JP6322200B2 - 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

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Publication number
JP6322200B2
JP6322200B2 JP2015542135A JP2015542135A JP6322200B2 JP 6322200 B2 JP6322200 B2 JP 6322200B2 JP 2015542135 A JP2015542135 A JP 2015542135A JP 2015542135 A JP2015542135 A JP 2015542135A JP 6322200 B2 JP6322200 B2 JP 6322200B2
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JP
Japan
Prior art keywords
ethyl
purin
pyrrolidin
amino
methylpyrimidin
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Japanese (ja)
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JP2016502522A (ja
JP2016502522A5 (enExample
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
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
ヤン，リーピン
ムウ，チヤンウエイ
ワン，シヤオナ
シー，フオン
イエ，バイジユイン
ジヤーン，スーシーン
ジヤオ，シヤオリ
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
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Publication of JP2016502522A publication Critical patent/JP2016502522A/ja
Publication of JP2016502522A5 publication Critical patent/JP2016502522A5/ja
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    • 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
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • A61K31/505—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
    • 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
    • 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
    • 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)
  • 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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015542135A 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 Active JP6322200B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261727392P 2012-11-16 2012-11-16
US61/727,392 2012-11-16
PCT/CN2013/001395 WO2014075393A1 (en) 2012-11-16 2013-11-15 Purine inhibitors of human phosphatidylinositol 3-kinase delta

Publications (3)

Publication Number Publication Date
JP2016502522A JP2016502522A (ja) 2016-01-28
JP2016502522A5 JP2016502522A5 (enExample) 2016-12-22
JP6322200B2 true JP6322200B2 (ja) 2018-05-09

Family

ID=50730542

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015542135A Active JP6322200B2 (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) US9938281B2 (enExample)
EP (1) EP2920172B1 (enExample)
JP (1) JP6322200B2 (enExample)
KR (1) KR20150084992A (enExample)
CN (1) CN104918940B (enExample)
AU (1) AU2013347539B2 (enExample)
BR (1) BR112015011147A8 (enExample)
CA (1) CA2891013A1 (enExample)
MX (1) MX2015006192A (enExample)
RU (1) RU2661896C2 (enExample)
WO (1) WO2014075393A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
MX358640B (es) 2008-01-04 2018-08-29 Intellikine Llc Isoquinolin-1 (2h) -onas y tieno [2,3-d]pirimidin-4(3h) -onas substituidas, y metodos de uso de las mismas.
TWI546305B (zh) 2011-01-10 2016-08-21 英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
CN105102000B (zh) 2012-11-01 2021-10-22 无限药品公司 使用pi3激酶亚型调节剂的癌症疗法
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015178955A1 (en) * 2014-05-19 2015-11-26 Eternity Bioscience Inc. Substituted ethynyl heterobicyclic compounds as tyrosine kinase inhibitors
WO2015188369A1 (en) * 2014-06-13 2015-12-17 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
KR101710127B1 (ko) 2014-08-29 2017-02-27 한화제약주식회사 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민
WO2017000125A1 (en) 2015-06-29 2017-01-05 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
WO2017166104A1 (en) * 2016-03-30 2017-10-05 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
EP3474856B1 (en) 2016-06-24 2022-09-14 Infinity Pharmaceuticals, Inc. Combination therapies
IL266109B2 (en) * 2016-10-21 2025-05-01 Nimbus Lakshmi Inc Tyk2 inhibitors and uses thereof
CN108892635A (zh) * 2018-09-07 2018-11-27 江苏工程职业技术学院 一种西沙必利关键中间体的制备方法
CN114269383A (zh) * 2019-01-08 2022-04-01 菲斯生物制药公司 金属酶抑制剂化合物
PH12022551379A1 (en) 2019-12-06 2023-05-03 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
WO2024083237A1 (en) * 2022-10-20 2024-04-25 Impact Therapeutics (Shanghai) , Inc Substituted heteroaryl bicyclic compounds as usp1 inhibitors and the use thereof
IL321433A (en) 2022-12-16 2025-08-01 Astrazeneca Ab Purines 2,6,9 trimethylated

