453560-57-1

Upstream product

• 54962-75-3 [3-bromo-5-(trifluoromethyl)phenyl]amine 
• 121-01-7 4-nitro-2-trifluoromethyl-aniline 
• 400-66-8 2-bromo-4-nitro-6-trifluoromethylaniline 
• 108761-81-5 2-bromo-4-amino-6-trifluoromethylaniline 
• 1431291-92-7 2-bromo-4-acetamido-6-trifluoromethylaniline 
• 31951-12-9 4-tert-butyl-3-nitro-phenylamine 
• 108-24-7 acetic anhydride 

Downstream Products

• 453560-58-2 XI-N-[3-(3-piperidin-1-yl-propyl)-5-trifluoromethyl-phenyl]-acetamide 
• 1135493-45-6 N-[3-(3-morpholin-4-yl-propyl)-5-trifluoromethyl-phenyl]-acetamide 
• 337535-60-1 N-[4'-[1-hydroxy-2-methyl-1-(1-trityl-1H-imidazol-4-yl)propyl]-5-(trifluoromethyl)-[1,1'-biphenyl]-3-yl]acetamide 
• 1451065-57-8 C₇H₃BrF₃O₃S^(1-)*K⁽¹⁺⁾ 
• 1451065-56-7 2-bromo-4-acetamido-6-trifluoromethybenzenesulfonic acid 
• 1431291-90-5 2-bromo-4-amino-6-trifluoromethybenzenesulfonic acid 
• 1431291-89-2 2-bromo-6-trifluoromethybenzenesulfonic acid 
• 1431291-88-1 2-bromo-6-trifluoromethybenzenesulfonyl chloride 
• 1431291-87-0 2-bromo-6-trifluoromethyl-N-(5,8-dimethoxy-1,2,4-triazolo[1,5-c]pyrimidine-2-yl)benzenesulfonamide 
• 219714-96-2 penoxsulam 
• 1198181-28-0 N-[3-(3-hydroxypyrrolidin-1-yl)-5-(trifluoromethyl)phenyl]-N-methylacetamide 
• 1198180-44-7 ({1-[3-(methylamino)-5-(trifluoromethyl)phenyl]pyrrolidin-3-yl}oxy)acetic acid 
• 1198181-25-7 N-[3-bromo-5-(trifluoromethyl)phenyl]-N-methylacetamide 
• 1135493-55-8 N-[3-(1-methylpiperidin-4-yl)-5-trifluoromethyl-phenyl]-acetamide 

Relevant academic research and scientific papers

An efficient synthesis of 2-(2,2-difluoroethoxy)-6-trifluoromethyl-n-(5,8- dimethoxy-1,2,4-triazolo[1,5-c]pyrimidine-2-yl) benzenesulfonamide: Penoxsulam

An efficient nine-step synthesis of 2-(2,2-difluoroethoxy)-6- trifluoromethyl-N-(5,8-dimethoxy-1,2,4-triazolo[1,5-c] - pyrimidine-2-yl) benzenesulfonamide has been developed. The starting material 4-nitro-2-(trifluoromethyl)aniline starting material was converted via 2-bromo-4-amino-6-trifluoromethylaniline and 2-bromo-4-acetamido-6- trifluoromethylbenzenesulfonic acid to 2-bromo-6-trilfuoromethylbenzenesulfonic acid. This was then combined with 2-amino-5,8-dimethoxy-1,2,4-triazolo[1.5-c] pyrimidine to give the target molecule. Compared with the reported method, this approach has advantages in its shorter reaction time, milder reaction conditions and easier purifiction. Moreover, the overall yield has been improved to 22.9% which is twice of that of the reported method.

HETEROCYCLIC COMPOUND

The present invention relates to a compound represented by wherein each symbol is as defined in the specification, a salt thereof and the like.

HETEROCYCLIC COMPOUND

The present invention relates to a compound represented by wherein each symbol is as defined in the specification, a salt thereof and the like.

BENZENE OR THIOPHENE DERIVATIVE AND USE THEREOF AS VAP-1 INHIBITOR

The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.

COMPOUNDS AND METHODS OF USE

Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

SUBSTITUTED ARYL-AMINE DERIVATIVES AND METHODS OF USE

The present invention provides classes of compounds, including-their pharmaceutically acceptable derivatives, useful for treating angiogenesis and related diseases such as cancer. Formula I and II wherein R is a 9- or 10-membered heterocyclyl ring selected from 7-isoquinolinyl,..2-methyl-3-oxo-2,3-dihydroindazol-6-yl, [1,6]-naphthydrin-3-yl, [1,7]-naphthydrin-2-yl, 1-oxo-2,3-dihydrobenzofuran-4-yl, 3-oxo-2,3-dihydrobenzofuran-5-yl, dihydro-benzodioxinyl, 6-quinazolinyl, 2-amino-6-quinazolinyl, 4-methylamino-6-quinazolinyl, 2,4-diamino-6 quinazolinyl, 3-oxo-3,4-dihydro-1,4-benzoxazin-6-yl, 2,2-difluoro-l;3-benzodioxol-5-yl and 2,2,3,3 tetrafluoro-2,3-dihydro-l,4-benzodioxin-6-yl, each of which is optionally substituted with one or more substituents selected from halo, haloakyl, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, N-dimethylamino-C1-6-alkyl, N-dimethylamino-C1-6-alkoxy, amino, alkyl-carbonylamino, morpholino-sulfonyl, amino-sulfonyl, oxazolyl, pyrrolyl,4 morpholinyl, carboxyl, cyano, and acetyl; wherein R1 in formula I is selected from unsubstituted or substituted phenyl, 5-6 membered heteroaryl, 9-10 membered bicyclic heterocyclyl and 11-14 membered tricyclic heterocyclyl, and R1 in formula II is selected from specific bicyclic heterocycles.

SUBSTITUTED ANTHRANILIC AMIDE DERIVATIVES AND METHODS OF USE

Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Substituted alkylamine derivatives and methods of use

Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.