16694-18-1

Usage

Uses

Used in Pharmaceutical Industry:
2-Thiophenecarboxylic acid, 4-bromo-, is used as an intermediate for the synthesis of N-(4-Bromo-2-thienyl)-carbamic Acid 1,1-Dimethylethyl Ester (B688120), a compound with potential therapeutic applications.
Used in Enzyme Inhibition:
2-Thiophenecarboxylic acid, 4-bromo-, has been shown to have potency as a novel D-Amino Acid Oxidase (DAO) inhibitor. This makes it a promising candidate for the development of new drugs targeting DAO-related diseases and conditions.

Upstream product

• 3140-92-9 2,4-dibromothiophene 
• 109-72-8 n-butyllithium 
• 60-29-7 diethyl ether 
• 15719-64-9 methylammonium carbonate 
• 7209-11-2 2-acetyl-4-bromothiopene 
• 7311-66-2 3,4-dibromo-2-thiophenecarboxylic acid 
• 18791-75-8 4-Bromothiophen-2-aldehyde 
• 124-38-9 carbon dioxide 
• 3141-24-0 2,3,5-tribromothiophene 
• 74-96-4 ethyl bromide 
• 53317-05-8 3,4,5-tribromo-2-thiophene carboxylic acid 
• 7758-19-2 sodium chlorite 
• 62224-17-3 4-bromothiophene-2-carboxylic acid ethyl ester 
• 62224-16-2 4-bromothiophene-2-carboxylic acid methyl ester 

Downstream Products

• 872-31-1 3-Bromothiophene 
• 62224-16-2 4-bromothiophene-2-carboxylic acid methyl ester 
• 58777-65-4 4-Bromothiophene-2-carboxylic acid chloride 
• 666721-06-8 4-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxylic acid 
• 666721-04-6 4-[4-(trifluoromnethoxy)phenyl]thiophene-2-carbonyl chloride 
• 666721-21-7 4-(4-Hydroxyphenyl)-N-(2-morpholin-4-ylethyl)thiophene-2-carboxamide 
• 820223-49-2 (R)-{[4-(4-trifluoromthoxyphenyl)thien-2-yl]carboxamido}(phenyl)propanoic acid 
• 666721-23-9 4-(5-{[(2-Morpholin-4-ylethyl)amino]carbonyl}thien-3-yl)phenyl trifluoromethanesulphonate 
• 666721-60-4 trans-4-({[4-(4-trifluoromethoxyphenyl)thien-2-yl]-carboxamido}methyl)cyclohexanecarboxylic acid 
• 237384-71-3 Methyl 4-(4-phenyl-1,3-thiazol-2-yl)thiophene-2-carboxylate 
• 77133-27-8 4-methoxythiophene-2-carboxylic acid 
• 66938-33-8 (4-bromo-2-thienyl)(4-methoxyphenyl)methanone 
• 111690-61-0 (3-bromo-2-thienyl)(4-methoxyphenyl)methanone ethylene ketal 
• 111690-62-1 (4-trifluoroacetyl-2-thienyl)(4-methoxyphenyl)methanone hydrate 

Relevant academic research and scientific papers

COMPOSITIONS AND METHODS OF TARGETING MUTANT K-RAS

Compounds and compositions are presented that inhibit K-Ras, and especially mutant K-Ras. Certain compounds preferentially or even selectively inhibit specific forms of mutant K-Ras, and particularly the G12D mutant form.

SUBSTITUTED (THIOPHENYL-CARBONYL)IMIDAZOLIDINONES, AND USE THEREOF

The present invention relates to novel substituted (thiophenyl-carbonyl)imidazolidinones, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.

Direct bromination of ethyl 5-alkylthiophene-2-carboxylates

Approaches to brominated thiophene-2-carboxylic acids by electrophilic bromination of the corresponding acids and esters were compared and investigated. A synthetic route was developed involving direct bromination of ethyl 5-alkylthiophene-2-carboxylates followed by saponification of the resulting ethyl 5-alkyl-4-bromothiophene-2-carboxylates. The key bromination step is selective in dichloromethane solution at 0-5 °C and furnishes the corresponding ethyl 5-alkyl-4-bromothiophene-2-carboxylates in excellent yields. No migration or isomerization of the alkyl substituents was observed. Georg Thieme Verlag Stuttgart New York.

AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors

A new class of MMP-12 inhibitors was discovered and optimized using structure-based drug design methods. Modeling studies using a known MMP-12 crystal structure identified a new interaction mode for these new MMP-12 inhibitors. Further optimization resulted in the discovery of a compound displaying nanomolar activity against MMP-12 and which was co-crystallized with MMP-12.

BIARYL LINKED HYDROXAMATES: PREPARATION AND PHARMACEUTICAL APPLICATIONS

The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to biaryl containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities. Formula (I), where Z is a single bond or C1-C4 hydrocarbon, A is an aromatic ring, B is an aromatic ring.

Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions

Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.

Novel thiophene derivatives, their process of preparation and the pharmaceutical compositions which comprise them

A compound of formula (I) selected from: wherein: X represents oxygen or sulphur, Y represents oxygen, —NH— or —N(C1-C6)alkyl-, Ra represents hydrogen, halogen, (C1-C3)alkyl, hydroxyl or (C1-C3)alkoxy, Rb represents hydrogen, halogen or (C1-C3)alkyl, A represents phenyl, pyridyl, (C5-C6)cycloalkyl or (C5-C6)cycloalkenyl, R1 and R2 each represent a group selected from hydrogen, halogen, cyano, nitro, haloalkyl, haloalkoxy, alkyl, alkenyl, alkynyl, —OR4, —NR4R5, —S(O)nR4, —C(O)R4, —CO2R4, —O—C(O)R4, —C(O)NR4R5, —NR5—C(O)R4, —NR5—SO2R4, -T-CN, -T-OR4, -T-OCF3, -T- NR4R5, -T-S(O)nR4, -T-C(O)R4, -T-CO2R4, -T-O—C(O)R4, -T-C(O)NR4R5, -T-NR4—C(O)R5, -T-NR4—SO2R5, —R6 and -T-R6 in which n, T, R4, R5 and R6 are as defined in the description, R3 represents an —R7 or —U—R11 group in which R7 represents hydrogen, alkyl, aryl, cycloalkyl or heterocycle, U represents a linear or branched alkylene chain and R11 is defined in the description, their optical isomers or their addition salts with a pharmaceutically acceptable acid or base, and their use as inhibitor of metalloproteinase and more specifically of metalloproteinase-12.

ISOQUINOLINONE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS

This invention is directed to isoquinolinone derivatives and their use in modulating the activity of orphan nuclear receptors, pharmaceutical compositions containing such derivatives, and methods of using such derivatives in treating disease-states associ

NOVEL THIOPHENE AMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS

Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.