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
US5117830A (en) 1990-11-08 1992-06-02 Whitby Research, Inc. Method of determining viability of tissue
US5877179A (en) * 1992-09-29 1999-03-02 The United States Of America As Represented By The Department Of Health And Human Services Xanthines for identifying CFTR--binding compounds useful for activating chloride conductance in animal cells
RU2112765C1 (ru) * 1993-02-09 1998-06-10 Дзе Велкам Фаундейшн Лимитед ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ПРОЯВЛЯЮЩАЯ АКТИВНОСТЬ ПРОТИВ ВИРУСНОЙ ИНФЕКЦИИ И β D-АРАБИНОФУРАНОЗИЛ-2-АМИНО-6-МЕТОКСИ-9Н-ПУРИНЫ
US5670501A (en) * 1994-09-01 1997-09-23 Discovery Therapeutics, Inc. N-substituted 9-alkyladenines
EE200100502A (et) * 1999-03-26 2002-12-16 Astrazeneca Ab Ühendid
WO2004112793A1 (en) 2003-05-23 2004-12-29 Chiron Corporation Guanidino-substituted quinazolinone compounds as mc4-r agonists
EP1751159A2 (en) * 2004-04-28 2007-02-14 Cv Therapeutics, Inc. Purine derivatives as a1 adenosine receptor antagonists
WO2005113556A1 (en) 2004-05-13 2005-12-01 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
JP4820290B2 (ja) 2004-05-13 2011-11-24 第一三共株式会社 置換ピロリジン誘導体
WO2006099204A1 (en) 2005-03-11 2006-09-21 Aderis Pharmaceuticals, Inc. Substituted 9-alkyladenines and the use thereof
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
US7795427B2 (en) * 2006-02-14 2010-09-14 New York University Methods for inhibiting osteoclast differentiation, formation, or function and for increasing bone mass
AR079529A1 (es) * 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
US8759359B2 (en) * 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
DE102010011431A1 (de) * 2009-12-23 2011-06-30 WABCO GmbH, 30453 Ventileinrichtung für eine Luftfederungsanlage
NZ627520A (en) 2010-03-10 2015-10-30 Astrazeneca Ab 4-phenyl pyridine analogues as protein kinase inhibitors
CN102869359A (zh) 2010-03-17 2013-01-09 弗·哈夫曼-拉罗切有限公司 咪唑并吡啶和嘌呤化合物、组合物和使用方法
MX2012015143A (es) * 2010-06-30 2013-07-03 Amgen Inc Compuestos heterociclicos que contienen nitrogeno como inhibidores de pi3k delta.
UA112517C2 (uk) * 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
ES2612503T3 (es) * 2010-09-14 2017-05-17 Exelixis, Inc. Compuestos 9H-purina como inhibidores de PI3K-delta y métodos para su preparación
EP2632898A4 (en) * 2010-10-29 2014-04-02 Biogen Idec Inc HETEROCYCLIC TYROSINE KINASE HEMMER
EP2518070A1 (en) * 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
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
BR112015011147A2 (pt) 2017-07-11
RU2661896C2 (ru) 2018-07-23
CA2891013A1 (en) 2014-05-22
BR112015011147A8 (pt) 2019-10-01
EP2920172A4 (en) 2016-05-25
KR20150084992A (ko) 2015-07-22
AU2013347539B2 (en) 2017-06-15
EP2920172A1 (en) 2015-09-23
EP2920172B1 (en) 2019-12-25
RU2015122894A (ru) 2017-01-10
US20160207926A1 (en) 2016-07-21
CN104918940A (zh) 2015-09-16
MX2015006192A (es) 2015-08-10
CN104918940B (zh) 2017-03-08
AU2013347539A1 (en) 2015-05-07
US9938281B2 (en) 2018-04-10
JP2016502522A (ja) 2016-01-28
WO2014075393A1 (en) 2014-05-22

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