JP2024517861A - PKC-θモジュレーター - Google Patents

PKC-θモジュレーター Download PDF

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Publication number
JP2024517861A
JP2024517861A JP2023568277A JP2023568277A JP2024517861A JP 2024517861 A JP2024517861 A JP 2024517861A JP 2023568277 A JP2023568277 A JP 2023568277A JP 2023568277 A JP2023568277 A JP 2023568277A JP 2024517861 A JP2024517861 A JP 2024517861A
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group
hydrogen
mmol
compound
ring
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JP2024517861A5 (https=
Inventor
レイ,ピーター
ブラッドリー,アンソニー
リチャーズ,サイモン
サントス,カタリナ
ベスナード,ジェレミー
メネロル,ジェローム
スショー,ヴィルジニー
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Exscientia Ltd
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Exscientia Ltd
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Publication of JP2024517861A5 publication Critical patent/JP2024517861A5/ja
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
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    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Amplifiers (AREA)
  • Optical Communication System (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2023568277A 2021-05-06 2022-05-06 PKC-θモジュレーター Pending JP2024517861A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB202106485 2021-05-06
GB2106485.2 2021-05-06
PCT/GB2022/051166 WO2022234298A1 (en) 2021-05-06 2022-05-06 Pkc-theta modulators

Publications (2)

Publication Number Publication Date
JP2024517861A true JP2024517861A (ja) 2024-04-23
JP2024517861A5 JP2024517861A5 (https=) 2025-12-01

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JP2023568277A Pending JP2024517861A (ja) 2021-05-06 2022-05-06 PKC-θモジュレーター

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US (2) US20240262821A1 (https=)
EP (1) EP4333982A1 (https=)
JP (1) JP2024517861A (https=)
KR (1) KR20240024062A (https=)
CN (1) CN117355522A (https=)
AU (1) AU2022269883A1 (https=)
BR (1) BR112023022706A2 (https=)
CA (1) CA3213703A1 (https=)
CL (1) CL2023003246A1 (https=)
CO (1) CO2023014939A2 (https=)
IL (1) IL307665A (https=)
MX (1) MX2023013013A (https=)
PE (1) PE20240070A1 (https=)
WO (1) WO2022234298A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20250019A1 (es) * 2021-05-06 2025-01-07 Exscientia Ai Ltd MODULADORES DE PKC-theta
WO2025235367A1 (en) * 2024-05-06 2025-11-13 D. E. Shaw Research, Llc Azaindolinone compounds as kca3.1 potassium channel blockers
WO2025255292A1 (en) * 2024-06-06 2025-12-11 Bristol-Myers Squibb Company Pkc-theta inhibitors, compositions, and methods of use
WO2025255288A1 (en) * 2024-06-06 2025-12-11 Bristol-Myers Squibb Company Pkc-theta inhibitors, compositions, and methods of use
WO2025255298A1 (en) * 2024-06-06 2025-12-11 Bristol-Myers Squibb Company Pkc-theta inhibitors, compositions, and methods of use

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011502994A (ja) * 2007-11-02 2011-01-27 バーテックス ファーマシューティカルズ インコーポレイテッド タンパク質キナーゼC−θとしての[1H−ピラゾロ[3,4−B]ピリジン−4−イル]−フェニレンまたは−ピリジン−2−イル誘導体
JP2011510985A (ja) * 2008-02-04 2011-04-07 サイトキネティックス, インコーポレイテッド 特定の化学的実体、組成物および方法
JP2013525481A (ja) * 2010-05-05 2013-06-20 バーテックス ファーマシューティカルズ インコーポレイテッド PKC−θインヒビターとして有用な4置換ピラゾロピリミジン
JP2017502957A (ja) * 2013-12-26 2017-01-26 武田薬品工業株式会社 モノアシルグリセロールリパーゼ(magl)阻害剤としての4−(ピペラジン−1−イル)−ピロリジン−2−オン化合物
JP2019528275A (ja) * 2016-08-16 2019-10-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung 可逆性btk阻害剤としてのオキソ−イミダゾピリジン及びその使用
WO2020240586A1 (en) * 2019-05-28 2020-12-03 Mankind Pharma Ltd. Novel compounds for inhibition of janus kinase 1
CN112480116A (zh) * 2019-09-11 2021-03-12 南京正大天晴制药有限公司 Pkb抑制剂
WO2022234299A1 (en) * 2021-05-06 2022-11-10 Exscientia Ai Limited Pkc-theta modulators

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0920382D0 (en) 2009-11-20 2010-01-06 Univ Dundee Design of molecules
US9556126B2 (en) 2013-12-20 2017-01-31 Signal Pharmaceuticals, Llc Substituted diaminopyrimidyl compounds, compositions thereof, and methods of treatment therewith

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011502994A (ja) * 2007-11-02 2011-01-27 バーテックス ファーマシューティカルズ インコーポレイテッド タンパク質キナーゼC−θとしての[1H−ピラゾロ[3,4−B]ピリジン−4−イル]−フェニレンまたは−ピリジン−2−イル誘導体
JP2011510985A (ja) * 2008-02-04 2011-04-07 サイトキネティックス, インコーポレイテッド 特定の化学的実体、組成物および方法
JP2013525481A (ja) * 2010-05-05 2013-06-20 バーテックス ファーマシューティカルズ インコーポレイテッド PKC−θインヒビターとして有用な4置換ピラゾロピリミジン
JP2017502957A (ja) * 2013-12-26 2017-01-26 武田薬品工業株式会社 モノアシルグリセロールリパーゼ(magl)阻害剤としての4−(ピペラジン−1−イル)−ピロリジン−2−オン化合物
JP2019528275A (ja) * 2016-08-16 2019-10-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung 可逆性btk阻害剤としてのオキソ−イミダゾピリジン及びその使用
WO2020240586A1 (en) * 2019-05-28 2020-12-03 Mankind Pharma Ltd. Novel compounds for inhibition of janus kinase 1
CN112480116A (zh) * 2019-09-11 2021-03-12 南京正大天晴制药有限公司 Pkb抑制剂
WO2022234299A1 (en) * 2021-05-06 2022-11-10 Exscientia Ai Limited Pkc-theta modulators

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MX2023013013A (es) 2024-03-25
US20260035367A1 (en) 2026-02-05
PE20240070A1 (es) 2024-01-11
AU2022269883A1 (en) 2023-10-19
CO2023014939A2 (es) 2024-02-15
IL307665A (en) 2023-12-01
KR20240024062A (ko) 2024-02-23
CL2023003246A1 (es) 2024-04-26
BR112023022706A2 (pt) 2024-01-16
CN117355522A (zh) 2024-01-05
US20240262821A1 (en) 2024-08-08
EP4333982A1 (en) 2024-03-13
WO2022234298A1 (en) 2022-11-10
CA3213703A1 (en) 2022-11-10

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