JP6122877B2 - ユビキチン活性化酵素のピラゾロピリミジニル阻害剤 - Google Patents

ユビキチン活性化酵素のピラゾロピリミジニル阻害剤 Download PDF

Info

Publication number
JP6122877B2
JP6122877B2 JP2014557765A JP2014557765A JP6122877B2 JP 6122877 B2 JP6122877 B2 JP 6122877B2 JP 2014557765 A JP2014557765 A JP 2014557765A JP 2014557765 A JP2014557765 A JP 2014557765A JP 6122877 B2 JP6122877 B2 JP 6122877B2
Authority
JP
Japan
Prior art keywords
halo
aliphatic
compound
pharmaceutically acceptable
acceptable salt
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.)
Expired - Fee Related
Application number
JP2014557765A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015508775A5 (enExample
JP2015508775A (ja
Inventor
ローシャン アフローゼ,
ローシャン アフローゼ,
インドゥ ティー. バラサン,
インドゥ ティー. バラサン,
ジェフェリー ピー. チャバリ,
ジェフェリー ピー. チャバリ,
ポール イー. フレミング,
ポール イー. フレミング,
ジェフェリー エル. ゴーリン,
ジェフェリー エル. ゴーリン,
マリオ ジラード,
マリオ ジラード,
スティーブン ピー. ラングストン,
スティーブン ピー. ラングストン,
フランソワ アール. ソーシー,
フランソワ アール. ソーシー,
ツ−チン ウォン,
ツ−チン ウォン,
インチュン イエ,
インチュン イエ,
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.)
Millennium Pharmaceuticals Inc
Original Assignee
Millennium Pharmaceuticals Inc
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 Millennium Pharmaceuticals Inc filed Critical Millennium Pharmaceuticals Inc
Publication of JP2015508775A publication Critical patent/JP2015508775A/ja
Publication of JP2015508775A5 publication Critical patent/JP2015508775A5/ja
Application granted granted Critical
Publication of JP6122877B2 publication Critical patent/JP6122877B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2014557765A 2012-02-17 2013-02-14 ユビキチン活性化酵素のピラゾロピリミジニル阻害剤 Expired - Fee Related JP6122877B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261600070P 2012-02-17 2012-02-17
US61/600,070 2012-02-17
PCT/US2013/026113 WO2013123169A1 (en) 2012-02-17 2013-02-14 Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme

Publications (3)

Publication Number Publication Date
JP2015508775A JP2015508775A (ja) 2015-03-23
JP2015508775A5 JP2015508775A5 (enExample) 2017-03-16
JP6122877B2 true JP6122877B2 (ja) 2017-04-26

Family

ID=48982730

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014557765A Expired - Fee Related JP6122877B2 (ja) 2012-02-17 2013-02-14 ユビキチン活性化酵素のピラゾロピリミジニル阻害剤

Country Status (30)

Country Link
US (4) US9290500B2 (enExample)
EP (3) EP3536692B1 (enExample)
JP (1) JP6122877B2 (enExample)
KR (1) KR20140123104A (enExample)
CN (1) CN104136399B (enExample)
AR (1) AR092797A1 (enExample)
BR (1) BR112014020365B1 (enExample)
CA (1) CA2864672C (enExample)
CL (1) CL2014002181A1 (enExample)
CO (1) CO7071135A2 (enExample)
CR (1) CR20140380A (enExample)
DO (1) DOP2014000187A (enExample)
EA (1) EA035020B1 (enExample)
EC (1) ECSP14019113A (enExample)
ES (1) ES2739150T3 (enExample)
GE (1) GEP201706687B (enExample)
HK (1) HK1201817A1 (enExample)
IL (1) IL234016A0 (enExample)
MA (1) MA35932B1 (enExample)
MX (1) MX352963B (enExample)
NZ (1) NZ628969A (enExample)
PE (1) PE20142244A1 (enExample)
PH (1) PH12014501832A1 (enExample)
SG (2) SG10201606581RA (enExample)
TN (1) TN2014000351A1 (enExample)
TW (1) TWI593688B (enExample)
UA (1) UA116534C2 (enExample)
UY (1) UY34629A (enExample)
WO (1) WO2013123169A1 (enExample)
ZA (1) ZA201406103B (enExample)

