IL272988B - Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors - Google Patents

Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors

Info

Publication number
IL272988B
IL272988B IL272988A IL27298820A IL272988B IL 272988 B IL272988 B IL 272988B IL 272988 A IL272988 A IL 272988A IL 27298820 A IL27298820 A IL 27298820A IL 272988 B IL272988 B IL 272988B
Authority
IL
Israel
Prior art keywords
compound
6alkyl
optionally substituted
heterocyclyl
substituent
Prior art date
Application number
IL272988A
Other languages
English (en)
Hebrew (he)
Other versions
IL272988A (en
Original Assignee
Beigene 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 Beigene Ltd filed Critical Beigene Ltd
Publication of IL272988A publication Critical patent/IL272988A/en
Publication of IL272988B publication Critical patent/IL272988B/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/535—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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • 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

Landscapes

  • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
IL272988A 2017-09-08 2018-09-07 Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors IL272988B (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2017101058 2017-09-08
CN2017119373 2017-12-28
CN2018086555 2018-05-11
PCT/CN2018/104559 WO2019047915A1 (en) 2017-09-08 2018-09-07 IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS

Publications (2)

Publication Number Publication Date
IL272988A IL272988A (en) 2020-04-30
IL272988B true IL272988B (en) 2022-08-01

Family

ID=65633578

Family Applications (1)

Application Number Title Priority Date Filing Date
IL272988A IL272988B (en) 2017-09-08 2018-09-07 Imidazo-[1,5-a]pyrazine derivatives as pi3k-delta inhibitors

Country Status (21)

Country Link
US (3) US11220506B2 (https=)
EP (2) EP3679042B1 (https=)
JP (1) JP7128264B2 (https=)
KR (1) KR20200052297A (https=)
CN (2) CN111704615B (https=)
AU (2) AU2018328569B2 (https=)
BR (1) BR112020004500A2 (https=)
CA (1) CA3072842A1 (https=)
DK (1) DK3679042T3 (https=)
ES (1) ES2944658T3 (https=)
FI (1) FI3679042T3 (https=)
HU (1) HUE061898T2 (https=)
IL (1) IL272988B (https=)
MX (1) MX2020002630A (https=)
NZ (1) NZ761680A (https=)
PL (1) PL3679042T3 (https=)
PT (1) PT3679042T (https=)
SG (1) SG11202001286SA (https=)
TW (2) TWI817956B (https=)
WO (1) WO2019047915A1 (https=)
ZA (1) ZA202000875B (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202233190A (zh) 2016-12-07 2022-09-01 英屬開曼群島商百濟神州有限公司 作為ＰＩ３Ｋδ抑制劑的咪唑並［１，５－Ａ］吡衍生物
TWI817956B (zh) 2017-09-08 2023-10-11 英屬開曼群島商百濟神州有限公司 咪唑並[1,5-A]吡嗪衍生物作爲PI3Kδ 抑制劑
JP2023503230A (ja) * 2019-11-21 2023-01-27 ベイジーン リミテッド Ｐｉ３キナーゼデルタ阻害剤との組合せで抗ｏｘ４０抗体を用いる癌治療の方法
JP2024521763A (ja) * 2021-05-27 2024-06-04 ベイジーン スウィッツァーランド ゲーエムベーハー Ｐｉ３ｋデルタ阻害剤の塩、その結晶形態、調製方法、及び使用
KR20240060647A (ko) * 2021-09-14 2024-05-08 베이진 엘티디 Btk 저해제와 pi3 키나제 저해제의 조합물을 이용하는 암 치료 방법

