153910-63-5

Upstream product

• 990-91-0 dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate 
• 134098-64-9 2‐{3‐[(O‐tert‐butyldimethylsilyl)hydroxy]‐1,1‐dimethylpropyl}‐3,5‐dimethylphenol 
• 924-50-5 Methyl 3,3-dimethylacrylate 
• 108-68-9 3,5-Dimethylphenol 
• 40662-14-4 4,4,5,7-tetramethyl-3,4-dihydrocoumarin 
• 129967-42-6 2‐(3‐hydroxy‐1,1‐dimethylpropyl)‐3,5‐dimethylphenol 

Downstream Products

• 153910-64-6 3-(2-((bis(benzyloxy)phosphoryl)oxy)-4,6-dimethylphenyl)-3-methylbutanoic acid 
• 1581704-58-6 ((S)-3-((2R,3S)-3-carbamoyl-6,6,6-trifluoro-2-(3,3,3-trifluoropropyl)hexanamido)-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)methyl3-(2-((bis(benzyloxy)phosphoryl)oxy)-4,6-dimethylphenyl)-3-methylbutanoate 
• 183867-87-0 (S)-6-Benzyloxycarbonylamino-2-{3-[2-(bis-benzyloxy-phosphoryloxy)-4,6-dimethyl-phenyl]-3-methyl-butyrylamino}-hexanoic acid methyl ester 
• 183867-89-2 (S)-2-{3-[2-(Bis-benzyloxy-phosphoryloxy)-4,6-dimethyl-phenyl]-3-methyl-butyrylamino}-succinic acid 4-benzyl ester 1-methyl ester 
• 183867-86-9 (S)-2-{3-[2-(Bis-benzyloxy-phosphoryloxy)-4,6-dimethyl-phenyl]-3-methyl-butyrylamino}-3-phenyl-propionic acid methyl ester 
• 183867-84-7 Phosphoric acid dibenzyl ester 2-[2-(4-methoxy-phenylcarbamoyl)-1,1-dimethyl-ethyl]-3,5-dimethyl-phenyl ester 
• 183867-85-8 {3-[2-(Bis-benzyloxy-phosphoryloxy)-4,6-dimethyl-phenyl]-3-methyl-butyrylamino}-acetic acid methyl ester 
• 183867-91-6 Phosphoric acid mono-{2-[2-(4-methoxy-phenylcarbamoyl)-1,1-dimethyl-ethyl]-3,5-dimethyl-phenyl} ester 
• 153910-62-4 3-(2-((bis(benzyloxy)phosphoryl)oxy)-4,6-dimethylphenyl)-3-methylbutanoic acid 

Relevant academic research and scientific papers

A General Approach to Enzyme-Responsive Liposomes

Liposomes are effective nanocarriers due to their ability to deliver encapsulated drugs to diseased cells. Nevertheless, liposome delivery would be improved by enhancing the ability to control the release of contents at the target site. While various stimuli have been explored for triggering liposome release, enzymes provide excellent targets due to their common overexpression in diseased cells. We present a general approach to enzyme-responsive liposomes exploiting targets that are commonly aberrant in disease, including esterases, phosphatases, and β-galactosidases. Responsive lipids correlating with each enzyme family were designed and synthesized bearing an enzyme substrate moiety attached via a self-immolating linker to a non-bilayer lipid scaffold, such that enzymatic hydrolysis triggers lipid decomposition to disrupt membrane integrity and release contents. Liposome dye leakage assays demonstrated that each enzyme-responsive liposome yielded significant content release upon enzymatic treatment compared to minimal release in controls. Results also showed that fine-tuning liposome composition was critical for controlling release. DLS analysis showed particle size increases in the cases of esterase- and β-galactosidase-responsive lipids, supporting alterations to membrane properties. These results showcase an effective modular strategy that can be tailored to target different enzymes, providing a promising new avenue for advancing liposomal drug delivery.

INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE

The present invention provides a compound of formula (II): an inhibitor of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases. Its prodrugs are disclosed.

Combretastatin analogue water-soluble pre-- prodrug and its preparation method

The invention relates to a combretastatin A-4 analogue pro-prodrug, and a preparation method thereof. The structure formula of the combretastatin A-4 analogue pro-prodrug is represented by a formula in the invention; and the combretastatin A-4 analogue pr

PRODRUGS OF 1,4-BENZODIAZEPINONE COMPOUNDS

Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein.

ANTI-VIRAL COMPOUNDS

Compounds effective in inhibiting replication of Hepatitis C virus ( HCV ) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, coformulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.

Phosphate prodrugs for amines utilizing a fast intramolecular hydroxy amide lactonization

A novel phosphate prodrug system for amines, amino acids, peptides, and peptide mimetics, which utilizes a fast hydroxy amide lactonization of a 3-(2'-hydroxy-4',6'-dimethylphenyl)-3,3-dimethylpropionic amide system, was developed. Prodrugs of five model amine/amino acids, including p-anisidine, GlyOMe, PheOMe, LysOMe, and Asp-α-OMe, were synthesized. The syntheses of these model phosphate prodrugs were accomplished by coupling the amine or the protected amino acids with 3-[2'-(dibenzylphosphono)oxy-4',6'-dimethylphenyl]-3,3-dimethylpropion ic acid using coupling agents such as bis(2-oxo-3-oxazolidinyl)phosphinic chloride and 1-(3-dimethylamino)propyl)-3-ethylcarbodiimide hydrochloride, followed by hydrogenolysis. These phosphate prodrugs were evaluated as substrates for the human placental alkaline phosphatase (AP). The structural features of the amine/amino acids attached to the carboxylic acid group of the promoiety were not found to significantly affect the substrate activity for AP, as evidenced by the small variations observed in the Michaelis-Menten parameters (K(m) and V(max)) of the phosphate prodrugs. Results obtained from this study suggest that such a phosphate prodrug system may be applied to a variety of structurally diverse amine-containing drugs.

Benzoate derivatives of taxol

This invention relates to a compound of formula I STR1 or a pharmaceutically acceptable salt thereof, in which R2 is a radical of the formula STR2 in which Ra and Rb are independently hydrogen or C1-6 alkyl, said C1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C1-6 alkyl) amino; or NRa Rb together represents a radical of the formula STR3 in which y is one to three, and Ra is as defined above; Rp and Rr are independently same or different C1-6 alkyl; R1 is hydrogen or a radical Z of the formula STR4 in which Q is --(CH2)f --, optionally substituted with one to six same or different C1-6 alkyl or C3-6 cycloalkyl, or a carbon atom of said --(CH2)f -- radical may also be a part of C3-6 cycloalkylidene; R3 and R4 are independently hydrogen or C1-6 alkyl, or R3 and R4 taken together with the carbon atom to which they are attached form C3-6 cycloalkylidene; R5 is --OC(=O)R, --OP=O(OH)2 or --CH2 OP=O(OH)2, in which R is C1-6 alkyl; R6, R7, R8 and R9 are independently halogen, C1-6 alkyl, C1-6 alkoxy or hydrogen, but when R5 is --OC(=O)R, one of R6, R7, R8 or R9 is --OP=O(OH)2 ; f is 2 to 6; n is O, and m is 1 or 0 when R5 is --CH2 OP=O(OH)2 ; and n is 1 or 0, and m is 1 when R5 is --OC(=O)R or --OP=O(OH)2. Also provided by this invention are pharmaceutical formulations and a method for treating mammalian tumors with a compound of formula I.

Phosphonooxy and carbonate derivatives of taxol

The present invention is directed to novel taxol derivatives useful as anti-tumor agents. Also provided by this invention is pharmaceutical formulations and methods of treating mammalian tumors with the compounds of this invention.