JP2022512128A - 医薬化合物およびユビキチン特異的プロテアーゼ１９（ｕｓｐ１９）阻害剤としてのその使用 - Google Patents

医薬化合物およびユビキチン特異的プロテアーゼ１９（ｕｓｐ１９）阻害剤としてのその使用 Download PDF

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JP2022512128A
JP2022512128A JP2021532111A JP2021532111A JP2022512128A JP 2022512128 A JP2022512128 A JP 2022512128A JP 2021532111 A JP2021532111 A JP 2021532111A JP 2021532111 A JP2021532111 A JP 2021532111A JP 2022512128 A JP2022512128 A JP 2022512128A
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methyl
hydroxy
azaspiro
decane
carbonyl
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JP2021532111A
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JP2022512128A5 (https=
JPWO2020115501A5 (https=
Inventor
サミュエル シェイン ラウントゥリー，ジェイムズ
クリストファー ホワイトヘッド，スティーブン
ピオトル トレデル，アダム
エマ プロクター，ローレン
デイビッド シェパード，スティーブン
ブルカンプ，フランク
リタ カストロ コスタ，ジョアナ
オダウド，コリン
ハリソン，ティモシー
ダンカン ヘルム，マシュー
ロジツカ，エヴェリナ
クランストン，アーロン
ジャック，グザヴィエ
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Almac Discovery Ltd
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Almac Discovery Ltd
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Priority claimed from GBGB1819937.2A external-priority patent/GB201819937D0/en
Priority claimed from GBGB1904339.7A external-priority patent/GB201904339D0/en
Priority claimed from GBGB1911311.7A external-priority patent/GB201911311D0/en
Application filed by Almac Discovery Ltd filed Critical Almac Discovery Ltd
Publication of JP2022512128A publication Critical patent/JP2022512128A/ja
Publication of JP2022512128A5 publication Critical patent/JP2022512128A5/ja
Publication of JPWO2020115501A5 publication Critical patent/JPWO2020115501A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/5375—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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
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  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2021532111A 2018-12-06 2019-12-06 医薬化合物およびユビキチン特異的プロテアーゼ１９（ｕｓｐ１９）阻害剤としてのその使用 Pending JP2022512128A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB1819937.2 2018-12-06
GBGB1819937.2A GB201819937D0 (en) 2018-12-06 2018-12-06 Pharmaceutical compounds
GBGB1904339.7A GB201904339D0 (en) 2019-03-28 2019-03-28 Pharmaceutical compounds
GB1904339.7 2019-03-28
GB1911311.7 2019-08-07
GBGB1911311.7A GB201911311D0 (en) 2019-08-07 2019-08-07 Pharmaceutical compounds
PCT/GB2019/053457 WO2020115501A1 (en) 2018-12-06 2019-12-06 Pharmaceutical compounds and their use as inhibitors of ubiquitin specific protease 19 (usp19)

Publications (3)

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JP2022512128A true JP2022512128A (ja) 2022-02-02
JP2022512128A5 JP2022512128A5 (https=) 2023-01-11
JPWO2020115501A5 JPWO2020115501A5 (https=) 2023-01-11

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JP2021532111A Pending JP2022512128A (ja) 2018-12-06 2019-12-06 医薬化合物およびユビキチン特異的プロテアーゼ１９（ｕｓｐ１９）阻害剤としてのその使用

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US (1) US20220033397A1 (https=)
EP (1) EP3890829A1 (https=)
JP (1) JP2022512128A (https=)
KR (1) KR20210102285A (https=)
CN (1) CN113365696A (https=)
AU (1) AU2019393162A1 (https=)
BR (1) BR112021010644A2 (https=)
CA (1) CA3121376A1 (https=)
IL (1) IL283706A (https=)
MX (1) MX2021006540A (https=)
SG (1) SG11202105913RA (https=)
WO (1) WO2020115501A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201801562D0 (en) * 2018-01-31 2018-03-14 Almac Diagnostics Ltd Pharmaceutical compounds
GB202104097D0 (en) 2021-03-24 2021-05-05 Almac Discovery Ltd Pharmaceutical compounds
GB202311227D0 (en) 2023-07-21 2023-09-06 Almac Discovery Ltd Pharmaceutical compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018020242A1 (en) * 2016-07-26 2018-02-01 Almac Discovery Limited Pharmaceutical compounds
JP2021525220A (ja) * 2018-01-31 2021-09-24 アルマック・ディスカバリー・リミテッドＡｌｍａｃ Ｄｉｓｃｏｖｅｒｙ Ｌｉｍｉｔｅｄ ４−ヒドロキシピペリジン誘導体およびユビキチン特異的プロテアーゼ１９（ｕｓｐ１９）の阻害剤としてのその使用

Family Cites Families (10)

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Publication number Priority date Publication date Assignee Title
AUPO111096A0 (en) * 1996-07-18 1996-08-08 Fujisawa Pharmaceutical Co., Ltd. New compound
ES2309206T3 (es) 2001-10-02 2008-12-16 Smithkline Beecham Corporation Compuestos quimicos.
EP2565186A1 (en) * 2011-09-02 2013-03-06 Hybrigenics S.A. Selective and reversible inhibitors of ubiquitin specific protease 7
MA41291A (fr) * 2014-12-30 2017-11-07 Forma Therapeutics Inc Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer
AR103297A1 (es) * 2014-12-30 2017-05-03 Forma Therapeutics Inc Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina
EP3253765A1 (en) * 2015-02-05 2017-12-13 Forma Therapeutics, Inc. Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
HK1248220A1 (zh) * 2015-02-05 2018-10-12 Forma Therapeutics, Inc. 喹唑啉酮和偶氮喹唑啉作为泛特丁胺蛋白酶7抑制剂
US9938300B2 (en) * 2015-02-05 2018-04-10 Forma Therapeutics, Inc. Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors
FR3052452B1 (fr) * 2016-06-10 2018-06-22 Les Laboratoires Servier Nouveaux derives de piperidinyle, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA3027008C (en) * 2016-06-10 2021-02-09 Les Laboratoires Servier (hetero)aryl-substituted-piperidinyl derivatives, a process for their preparation and pharmaceutical compositions containing them

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018020242A1 (en) * 2016-07-26 2018-02-01 Almac Discovery Limited Pharmaceutical compounds
JP2021525220A (ja) * 2018-01-31 2021-09-24 アルマック・ディスカバリー・リミテッドＡｌｍａｃ Ｄｉｓｃｏｖｅｒｙ Ｌｉｍｉｔｅｄ ４−ヒドロキシピペリジン誘導体およびユビキチン特異的プロテアーゼ１９（ｕｓｐ１９）の阻害剤としてのその使用

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ACS MED. CHEM. LETT., vol. 9, JPN6024001750, 2018, pages 238 - 243, ISSN: 0005243420 *
DIABETOLOGIA, vol. 62, JPN6024001749, 1 November 2018 (2018-11-01), pages 136 - 146, ISSN: 0005243419 *

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EP3890829A1 (en) 2021-10-13
CA3121376A1 (en) 2020-06-11
BR112021010644A2 (pt) 2021-09-28
AU2019393162A1 (en) 2021-06-17
IL283706A (en) 2021-07-29
MX2021006540A (es) 2021-07-07
KR20210102285A (ko) 2021-08-19
WO2020115501A1 (en) 2020-06-11
US20220033397A1 (en) 2022-02-03
CN113365696A (zh) 2021-09-07
SG11202105913RA (en) 2021-07-29

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