50780-50-2

Upstream product

• 109-02-4 4-methyl-morpholine 
• 100-02-7 4-nitro-phenol 
• 22128-62-7 carbonochloridic acid, chloromethyl ester 
• 144-55-8 sodium hydrogencarbonate 

Downstream Products

• 65815-76-1 O-4-nitrophenyl carbamate of piperidine 
• 101623-71-6 iodomethyl(4-nitrophenyl)carbonate 
• 100-02-7 4-nitro-phenol 
• 99068-88-9 p-nitrophenyl N-iso-propylcarbamate 
• 132906-07-1 chloromethyl N-benzyl carbamate 
• 124068-97-9 4‐nitrophenyl N‐benzylcarbamate 
• 101623-83-0 2,2-dimethylpropionyloxymethyl p-nitrophenyl carbonate 
• 194995-45-4 butyryloxymethyl p-nitrophenyl carbonate 
• 170097-82-2 benzoic acid 4-nitrophenoxycarbonyloxymethyl ester 
• 1427046-45-4 carbonic acid 7-[4-(4-benzo[b]thiophen-4-ylpiperazin-1-yl)butoxy]-2-oxo-2H-quinolin-1-ylmethyl ester 4-nitrophenyl ester 
• 3655-05-8 tert-butoxycarbonylglycine p-nitrophenylester 
• 194995-44-3 2-methylpropionic acid 4-nitro-phenoxycarbonyloxymethyl ester 
• 1541195-54-3 (bis(benzyloxy)phosphoryloxy)methyl 4-nitrophenylcarbonate 
• 1350836-93-9 C₁₆H₁₃N₅O₅ 

Relevant academic research and scientific papers

Macrocyclic prodrugs of a selective nonpeptidic direct thrombin inhibitor display high permeability, efficient bioconversion but low bioavailability

The only oral direct thrombin inhibitors that have reached the market, ximelagatran and dabigatran etexilat, are double prodrugs with low bioavailability in humans. We have evaluated an alternative strategy: the preparation of a nonpeptidic, polar direct

(3S,11aR)-6-[(phenylmethyl)oxy]-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-9 and/or (3S,11aR)-6-[(phenymethyl)oxy]-8-bromo-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-10

The compounds are intermediates in the preparation of therapeutic agents useful in the treatment of viral infections, particularly HIV infection. The compounds are (3S,11aR)-6-[(phenylmethyl)oxy]-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-9 and/or (3S,11aR)-6-[(phenylmethyl)oxy]-8-bromo-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-dione of the formula P-10.

Synthesis of a novel cyclic prodrug of S -allyl-glutathione able to attenuate LPS-induced ROS production through the inhibition of MAPK pathways in U937 cells

A novel cyclic prodrug of S-allyl-glutathione (CP11), obtained by using an acyloxy-alkoxy linker, was estimated for its pharmacokinetic and biological properties. The stability of CP11 was evaluated at pH 1.2, 7.4, in simulated fluids with different concentrations of enzymes, and in human plasma. The anti-inflammatory ability of CP11 was assessed in U937 cells, an immortalized human monocyte cell line. Results showed that CP11 is stable at acidic pH showing a possible advantage for oral delivery due to the longer permanence in the stomach. Having a permeability coefficient of 2.49 × 10-6 cm s-1, it was classified as discrete BBB-permeable compound. Biological studies revealed that CP11 is able to modulate inflammation mediated by LPS in U937 cells preventing the increase of ROS intracellular levels through interaction with the MAPK pathway.

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.

Pharmaceutical composition for the treatment or prevention of stroke and systemic embolism

The present invention relates to a prodrug useful for treating or preventing a stroke and systemic embolism and suitable for being effectively used in the oral delivery of dabigatran, and to a compound represented by chemical formula 1, a pharmaceutically acceptable salt thereof, and a hydrate thereof or a solvate thereof. The compound represented by the chemical formula 1, the pharmaceutically acceptable salt thereof, and the hydrate thereof or the solvate thereof are useful for treating or preventing a stroke and systemic embolism, and is suitable for being effectively used in oral delivery since the absorption rate, that is, bioavailability of dabigatran is improved.(AA) DSC curve of dabigatran pivoxyl (+)-(1S)- campo-10-sulfonateCOPYRIGHT KIPO 2015

CHEMICAL CROSSLINKERS AND COMPOSITIONS THEREOF

Chemical crosslinkers and methods of their synthesis are disclosed.

PROSTAGLANDIN-BISPHOSPHONATE CONJUGATE COMPOUNDS, METHODS OF MAKING SAME, AND USES THEREOF

The invention provides, in part, amino-bisphosphonate-prostaglandin conjugate compounds as well as methods for their synthesis. Said compounds may be used as EP4 agonist compounds in the prevention or treatment of conditions associated with abnormal or excessive bone loss, with abnormal or reduced bone resorption, or with abnormal calcium metabolism.

Azidomethyl 4-nitrophenyl carbonate-A reagent for the one-step introduction of the azidomethyloxycarbonyl (Azoc) protecting group

Presented here is the three-step synthesis of azidomethyl 4-nitrophenyl carbonate in 58% overall yield. This carbonate allows for the high-yielding (≥90%) introduction of the phosphine-labile azidomethyloxycarbonyl (Azoc) protecting group in one step. The reagent protects a range of amines, including amino acids. For nonionic substrates, pure carbamates are obtained after extractive workup. Georg Thieme Verlag Stuttgart - New York.

CHEMICAL COMPOUNDS

The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.

Design, synthesis, and evaluation of novel mutual prodrugs (hybrid drugs) of all-trans-retinoic acid and histone deacetylase inhibitors with enhanced anticancer activities in breast and prostate cancer cells in vitro

Novel mutual prodrugs (MPs) of ATRA (all-trans-retinoic acid) and HDIs (histone deacetylase inhibitors) (10, 13, 17-19) connected via glycine acyloxyalkyl carbamate linker (AC linker) or through a benzyl ester linker (1,6-elimination linker) were rationally designed and synthesized. Most of our novel MPs were potent inhibitors of growth of several hormone-insensitive/drug resistant breast cancer cell lines and the hormone-insensitive PC-3 prostate cancer cell line. The novel MPs exhibited differential antiproliferative potencies in both MDA-MB-231 and PC-3 cell lines. Whereas 19 (VNLG/124) [4-(butanoyloxymethyl)phenyl(2E,4E,6E,8E)-3,7-dimethyl-9-(2,6, 6-trimethylcyclohex-1-enyl)nona-2,4,6,8-tetraenoate] with a GI50 of 10 nM was the most potent MP versus the MDA-MB-231 cells, 13 (VNLG/66) [{N-[N-{2-[4-{[3-pyridylmethoxy)carbonyamino]-methyl}phenyl)carbonylamino] phenyl} carbamoylcarbamoyloxy}methyl(2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6- trimethyl cyclohex-1-enyl)nona-2,4,6,8-tetraenoate] with a GI50 = 40 nM was the most potent versus the PC-3 cells. MP 19 exhibited the most benefit because its GI50 of 10 nM versus MDA-MB-231 cells was remarkably 1085-fold lower than that of parent ATRA and over 100000-fold lower than butyric acid (BA).