Families Citing this family (10)

* 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
CN104136399B (zh) 2012-02-17 2018-08-07 米伦纽姆医药公司 泛素活化酶的吡唑并嘧啶基抑制剂
JP2015524442A (ja) 2012-08-03 2015-08-24 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. Uba6のインドール置換ピロロピリミジニル阻害剤
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
BR112016030787B1 (pt) 2014-07-01 2022-12-20 Takeda Pharmaceutical Company Limited Entidade química, composição farmacêutica e seu uso
TW201628621A (zh) 2014-10-29 2016-08-16 千禧製藥公司 泛素活化酶抑制劑及輻射之施用
US20180133221A1 (en) * 2014-10-29 2018-05-17 Millennium Pharmaceuticals, Inc. Administration of ubiquitin-activating enzyme inhibitor and chemotherapeutic agents
US11155560B2 (en) 2018-10-30 2021-10-26 Kronos Bio, Inc. Substituted pyrazolo[1,5-a]pyrimidines for modulating CDK9 activity
CN117412973A (zh) * 2021-05-31 2024-01-16 上海瑛派药业有限公司 含氮稠合杂芳双环化合物作为usp1抑制剂及其应用
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
JP2005524662A (ja) 2002-02-28 2005-08-18 ビオタ インコーポレーティッド ヌクレオシド5’−一リン酸模倣物およびこれらのプロドラッグ
DE60313872T2 (de) 2002-09-04 2008-01-17 Schering Corp. Pyrazoloä1,5-aüpyrimidine als hemmstoffe cyclin-abhängiger kinasen
ES2285164T3 (es) 2002-09-04 2007-11-16 Schering Corporation Pirazolopirimidinas como inhibidores de quinasas dependientes de ciclina.
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7196092B2 (en) 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
US20070179161A1 (en) 2003-03-31 2007-08-02 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
EP1680431A1 (en) 2003-10-17 2006-07-19 Rigel Pharmaceuticals, Inc. Benzothiazole and thiazole'5,5-b!pyridine compositions and their use as ubiquitin ligase inhibitors
US20050282818A1 (en) 2004-06-22 2005-12-22 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
PT1848718E (pt) 2005-02-04 2012-10-11 Millennium Pharm Inc Inibidores de enzimas de activação e1
CN101321759A (zh) 2005-10-06 2008-12-10 先灵公司 作为蛋白激酶抑制剂的吡唑并嘧啶化合物
KR101450535B1 (ko) 2006-02-02 2014-10-14 밀레니엄 파머슈티컬스 인코퍼레이티드 E1 활성화 효소의 억제제
WO2007099021A1 (en) * 2006-02-28 2007-09-07 Sez Ag Device and method for liquid treating disc-like articles
US8008307B2 (en) 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
EA201501088A1 (ru) * 2006-08-08 2017-01-30 Миллениум Фармасьютикалз, Инк. Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов
TWI519508B (zh) 2007-06-12 2016-02-01 Achaogen Inc 抗菌劑
WO2009042013A1 (en) 2007-08-02 2009-04-02 Millennium Pharmaceuticals, Inc. Process for the synthesis of e1 activating enzyme inhibitors
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
SG175929A1 (en) 2009-05-14 2011-12-29 Millennium Pharm Inc Hydrochloride salt of ((1s,2s,4r)-4-{4-[(1s)-2,3-dihydro-1h-inden-1-ylamino]-7h-pyrrolo [2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulfamate
JP5879273B2 (ja) 2010-03-01 2016-03-08 ジーティーエックス・インコーポレイテッド 癌を処置するための化合物
US20120077814A1 (en) 2010-09-10 2012-03-29 Zhong Wang Sulfonamide, sulfamate, and sulfamothioate derivatives
SG11201400102WA (en) 2011-08-24 2014-03-28 Millennium Pharm Inc Inhibitors of nedd8-activating enzyme
CN104136399B (zh) 2012-02-17 2018-08-07 米伦纽姆医药公司 泛素活化酶的吡唑并嘧啶基抑制剂
JP2015524442A (ja) 2012-08-03 2015-08-24 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. Uba6のインドール置換ピロロピリミジニル阻害剤
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
BR112016030787B1 (pt) 2014-07-01 2022-12-20 Takeda Pharmaceutical Company Limited Entidade química, composição farmacêutica e seu uso

