EA201170052A1 - Производные тиофена или тиазола и их применение как ингибиторов pi3k - Google Patents

Производные тиофена или тиазола и их применение как ингибиторов pi3k

Info

Publication number
EA201170052A1
EA201170052A1 EA201170052A EA201170052A EA201170052A1 EA 201170052 A1 EA201170052 A1 EA 201170052A1 EA 201170052 A EA201170052 A EA 201170052A EA 201170052 A EA201170052 A EA 201170052A EA 201170052 A1 EA201170052 A1 EA 201170052A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tiophene
thiazole
derivatives
application
pi3k inhibitors
Prior art date
Application number
EA201170052A
Other languages
English (en)
Inventor
Дэвид П. Кардин
Джеффри Л. Голин
Пол Д. Гринспан
Степан Вискоцил
Тяньлинь Сюй
Кристелль С. Рену
Original Assignee
Милленниум Фармасьютикалз, Инк.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41010579&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201170052(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Милленниум Фармасьютикалз, Инк. filed Critical Милленниум Фармасьютикалз, Инк.
Publication of EA201170052A1 publication Critical patent/EA201170052A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

В изобретении предлагаются соединения формулы Iгде R, R, CY, Y, Y, X, Xи Хявляются такими, как описано в описании. Соединения являются ингибиторами PI3K и, таким образом, пригодны для лечения пролиферативных, воспалительных или сердечно-сосудистых расстройств.
EA201170052A 2008-06-19 2009-06-17 Производные тиофена или тиазола и их применение как ингибиторов pi3k EA201170052A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13248408P 2008-06-19 2008-06-19
PCT/US2009/003607 WO2009154741A1 (en) 2008-06-19 2009-06-17 Thiophene or thiazole derivatives and their use as pi3k inhibitors

Publications (1)

Publication Number Publication Date
EA201170052A1 true EA201170052A1 (ru) 2011-06-30

Family

ID=41010579

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170052A EA201170052A1 (ru) 2008-06-19 2009-06-17 Производные тиофена или тиазола и их применение как ингибиторов pi3k

Country Status (21)

