123724-16-3

Usage

Uses

Used in Pharmaceutical and Medical Applications:
p-(2-Quinolinylmethoxy)benzoic acid is used as an anti-cancer agent for its ability to inhibit the growth of cancer cells. It targets various cellular pathways and mechanisms, making it a promising candidate for cancer treatment.
Used in Anti-inflammatory Applications:
p-(2-Quinolinylmethoxy)benzoic acid is used as an anti-inflammatory agent due to its ability to reduce inflammation, which can be beneficial in treating various inflammatory conditions.
Used in Neuroprotective Applications:
p-(2-Quinolinylmethoxy)benzoic acid is used as a neuroprotective agent for its potential to protect neurons from damage, which can be useful in the treatment of neurodegenerative diseases.
Used in Antiviral Therapy:
p-(2-Quinolinylmethoxy)benzoic acid is used as a potential inhibitor of the enzyme N-myristoyltransferase, which plays a role in the replication of certain viruses. This makes it a candidate for the development of antiviral therapies.

Upstream product

• 1780-17-2 quinolin-2-ylmethanol 
• 19575-07-6 quinoline-2-carboxylic acid methyl ester 
• 871507-14-1 N-methoxy-N-methyl-4-(quinolin-2-ylmethoxy)-benzamide 
• 99-76-3 methyl 4-hydroxylbenzoate 
• 4377-41-7 2-Chloromethylquinoline 
• 137426-86-9 4-(2-Quinolinylmethoxy)benzoic acid methyl ester 

Downstream Products

• 1354404-44-6 N-methyl-N-(pyridin-4-yl)-4-(quinolin-2-ylmethoxy)benzamide 
• 1454918-39-8 N-Methyl-N-phenyl-4-(quinolin-2-ylmethoxy)benzamide 
• 871507-11-8 2-((4-(4-(pyridin-4-yl)-1H-pyrazol-5-yl)phenoxy)methyl)quinoline 
• 871507-16-3 3-(dimethylamino)-2-(pyridin-4-yl)-1-(4-(quinolin-2-ylmethoxy)phenyl)prop-2-en-1-one 
• 871507-15-2 2-pyridin-4-yl-1-[4-(quinolin-2-ylmethoxy)-phenyl]-ethanone 
• 871507-14-1 N-methoxy-N-methyl-4-(quinolin-2-ylmethoxy)-benzamide 
• 898562-94-2 2-({4-[1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl]phenoxy}methyl)quinoline 
• 898562-93-1 2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-5-yl)phenoxy)methyl)quinoline 
• 123724-08-3 4-Methyl-N-[4-(quinolin-2-ylmethoxy)-benzoyl]-benzenesulfonamide 
• 134138-88-8 4-(quinolin-2-ylmethyloxy)benzoyl chloride 

Relevant academic research and scientific papers

Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1

G-protein-coupled receptors (GPCRs) are the molecular target of 40% of marketed drugs and the most investigated structures to develop novel therapeutics. Different members of the GPCRs superfamily can modulate the same cellular process acting on diverse pathways, thus representing an attractive opportunity to achieve multitarget drugs with synergic pharmacological effects. Here, we present a series of compounds with dual activity toward cysteinyl leukotriene receptor 1 (CysLT1R) and G-protein-coupled bile acid receptor 1 (GPBAR1). They are derivatives of REV5901-the first reported dual compound-with therapeutic potential in the treatment of colitis and other inflammatory processes. We report the binding mode of the most active compounds in the two GPCRs, revealing unprecedented structural basis for future drug design studies, including the presence of a polar group opportunely spaced from an aromatic ring in the ligand to interact with Arg792.60 of CysLT1R and achieve dual activity.

ARYL- AND HETEROARYLAMID DERIVATIVES AS PDE10A ENZYME INHIBITOR

The invention relates to compounds of the formula and their use as pharmaceutical ingredients, in particular for the treatment of CNS related diseases (PDE 10A inhibitors).

Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain

2-((4-(1-[11C]Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy) methyl)-quinoline (MP-10), a specific PDE10A inhibitor (IC50 = 0.18 nM with 100-fold selectivity over other PDEs), was radiosynthesized by alkylation of the desmethyl precursor with [11C]CH3I, ～45% yield, >92% radiochemical purity, >370 GBq/μmol specific activity at end of bombardment (EOB). Evaluation in Sprague-Dawley rats revealed that [11C]MP-10 had highest brain accumulation in the PDE10A enriched-striatum, the 30 min striatum: cerebellum ratio reached 6.55. MicroPET studies of [11C]MP-10 in monkeys displayed selective uptake in striatum. However, a radiolabeled metabolite capable of penetrating the blood-brain-barrier may limit the clinical utility of [11C]MP-10 as a PDE10A PET tracer.

BICYCLIC HETEROARYL COMPOUNDS AS PDE10 INHIBITORS

The invention pertains to tricyclic heteraaryi compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds which are selective inhibitors of PDE 10. The invention further relates to pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom.

Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3- yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia

By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique "selectivity pocket" for PDE10A inhibitors, and interactions within this pocket allowed the design of highly selective and potent PDE10A inhibitors. Further optimization of brain penetration and drug-like properties led to the discovery of 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920). This PDE10A inhibitor is the first reported clinical entry for this mechanism in the treatment of schizophrenia.

Heteroaromatic quinoline compounds

The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.

PHOSPHODIESTERASE 10 INHIBITION AS TREATMENT FOR OBESITY-RELATED AND METABOLIC SYNDROME-RELATED CONDITIONS

The present invention provides methods to decrease body weight and/or body fat in animals, e.g., in the treatment of overweight or obese patients (e.g., humans or companion animals), or as a means to produce leaner meat in food stock animals (e.g., cattle, chickens, pigs), methods to treat non-insulin dependent diabetes (NIDDM), metabolic syndrome, or glucose intolerance, in patients in need thereof by administering a PDE10 inhibitor (alone or in combination with another therapeutic agent), kits for the above-identified therapeutic uses, and methods of identifying PDE10 inhibitors for the above-described therapeutic uses.

CYANOMETHYLPYRIDINE DERIVATIVES

The present invention relates to new cyanomethylpyridine dervatives of formula I wherein Y represents N or CH;R1 represents hydrogen, fluoro, chloro, difluoro or dichloro; R2 represents hydrogen or C1-4alkyl;n is 0 or 1; p is 0 or 1; A represents a covalent bond or a group of formula -CONHC-H(Ar)-, -NHCH(Ar)-, -S02NHCH(Ar)-,NHCONHCH(Ar) or OCONHCH(Ar),and when p is 1,A can also represent CH(Ar)NH; and AT represents phenyl or phenyl substituted with halogen,C M alkyl, C1-4 alkoxy or trifluoromethyl. These compounds are PAF antagonist and/or 5-lipoxygenase inhibitors.