18807-71-1

Usage

Chemical Properties

White crystalline powder

InChI:InChI=1/C10H14N2O2.ClH/c11-6-7-12-10(13)14-8-9-4-2-1-3-5-9;/h1-5H,6-8,11H2,(H,12,13);1H

Upstream product

• 72080-83-2 2-benzyloxycarbonylaminoethylamine 
• 146552-66-1 benzyl (2-azidoethyl)carbamate 
• 13139-17-8 N-(Benzyloxycarbonyloxy)succinimide 
• 107-15-3 ethylenediamine 
• 501-53-1 benzyl chloroformate 
• 61495-86-1 N,N-Bis-Carbobenzyloxyethylenediamine 
• 18807-67-5 1,2-Ethanediylbis(phenylmethyl carbamate) 
• 77153-05-0 N¹-benzyloxycarbonyl-N²-t-butoxycarbonyl-1,2-ethanediamine 
• 886-64-6 N^β-benzyloxycarbonyl-β-alaninamide 

Downstream Products

• 80262-90-4 [2-(1-Methylene-3-oxo-1,3-dihydro-isoindol-2-yl)-ethyl]-carbamic acid benzyl ester 
• 80262-86-8 2-<2-<(benzyloxycarbonyl)amino>ethyl>-1,3-dihydro-3-oxo-1-methyl-1H-isoindole-1-carbonitrile 
• 82825-43-2 Boc-Asp(OBzl)EDA-Z 
• 183444-81-7 {(S)-5-(2-Benzyloxycarbonylamino-ethylcarbamoyl)-5-[(S)-2-((R)-2-tert-butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-pentyl}-carbamic acid tert-butyl ester 
• 183444-82-8 {(S)-5-(2-Benzyloxycarbonylamino-ethylcarbamoyl)-5-[(S)-2-((R)-2-tert-butoxycarbonylamino-propionylamino)-3-phenyl-propionylamino]-pentyl}-carbamic acid tert-butyl ester 
• 205874-86-8 N¹-benzyloxycarbonyl-N²-(N^α-t-butoxycarbonyl-N^g-tosylarginyl)-1,2-ethanediamine 
• 296239-32-2 N-[2-(benzyloxycarbonylamino)ethyl]perfluorooctylsulfonamide 
• 296239-34-4 2H,2H,4H,4H,5H,5H-3-oxa-perfluorotridecanoic acid N-[2-benzyloxycarboxylamino-ethyl]-amide 
• 277329-79-0 methyl (2S)-3-[(tert-Butoxy)carbonylamino]-2-{[(4-{4-[({2-[(phenylmethoxy)carbonylamino]ethyl}amino)sulfonyl]phenyl}phenyl)sulfonyl]amino}propanoate 
• 1042124-57-1 (S)-2-(2,2-dimethoxyethylamino)-N-(2-(benzyloxycarbonylamino)ethyl)-3-phenylpropanamide 
• 146553-00-6 (S)-tert-butyl (1-((2-(((benzyloxy)carbonyl)amino)ethyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate 
• 1221567-05-0 tert-butyl 4-(2-(benzyloxycarbonylamino)ethylcarbamoyl)piperidine-1-carboxylate 
• 1612182-24-7 benzyl N-(2-{[2-amino-6-(2,3-dimethylphenyl)pyrimidin-4-yl]amino}ethyl)carbamate 

Relevant academic research and scientific papers

NOVEL ANTIBACTERIAL 3"-DERIVATIVES OF 4,6-DISUBSTITUTED 2,5-DIDEOXYSTREPTAMINE AMINOGLYCOSIDE ANTIBIOTICS

The present invention relates to novel aminoglycoside compounds having antimicrobial properties and being suitable, for example, as therapeutic agents for use in the treatment of mammalian disease and in particular to novel therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes. The invention further relates to compounds for use in the treatment of diseases whose treatment is made otherwise difficult due to antibiotic-class-related bacterial resistance and provides novel therapeutic agents suitable for use in the treatment of multidrug-resistant (MDR) infections.

