- Nickel-Catalyzed Hydrodeoxygenation of Aryl Sulfamates with Alcohols as Mild Reducing Agents
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The nickel-catalyzed hydrodeoxygenation of aryl sulfamates has been developed with alcohols as mild reductants. A variety of functional groups and heterocycles were tolerated in this reaction system to give the desired products in high yields. In addition, the gram-scale process and stepwise cine-substitution were also achieved with high efficiency.
- Matsuo, Kasumi,Kuriyama, Masami,Yamamoto, Kosuke,Demizu, Yosuke,Nishida, Koyo,Onomura, Osamu
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p. 4449 - 4460
(2021/08/25)
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- Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitors
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p53-MDM2/MDMX interaction inhibitors represent the prospective agents for targeted anticancer therapy in tumors expressing wild-type p53 protein. Imidazoline-based MDM2-targeted inhibitors of such type, nutlins, contain halogen-substituted phenyl rings, w
- Bazanov, Daniil R.,Kopeina, Gelina S.,Lozinskaya, Natalia A.,Maksutova, Anita I.,Pervushin, Nikolay V.,Savin, Egor V.,Sosonyuk, Sergey E.,Tsymliakov, Michael D.
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p. 2216 - 2227
(2021/10/14)
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- Quinoline-based compound and selective androgen receptor agonist comprising the same
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Provided are a novel quinoline-based compound, a pharmaceutical composition containing the quinoline-based compound, and a method for producing the quinoline-based compound. The quinoline-based compound acts on an androgen receptor to increase activities of the androgen receptor, and thus can be favorably used as an agent for treating and preventing diseases or conditions, in which the increased activities of the androgen can lead to improvement of symptoms or the responsiveness to treatment, for example, various hormone-related diseases of the male or female, muscle-wasting disease, osteoporosis, and the like.COPYRIGHT KIPO 2016
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Paragraph 0505-0507
(2016/10/08)
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- Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
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The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
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Paragraph 2611
(2015/09/22)
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- Benzimidazole Derivatives, Compositions Containing Them, Preparation Thereof and Uses Thereof
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Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 11
(2008/12/08)
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- COMPOUNDS, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF III
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Compounds of Formula I, or pharmaceutically acceptable salts thereof: I (chemical formula to be inserted here - please see paper copy) wherein R1, R2, R3, R4, R5, R6 and G are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 18; 19
(2008/06/13)
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- Process for producing aromatic compound derivative by reaction of aromatic compound substituted with sulfamoyloxy, sulfinamoyloxy, or carbamoyloxy group, with nucleophilic agent
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A process for producing a compound represented by the following formula (I), which includes causing a compound represented by formula (II) to react with a nucleophilic agent: wherein X represents a substituent; R1 represents an electron-withdrawing substituent having a Hammett σp constant of more than 0; m represents an integer of 1 to 5; R2 represents a substituent; n represents an integer of 0 to 4; and m + n is from 1 to 5; wherein R1, m, R2, and n each have the same meanings to those in formula (I); R3 and R4 each independently represent an alkyl, aryl, or heterocyclic group; and Z represents C=O or S(O)p, wherein p is 1 or 2.
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Page/Page column 25; 26
(2008/06/13)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF
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Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 26-27
(2008/06/13)
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- Acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and their use as antiproliferative agents
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The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and methods of using the same as antiproliferative agents or to prevent apoptosis.
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- Synthesis and structure of 2-N,N-dimethyl- and 2-N,N-diethylsulfamoyl-1-(3-indolyl)-1,2-dihydroisoquinolines
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New sulfamoyl derivatives of (3-indolyl)-1,2-dihydroisoquinoline were prepared by reaction of isoquinoline and indole with sulfamoyl chlorides. The compounds were shown to exist in two isomeric forms by semiempirical quantum-chemical calculation in AMl ap
- Skrypnik,Vasil'eva,Lyashchuk,Bezrodnyi,Enya
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p. 577 - 580
(2007/10/03)
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- 8alpha-ACYLAMINO ERGOLINES AND USE AS PHARMACEUTICAL AGENTS
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8α-acylamino ergolines are useful dopamine agonists.
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- Preparation of 2-chloro-5-methyl-pyridine
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A process for the preparation of 2-chloro-5-methylpyridine of the formula STR1 which comprises reacting 3-methyl-pyridine-1-oxide of the formula STR2 with a chlorinating agent of the formula STR3 in which R1 represents alkyl, halogenoalkyl, cycloalkyl, optionally substituted aryl, NR2 R3 or OR4 in which R2 and R3 individually represent alkyl, cycloalkyl or aryl or together represent alkanediyl or oxaalkanediyl and R4 represents alkyl, cycloalkyl or optionally substituted aryl, in the presence of a basic organic nitrogen compound and in the presence of a diluent at a temperature between about -20° C. and +150° C.
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- N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same
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The case involves novel N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same. The N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidines are excellent eukalemic agents possessing diuretic and natriuretic properties.
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