JP6297582B2 - ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 - Google Patents

ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 Download PDF

Info

Publication number
JP6297582B2
JP6297582B2 JP2015542134A JP2015542134A JP6297582B2 JP 6297582 B2 JP6297582 B2 JP 6297582B2 JP 2015542134 A JP2015542134 A JP 2015542134A JP 2015542134 A JP2015542134 A JP 2015542134A JP 6297582 B2 JP6297582 B2 JP 6297582B2
Authority
JP
Japan
Prior art keywords
methyl
oxy
ethyl
purine
pyrrolidin
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.)
Expired - Fee Related
Application number
JP2015542134A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015537010A (ja
JP2015537010A5 (pt-PT
Inventor
アチヤブ，アブデルガニ・アベ
アルトマン，マイケル・デイー
デング，ヨンキ
グズイ，テイモシー
カツター，ソロモン
カツツ，ジエイソン・デイー
メソツト，ジヨーイ・エル
ジヨウ，フーア
マツゴーワン，メレデス
クリストフアー，マシユー・ピー
ガルシア，ユデイス
アンソニー，ネビル・ジヨン
フラデラ・リナス，フランシーズ・ハビエア
ムウ，チヤンウエイ
ジヤーン，スーシーン
ジヤーン，ローン
フオーン，キン・チユ
ルオン，シエンシユヨン
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 Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
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 Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of JP2015537010A publication Critical patent/JP2015537010A/ja
Publication of JP2015537010A5 publication Critical patent/JP2015537010A5/ja
Application granted granted Critical
Publication of JP6297582B2 publication Critical patent/JP6297582B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/36—Sulfur atom
    • C07D473/38—Sulfur atom attached in position 6
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015542134A 2012-11-16 2013-11-15 ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 Expired - Fee Related JP6297582B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261727416P 2012-11-16 2012-11-16
US61/727,416 2012-11-16
PCT/CN2013/001394 WO2014075392A1 (en) 2012-11-16 2013-11-15 Purine inhibitors of human phosphatidylinositol 3-kinase delta

Publications (3)

Publication Number Publication Date
JP2015537010A JP2015537010A (ja) 2015-12-24
JP2015537010A5 JP2015537010A5 (pt-PT) 2016-12-22
JP6297582B2 true JP6297582B2 (ja) 2018-03-20

Family

ID=50730541

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015542134A Expired - Fee Related JP6297582B2 (ja) 2012-11-16 2013-11-15 ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤

Country Status (11)

Country Link
US (1) US9730940B2 (pt-PT)
EP (1) EP2920171B1 (pt-PT)
JP (1) JP6297582B2 (pt-PT)
KR (1) KR20150082613A (pt-PT)
CN (1) CN104918939B (pt-PT)
AU (1) AU2013347538B2 (pt-PT)
BR (1) BR112015011148A8 (pt-PT)
CA (1) CA2891009A1 (pt-PT)
MX (1) MX2015006191A (pt-PT)
RU (1) RU2658006C2 (pt-PT)
WO (1) WO2014075392A1 (pt-PT)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
TW201444849A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途
TN2016000227A1 (fr) 2013-12-05 2017-10-06 Pfizer Pyrrolo[2,3-d]pyrimidinyle, pyrrolo[2,3-b]pyrazinyle et pyrollo[2,3-d]pyridinyle acrylamides.
EP3115362B1 (en) 2014-03-06 2019-06-12 Shanghai Haiyan Pharmaceutical Technology Co. Ltd. Piperidine derivatives as orexin receptor antagonist
CN104030998B (zh) * 2014-06-05 2015-11-18 华东师范大学 4-多氟烷基-4，5-二取代异噁唑衍生物及其制备方法
WO2016020784A1 (en) 2014-08-05 2016-02-11 Pfizer Inc. N-acylpyrrolidine ether tropomyosin-related kinase inhibitors
KR102455043B1 (ko) 2014-09-11 2022-10-13 얀센 파마슈티카 엔.브이. 치환된 2-아자바이사이클 및 오렉신 수용체 조절제로서의 이의 용도
EP3204379B1 (en) * 2014-10-10 2019-03-06 Genentech, Inc. Pyrrolidine amide compounds as histone demethylase inhibitors
US10189844B2 (en) 2016-02-04 2019-01-29 Chiesi Farmaceutici S.P.A. Pyrazole derivatives as phosphoinositide 3-kinases inhibitors
WO2017166104A1 (en) * 2016-03-30 2017-10-05 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
KR102493644B1 (ko) * 2016-09-14 2023-01-30 얀센 파마슈티카 엔.브이. 메닌-mll 상호작용의 스피로 바이사이클릭 억제제
US10494370B2 (en) 2017-08-16 2019-12-03 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a pyridine or pyrazine moiety, conjugates thereof, and methods and uses therefor
CN113620976B (zh) * 2020-05-09 2023-09-26 中国医学科学院药物研究所 噻唑并嘧啶类化合物及其制备方法、用途和药物组合物
JPWO2022209916A1 (pt-PT) * 2021-03-29 2022-10-06
CN113072480B (zh) * 2021-04-13 2022-09-30 常州佳德医药科技有限公司 一种手性(-)-5-氮杂螺[2.4]庚烷-7-醇、制备方法及应用
WO2024083237A1 (en) * 2022-10-20 2024-04-25 Impact Therapeutics (Shanghai) , Inc Substituted heteroaryl bicyclic compounds as usp1 inhibitors and the use thereof

