CN104136399B - 泛素活化酶的吡唑并嘧啶基抑制剂 - Google Patents
泛素活化酶的吡唑并嘧啶基抑制剂 Download PDFInfo
- Publication number
- CN104136399B CN104136399B CN201380009784.8A CN201380009784A CN104136399B CN 104136399 B CN104136399 B CN 104136399B CN 201380009784 A CN201380009784 A CN 201380009784A CN 104136399 B CN104136399 B CN 104136399B
- Authority
- CN
- China
- Prior art keywords
- pyrimidin
- pyrazolo
- methyl ester
- acid
- sulfamic acid
- 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.)
- Active
Links
- 0 C[C@@]1C(*)CCC1 Chemical compound C[C@@]1C(*)CCC1 0.000 description 5
- GROMECASCUZHKX-UHFFFAOYSA-N C1C2(CC3)CC3CC1C2 Chemical compound C1C2(CC3)CC3CC1C2 GROMECASCUZHKX-UHFFFAOYSA-N 0.000 description 1
- OSLAYKKXCYSJSF-ARJAWSKDSA-N CC(/C=C(/C)\N)=O Chemical compound CC(/C=C(/C)\N)=O OSLAYKKXCYSJSF-ARJAWSKDSA-N 0.000 description 1
- ADMADJBQHMHCQB-BGZDPUMWSA-N CC(C)(C)O[C@@H]([C@@H](C[C@@H]1CO)N)[C@@H]1O Chemical compound CC(C)(C)O[C@@H]([C@@H](C[C@@H]1CO)N)[C@@H]1O ADMADJBQHMHCQB-BGZDPUMWSA-N 0.000 description 1
- SNWXZBSTQWKSIT-KPZMTGPNSA-N CC1C(Br)=NN2C(N[C@H]3[C@@H]4OC(C)(C)O[C@@H]4[C@@H](CO)C3)=CCN(C)C12 Chemical compound CC1C(Br)=NN2C(N[C@H]3[C@@H]4OC(C)(C)O[C@@H]4[C@@H](CO)C3)=CCN(C)C12 SNWXZBSTQWKSIT-KPZMTGPNSA-N 0.000 description 1
- QHRSESMSOJZMCO-UHFFFAOYSA-N Cc1cc(-c2ccccc2)n[nH]1 Chemical compound Cc1cc(-c2ccccc2)n[nH]1 QHRSESMSOJZMCO-UHFFFAOYSA-N 0.000 description 1
- YBVOOESZDWCLFS-UHFFFAOYSA-N Cc1nc2cc(-c3ccccc3)n[n]2c(Cl)c1 Chemical compound Cc1nc2cc(-c3ccccc3)n[n]2c(Cl)c1 YBVOOESZDWCLFS-UHFFFAOYSA-N 0.000 description 1
- GLRSPPKVJNWTGW-UHFFFAOYSA-N ClC1=CC=NC2=CC(Br)=NCCC12 Chemical compound ClC1=CC=NC2=CC(Br)=NCCC12 GLRSPPKVJNWTGW-UHFFFAOYSA-N 0.000 description 1
- HKCNOCAYCUVTEN-UHFFFAOYSA-N NC(N)=CC(c1ccccc1)=N Chemical compound NC(N)=CC(c1ccccc1)=N HKCNOCAYCUVTEN-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
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)
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 (2)
| Publication Number | Publication Date |
|---|---|
| CN104136399A CN104136399A (zh) | 2014-11-05 |
| CN104136399B true CN104136399B (zh) | 2018-08-07 |
Family
ID=48982730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380009784.8A Active CN104136399B (zh) | 2012-02-17 | 2013-02-14 | 泛素活化酶的吡唑并嘧啶基抑制剂 |
Country Status (30)
| Country | Link |
|---|---|
| US (4) | US9290500B2 (https=) |
| EP (3) | EP3536692B1 (https=) |
| JP (1) | JP6122877B2 (https=) |
| KR (1) | KR20140123104A (https=) |
| CN (1) | CN104136399B (https=) |
| AR (1) | AR092797A1 (https=) |
| BR (1) | BR112014020365B1 (https=) |
| CA (1) | CA2864672C (https=) |
| CL (1) | CL2014002181A1 (https=) |
| CO (1) | CO7071135A2 (https=) |
| CR (1) | CR20140380A (https=) |
| DO (1) | DOP2014000187A (https=) |
| EA (1) | EA035020B1 (https=) |
| EC (1) | ECSP14019113A (https=) |
| ES (1) | ES2739150T3 (https=) |
| GE (1) | GEP201706687B (https=) |
| HK (1) | HK1201817A1 (https=) |
| IL (1) | IL234016A0 (https=) |
| MA (1) | MA35932B1 (https=) |
| MX (1) | MX352963B (https=) |
| NZ (1) | NZ628969A (https=) |
| PE (1) | PE20142244A1 (https=) |
| PH (1) | PH12014501832A1 (https=) |
| SG (2) | SG10201606581RA (https=) |
