354812-10-5

Upstream product

• 339365-14-9 1-(3-carbamoylthiophen-2-yl)urea 
• 14080-51-4 2-aminothiophene-3-carboxamide 
• 633309-16-7 5-bromo-2-[3-(2,2,2-trichloro-ethanoyl)-ureido]-thiophene-3-carboxylic acid amide 

Downstream Products

• 859809-34-0 5-(3-amino-phenylethynyl)-2-ureido-thiophene-3-carboxylic acid amide 
• 859809-22-6 5-[3-(tert-butyl-dimethyl-silanyloxy)-phenylethynyl]-2-ureido-thiophene-3-carboxylic acid amide 
• 728947-61-3 2-[(aminocarbonyl)amino]-5-(4-{[(2,2,2-trifluoroethyl)amino]methyl}phenyl)thiophene-3-carboxamide 
• 728947-63-5 2-[(aminocarbonyl)amino]-5-{4-[(bis-(2-methoxyethyl)amino)methyl]phenyl}thiopene-3-carboxamide 
• 494773-25-0 2-[(aminocarbonyl)amino]-5-[4-formylphenyl]thiophene-3-carboxamide 
• 728947-62-4 2-[(aminocarbonyl)amino]-5-{4-[(isopropylamino)methyl]phenyl}thiophene-3-carboxamide 
• 727741-81-3 2-[(aminocarbonyl)amino]-5-[2-{2-[{N-(2-chlorobenzyl)-N-methyl}amino]ethoxy}phenyl]thiophene-3-carboxamide 
• 869091-51-0 2-[(aminocarbonyl)amino]-5-(4-chlorobenzyl)thiophene-3-carboxamide 
• 1023699-90-2 cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-leucinate 
• 1023699-87-7 cyclopentyl N-{4-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-3-chlorobenzyl}-L-leucinate 
• 1023700-01-7 cyclopentyl N-(2-{4-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}ethyl)-L-leucinate 

Relevant academic research and scientific papers

Concise synthesis of tpca-1 and related thiophene-carboxamides by cross coupling

A synthesis of 5-substituted 2-[(aminocarbonyl)amino]-3-thiophene-carboxamides is described. The coupling reaction of 2-ureidothiophene-3-carboxamide and various aryl compounds allows the concise approach of promising candidates for IKK-2 inhibitor, such as TPCA-1.

IKK-β SERINE-THREONINE PROTEIN KINASE INHIBITORS

Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH-Y-L1-X1-(CH2)Z- wherein: z is 0 or 1; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non- natural alpha amino acid; Y is a bond, -C(=O)-, -S(=O)2-, -C(=O)O-, -C(=O)NR3-, - C(=S)-NR3, -C(=NH)-NR3 or -S(=O)2NR3- wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.

NF-:B INHIBITORS

The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I:B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor N

Novel Compounds

The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.