EA201400831A1 - Пиразолопиримидиниловые ингибиторы убиквитин-активирующего фермента - Google Patents

Пиразолопиримидиниловые ингибиторы убиквитин-активирующего фермента

Info

Publication number
EA201400831A1
EA201400831A1 EA201400831A EA201400831A EA201400831A1 EA 201400831 A1 EA201400831 A1 EA 201400831A1 EA 201400831 A EA201400831 A EA 201400831A EA 201400831 A EA201400831 A EA 201400831A EA 201400831 A1 EA201400831 A1 EA 201400831A1
Authority
EA
Eurasian Patent Office
Prior art keywords
ubiquitin
structural units
chemical structural
activating enzyme
pyrazolopyrimidinyl
Prior art date
Application number
EA201400831A
Other languages
English (en)
Other versions
EA035020B1 (ru
Inventor
Роушан Афроуз
Инду Т. Бхаратхан
Джеффри П. Сиаварри
Пол Е. Флеминг
Джеффри Л. Голин
Марио Жирард
Стивен П. Лэнгстон
Франсуа Р. Суси
Цу-Чин Вонг
Йингчун Йе
Original Assignee
Миллениум 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
Application filed by Миллениум Фармасьютикалз, Инк. filed Critical Миллениум Фармасьютикалз, Инк.
Publication of EA201400831A1 publication Critical patent/EA201400831A1/ru
Publication of EA035020B1 publication Critical patent/EA035020B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Раскрыты химические структурные единицы, которые ингибируют убиквитин-активирующий фермент (UAE), каждая из которых представляет собой соединение формулы Iили его фармацевтически приемлемую соль, где Y представляет собой формулу IIи W, Z, X, R, Rи Rопределены в описании изобретения; фармацевтические композиции, содержащие химические структурные единицы, и способы применения химических структурных единиц. Эти химические структурные единицы применимы для лечения нарушений, в частности нарушений пролиферации клеток, включая виды рака.
EA201400831A 2012-02-17 2013-02-14 Пиразолопиримидиниловые ингибиторы убиквитин-активирующего фермента EA035020B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261600070P 2012-02-17 2012-02-17
PCT/US2013/026113 WO2013123169A1 (en) 2012-02-17 2013-02-14 Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme

Publications (2)

Publication Number Publication Date
EA201400831A1 true EA201400831A1 (ru) 2014-12-30
EA035020B1 EA035020B1 (ru) 2020-04-17

Family

ID=48982730

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201400831A EA035020B1 (ru) 2012-02-17 2013-02-14 Пиразолопиримидиниловые ингибиторы убиквитин-активирующего фермента

Country Status (30)

Country Link
US (4) US9290500B2 (ru)
EP (3) EP3536692B1 (ru)
JP (1) JP6122877B2 (ru)
KR (1) KR20140123104A (ru)
CN (1) CN104136399B (ru)
AR (1) AR092797A1 (ru)
BR (1) BR112014020365B1 (ru)
CA (1) CA2864672C (ru)
CL (1) CL2014002181A1 (ru)
CO (1) CO7071135A2 (ru)
CR (1) CR20140380A (ru)
DO (1) DOP2014000187A (ru)
EA (1) EA035020B1 (ru)
EC (1) ECSP14019113A (ru)
ES (1) ES2739150T3 (ru)
GE (1) GEP201706687B (ru)
HK (1) HK1201817A1 (ru)
IL (1) IL234016A0 (ru)
MA (1) MA35932B1 (ru)
MX (1) MX352963B (ru)
NZ (1) NZ628969A (ru)
PE (1) PE20142244A1 (ru)
PH (1) PH12014501832A1 (ru)
SG (2) SG11201404757WA (ru)
TN (1) TN2014000351A1 (ru)
TW (1) TWI593688B (ru)
UA (1) UA116534C2 (ru)
UY (1) UY34629A (ru)
WO (1) WO2013123169A1 (ru)
ZA (1) ZA201406103B (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8008307B2 (en) 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
EP3536692B1 (en) 2012-02-17 2021-04-07 Millennium Pharmaceuticals, Inc. Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
EP2879681A4 (en) 2012-08-03 2015-12-23 Millennium Pharm Inc INDOINDUBSTITUTED PYRROLOPYRIMIDINYL HIBITORS OF UBA6
CN105492429A (zh) 2013-07-02 2016-04-13 米伦纽姆医药公司 Sumo活化酶的杂芳基抑制剂
JP6603712B2 (ja) * 2014-07-01 2019-11-06 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 Sumo活性化酵素の阻害薬として有用なヘテロアリール化合物
WO2016069392A1 (en) 2014-10-29 2016-05-06 Millennium Pharmaceuticals, Inc. Administration of ubiquitin-activating enzyme inhibitor and chemotherapeutic agents
JP6697453B2 (ja) 2014-10-29 2020-05-20 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Millennium Pharmaceuticals, Inc. ユビキチン活性化酵素阻害物質及び放射線の投与
CN112996790B (zh) 2018-10-30 2023-11-03 克洛诺斯生物公司 用于调节cdk9活性的化合物、组合物和方法
WO2023021498A1 (en) * 2021-08-16 2023-02-23 Moya Bio Ltd. Fused azole and furan based nucleoside analogs and uses thereof

