cas 81363-76-0, Isopropylsulfonamide | Articles data

Articles about 81363-76-0Total 21 be found

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Development of succinimide-based inhibitors for the mitochondrial rhomboid protease PARL
While the biochemistry of rhomboid proteases has been extensively studied since their discovery two decades ago, efforts to define the physiological roles of these enzymes are ongoing and would benefit from chemical probes that can be used to manipulate the functions of these proteins in their native settings. Here, we describe the use of activity-based protein profiling (ABPP) technology to conduct a targeted screen for small-molecule inhibitors of the mitochondrial rhomboid protease PARL, which plays a critical role in regulating mitophagy and cell death. We synthesized a series of succinimide-containing sulfonyl esters and sulfonamides and discovered that these compounds serve as inhibitors of PARL with the most potent sulfonamides having submicromolar affinity for the enzyme. A counterscreen against the bacterial rhomboid protease GlpG demonstrates that several of these compounds display selectivity for PARL over GlpG by as much as two orders of magnitude. Both the sulfonyl ester and sulfonamide scaffolds exhibit reversible binding and are able to engage PARL in mammalian cells. Collectively, our findings provide encouraging precedent for the development of PARL-selective inhibitors and establish N-[(arylsulfonyl)oxy]succinimides and N-arylsulfonylsuccinimides as new molecular scaffolds for inhibiting members of the rhomboid protease family.
Andrews, Charlotte L.,Cardozo, Joaquin M.,Chow, Alyssa S.,Crainic, Jennifer A.,Parsons, William H.,Rutland, Nicholas T.,Sheehan, Brendan K.
supporting information

(2021/08/04)

Primary Sulfonamide Synthesis Using the Sulfinylamine Reagent N-Sulfinyl- O-(tert-butyl)hydroxylamine, t-BuONSO
Sulfonamides have played a defining role in the history of drug development and continue to be prevalent today. In particular, primary sulfonamides are common in marketed drugs. Here we describe the direct synthesis of these valuable compounds from organometallic reagents and a novel sulfinylamine reagent, t-BuONSO. A variety of (hetero)aryl and alkyl Grignard and organolithium reagents perform well in the reaction, providing primary sulfonamides in good to excellent yields in a convenient one-step process.
Davies, Thomas Q.,Hall, Adrian,Skolc, David,Tilby, Michael J.,Willis, Michael C.
supporting information
p. 9495 - 9499
(2020/12/21)

THIAZOLIDINONE COMPOUNDS AND USE THEREOF
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
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Paragraph 0054; 0383-0384; 0393-0394

(2017/09/21)

CYCLOPROPYL FUSED INDOLOBENZAZEPINE HCV NS5B INHIBITORS
The invention encompasses compounds of formula (I) as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV
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Page/Page column 111

(2009/06/27)

Mild and general method for the synthesis of sulfonamides
Reaction of methyl sulfinates with lithium amides followed by 3-chloroperoxybenzoic acid oxidation of the resulting sulfinamides provides primary, secondary, and tertiary alkane-, arene-and heteroarenesulfonamides in high yields. This constitutes a mild and facile experimental protocol that avoids the use of hazardous, unstable, or volatile reagents and does not affect the configurational stability of the amines. Georg Thieme Verlag Stuttgart.
Garcia Ruano, Jose Luis,Parra, Alejandro,Yuste, Francisco,Mastranzo, Virginia M.
p. 311 - 319
(2008/12/22)

PYRIDAZINONE COMPOUNDS
The invention is directed to pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
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Page/Page column 166-167

(2008/12/07)

BENZIMIDAZOLONE CHYMASE INHIBITORS
Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.
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Page/Page column 145

(2009/01/20)

QUINOXALINE COMPOUNDS AND USE THEREOF
The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
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Page/Page column 87-88

(2008/12/08)

Compounds for the Treatment of Hepatitis C
The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 99

(2008/12/07)

