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1. WO2014174066 - CRYSTAL MODIFICATIONS OF ELOBIXIBAT

Publication Number WO/2014/174066
Publication Date 30.10.2014
International Application No. PCT/EP2014/058432
International Filing Date 25.04.2014
IPC
C07D 281/10 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
281Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
02Seven-membered rings
04having the hetero atoms in positions 1 and 4
08condensed with carbocyclic rings or ring systems
10condensed with one six-membered ring
A61K 31/554 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
554having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
A61P 1/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
CPC
A61K 31/554
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
554having at least one nitrogen and one sulfur as ring hetero atoms, e.g. chlothiapine, diltiazem
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
10Laxatives
A61P 1/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
12Antidiarrhoeals
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 1/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
18for pancreatic disorders, e.g. pancreatic enzymes
Applicants
  • ELOBIX AB [SE]/[SE]
Inventors
  • BOHLIN, Martin
  • TJERNELD, Erica
  • VESTERMARK, Andreas
  • YMÉN, Ingvar
Agents
  • NOVITAS PATENT AB
Priority Data
1350517-726.04.2013SE
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) CRYSTAL MODIFICATIONS OF ELOBIXIBAT
(FR) MODIFICATIONS CRISTALLINES D'ÉLOBIXIBAT
Abstract
(EN) The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2- phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.
(FR) La présente invention concerne des modifications cristallines de N-{(2R)-2-[({[3,3-dibutyl-7-(méthylthio)-1,1-dioxido-5-phényl-2,3,4,5-tétrahydro-1,5-benzothiazépin-8-yl]oxy}acétyl)amino]-2-phényléthanolyl}glycine (élobixibat), plus spécifiquement des modifications cristallines des formes I, IV, MeOH-1, EtOH-1, 1-PrOH-1 et 2-PrOH-1. L'invention porte également sur un procédé de préparation de ces modifications cristallines et sur une composition pharmaceutique comprenant la modification cristalline de forme IV.
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