JP2024518447A - ＰＫＣ－θモジュレーター - Google Patents

ＰＫＣ－θモジュレーター Download PDF

Info

Publication number
JP2024518447A
JP2024518447A JP2023568613A JP2023568613A JP2024518447A JP 2024518447 A JP2024518447 A JP 2024518447A JP 2023568613 A JP2023568613 A JP 2023568613A JP 2023568613 A JP2023568613 A JP 2023568613A JP 2024518447 A JP2024518447 A JP 2024518447A
Authority
JP
Japan
Prior art keywords
group
hydrogen
alkyl
mmol
halogen
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2023568613A
Other languages
English (en)
Japanese (ja)
Other versions
JP2024518447A5 (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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Exscientia Ltd
Original Assignee
Exscientia Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Exscientia Ltd filed Critical Exscientia Ltd
Publication of JP2024518447A publication Critical patent/JP2024518447A/ja
Publication of JP2024518447A5 publication Critical patent/JP2024518447A5/ja
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Amplifiers (AREA)
  • Optical Communication System (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2023568613A 2021-05-06 2022-05-06 ＰＫＣ－θモジュレーター Pending JP2024518447A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB2106486.0 2021-05-06
GB202106486 2021-05-06
PCT/GB2022/051167 WO2022234299A1 (en) 2021-05-06 2022-05-06 Pkc-theta modulators

Publications (2)

Publication Number Publication Date
JP2024518447A true JP2024518447A (ja) 2024-05-01
JP2024518447A5 JP2024518447A5 (https=) 2025-11-18

Family

ID=82100804

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2023568613A Pending JP2024518447A (ja) 2021-05-06 2022-05-06 ＰＫＣ－θモジュレーター

Country Status (14)

Country Link
US (1) US20240239794A1 (https=)
EP (1) EP4334316A1 (https=)
JP (1) JP2024518447A (https=)
KR (1) KR20240024063A (https=)
CN (1) CN117295738A (https=)
AU (1) AU2022269348A1 (https=)
BR (1) BR112023022883A2 (https=)
CA (1) CA3214088A1 (https=)
CL (1) CL2023003247A1 (https=)
CO (1) CO2023015005A2 (https=)
IL (1) IL307669A (https=)
MX (1) MX2023013012A (https=)
PE (1) PE20250019A1 (https=)
WO (1) WO2022234299A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022234298A1 (en) * 2021-05-06 2022-11-10 Exscientia Ai Limited Pkc-theta modulators
CN118772140B (zh) * 2023-04-07 2026-04-17 四川大学 一类化合物及其在治疗hDHODH介导的疾病中的用途
WO2025255294A1 (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 (4)

* 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
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
WO2020240586A1 (en) * 2019-05-28 2020-12-03 Mankind Pharma Ltd. Novel compounds for inhibition of janus kinase 1
WO2022234298A1 (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 (4)

* 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
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
WO2020240586A1 (en) * 2019-05-28 2020-12-03 Mankind Pharma Ltd. Novel compounds for inhibition of janus kinase 1
WO2022234298A1 (en) * 2021-05-06 2022-11-10 Exscientia Ai Limited Pkc-theta modulators

Also Published As

Publication number Publication date
IL307669A (en) 2023-12-01
KR20240024063A (ko) 2024-02-23
CA3214088A1 (en) 2022-11-10
WO2022234299A1 (en) 2022-11-10
AU2022269348A1 (en) 2023-10-26
CN117295738A (zh) 2023-12-26
MX2023013012A (es) 2024-03-25
CL2023003247A1 (es) 2024-04-26
BR112023022883A2 (pt) 2024-01-23
US20240239794A1 (en) 2024-07-18
CO2023015005A2 (es) 2024-02-05
EP4334316A1 (en) 2024-03-13
PE20250019A1 (es) 2025-01-07

Similar Documents

Publication Publication Date Title
JP7644517B2 (ja) Ｋｒａｓ突然変異型タンパク質阻害剤
CA3090482C (en) Tetrahydroquinazoline derivatives useful as anticancer agents
TWI637945B (zh) 可作為抗癌劑之經取代碳環核苷衍生物
JP2024518447A (ja) ＰＫＣ－θモジュレーター
TW202012415A (zh) 化學化合物
JP2020200338A (ja) Ｐｉｍキナーゼ阻害剤として有用なチアゾールカルボキサミドおよびピリジンカルボキサミド化合物
TW202142542A (zh) 藉由軛合ｂｔｋ抑制劑與ｅ３連接酶配位基降解布魯頓氏酪胺酸激酶（ｂｔｋ）及其使用方法
TW201938561A (zh) 化學化合物
WO2022106857A1 (en) Malt-1 modulators
WO2013051639A1 (ja) ピラゾロキノリン誘導体
CN116981675A (zh) 通过布鲁顿氏酪氨酸激酶（btk）抑制剂与e3连接酶配体的缀合降解btk和使用方法
JP2024517861A (ja) ＰＫＣ－θモジュレーター
CN115335376A (zh) 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶（btk）及其使用方法
US20240034731A1 (en) Aza-quinazoline compounds and methods of use
TW202438054A (zh) 作為ＭＴＡ－協同ＰＲＭＴ５抑制劑的５－胺基－６，８－二氫－１Ｈ－呋喃并［３，４－ｄ］吡咯并［３，２－ｂ］吡啶－２－甲醯胺衍生物
WO2016001077A1 (en) Compounds inhibiting the enzyme monopolar spindle 1 kinase,pharmaceutical compositions and uses thereof
WO2023177563A2 (en) Fused pyrazole amide analogs as glucosylceramide synthase inhibitors
CN121057733A (zh) 吡啶并咪唑酮化合物、其制备及其治疗用途
CN119403801A (zh) Lrrk2抑制剂
WO2026035945A9 (en) Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
EP4441034A1 (en) Fused pyrazole urea analogs as glucosylceramide synthase inhibitors

Legal Events

Date Code Title Description
A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20240717

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20250502

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20251027

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20260122

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20260127

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260413