92952-46-0

Usage

Uses

Used in Pharmaceutical Industry:
6,78,9 TETRAHYDROBEZ(G) ISATIN is used as an antitubercular agent for its potential to combat tuberculosis, a significant global health concern.
6,78,9 TETRAHYDROBEZ(G) ISATIN is used as an anti-inflammatory agent for its capacity to reduce inflammation, which can be beneficial in treating various inflammatory conditions.
6,78,9 TETRAHYDROBEZ(G) ISATIN is used as an analgesic agent for its pain-relieving properties, offering a potential alternative for managing pain in different clinical scenarios.
Used in Antimicrobial Applications:
6,78,9 TETRAHYDROBEZ(G) ISATIN is used as an antimicrobial agent for its potential to inhibit the growth of microorganisms, which could be instrumental in developing new antibiotics to address the growing issue of antibiotic resistance.
Used in Anticancer Applications:
6,78,9 TETRAHYDROBEZ(G) ISATIN is used as an anticancer agent for its potential to target and inhibit the growth of cancer cells, offering a new avenue for cancer treatment and research.
6,78,9 TETRAHYDROBEZ(G) ISATIN's unique structure and the breadth of its potential applications highlight its importance in the ongoing pursuit of innovative pharmaceutical solutions.

Upstream product

• 92952-47-1 C₁₂H₁₄N₂O₂ 
• 2217-41-6 1-amino-5,6,7,8-tetrahydronaphthalene 
• 92952-47-1 hydroxyimino-acetic acid-(5,6,7,8-tetrahydro-[1]naphthylamide) 
• 79-37-8 oxalyl dichloride 
• 6271-86-9 5-aminotetralin hydrochloride 

Downstream Products

• 110536-50-0 Benzoic acid [2-oxo-1,2,6,7,8,9-hexahydro-benzo[g]indol-(3E)-ylidene]-hydrazide 
• 924633-94-3 3-acetylamino-2-(4-chloro-benzyl)-7,8,9,10-tetrahydro-benzo[h]quinoline-4-carboxylic acid 
• 851546-73-1 2-(3,4-Dichlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid 
• 851546-71-9 3-Hydroxy-2-(4-trifluoromethoxy-benzyl)-7,8,9,10-tetrahydro-benzo[h]quinoline-4-carboxylic acid 
• 851546-61-7 2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid 
• 1067187-34-1 3-hydroxy-2-(2-phenylpropan-2-yl)-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid 
• 1067187-45-4 3-hydroxy-2-(1-phenylethyl)-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid 
• 1067186-60-0 3-hydroxy-2-(1-phenylcyclopropyl)-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid 
• 721942-75-2 1-amino-5,6,7,8-tetrahydro-[2]naphthoic acid 
• 924633-93-2 3-amino-2-(4-chloro-benzyl)-7,8,9,10-tetrahydro-benzo[h]quinoline-4-carboxylic acid 

Relevant academic research and scientific papers

Discovery of 2-[1-(4-Chlorophenyl)cyclopropyl]-3-hydroxy-8- (trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury

Previously, we reported the discovery of PSI-697 (1a), a C-2 benzyl substituted quinoline salicylic acid-based P-selectin inhibitor. It is active in a variety of animal models of cardiovascular disease. Compound 1a has also been shown to be well tolerated and safe in healthy volunteers at doses of up to 1200 mg in a phase 1 single ascending dose study. However, its oral bioavailability was low. Our goal was to identify a back up compound with equal potency, increased solubility, and increased exposure. We expanded our structure-activity studies in this series by branching at the α position of the C-2 benzyl side chain and through modification of substituents on the carboxylic A-ring of the quinoline. This resulted in discovery of PSI-421 with marked improvement in aqueous solubility and pharmacokinetic properties. This compound has shown oral efficacy in animal models of arterial and venous injury and was selected as a preclinical development compound for potential treatment of such diseases as atherosclerosis and deep vein thrombosis.

Methods and Compositions for Treatment of Scleritis and Related Disorders

The present teachings relate to the field of anti-inflammatory substances and more particularly to compounds that are useful for the treatment of scleritis, a scleritis symptom, or a scleritis-related disorder. In one aspect, methods of treating scleritis, a scleritis symptom, or a scleritis-related disorder generally include administering to a subject a compound of Formula I: or a pharmaceutically acceptable salt, hydrate or ester thereof, wherein W1, W2, R1, L, X, Y, Z, and n1 are defined as described herein.

Methods and Compositions for Selectin Inhibition

The present teachings relate to novel compounds of formula I: wherein the constituent variables are as defined herein. Compounds of the present teachings can act as antagonists of the mammalian adhesion proteins known as selecting. Methods for treating or preventing selectin-mediated disorders are provided, which include administration of these compounds in a therapeutically effective amount.

2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H] quinoline-4-carboxylic acid (PSI-697): Identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists

P-selectin-PSGL-1 interaction causes rolling of leukocytes on the endothelial cell surface, which subsequently leads to firm adherence and leukocyte transmigration through the vessel wall into the surrounding tissues. P-selectin is upregulated on the surface of both platelets and endothelium in a variety of atherosclerosis-associated conditions. Consequently, inhibition of this interaction by means of a small molecule P-selectin antagonist is an attractive strategy for the treatment of atherosclerosis. High-throughput screening and subsequent analoging had led to the identification of compound 1 as the lead candidate. Herein, we report the continuation of this work and the discovery of a second-generation series, the tetrahydrobenzoquinoline salicylic acids. These compounds have improved pharmacokinetic properties, and a number of them have shown oral efficacy in mouse and rat models of atherogenesis and vascular injury. The lead 31 (PSI-697), is currently in clinical development for the treatment of atherothrombotic vascular events.

Methods and compositions for selectin inhibition

The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compound of Formula I: wherein the constituent variables are defined herein.

Condensed indoline derivatives and their use as 5HT, in particular 5HT2c, receptor ligands

A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

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.

Hydrazone derivatives and their use

A method of antagonizing the biological effects of an excitatory amino acid of a subject in need of such antagonization, comprising the step of administering to said subject an effective excitatory amino acid antagonizing amount of an indole-2,3-dione-3-h