94994-39-5

Usage

Uses

Used in Pharmaceutical Industry:
4-[(TERT-BUTOXYCARBONYL)(METHYL)AMINO]BUTANOIC ACID is used as a building block for the preparation of substituted straight chain spiro derivatives. These derivatives act as menin/MLL protein/protein interaction inhibitors, which are useful for treating various diseases. By targeting the menin/MLL protein interaction, these inhibitors can potentially regulate gene expression and cellular processes, offering new therapeutic approaches for the treatment of diseases with complex molecular mechanisms.

Upstream product

• 1119-48-8 4-(methylamino)butyric acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 57294-38-9 N-(tert-butoxycarbonyl)-4-aminobutanoic acid 
• 74-88-4 methyl iodide 
• 872-50-4 1-methyl-pyrrolidin-2-one 
• 6976-17-6 4-(methylamino)butyric acid hydrochloride 
• 133171-74-1 methyl 4-[[(1,1-dimethylethoxy)carbonyl]methylamino]butanoic acid 

Downstream Products

• 95018-02-3 methyl N^a-(benzyloxycarbonyl)<thio>-L-cysteinate 
• 120984-59-0 tert-butyl methyl-(4-oxo-butyl)-carbamate 
• 1052648-34-6 5-(2-amino-6-{2-[4-(tert-butoxycarbonylmethylamino)butyrylamino]ethylsulfanyl}pyrimidin-4-yl)-2-methoxy-4-methylbenzoic acid methyl ester 
• 876016-45-4 C₂₅H₃₁N₃O₄ 
• 1253582-08-9 {3-[3-(2-{benzyl-[(R)-2-(8-benzyloxy-2-oxo-1,2-dihydroquinolin-5-yl)-2-(tert-butyldimethylsilanyloxy)ethyl]amino}ethyl)phenylcarbamoyl]-propyl}methylcarbamic acid tert-butyl ester 
• 872-50-4 1-methyl-pyrrolidin-2-one 
• 1290070-54-0 C₂HF₃O₂*C₁₁H₁₅NO₂ 
• 1290070-21-1 C₁₆H₂₃NO₄ 
• 1538609-66-3 {3-[6-[2-(4-cyano-phenyl)-2H-pyrazol-3-yl]-7-methyl-8-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-ylcarbamoyl]-propyl}-methyl-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

SUBSTITUTED STRAIGHT CHAIN SPIRO DERIVATIVES

Provided herein are pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, including but not limited to leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasms (MPN); and diabetes.

DC-SIGN ANTIBODY CONJUGATES COMPRISING STING AGONISTS

Provided herein are immunoconjugates comprising an anti-DC-SiGN antibody conjugated to a STING agonist. Also disclosed are methods of making the immunoconjugates and methods of treating cancer using the immunoconjugates.

ANTIBODY DRUG CONJUGATES

The present disclosure provides antibody drug conjugates comprising STING modulators. Also provided are compositions comprising the antibody drug conjugates. The compounds and compositions are useful for stimulating an immune response in a subject in need thereof. Formula (I):

The Role of N-Methyl Squaramides in a Hydrogen-Bonding Strategy to Fold Peptidomimetic Compounds

Small peptides and peptomimetic compounds are valuable tools to probe and study biological systems. Small synthetic peptide analogues adopt a given secondary structure driven by structural modules that organize the compound architecture. Among them, β- an

AZACARBOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND THERAPEUTIC USE OF SAME

The invention relates to novel azacarbonlines having formula (I), wherein: R3, R4 represent independently H; hal; CF3; substituted oxy, optionally substituted alkoxy; optionally substituted amino; substituted carbonyl; optionally substituted carboxyl; optionally substituted amide; sulphur, such as optionally substituted sulphones, sulphoxides or sulphides; linear, branched or cyclic C1-C10 alkyl optionally comprising an optionally substituted heteroatom; optionally substituted linear, branched or cyclic C2-C7 alkenyl; optionally substituted linear or branched C2-C6 alkynyl; optionally substituted aryl or heteroaryl; of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the use of same in therapeutics for the treatment of cancer and to synthesis methods.

Design, synthesis, and cyclization of 4-aminobutyric acid derivatives: Potential candidates as self-immolative spacers

Self-immolative spacers have gained significant interest in recent years due to their utility in numerous prodrug, sensor and drug delivery systems. However, there are a very limited number of spacers that are capable of undergoing spontaneous and rapid reactions under mild conditions. To address this need, 4-aminobutyric acid derivatives were explored as a potential class of self-immolative spacers. Using a modular approach, eleven N- and α-substituted derivatives of 4-aminobutyric acid were synthesized, and their intramolecular cyclizations to γ-lactams were studied. Kinetics experiments were carried out at physiological pH and temperature, and the observed half-lives for the spacers ranged from 2 to 39 s, depending on the molecular structure. In addition, the pH dependence of the cyclization rate was also explored and it was found that cyclization still occurred rapidly at mildly acidic pH. Therefore, this class of compounds exhibits promise for incorporation into a variety of self-immolative systems where rapid cyclization reactions are desired.

DIAMIDE COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND β2 ADRENERGIC RECEPTOR AGONIST ACTIVITY

This invention relates to a compound of formula I; or a pharmaceutically acceptable salt thereof. Such compounds possess both muscarinic receptor antagonist and β2 adrenergic receptor agonist activities. The invention also relates to pharmaceutical compositions comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compounds as bronchodilating agents to treat pulmonary disorders.

Renin Inhibitors

Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

NITROGEN-BASED LINKERS FOR ATTACHING MODIFYING GROUPS TO POLYPEPTIDES AND OTHER MACROMOLECULES

The present invention relates to a compound comprising a peptide moiety, a linker moiety and a water-soluble polymer moiety such as a poly(ethylene glycol) moiety. The linker moiety is between the peptide moiety and the water-soluble polymer moiety. In certain embodiments, the linker moiety has the structure: wherein α, β, and γ are each integers whose values are independently selected. In other embodiments the linker moiety has the following structure: wherein κ, ρ, and τ are each integers whose values are independently selected. In other embodiments the linker moiety has the following structure: wherein χ, φ, γ, and η are each integers whose values are independently selected. Alternatively, the linker structure may have the following structure: wherein λ and μ are each integers whose values are independently selected.

Synthesis and evaluation of xanomeline analogs-Probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor

A series of xanomeline analogs were synthesized and evaluated for binding at the M1 muscarinic acetylcholine receptor (M1 receptor). Specifically, compounds that substitute the O-hexyl chain of xanomeline with polar, ionizable, or conformationally restricted moieties were assessed for their ability to bind to the M1 receptor in a wash-resistant manner (persistent binding). From our screen, several novel ligands that persistently bind to the M1 receptor with greater affinity than xanomeline were discovered. Results indicate that persistent binding may arise not only from hydrophobic interactions but also from ionic interactions with a secondary M1 receptor binding site. Herein, a qualitative model that accounts for both binding scenarios is proposed and applied to understand the structural basis to wash-resistant binding and long-acting effects of xanomeline-based compounds.