105258-93-3

Usage

Uses

Used in Pharmaceutical Research:
N-CBZ-3-OXOAZETIDINE is used as a key intermediate in the synthesis of pharmaceutical compounds for its potential antiviral and antitumor properties. Its unique structure allows for the development of new drugs with improved efficacy and reduced side effects.
Used in Organic Synthesis:
N-CBZ-3-OXOAZETIDINE is used as a building block in organic synthesis for the creation of complex organic molecules. Its reactivity and stability make it a valuable component in the synthesis of various organic compounds.
Used in Peptide-based Drug Preparation:
N-CBZ-3-OXOAZETIDINE is used as a component in the preparation of peptide-based drugs due to its ability to form stable complexes with metal ions. This property enhances the stability and bioavailability of peptide-based drugs, improving their therapeutic outcomes.
Used in Metal Coordination Chemistry:
N-CBZ-3-OXOAZETIDINE is used in metal coordination chemistry for its ability to form stable complexes with metal ions. This property allows it to be employed in the development of new materials with unique properties, such as catalysts, sensors, and drug delivery systems.

InChI:InChI=1/C11H11NO3/c13-10-6-12(7-10)11(14)15-8-9-4-2-1-3-5-9/h1-5H,6-8H2

Upstream product

• 40320-60-3 N-benzhydryl 3-azetidinone 
• 501-53-1 benzyl chloroformate 
• 1138-80-3 N-(Benzyloxycarbonyl)glycine 
• 17557-84-5 3-oxoazetidine hydrochloride salt 
• 128117-22-6 1-Benzyloxycarbonyl-3-hydroxyazetidine 
• 55378-79-5 C₁₃H₁₅NO₆ 
• 67865-70-7 1-diazo-3-(N-benzyloxycarbonyl)amino-2-propanone 

Downstream Products

• 870859-07-7 benzyl 3-[(R)-1-(naphthalen-1-yl)ethylamino]-azetidine-1-carboxylate 
• 934665-74-4 benzyl 3-hydroxy-3-(2-oxocyclohexyl)azetidine-1-carboxylate 

Relevant academic research and scientific papers

Intramolecular N-H insertion of α-diazocarbonyls catalyzed by Cu(acac)2: An efficient route to derivatives of 3-oxoazetidines, 3-oxopyrrolidines and 3-oxopiperidines

Cu(acac)2 was found to be an efficient catalyst for the intramolecular N-H insertion by carbenoids. The competitive intramolecular C-H insertion by carbenoids is not a problem in the diazo decomposition reaction with Cu(acac)2 as catalyst. The reaction provided derivatives of 3-oxoazetidine, 3-oxopyrrolidine and 3-oxopiperidine in moderate to good yields.

Arylamine compound, pharmaceutical composition containing arylamine compound as well as preparation method and application of arylamine compound

The present invention relates to an arylamine compound of a formula (I), a pharmaceutical composition comprising the same, a preparation method of the arylamine compound and application of the pharmaceutical composition in the prevention or treatment of diseases or conditions associated with RET activity.

Packaging comprising forms of sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide

The invention relates to a packaging comprising a multitude (A) of at least 2 administration units comprising polymorphic trihydrated forms of sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide; or (B) of at least 2 administration units comprising polymorphic solvated or desolvated forms of sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide.

PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF

The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

N- (6- ( (2R,3S) -3,4-DIHYDROXYBUTAN-2-YLOXY) -2- (4 - FLUOROBENZYLTHIO) PYRIMIDIN- 4 - YL) -3- METHYLAZETIDINE- 1 - SULFONAMIDE AS CHEMOKINE RECEPTOR MODULATOR

There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.

METHODS OF USING MEK INHIBITORS

The present invention provides methods of treating cancer by administering a compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments.

METHODS OF USING COMBINATIONS OF MEK AND JAK-2 INHIBITORS

A method of treating a disease in a mammal, comprising administering to the mammal a therapeutically effective amount of a MEK compound of Formula I(M), or a pharmaceutical composition comprising a therapeutically effective amount of a MEK compound of Formula I(M) and a pharmaceutically acceptable carrier, in combination with a therapeutically effective amount of a JAK-2 compound of Formula I(J), or a pharmaceutical composition comprising a therapeutically effective amount of a JAK-2 compound of Formula I(J) and a pharmaceutically acceptable carrier, wherein the MEK compound of Formula I(M) and JAK-2 compound of Formula I(J) are as defined in the specification.

ARYLALKYLAMINES AND PROCESS FOR PRODUCTION THEREOF

The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensiing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc. The symbols in the formula represent the following meanings: Ar: optionally substituted aryl or optionally substituted heteroaryl here, the cyclic portion of the heteroaryl is bicyclic heterocyclic ring in which 5- to 6-membered monocyclic heterocyclic ring containing 1 or 2 hetero atom(s) and benzene ring are fused; R 1 : a group selected from the group consisting of optionally substituted cyclic hydrocarbon group, and optionally substituted heterocyclic group; n: an integer of 1 to 3; X: single bonding arm, -CH 2 -, -CO- , - (CH 2 ) m -CO- , -CH (R 2 ) -CO-, - (CH 2 ) p -Y-(C(R 3 ) (R 4 )) q -CO-, -NH-CO- or -N(R 5 ) -CO-; in the above-mentioned respective definitions of the X, the bonding arm described at the left end represents a bond with R 1 ; m is an integer of 1 to 3; p is an integer of 0 to 2; q is an integer of 0 to 2; Y: -O- or -SO 2 -; R 2 : phenyl or lower alkyl; R 3 , R 4 : each independently represents hydrogen atom or lower alkyl; R 5 : lower alkyl; provided that the ring portion of the group represented by R 1 is neither naphthylidine nor partially saturated group thereof, and, when X is -CH 2 - or -CO-, R 1 is not naphthyl.

Serine and threonine β-lactones: A new class of hepatitis A virus 3C cysteine proteinase inhibitors

Hepatitis A virus (HAV) 3C enzyme is a cysteine proteinase essential for viral replication and infectivity and represents a target for the development of antiviral drugs. A number of serine and threonine β-lactones were synthesized and tested against HAV 3C proteinase. The D-N-Cbz-serine β-lactone 5a displays competitive reversible inhibition with a Ki value of 1.50 × 10-6 M. Its enantiomer, L-N-Cbz-serine β-lactone 5b is an irreversible inactivator with kinact = 0.70 min-1, KI = 1.84 × 10-4 M and kinact/KI = 3800 M-1 min-1. Mass spectrometry and HMQC NMR studies using 13C-labeled 5b show that inactivation of the enzyme occurs by nucleophilic attack of the cysteine thiol (Cys-172) at the β-position of the oxetanone ring. Although the N-Cbz-serine β-lactones 5a and 5b display potent inhibition, other related analogues with an N-Cbz side chain, such as the five-membered ring homoserine γ-lactones 14a and 14b, the four-membered ring β-lactam 33, 2-methylene oxetane 34, cyclobutanone 36, and 3-azetidinone 39, fail to give significant inhibition of HAV 3C proteinase, thus demonstrating the importance of the β-lactone ring for binding.