AU2019317625B2 - Pyrrolopyrimidine ITK inhibitors - Google Patents

Pyrrolopyrimidine ITK inhibitors Download PDF

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Publication number
AU2019317625B2
AU2019317625B2 AU2019317625A AU2019317625A AU2019317625B2 AU 2019317625 B2 AU2019317625 B2 AU 2019317625B2 AU 2019317625 A AU2019317625 A AU 2019317625A AU 2019317625 A AU2019317625 A AU 2019317625A AU 2019317625 B2 AU2019317625 B2 AU 2019317625B2
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AU
Australia
Prior art keywords
pyrrolo
amino
pyrimidin
prop
methylpiperidin
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AU2019317625A
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AU2019317625A1 (en
Inventor
David Anderson
James Blinn
Richard HEIER
Susan Hockerman
Eric Jacobsen
Paramita MUKHERJEE
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Aclaris Therapeutics Inc
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Aclaris Therapeutics Inc
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    • 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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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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)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2019317625A 2018-08-10 2019-08-12 Pyrrolopyrimidine ITK inhibitors Active AU2019317625B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862717400P 2018-08-10 2018-08-10
US62/717,400 2018-08-10
PCT/US2019/046182 WO2020033955A1 (en) 2018-08-10 2019-08-12 Pyrrolopyrimidine itk inhibitors

Publications (2)

Publication Number Publication Date
AU2019317625A1 AU2019317625A1 (en) 2021-02-18
AU2019317625B2 true AU2019317625B2 (en) 2025-02-27

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AU2019317625A Active AU2019317625B2 (en) 2018-08-10 2019-08-12 Pyrrolopyrimidine ITK inhibitors

Country Status (13)

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US (4) US11021482B2 (https=)
EP (1) EP3833350A4 (https=)
JP (2) JP7591500B2 (https=)
KR (1) KR102849047B1 (https=)
CN (2) CN119080779A (https=)
AU (1) AU2019317625B2 (https=)
BR (1) BR112021002479A2 (https=)
CA (1) CA3109192A1 (https=)
IL (1) IL280593A (https=)
MX (1) MX2021001558A (https=)
PH (1) PH12021550187A1 (https=)
SG (1) SG11202100525SA (https=)
WO (1) WO2020033955A1 (https=)

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EP3710431A4 (en) 2017-11-03 2021-07-07 Aclaris Therapeutics, Inc. SUBSTITUTED PYRROLOPYRIMIDINE-BASED JAK INHIBITORS AND THEIR MANUFACTURING AND USE PROCEDURES
WO2020033955A1 (en) * 2018-08-10 2020-02-13 Aclaris Therapeutics, Inc. Pyrrolopyrimidine itk inhibitors
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
WO2020223728A1 (en) 2019-05-02 2020-11-05 Aclaris Therapeutics, Inc. Substituted pyrrolopyridines as jak inhibitors
CN114787363A (zh) 2019-10-01 2022-07-22 恩派瑞安神经科学公司 对真菌进行遗传工程化以调节色胺表达
TW202207918A (zh) * 2020-05-14 2022-03-01 美商施萬生物製藥研發Ｉｐ有限責任公司 腸道選擇性ｊａｋ３抑制劑的投與
KR102560138B1 (ko) * 2020-06-15 2023-07-27 경북대학교 산학협력단 신경교세포 표현형 기반의 siRNA 다중 스크리닝을 통해 선별된 신경교세포 인산화효소의 신경염증 조절 용도
CN114887080B (zh) * 2020-12-08 2023-10-31 深圳瑞吉生物科技有限公司 一种mRNA剂型的免疫抑制剂及其在制备肿瘤治疗药物中的应用
CN113350346B (zh) * 2021-06-01 2023-06-27 广西医科大学第一附属医院 长春新碱在预防或治疗心肌纤维化中的应用
KR20230019801A (ko) * 2021-08-02 2023-02-09 한국화학연구원 신규한 피롤로 피리미딘 유도체 화합물, 이의 제조방법, 및 이를 유효성분으로 포함하는 대사성 간질환의 예방 또는 치료용 약학적 조성물
CN113571191A (zh) * 2021-08-31 2021-10-29 复旦大学附属中山医院 免疫检查点抑制剂相关mace发生风险的预测方法
WO2023110843A1 (en) * 2021-12-15 2023-06-22 Almirall, S.A. Heterobicyclic derivatives as itk inhibitors
EP4457336A4 (en) 2021-12-31 2026-01-14 Empyrean Neuroscience Inc ORGANISMS GENETICALLY MODIFIED TO PRODUCE PSYCHOTROPIC ALKALOIDS
EP4615440A1 (en) * 2022-11-08 2025-09-17 Aclaris Therapeutics, Inc. Pyrrolopyrimidine compositions for treatment of itk mediated conditions
CN116115760A (zh) * 2022-12-15 2023-05-16 浙江大学 Eed抑制剂在制备治疗神经免疫性疾病药物中的应用
WO2025144781A1 (en) * 2023-12-28 2025-07-03 Aclaris Therapeutics, Inc. Crystalline polymorph of an itk inhibitor
WO2025144783A1 (en) * 2023-12-28 2025-07-03 Aclaris Therapeutics, Inc. Methods of synthesizing substituted pyrrolopyrimidine compounds
CN117982685B (zh) * 2024-01-26 2025-05-30 北京大学人民医院 用于骨肉瘤检测的光学分子成像探针及其制备方法和应用
WO2025181247A1 (en) * 2024-02-28 2025-09-04 Almirall, S.A. Heterobicyclic derivatives as itk inhibitors
WO2025235366A1 (en) * 2024-05-07 2025-11-13 Aclaris Therapeutics, Inc. Pyrrolopyrimidine compositions for treatment of atopic dermatitis

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MX2021001558A (es) 2021-04-28
PH12021550187A1 (en) 2022-02-14
IL280593A (en) 2021-03-25
KR20210044822A (ko) 2021-04-23
WO2020033955A1 (en) 2020-02-13
CN119080779A (zh) 2024-12-06
KR102849047B1 (ko) 2025-08-22
EP3833350A1 (en) 2021-06-16
CN112823005A (zh) 2021-05-18
US11021482B2 (en) 2021-06-01
JP7591500B2 (ja) 2024-11-28
JP2021534244A (ja) 2021-12-09
US20200048262A1 (en) 2020-02-13
US11820775B2 (en) 2023-11-21
AU2019317625A1 (en) 2021-02-18
US20260035373A1 (en) 2026-02-05
US12297203B2 (en) 2025-05-13
US20220348579A1 (en) 2022-11-03
BR112021002479A2 (pt) 2021-07-27
CN112823005B (zh) 2024-08-20
EP3833350A4 (en) 2022-05-18
JP2025037892A (ja) 2025-03-18
US20240132505A1 (en) 2024-04-25
CA3109192A1 (en) 2020-02-13
SG11202100525SA (en) 2021-02-25

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