- Regioselective C(sp3)-H alkylation of a fructopyranose derivative by 1,6-HAT
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Regioselective C(sp3)-H alkylation of a fructopyranose derivative using electron-deficient alkenes as alkylation reagents was achieved. The reaction proceededvia1,6-hydrogen atom transfer under photoredox iridium catalysis. Several functional g
- Li, Yanru,Miyamoto, Shoto,Torigoe, Takeru,Kuninobu, Yoichiro
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- Intramolecular C?H Amination of N-Alkylsulfamides by tert-Butyl Hypoiodite or N-Iodosuccinimide
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1,3-Diamines are an important class of compounds that are broadly found in natural products and are also widely used as building blocks in organic synthesis. Although the intramolecular C?H amination of N-alkylsulfamide derivatives is a reliable method for the construction of 1,3-diamine structures, the majority of these methods involve the use of a transition-metal catalyst. We herein report on a new transition-metal-free method using tert-butyl hypoiodite (t-BuOI) or N-iodosuccinimide (NIS), enabling secondary non-benzylic and tertiary C?H amination reactions to proceed. The cyclic sulfamide products can be easily transformed into 1,3-diamines. Mechanistic investigations revealed that amination reactions using t-BuOI or NIS each proceed via different pathways.
- Kiyokawa, Kensuke,Jou, Keisuke,Minakata, Satoshi
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supporting information
p. 13971 - 13976
(2021/08/30)
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- Catalytic Sulfamoylation of Alcohols with Activated Aryl Sulfamates
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We report a new catalytic method for alcohol sulfamoylation that deploys electron-deficient aryl sulfamates as activated group transfer reagents. The reaction utilizes the simple organic base N-methylimidazole, proceeds under mild conditions, and provides
- Rapp, Peter B.,Murai, Koichi,Ichiishi, Naoko,Leahy, David K.,Miller, Scott J.
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supporting information
p. 168 - 174
(2019/12/30)
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- BROMODOMAIN-INHIBITING COMPOUNDS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME FOR PREVENTING OR TREATING A CANCER
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Provided is a novel compound having bromodomain and extra terminal domain (BET) protein inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of precancerous transformation or cancer.
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Page/Page column 45
(2015/11/27)
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- p27 PROTEIN INDUCER
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The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G 1 , G 2 , G 3 and G 8 are each independently selected from -N= etc., Ring G 6 is selected from divalent aryl etc., A is selected from amino etc., G 4 is selected from oxygen etc., G 5 is selected from oxygen etc., G 7 is selected from -CH 2 - etc., and R 2 is selected from C 1-6 alkyl etc.
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Paragraph 1819-1823
(2016/10/08)
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- Novel Sulfonaminoquinoline Hepcidin Antagonists
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The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
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Page/Page column 158
(2012/09/05)
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- Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituent
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Design and synthesis of a series of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d] pyrimidines as potent and selective inhibitors of the mammalian target of rapamycin (mTOR) are described. Optimization of the 6-aryl substituent led to the discovery of inhibitors carrying 6-ureidophenyl groups, the first reported active site inhibitors of mTOR with subnanomolar inhibitory concentrations. The data presented in this paper show that 6-arylureidophenyl substituents led to potent mixed inhibitors of mTOR and phosphatidylinositol 3-kinase α (PI3K-α), whereas 6-alkylureidophenyl appendages gave highly selective mTOR inhibitors. Combination of 6-alkylureidophenyl groups with 1-carbamoylpiperidine substitution resulted in compounds with subnanomolar IC50 against mTOR and greater than 1000-fold selectivity over PI3K-α. In addition, structure based drug design resulted in the preparation of several 6-arylureidophenyl-1H-pyrazolo[3,4-d]pyrimidines, substituted in the 4-position of the arylureido moiety with water solubilizing groups. These compounds combined potent mTOR inhibition (IC50501 nM). 2009 American Chemical Society.
- Verheijen, Jeroen C.,Richard, David J.,Curran, Kevin,Kaplan, Joshua,Lefever, Mark,Nowak, Pawel,Malwitz, David J.,Brooijmans, Natasja,Toral-Barza, Lourdes,Zhang, Wei-Guo,Lucas, Judy,Hollander, Irwin,Ayral-Kaloustian, Semiramis,Mansour, Tarek S.,Yu, Ker,Zask, Arie
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supporting information; experimental part
p. 8010 - 8024
(2010/07/04)
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- THROMBIN INHIBITORS
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The present invention relates to a compound having formula I:and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagulants.