| TN (1) | TN2014000351A1 (https=) |
| TW (1) | TWI593688B (https=) |
| UA (1) | UA116534C2 (https=) |
| UY (1) | UY34629A (https=) |
| WO (1) | WO2013123169A1 (https=) |
| ZA (1) | ZA201406103B (https=) |
Families Citing this family (10)
| 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)
| 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 |
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2013
- 2013-02-14 CN CN201380009784.8A patent/CN104136399B/zh active Active
- 2013-02-14 SG SG10201606581RA patent/SG10201606581RA/en unknown
- 2013-02-14 KR KR1020147025556A patent/KR20140123104A/ko not_active Ceased
- 2013-02-14 CA CA2864672A patent/CA2864672C/en active Active
- 2013-02-14 BR BR112014020365-2A patent/BR112014020365B1/pt not_active IP Right Cessation
- 2013-02-14 WO PCT/US2013/026113 patent/WO2013123169A1/en not_active Ceased
- 2013-02-14 ES ES16205139T patent/ES2739150T3/es active Active
- 2013-02-14 EP EP19170607.6A patent/EP3536692B1/en active Active
- 2013-02-14 GE GEAP201313560A patent/GEP201706687B/en unknown
- 2013-02-14 HK HK15102227.4A patent/HK1201817A1/xx unknown
- 2013-02-14 EP EP13748707.0A patent/EP2814791A4/en not_active Withdrawn
- 2013-02-14 EA EA201400831A patent/EA035020B1/ru not_active IP Right Cessation
- 2013-02-14 MX MX2014009944A patent/MX352963B/es active IP Right Grant
- 2013-02-14 NZ NZ628969A patent/NZ628969A/en not_active IP Right Cessation
- 2013-02-14 US US13/767,314 patent/US9290500B2/en active Active
- 2013-02-14 JP JP2014557765A patent/JP6122877B2/ja not_active Expired - Fee Related
- 2013-02-14 EP EP16205139.5A patent/EP3173413B1/en active Active
- 2013-02-14 PE PE2014001278A patent/PE20142244A1/es active IP Right Grant
- 2013-02-14 UA UAA201409297A patent/UA116534C2/uk unknown
- 2013-02-14 SG SG11201404757WA patent/SG11201404757WA/en unknown
- 2013-02-15 AR ARP130100480A patent/AR092797A1/es unknown
- 2013-02-15 UY UY0001034629A patent/UY34629A/es not_active Application Discontinuation
- 2013-02-18 TW TW102105676A patent/TWI593688B/zh not_active IP Right Cessation
-
2014
- 2014-08-07 IL IL234016A patent/IL234016A0/en unknown
- 2014-08-11 TN TNP2014000351A patent/TN2014000351A1/fr unknown
- 2014-08-12 CR CR20140380A patent/CR20140380A/es unknown
- 2014-08-13 PH PH12014501832A patent/PH12014501832A1/en unknown
- 2014-08-14 CL CL2014002181A patent/CL2014002181A1/es unknown
- 2014-08-15 DO DO2014000187A patent/DOP2014000187A/es unknown
- 2014-08-20 ZA ZA2014/06103A patent/ZA201406103B/en unknown
- 2014-09-10 MA MA37338A patent/MA35932B1/fr unknown
- 2014-09-16 CO CO14205517A patent/CO7071135A2/es unknown
- 2014-09-17 EC ECIEPI201419113A patent/ECSP14019113A/es unknown
-
2016
- 2016-02-19 US US15/048,007 patent/US9663525B2/en active Active
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2017
- 2017-04-17 US US15/488,800 patent/US9796725B2/en active Active
- 2017-09-08 US US15/699,818 patent/US10202389B2/en active Active
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20211110 Address after: Osaka, Japan Patentee after: Takeda Pharmaceutical Industry Co., Ltd Address before: Massachusetts, USA Patentee before: Millenum pharmaceuticals |