850252-34-5

Usage

Uses

Since the specific uses of [402960-19-4], C9H18N2O2, 186.40 are not provided in the given information, it is not possible to list its applications according to the materials. However, based on its molecular formula, it can be inferred that the chemical may have potential applications in various industries. Some possible applications could include:
Used in Pharmaceutical Industry:
[402960-19-4], C9H18N2O2, 186.40 could be used as a pharmaceutical compound for [application reason], such as drug development or as an active ingredient in medications.
Used in Agrochemical Industry:
[402960-19-4], C9H18N2O2, 186.40 could be used as an agrochemical compound for [application reason], such as a pesticide or a fertilizer additive.
Used in Materials Science:
[402960-19-4], C9H18N2O2, 186.40 could be used as a material in materials science for [application reason], such as a component in polymers or a precursor in the synthesis of other materials.

Upstream product

• 856707-38-5 acetic acid (2S)-2-tert-butoxycarbonylamino-1-cyclopropylcarbamoylpentyl ester 
• 160801-73-0 (S)-tert-butyl 1-(methoxy(methyl)amino)-1-oxopentan-2-ylcarbamate 
• 160801-74-1 (2S)-2-(1,1-dimethylethoxycarbonylamino)pentanal 
• 53308-95-5 N-tert-butoxycarbonyl-L-norvaline 
• 944716-71-6 (2S,3S)-N-cyclopropyl-3-(tert-butoxycarbonyl)amino-2-hydroxyhexanoic acid amide 
• 856707-39-6 (3S,3S)-N-cyclopropyl-3-(tert-butoxycarbonyl)amino-2-hydroxyhexanoic acid amide 

Downstream Products

• 865469-57-4 C₃₅H₆₁N₅O₉S 
• 865469-70-1 C₃₃H₅₅N₅O₇S 
• 402959-36-8 (1S,3aR,6aS)-2-[(2S)-2-[[(2S)-2-cyclohexyl-2-[(2-pyrazinylcarbonyl)amino] acetyl]amino]-3,3-dimethylbutanoyl]-N-[(1S)-1-[(cyclopropylamino)(hydroxy)acetyl]butyl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamide 
• 856707-40-9 C₃₆H₅₅N₇O₆ 
• 856707-67-0 C₃₆H₆₁N₅O₇ 
• 856707-62-5 C₃₇H₅₆N₆O₆ 
• 850251-51-3 pyrazine-2-carboxylic acid [(1-{4-(5-chloro-pyridin-2-yloxy)-2-[1-(cyclopropylcarbamoyl-hydroxy-methyl)-butylcarbamoyl]-pyrrolidine-1-carbonyl}-2,2-dimethyl-propylcarbamoyl)-cyclohexyl-methyl]-amide 

Relevant academic research and scientific papers

Discovery of narlaprevir (SCH 900518): A potent, second generation HCV NS3 serine protease inhibitor

Boceprevir (SCH 503034), 1, a novel HCV NS3 serine protease inhibitor discovered in our laboratories, is currently undergoing phase III clinical trials. Detailed investigations toward a second generation protease inhibitor culminated in the discovery of narlaprevir (SCH 900518), 37, with improved potency (～10-fold over 1), pharmacokinetic profile and physicochemical characteristics, currently in phase II human trials. Exploration of synthetic sequence for preparation of 37 resulted in a route that required no silica gel purification for the entire synthesis.

Discovery of potent sulfonamide P4-capped ketoamide second generation inhibitors of hepatitis C virus NS3 serine protease with favorable pharmacokinetic profiles in preclinical species

Hepatitis is a disease characterized by inflammation of the liver, usually producing swelling and, in many cases, permanent damage to liver tissues. Viral hepatitis C (HCV), a small (+)-RNA virus, infects chronically 3% of the world's population. Boceprevir, SCH 503034, (1) our first generation HCV inhibitor, has already established proof-of- concept and is currently in late stage (phase III) clinical trials. In view of the positive data from our first generation compound, further work aimed at optimizing its overall profile was undertaken. Herein, we report that extension of our earlier inhibitor to the P4 pocket by introducing a new sulfonamide moiety and optimization of the P1/P1′ capping led to the discovery of a novel series of inhibitors of the HCV NS3 serine protease. Optimization of the P1 residue significantly improved potency and selectivity. The combination of optimal moieties led to the discovery of compound 47 which, in addition to being a potent inhibitor of HCV subgenomic RNA replication, was also found to have good PK profile in rat, dog and monkey.

Inhibitors of hepatitis C virus NS3/4A: α-Ketoamide based macrocyclic inhibitors

A novel series of hepatitis C virus (HCV) NS3/4A protease inhibitors bearing a P2-P4 macrocycle and a P1-P1′ α-ketoamide serine trap is reported. The NS3 protease, which is essential for viral replication, is considered one of the most attractive targets

COMPOUNDS THAT INHIBIT PROTEASE CATHEPSIN S AND HCV REPLICATION

The present invention is directed to compounds that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer's disease,

HCV INHIBITORS

The present invention is directed to compounds that are antiviral agents. Specifically, the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

HCV INHIBITORS

The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Pharmaceutical formulations and methods of treatment using the same

Pharmaceutical formulations containing at least one compound of Formulae I-XXVI herein and at least one surfactant. Pharmaceutically acceptable carriers and excipients may also be included in the formulations. The formulations of the present invention are suited for use in single unit dosages.

Liver/plasma concentration ratio for dosing hepatitis C virus protease inhibitor

Compositions and therapeutic combinations are provided including at least one compound selected from the group consisting of compounds of Formulae I to XXVI as defined herein as well as methods of treatment, prevention or amelioration of one or more symptoms of hepatitis C, treating disorders associated with HCV virus, modulating activity of HCV protease, in which liver to plasma concentration ratio of the compound ranges from about 2:1 to about 10:1.

Methods of treating hepatitis C virus

Methods for preventing, ameliorating or treating one or more symptoms of Hepatitis C virus (HCV), modulating HCV protease activity and/or inhibiting cathepsin activity in a subject, wherein the methods comprise administering to a subject in need of such treatment a dosage formulation containing at least one compound of Formulae I-XXVI herein, wherein the dosage formulation is capable of maintaining an average Cmin plasma concentration of the compound at or above 10 ng/ml.

Controlled-release formulation

Controlled-release dosage formulations including at least one compound of Formulae I to XXVI herein and a controlled-release carrier and methods of treatment using the same are provided.