AU2021381009A1 - Malt-1 modulators - Google Patents

Malt-1 modulators Download PDF

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Publication number
AU2021381009A1
AU2021381009A1 AU2021381009A AU2021381009A AU2021381009A1 AU 2021381009 A1 AU2021381009 A1 AU 2021381009A1 AU 2021381009 A AU2021381009 A AU 2021381009A AU 2021381009 A AU2021381009 A AU 2021381009A AU 2021381009 A1 AU2021381009 A1 AU 2021381009A1
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AU
Australia
Prior art keywords
alkyl
group
mmol
compound
hydrogen
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
AU2021381009A
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English (en)
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AU2021381009A9 (en
Inventor
Jeremy Besnard
Claire Christiane Ginette BLANGER
Anthony Bradley
Lorène Nathalie Sabine CAZAUX-LEROU
Andrew John Cooke
David Evans
Sylvie Félicité GOMEZ
Marta PINTO
Sabrina Pucci
Chris RADOUX
Peter Ray
Simon Richards
Catarina SANTOS
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.)
Recursion Pharmaceuticals Inc
Original Assignee
Exscientia Ltd
Exscientia AI 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, Exscientia AI Ltd filed Critical Exscientia Ltd
Publication of AU2021381009A1 publication Critical patent/AU2021381009A1/en
Publication of AU2021381009A9 publication Critical patent/AU2021381009A9/en
Assigned to RECURSION PHARMACEUTICALS, INC. reassignment RECURSION PHARMACEUTICALS, INC. Request for Assignment Assignors: EXSCIENTIA AI LIMITED
Pending legal-status Critical Current

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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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/505—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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07D471/22—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 systems contains four 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Electrochromic Elements, Electrophoresis, Or Variable Reflection Or Absorption Elements (AREA)
  • Holo Graphy (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2021381009A 2020-11-23 2021-11-23 Malt-1 modulators Pending AU2021381009A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB2018412.3 2020-11-23
GBGB2018412.3A GB202018412D0 (en) 2020-11-23 2020-11-23 Malt-1 modulators ii
PCT/GB2021/053031 WO2022106857A1 (en) 2020-11-23 2021-11-23 Malt-1 modulators

Publications (2)

Publication Number Publication Date
AU2021381009A1 true AU2021381009A1 (en) 2023-06-08
AU2021381009A9 AU2021381009A9 (en) 2024-07-25

Family

ID=74046962

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021381009A Pending AU2021381009A1 (en) 2020-11-23 2021-11-23 Malt-1 modulators

Country Status (12)

Country Link
US (2) US20250051327A1 (https=)
EP (1) EP4247492A1 (https=)
JP (1) JP2023550122A (https=)
KR (1) KR20230112678A (https=)
CN (1) CN116528857A (https=)
AU (1) AU2021381009A1 (https=)
CA (1) CA3196526A1 (https=)
CO (1) CO2023007626A2 (https=)
GB (1) GB202018412D0 (https=)
IL (1) IL303036A (https=)
MX (1) MX2023005928A (https=)
WO (1) WO2022106857A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202345806A (zh) 2022-03-31 2023-12-01 美商艾伯維有限公司 噻唑并〔５，４－ｂ〕吡啶ｍａｌｔ－１抑制劑
EP4638458A1 (en) * 2022-12-23 2025-10-29 Janssen Pharmaceutica NV Malt1 inhibitors
CN121419973A (zh) * 2023-06-30 2026-01-27 詹森药业有限公司 Malt1抑制剂
WO2025059027A1 (en) * 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors
WO2025223516A1 (zh) * 2024-04-24 2025-10-30 首药控股(北京)股份有限公司 一种抑制剂杂环化合物
WO2025223551A1 (en) * 2024-04-26 2025-10-30 Janssen Pharmaceutica Nv Formulations, crystalline forms and dosage regimens of a malt1 inhibitor
WO2025224298A1 (en) * 2024-04-26 2025-10-30 Janssen Pharmaceutica Nv Inhibitors of malt1 and methods of their use
WO2026003045A1 (en) 2024-06-26 2026-01-02 Janssen Pharmaceutica Nv Synthesis of a malt1 inhibitor
WO2026003049A1 (en) * 2024-06-26 2026-01-02 Janssen Pharmaceutica Nv Malt1 inhibitors
WO2026003043A1 (en) * 2024-06-26 2026-01-02 Janssen Pharmaceutica Nv Malt1 inhibitors
WO2026003039A1 (en) * 2024-06-26 2026-01-02 Janssen Pharmaceutica Nv Malt1 inhibitors
WO2026003051A1 (en) * 2024-06-26 2026-01-02 Janssen Pharmaceutica Nv Crystalline forms
WO2026017148A1 (zh) * 2024-07-19 2026-01-22 上海拓界生物医药科技有限公司 一种malt1抑制剂及其制备方法和用途