Analogs of isovaleramide, a pharmaceutical composition including the same, and a method of treating central nervous system conditions or diseases
An isovaleramide analog having at least one of an increased potency, an increased half-life, and an increased stability compared to isovaleramide. The isovaleramide analog is a cyclic analog or a noncyclic analog. The isovaleramide analog is formulated into a pharmaceutical composition. A method of treating a central nervous system condition or disease is also disclosed. The method comprises administering an isovaleramide analog to a patient suffering from the central nervous system condition or disease.
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Page/Page column 7

(2010/02/15)

Biaryl sulfonamides and methods for using same
The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.
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Page/Page column 52

(2010/02/12)

HETEROCYCLIC COMPOUND DERIVATIVES AND MEDICINES
The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition comprising a compound represented by the following formula [1]: (R1 and R2 are the same or different and each represents optionally substituted aryl, Y represents N or CH, Z represents N or CH, A represents NH, NR5, O, S, or ethylene, R5 represents alkyl, D represents alkylene or alkenylene, E represents phenylene or single bond, G represents O, S, or CH2, R3 and R4 are the same or different and each represents hydrogen or alkyl, Q represents carboxy, alkoxycarbonyl, tetrazolyl, carbamoyl, or N-(alkylsulfonyl)carbamoyl), or a pharmaceutically acceptable salt thereof as an active ingredient.
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Page 31

(2010/02/05)

A reversible safety-catch method for the hydrogenolysis of N-benzyl moieties
The benzyl groups of β-hydroxy-N-benzyl sulfonamides are labile toward hydrogenolysis-unlike N-benzyl sulfonamides lacking the β-hydroxy moiety. We find that N-acyl-N-benzyl sulfonamides undergo hydrogenolysis under very mild conditions. Based upon these observations, we developed a reversible safety-catch method using tert-butoxycarbonyl moieties to activate N-benzyl sulfonamides toward hydrogenolysis. We also explored the utility of the safety-catch activation method for other nitrogen-based functionality such as N-benzyl carboxamides, imides, and related functionality.
Johnson II, David C.,Widlanski, Theodore S.
p. 8483 - 8487
(2007/10/03)

Anti-viral compounds
PCT No. PCT/US98/01030 Sec. 371 Date Jul. 2, 1999 Sec. 102(e) Date Jul. 2, 1999 PCT Filed Jan. 20, 1998 PCT Pub. No. WO98/31363 PCT Pub. Date Jul. 23, 1998The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof. These compounds inhibit the growth of piconaviruses, such as rhinoviruses, Hepatitus viruses, cardioviruses, polioviruses, enteroviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus.
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(2008/06/13)

SUBSTITUTED PHTHALAZINONES AS NEUROTENSIN ANTAGONISTS
Novel substituted phthalazinones of the formula (I) STR1 are useful as neurotensin antagonists.
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(2008/06/13)

Die elektrochemische fluorierung von alkansulfonamiden und alkandisulfonamiden
Alkane sulphonylamides and disulphonylamides are stable in anhydrous (HF)x and undergo quantitative fission of S-N bonds during electrochemical fluorination. Besides NF3, the corresponding perfluoroalkane sulphonyl fluorides and disulphonyl fluorides are formed.
Satori,Juenger
p. 71 - 75
(2007/10/03)

METHODS OF TREATING CARDIAC ARRHYTHMIA
Benzodiazepine analogs have been found to be useful in treating cardiac abnormalities.
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(2008/06/13)

Benzodiazepine derivatives, compositions containing them and their use in therapy
Compounds of formula (I), and salts and prodrugs thereof wherein: R1 represents optionally substituted C? ??alkyl or C???cycloalkyl; R2 represents an optionally substituted phenyl or pyridyl group; R3 represents C??? alkyl or halo; R? represents C??? cycloalkyl; X is 0, 1, 2 or 3; are CCK and/or gastrin antagonists. They and compositions thereof are therefore useful in therapy.
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(2008/06/13)

Herbicidal substituted benzoylsulfonamides
Compound of the formula STR1 in which A is O, S, or NR3 ; G is CH or N; R and R1 are independently alkyl, alkoxy, haloalkoxy or alkylamino; R2 is phenyl, substituted phenyl, alkyl, cycloalkyl, haloalkyl or --CH2 [(R4)C(R5)n --Z; R3 and R7 are, independently, hydrogen, alkyl, --C(O)NH2 or --C(O)alkyl; R4 and R5 are independently hydrogen, alkyl, or halogen; R6 is halogen, alkyl, alkoxy, haloalkoxy, NO2, amino, alkyl substituted amino, or acyl substituted amino; n is 0 to 5; Z is cyano, amino, alkylamino, dialkylamino, --NHCO2 alkyl, alkoxy, alkylthio, alkylsulfonyl, alkenyl, alkynyl, phenyl or substituted phenyl; and Q is hydrogen, halogen, alkyl, alkoxy, haloalkoxy, nitro, amino, haloalkyl, alkythio, alkylsulfonyl, phenyl, substituted phenyl or phenoxy; or a 5 or 6 membered aromatic heterocycle having the formula STR2 in which "m" is 0 or 1; A' is O, S, or NR7 ; and X, X', Y, Y', W, W', V, V', U and Z' are independently N, O, S, --CH-- or --CR6. Intermediates for preparation of the benzoylsulfonamides are also disclosed.
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(2008/06/13)

Preparation of amidosulfonic acids
Amidosulfonic acids are prepared by reacting ureas with oleum of a particular composition, first at a low temperature and then at a higher temperature, in the presence of an organic solvent. The products are starting materials for the preparation of dyes and pesticides.
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(2008/06/13)

Manufacture of amidosulfonic acids
Amidosulfonic acids are manufactured by reacting Schiff bases first with sulfur trioxide and then with water. The compounds obtainable by the process of the invention are sweeteners (especially in the case of cyclohexylamidosulfonic acid and its calcium, sodium and potassium salts), and valuable starting materials for the manufacture of sweeteners, dyes and pesticides.
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(2008/06/13)

Chemical Properties

Melting Point: 61-65 °C(Solv: chloroform (67-66-3); carbon tetrachloride (56-23-5))
Boiling Point: 216.5 °C at 760 mmHg
Flash Point:84.7 °C
Density: 1.194 g/cm³
Storage Temp.:Sealed in dry,Room Temperature
Vapor Pressure: 0.14mmHg at 25°C
Refractive Index: 1.461
PKA: 10.69±0.60(Predicted)
PSA: 68.54000
LogP: 1.46440

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Chemical Properties

Melting Point: 61-65 °C(Solv: chloroform (67-66-3); carbon tetrachloride (56-23-5))

Boiling Point: 216.5 °C at 760 mmHg

Flash Point:84.7 °C

Density: 1.194 g/cm³

Storage Temp.:Sealed in dry,Room Temperature

Vapor Pressure: 0.14mmHg at 25°C

Refractive Index: 1.461

PKA: 10.69±0.60(Predicted)

PSA: 68.54000

LogP: 1.46440

Global suppliers and manufacturers of 81363-76-0total 42 suppliers on LookChem

Article Database

81363-76-0

Articles about 81363-76-0Total 21 be found

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Chemical Properties

Melting Point: 61-65 °C(Solv: chloroform (67-66-3); carbon tetrachloride (56-23-5))

Boiling Point: 216.5 °C at 760 mmHg

Flash Point:84.7 °C

Density: 1.194 g/cm3

Storage Temp.:Sealed in dry,Room Temperature

Vapor Pressure: 0.14mmHg at 25°C

Refractive Index: 1.461

PKA: 10.69±0.60(Predicted)

PSA: 68.54000

LogP: 1.46440

Global suppliers and manufacturers of 81363-76-0total 42 suppliers on LookChem

Density: 1.194 g/cm³