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2477795A1 (en) 2002-02-28 2003-09-12 Kandasamy Sakthivel Nucleoside 5'-monophosphate mimics and their prodrugs
CN1310918C (zh) 2002-09-04 2007-04-18 先灵公司 作为细胞周期蛋白依赖激酶抑制剂的吡唑并嘧啶
US7196092B2 (en) 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
ATE362474T1 (de) 2002-09-04 2007-06-15 Schering Corp Pyrazolo(1,5-a)pyrimidine als hemmstoffe cyclin- abhängiger kinasen
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
WO2004087707A1 (en) 2003-03-31 2004-10-14 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
JP2005008581A (ja) * 2003-06-20 2005-01-13 Kissei Pharmaceut Co Ltd 新規なピラゾロ[1,5−a]ピリミジン誘導体、それを含有する医薬組成物およびそれらの用途
WO2005037845A1 (en) 2003-10-17 2005-04-28 Rigel Pharmaceuticals, Inc. Benzothiazole and thiazole[5,5-b] pyridine compositions and their use as ubiquitin ligase inhibitors
WO2006002284A1 (en) 2004-06-22 2006-01-05 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
PL1848718T3 (pl) 2005-02-04 2012-12-31 Millennium Pharm Inc Inhibitory enzymów hamujących E1
EP1940847A2 (en) 2005-10-06 2008-07-09 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
PT1989206E (pt) * 2006-02-02 2012-10-15 Millennium Pharm Inc Inibidores da enzima de ativação e1
WO2007099021A1 (en) * 2006-02-28 2007-09-07 Sez Ag Device and method for liquid treating disc-like articles
AU2007281993B2 (en) * 2006-08-08 2013-08-29 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
US8008307B2 (en) 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
TWI519508B (zh) 2007-06-12 2016-02-01 Achaogen Inc 抗菌劑
KR20100066475A (ko) * 2007-08-02 2010-06-17 밀레니엄 파머슈티컬스 인코퍼레이티드 E1 활성화 효소 억제제의 합성 방법
US9216983B2 (en) 2007-12-21 2015-12-22 Board Of Regents, University Of Texas System Dihydroorotate dehydrogenase inhibitors with selective anti-malarial activity
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
WO2010088518A2 (en) 2009-01-31 2010-08-05 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
KR20120024715A (ko) * 2009-05-14 2012-03-14 밀레니엄 파머슈티컬스 인코퍼레이티드 ((1s,2s,4r)?4?{4?〔(1s)?2,3?디하이드로?1h?인덴?1?일아미노〕?7h?피롤로〔2,3?d〕피리미딘?7?일}?2?하이드록시사이클로펜틸)메틸 설파메이트의 하이드로클로라이드 염
EP3064204A1 (en) 2010-03-01 2016-09-07 GTx, Inc. Compounds for treatment of cancer
US20120077814A1 (en) 2010-09-10 2012-03-29 Zhong Wang Sulfonamide, sulfamate, and sulfamothioate derivatives
US8809356B2 (en) 2011-08-24 2014-08-19 Millennium Pharmaceuticals, Inc. Inhibitors of NEDD8-activating enzyme
EP3536692B1 (en) 2012-02-17 2021-04-07 Millennium Pharmaceuticals, Inc. Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
EP2879681A4 (en) 2012-08-03 2015-12-23 Millennium Pharm Inc INDOINDUBSTITUTED PYRROLOPYRIMIDINYL HIBITORS OF UBA6
CN105492429A (zh) 2013-07-02 2016-04-13 米伦纽姆医药公司 Sumo活化酶的杂芳基抑制剂
JP6603712B2 (ja) 2014-07-01 2019-11-06 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 Sumo活性化酵素の阻害薬として有用なヘテロアリール化合物

