HRP20190842T1 - Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida - Google Patents

Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida Download PDF

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HRP20190842T1
HRP20190842T1 HRP20190842TT HRP20190842T HRP20190842T1 HR P20190842 T1 HRP20190842 T1 HR P20190842T1 HR P20190842T T HRP20190842T T HR P20190842TT HR P20190842 T HRP20190842 T HR P20190842T HR P20190842 T1 HRP20190842 T1 HR P20190842T1
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Croatia
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water
isoxazolo
azepin
chlorophenyl
benzo
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HRP20190842TT
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English (en)
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Michael L. Hall
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Constellation Pharmaceuticals, Inc.
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Publication of HRP20190842T1 publication Critical patent/HRP20190842T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • 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
    • A61P31/12—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (13)

1. Kristalni monohidrat oblika A 2-((4S)-6-(4-hlorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida, pri čemu je kristalni oblik naznačen time što se najmanje tri najviše vrijednosti rendgenske difrakcije praha dostiže pod 2Θkutevima odabranim od 4,73°, 18,09°, 18,48°, 18,80°, 19,70°, i 25,17°.
2. Kristalni monohidrat oblika A sukladno patentnom zahtjevu 1, pri čemu je taj kristalni oblik naznačen time što se najmanje četiri najviših vrijednosti rendgenske difrakcije praha dostiže pod 2Θ kutevima odabranim od 4,73°, 18,.09°, 18,48°, 18,80°, 19,70°, i 25,17°.
3. Kristalni monohidrat oblika A sukladno patentnom zahtjevu 1 ili 2, pri čemu je taj kristalni oblik naznačen time što se najmanje pet najviših vrijednosti rendgenske difrakcije praha dostiže pod 2Θ kutevima odabranim od 4,73°, 18,09°, 18,48°, 18,80°, 19,70°, i 25,17°.
4. Kristalni monohidrat oblika A sukladno bilo kojem od patentnih zahtjeva 1 do 3, pri čemu je, taj kristalni oblik naznačen time što se najviše vrijednosti rendgenske difrakcije praha dostižu pod 2Θkutevima 4,73°, 18,09°, 18,48°, 18,80°, 19,70°, i 25,17°.
5. Kristalni monohidrat oblika A sukladno bilo kojem od patentnih zahtjeva 1 do 4, pri čemu je taj kristalni oblik naznačen time što se najviše vrijednosti rendgenske difrakcije praha dostižu pod 2Θ kutevima 4,73°, 9,42°, 12,91°, 18,09°, 18,48°, 18,80°, 19,70°, 21,42°, i 25,17°.
6. Kristalni monohidrat oblika A sukladno bilo kojem od patentnih zahtjeva 1 do 5, pri čemu je taj kristalni oblik naznačen time što se najviše vrijednosti rendgenske difrakcije praha dostižu pod 2Θ kutevima 4,73°, 8,11°, 9,42°, 12,91°, 14,10°, 14,97°, 18,09°, 18,48°, 18,80°, 19,70°, 21,42°, i 25,17°, 26,07°, i 26,53°.
7. Farmaceutski pripravak koji sadrži oblik kristalnog monohidrata sukladno bilo kojem od patentnih zahtjeva 1 do 6; i farmacutski prihvatljiv nosač ili otapalo.
8. Kristalni monohidrat oblika A 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida sukladno bilo kojem od patentnih zahtjeva radi liječenja proliferativnog poremećaja, bolesti upale, sepse, autoimunih bolesti, ili virusne infekcije.
9. Kristalni monohidrat oblika A 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida za uporabu sukladno patentnom zahtjevu 8, pri čemu je taj poremećaj karcinom.
10. Postupak dobivanja kristalnog monohidrata oblika A 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida, taj postupak obuhvaća: stvaranje kristalnog monohidrata oblika A iz otopine koja sadrži amorfni 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamid i vodu; ili iz mješavine koja sadrži amorfni 2-((4S)-6-(4-klorofenil)-1-metil-4H-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamid, i kombinaciju vode i organskog otapala.
11. Postupak sukladno patentnom zahtjevu 10, pri čemu se kombinacija vode i organskog otapala izabire od etanola/vode, izopropanola/vode, tetrahidrofurana/vode, acetona/vode, metanola/vode, i acetonitrila/vode.
12. Postupak sukladno patentnom zahtjevu 10 ili 11, pri čemu je kombinacija vode i organskog otapala etanol/voda.
13. Postupak sukladno bilo kojem od patentnih zahtjeva 10 do 12, pri čemu je kombinacija vode i organskog otapala u odnosu od 60:40 mješavine etanola/vode
HRP20190842TT 2014-06-20 2019-05-07 Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida HRP20190842T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462014782P 2014-06-20 2014-06-20
EP15733597.7A EP3157928B1 (en) 2014-06-20 2015-06-18 Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
PCT/US2015/036347 WO2015195862A1 (en) 2014-06-20 2015-06-18 Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4s5-e]azepin-4-yl)acetamide

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HRP20190842T1 true HRP20190842T1 (hr) 2019-08-09

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HRP20190842TT HRP20190842T1 (hr) 2014-06-20 2019-05-07 Kristalni oblici 2-((4s)-6-(4-hlorofenil)-1-metil-4h-benzo[c]izoksazolo[4,5-e]azepin-4-il)acetamida

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US (1) US9969747B2 (hr)
EP (1) EP3157928B1 (hr)
JP (1) JP6682522B2 (hr)
CN (1) CN106687463B (hr)
CA (1) CA2952830C (hr)
CY (1) CY1121997T1 (hr)
DK (1) DK3157928T3 (hr)
ES (1) ES2725928T3 (hr)
HR (1) HRP20190842T1 (hr)
HU (1) HUE043441T2 (hr)
LT (1) LT3157928T (hr)
PL (1) PL3157928T3 (hr)
PT (1) PT3157928T (hr)
RS (1) RS58730B1 (hr)
SI (1) SI3157928T1 (hr)
TR (1) TR201906788T4 (hr)
WO (1) WO2015195862A1 (hr)

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WO2021091535A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor
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JP2024517472A (ja) 2021-05-11 2024-04-22 コンステレーション・ファーマシューティカルズ・インコーポレイテッド 貧血を処置するためのペラブレシブの使用
WO2023147149A1 (en) * 2022-01-31 2023-08-03 Constellation Pharmaceuticals, Inc. Anhydrous crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide

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RS58730B1 (sr) 2019-06-28
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