CA2891009A1 - 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
CA2891009A1
CA2891009A1 CA2891009A CA2891009A CA2891009A1 CA 2891009 A1 CA2891009 A1 CA 2891009A1 CA 2891009 A CA2891009 A CA 2891009A CA 2891009 A CA2891009 A CA 2891009A CA 2891009 A1 CA2891009 A1 CA 2891009A1
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CA
Canada
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.)
Abandoned
Application number
CA2891009A
Other languages
English (en)
French (fr)
Inventor
Abdelghani Abe Achab
Michael D. Altman
Yongqi Deng
Timothy Guzi
Solomon Kattar
Jason D. Katz
Joey L. Methot
Hua Zhou
Meredeth MCGOWAN
Matthew P. CHRISTOPHER
Yudith Garcia
Neville John ANTHONY
Francesc Xavier FRADERA LLINAS
Changwei Mu
Sixing ZHANG
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 CA2891009A1 publication Critical patent/CA2891009A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06Heterocyclic 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
    • 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
    • C07D473/28Oxygen atom
    • 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
    • C07D473/28Oxygen atom
    • C07D473/30Oxygen atom attached in position 6, e.g. hypoxanthine
    • 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
    • C07D473/36Sulfur atom
    • C07D473/38Sulfur atom attached in position 6
    • 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

  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
CA2891009A 2012-11-16 2013-11-15 Purine inhibitors of human phosphatidylinositol 3-kinase delta Abandoned CA2891009A1 (en)

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 (1)

Publication Number Publication Date
CA2891009A1 true CA2891009A1 (en) 2014-05-22

Family

ID=50730541

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2891009A Abandoned CA2891009A1 (en) 2012-11-16 2013-11-15 Purine inhibitors of human phosphatidylinositol 3-kinase delta

Country Status (11)

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

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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
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
MD4649C1 (ro) 2013-12-05 2020-04-30 Pfizer Inc. Pirol[2,3-d]pirimidinil, pirol[2,3-b]pirazinil şi pirol[2,3-d]piridinil acrilamide
JP6262885B2 (ja) * 2014-03-06 2018-01-17 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. オレキシン受容体拮抗剤としてのピペリジン誘導体
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
MX2017003254A (es) 2014-09-11 2017-10-12 Janssen Pharmaceutica Nv 2-azabiciclos sustituidos y su uso como moduladores de receptores de orexina.
CN107912040B (zh) * 2014-10-10 2021-04-06 基因泰克公司 作为组蛋白脱甲基酶抑制剂的吡咯烷酰胺化合物
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
SI3512857T1 (sl) * 2016-09-14 2021-07-30 Janssen Pharmaceutica Nv Spiro biciklični zaviralci interakcije menin-MLL
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
IL293965A (en) 2019-12-19 2022-08-01 Janssen Pharmaceutica Nv History of Spiro straight chain transformed
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
CN117203212A (zh) * 2021-03-29 2023-12-08 株式会社钟化 (2-甲基嘧啶-5-基)硼酸衍生物的制造方法
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

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US5670501A (en) 1994-09-01 1997-09-23 Discovery Therapeutics, Inc. N-substituted 9-alkyladenines
EP1278748B1 (en) * 2000-04-25 2011-03-23 ICOS Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
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Also Published As

Publication number Publication date
US20150353552A1 (en) 2015-12-10
WO2014075392A1 (en) 2014-05-22
CN104918939B (zh) 2018-08-28
EP2920171B1 (en) 2018-08-29
MX2015006191A (es) 2015-08-10
JP2015537010A (ja) 2015-12-24
AU2013347538B2 (en) 2017-04-27
EP2920171A1 (en) 2015-09-23
AU2013347538A1 (en) 2015-05-07
RU2015122895A (ru) 2017-01-10
KR20150082613A (ko) 2015-07-15
US9730940B2 (en) 2017-08-15
BR112015011148A8 (pt) 2019-10-01
EP2920171A4 (en) 2016-06-22
RU2658006C2 (ru) 2018-06-19
CN104918939A (zh) 2015-09-16
BR112015011148A2 (pt) 2017-07-11
JP6297582B2 (ja) 2018-03-20

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20181031

FZDE Discontinued

Effective date: 20210831