476615-23-3

Upstream product

• 39787-83-2 2-methoxy-4-nitrobenzoyl chloride 
• 100-36-7 N,N-diethylethylenediamine 
• 39106-79-1 methyl 2-methoxy-4-nitrobenzoate 
• 39614-82-9 2-hydroxy-4-nitrobenzoyl chloride 
• 2597-56-0 4-nitro-o-anisic acid 
• 108-00-9 N,N-dimethylethylenediamine 

Downstream Products

• 848771-79-9 N-(2-diethylamino-ethyl)-2-methoxy-4-methylamino-benzamide 
• 3761-48-6 1112JDO 

Relevant academic research and scientific papers

Synthesis of N-(2-diethylamino-ethyl)-4-(4-fluoro-benzamido)-2-methoxybenzamide (desiodo-MIP-1145) by coupling technique and its radioiodination: a potential melanoma imaging agent

Radioiodinated MIP-1145, which specifically targets melanin, is an ideal candidate for targeted therapy of melanoma. An analogue of MIP-1145 lacking the iodo-substituent (desiodo-MIP-1145) was synthesized as a labeling precursor in three simple steps. The radioiodination of desiodo-MIP-1145 by iodine-125 was carried out via an electrophilic substitution reaction. An optimization study for the iodination reaction was carried out. The labeled compound was isolated and purified by means of electrophoresis and HPLC. The maximum radiochemical yield, 76%, was obtained with radiochemical purity greater than 99%. The log P value for [125I]MIP-1145 was measured as 4.5.

RADIOHALOGENATED BENZAMIDE DERIVATIVES AND THEIR USE IN TUMOR DIAGNOSIS AND TUMOR THERAPY

This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.

Radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy

This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.

4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists

Synthesis, in vitro biological evaluation and structure-activity relationships of novel hMCH1R-antagonists are disclosed. The nature of the amine side chains could be varied considerably in contrast to the central benzamide scaffold and aromatic substituents.

NOVEL BENZAMIDE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS

Novel compounds of Formula I which modulate MCH activity are disclosed, in which A is a linker, Ar, is an aryl or heteroaryl group; R1 is hydrogen or a lower alkoxy group; Q together with the carbonyl forms an amide group, which is further substituted with an amine group; R5 is hydrogen, halogen atoms, alkoxy groups, hydroxy, alkylamino groups, dialkylamino groups, hydroxylalkyl groups, carboxamido groups, acylamido groups, acyl groups,-CHO, nitrile, alkyl, alkenyl or alkynyl groups,-SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as-CH2CF3,-CF2CF3,-CF3,-OCF3,-SCF3;-SO2NH2,-SO2NHAlk,-SO2NAlk2,-SO2AIk; R8 is hydrogen, halogen atoms, alkyl, alkenyl or alkynyl groups, cycloalkyl groups, alkylcycloalkyl groups, alkoxy groups, dialkylamino groups,-CONHAIk,-CONAIk2,-NHCO-Alk,-CO-Alk,-SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as-CH2CF3,-CF2CF3,-CF3,-OCF3,-SCF3; X is H, F, Cl, Br, I,-SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as-CH2CF3,-CF2CF3,-CF3,-OCF3,-SCF3; OCH3 or lower alkyl or alkenyl group; and which are useful in the treatment or prevention of e.g. obesity, depression, diabetes, bulimia etc.

Drug evolution concept in drug design: 1. Hybridization method

A novel concept, "drug evolution", is proposed to develop chemical libraries that have a high probability of finding drugs or drug candidates. It converts biological evolution into chemical evolution. In this paper, we present "hybridization" drug evolution, which is the equivalent of sexual recombination of parental genomes in biological evolution. The hybridization essentially shuffles the building blocks of the parent drugs and ought to drug(s); no drug evolution can otherwise occur. We hybridized two drugs, benzocaine and metoclopramide and generated 16 molecules that include the parent drugs, four known drugs, and two molecules whose therapeutic activities are reported. The unusually high number of drugs and drug candidates in the library encourages high expectations of finding new drug(s) or drug candidate(s) within the remaining eight compounds. Interestingly, the therapeutic applications of the eight drugs or drug candidates in the library are fairly diverse as 38 therapeutic applications and 25 molecular targets are counted. Therefore, the library fits as a general chemical library for unspecified therapeutic activities. The hybridization of other two drugs, aspirin and cresotamide, is also described to demonstrate the generality of the method.

NOVEL METHOXYBENZAMIDE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS

Novel compounds of Formula (I) which modulate MCH activity are disclosed, in which A is a linker; Ar1 is an aryl or heteroaryl group; R1 is a lower alkoxy group; R2 is an R1 group or hydrogen, an OH or an NH2 group, Q together with the carbonyl forms an amide group, which is further substituted with an amine group; R5 is selected from hydrogen, halogen atoms, alkoxy groups, hydroxy, alkylamino groups, dialkylamino groups, hydroxylalkyl groups, carboxamido groups, acylamido groups, acyl groups, -CHO, nitrile, alkyl, alkenyl or alkynyl groups, -SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as -CH2CF3, -CF2CF3, -CF3, -OCF3, -SCF3; -SO2NH2, -SO2NHAlk, -SO2NAlk2, -SO2Alk; X is H, F, Cl, Br, I, -SCH3, -CF3, -OCF3, -SCF3, OCH3, or lower alkyl or alkenyl group; R8 is halogen atoms, alkyl, alkenyl or alkynyl groups, cycloalkyl groups, aryl groups, heteroaryl groups, heterocyclyl groups, alkylcycloalkyl groups, alkylaryl groups, alkylheterocyclyl groups, alkylheteroaryl groups, arylalkoxy groups, aryloxy groups, alkoxy groups, dialkylamino groups, -CONHAlk, -CONHAr, -CONAlk2, -NHCO-Alk, -NHCO-Ar, -CO-Alk, -CO-Ar, -SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups; or R8 is R6-Ar2-B-, in which B is a single bond or a connecting moiety; Ar2 is an Ar1 group; R6 is an R5 group; and which are useful in the treatment or prevention of e.g. obesity, depression, diabetes, bulimia etc.