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT95516A (pt) * 1989-10-06 1991-08-14 Wellcome Found Processo para a preparacao de derivados de 2',3'-didesoxi nucleosidos 6-substituidos
US5670501A (en) 1994-09-01 1997-09-23 Discovery Therapeutics, Inc. N-substituted 9-alkyladenines
DK1278748T3 (da) 2000-04-25 2011-04-18 Icos Corp Inhibitorer af human phosphatidyl-inositol 3-kinase delta
AU8294101A (en) * 2000-07-21 2002-02-05 Gilead Sciences Inc Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
SE0300456D0 (sv) * 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
JP2006527213A (ja) * 2003-06-12 2006-11-30 ノボ　ノルディスク　アクティーゼルスカブ ホルモン感受性リパーゼの阻害剤として使用するための、置換ピペリジンカルバメート
CA2565037A1 (en) 2004-04-28 2005-11-10 Cv Therapeutics, Inc. Purine derivatives as a1 adenosine receptor antagonists
US8008307B2 (en) * 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
MY157177A (en) * 2006-08-08 2016-05-13 Millennium Pharm Inc Heteroaryl compounds useful as inhibitors of e1 activating enzymes
AU2009269087A1 (en) 2008-07-07 2010-01-14 Xcovery Holding Company Llc PI3K isoform selective inhibitors
WO2011075643A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
EP2588473A1 (en) 2010-06-30 2013-05-08 Amgen Inc. Nitrogen containing heterocyclic compounds as pik3 -delta inhibitors
UA112517C2 (uk) * 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
WO2012037204A1 (en) 2010-09-14 2012-03-22 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
ES2612503T3 (es) * 2010-09-14 2017-05-17 Exelixis, Inc. Compuestos 9H-purina como inhibidores de PI3K-delta y métodos para su preparación
CN102838600A (zh) * 2011-06-24 2012-12-26 山东亨利医药科技有限责任公司 苯基喹唑啉类PI3Kδ抑制剂

Also Published As

Publication number Publication date
RU2015122895A (ru) 2017-01-10
BR112015011148A2 (pt) 2017-07-11
MX2015006191A (es) 2015-08-10
BR112015011148A8 (pt) 2019-10-01
AU2013347538B2 (en) 2017-04-27
CN104918939B (zh) 2018-08-28
EP2920171B1 (en) 2018-08-29
US20150353552A1 (en) 2015-12-10
RU2658006C2 (ru) 2018-06-19
EP2920171A1 (en) 2015-09-23
JP2015537010A (ja) 2015-12-24
US9730940B2 (en) 2017-08-15
WO2014075392A1 (en) 2014-05-22
CN104918939A (zh) 2015-09-16
KR20150082613A (ko) 2015-07-15
CA2891009A1 (en) 2014-05-22
AU2013347538A1 (en) 2015-05-07
EP2920171A4 (en) 2016-06-22

Similar Documents

Publication Publication Date Title
JP6297582B2 (ja) ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤
JP6322200B2 (ja) ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤
EP3154976B1 (en) Purine inhibitors of human phosphatidylinositol 3-kinase delta
KR20170068585A (ko) 야누스 키나제 억제제로서의 에틸 N-Boc 피페리디닐 피라졸로 피리돈
US20240109917A1 (en) Pyrazolothiazole carboxamides and their uses as pdgfr inhibitors
AU2014234908A1 (en) N-(2-cyano heterocyclyl)pyrazolo pyridones as Janus kinase inhibitors
EP3313397B1 (en) Purine inhibitors of human phosphatidylinositol 3-kinase delta
CN116802184A (zh) 吡唑并噻唑甲酰胺及其作为pdgfr抑制剂的用途
TW202225163A (zh) 芳香雜環類化合物、藥物組合物及其應用
KR20150130310A (ko) 야누스 키나제 억제제로서의 같은자리 치환된 시아노에틸피라졸로 피리돈

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161102

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20161102

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170831

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170905

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171010

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20171128

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180123

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: 20180206

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20180221

R150 Certificate of patent or registration of utility model

Ref document number: 6297582

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees