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1. WO2013095169 - CRYSTALLINE MINOCYCLINE THERMO-RESISTANT OBTAINED BY RECRYSTALLIZATION WITH CARBON DIOXIDE

Publication Number WO/2013/095169
Publication Date 27.06.2013
International Application No. PCT/PT2012/000051
International Filing Date 17.12.2012
IPC
C07C 237/26 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
24having 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
26of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
A61K 31/65 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
65Tetracyclines
A61P 31/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
CPC
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07C 237/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
24having 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
26of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
C07C 2603/46
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2603Systems containing at least three condensed rings
02Ortho- or ortho- and peri-condensed systems
40containing four condensed rings
42containing only six-membered rings
44Naphthacenes; Hydrogenated naphthacenes
461,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
Applicants
  • INSTITUTO SUPERIOR TÉCNICO [PT]/[PT]
  • UNIVERSIDADE DE LISBOA [PT]/[PT]
Inventors
  • RODRIGUES, Miguel Ângelo Joaquim
  • PADRELA, Luís Miguel Borges
  • MATOS, Henrique Aníbal Santos de
  • AZEVEDO, Edmundo José Simões Gomes de
  • PINHEIRO, Lídia Maria Veloso
  • BETTENCOURT, Ana Francisca Campos Simão
  • CASTRO, Matilde Luz Santos Duque Fonseca E
  • ALMEIDA, António José Leitão das Neves
  • DUARTE, Maria Aida da Costa e Silva da Conceição
Agents
  • OLIVEIRA, Arlindo Manuel Limede de [PT]/[PT]
Priority Data
10606319.12.2011PT
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CRYSTALLINE MINOCYCLINE THERMO-RESISTANT OBTAINED BY RECRYSTALLIZATION WITH CARBON DIOXIDE
(FR) MINOCYCLINE CRISTALLINE THERMORÉSISTANTE OBTENUE PAR RECRISTALLISATION AVEC DU DIOXYDE DE CARBONE
Abstract
(EN)
The present invention relates to a novel form of minocycline chlorohydrate characterized in that- it is crystalline and it presents characteristic powder X-ray diffraction pattern and infrared spectrum. This new polymorph constitutes the most stable form of minocycline with a melting point much higher than that of other known crystalline forms of minocycline. The process of production of this new minocycline polymorphic form consists in the dissolution of carbon dioxide in solutions or suspensions of minocycline chlorohydrate with organic solvents, under certain conditions of pressure and temperature. The present invention places minocycline in the restrict group of antibiotics with a melting temperature higher than the sterilization temperature, which enhances new applications and allows the optimization of production at industrial
(FR)
La présente invention se rapporte à une nouvelle forme de chlorhydrate de minocycline caractérisée en ce qu' - il est cristallin et il présente un spectre infrarouge et une figure de diffraction de rayons X sur poudre caractéristiques. Ce nouveau polymorphe constitue la forme la plus stable de minocycline avec un point de fusion beaucoup plus élevé que celui d'autres formes cristallines de minocycline connues. Le processus de production de cette nouvelle forme polymorphe de minocycline consiste à dissoudre du dioxyde de carbone dans des solutions ou suspensions de chlorhydrate de minocycline avec des solvants organiques, dans certaines conditions de pression et de température. La présente invention place la minocycline dans le groupe restreint des antibiotiques ayant une température de fusion supérieure à la température de stérilisation, ce qui améliore les nouvelles et permet l'optimisation de production à l'échelle industrielle.
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Latest bibliographic data on file with the International Bureau