JP7266592B2 - ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用 - Google Patents

ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用 Download PDF

Info

Publication number
JP7266592B2
JP7266592B2 JP2020521968A JP2020521968A JP7266592B2 JP 7266592 B2 JP7266592 B2 JP 7266592B2 JP 2020521968 A JP2020521968 A JP 2020521968A JP 2020521968 A JP2020521968 A JP 2020521968A JP 7266592 B2 JP7266592 B2 JP 7266592B2
Authority
JP
Japan
Prior art keywords
amino
methoxy
pyrimidin
yloxy
pyridin
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.)
Active
Application number
JP2020521968A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020537671A (ja
JP2020537671A5 (enExample
Inventor
アール. カラ,シュリニヴァーサ
シャオ,ユーファン
エー. シェーラー,ブライアン
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of JP2020537671A publication Critical patent/JP2020537671A/ja
Publication of JP2020537671A5 publication Critical patent/JP2020537671A5/ja
Application granted granted Critical
Publication of JP7266592B2 publication Critical patent/JP7266592B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020521968A 2017-10-17 2018-10-17 ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用 Active JP7266592B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762573251P 2017-10-17 2017-10-17
US62/573,251 2017-10-17
PCT/US2018/056190 WO2019079373A1 (en) 2017-10-17 2018-10-17 PYRIMIDINE TBK / IKKε INHIBITORY COMPOUNDS AND USES THEREOF

Publications (3)

Publication Number Publication Date
JP2020537671A JP2020537671A (ja) 2020-12-24
JP2020537671A5 JP2020537671A5 (enExample) 2021-11-25
JP7266592B2 true JP7266592B2 (ja) 2023-04-28

Family

ID=64110185

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020521968A Active JP7266592B2 (ja) 2017-10-17 2018-10-17 ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用

Country Status (14)

Country Link
US (1) US20230019491A1 (enExample)
EP (1) EP3697772A1 (enExample)
JP (1) JP7266592B2 (enExample)
KR (1) KR20200072519A (enExample)
CN (1) CN111247135A (enExample)
AU (1) AU2018352699A1 (enExample)
BR (1) BR112020007466A2 (enExample)
CA (1) CA3078579A1 (enExample)
IL (1) IL273891A (enExample)
MX (1) MX2020003507A (enExample)
RU (1) RU2020115596A (enExample)
SG (1) SG11202003407VA (enExample)
TW (1) TWI802604B (enExample)
WO (1) WO2019079373A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11440899B2 (en) * 2017-10-17 2022-09-13 Merck Patent Gmbh Pyrimidine TBK/IKKe inhibitor compounds and uses thereof
KR102695210B1 (ko) 2018-06-05 2024-08-13 크리네틱스 파마슈티칼스, 인크. 멜라노코르틴 아형-2 수용체(mc2r) 길항제 및 이의 용도
CN112552280A (zh) * 2019-09-25 2021-03-26 常州强力先端电子材料有限公司 一种高产酸的磺酰亚胺类光产酸剂
WO2021091788A1 (en) * 2019-11-07 2021-05-14 Crinetics Pharmaceuticals, Inc. Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
JP7672406B2 (ja) 2019-12-18 2025-05-07 クリネティックス ファーマシューティカルズ,インク. Gem-二置換ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
JP7651574B2 (ja) 2019-12-23 2025-03-26 クリネティックス ファーマシューティカルズ,インク. スピロ環式ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
BR112023018816A2 (pt) 2021-03-19 2023-10-31 Crinetics Pharmaceuticals Inc Antagonista do receptor de melanocortina subtipo-2 (mc2r) para o tratamento de doença
CN117447407B (zh) * 2023-12-19 2024-06-11 潍坊医学院 一种JAK2抑制剂Pacritinib及其中间体的制备方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010514822A (ja) 2007-01-05 2010-05-06 サノフイ−アベンテイス 新規なフェニル(4−フェニルピリミジン−2−イル)アミン誘導体、薬物としてのこれらの調製、医薬組成物および基本的にikk阻害剤としてのこれらの使用
JP2010538076A (ja) 2007-09-04 2010-12-09 ザ スクリプス リサーチ インスティチュート タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン
JP2013507449A (ja) 2009-10-12 2013-03-04 ミレクシス, インコーポレイテッド TBK1および/またはIKKεの阻害剤としてのアミノ−ピリミジン化合物
JP2013531055A (ja) 2010-07-19 2013-08-01 ドメイネクス リミテッド プロテインキナーゼIKKε及び/又はTBK−1の阻害剤としてのピリミジン化合物、それらの製造方法及びそれらを含む医薬組成物
JP2014510794A (ja) 2011-04-12 2014-05-01 アルツハイマーズ・インスティテュート・オブ・アメリカ・インコーポレイテッド IKK関連キナーゼεおよびTANK結合キナーゼ1の阻害剤の組成物および治療的使用
JP2014526447A (ja) 2011-09-09 2014-10-06 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング キナーゼインヒビターとしてのベンゾニトリル誘導体
WO2017003995A1 (en) 2015-06-29 2017-01-05 Merck Patent Gmbh TBK/IKKε INHIBITOR COMPOUNDS AND USES THEREOF

