304873-62-9

Usage

Uses

Used in Organic Synthesis:
2-Boc-amino-4-hydroxymethylpyridine serves as a key intermediate in organic synthesis, where its Boc protecting group allows chemists to selectively modify other parts of the molecule without affecting the amine group. This selective reactivity is crucial for the synthesis of complex organic compounds.
Used in Pharmaceutical Research and Drug Discovery:
In pharmaceutical research, 2-Boc-amino-4-hydroxymethylpyridine is employed as a building block for the development of new drugs. Its structural features, including the pyridine ring and the hydroxymethyl group, contribute to the molecule's reactivity and potential interactions with biological targets, making it a valuable component in the creation of biologically active molecules.
Used in the Synthesis of Biologically Active Molecules:
2-Boc-amino-4-hydroxymethylpyridine's versatility and reactivity make it suitable for the synthesis of a range of biologically active molecules. The hydroxymethyl group provides opportunities for further derivatization, which can enhance the molecule's ability to interact with biological systems, potentially leading to the discovery of new therapeutic agents.
Overall, 2-Boc-amino-4-hydroxymethylpyridine is a valuable chemical entity in the fields of organic synthesis and pharmaceutical research, offering a foundation for the development of innovative compounds with potential applications in medicine and other industries.

InChI:InChI=1/C11H16N2O3/c1-11(2,3)16-10(15)13-9-6-8(7-14)4-5-12-9/h4-6,14H,7H2,1-3H3,(H,12,13,15)

Upstream product

• 90101-20-5 tert-Butyl N-(4-methyl-pyridin-2-yl)carbamate 
• 695-34-1 2-Amino-4-methylpyridine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 6937-03-7 methyl 2-aminoisonicotinate 
• 304873-65-2 2-[N,N-mono-(tert-butoxycarbonyl)amino]-pyridyl-4-aldehyde 
• 13362-28-2 2-aminoisonicotinic acid 
• 6313-54-8 2-chloroisonicotinic acid, 
• 305329-03-7 2-[N,N-bis(tert-butoxycarbonyl)amino]isonicotinic acid ethyl ester 
• 639091-75-1 methyl 2-[(tert-butoxycarbonyl)amino]isonicotinate 
• 105250-17-7 2-amino-4-hydroxymethylpyridine 

Downstream Products

• 304873-65-2 2-[N,N-mono-(tert-butoxycarbonyl)amino]-pyridyl-4-aldehyde 
• 1446252-28-3 (Z)-4-(4-fluorostyryl)-pyridin-2-amine 
• 1446252-29-4 (Z)-tert-butyl 4-(4-fluorostyryl)pyridin-2-yl(isopropyl)carbamate 
• 1446252-30-7 (Z)-4-(4-fluorostyryl)-N-isopropylpyridin-2-amine 
• 1446252-33-0 (E)-ethyl 3-(2-(tert-butoxycarbonylamino)pyridin-4-yl)-2-phenyl-acrylate 
• 1446252-34-1 (E)-ethyl 3-(2-(tert-butoxycarbonylamino)pyridin-4-yl)-2-(4-fluorophenyl) acrylate 
• 1446252-36-3 (E)-ethyl 3-(2-aminopyridin-4-yl)-2-phenyl acrylate 
• 1446252-37-4 (E)-ethyl 3-(2-aminopyridine-4-yl)-2-(4-fluorophenyl)acrylate 
• 1446252-38-5 (E)-ethyl 2-(4-fluorophenyl)-3-(2-(isopropylamino)pyridin-4-yl)acrylate 
• 1446252-39-6 3-[2-(tert-butoxycarbonyl-isopropyl-amino)-pyridin-4-yl]-2-(4-fluoro-phenyl)-acrylic acid ethyl ester 
• 1446252-27-2 tert-butyl [(Z)-4-(4-fluorostyryl)pyridin-2-yl] carbamate 

Relevant academic research and scientific papers

AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.

CONJUGATE OF MONOMETHYL AURISTATIN F AND TRASTUZUMAB AND ITS USE FOR THE TREATMENT OF CANCER

The present invention relates to an antibody-drug-conjugate or pharmaceutical composition comprising the same. From one aspect, the invention relates to an antibody-drug-conjugate (ADC) comprising an antibody consisting of the Trastuzumab or a biosimilar thereof, said antibody being conjugated to at least one drug consisting of a monomethyl auristatin F derivative. The invention also comprises method of treatment of cancer comprising administering to the subject an effective amount of said antibody-drug-conjugate or composition comprising the same.

