13737-35-4

Upstream product

• 644-36-0 o-methylphenylacetic acid 
• 34241-39-9 azobisisobutyronitrile 
• 22364-68-7 2-tolylmethylnitrile 
• 4385-35-7 isochroman-3-one 

Downstream Products

• 39191-76-9 ethyl 2-(2-(bromomethyl)phenyl)acetate 
• 39113-16-1 N-(3-Oxo-3,4-dihydro-1H-isoquinolin-2-yl)-acetamide 
• 39113-24-1 2-ureido-1,4-dihydroisoquinolin-3(2H)-one 
• 39113-05-8 2-{[1-Phenyl-meth-(Z)-ylidene]-amino}-1,4-dihydro-2H-isoquinolin-3-one 
• 39113-15-0 N-(3-oxo-3,4-dihydroisoquinolin-2(1H)-yl)benzamide 
• 39113-07-0 2-{[1-(3,4-Dichloro-phenyl)-meth-(Z)-ylidene]-amino}-1,4-dihydro-2H-isoquinolin-3-one 
• 39113-18-3 3,4-Dichloro-N-(3-oxo-3,4-dihydro-1H-isoquinolin-2-yl)-benzamide 
• 39113-25-2 2-(N'-phenylureido)-1,4-dihydroisoquinolin-3(2H)-one 
• 13737-37-6 methyl 2-[2-(bromomethyl)phenyl]acetate 
• 138786-44-4 methyl <2-(iodomethyl)phenyl>acetate 
• 138786-45-5 (2-{5-[3-((E)-2-Quinolin-2-yl-vinyl)-phenyl]-tetrazol-2-ylmethyl}-phenyl)-acetic acid 
• 138786-47-7 2-<<5-<3-(2-quinolin-2-ylethenyl)phenyl>-2H-tetrazol-2-yl>methyl>benzeneacetic acid methyl ester 
• 138786-42-2 2-<<5-<3-(quinolin-2-ylmethoxy)phenyl>-2H-tetrazol-2-yl>methyl>benzeneacetic acid 
• 138813-29-3 2-<<5-<3-(quinolin-2-ylmethoxy)phenyl>-2H-tetrazol-2-yl>methyl>benzeneacetic acid methyl ester 

Relevant academic research and scientific papers

Novel imidazobenzazepine derivatives as dual H1/5-HT 2A antagonists for the treatment of sleep disorders

A novel imidazobenzazepine template (5a) with potent dual H 1/5-HT2A antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R1-2-R-5H-imidazo[1,2-b][2]benzazepin-11-yl)-1-piperazinyl]- 2,2-dimethylpropanoic acids (e.g., 9, 19, 20, and 21), characterized by potent and balanced H1/5-HT2A receptor antagonist activities and good developability profiles.

IMIDAZOBENZAZEPINE COMPOUNDS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM (CNS) DISEASES

This invention relates to novel novel imidazobenzazepine derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.

Synthesis and structure activity relationships of novel non-peptidic metallo-aminopeptidase inhibitors

Racemic derivatives of 3-amino-2-tetralone were synthesised and evaluated for their ability to inhibit metallo-aminopeptidase activities. New compounds substituted in position 2 by methyl ketone, substituted oximes or hydroxamic acids as well as heterocyclic derivatives were evaluated against representative members of zinc-dependent aminopeptidases: leucine aminopeptidase (E.C. 3.4.11.1), aminopeptidase-N (E.C. 3.4.11.2), Aeromonas proteolytica aminopeptidase (E.C. 3.4.11.10), and the aminopeptidase activity of leukotriene A4 hydrolase (E.C. 3.3.2.6). Several compounds showed Ki values in the low micromolar range against the 'one-zinc' aminopeptidases, while most of them were rather poor inhibitors of the 'two-zinc' enzymes. This interesting selectivity profile may guide the design of new, specific inhibitors of target mammalian aminopeptidases with one active site zinc.

SUBSTITUTED PYRIDINONES

Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.

Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position

Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the α-thrombin-hirugen complex provides an explanation for these unanticipated results.

Tripeptidylpeptidase inhibitors

A compound of formula wherein the substituents are defined as in the specification and salts or hydrates thereof is disclosed as well as a method of treating disorders associated with the inactivation or excessive degradation of cholecystokinin.

Thrombin inhibitors

Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.

Thrombin inhibitors

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.

Substituted sulfonamides, process of preparation and medicines containing same

The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts possibly in the form of complexes, esters and amides thereof, represented by the formula: STR1

4-Amido-2-carboxytetrahydroquinolines. Structure-Activity Relationships for Antagonism at the Glycine Site of the NMDA Receptor

trans-2-Carboxy-5,7-dichloro-4-amidotetrahydroquinolines, evolved from the lead 5,7-dichlorokynurenic acid, have been synthesized and tested for in vitro antagonist activity at the glycine site on the N-methyl-D-aspartate (NMDA) receptor.Optimization of the 4-substituent has provided antagonists having nanomolar affinity, including the urea trans-2-carboxy-5,7-dichloro-4-amino>-1,2,3,4-tetrahydroquinoline (35; IC50 = 7.4 nM vs glycine binding; Kb = 130 nM for block of NMDA responses in the rat cortical slice), which is one of the most poten t NMDA antagonists yet found.The absolute stereochemical requirements for binding were found to be 2S,4R, showing that, in common with other glycine-site NMDA receptor ligands, the unnatural configuration at the α-amino acid center is required.The preferred conformation of the trans-2,4-disubstituted tetrahydroquinoline system, as shown by X-ray crystallography and 1H NMR studies, places the 2-carboxyl pseudoequatorial and the 4-substituent pseudoaxial.Modifications of the 4-amide show that bulky substituents are tolerated and reveal the critical importance for activity of correct positioning of the carbonyl group.The high affinity of trans-2-carboxy-5,7-dichloro-4--1,2,3,4-tetrahydroquinoline (55; IC50 = 6 nM) suggests that the Z,Z-conformer of the phenyl urea moiety in 35 is recognized by the receptor.Molecular modeling studies show that the 4-carbonyl groups of the kynurenic acids, the tetrahydroquinolines, and related antagonists based on N-(chlorophenyl)glycine, can interact with a single putative H-bond donor on the receptor.The results allow the establishment of a three-dimensional pharma cophore of the glycine receptor antagonist site, incorporating a newly defined bulk tolerance/hydrophobic region.