CN116528857A - Malt-1调节剂 - Google Patents

Malt-1调节剂 Download PDF

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Publication number
CN116528857A
CN116528857A CN202180078754.7A CN202180078754A CN116528857A CN 116528857 A CN116528857 A CN 116528857A CN 202180078754 A CN202180078754 A CN 202180078754A CN 116528857 A CN116528857 A CN 116528857A
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China
Prior art keywords
hydrogen
alkyl
mmol
methyl
alkoxy
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Pending
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CN202180078754.7A
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English (en)
Chinese (zh)
Inventor
彼得·雷
大卫·埃文斯
安东尼·布拉德利
克里斯·拉杜
西蒙·理查兹
卡塔琳娜·桑托斯
杰里米·贝斯纳德
安德鲁·约翰·库克
西尔维·费利西泰·戈麦斯
洛雷纳·娜塔莉·萨宾·卡索·勒鲁
玛尔塔·平托
萨布丽娜·普驰
克莱尔·克里斯蒂安娜·吉内特·布兰格
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Aix Saianxia Artificial Intelligence Co ltd
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Aix Saianxia Artificial Intelligence Co ltd
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Publication of CN116528857A publication Critical patent/CN116528857A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • C07D471/02—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
    • 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)
CN202180078754.7A 2020-11-23 2021-11-23 Malt-1调节剂 Pending CN116528857A (zh)

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 (1)

Publication Number Publication Date
CN116528857A true CN116528857A (zh) 2023-08-01

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Family Applications (1)

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CN202180078754.7A Pending CN116528857A (zh) 2020-11-23 2021-11-23 Malt-1调节剂

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=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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

Families Citing this family (11)

* Cited by examiner, † Cited by third party
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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
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

Citations (7)

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WO2003004020A1 (de) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Heteroarylcarbonsäureamide, ihre herstellung und ihre verwendung als inhibitoren des mikrosmalen triglycerid-transferproteins (mtp)
WO2012143796A2 (en) * 2011-04-21 2012-10-26 Institut Pasteur Korea Anti-inflammation compounds
WO2013117645A1 (en) * 2012-02-10 2013-08-15 Galapagos Nv Imidazo [4, 5 -c] pyridine derivatives useful for the treatment of degenerative and inflammatory diseases
CN107614499A (zh) * 2015-05-29 2018-01-19 帝人制药株式会社 吡啶并［3，4‑d］嘧啶衍生物及其药学上可允许的盐
WO2018226150A1 (en) * 2017-06-05 2018-12-13 Medivir Aktiebolag Pyrazolopyrimidine as malt-1 inhibitors
CN110214136A (zh) * 2016-12-21 2019-09-06 詹森药业有限公司 作为malt1抑制剂的吡唑衍生物
CN116916924A (zh) * 2020-10-16 2023-10-20 稀有生物科学股份有限公司 Malt1调节剂及其用途

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ME01526B (me) * 2009-02-26 2014-04-20 Boehringer Ingelheim Int Jedinjenja kao b1 antagonisti bradikinina
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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
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
WO2018078042A1 (en) * 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising administration of imidazopyrazinones
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
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
WO2022081995A1 (en) * 2020-10-16 2022-04-21 Rheos Medicines, Inc. Malt1 modulators and uses thereof

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Publication number Priority date Publication date Assignee Title
WO2003004020A1 (de) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Heteroarylcarbonsäureamide, ihre herstellung und ihre verwendung als inhibitoren des mikrosmalen triglycerid-transferproteins (mtp)
WO2012143796A2 (en) * 2011-04-21 2012-10-26 Institut Pasteur Korea Anti-inflammation compounds
US20140155387A1 (en) * 2011-04-21 2014-06-05 Qurient, Co. Ltd. Anti-Inflammation Compounds
WO2013117645A1 (en) * 2012-02-10 2013-08-15 Galapagos Nv Imidazo [4, 5 -c] pyridine derivatives useful for the treatment of degenerative and inflammatory diseases
CN107614499A (zh) * 2015-05-29 2018-01-19 帝人制药株式会社 吡啶并［3，4‑d］嘧啶衍生物及其药学上可允许的盐
CN110214136A (zh) * 2016-12-21 2019-09-06 詹森药业有限公司 作为malt1抑制剂的吡唑衍生物
WO2018226150A1 (en) * 2017-06-05 2018-12-13 Medivir Aktiebolag Pyrazolopyrimidine as malt-1 inhibitors
CN116916924A (zh) * 2020-10-16 2023-10-20 稀有生物科学股份有限公司 Malt1调节剂及其用途

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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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US20260109698A1 (en) 2026-04-23
IL303036A (en) 2023-07-01
CA3196526A1 (en) 2022-05-27
GB202018412D0 (en) 2021-01-06
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
AU2021381009A1 (en) 2023-06-08
WO2022106857A1 (en) 2022-05-27
EP4247492A1 (en) 2023-09-27

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