COMPOSITION FOR THE TREATMENT OF IGF-1R EXPRESSING CANCER

The present invention relates to a method for the treatment of IGF-IR expressing cancers as well as to a compositions and a kit for said traitment. From one aspect, the invention reates to the combined use of a first antibody for the determination of the IGF-IR status of a cancer and a second antibody used as an ADC for the treatment of said cancer.

Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening

Here we report the discovery of a selective inhibitor of Aurora A, a key regulator of cell division and potential anticancer target. We used the atom category extended ligand overlap score (xLOS), a 3D ligand-based virtual screening method recently developed in our group, to select 437 shape and pharmacophore analogs of reference kinase inhibitors. Biochemical screening uncovered two inhibitor series with scaffolds unprecedented among kinase inhibitors. One of them was successfully optimized by structure-based design to a potent Aurora A inhibitor (IC50 = 2 nM) with very high kinome selectivity for Aurora kinases. This inhibitor locks Aurora A in an inactive conformation and disrupts binding to its activator protein TPX2, which impairs Aurora A localization at the mitotic spindle and induces cell division defects. This phenotype can be rescued by inhibitor-resistant Aurora A mutants. The inhibitor furthermore does not induce Aurora B specific effects in cells.

CONJUGATE OF MONOMETHYL AURISTATIN F AND TRASTUZUMAB AND ITS USE FOR THE TREATMENT OF CANCER

The present invention relates to an antibody-drug-conjugate. From one aspect, the invention relates to an antibody-drug-conjugate comprising an antibody consisting of the Trastuzumab, said antibody being conjugated to at least one drug consisting of a monomethyl auristatin F derivative. The invention also comprises method of treatment and the use of said antibody-drug-conjugate for the treatment of cancer.

IGF-1R ANTIBODY-DRUG-CONJUGATE AND ITS USE FOR THE TREATMENT OF CANCER

The present invention relates to an antibody-drug-conjugate capable of binding IGF-1R. From one aspect, the invention relates to an antibody-drug-conjugate comprising an antibody capable of binding to IGF-1R, said antibody being conjugated to at least one drug selected from derivatives of dolastatin 10 and auristatins. The invention also comprises method of treatment and the use of said antibody-drug- conjugate for the treatment of cancer.

ANTIBODY-DRUG-CONJUGATE AND ITS USE FOR THE TREATMENT OF CANCER

The present invention relates to an antibody-drug-conjugate. From one aspect, the invention relates to an antibody-drug-conjugate comprising an antibody capable of binding to a Target, said antibody being conjugated to at least one drug selected from derivatives of dolastatin 10 and auristatins. The invention also comprises method of treatment and the use of said antibody-drug-conjugate for the treatment of cancer.

DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS

The present invention concerns a compound of following formula (I): where: - R1 is H or OH, - R2 is a (C1-C6)alkyl, COOH, COO-((C1-C6)alkyl) or thiazolyl group, - R3 is H or a (C1-C6)alkyl group, and - R4 is: ■ a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR5R6, ■ -(CH2CH2X1)(CH2CH2X2)a2(CH2CH2X3)a3(CH2CH2X4)a4(CH2CH2X5)a5R7, ■ an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or ■ a heterocycle-(C1-C8)alkyl group optionally substituted by one or more groups chosen from among (C1-C6)alkyl, OH and NR12R13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS

The present invention concerns a compound of following formula (I) where: - R1 is H or OH, - R2 is a (C1-C6)alkyl, COOH, COO-((C1-C6)alkyl) or thiazolyl group, - R3 is H or a (C1-C6)alkyl group, and - R4 is an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS

The present invention concerns a compound of following formula (I) where: - R1 is H or OH, - R2 is a (C1-C6)alkyl, COOH, COO-((C1-C6)alkyl) or thiazolyl group, - R3 is H or a (C1-C6)alkyl group, and - R4 is: - an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or - a heterocycle-(C1-C8)alkyl group optionally substituted by one or more groups chosen from among (C1-C6)alkyl, OH and NR12R13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.