199850-56-1

Usage

Uses

Used in Pharmaceutical Research and Development:
BENZOIC ACID, 2-AMINO-4-CHLORO-5-IODO-, METHYL ESTER is used as a key intermediate in the synthesis of pharmaceutical compounds for various therapeutic applications. Its unique structure allows for the development of new drugs with specific targeting and therapeutic properties.
Used in Organic Synthesis:
In the field of organic synthesis, BENZOIC ACID, 2-AMINO-4-CHLORO-5-IODO-, METHYL ESTER serves as a building block for the creation of complex organic molecules. Its reactivity and functional groups make it a versatile component in the synthesis of a wide range of organic compounds.
Used in Medicinal Chemistry:
BENZOIC ACID, 2-AMINO-4-CHLORO-5-IODO-, METHYL ESTER is employed in medicinal chemistry for the design and synthesis of novel drug candidates. Its potential applications in the development of new drugs and medical treatments highlight its importance in advancing pharmaceutical research and innovation.

Upstream product

• 5900-58-3 2-amino-4-chloro-benzoic acid methyl ester 
• 147778-06-1 2-acetylamino-4-chlorobenzoic acid methyl ester 
• 717879-44-2 methyl 2-amino-4-tert-butylbenzoate 

Downstream Products

• 199861-83-1 4-chloro-2-[2-(3,5-dimethylphenyl)-acetylamino]-5-iodo-benzoic acid methyl ester 
• 199850-51-6 4-chloro-2-[2-(5-chlorothiophen-2-yl)-acetylamino]-5-iodo-benzoic acid methyl ester 
• 671232-87-4 methyl 4-chloro-5-iodo-2-N-(3,4,5-trimethylphenyl)acetylaminobenzoate 
• 540501-04-0 2-amino-4-chloro-5-iodobenzoic acid 
• 335293-21-5 methyl 2-N-acetylamino-4-chloro-5-iodobenzoate 

Relevant academic research and scientific papers

A targeted delivery strategy for the development of potent trypanocides

A new drug delivery strategy was investigated for the development of potent anti-parasitic compounds against Trypanosoma brucei, the causative agent of African sleeping sickness. Thus, potent in vitro hexokinase inhibitors were rendered cytotoxic by appending a tripeptide peroxosomal targeting sequence that facilitated delivery of the molecular cargo to the appropriate organelle in the parasite.

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

A series of potent quinazolinedione sulfonamide antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor were designed and synthesized. The structure–activity relationships (SAR) and in vivo activity of the series were investigated. In particular, compound 1 S (selurampanel; N-[7-isopropyl-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1H-quinazolin-3-yl]methanesulfonamide) has shown excellent oral potency against maximal electroshock seizure (MES)-induced generalized tonic–clonic seizures in rodents as well as significant activity in patients suffering from various forms of epilepsy. The X-ray crystal structure of selurampanel bound to the AMPA receptor hGluA was also obtained.

INHIBITORS OF KRAS G12C

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

QUINOLINONE DERIVATIVES

The present invention relates to compounds of the formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds as activators of AMPK.

5, 7-DIHYDRO- 6H-PYRIMIDO [ 5, 4-D] [ 1 ] BENZAZEPIN-6-THIONES AS PLK INHIBITORS

This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

BENZIMIDAZOLE QUINOLINONES AND USES THEREOF

Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.

Synthesis of two non-peptidyl GnRH receptor antagonists via [ 14C]carbonylation

In support of a program to develop a new gonadotropin releasing hormone (GnRH) receptor antagonist, two 14C labelled candidate tracers, 14C-1 and 14C-2, were synthesized for utilization in metabolism studies. A slight modi

A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor

Extensive development of the structure - activity relationships of a screening lead determined three important pharmacophores for gonadotropin-releasing hormone (GnRH) receptor antagonist activity. Incorporation of the 3,4,5-trimethylphenyl group at the 3

Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.

Quinolones as gonadotropin releasing hormone (GnRH) antagonists: Simultaneous optimization of the C(3)-aryl and C(6)-substituents

A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3,4,5-trimethylphenyl substituent (23h) was found to be optimal. (C) 2000 Elsevier Science Ltd. All rights reserved.