6134-54-9Relevant academic research and scientific papers
N-Atom Deletion in Nitrogen Heterocycles
Qin, Haitao,Cai, Wangshui,Wang, Shuang,Guo, Ting,Li, Guigen,Lu, Hongjian
, p. 20678 - 20683 (2021/08/25)
Excising the nitrogen in secondary amines, and coupling the two residual fragments is a skeletal editing strategy that can be used to construct molecules with new skeletons, but which has been largely unexplored. Here we report a versatile method of N-atom excision from N-heterocycles. The process uses readily available N-heterocycles as substrates, and proceeds by N-sulfonylazidonation followed by the rearrangement of sulfamoyl azide intermediates, providing various cyclic products. Examples are provided of deletion of nitrogen from natural products, synthesis of chiral O-heterocycles from commercially available chiral β-amino alcohols, formal inert C?H functionalization through a sequence of N-directed C?H functionalization and N-atom deletion reactions in which the N-atom can serve as a traceless directing group.
INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
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Paragraph 001383-001385, (2021/10/15)
Compounds of Formula (I) and methods of inhibiting the replication of viruses in a biological sample or patient, of reducing the amount of viruses in a biological sample or patient, and of treating a virus infection in a patient, comprising administering to said biological sample or patient an effective amount of a compound represented by Formula (I), a compound of Table A or B or a pharmaceutically acceptable salt thereof.
As a new polyphenylenepolymethylenepolyisocyanate deriv. SGLT2 inhibitor
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Paragraph 0364-0365, (2016/10/09)
A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.
FUSED HETEROCYCLIC COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATORS
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Page/Page column 32, (2012/08/28)
Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
TRIAZOLONES AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 149-150, (2011/09/19)
This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
SUBSTITUTED PARA-BIPHENYLOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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Page/Page column 45, (2011/04/19)
The present invention relates to a series of substituted para-biphenyloxymethyl dihydro oxazolopyrimidinones of formula (I) as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of
Anti-cancer agents and uses thereof
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Page/Page column 27, (2008/12/08)
The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
Anti-cancer agents and uses thereof
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Page/Page column 27, (2008/06/13)
The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3—R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.
Two classes of p38α MAP kinase inhibitors having a common diphenylether core but exhibiting divergent binding modes
Michelotti, Enrique L.,Moffett, Kristofer K.,Nguyen, Duyan,Kelly, Martha J.,Shetty, Rupa,Chai, Xiaomei,Northrop, Katrina,Namboodiri, Variketta,Campbell, Brandon,Flynn, Gary A.,Fujimoto, Ted,Hollinger, Frank P.,Bukhtiyarova, Marina,Springman, Eric B.,Karpusas, Michael
, p. 5274 - 5279 (2007/10/03)
Two new classes of diphenylether inhibitors of p38α MAP kinase are described. Both chemical classes are based on a common diphenylether core that is identified by simulated fragment annealing as one of the most favored chemotypes within a prominent hydrophobic pocket of the p38α ATP-binding site. In the fully elaborated molecules, the diphenylether moiety acts as an anchor occupying the deep pocket, while polar extensions make specific interactions with either the adenine binding site or the phosphate binding site of ATP. The synthesis, crystallographic analysis, and biological activity of these p38α inhibitors are discussed.
Intermediate Formation ofMetacyclophane on Flash Vacuum Thermolysis
Kostermans, Gerardus, B. M.,Dansik, Paul van,Wolf, Willem H. de,Bickelhaupt, Friedrich
, p. 4531 - 4534 (2007/10/02)
Pyrolysis of 2,6-tetramethylene Dewar benzene (2a) under flash vacuum thermolysis (FVT) conditions at 400 deg C gave 6- and 5-methylindan (8a (2.5percent) and 10a (2.5percent), respectively) as well tetralin (5a) (45percent).These products indicate that metacyclophane (1a) was formed in the gas phase, but it decomposed under the reaction conditions either via homolytic cleavage of one of the benzylic bonds to yield a diradical (6a) leading to 8a and 10a or it gave 5a via benzvalene intermediate (4a).Deuterium labeling supports the proposed mechanism.A very similar course of events was observed on FVT of metacyclophane at 600 deg C; it yielded methyl-substituted tetralins (8c, 10c) as the sole products.The analogies and differences in the behavior of the two metacyclophanes are discussed.
