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Treatment paradigm for an Anti-cd19 antibody and venetoclax combination treatment

an anti-cd19 antibody and treatment paradigm technology, applied in the field of treatment paradigm for anticd19 antibody and venetoclax combination treatment, can solve the problem of dramatic decrease in the activity of the enzyme, and achieve the effect of facilitating the processing of active compounds and preventing inactivation

Pending Publication Date: 2021-09-23
MORFOZIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a compound that can be administered through various routes such as injection or oral application. It can be coated to prevent inactivation and can be formulated as a solution, gel, or cream for topical administration. The compound can be mixed with other materials like carriers, diluents, and excipients to facilitate processing and can take a form suitable for multiple modes of administration like injection, nasal, and vaginal.

Problems solved by technology

It is well recognized that agents which bind to and inactivate the active site metal ion dramatically decrease the activity of the enzyme.
The lack of optimal selectivity can be a cause for clinical toxicity due to unintended inhibition of these off-target metalloenzymes.

Method used

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  • Treatment paradigm for an Anti-cd19 antibody and venetoclax combination treatment
  • Treatment paradigm for an Anti-cd19 antibody and venetoclax combination treatment
  • Treatment paradigm for an Anti-cd19 antibody and venetoclax combination treatment

Examples

Experimental program
Comparison scheme
Effect test

example 1

1-(6,7-Bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1H-1,2,3-triazol-4-yl)propan-1-ol (3)

[0139]To a stirred solution of A (18 g, 69 mmol) in DCM (180 mL) was added BBr3 (87.2 g, 348 mmol) dropwise at −40° C. After completion of addition, stirring was continued for 1 h at −40° C. and 1 h at RT. The reaction mixture was poured into cold water and aqueous layer was then extracted with DCM (2×200 mL). The combined organic extracts were washed with water (100 mL), brine (100 mL) and dried over anhydrous Na2SO4. After filtration and evaporation of solvent under reduced pressure, the crude material was purified by column chromatography (SiO2, 100-200 mesh) to afford K (9.0 g, 39 mmol, 56%) as a brown solid. 1H NMR (200 MHz, CDCl3): δ□8.29 (s, 1H), 7.88 (dd, J=8.8, 1.6 Hz, 1H), 7.68 (d, J=8.6 Hz, 1H), 7.36 (s, 1H), 7.26 (s, 1H), 5.88 (br s, 2H), 3.79-3.63 (m, 1H), 1.27 (d, J=6.8 Hz, 6H).

To a stirred solution of K (5.0 g, 21.7 mmol) in DMF (50 mL) were added ethyl bromo difluoroacetate (...

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Abstract

The instant invention describes pharmaceutical compositions and dosing regimens comprising seviteronel and / or dexamethasone, and methods of treating diseases, disorders or symptoms thereof.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. Provisional Application No. 62 / 595,918, filed Dec. 7, 2017, which is incorporated herein by reference in its entirety.BACKGROUND[0002]Living organisms have developed tightly regulated processes that specifically import metals, transport them to intracellular storage sites and ultimately transport them to sites of use. One of the most important functions of metals such as zinc and iron in biological systems is to enable the activity of metalloenzymes. Metalloenzymes are enzymes that incorporate metal ions into the enzyme active site and utilize the metal as a part of the catalytic process. More than one-third of all characterized enzymes are metalloenzymes.[0003]The function of metalloenzymes is highly dependent on the presence of the metal ion in the active site of the enzyme. It is well recognized that agents which bind to and inactivate the active site metal ion dramatically decrease the activity...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07K16/28A61K31/635
CPCC07K16/2803A61K2039/545A61K31/635A61K31/09A61K31/4192A61K31/573A61P35/00C07D249/04A61K2300/00C07K2317/565
Inventor KELEMEN, PETERSCHWARZ, MICHAELWINDERLICH, MARKHEEGER, STEFFENWEINELT, DOMINIKA
Owner MORFOZIS AG
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