SI3077389T1 - Kristalinična oblika (s)-(2-(6-kloro-7-metil-1h-benzo(d)imidazol-2-il)- 2-metilpirolidin-1-il)(5-metoksi-2-(2h-1,2,3-triazol-2-il)fenil)metanona in njena uporaba kot antagonisti oreksinskega receptorja - Google Patents

Kristalinična oblika (s)-(2-(6-kloro-7-metil-1h-benzo(d)imidazol-2-il)- 2-metilpirolidin-1-il)(5-metoksi-2-(2h-1,2,3-triazol-2-il)fenil)metanona in njena uporaba kot antagonisti oreksinskega receptorja Download PDF

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SI3077389T1
SI3077389T1 SI201430489T SI201430489T SI3077389T1 SI 3077389 T1 SI3077389 T1 SI 3077389T1 SI 201430489 T SI201430489 T SI 201430489T SI 201430489 T SI201430489 T SI 201430489T SI 3077389 T1 SI3077389 T1 SI 3077389T1
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crystalline form
methylpyrrolidin
triazol
imidazol
benzo
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SI201430489T
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Christoph Boss
Christine Brotschi
Markus Gude
Bibia Heidmann
Thierry Sifferlen
Raumer Markus Von
Jodi T. Williams
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Idorsia Pharmaceuticals Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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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Claims (16)

