CA2891013A1 - Purine inhibitors of human phosphatidylinositol 3-kinase delta - Google Patents

Purine inhibitors of human phosphatidylinositol 3-kinase delta Download PDF

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Publication number
CA2891013A1
CA2891013A1 CA2891013A CA2891013A CA2891013A1 CA 2891013 A1 CA2891013 A1 CA 2891013A1 CA 2891013 A CA2891013 A CA 2891013A CA 2891013 A CA2891013 A CA 2891013A CA 2891013 A1 CA2891013 A1 CA 2891013A1
Authority
CA
Canada
Prior art keywords
purin
ethyl
pyrrolidin
methylpyrimidin
amino
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.)
Abandoned
Application number
CA2891013A
Other languages
English (en)
French (fr)
Inventor
Abdelghani Abe Achab
Michael D. Altman
Yongqi Deng
Solomon Kattar
Jason D. Katz
Joey L. Methot
Hua Zhou
Meredeth MCGOWAN
Matthew P. CHRISTOPHER
Yudith Garcia
Neville John ANTHONY
Francesc Xavier FRADERA LLINAS
Liping Yang
Changwei Mu
Xiaona Wang
Feng Shi
Baijun YE
Sixing ZHANG
Xiaoli Zhao
Rong Zhang
Kin Chiu Fong
Xiansheng LENG
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 CA2891013A1 publication Critical patent/CA2891013A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2891013A 2012-11-16 2013-11-15 Purine inhibitors of human phosphatidylinositol 3-kinase delta Abandoned CA2891013A1 (en)

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 (1)

Publication Number Publication Date
CA2891013A1 true CA2891013A1 (en) 2014-05-22

Family

ID=50730542

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2891013A Abandoned CA2891013A1 (en) 2012-11-16 2013-11-15 Purine inhibitors of human phosphatidylinositol 3-kinase delta

Country Status (11)

Country Link
US (1) US9938281B2 (OSRAM)
EP (1) EP2920172B1 (OSRAM)
JP (1) JP6322200B2 (OSRAM)
KR (1) KR20150084992A (OSRAM)
CN (1) CN104918940B (OSRAM)
AU (1) AU2013347539B2 (OSRAM)
BR (1) BR112015011147A8 (OSRAM)
CA (1) CA2891013A1 (OSRAM)
MX (1) MX2015006192A (OSRAM)
RU (1) RU2661896C2 (OSRAM)
WO (1) WO2014075393A1 (OSRAM)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009088990A1 (en) 2008-01-04 2009-07-16 Intellikine, Inc. Certain chemical entities, compositions and methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
NZ612909A (en) 2011-01-10 2015-09-25 Infinity Pharmaceuticals Inc Processes for preparing isoquinolinones and solid forms of isoquinolinones
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
CA2890105C (en) 2012-11-01 2023-03-21 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
US10144737B2 (en) * 2014-05-19 2018-12-04 Jiangsu Hengrui Medicine Co., Ltd. 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
WO2017223422A1 (en) 2016-06-24 2017-12-28 Infinity Pharmaceuticals, Inc. Combination therapies
AU2017345736B2 (en) 2016-10-21 2022-04-07 Takeda Pharmaceutical Company Limited 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
AU2020207051B2 (en) * 2019-01-08 2025-07-24 Corxel Pharmaceuticals Hong Kong Limited Metalloenzyme inhibitor compounds
MX2022006865A (es) 2019-12-06 2022-07-11 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio.
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
CN120092008A (zh) * 2022-10-20 2025-06-03 上海瑛派药业有限公司 取代的杂芳基双环化合物作为usp1抑制剂及其应用
US20240247001A1 (en) 2022-12-16 2024-07-25 Astrazeneca Ab 2,6,9-trisubstituted purines

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
KR20010108394A (ko) 1999-03-26 2001-12-07 다비드 에 질레스 신규 화합물
JP2007501861A (ja) 2003-05-23 2007-02-01 カイロン コーポレイション Mc4−rアゴニストとしてのグアニジノ置換キナゾリノン化合物
CA2565037A1 (en) 2004-04-28 2005-11-10 Cv Therapeutics, Inc. Purine derivatives as a1 adenosine receptor antagonists
ES2873875T3 (es) * 2004-05-13 2021-11-04 Icos Corp Quinazolinonas como inhibidores de fosfatidilinositol 3-quinasa delta humano
WO2005111015A1 (ja) 2004-05-13 2005-11-24 Daiichi Pharmaceutical Co., Ltd. 置換ピロリジン誘導体
US20080161327A1 (en) * 2005-03-11 2008-07-03 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
US8759359B2 (en) * 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
TW201130842A (en) * 2009-12-18 2011-09-16 Incyte Corp Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
DE102010011431A1 (de) * 2009-12-23 2011-06-30 WABCO GmbH, 30453 Ventileinrichtung für eine Luftfederungsanlage
EA201201274A1 (ru) 2010-03-10 2013-04-30 Инджениум Фармасьютиклз Гмбх Ингибиторы протеинкиназ
RU2012141536A (ru) 2010-03-17 2014-04-27 Ф. Хоффманн-Ля Рош Аг Имидазопиридины, композиции и способы применения
CA2803620A1 (en) * 2010-06-30 2012-01-05 Amgen Inc. Heterocyclic compounds and their uses
UA112517C2 (uk) * 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
JP5954838B2 (ja) 2010-09-14 2016-07-20 エクセリクシス, インク. Pi3k−デルタの阻害剤ならびにそれらの使用法および製造法
US9273028B2 (en) 2010-10-29 2016-03-01 Biogen Ma Inc. Heterocyclic tyrosine kinase inhibitors
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
MX2015006192A (es) 2015-08-10
AU2013347539A1 (en) 2015-05-07
BR112015011147A8 (pt) 2019-10-01
JP6322200B2 (ja) 2018-05-09
JP2016502522A (ja) 2016-01-28
EP2920172B1 (en) 2019-12-25
RU2661896C2 (ru) 2018-07-23
CN104918940B (zh) 2017-03-08
EP2920172A4 (en) 2016-05-25
WO2014075393A1 (en) 2014-05-22
EP2920172A1 (en) 2015-09-23
KR20150084992A (ko) 2015-07-22
US20160207926A1 (en) 2016-07-21
BR112015011147A2 (pt) 2017-07-11
US9938281B2 (en) 2018-04-10
AU2013347539B2 (en) 2017-06-15
CN104918940A (zh) 2015-09-16
RU2015122894A (ru) 2017-01-10

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20181101

FZDE Discontinued

Effective date: 20210831