RU2661896C2 - Пуриновые ингибиторы фосфатидилинозитол-3-киназы дельта человека - Google Patents

Пуриновые ингибиторы фосфатидилинозитол-3-киназы дельта человека Download PDF

Info

Publication number
RU2661896C2
RU2661896C2 RU2015122894A RU2015122894A RU2661896C2 RU 2661896 C2 RU2661896 C2 RU 2661896C2 RU 2015122894 A RU2015122894 A RU 2015122894A RU 2015122894 A RU2015122894 A RU 2015122894A RU 2661896 C2 RU2661896 C2 RU 2661896C2
Authority
RU
Russia
Prior art keywords
ethyl
purin
pyrrolidin
amino
amine
Prior art date
Application number
RU2015122894A
Other languages
English (en)
Russian (ru)
Other versions
RU2015122894A (ru
Inventor
Абделгхани Абе АЧАБ
Майкл Д. АЛЬТМАН
Йонгки ДЕНГ
Соломон Каттар
Джейсон Д. КАТЦ
Джон Л. МЕТОТ
Хуа Чжоу
Мередет МАКГОВАН
Мэттью П. КРИСТОФЕР
Юдит ГАРСИЯ
Невилл Джон ЭНТОНИ
ЛЬИНАС Франсеск Ксавьер ФРАДЕРА
Липин ЯН
Чанвэй МУ
Сяона ВАН
Фэн ШИ
Байцзюнь Е
Сисин ЧЖАН
Сяоли ЧЖАО
Жун ЧЖАН
Кин Чиу Фонг
Сяньшэн ЛЭН
Original Assignee
Мерк Шарп И Доум Корп.
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 Мерк Шарп И Доум Корп. filed Critical Мерк Шарп И Доум Корп.
Publication of RU2015122894A publication Critical patent/RU2015122894A/ru
Application granted granted Critical
Publication of RU2661896C2 publication Critical patent/RU2661896C2/ru

Links

Classifications

    • 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
    • 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
    • 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)
RU2015122894A 2012-11-16 2013-11-15 Пуриновые ингибиторы фосфатидилинозитол-3-киназы дельта человека RU2661896C2 (ru)

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 (2)

Publication Number Publication Date
RU2015122894A RU2015122894A (ru) 2017-01-10
RU2661896C2 true RU2661896C2 (ru) 2018-07-23

Family

ID=50730542

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2015122894A RU2661896C2 (ru) 2012-11-16 2013-11-15 Пуриновые ингибиторы фосфатидилинозитол-3-киназы дельта человека

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
BRPI0906473A8 (pt) 2008-01-04 2016-02-10 Intellikine Inc Certas entidades químicas, composições e métodos
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
EP3238722B1 (en) 2011-01-10 2019-03-13 Infinity Pharmaceuticals, Inc. 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
RU2702908C2 (ru) 2012-11-01 2019-10-14 Инфинити Фармасьютикалз, Инк. Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
EP3145512B1 (en) * 2014-05-19 2019-07-17 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
EP3474856B1 (en) 2016-06-24 2022-09-14 Infinity Pharmaceuticals, Inc. Combination therapies
CN110300590A (zh) 2016-10-21 2019-10-01 林伯士拉克许米公司 Tyk2抑制剂及其用途
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
CA3126224A1 (en) * 2019-01-08 2020-07-16 Corxel Pharmaceuticals Hong Kong Limited Metalloenzyme inhibitor compounds
PH12022551379A1 (en) 2019-12-06 2023-05-03 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
WO2024083237A1 (en) * 2022-10-20 2024-04-25 Impact Therapeutics (Shanghai) , Inc Substituted heteroaryl bicyclic compounds as usp1 inhibitors and the use thereof
AR131380A1 (es) 2022-12-16 2025-03-12 Astrazeneca Ab Purinas 2,6,9-trisustituidas