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GB0012240D0 (en) 2000-05-19 2000-07-12 Merck Sharp & Dohme Therapeutic agents
DE10132686A1 (de) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Heteroarylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel
JP2006522127A (ja) * 2003-04-01 2006-09-28 スミスクライン ビーチャム コーポレーション イミダゾトリアジン化合物
ME01526B (me) * 2009-02-26 2014-04-20 Boehringer Ingelheim Int Jedinjenja kao b1 antagonisti bradikinina
GB0920382D0 (en) 2009-11-20 2010-01-06 Univ Dundee Design of molecules
KR102104125B1 (ko) * 2011-04-21 2020-05-29 재단법인 한국파스퇴르연구소 소염 화합물
UY34615A (es) * 2012-02-10 2013-09-30 Galapagos Nv Nuevos compuestos útiles para el tratamiento de enfermedades degenerativas e inflamatorias.
US9493481B2 (en) * 2012-02-23 2016-11-15 Vanderbilt University Substituted 5-aminothieno[2,3—C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
JPWO2015098991A1 (ja) * 2013-12-26 2017-03-23 東レ株式会社 Ｎ−アルキルアミド誘導体及びその医薬用途
SG11201607895PA (en) 2014-05-28 2016-12-29 Novartis Ag Novel pyrazolo pyrimidine derivatives and their use as malt1 inhibitors
SG11201709837RA (en) * 2015-05-29 2017-12-28 Teijin Pharma Ltd PYRIDO[3,4-d]PYRIMIDINE DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
US9708333B2 (en) * 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
AU2016352813B2 (en) 2015-11-13 2019-09-19 Novartis Ag Novel pyrazolo pyrimidine derivatives
JP6902040B2 (ja) * 2016-01-28 2021-07-14 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 免疫チェックポイント阻害剤の効力を増強する方法
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JP2018135274A (ja) * 2017-02-20 2018-08-30 Ａｇｃ株式会社 多環芳香族炭化水素を光触媒とするフルオロメチル基含有化合物の製造方法
JP6891047B2 (ja) * 2017-05-31 2021-06-18 国立大学法人 名古屋工業大学 光学活性トリフルオロメチル基含有アミノ酸誘導体の製造方法
WO2018226150A1 (en) * 2017-06-05 2018-12-13 Medivir Aktiebolag Pyrazolopyrimidine as malt-1 inhibitors
TWI848400B (zh) 2018-11-28 2024-07-11 日商武田藥品工業股份有限公司 雜環化合物及醫藥
JP7818011B2 (ja) * 2020-10-16 2026-02-19 レラファイド バイオサイエンシーズ， インコーポレイテッド Ｍａｌｔ１モジュレーターおよびその使用
WO2022081995A1 (en) * 2020-10-16 2022-04-21 Rheos Medicines, Inc. Malt1 modulators and uses thereof

Also Published As

Publication number Publication date
KR20230112678A (ko) 2023-07-27
US20260109698A1 (en) 2026-04-23
IL303036A (en) 2023-07-01
CA3196526A1 (en) 2022-05-27
GB202018412D0 (en) 2021-01-06
CN116528857A (zh) 2023-08-01
US20250051327A1 (en) 2025-02-13
CO2023007626A2 (es) 2023-08-18
JP2023550122A (ja) 2023-11-30
MX2023005928A (es) 2023-09-07
AU2021381009A9 (en) 2024-07-25
WO2022106857A1 (en) 2022-05-27
EP4247492A1 (en) 2023-09-27

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Owner name: RECURSION PHARMACEUTICALS, INC.

Free format text: FORMER APPLICANT(S): EXSCIENTIA AI LIMITED