88135-16-4

Upstream product

• 22509-50-8 2,6-dichloro-4-nitrobenzoic acid 
• 99-99-0 1-methyl-4-nitrobenzene 
• 7149-69-1 1,3-dichloro-2-methyl-5-nitrobenzene 

Downstream Products

• 232275-50-2 methyl 2,6-dichloro-4-nitrobenzoate 
• 232275-55-7 2,6-dichloro-4-fluorobenzoic acid 
• 232275-51-3 4-bromo-2,6-dichloro-benzoic acid 
• 4641-38-7 2,6-Dichloro-4-hydroxybenzoic acid 
• 232275-49-9 methyl 4-amino-2,6-dichlorobenzoate 
• 232275-53-5 methyl 4-bromo-2,6-dichlorobenzoate 
• 232275-56-8 methyl 2,6-dichloro-4-fluorobenzoate 

Relevant academic research and scientific papers

A kind of the second aryl amine derivative and its preparation method, pharmaceutical composition and use thereof

The invention provides diarylamide type derivatives having a structure shown as a formula (I) as follows, or pharmaceutically acceptable salts thereof, a preparing method of the derivatives, compositions containing the derivatives and the pharmaceutically acceptable salts, and medicine uses of the derivatives and the pharmaceutically acceptable salts. The diarylamide type derivatives having the structure shown as the formula (I) or the pharmaceutically acceptable salts thereof have antagonistic effects on FXR. Integral animal experiments show that the compounds have effects of decreasing blood sugar and reducing blood fat. The compounds can be used for treating hyperlipidemia and type 2 diabetes mellitus.

Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: Discovery of TR-14035, a dual α4β7/α4β1 integrin antagonist

α4β1 and α4β7 integrins are key regulators of physiologic and pathologic responses in inflammation and autoimmune disease. The effectiveness of anti-integrin antibodies to attenuate a number of inflammatory/immune conditions provides a strong rationale to target integrins for drug development. Important advances have been made in identifying potent and selective candidates, peptides and peptidomimetics, for further development. Herein, we report the discovery of a series of novel N-benzoyl-L-biphenylalanine derivatives that are potent inhibitors of α4 integrins. The potency of the initial lead compound (1: IC50 α4β7/α4β1 =5/33 μM) was optimized via sequential manipulation of substituents to generate low nM, orally bioavailable dual α4β1/α4β7 antagonists. The SAR also led to the identification of several subnanomolar antagonists (134, 142, and 143). Compound 81 (TR-14035; IC50 α4β7/α4β1 =7/87 nM) has completed Phase I studies in Europe. The synthesis, SAR and biological evaluation of these compounds are described.

Benzylideneamino- and phenylacetylguanidines and their pharmaceutical uses

Compounds of formula (I): STR1 or a salt or acyl derivative thereof; wherein Y is either --CH=N or STR2 R1 is hydroxy, halogen, (C1-4) alkyl, or (C1-4)alkoxy, R2 is a nitrogen-containing, basic substituent, R3 is hydrogen, hydroxy, halogen, (C1-4) alkyl, (C1-4) alkoxy or a nitrogen-containing, basic substituent, and R4 is hydrogen or hydroxy, are useful in treating diarrhoea and scours.