Country Link
US (3) US8183240B2 (ru)
EP (1) EP2313399B1 (ru)
JP (1) JP5596026B2 (ru)
KR (1) KR20110018451A (ru)
CN (1) CN102066365A (ru)
AU (1) AU2009260782B2 (ru)
BR (1) BRPI0914223A2 (ru)
CA (1) CA2727069A1 (ru)
CL (1) CL2010001474A1 (ru)
CO (1) CO6331431A2 (ru)
CR (1) CR20110032A (ru)
EA (1) EA201170052A1 (ru)
ES (1) ES2491522T3 (ru)
GE (1) GEP20125650B (ru)
IL (1) IL210055A0 (ru)
MA (1) MA32468B1 (ru)
MX (1) MX2010014125A (ru)
NZ (1) NZ589844A (ru)
UA (1) UA106206C2 (ru)
WO (1) WO2009154741A1 (ru)
ZA (1) ZA201008875B (ru)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5581219B2 (ja) 2008-01-25 2014-08-27 ミレニアム ファーマシューティカルズ， インコーポレイテッド チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用
MX2010014125A (es) * 2008-06-19 2011-02-24 Millennium Pharm Inc Derivados de tiofeno o tiazol y su uso como inhibidores de p13k.
JP2012516329A (ja) * 2009-01-30 2012-07-19 ミレニアム ファーマシューティカルズ， インコーポレイテッド Ｐｉ３ｋ阻害剤としてのヘテロアリールおよびその使用
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
JP2013533318A (ja) * 2010-08-11 2013-08-22 ミレニアム ファーマシューティカルズ， インコーポレイテッド ヘテロアリールおよびその使用
AR082665A1 (es) * 2010-08-11 2012-12-26 Millennium Pharm Inc Derivados heteroarilicos inhibidores de quinasas pi3k, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos proliferativos, inflamatorios y/o cardiovasculares
WO2012021611A1 (en) * 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
JP5726635B2 (ja) 2010-08-25 2015-06-03 株式会社Ｎｔｔドコモ マルチモードフロントエンド回路
TW201307309A (zh) 2010-10-13 2013-02-16 Millennium Pharm Inc 雜芳基化合物及其用途
CN102503930B (zh) * 2011-10-28 2014-07-02 浙江大学 3,4,5,-三取代氨基噻吩类化合物及其制备和用途
KR102038462B1 (ko) 2011-12-15 2019-10-31 노파르티스 아게 Pi3k의 활성 또는 기능의 억제제의 용도
WO2013096642A1 (en) * 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
CA2865642C (en) * 2012-03-14 2021-10-26 Salk Institute For Biological Studies Adenoviral tumor diagnostics
EP2971008B1 (en) 2013-03-14 2018-07-25 Salk Institute for Biological Studies Oncolytic adenovirus compositions
CA2905123A1 (en) 2013-03-15 2014-09-18 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
CN106164071B (zh) * 2014-02-14 2019-09-10 不列颠哥伦比亚大学 作为治疗剂的人雄激素受体dna-结合结构域(dbd)化合物及其使用方法
JP7015551B2 (ja) 2016-02-23 2022-02-15 ソーク インスティテュート フォー バイオロジカル スタディーズ ウイルス動態への影響を最小限にするための治療用アデノウイルスにおける外因性遺伝子発現
CA3013637A1 (en) 2016-02-23 2017-08-31 Salk Institute For Biological Studies High throughput assay for measuring adenovirus replication kinetics
CN110062630A (zh) 2016-12-12 2019-07-26 萨克生物研究学院 肿瘤靶向合成腺病毒及其用途
JP7498199B2 (ja) 2019-06-28 2024-06-11 ファイザー・インク 種々の疾患を処置するために有用なｂｃｋｄｋ阻害剤としての５－（チオフェン－２－イル）－１ｈ－テトラゾール誘導体
CN110759900B (zh) * 2019-10-25 2021-07-30 沈阳药科大学 噻吩类化合物的制备方法和用途
EP4285723A3 (en) 2019-12-20 2024-03-27 Bayer Aktiengesellschaft Substituted thiophene carboxamides, thiophene carboxylic acids and derivatives thereof
CN113527281B (zh) * 2020-04-20 2023-12-22 昆山彭济凯丰生物科技有限公司 杂环化合物及其制备方法和应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD275870A1 (de) 1988-09-27 1990-02-07 Univ Leipzig Verfahren zur herstellung von in 5-position verschiedenartig substituierten 3-aminothiophen-4-carbonitrilen
AU2005325271A1 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. PDE4B inhibitors and uses therefor
GB0508472D0 (en) * 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
RU2439074C2 (ru) 2006-04-26 2012-01-10 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНОЕ ТИЕНО[3,2-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (РI3К)
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CA2660758A1 (en) * 2006-08-24 2008-02-27 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
EP2207781B1 (en) * 2007-09-24 2012-11-28 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
JP5581219B2 (ja) 2008-01-25 2014-08-27 ミレニアム ファーマシューティカルズ， インコーポレイテッド チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用
MX2010014125A (es) * 2008-06-19 2011-02-24 Millennium Pharm Inc Derivados de tiofeno o tiazol y su uso como inhibidores de p13k.

Also Published As

Publication number Publication date
MA32468B1 (fr) 2011-07-03
US8440664B2 (en) 2013-05-14
WO2009154741A1 (en) 2009-12-23
GEP20125650B (en) 2012-09-25
CN102066365A (zh) 2011-05-18
AU2009260782B2 (en) 2014-12-11
MX2010014125A (es) 2011-02-24
JP2011524904A (ja) 2011-09-08
KR20110018451A (ko) 2011-02-23
US8183240B2 (en) 2012-05-22
WO2009154741A8 (en) 2010-03-25
EP2313399B1 (en) 2014-05-28
JP5596026B2 (ja) 2014-09-24
NZ589844A (en) 2012-11-30
EP2313399A1 (en) 2011-04-27
CA2727069A1 (en) 2009-12-23
ES2491522T3 (es) 2014-09-08
BRPI0914223A2 (pt) 2019-09-24
US20120202812A1 (en) 2012-08-09
US20100075951A1 (en) 2010-03-25
ZA201008875B (en) 2012-02-29
IL210055A0 (en) 2011-02-28
CO6331431A2 (es) 2011-10-20
AU2009260782A1 (en) 2009-12-23
US20130217689A1 (en) 2013-08-22
CR20110032A (es) 2011-03-14
UA106206C2 (ru) 2014-08-11
CL2010001474A1 (es) 2011-04-29

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