DK2296464T3 - Salte og polymorfer af en tetracyclinforbindelse - Google Patents

Salte og polymorfer af en tetracyclinforbindelse Download PDF

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DK2296464T3
DK2296464T3 DK09751737.9T DK09751737T DK2296464T3 DK 2296464 T3 DK2296464 T3 DK 2296464T3 DK 09751737 T DK09751737 T DK 09751737T DK 2296464 T3 DK2296464 T3 DK 2296464T3
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compound
solvents
polymorph
tosylate salt
combination
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DK09751737.9T
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Raymond Cvetovich
Tadeusz Warchol
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Paratek Pharm Innc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/65—Tetracyclines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/22—Separation; Purification; Stabilisation; Use of additives
    • C07C231/24—Separation; Purification
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Claims (19)

1. Krystallinsk form af et tosylatsalt af forbindelse 1:
(i)·
2. Polymorf af den krystallinske form ifølge krav 1, kendetegnet ved et røntgenpulverdiffraktionsmønster, der indbefatter toppe ved ca. 8,06, 13,02 og 18,83 °20 ved anvendelse af Cu Κα-stråling eller toppe ved ca. 8,06, 11,41, 13,02, 18,83, 20,54 og 24,53 °20 ved anvendelse af Cu Κα-stråling eller toppe ved ca. 5,60, 8,06, 8,57, 11,41, 13,02, 15,58, 18,83, 20,54 og 24,53 °20 ved anvendelse af Cu Κα-stråling, eller ved et røntgenpulverdiffraktionsmønster, som i alt væsentligt svarer til det, som er angivet i figur 8.
3. Polymorf ifølge krav 2, som er opnået ved krystallisering af et tosylatsalt af forbindelse 1: OX fra isopropanol.
4. Fremgangsmåde til fremstilling af et stabilt krystallinsk tosylatsalt af forbindelse 1:
(i), hvor fremgangsmåden omfatter: opløsning af en fri base af forbindelse 1 i et første opløsningsmiddel eller en første kombination af opløsningsmidler for at danne en første opløsning; opløsning af p-toluensulfonsyre i et andet opløsningsmiddel eller en anden kombination af opløsningsmidler for at danne en anden opløsning; kombinering af den første og den anden opløsning for at danne en tredje opløsning; og tilsætning af en form 1-polymorf af et tosylatsalt af forbindelse 1 som en podekrystal til den tredje opløsning for at danne en fjerde opløsning.
5. Fremgangsmåde ifølge krav 4, hvor det første opløsningsmiddel/den første kombination af opløsningsmidler og det andet opløsningsmiddel/den anden kombination af opløsningsmidler er ens eller forskellige.
6. Fremgangsmåde ifølge krav 4, hvor den første kombination af opløsningsmidler og den anden kombination af opløsningsmidler hver uafhængigt er en kombination af alkoholiske opløsningsmidler.
7. Fremgangsmåde ifølge krav 6, hvor den første kombination af opløsningsmidler og den anden kombination af opløsningsmidler hver uafhængigt er en kombination af to alkoholiske opløsningsmidler, eventuelt hvor de to alkoholiske opløsningsmidler er ethanol og isopropanol, for eksempel hvor ethanolet og isopropanolet er til stede i et volumen:volumen-forhold på 2:1.
8. Fremgangsmåde ifølge krav 4, hvor den første kombination af opløsningsmidler og den anden kombination af opløsningsmidler hver omfatter et alkoholisk opløsningsmiddel, som eventuelt er methanol, og et anti-opløsningsmiddel, som eventuelt er valgt blandt en keton, en ester og en ether (f.eks. methyl-t-butylether).
9. Fremgangsmåde ifølge krav 4, hvor den første kombination af opløsningsmidler og den anden kombination af opløsningsmidler hver omfatter methanol og methyl-t-butylether, eventuelt hvor methanolet og methyl-t-butyletheren er til stede i et volumen:volumen-forhold på 1:1,2.
10. Fremgangsmåde ifølge krav 4, hvor p-toluensulfonsyren tilvejebringes i en mængde på fra 25 til 75 vægtprocent i forhold til mængden af forbindelsen 1.
11. Fremgangsmåde ifølge krav 4, hvor p-toluensulfonsyren tilvejebringes i form af et p-toluensulfonsyre-monohydrat.
12. Fremgangsmåde ifølge krav 4, hvor den fjerde opløsning danner en opslæmning efter omrøring, og hvor fremgangsmåden eventuelt endvidere omfatter tørring af opslæmningen.
13. Polymorf af et tosylatsalt af forbindelse 1:
(i), som er opnået ved fremgangsmåden ifølge krav 4.
14. Polymorf af den krystallinske form ifølge krav 1, kendetegnet ved et røntgenpulverdiffraktionsmønster, der indbefatter toppe ved ca. 5,11 og 15,60 °2Θ ved anvendelse af Cu Κα-stråling eller toppe ved ca. 5,11, 8,89, 10,34, 11,76 og 15,60 °26 ved anvendelse af Cu Κα-stråling eller toppe ved ca. 5,11, 8,89, 10,34, 11,76, 13,70, 14,81 og 15,60 °26 ved anvendelse af Cu Κα-stråling, eller ved et røntgenpulverdiffraktionsmønster, som i alt væsentligt svarer til det, som er angivet i figur 10.
15. Polymorf af den krystallinske form ifølge krav 1, kendetegnet ved et røntgenpulverdiffraktionsmønster, der indbefatter toppe ved ca. 11,88 og 16,12 °26 ved anvendelse af Cu Κα-stråling eller toppe ved ca. 7,82, 11,88, 16,12 og 21,46 °26 ved anvendelse af Cu Κα-stråling eller toppe ved ca. 7,82, 11,88, 12,68, 16,12, 18,63, 21,46 og 23,74 °26 ved anvendelse af Cu Κα-stråling, eller ved et røntgenpulverdiffraktionsmønster, som i alt væsentligt svarer til det, som er angivet i figur 9.
16. Polymorf ifølge krav 14, som er opnået ved krystallisering af et tosylatsalt af forbindelse 1:
(IX fra acetone, methylethylketon, methylpentanon eller ethylacetat.
17. Polymorf ifølge krav 15, som er opnået ved krystallisering af et tosylatsalt af forbindelse 1:
OX fra dichlormethan.
18. Farmaceutisk sammensætning, som omfatter den krystallinske form ifølge krav 1 eller polymorfen ifølge et hvilket som helst af kravene 2 og 13-15 og en farmaceutisk acceptabel diluent, excipiens eller bærer.
19. Farmaceutisk sammensætning ifølge krav 18, hvori polymorfen forefindes i ren form.
DK09751737.9T 2008-05-23 2009-05-26 Salte og polymorfer af en tetracyclinforbindelse DK2296464T3 (da)

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US12871208P 2008-05-23 2008-05-23
PCT/US2009/045143 WO2009143509A1 (en) 2008-05-23 2009-05-26 Salts and polymorphs of a tetracycline compound

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EP (3) EP2296464B1 (da)
JP (6) JP5727930B2 (da)
KR (1) KR101679362B1 (da)
CN (4) CN102105058B (da)
AR (1) AR075447A1 (da)
AU (2) AU2009248795B2 (da)
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CA (2) CA2724897C (da)
CO (1) CO6300898A2 (da)
CY (2) CY1116436T1 (da)
DK (2) DK2296464T3 (da)
EC (1) ECSP10010704A (da)
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HR (2) HRP20150584T1 (da)
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MY (1) MY156254A (da)
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PL (2) PL2807926T3 (da)
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TW (5) TWI680117B (da)
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