DK3078667T3 - Formulering af borsyreforbindelser - Google Patents

Formulering af borsyreforbindelser Download PDF

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Publication number
DK3078667T3
DK3078667T3 DK16157001.5T DK16157001T DK3078667T3 DK 3078667 T3 DK3078667 T3 DK 3078667T3 DK 16157001 T DK16157001 T DK 16157001T DK 3078667 T3 DK3078667 T3 DK 3078667T3
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DK
Denmark
Prior art keywords
compound
mannitol
boronic acid
formula
alkyl
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DK16157001.5T
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English (en)
Inventor
Shanker Gupta
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The United States Of America Represented By The Sec Dep Of Health And Human Services
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Claims (12)

1. Fremgangsmåde til fremstilling af en lyofiliseret forbindelse med formlen (1):
hvor P er hydrogen eller en aminogruppebeskyttende enhed; R er hydrogen eller alkyl; A er 0, 1 eller 2; R1, R2 og R3 hver især uafhængigt er hydrogen, alkyl, cycloalkyl, aryl eller -CH2-R5; R5 i hvert tilfælde er aryl, aralkyl, alkaryl, cycloalkyl, heterocyclyl, heteroaryl eller -W-R6, hvor W er et chalcogen, og R6 er alkyl; hvor ringdelen af hvert aryl, aralkyl, alkyaryl, cykloalkyl, heterocyclyl eller heteroaryl i R1, R2, R3 eller R5 eventuelt kan være substitueret; og Z1 og Z2 sammen danner en enhed, der er afledt af mannitol; hvilken fremgangsmåde omfatter: (a) fremstilling af en blanding omfattende (i) vand, (ii) en forbindelse med formel (3)
(3) hvor P, R, A, R1, R2, og R3 er som beskrevet ovenfor; og Z' og Z" er OH; (iii) mannitol; og (iv) et vandblandbart opløsningsmiddel; hvor mannitol og forbindelsen med formel (3) er til stede i et w/w-forhold på 10:1; og (b) lyofilisering af blandingen; hvor: forbindelsen med formel (1) er en mannitolester af /V-(2-pyrazin)carbonyl-L-phenylalanin-L-leucinborsyre; og forbindelsen med formel (3) er /\/-(2-pyrazin)carbonyl-L-phenylalanin-L-leucin-borsyre.
2. Fremgangsmåde ifølge krav 1, hvor mannitol er D-mannitol, og forbindelsen med formel (1) er D-mannitol /\/-(2-pyrazin)carbonyl-L-phenylalanin-L-leucin-boronat.
3. Fremgangsmåde ifølge krav 1, hvor det vandblandbare opløsningsmiddel er en alkohol.
4. Fremgangsmåde ifølge krav 3, hvor den vandige opløsningsmiddelblanding omfatter 5 % til 95 % v/v alkohol.
5. Fremgangsmåde ifølge krav 3, hvor alkoholen er tø/7-butanol.
6. Fremgangsmåde ifølge krav 5, hvor den vandige opløsningsmiddelblanding omfatter 40 % v/v tø/7-butanol.
7. Lyofiliseret sammensætning omfattende en forbindelse med formlen (1):
O) hvor P er hydrogen eller en aminogruppebeskyttende enhed; R er hydrogen eller alkyl; A er 0, 1 eller 2; R1, R2 R3 hver især uafhængigt er hydrogen, alkyl, cycloalkyl, aryl eller -CH2-R5; R5 i hvert tilfælde er aryl, aralkyl, alkaryl, cycloalkyl, heterocyclyl, heteroaryl eller -W-R6, hvor W er et chalcogen, og R6 er alkyl; hvor ringdelen af hvert aryl, aralkyl, alkyaryl, cykloalkyl, heterocyclyl eller heteroaryl i R1, R2, R3 eller R5 eventuelt kan være substitueret; og Z1 og Z2 sammen danner en enhed, der er afledt af mannitol; hvor den lyofiliserede sammensætning er fremstillet ved en fremgangsmåde, der omfatter: (a) fremstilling af en blanding omfattende (i) vand,
(ii) en forbindelse med formel (3)
(3) hvor P, R, A, R1, R2, og R3 er som beskrevet ovenfor; og Z' og Z" er OH; (iii) mannitol; og (iv) et vandblandbart opløsningsmiddel; hvor mannitol og forbindelsen med formel (3) er til stede i et w/w-forhold på 10:1; og (b) lyofilisering af blandingen; hvor: forbindelsen med formel (1) er en mannitolester af /V-(2-pyrazin)carbonyl-L-phenylalanin-L-leucinborsyre; og forbindelsen med formel (3) er /V-(2-pyrazin)carbonyl-L-phenylalanin-L-leucin-borsyre.
8. Lyofiliseret sammensætning ifølge krav 7, hvor mannitol er D-mannitol, og forbindelsen med formel (1) er D-mannitol /V-(2-pyrazin)carbonyl-L-phenylala-nin-L-leucinboronat.
9. Lyofiliseret sammensætning ifølge krav 7, hvor det vandblandbare opløsningsmiddel er en alkohol.
10. Lyofiliseret sammensætning ifølge krav 9, hvor den vandige opløsningsmiddelblanding omfatter 5 % til 95 % v/v alkohol.
11. Lyofiliseret sammensætning ifølge krav 9, hvor alkoholen er tø/'f-butanol.
12. Lyofiliseret sammensætning ifølge krav 11, hvor den vandige opløsningsmiddelblanding omfatter 40 % v/v tø/'f-butanol.
DK16157001.5T 2001-01-25 2002-01-25 Formulering af borsyreforbindelser DK3078667T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26416001P 2001-01-25 2001-01-25
EP10006835.2A EP2251344B2 (en) 2001-01-25 2002-01-25 Formulation of boronic acid compounds

Publications (1)

Publication Number Publication Date
DK3078667T3 true DK3078667T3 (da) 2019-01-07

Family

ID=23004871

Family Applications (3)

Application Number Title Priority Date Filing Date
DK02709145.3T DK1355910T3 (da) 2001-01-25 2002-01-25 Formulering af borsyreforbindelser
DK10006835.2T DK2251344T3 (da) 2001-01-25 2002-01-25 Formulering af boronsyreforbindelser
DK16157001.5T DK3078667T3 (da) 2001-01-25 2002-01-25 Formulering af borsyreforbindelser

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DK10006835.2T DK2251344T3 (da) 2001-01-25 2002-01-25 Formulering af boronsyreforbindelser

Country Status (15)

Country Link
US (5) US6713446B2 (da)
EP (4) EP2251344B2 (da)
JP (2) JP4162491B2 (da)
AT (1) ATE501157T1 (da)
AU (1) AU2002243646B2 (da)
CA (2) CA2435146C (da)
CY (2) CY1111488T1 (da)
DE (1) DE60239384D1 (da)
DK (3) DK1355910T3 (da)
ES (3) ES2359391T3 (da)
FI (1) FI2251344T4 (da)
HK (1) HK1149936A1 (da)
PT (2) PT1355910E (da)
TR (1) TR201819416T4 (da)
WO (2) WO2002059130A1 (da)

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