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JP2005089352A (ja) * 2003-09-16 2005-04-07 Kissei Pharmaceut Co Ltd 新規なイミダゾ［１，５−ａ］ピラジン誘導体、それを含有する医薬組成物およびそれらの用途
KR100872204B1 (ko) * 2003-10-15 2008-12-09 오에스아이 파마슈티컬스, 인코포레이티드 이미다조피라진 티로신 키나제 억제제
US7659274B2 (en) * 2006-01-25 2010-02-09 Osi Pharmaceuticals, Inc. Unsaturated mTOR inhibitors
JP2012524063A (ja) * 2009-04-15 2012-10-11 アストラゼネカ・アクチエボラーグ アルツハイマー病などのグリコーゲンシンターゼキナーゼ３関連障害の治療に有用なイミダゾール置換ピリミジン
SG175195A1 (en) * 2009-04-16 2011-11-28 Ct Nac Investigaciones Oncologicas Cnio Imidazopyrazines for use as kinase inhibitors
CA2825028A1 (en) * 2011-02-09 2012-08-16 F. Hoffman-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
EP2802586B1 (en) * 2012-01-10 2016-05-25 Bayer Intellectual Property GmbH Substituted imidazopyrazines as akt kinase inhibitors
EP2914296B2 (en) * 2012-11-01 2021-09-29 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
TWI687220B (zh) * 2013-03-01 2020-03-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
SG11201509842SA (en) 2013-05-30 2015-12-30 Infinity Pharmaceuticals Inc Treatment of cancers using pi3 kinase isoform modulators
US20210317140A1 (en) * 2013-10-18 2021-10-14 Medivation Technologies, Inc. Heterocyclic Compounds and Methods of Use
MA40596B1 (fr) * 2014-08-11 2021-12-31 Acerta Pharma Bv Combinaisons thérapeutiques d'un inhibiteur de btk et d'un inhibiteur de bcl-2
AR102220A1 (es) * 2015-10-08 2017-02-15 Incyte Corp Imidazopiridinas e imidazopirazinas como inhibidores de lsd1
DK3472160T3 (da) * 2016-06-16 2021-05-10 Janssen Pharmaceutica Nv Bicykliske pyridin-, pyrazin- og pyrimidinderivater som pi3k-beta-inhibitorer
TW202233190A (zh) 2016-12-07 2022-09-01 英屬開曼群島商百濟神州有限公司 作為ＰＩ３Ｋδ抑制劑的咪唑並［１，５－Ａ］吡衍生物
TWI817956B (zh) 2017-09-08 2023-10-11 英屬開曼群島商百濟神州有限公司 咪唑並[1,5-A]吡嗪衍生物作爲PI3Kδ 抑制劑

Also Published As

Publication number Publication date
MX2020002630A (es) 2020-07-20
NZ761680A (en) 2023-03-31
EP3679042A4 (en) 2021-01-13
CN111704615A (zh) 2020-09-25
JP7128264B2 (ja) 2022-08-30
BR112020004500A2 (pt) 2020-12-01
ES2944658T3 (es) 2023-06-23
AU2018328569B2 (en) 2023-07-27
US20220081447A1 (en) 2022-03-17
HUE061898T2 (hu) 2023-08-28
ZA202000875B (en) 2021-07-28
IL272988A (en) 2020-04-30
TW202336010A (zh) 2023-09-16
EP3679042B1 (en) 2023-03-01
PL3679042T3 (pl) 2023-09-04
AU2018328569A1 (en) 2020-02-27
US11905294B2 (en) 2024-02-20
JP2020534259A (ja) 2020-11-26
FI3679042T3 (fi) 2023-05-15
CA3072842A1 (en) 2019-03-14
DK3679042T3 (da) 2023-05-01
WO2019047915A1 (en) 2019-03-14
KR20200052297A (ko) 2020-05-14
CN111704615B (zh) 2023-02-17
TWI817956B (zh) 2023-10-11
PT3679042T (pt) 2023-05-18
EP3679042A1 (en) 2020-07-15
TW201920116A (zh) 2019-06-01
US11220506B2 (en) 2022-01-11
AU2023254925A1 (en) 2023-11-16
CN111051312A (zh) 2020-04-21
EP4219502A1 (en) 2023-08-02
SG11202001286SA (en) 2020-03-30
US20240150361A1 (en) 2024-05-09
US20200207774A1 (en) 2020-07-02

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