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- Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. 1wherein: Z is 2Q is selected from the group consisting of: 3—W— is 4—represents a carbon-carbon bond or does not exist; and A is NR13R14.
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(2010/02/05)
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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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- Thrombin inhibitors
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The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagula
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- Non-imidazole benzodiazepine inhibitors of farnesyl protein transferase
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Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof.
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- 3(5)-Heteroaryl substituted pyrazoles as p38 kinase inhibitors
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A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I
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(2008/06/13)
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- Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
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Compounds the formula STR1 their use as farnesyl transferase protein inhibitors and pharmaceutical compositions containing them are disclosed, especially compounds of the formula STR2 wherein R1, R2 and R3 are halo, A and B are each H2, and R is as defined in the specification.
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- Sulfanomide herbicides
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A compound having the formula STR1 wherein A is CR7 ; and R1 through R7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containi
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- Sulfamates as antiglaucoma agents
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Sulfamate esters of the formula where A is aryloxyalkyl, p is the number of unreacted hydroxy groups present on the alkyl moiety and may be zero, z is the number of --OS(O)2 NR1 R2 groups attached to carbons of the alkyl moiety and is always at least one; R1 and R2 are selected from hydrogen, loweralkyl, carboxy, and the like are useful in treating glaucoma.
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- Compounds having one or more aminosulfaonyloxy radicals useful as pharmaceuticals
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Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O) 2 NR 1 R 2 ] zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O) 2 NR 1 R 2 groups and is always at least one; R 1 and R 2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.
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- Sulfamidosulfonamide derivatives and herbicides
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A sulfamidosulfonamide derivative of the formula (1) and an agriculturally suitable salt thereof: STR1 wherein Q is STR2 X is an oxygen atom or a sulfur atom; and G is STR3 which are useful as herbicide.
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- Aryl and aryloxyalkyl sulfamate esters useful as anticonvulsants
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Herein disclosed is a method of treating convulsions with a pharmaceutical composition containing a compound of the formula: where A is an aryl, arylalkyl, or aryloxyalkyl group and is substituted on 1 or more carbon atoms with a sulfamate group (--OSO2 NR1 R2) wherein R1 and R2, same or different, are hydrogen or loweralkyl wherein p is 0 or 1 and is the number of untreated hydroxyl groups and z is 1 or 2 and is the number of --OS(O2)NR1 R2 groups. Aryl is selected from phenyl, substituted phenyl, pyridinyl, naphthyl, quinolinyl, and the like. Phenyl substituents are selected from hydrogen, halo, hydroxy, phenyl, phenoxy, benzoyl, loweralkyl, loweralkoxy, carboxy, amino, loweralkylamino, diloweralkylamino, acetamido, cyano, nitro, loweralkoxycarboyl, aminosulfonyl, imidazolyl, triazolyl, and the like. Novel compounds not previously disclosed are also described.
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- Preparation of sulfamyl halides
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Sulfamyl halides are prepared by reacting sulfamic acids with halogen in the presence of phosphorus or of a phosphorus trihalide; the sulfamic acid can first be prepared from an isocyanate or urea and then be reacted as above in a one-vessel method. The compounds obtainable by the process of the invention are valuable starting materials for the preparation of crop protection agents, dyes and drugs.
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- Thiaziridine 1,1-Dioxides
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Experiments towards a 1,3-elimination of hydrogen halides from α-chlorosulfonamides, α-bromosulfonamides, and N-chlorosulfonamides did not yield isolable thiaziridine 1,1-dioxides 4.Therefore, at -78 deg C, the diazoalkanes 10 were allowed to react with N-sulfonylamines 14 generated in situ by hydrogen chloride elimination from sulfamoylchlorides with triethylamine.If the work-up temperature was kept below -30 deg C, from tert-alkyldiazomethanes and tert-alkylsulfamoylchlorides the 2,3-di-tert-alkylthiaziridine 1,1-dioxides 4f - i were obtained in 32 - 47 percent yield.They form colorless, thermally labile crystals.Their structure was based on IR, UV and 1H-NMR spectra as well as on the quantitative thermal decomposition into sulfur dioxide and aldimines.The disubstituted diazomethanes 23 reacted with tert-butylsulfonylamine affording, besides N-tert-butylketimines (the decomposition products of intermediate trisubstituted thiaziridine 1,1-dioxides 21), tert-butylsulfinylamine 25 and ketones 26.The latter products presumably resulted from the cheletropic decomposition of the oxathiiranes 24.
- Quast, Helmut,Kees, Frieder
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p. 774 - 786
(2007/10/02)
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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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