TWI762534B - 作為ＰＩ３Ｋδ抑制劑的咪唑並[1,5-A]吡衍生物 - Google Patents

作為ＰＩ３Ｋδ抑制劑的咪唑並[1,5-A]吡衍生物 Download PDF

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Publication number
TWI762534B
TWI762534B TW106143023A TW106143023A TWI762534B TW I762534 B TWI762534 B TW I762534B TW 106143023 A TW106143023 A TW 106143023A TW 106143023 A TW106143023 A TW 106143023A TW I762534 B TWI762534 B TW I762534B
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TW
Taiwan
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compound
alkyl
heteroaryl
chloro
cycloalkyl
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TW106143023A
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English (en)
Chinese (zh)
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TW201833113A (zh
Inventor
李菁
趙海波
志偉 王
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英屬開曼群島商百濟神州有限公司
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    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW106143023A 2016-12-07 2017-12-07 作為ＰＩ３Ｋδ抑制劑的咪唑並[1,5-A]吡衍生物 TWI762534B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2016108897 2016-12-07
WOPCT/CN2016/108897 2016-12-07

Publications (2)

Publication Number Publication Date
TW201833113A TW201833113A (zh) 2018-09-16
TWI762534B true TWI762534B (zh) 2022-05-01

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ID=62491736

Family Applications (2)

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TW106143023A TWI762534B (zh) 2016-12-07 2017-12-07 作為ＰＩ３Ｋδ抑制劑的咪唑並[1,5-A]吡衍生物
TW111114434A TW202233190A (zh) 2016-12-07 2017-12-07 作為ＰＩ３Ｋδ抑制劑的咪唑並［１，５－Ａ］吡衍生物

Family Applications After (1)

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TW111114434A TW202233190A (zh) 2016-12-07 2017-12-07 作為ＰＩ３Ｋδ抑制劑的咪唑並［１，５－Ａ］吡衍生物

Country Status (16)

Country Link
US (2) US11136323B2 (enExample)
EP (1) EP3551630A4 (enExample)
JP (2) JP7064495B2 (enExample)
KR (1) KR20190091339A (enExample)
CN (2) CN114805366A (enExample)
AU (2) AU2017372377B2 (enExample)
BR (1) BR112019011847A2 (enExample)
CA (1) CA3045959A1 (enExample)
EA (1) EA201991355A1 (enExample)
IL (2) IL266986B (enExample)
MX (1) MX394882B (enExample)
NZ (1) NZ754944A (enExample)
SG (1) SG10201912192RA (enExample)
TW (2) TWI762534B (enExample)
WO (1) WO2018103688A1 (enExample)
ZA (1) ZA201903286B (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3551630A4 (en) 2016-12-07 2020-07-15 Beigene, Ltd. IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS
IL272988B (en) 2017-09-08 2022-08-01 Beigene Ltd Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors
US20230011916A1 (en) * 2019-11-21 2023-01-12 Beigene, Ltd. Methods of cancer treatment using anti-ox40 antibodies in combination with pi3 kinase delta inhibitors
KR102344185B1 (ko) * 2020-02-26 2021-12-27 계명대학교 산학협력단 신규한 Pim 키나아제 억제제 및 이의 용도
IL308856A (en) * 2021-05-27 2024-01-01 Beigene Switzerland Gmbh SALTS OF A PI3Kdelta INHIBITOR, CRYSTALLINE FORMS, METHODS OF PREPARATION, AND USES THEREFORE
JP2024535799A (ja) * 2021-09-14 2024-10-02 ベイジーン スウィッツァーランド ゲーエムベーハー Ｂｔｋ阻害剤及びｐｉ３キナーゼ阻害剤の組み合わせを使用したがん治療の方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005037836A2 (en) * 2003-10-15 2005-04-28 Osi Pharmaceuticals, Inc. Imidazo ‘1, 5 - a ! pyrazine tyrosine kinase inhibitors
WO2015058084A1 (en) * 2013-10-18 2015-04-23 Medivation Technologies, Inc. Heterocyclic compounds and methods of use

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ596185A (en) 2009-04-16 2013-01-25 Ct Nac Investigaciones Oncologicas Cnio Imidazopyrazines for use as kinase inhibitors
RU2013138835A (ru) 2011-02-09 2015-03-20 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения в качестве ингибиторов pi3 киназы
WO2013104610A1 (en) * 2012-01-10 2013-07-18 Bayer Intellectual Property Gmbh Substituted imidazopyrazines as akt kinase inhibitors
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
ES2834638T3 (es) * 2013-05-30 2021-06-18 Infinity Pharmaceuticals Inc Tratamiento de cánceres usando moduladores de isoforma de PI3 cinasa
RS62713B1 (sr) 2014-08-11 2022-01-31 Acerta Pharma Bv Terapeutske kombinacije btk inhibitora i bcl-2 inhibitora
EP3551630A4 (en) * 2016-12-07 2020-07-15 Beigene, Ltd. IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS
IL272988B (en) 2017-09-08 2022-08-01 Beigene Ltd Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005037836A2 (en) * 2003-10-15 2005-04-28 Osi Pharmaceuticals, Inc. Imidazo ‘1, 5 - a ! pyrazine tyrosine kinase inhibitors
WO2015058084A1 (en) * 2013-10-18 2015-04-23 Medivation Technologies, Inc. Heterocyclic compounds and methods of use

Also Published As

Publication number Publication date
TW202233190A (zh) 2022-09-01
EP3551630A1 (en) 2019-10-16
US20190367523A1 (en) 2019-12-05
US11136323B2 (en) 2021-10-05
JP7064495B2 (ja) 2022-05-10
AU2017372377B2 (en) 2022-03-03
IL266986B (en) 2022-03-01
IL290419A (en) 2022-04-01
US11725012B2 (en) 2023-08-15
AU2017372377A1 (en) 2019-07-18
TW201833113A (zh) 2018-09-16
JP2022090051A (ja) 2022-06-16
EP3551630A4 (en) 2020-07-15
MX2019006612A (es) 2019-08-01
IL290419B2 (en) 2023-02-01
CA3045959A1 (en) 2018-06-14
CN114805366A (zh) 2022-07-29
NZ754944A (en) 2023-02-24
MX394882B (es) 2025-03-24
WO2018103688A1 (en) 2018-06-14
AU2022203737A1 (en) 2022-06-23
CN110267959A (zh) 2019-09-20
CN110267959B (zh) 2022-05-27
ZA201903286B (en) 2021-01-27
SG10201912192RA (en) 2020-02-27
KR20190091339A (ko) 2019-08-05
IL266986A (en) 2019-07-31
US20220098202A1 (en) 2022-03-31
JP2020500909A (ja) 2020-01-16
IL290419B (en) 2022-10-01
EA201991355A1 (ru) 2019-11-29
BR112019011847A2 (pt) 2019-10-29

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