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2011075643A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
WO2011076302A1 (de) * 2009-12-23 2011-06-30 Wabco Gmbh & Co. Ohg Ventileinrichtung für eine luftfederungsanlage
WO2012003264A1 (en) * 2010-06-30 2012-01-05 Amgen Inc. Nitrogen containing heterocyclic compounds as pik3 -delta inhibitors
WO2012037226A1 (en) * 2010-09-14 2012-03-22 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
WO2012058645A1 (en) * 2010-10-29 2012-05-03 Biogen Idec Ma Inc. Heterocyclic tyrosine kinase 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

Family Cites Families (19)

* 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
US5670501A (en) * 1994-09-01 1997-09-23 Discovery Therapeutics, Inc. N-substituted 9-alkyladenines
AU4157500A (en) * 1999-03-26 2000-10-16 Astrazeneca Ab Novel compounds
EP1651229A1 (en) 2003-05-23 2006-05-03 Chiron Corporation Guanidino-substituted quinazolinone compounds as mc4-r agonists
CA2565037A1 (en) * 2004-04-28 2005-11-10 Cv Therapeutics, Inc. Purine derivatives as a1 adenosine receptor antagonists
US7977327B2 (en) 2004-05-13 2011-07-12 Daiichi Sankyo Company, Limited Substituted pyrrolidine derivative
LT2612862T (lt) 2004-05-13 2017-01-25 Icos Corporation Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai
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
WO2011075630A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors
EA201201274A1 (ru) 2010-03-10 2013-04-30 Инджениум Фармасьютиклз Гмбх Ингибиторы протеинкиназ
US20130096104A1 (en) * 2010-03-17 2013-04-18 Genentech, Inc. Imidazopyridine compounds, compositions and methods of use
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
EP2518070A1 (en) * 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2011075643A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
WO2011076302A1 (de) * 2009-12-23 2011-06-30 Wabco Gmbh & Co. Ohg Ventileinrichtung für eine luftfederungsanlage
WO2012003264A1 (en) * 2010-06-30 2012-01-05 Amgen Inc. Nitrogen containing heterocyclic compounds as pik3 -delta inhibitors
WO2012037226A1 (en) * 2010-09-14 2012-03-22 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
WO2012058645A1 (en) * 2010-10-29 2012-05-03 Biogen Idec Ma Inc. Heterocyclic tyrosine kinase 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
EP2920172B1 (en) 2019-12-25
JP2016502522A (ja) 2016-01-28
EP2920172A4 (en) 2016-05-25
CN104918940B (zh) 2017-03-08
BR112015011147A2 (pt) 2017-07-11
WO2014075393A1 (en) 2014-05-22
BR112015011147A8 (pt) 2019-10-01
AU2013347539B2 (en) 2017-06-15
CN104918940A (zh) 2015-09-16
US9938281B2 (en) 2018-04-10
JP6322200B2 (ja) 2018-05-09
KR20150084992A (ko) 2015-07-22
EP2920172A1 (en) 2015-09-23
MX2015006192A (es) 2015-08-10
CA2891013A1 (en) 2014-05-22
RU2015122894A (ru) 2017-01-10
AU2013347539A1 (en) 2015-05-07
US20160207926A1 (en) 2016-07-21

Similar Documents

Publication Publication Date Title
US9938281B2 (en) Purine inhibitors of human phosphatidylinositol 3-kinase delta
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
US10336762B2 (en) Pyrrolo[1,2-b]pyridazine derivatives
EP4626554A1 (en) Glutarimide-containing kras-mutant degrader compounds and uses thereof
EP3154976B1 (en) Purine inhibitors of human phosphatidylinositol 3-kinase delta
TWI922529B (zh) 化合物、組合物及方法
IL300289A (en) Compounds, preparations and methods
WO2022165530A1 (en) Small molecule inhibitors of salt inducible kinases
JP7834249B2 (ja) サイクリン依存性キナーゼ（ｃｄｋ２）阻害薬
EP3313397B1 (en) Purine inhibitors of human phosphatidylinositol 3-kinase delta

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20201116