Also Published As

Publication number Publication date
US9290500B2 (en) 2016-03-22
US20170217968A1 (en) 2017-08-03
SG10201606581RA (en) 2016-09-29
US20130217682A1 (en) 2013-08-22
KR20140123104A (ko) 2014-10-21
IL234016A0 (en) 2014-09-30
SG11201404757WA (en) 2014-09-26
GEP201706687B (en) 2017-06-26
HK1201817A1 (en) 2015-09-11
ECSP14019113A (es) 2015-09-30
WO2013123169A1 (en) 2013-08-22
US9796725B2 (en) 2017-10-24
PE20142244A1 (es) 2015-01-07
EP2814791A4 (en) 2015-08-19
US20160244455A1 (en) 2016-08-25
TW201345909A (zh) 2013-11-16
BR112014020365B1 (pt) 2023-02-23
EA201400831A1 (ru) 2014-12-30
AR092797A1 (es) 2015-05-06
ZA201406103B (en) 2017-11-29
CA2864672C (en) 2018-01-09
MX2014009944A (es) 2014-11-10
PH12014501832A1 (en) 2014-11-17
US20170369499A1 (en) 2017-12-28
US10202389B2 (en) 2019-02-12
CR20140380A (es) 2014-10-28
TWI593688B (zh) 2017-08-01
ES2739150T3 (es) 2020-01-29
EP2814791A1 (en) 2014-12-24
EP3173413A1 (en) 2017-05-31
MX352963B (es) 2017-12-15
UY34629A (es) 2013-09-02
EP3536692A1 (en) 2019-09-11
EP3173413B1 (en) 2019-05-01
CN104136399B (zh) 2018-08-07
DOP2014000187A (es) 2014-10-15
NZ628969A (en) 2017-03-31
CL2014002181A1 (es) 2014-12-12
TN2014000351A1 (en) 2015-12-21
CO7071135A2 (es) 2014-09-30
BR112014020365A2 (pt) 2020-12-22
CA2864672A1 (en) 2013-08-22
CN104136399A (zh) 2014-11-05
US20140088096A9 (en) 2014-03-27
EP3536692B1 (en) 2021-04-07
EA035020B1 (ru) 2020-04-17
MA35932B1 (fr) 2014-12-01
UA116534C2 (uk) 2018-04-10
JP2015508775A (ja) 2015-03-23
US9663525B2 (en) 2017-05-30

Similar Documents

Publication Publication Date Title
JP6122877B2 (ja) ユビキチン活性化酵素のピラゾロピリミジニル阻害剤
TWI798635B (zh) 吡啶並嘧啶酮類化合物及其應用
JP2015508775A5 (enExample)
EP2382207B1 (en) Pi3k/mtor kinase inhibitors
JP2022078315A (ja) Mk2阻害剤およびその使用
TW202509040A (zh) 三環類化合物及其用途
TWI580679B (zh) 雜芳基並嘧啶類衍生物、其製備方法和用途
EP2483272A2 (en) Pi3k (delta) selective inhibitors
EP3398947A1 (en) Nitrogen-containing fused heterocyclic compound, as well as preparation method, intermediate, composition and application thereof
JP6118890B2 (ja) 癌の治療のための6−(4−(1−アミノ−3−ヒドロキシシクロブチル)フェニル)−5−フェニル−(フロ、チエノ、又はピロロ)[2,3−d]ピリミジン−4−オン誘導体
CN114369097B (zh) 杂芳环类AhR抑制剂
HK1238244A1 (en) Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
HK1222388B (en) Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
HK1222388A1 (en) Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160212

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160212

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20160818

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160913

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20161208

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20170210

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20170303

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20170403

R150 Certificate of patent or registration of utility model

Ref document number: 6122877

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees