85124-17-0

Usage

Chemical classification

Indole derivative, acetamide family

Potential applications

Pharmaceuticals, medicinal chemistry, drug discovery and development

Biological activities

Unknown, but of interest for further study

Structural properties

2,3-dioxo-2,3-dihydro-1H-indol-1-yl group attached to an acetamide functional group

Importance

Valuable compound for research and potential use in various industries

Upstream product

• 91-56-5 indole-2,3-dione 
• 79-07-2 Chloroacetamide 
• 683-57-8 bromo-acetic acid amide 
• 19612-82-9 2-(2,3-dioxoindolin-1-yl)acetyl chloride 

Downstream Products

• 1650570-71-0 (Z)-2-(3-(1,3-dimethyl-2,7-dioxo-3a,9a-diphenyl-1,2,3,3a,9,9a-hexahydroimidazo[4,5-e]thiazolo[3,2-b]-1,2,4-triazin-6(7H)-ylidene)-2-oxo-1,2-dihydro-3H-indolyl-1-)acetamide 

Relevant academic research and scientific papers

KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME

The invention is directed to a compound represented by the following structural formula pharmaceutically acceptable salts thereof: (I). Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.

Discovery of indolone acetamides as novel SV2A ligands with improved potency toward seizure suppression

(Chemical Equation Presented) Capitalizing on the proven clinical efficacy of levetiracetam as an antiepileptic drug, a drug discovery program lead to the identification of a new generation of SV2A ligands with equal or better tolerability profiles than levetiracetam, and improved potency toward seizure suppression in animal models.

Practical syntheses of oxindole derivatives: Chemical development towards 2-(5-chloro-2-oxo-2,3-dihydroindol-1-yl)acetamide and (S)-2-(5-Chloro-2-oxo-2,3- dihydroindol-1-yl)propionamide

We describe development of scalable syntheses of novel oxindole-type SV2A ligands with improved potency towards seizure suppression.

Reaction of isatin-1-acetamides with alkoxides: Synthesis of novel 1,4-dihydro-3-hydroxy-4-oxo-2-quinolinecarboxamides

The study of the reactivity of a series of isatin-1-acetamides with hot alkoxides is described. These reactions lead to 1,4-dihydro-3-hydroxy-4-oxo-2- quinolinecarboxamides as main products, and 3-hydroxy-2-oxindoles as well as other minor products. Exper

Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists

We report a novel chemical class of potent oxytocin receptor antagonists showing a high degree of selectivity against the closely related vasopressin receptors (Via, V1b, V2). An initial compound, 7, was shown to be active in an animal model of preterm labor when administered by the intravenous but not by the oral route. Stepwise SAR investigations around the different structural elements revealed one position, the arenesulfonyl moiety, to be amenable to structural changes. Consequently, this position was used to introduce a variety of substituents to improve the physicochemical properties. Some of the resulting analogues were found to be superior to 7 both in terms of potency in vitro and aqueous solubility, which translated into significantly improved efficacy in the animal model after intravenous and oral administration. The best compound, 73, potently inhibited oxytocin-induced uterine contractions in nonpregnant rats and reduced spontaneous uterine contractions in late-term pregnant rats.

Parallel synthesis of isatin-based serine protease inhibitors

The synthesis of N-functionalised isatins using parallel, solution synthesis is described. Functionalised polymers were employed as stoichiometric and catalytic reagents as well as purification media in the exercise, and the derivatives were screened against a panel of serine proteases; high percentage inhibition was observed in several cases. (C) 2000 Elsevier Science Ltd.

Isatine derivatives, and their method of use

A method of treatment of central nervous system disorders with compounds having the formula STR1 and isomers thereof wherein R 1, R 2, R 4, R 5, R 6, and R 7 and as defined in the specification; as well as pharmaceutical compositions thereof.

Isatine derivatives, their preparation and use

A method of treatment with compounds having the formula STR1 R 1 is hydrogen, C 1-6 -alkyl which may be branched, C 3-7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C 1-6 -alkoxy, CH 2 CO 2 R'' wherein R'' is hydrogen or C 1-6 -alkyl which may be branched, CH 2 CN, CH 2 CONR IV R V wherein R IV and R V independently are hydrogen or C 1-6 -alkyl, or CH 2 C( NOH)NH 2 ; R 2 is hydrogen, benzyl, C 1-6 -alkyl which may be branched, or C 3-7 -cycloalkyl; R 4, R 5, R 6, R 7 independently are hydrogen, C 1-6 -alkyl which may be branched, phenyl, halogen, C 1-6 -alkoxy, NO 2, CN, CF 3, OCF 3, or SO 2 NR""R''"" wherein R"" and R''"" independently are hydrogen, aralkoxy, aralkyl, or C 1-6 -alkyl; or R 6 and R 7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO 2, CF 3, CN, OCF 3, SO 2 NR"" R""'' wherein R"" and R""'' independently are hydrogen, aralkoxy, aralkyl, or C 1-6 -alkyl, and R 4 and R 5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel.The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.