5105-79-3

Upstream product

• 5105-78-2 4-(benzyloxycarbonylamino)butyric acid 
• 115-11-7 isobutene 
• 36805-97-7 N,N-dimethylformamide di-tert-butyl acetal 
• 75-65-0 tert-butyl alcohol 
• 507-19-7 t-butyl bromide 
• 104-57-4 benzyl formate 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 1296665-15-0 ethyl 5-(2-(benzyloxy)ethyl)-3-(3-(tert-butoxycarbonyl)propyl)-6-methyl-3H-pyrimidin-4-one-2-carboxylate 
• 5105-84-0 N^α--N^γ-<3-tert-butoxycarbonylpropyl>-L-glutaminyl-L-phenylalanin-tert-butylester 
• 5105-80-6 N--γ-L-glutaminyl-γ-Aminobuttersaeure-tert-butylester 
• 5105-92-0 N^α-Benzyloxycarbonyl-N^γ-(3-tert.-butoxycarbonyl-propyl)-L-glutaminsaeure-benzylester 
• 5105-94-2 N-(Benzyloxycarbonyl-α-L-glutamyl)-γ-aminobuttersaeure-tert.-butylester 
• 5105-82-8 N^α--N^γ-<3-tert-butoxycarbonyl-propyl>-L-glutaminyl-L-leucin-tert-butylester 
• 5105-81-7 N^α--N^γ-<3-tert-butoxycarbonyl-propyl>-L-glutaminyl-glycin-tert-butylester 
• 100702-80-5 tert-butyl 4-<(benzyoxycarbonyl)amino>-2-(hydroxymethyl)-2-(phenylseleno)butanoate 
• 100702-81-6 tert-butyl (E)-4-<(benzyoxycarbonyl)amino>-2-(hydroxymethyl)-2-butenoate 
• 100702-82-7 tert-butyl (Z)-4-<(benzyoxycarbonyl)amino>-2-(chloromethyl)-2-butenoate 
• 100702-83-8 tert-butyl (Z)-4-<(benzyoxycarbonyl)amino>-2-(fluoromethyl)-2-butenoate 
• 120686-44-4 4-[(E)-2-(Benzyloxycarbamoyl-methyl)-3-phenyl-acryloylamino]-butyric acid tert-butyl ester 
• 120686-27-3 (E)-3-(3-tert-Butoxycarbonyl-propylcarbamoyl)-4-phenyl-but-3-enoic acid ethyl ester 
• 120686-35-3 (E)-3-(3-tert-Butoxycarbonyl-propylcarbamoyl)-4-phenyl-but-3-enoic acid 

Relevant academic research and scientific papers

CONJUGATES OF A CELL-BINDING MOLECULE WITH CAMPTOTHECIN ANALOGS

Provided are conjugates of camptothecin analogs with a cell-binding molecule of formula (I), wherein R1, R2, R3, R4, R5, X, L, n, m, T and ----- are defined herein. It also provides methods of making the conjugates of camptothecin analogs to a cell-binding agent, as well as methods of using the conjugates in targeted treatment of cancer, infection, and immunological disorders.

A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS

The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.

CONJUGATION LINKERS CONTAINING 2,3-DIAMINOSUCCINYL GROUP

Provided is a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (adual-linker) containing a 2, 3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES

A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

A series of (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylamide derivatives were designed and synthesized as new estrogen-related receptor α (ERRα) degraders based on the proteolysis targeting chimera (PROTAC) concept. One of the representative compounds 6c is capable of specifically degrading ERRα protein by >80% at a relatively low concentration of 30 nM, becoming one of the most potent and selective ERRα degraders to date. Compound 6c could be utilized as a new powerful research tool for further biological investigation of ERRα.

A MedChem toolbox for cereblon-directed PROTACs

A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.

A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS

The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.

CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE

What provided is the conjugation of cytotoxic to a cell-binding molecule with a bis-linker(dual-linker) as shown in Formula (I). It provides bis-linkage methods of making a conjugate of a cytotoxic drug molecule to a cell-binding agent in a specific manner. It also relates to application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.

Aldosterone derivative, preparation method thereof and aldosterone homogeneous enzyme immunoassay reagent

The invention discloses an aldosterone derivative, a preparation method thereof, an aldosterone homogeneous enzyme immunoassay reagent and preparation and detection methods thereof. The aldosterone derivative has a structure shown as a formula (I), an aldosterone immunogen with high immunogenicity and an antibody of the aldosterone immunogen are prepared from the aldosterone derivative, and the aldosterone homogeneous enzyme immunoassay reagent prepared from the antibody can be used for realizing high-flux and high-speed detection of aldosterone on a fully-automatic biochemical analyzer.

LIPOPEPTIDE COMPOUNDS FOR THE TREATMENT OF PAIN DISORDERS

The invention is based on the discovery of a new bacterial compound with analgesic properties which could be used as a new tool for the treatment of pain disorders such as visceral pain. Studying the mechanisms implicated in analgesic properties of the probiotic Escherichia coli strain Nissle 1917 (EcN), inventors characterized, the amino fatty acids produced by EcN, which display the Ecn analgesic properties. One of these compounds inhibits the hypersensitivity to colorectal distension induced by capsaicin, which is a very powerful nociceptive compound and acts via the GABA B receptor. Furthermore, inventors demonstrate that this compound is able to cross the cellular epithelial barrier (such as the intestinal epithelium). Thus, the invention relates to a lipopetide compound, derived from gamma-aminobutyric acid. The invention also relates to a lipopeptide compound according to the invention for the treatment of treating pain disorder, such as somatic pain and visceral pain.