1641-41-4Relevant articles and documents
Designer Outer Membrane Protein Facilitates Uptake of Decoy Molecules into a Cytochrome P450BM3-Based Whole-Cell Biocatalyst
Karasawa, Masayuki,Shoji, Osami,Stanfield, Joshua Kyle,Suzuki, Kazuto,Yonemura, Kai
supporting information, (2021/12/16)
We report an OmpF loop deletion mutant, which improves the cellular uptake of external additives into an Escherichia coli whole-cell biocatalyst. Through co-expression of the OmpF mutant with wild-type P450BM3 in the presence of decoy molecules, the yield
Imidazo ring PAR4 antagonist and medical applications thereof
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Paragraph 0200-0203, (2020/01/12)
The invention relates to an imidazo ring compound represented by formula (I) or formula (II), or a pharmaceutically acceptable salt or ester or solvate thereof. The compound disclosed by the inventioncan be used for preparing medicines for preventing or treating thromboembolic diseases.
BICYCLIC COMPOUNDS AS INHIBITORS OF PD1/PD-L1 INTERACTION/ACTIVATION
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Paragraph 00098, (2019/10/04)
The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation.
Benzene and fat ring structure of amino acetyl amine compound and use thereof (by machine translation)
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Paragraph 0094; 0098; 0099, (2019/01/06)
The invention relates to a fat ring structure containing benzimidazole amino acetyl amine compound and use thereof. The amino acetamide compounds the amino acetamide compounds, the compounds of the formula I, or its optically active isomer or a pharmaceutically acceptable salt: In formula I, R1 Hydrogen, C1 - C6 Straight or branched chain alkyl or phenyl; R2 For C1 - C7 Straight or branched chain alkyl, 5 - 6 membered of aralkyl, heteroaromatic ring group or cycloalkyl, or substituted 5 - 6 membered aromatic ring radical of, aromatic heterocyclic base or cycloalkyl; A is alkylene or carbonyl; n is 1 - 3 of the integer; wherein the substituted 5 - 6 membered of aralkyl, heteroaromatic ring group or cycloalkyl substituted group is selected from the following groups in one or more than two: halogen, C1 - C3 Alkyl or alkoxy, C1 - C3 Fluorine-containing alkyl group or a fluorine-containing alkyl oxy, nitro or cyano; states fragrance heterocyclic radical of the hetero atom as the nitrogen or sulfur; m is 1 - 3 of the integer. The present invention provides amino acetyl amine compound can be used as antiepileptic drug or ion channel blockers. (by machine translation)
BENZOISOQUINOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 32, (2018/02/28)
The present invention is directed to substituted benzoisoquinolinone compounds, their salts, pharmaceutical compositions comprising them and their use in therapy. In particular, the invention is directed substituted benzoisoquinolinone compounds which are muscarinic M1 receptor positive allosteric modulators. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M1 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M1 receptors are involved.
QUINAZOLINE COMPOUNDS USEFUL AS M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 64; 65, (2017/09/27)
The present invention is directed to compounds of Formula (I): (Formula (I)) and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R7, R8, R9, R11, n and p are defined herein. The compounds of Formula (I) are M1 receptor positive allosteric modulators that are useful in the treatment of diseases in which the M1 receptor is involved, including Alzheimer's disease, schizophrenia, pain and sleep disorders. The invention also relates to pharmaceutical compositions comprising a compound of Formula (I) and a pharmaceutically acceptable carrier, and to methods of using the compounds of Formula (I) in the treatment of diseases mediated by the M1 receptor.
CYCLIC PEROXIDE OXIDATION OF AROMATIC COMPOUND PRODUCTION AND USE THEREOF
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Page/Page column 9; 10, (2014/10/15)
The present invention provides a method for converting an aromatic hydrocarbon to a phenol by providing an aromatic hydrocarbon comprising one or more aromatic C-H bonds and one or more activated C-H bonds in a solvent; adding a phthaloyl peroxide to the solvent; converting the phthaloyl peroxide to a di-radical; contacting the di-radical with the one or more aromatic C-H bonds; oxidizing selectively one of the one or more aromatic C-H bonds in preference to the one or more activated C-H bonds; adding a hydroxyl group to the one of the one or more aromatic C-H bonds to form one or more phenols; and purifying the one or more phenols.
Metal-free oxidation of aromatic carbon-hydrogen bonds through a reverse-rebound mechanism
Yuan, Changxia,Liang, Yong,Hernandez, Taylor,Berriochoa, Adrian,Houk, Kendall N.,Siegel, Dionicio
, p. 192 - 196 (2013/08/23)
Methods for carbon-hydrogen (C-H) bond oxidation have a fundamental role in synthetic organic chemistry, providing functionality that is required in the final target molecule or facilitating subsequent chemical transformations. Several approaches to oxidizing aliphatic C-H bonds have been described, drastically simplifying the synthesis of complex molecules. However, the selective oxidation of aromatic C-H bonds under mild conditions, especially in the context of substituted arenes with diverse functional groups, remains a challenge. The direct hydroxylation of arenes was initially achieved through the use of strong Bronsted or Lewis acids to mediate electrophilic aromatic substitution reactions with super-stoichiometric equivalents of oxidants, significantly limiting the scope of the reaction. Because the products of these reactions are more reactive than the starting materials, over-oxidation is frequently a competitive process. Transition-metal-catalysed C-H oxidation of arenes with or without directing groups has been developed, improving on the acid-mediated process; however, precious metals are required. Here we demonstrate that phthaloyl peroxide functions as a selective oxidant for the transformation of arenes to phenols under mild conditions. Although the reaction proceeds through a radical mechanism, aromatic C-H bonds are selectively oxidized in preference to activated-H bonds. Notably, a wide array of functional groups are compatible with this reaction, and this method is therefore well suited for late-stage transformations of advanced synthetic intermediates. Quantum mechanical calculations indicate that this transformation proceeds through a novel addition-abstraction mechanism, a kind of 'reverse-rebound' mechanism as distinct from the common oxygen-rebound mechanism observed for metal-oxo oxidants. These calculations also identify the origins of the experimentally observed aryl selectivity.
Novel Bicyclic Pyridinones
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Page/Page column 69, (2012/10/08)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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Page/Page column 118-119, (2011/07/06)
The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
