JP7478676B2 - Ｇａｂａ ａ ａｌｐｈａ５ ｐａｍとしての新規イソオキサゾリルエーテル誘導体 - Google Patents

Ｇａｂａ ａ ａｌｐｈａ５ ｐａｍとしての新規イソオキサゾリルエーテル誘導体 Download PDF

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JP7478676B2
JP7478676B2 JP2020569188A JP2020569188A JP7478676B2 JP 7478676 B2 JP7478676 B2 JP 7478676B2 JP 2020569188 A JP2020569188 A JP 2020569188A JP 2020569188 A JP2020569188 A JP 2020569188A JP 7478676 B2 JP7478676 B2 JP 7478676B2
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methyl
pyridazin
isoxazol
methylpyridin
oxa
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JP2021527099A (ja
JPWO2019238633A5 (https=
JP2021527099A5 (https=
Inventor
チェチェーレ，ジュゼッペ
グレープケ・ツビンデン，カトリン
ヘルナンデス，マリア－クレメンシア
クヌスト，ヘンナー
コブレット，アンドレアス
パティニー－アダム，アンジェリーク
ピナール，エマニュエル
ランツ－シュミット，ヴァレリー
シュタイナー，サンドラ
オリバーレス・モラレス，アンドレス・ミゲル
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • 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
    • 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
    • C07D491/08—Bridged 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2020569188A 2018-06-13 2019-06-11 Ｇａｂａ ａ ａｌｐｈａ５ ｐａｍとしての新規イソオキサゾリルエーテル誘導体 Active JP7478676B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP18177522.2 2018-06-13
EP18177522 2018-06-13
EP18177825 2018-06-14
EP18177825.9 2018-06-14
PCT/EP2019/065129 WO2019238633A1 (en) 2018-06-13 2019-06-11 New isoxazolyl ether derivatives as gaba a alpha5 pam

Publications (4)

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JP2021527099A JP2021527099A (ja) 2021-10-11
JPWO2019238633A5 JPWO2019238633A5 (https=) 2022-06-13
JP2021527099A5 JP2021527099A5 (https=) 2022-06-13
JP7478676B2 true JP7478676B2 (ja) 2024-05-07

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JP2020569188A Active JP7478676B2 (ja) 2018-06-13 2019-06-11 Ｇａｂａ ａ ａｌｐｈａ５ ｐａｍとしての新規イソオキサゾリルエーテル誘導体

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US (1) US11840528B2 (https=)
EP (1) EP3807269A1 (https=)
JP (1) JP7478676B2 (https=)
KR (1) KR20210021019A (https=)
CN (1) CN112424196A (https=)
AU (1) AU2019286312B2 (https=)
BR (1) BR112020025355A2 (https=)
CA (1) CA3102101A1 (https=)
CL (1) CL2020003214A1 (https=)
CR (1) CR20200610A (https=)
IL (1) IL279266B2 (https=)
MA (1) MA52868A (https=)
MX (1) MX2020013518A (https=)
PE (1) PE20210555A1 (https=)
PH (1) PH12020500674A1 (https=)
SG (1) SG11202012200QA (https=)
TW (1) TWI816812B (https=)
WO (1) WO2019238633A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI901650B (zh) 2020-03-26 2025-10-21 匈牙利商羅特格登公司 啶及吡啶并〔３，４－ｃ〕嗒衍生物
EP4149933B1 (en) * 2020-05-13 2024-06-12 F. Hoffmann-La Roche AG New triazolyl derivatives as gaba a alpha5 pam
HU231691B1 (hu) 2021-09-29 2025-10-28 Richter Gedeon Nyrt GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok
WO2026009854A1 (ja) * 2024-07-01 2026-01-08 日本たばこ産業株式会社 ピリダジノン化合物及びその医薬用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011505402A (ja) 2007-12-04 2011-02-24 エフ．ホフマン−ラ ロシュ アーゲー イソオキサゾロ−ピリダジン誘導体
JP2011505401A (ja) 2007-12-04 2011-02-24 エフ．ホフマン−ラ ロシュ アーゲー イソオキサゾロ−ピリジン誘導体
JP2011523945A (ja) 2008-05-19 2011-08-25 サノビオン ファーマシューティカルズ インク イミダゾ［１，２−ａ］ピリジン化合物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2682301A1 (en) * 2007-04-18 2008-10-30 Astrazeneca Ab Xanthine compounds having a positive allosteric gabab receptor modulator effect
JP5460858B2 (ja) * 2009-05-05 2014-04-02 エフ．ホフマン−ラ ロシュ アーゲー イソオキサゾール−ピラゾール誘導体
US8604062B2 (en) 2011-10-20 2013-12-10 Hoffman-La Roche Inc. Process for the preparation of isoxazolyl-methoxy nicotinic acids
US8785435B2 (en) 2011-10-20 2014-07-22 Hoffmann-La Roche Inc. Solid forms
BR112019006571A2 (pt) 2016-12-08 2019-07-02 F. Hoffmann-La Roche Ag derivados de éter de isoxazolila como gaba a alfa5 pam

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011505402A (ja) 2007-12-04 2011-02-24 エフ．ホフマン−ラ ロシュ アーゲー イソオキサゾロ−ピリダジン誘導体
JP2011505401A (ja) 2007-12-04 2011-02-24 エフ．ホフマン−ラ ロシュ アーゲー イソオキサゾロ−ピリジン誘導体
JP2011523945A (ja) 2008-05-19 2011-08-25 サノビオン ファーマシューティカルズ インク イミダゾ［１，２−ａ］ピリジン化合物

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JP2021527099A (ja) 2021-10-11
BR112020025355A2 (pt) 2021-03-09
CA3102101A1 (en) 2019-12-19
CL2020003214A1 (es) 2021-05-07
SG11202012200QA (en) 2021-01-28
US11840528B2 (en) 2023-12-12
AU2019286312A1 (en) 2021-01-07
MX2020013518A (es) 2021-02-26
MA52868A (fr) 2021-04-21
PE20210555A1 (es) 2021-03-17
PH12020500674A1 (en) 2021-06-07
KR20210021019A (ko) 2021-02-24
WO2019238633A1 (en) 2019-12-19
AU2019286312B2 (en) 2023-08-17
TWI816812B (zh) 2023-10-01
TW202016106A (zh) 2020-05-01
IL279266B2 (en) 2024-03-01
US20210094945A1 (en) 2021-04-01
EP3807269A1 (en) 2021-04-21
CR20200610A (es) 2021-02-05
IL279266B1 (en) 2023-11-01
IL279266A (en) 2021-01-31
CN112424196A (zh) 2021-02-26

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