inhibition by small molecule 1H-pyrazolo
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists
Lu, Hongfu,Yang, Ting,Xu, Zhongmiao,Lin, Xichen,Ding, Qian,Zhang, Yueting,Cai, Xin,Dong, Kelly,Gong, Sophie,Zhang, Wei,Patel, Metul,Copley, Royston C. B.,Xiang, Jianing,Guan, Xiaoming,Wren, Paul,Ren, Feng
supporting information, p. 2518 - 2532 (2018/03/26)
CXCR2 has emerged as a therapeutic target for not only peripheral inflammatory diseases but also neurological abnormalities in the central nervous system (CNS). Herein, we describe the discovery of a novel 1-cyclopentenyl-3-phenylurea series as potent and CNS penetrant CXCR2 antagonists. Extensive SAR studies, wherein molecules' property forecast index (PFI) was carefully optimized for overall balanced developability profiles, led to the discovery of the advanced lead compound 68 with a desirable PFI. Compound 68 demonstrated good in vitro pharmacology with excellent selectivity over CXCR1 and other chemokine receptors. Rat and dog pharmacokinetics (PK) revealed good oral bioavailability, high oral exposure, and desirable elimination half-life of the compound in both species. In addition, the compound demonstrated dose-dependent efficacy in the in vivo pharmacology neutrophil infiltration "air pouch" model in rodents after oral administration. Further, compound 68 is a CNS penetrant molecule with high unbound fraction in brain tissue.
Amino 6-membered ring derivative and pharmaceutical applications thereof including the use for manufacturing dipeptidyl peptidase-4(IDPP-IV) inhibitor
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Page/Page column 98; 99, (2017/07/31)
The present invention relates to an amino 6-membered ring derivative and pharmaceutical applications thereof, which specifically relates to the amino 6-membered ring derivative represented by the general formula (I) or stereoisomers thereof, pharmaceutically acceptable salts thereof, a prodrug, a pharmaceutical composition comprising the derivative, and the pharmaceutical use for manufacturing dipeptidyl peptidase-4(IDPP-IV) inhibitor, wherein the definition of each substituent in the general formula (I) is the same as described in the specification.
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies
Bezen?on, Olivier,Heidmann, Bibia,Siegrist, Romain,Stamm, Simon,Richard, Sylvia,Pozzi, Davide,Corminboeuf, Olivier,Roch, Catherine,Kessler, Melanie,Ertel, Eric A.,Reymond, Isabelle,Pfeifer, Thomas,De Kanter, Ruben,Toeroek-Schafroth, Michael,Moccia, Luca G.,Mawet, Jacques,Moon, Richard,Rey, Markus,Capeleto, Bruno,Fournier, Elvire
supporting information, p. 9769 - 9789 (2017/12/26)
We report here the discovery and pharmacological characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain penetration, and the search for an aminopyrazole metabolite that would be negative in an Ames test. This resulted in the preparation and complete characterization of compound 66b (ACT-709478), which has been selected as a clinical candidate.
1 -(CYCLOPENT-2-EN-1 -YL)-3-(2-HYDROXY-3-(ARYLSULFONYL)PHENYL)UREA DERIVATIVES AS CXCR2 INHIBITORS
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Page/Page column 169, (2015/12/18)
The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
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Page/Page column 124; 125, (2013/04/25)
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and N-oxides thereof,that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
Herbicidal oxetane and thiaetane derivatives
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, (2008/06/13)
Oxetane and thiaetane derivatives of the formula I in which, Q is oxygen, sulfur, -COO-, -Z-CH(R3)-COO-, or CO-Y4-CH(R10)-COO-;, W is and R1 is hydrogen or fluorine; R2 is halogen or cyano; R3 and R10 independently of one another are hydrogen or C1-C3alkyl; R4 is hydrogen, fluorine, chlorine, bromine, C1-C4alkyl or trifluoromethyl; R5 and R7 independently of one another are C1-C4alkyl; R6 and R8 independently of one another are hydrogen or C1-C4alkyl; R9 is hydrogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C4alkoxy-C1-C4alkyl or C1-C7haloalkyl; X is oxygen or sulfur; Y1, Y2, Y3, Y4, Y5 and Y6 independently of one another are oxygen or sulfur; Z is oxygen or sulfur; n is 0; 1, 2, 3 or 4; and q is 1 or 2, have good selective herbicidal properties when used pre- or post-emergence.