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Compound, synthetic intermediate, use, pharmaceutical composition, and neuromodulatory therapeutic method

A technology of compounds, uses, applied in pharmaceutical sciences, chemistry and biology, medicine

Pending Publication Date: 2020-03-17
REMER CONSULTORES ASSESSORIA EMPRESARIAL LTDA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the neurodegenerative component of the disease remains the greatest challenge for new treatments

Method used

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  • Compound, synthetic intermediate, use, pharmaceutical composition, and neuromodulatory therapeutic method
  • Compound, synthetic intermediate, use, pharmaceutical composition, and neuromodulatory therapeutic method
  • Compound, synthetic intermediate, use, pharmaceutical composition, and neuromodulatory therapeutic method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0209] Example 1. Stability test under extreme conditions - superiority of compounds of the present invention over vasopressin sex

[0210] In this embodiment, the stability of the compounds of the invention in the NFKF embodiment was compared to the stability of vasopressin (Hp, PVNFKFLSH) under extreme conditions. Hp is known to have problems with fibril formation and its variants contain more amino acids. Two separate tests were performed on NFKF and Hp samples, namely stability testing by freezing for 24 h and heating at 100 °C for 10 min.

[0211] figure 1 The results showed that by freezing for 24h, a considerable part of Hp was lost or degraded (from 140 to 97, i.e. about 31%), such as by HPLC (analytical column is 2.1mm, 10-60% B gradient operation. Solvent A is water / 0.1% TFA, solvent B is acetonitrile / 0.075% TFA) as evidenced by measurements. On the other hand, the compounds of the invention in the NFKF embodiment are much more stable and degrade considerabl...

Embodiment 2

[0213] Example 2. Compounds R 1 -N-AA 1 -K-AA 2 -R 2 Use in the preparation of pharmaceutical compositions

[0214] In this embodiment, compound R 1 -N-AA 1 -K-AA 2 -R 2 is the tetrapeptide NFKF, which was synthesized by chemical synthesis. The peptide has been used in the preparation of an oral liquid pharmaceutical composition comprising 2.7x10 -4 Moles of the peptide and a pharmaceutically acceptable carrier. In this embodiment, the carrier is saline and the pharmaceutical composition is a solution for oral administration. The composition is used for in vivo oral administration to mammals in the following Examples 3-8.

[0215] In other embodiments, the pharmaceutical composition is in the form of tablets, gels, oral liquids or syrups, capsules, suppositories, injections, inhalable forms or adherent forms, optionally containing other active ingredients.

Embodiment 3

[0216] Example 3. Comparison of pharmaceutical compositions comprising compound NFKF with pharmaceutical compositions comprising Hp - in vivo assay test result

[0217] In this example, the effect of the composition of the invention is compared with that of a pharmaceutical composition containing vasopressin (Hp or PVNFKFLSH), whose use as an anticonvulsant is a co-pending project of the same inventor Patent application PCT / BR2017 / 050313.

[0218] figure 2 Test results for NFKF, the compound of the invention, are shown and compared to vasopressin test results, both in the pilocarpine model. The percentage of time relative to the first salivation of the control after the administration of the following therapeutic doses is given: control (saline); vasopressin (Hp or PVNFKFLSH, 0.551334 μmol / kg); vasopressin (0.91889 μmol / kg kg); the peptide NFKF of the present invention (0.540882 μmol / kg); NFKF (0.901469 μmol / kg); or PEP-19 (DIIADDEPLT, 0.908117 μmol / kg). Asterisks indi...

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Abstract

The present invention falls within the fields of pharmacy, medicine, chemistry and biotechnology. The compound of the present invention is a peptide and has shown surprising stability and ease of handling in comparison to the most similar peptide compounds. The pharmaceutical composition of the invention comprises said peptide compound and has shown surprising therapeutic results even when administered orally. In some embodiments, administration of the composition of the invention has delivered superior therapeutic results in comparison to the effects of hemopressin and cannabidiol. In some embodiments, oral administration of the composition of the invention provides significant and surprising results with respect to neuromodulation, in both curative and prophylactic treatment of convulsions, pain threshold modulation and important neuroprotection, also substantially reducing the clinical symptoms of multiple sclerosis.

Description

technical field [0001] The invention belongs to the fields of pharmaceutical science, medicine, chemistry and biotechnology. More specifically, the present invention describes a compound and its use for the preparation of ligands of diagnostic and / or therapeutic value, synthetic intermediates in the preparation of compounds of pharmaceutical value, the use of compounds for the preparation of medicaments , Pharmaceutical compositions and methods of treatment comprising said compounds. The compounds of the present invention are peptidic compounds and exhibit surprising stability and ease of handling compared to more closely related peptidic compounds. The pharmaceutical composition of the present invention comprises said peptide compound and shows surprising therapeutic results even when administered orally. In some embodiments, administration of the compositions of the invention provides superior therapeutic outcomes compared to the effects of hemopressin and cannabidiol. In...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/093C07K5/113C07K7/06A61K38/06A61K38/07A61K38/08G01N33/68A61P25/04A61P25/06A61P25/08A61P25/28A61P1/00A61P9/12A61P19/10A61P3/04A61P3/10A61P3/14A61P5/00A61P5/14
CPCA61P1/00A61P3/04A61P3/10A61P3/14A61P5/00A61P5/14A61P9/12A61P19/10A61P25/04A61P25/06A61P25/08A61P25/28C07K7/06C07K5/06121C07K5/0819C07K5/0812C07K5/06078C07K5/06086C07K5/1021A61K38/00G01N33/948A61P29/00C07K5/101
Inventor R·A·雷默A·S·海曼
Owner REMER CONSULTORES ASSESSORIA EMPRESARIAL LTDA
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