Catalytic Staudinger Reduction at Room Temperature

We report an efficient catalytic Staudinger reduction at room temperature that enables the preparation of a structurally diverse set of amines from azides in excellent yields. The reaction is based on the use of catalytic amounts of triphenylphosphine as a phosphine source and diphenyldisiloxane as a reducing agent. Our catalytic Staudinger reduction exhibits a high chemoselectivity, as exemplified by reduction of azides over other common functionalities, including nitriles, alkenes, alkynes, esters, and ketones.

MIC-1 Compounds and Uses Thereof

The invention relates to MIC-1 compounds. More specifically it relates to compounds comprising a MIC-1 polypeptide with an N-terminal amino acid extension and a protractor wherein the amino acid extension comprises 3 to 36 amino acid residues and where the MIC-1 polypeptide and the N-terminal amino acid extension together have a calculated pI lower than 6.5. The compounds of the invention have MIC-1 activity. The invention also relates to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable excipients, as well as the medical use of the compounds.

PHARMACEUTICAL COMPOSITIONS OF FGF21 DERIVATIVES AND USES THEREOF

The present invention relates to pharmaceutical compositions. In particular compositions comprising derivatives of analogues of FGF21, more in particular to analogues of FGF21 having a side chain attached to a cysteine in the C-terminal part of FGF21. The invention also relates to pharmaceutical compositions comprising such FGF21 derivatives and pharmaceutically acceptable excipients, as well as the medical use of such compositions.

FGF21 DERIVATIVES AND USES THEREOF

The invention relates to a derivative of a FGF21 protein having a cysteine residue at a position corresponding to position 167, 169, 170, 171, 172, 173, 174, 175 and in particular position 180 or position 181 of mature human FGF21 and derivatives thereof having a side chain attached to this cysteine. The FGF21 derivatives of the invention display high potency towards the FGF receptors. The invention also relates to pharmaceutical compositions comprising such FGF21 derivatives and pharmaceutically acceptable excipients, as well as the medical use of the FGF21 derivatives.

HYDRAZINYL-PYRROLO COMPOUNDS AND METHODS FOR PRODUCING A CONJUGATE

The present disclosure provides conjugate structures and hydrazinyl-pyrrolo compound structures used to produce these conjugates. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same. Aspects of the present disclosure include a pharmaceutical composition. The pharmaceutical composition includes a conjugate as described herein and a pharmaceutically acceptable excipient. Aspects of the present disclosure include a method of delivering a conjugate to a subject. The method includes administering to the subject an effective amount of a conjugate as described herein. Aspects of the present disclosure include a method of treating a condition in a subject.

Solid phase synthesis of peptide hydroxamic acids on poly(ethylene glycol)-based support

A novel resin designed for solid-phase synthesis of peptide hydroxamic acids (PHA) combining the trityl linker with poly(ethylene glycol)-based support, ChemMatrix type, is described. The synthesis of PHA can be performed according to a standard protocol,

Branched peptide linkers

Conjugates containing a targeting ligand, such as an antibody, a therapeutically active drug and a branched peptide linker. The branched peptide linker contains two or more amino acid moieties that provide an enzyme cleavage site. The number of drugs capable of being bonded to the branched linkers varies by a factor of two for each generation of branching.

Doxorubicin immunoconjugates containing bivalent, lysosomally-Cleavable dipeptide linkages

Bivalent doxorubicin (DOX)-dipeptides (16a-c) were prepared and conjugated to the monoclonal antibody BR96. The dipeptides are cleaved by lysosomal proteases following internalization of the resulting immunoconjugates. Conjugate 18b demonstrated antigen-s

Epoxysuccinamide derivative or salt thereof

PCT No. PCT/JP98/01778 Sec. 371 Date Dec. 17, 1998 Sec. 102(e) Date Dec. 17, 1998 PCT Filed Apr. 17, 1998 PCT Pub. No. WO98/47887 PCT Pub. Date Oct. 29, 1998The invention relates an epoxysuccinamide derivative represented by a formula (I): wherein R1 represents a hydrogen atom, an alkyl or aminoalkyl group, R2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R1 and R2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R3 and R4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.