RU2658006C2 - Пуриновые ингибиторы человеческой фосфатидилинозит 3-киназы дельта - Google Patents

Пуриновые ингибиторы человеческой фосфатидилинозит 3-киназы дельта Download PDF

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RU2658006C2
RU2658006C2 RU2015122895A RU2015122895A RU2658006C2 RU 2658006 C2 RU2658006 C2 RU 2658006C2 RU 2015122895 A RU2015122895 A RU 2015122895A RU 2015122895 A RU2015122895 A RU 2015122895A RU 2658006 C2 RU2658006 C2 RU 2658006C2
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methyl
oxy
ethyl
pyrrolidin
purine
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RU2015122895A
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Russian (ru)
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RU2015122895A (ru
Inventor
Абделгхани Абе АЧАБ
Майкл Д. АЛЬТМАН
Йонгки ДЕНГ
Тимоти ГЮЗИ
Соломон Каттар
Джейсон Д. КАТЦ
Джон Л. МЕТОТ
Хуа Чжоу
Мередет МАКГОВАН
Мэттью П. КРИСТОФЕР
Юдит ГАРСИЯ
Невилл Джон ЭНТОНИ
ЛЬИНАС Франсеск Ксавьер ФРАДЕРА
Чанвэй МУ
Сисин ЧЖАН
Жун ЧЖАН
Кин Чиу Фонг
Сяньшэн ЛЭН
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Мерк Шарп И Доум Корп.
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    • 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
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
RU2015122895A 2012-11-16 2013-11-15 Пуриновые ингибиторы человеческой фосфатидилинозит 3-киназы дельта RU2658006C2 (ru)

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

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RU2015122895A RU2015122895A (ru) 2017-01-10
RU2658006C2 true RU2658006C2 (ru) 2018-06-19

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RU2015122895A RU2658006C2 (ru) 2012-11-16 2013-11-15 Пуриновые ингибиторы человеческой фосфатидилинозит 3-киназы дельта

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

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RU2852176C1 (ru) * 2019-09-16 2025-12-04 Aтен Порус Лайфсайнсес Пвт. Лтд. 2-амино-s6-замещенные тиопуриновые соединения в качестве ингибиторов белка enpp1

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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
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
LT3077395T (lt) 2013-12-05 2018-02-12 Pfizer Inc. Pirolo[2,3-d]pirimidinilo, pirolo[2,3-b]pirazinilo ir pirolo[2,3-d]piridinilo akrilamidai
WO2015131773A1 (zh) * 2014-03-06 2015-09-11 上海海雁医药科技有限公司 作为食欲素受体拮抗剂的哌啶衍生物
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
JP6715239B2 (ja) 2014-09-11 2020-07-01 ヤンセン ファーマシューティカ エヌ.ベー. 置換2−アザ二環式化合物及びオレキシン受容体調節因子としてのその使用
EP3204379B1 (en) * 2014-10-10 2019-03-06 Genentech, Inc. Pyrrolidine amide compounds as histone demethylase inhibitors
WO2017134053A1 (en) * 2016-02-04 2017-08-10 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
AU2017326487B2 (en) * 2016-09-14 2021-08-05 Janssen Pharmaceutica Nv Spiro bicyclic inhibitors of menin-MLL interaction
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
UY38988A (es) 2019-12-19 2021-06-30 Janssen Pharmaceutica Nv Derivados espiráncos sustituidos de cadena lineal
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
JP7736782B2 (ja) * 2021-03-29 2025-09-09 株式会社カネカ (2-メチルピリミジン-5-イル)ボロン酸誘導体の製造方法
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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Kochergin P M; Gromov M Yu; Aleksandrova E V; Skachilova S Ya. Synthesis and some properties of 6-.beta.-oxoalkyl(aralkyl, hetaralkyl, cycloalkyl)thiopurines,Chemistry of Heterocyclic Compounds, 1993, vol 29, No.11, страницы 1335-1339. EP 0421819 A1, WELLCOME FOUND, 10.04.1991 (примеры 21, 22). SCHABEL F M Jr; MONTGOMERY J A; SKIPPER H E; LASTER W R Jr; THOMSON J R. Experimental evaluation of potential anticancer agents. I. Quantitative therapeutic evaluation of certain purine analogs CANCER RESEARCH, 1961, vol 21, pages 690-699. Camilla M Smith; Fontanelle Lydia J; Lalanne Marcel; Henderson3 J Frank Inhibition of Purine Ribonucleotide and Phosphoribosyl Pyrophosphate Synthesis by 6-Cyclopentylthio-9-hydroxymethylpurine and Structurally Related Compounds1, CANCER RESEARCH, 1974,Vol: 34, Nr: 3, Page(s): 463-467. Temple; Carroll; Et Al LIPID-SOLUABLE DERIVATIVES OF 6-MERCAPTOPURINE J.MED.CHEM, 1968,Vol: 11, Nr: 1, Page(s): 41-44 (см. соединение 9). *
SCHABEL F M Jr; MONTGOMERY J A; SKIPPER H E; LASTER W R Jr; THOMSON J R. Experimental evaluation of potential anticancer agents. I. Quantitative therapeutic evaluation of certain purine analogs CANCER RESEARCH, 1961, vol 21, pages 690-699. *
Temple; Carroll; Et Al LIPID-SOLUABLE DERIVATIVES OF 6-MERCAPTOPURINE J.MED.CHEM, 1968,Vol: 11, Nr: 1, Page(s): 41-44 (см. соединение 9). *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2852176C1 (ru) * 2019-09-16 2025-12-04 Aтен Порус Лайфсайнсес Пвт. Лтд. 2-амино-s6-замещенные тиопуриновые соединения в качестве ингибиторов белка enpp1
RU2852176C9 (ru) * 2019-09-16 2026-07-13 Aтен Порус Лайфсайнсес Пвт. Лтд. 2-амино-s6-замещенные тиопуриновые соединения в качестве ингибиторов белка enpp1

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US9730940B2 (en) 2017-08-15
CA2891009A1 (en) 2014-05-22
MX2015006191A (es) 2015-08-10
RU2015122895A (ru) 2017-01-10
EP2920171A1 (en) 2015-09-23
WO2014075392A1 (en) 2014-05-22
JP2015537010A (ja) 2015-12-24
EP2920171B1 (en) 2018-08-29
JP6297582B2 (ja) 2018-03-20
AU2013347538A1 (en) 2015-05-07
EP2920171A4 (en) 2016-06-22
BR112015011148A2 (pt) 2017-07-11
CN104918939B (zh) 2018-08-28
CN104918939A (zh) 2015-09-16
BR112015011148A8 (pt) 2019-10-01
KR20150082613A (ko) 2015-07-15
US20150353552A1 (en) 2015-12-10
AU2013347538B2 (en) 2017-04-27

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