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010514822A (ja) 2007-01-05 2010-05-06 サノフイ−アベンテイス 新規なフェニル(4−フェニルピリミジン−2−イル)アミン誘導体、薬物としてのこれらの調製、医薬組成物および基本的にikk阻害剤としてのこれらの使用
JP2010538076A (ja) 2007-09-04 2010-12-09 ザ スクリプス リサーチ インスティチュート タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン
JP2013507449A (ja) 2009-10-12 2013-03-04 ミレクシス, インコーポレイテッド TBK1および/またはIKKεの阻害剤としてのアミノ−ピリミジン化合物
JP2013531055A (ja) 2010-07-19 2013-08-01 ドメイネクス リミテッド プロテインキナーゼIKKε及び/又はTBK−1の阻害剤としてのピリミジン化合物、それらの製造方法及びそれらを含む医薬組成物
JP2014510794A (ja) 2011-04-12 2014-05-01 アルツハイマーズ・インスティテュート・オブ・アメリカ・インコーポレイテッド IKK関連キナーゼεおよびTANK結合キナーゼ1の阻害剤の組成物および治療的使用
JP2014526447A (ja) 2011-09-09 2014-10-06 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング キナーゼインヒビターとしてのベンゾニトリル誘導体
WO2017003995A1 (en) 2015-06-29 2017-01-05 Merck Patent Gmbh TBK/IKKε INHIBITOR COMPOUNDS AND USES THEREOF

Also Published As

Publication number Publication date
MX2020003507A (es) 2020-07-22
EP3697772A1 (en) 2020-08-26
RU2020115596A3 (enExample) 2021-11-18
SG11202003407VA (en) 2020-05-28
RU2020115596A (ru) 2021-11-18
IL273891A (en) 2020-05-31
JP2020537671A (ja) 2020-12-24
AU2018352699A1 (en) 2020-05-28
TWI802604B (zh) 2023-05-21
CN111247135A (zh) 2020-06-05
US20230019491A1 (en) 2023-01-19
TW201922735A (zh) 2019-06-16
KR20200072519A (ko) 2020-06-22
CA3078579A1 (en) 2019-04-25
WO2019079373A1 (en) 2019-04-25
BR112020007466A2 (pt) 2020-09-24

Similar Documents

Publication Publication Date Title
TWI802604B (zh) 嘧啶TBK/IKKε抑制劑化合物及其用途
AU2015349899B2 (en) Heteroaryl compounds as IRAK inhibitors and uses thereof
US10428080B2 (en) TBK/IKK inhibitor compounds and uses thereof
JP7651590B2 (ja) アミノピリミジン誘導体およびアリール炭化水素受容体モジュレーターとしてのその使用
JP7284161B2 (ja) ピリミジンTBK/IKKεインヒビター化合物およびそれらの使用
HK40086197A (en) Aminopyrimidine derivatives and their use as aryl hydrocarbon receptor modulators
HK1242303A1 (en) Heteroaryl compounds as irak inhibitors and uses thereof
HK1242303B (en) Heteroaryl compounds as irak inhibitors and uses thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211015

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20211015

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220922

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20221020

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20230119

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230316

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20230404

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20230418

R150 Certificate of patent or registration of utility model

Ref document number: 7266592

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150