  1. Kristalinična oblika (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2-metilpirolidin-1 -il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanona in njena uporaba kot antagonisti oreksinskega receptorja Patentni zahtevki
    1. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2- metilpirolidin-1 -il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon; označena s: • prisotnostjo vrhov v diagramu rentgenske praškovne difrakcije pri naslednjih uklonskih kotih 2Θ: 8,6°, 15,2° in 21,3°; ali • prisotnostjo vrhov v diagramu rentgenske praškovne difrakcije pri naslednjih uklonskih kotih 2Θ: 13,4°, 18,3° in 24,0°.
  2. 2. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po zahtevku 1, označena s prisotnostjo vrhov v diagramu rentgenske praškovne difrakcije pri naslednjih uklonskih kotih 2Θ: 8,6°, 15,2° in 21,3°.; pri čemer diagram rentgenske praškovne difrakcije dobimo z uporabo kombiniranega sevanja Cu Ka1 in Ka2 brez odvzemanja Ka2; in natančnost vrednosti 2Θ je v območju 2Θ +/- 0,2°.
  3. 3. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po zahtevku 1, označena s prisotnostjo vrhov v diagramu rentgenske praškovne difrakcije pri naslednjih uklonskih kotih 2Θ: 8,6°, 11,5°, 13,4°, 14,6°, 15,2°, 15,5°, 19,3°, 21,3°, 22,4° in 26,4°.; pri čemer diagram rentgenske praškovne difrakcije dobimo z uporabo kombiniranega sevanja Cu Ka1 in Ka2 brez odvzemanja Ka2; in natančnost vrednosti 2Θ je v območju 2Θ +/- 0,2°.
  4. 4. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2I3-triazol-2-i)fenil)metanon po zahtevkih 2 ali 3, ki v bistvu kaže vzorec rentgenske praškovne difrakcije, kot je prikazan na sliki 2.
  5. 5. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 2 do 4, pri čemer je kristalinična oblika hemihidrat.
  6. 6. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 2 do 5, ki jo dobimo: a) z mešanjem 2 g SPOJINE kot amorfnega materiala z 8 ml zmesi etanola/vode z razmerjem volumen/volumen 1/4; b) z dodajanjem okoli 0,05 g kristalizacijskih nastavkov SPOJINE v kristalinični obliki 1; c) s stresanjem pri 300 vrt/min okoli 16 ur pri sobni temperaturi; d) s filtriranjem in izpiranjem kolača z 2 ml etanola/vode 1/4 (v/v) in sušenjem produkta pri sobni temperaturi in znižanim tlakom okoli 10 mbar4 ure; in e) z odprtim uravnoteženjem pri sobni temperaturi in okoli 60-odstotni relativni vlagi 2 uri.
  7. 7. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po zahtevku 1, označena s prisotnostjo vrhov v diagramu rentgenske praškovne difrakcije pri naslednjih uklonskih kotih 2Θ: 13,4°, 18,3° in 24,0°.; pri čemer diagram rentgenske praškovne difrakcije dobimo z uporabo kombiniranega sevanja Cu Ka1 in Ka2 brez odvzemanja Ka2; in natančnost vrednosti 2Θ je v območju 2Θ +/- 0,2°.
  8. 8. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1)2,3-triazol-2-il)fenil)metanon po zahtevku 1, označena s prisotnostjo vrhov v diagramu rentgenske praškovne difrakcije pri naslednjih uklonskih kotih 2Θ: 10,9°, 13,4°, 14,3°, 14,9°, 18,3°, 20,9°, 21,1°, 21,8°, 24,0° in 30,1°.; pri čemer diagram rentgenske praškovne difrakcije dobimo z uporabo kombiniranega sevanja Cu Ka1 in Ka2 brez odvzemanja Ka2; in natančnost vrednosti 2Θ je v območju 2Θ +/- 0,2°.
  9. 9. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-i)fenil)metanon po zahtevkih 7 ali 8, ki v bistvu kaže vzorec rentgenske praškovne difrakcije, kot je prikazan na sliki 3.
  10. 10. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2I3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 7 do 9, pri čemer je kristalinična oblika anhidrat.
  11. 11. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2- metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 7 do 10, ki jo dobimo z: a) mešanjem 10 mg SPOJINE v kristalinični obliki 1 v 0,05 ml acetonitrila; b) mešanjem v zaprti 4-ml viali do tri dni; c) izoliranjem; in sušenjem pri znižanem tlaku in sobni temperaturi 2 uri.
  12. 12. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 1 do 11 za uporabo kot zdravilo.
  13. 13. Farmacevtski sestavek, ki obsega kot učinkovino kristalinično obliko spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 1 do 11, in vsaj en farmacevtsko sprejemljiv nosilec.
  14. 14. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 1 do 11 za uporabo pri proizvodnji farmacevtskega sestavka, pri čemer farmacevtski sestavek obsega kot učinkovino spojino (S)-(2-(6-kloro-7-metil-1 H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon, in vsaj en farmacevtsko sprejemljiv nosilni material.
  15. 15. Kristalinična oblika spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 1 do 11 ali farmacevtski sestavek po zahtevku 13 za uporabo pri zdravljenju ali preprečevanju bolezni ali motnje, ki sta izbrani iz skupine, ki sestoji iz motenj spanja, izbranih iz skupine, ki sestoji iz disomnij, parasomniji, motenj spanja, povezanih s splošnih zdravstvenim stanjem in motenj spanja, povzročenih s snovmi; anksioznostnih motenj; in motenj odvisnosti.
  16. 16. Uporaba kristalinične oblikea spojine (S)-(2-(6-kloro-7-metil-1H-benzo[d]imidazol-2-il)-2-metilpirolidin-1-il)(5-metoksi-2-(2H-1,2,3-triazol-2-il)fenil)metanon po katerem koli od zahtevkov od 1 do 11 za pripravo zdravila za zdravljenje ali preprečevanje bolezni ali motnje, ki sta izbrani iz skupine, ki sestoji iz motenj spanja, anksioznostnih motenj, motenj odvisnosti, kognitivnih disfunkcij, motenj razpoloženja in motenj teka.
SI201430489T 2013-12-03 2014-12-02 Kristalinična oblika (s)-(2-(6-kloro-7-metil-1h-benzo(d)imidazol-2-il)- 2-metilpirolidin-1-il)(5-metoksi-2-(2h-1,2,3-triazol-2-il)fenil)metanona in njena uporaba kot antagonisti oreksinskega receptorja SI3077389T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IB2013060596 2013-12-03
EP14824107.8A EP3077389B1 (en) 2013-12-03 2014-12-02 Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists
PCT/IB2014/066508 WO2015083070A1 (en) 2013-12-03 2014-12-02 Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists

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US (1) US9914720B2 (sl)
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KR (1) KR102361418B1 (sl)
CN (1) CN105793257B (sl)
AU (1) AU2014358742B2 (sl)
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CL (1) CL2016001342A1 (sl)
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