DK2571874T3 - En krystallinsk form af (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat - Google Patents

En krystallinsk form af (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat Download PDF

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DK2571874T3
DK2571874T3 DK11721413.0T DK11721413T DK2571874T3 DK 2571874 T3 DK2571874 T3 DK 2571874T3 DK 11721413 T DK11721413 T DK 11721413T DK 2571874 T3 DK2571874 T3 DK 2571874T3
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thiophene
crystalline form
chloro
benzo
quinuclidin
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DK11721413.0T
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Patricia Oliver-Shaffer
Gideon Shapiro
Richard Chesworth
Muneki Kishida
Takayuki Ishige
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Forum Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4833—Encapsulating processes; Filling of capsules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B29/00—Single crystals or homogeneous polycrystalline material with defined structure characterised by the material or by their shape
    • C30B29/54—Organic compounds
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B7/00—Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions
    • C30B7/08—Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions by cooling of the solution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Materials Engineering (AREA)
  • Metallurgy (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)

Claims (12)

1. Krystallinsk Form I af (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamid-hydrochlorid-monohydrat, kendetegnet ved et røntgenpulverdiffraktionsmønster med toppe udtrykt som 2Θ ved en eller begge af 17,48 og 20,58 ± 0,20 grader, når målt i forhold til en intern silicium-standard og kendetegnet ved et røntgen-pulverdiffraktionsmønster yderligere med mindst fire toppe, seks toppe, otte toppe eller alle toppe udtrykt som 2Θ ved 4,50, 9,04, 14,60, 15,14, 15,80, 16,60, 18,16, 18,44, 19,48, 21,74 og 25,46 ± 0,20 grader, når målt i forhold til en intern silicium-standard.
2. Krystallinsk Form II af (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat, kendetegnet ved et røntgenpulverdiffraktionsmønster med toppe udtrykt som 2Θ ved en eller begge af 21,16 og 21,38 ± 0,20 grader, når målt i forhold til en intern silicium-standard og kendetegnet ved et røntgen-pulverdiffraktionsmønster yderligere med mindst fire toppe, seks toppe, otte toppe eller alle toppe udtrykt som 2Θ ved 4,48, 9,00, 13,58, 15,62, 16,48, 19,02, 19,44, 22,46 og 25,00 ± 0,20 grader, når målt i forhold til en intern silicium-standard.
3. Farmaceutisk sammensætning omfattende: en terapeutisk effektiv mængde af den krystallinske form ifølge krav 1 eller 2.
4. Den farmaceutiske sammensætning ifølge krav 3 til anvendelse i en fremgangsmåde til behandling af kognitivt tab i et individ som lider af Alzheimers sygdom.
5. Den farmaceutiske sammensætning ifølge krav 3 til anvendelse i en fremgangsmåde til behandling af kognitivt tab i et individ som lider af skizofreni.
6. Den farmaceutiske sammensætning ifølge krav 3 til anvendelse i en fremgangsmåde til forbedring af kognition i et individ som lider af Alzheimers sygdom.
7. Den farmaceutiske sammensætning ifølge krav 3 til anvendelse i en fremgangsmåde til forbedring af kognition i et individ som lider af skizofreni.
8. Fremgangsmåde til fremstilling afen farmaceutisk sammensætning, fremgangsmåden omfattende: at kombinere den krystallinske form ifølge krav 1 eller 2 med en excipiens eller farmaceutisk acceptabel bærer.
9. Fremgangsmåde til fremstilling af den krystallinske form I ifølge krav 1, fremgangsmåden omfattende: a) at opvarme 10-30 vægtprocent af (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid i acetonitril eller et vandigt acetonitril til mellem 60 °C og kogepunktet af opløsningen; b) eventuelt at tilsætte vand til blandingen for fuldkommen at opløse (R)-7-chloro-N(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochloriden; c) at afkøle opløsningen indtil krystaller er akkurat synlige; d) hvis vandindholdet er større end 3 % (v/v) når krystaller er akkurat synlige, at tilsætte acetonitril til blandingen, således at vandindholdet er mindre end 3 % (v/v); e) at afkøle den resulterende blanding til under 15 °C; og f) at isolere krystallinsk (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat.
10. Fremgangsmåden ifølge krav 9, hvor vandet tilsat i trin a) ikke bringer vandindholdet af blandingen over 30 % (v/v), hvor (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid er til stede med 15-25 vægtprocent i trin a), hvor fremgangsmåden yderligere omfatter at tilsætte Form I (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b ]thiophen-2-carboxamid-hydrochlorid-monohydrat til blandingen efter krystaller er akkurat synlige, eller hvor trin c) omfatter at afkøle opløsningen til under 55 °C.
11. Fremgangsmåde til fremstilling af den krystallinske form II ifølge krav 2, fremgangsmåden omfattende: a) at opvarme 5-15 vægtprocent af (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid i 2-butanol eller et vandigt 2-butanol til mellem 60° C og kogepunktet af opløsningen; b) hvis vandindholdet er mindre end 5 % (v/v), at tilsætte vand til blandingen således at vandindholdet ikke er mindre end 5 % (v/v); c) at afkøle opløsningen til under 10 °C; d) at holde den resulterende blanding ved under 10 °C; og e) at isolere krystallinsk (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat.
12. Fremgangsmåde til fremstilling af den krystallinske form II ifølge krav 2, fremgangsmåden omfattende: a) at tilsætte (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid til acetonitril eller vandig acetonitril for at fremstille en sammensætning, som er 10-20 vægtprocent af (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid; b) eventuelt at tilsætte vand til sammensætningen for at gøre vandindholdet 6-10 %; c) eventuelt at afkøle opløsningen til under 10 °C; d) at tillader krystaller at dannes; og e) at isolere krystallinsk (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat.
DK11721413.0T 2010-05-17 2011-05-17 En krystallinsk form af (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat DK2571874T3 (da)

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US34536310P 2010-05-17 2010-05-17
US35209210P 2010-06-07 2010-06-07
PCT/US2011/036844 WO2011146511A1 (en) 2010-05-17 2011-05-17 A crystalline form of (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate

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DK11721413.0T DK2571874T3 (da) 2010-05-17 2011-05-17 En krystallinsk form af (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophen-2-carboxamid-hydrochlorid-monohydrat

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KR101898107B1 (ko) 2018-09-12
PL2571874T3 (pl) 2016-09-30
CR20120585A (es) 2013-05-16
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US20160137638A1 (en) 2016-05-19
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US20140249179A1 (en) 2014-09-04
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