Also Published As

Publication number Publication date
PH12014501832A1 (en) 2014-11-17
US20170369499A1 (en) 2017-12-28
US10202389B2 (en) 2019-02-12
WO2013123169A1 (en) 2013-08-22
EP3536692A1 (en) 2019-09-11
HK1201817A1 (en) 2015-09-11
BR112014020365A2 (pt) 2020-12-22
EP3173413B1 (en) 2019-05-01
TWI593688B (zh) 2017-08-01
US20170217968A1 (en) 2017-08-03
JP2015508775A (ja) 2015-03-23
MX352963B (es) 2017-12-15
EP3173413A1 (en) 2017-05-31
EP2814791A1 (en) 2014-12-24
UA116534C2 (uk) 2018-04-10
MA35932B1 (fr) 2014-12-01
CN104136399A (zh) 2014-11-05
ES2739150T3 (es) 2020-01-29
US9663525B2 (en) 2017-05-30
TN2014000351A1 (en) 2015-12-21
UY34629A (es) 2013-09-02
CN104136399B (zh) 2018-08-07
MX2014009944A (es) 2014-11-10
GEP201706687B (en) 2017-06-26
EA035020B1 (ru) 2020-04-17
CO7071135A2 (es) 2014-09-30
JP6122877B2 (ja) 2017-04-26
SG11201404757WA (en) 2014-09-26
US9796725B2 (en) 2017-10-24
CA2864672C (en) 2018-01-09
EP3536692B1 (en) 2021-04-07
CA2864672A1 (en) 2013-08-22
CR20140380A (es) 2014-10-28
BR112014020365B1 (pt) 2023-02-23
KR20140123104A (ko) 2014-10-21
NZ628969A (en) 2017-03-31
US20160244455A1 (en) 2016-08-25
US20130217682A1 (en) 2013-08-22
DOP2014000187A (es) 2014-10-15
IL234016A0 (en) 2014-09-30
SG10201606581RA (en) 2016-09-29
US9290500B2 (en) 2016-03-22
ZA201406103B (en) 2017-11-29
ECSP14019113A (es) 2015-09-30
US20140088096A9 (en) 2014-03-27
AR092797A1 (es) 2015-05-06
PE20142244A1 (es) 2015-01-07
CL2014002181A1 (es) 2014-12-12
TW201345909A (zh) 2013-11-16
EP2814791A4 (en) 2015-08-19

Similar Documents

Publication Publication Date Title
EA201400831A1 (ru) Пиразолопиримидиниловые ингибиторы убиквитин-активирующего фермента
PH12017502141A1 (en) Compounds and their methods of use
UA111382C2 (uk) Інгібітори протеїнкінази
PH12015500260A1 (en) Neprilysin inhibitors
NZ630925A (en) Pyrazolopyrimidine compounds as kinase inhibitors
EA201490673A1 (ru) Производные пирролопиримидина и пурина
EA201590879A1 (ru) Арилконденсированные и гетероарилконденсированные лактамы
MX2013008212A (es) Derivados de 7-azaindol.
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201590224A1 (ru) Имидазотриазинкарбонитрилы, используемые в качестве ингибиторов киназы
MX340402B (es) Inhibidores triciclicos de cinasas.
MX2015012850A (es) Inhibidores de la arginina metiltransferasa y usos de los mismos.
EA201301209A1 (ru) Производные пирролотриазинона в качестве ингибиторов p13k
EA201201677A1 (ru) Производные гетероарилимидазолона в качестве ингибиторов jak
UA111744C2 (uk) ЗАМІЩЕНІ ПІРИДОПІРАЗИНИ ЯК ІНГІБІТОРИ Syk
MX340756B (es) Compuestos de quinazolina como inhibidores de serina/treonina quinasa.
EA201490471A1 (ru) Пиридазиноновые соединения и их применение в качестве ингибиторов daao
EA201491013A1 (ru) Пиразиновые ингибиторы киназы
EA201490643A1 (ru) Новые производные бетулиновой кислоты с противовирусной активностью
EA201590787A1 (ru) Замещенные пиридопиразины в качестве ингибиторов syk
EA201590656A1 (ru) Азаиндолины
TN2014000077A1 (en) Pyridazinone compounds and their use as daao inhibitors
UA111851C2 (uk) Сполуки піридазинону та їх використання як інгібіторів daao
GB201016442D0 (en) Novel acridine derivatives

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

PC4A Registration of transfer of a eurasian patent by assignment