PE20142244A1 - Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina - Google Patents
Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitinaInfo
- Publication number
- PE20142244A1 PE20142244A1 PE2014001278A PE2014001278A PE20142244A1 PE 20142244 A1 PE20142244 A1 PE 20142244A1 PE 2014001278 A PE2014001278 A PE 2014001278A PE 2014001278 A PE2014001278 A PE 2014001278A PE 20142244 A1 PE20142244 A1 PE 20142244A1
- Authority
- PE
- Peru
- Prior art keywords
- activating enzyme
- compound
- ubiquitin activating
- sulfamate
- rac
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- -1 PYRAZOLOPYRIMIDINYL Chemical class 0.000 title 1
- 102000018478 Ubiquitin-Activating Enzymes Human genes 0.000 title 1
- 108010091546 Ubiquitin-Activating Enzymes Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- IIACRCGMVDHOTQ-UHFFFAOYSA-N sulfamic acid Chemical compound NS(O)(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-N 0.000 abstract 2
- WITMXBRCQWOZPX-UHFFFAOYSA-N 1-phenylpyrazole Chemical compound C1=CC=NN1C1=CC=CC=C1 WITMXBRCQWOZPX-UHFFFAOYSA-N 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000044159 Ubiquitin Human genes 0.000 abstract 1
- 108090000848 Ubiquitin Proteins 0.000 abstract 1
- 230000003213 activating effect Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical group C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 abstract 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
- 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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA I O UNA SAL FARMACEUTICAMENTE ACEPTABLE, DONDE: W ES -N(R*3)-; R*3 ES H, ALQUILO C1-C3; Y ES UN COMPUESTO DE FORMULA II, DONDE: RY1, RY2 Y RY3 SON H, HALO, ALIFATICO C1-C3, ENTRE OTROS; Z ES ARILO OPCIONALMENTE SUSTITUIDO, ARILO FUSIONADO, HETEROARILO, ENTRE OTROS; SON COMPUESTOS PREFERIDOS: (RAC)-REL-SULFAMATO DE ((1R,2R,3S,4R)-2,3-DIHIDROXI-4-(2-FENILPIRAZOLO[1,5-A]PIRIMIDIN-7-ILAMINO)CICLOPENTIL)METILO; (RAC)-REL-SULFAMATO DE ((1R,2R,3S,4R)-4-(2-(BIFENIL-3-IL)PIRAZOLO[1,5-A]PIRIMIDIN-7-ILAMINO)-2,3-DIHIDROXICICLOPENTIL)METILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE LA ENZIMA ACTIVADORA DE UBIQUITINA (UAE). UTIL EN EL TRATAMIENTO DEL CANCER.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261600070P | 2012-02-17 | 2012-02-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20142244A1 true PE20142244A1 (es) | 2015-01-07 |
Family
ID=48982730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2014001278A PE20142244A1 (es) | 2012-02-17 | 2013-02-14 | Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina |
Country Status (30)
| Country | Link |
|---|---|
| US (4) | US9290500B2 (es) |
| EP (3) | EP2814791A4 (es) |
| JP (1) | JP6122877B2 (es) |
| KR (1) | KR20140123104A (es) |
| CN (1) | CN104136399B (es) |
| AR (1) | AR092797A1 (es) |
| BR (1) | BR112014020365B1 (es) |
| CA (1) | CA2864672C (es) |
| CL (1) | CL2014002181A1 (es) |
| CO (1) | CO7071135A2 (es) |
| CR (1) | CR20140380A (es) |
| DO (1) | DOP2014000187A (es) |
| EA (1) | EA035020B1 (es) |
| EC (1) | ECSP14019113A (es) |
| ES (1) | ES2739150T3 (es) |
| GE (1) | GEP201706687B (es) |
| HK (1) | HK1201817A1 (es) |
| IL (1) | IL234016A0 (es) |
| MA (1) | MA35932B1 (es) |
| MX (1) | MX352963B (es) |
| NZ (1) | NZ628969A (es) |
| PE (1) | PE20142244A1 (es) |
| PH (1) | PH12014501832A1 (es) |
| SG (2) | SG10201606581RA (es) |
| TN (1) | TN2014000351A1 (es) |
| TW (1) | TWI593688B (es) |
| UA (1) | UA116534C2 (es) |
| UY (1) | UY34629A (es) |
| WO (1) | WO2013123169A1 (es) |
| ZA (1) | ZA201406103B (es) |
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 |
| UA116534C2 (uk) | 2012-02-17 | 2018-04-10 | Мілленніум Фармасьютікалз, Інк. | Піразолопіримідинілові інгібітори убіквітинактивуючого ферменту |
| CN104684559A (zh) | 2012-08-03 | 2015-06-03 | 米伦纽姆医药公司 | 针对Uba6的吲哚取代的吡咯并嘧啶基抑制剂 |
| EP3016934B1 (en) | 2013-07-02 | 2018-01-10 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as inhibitors of sumo activating enzyme |
| MX376054B (es) | 2014-07-01 | 2025-03-07 | Takeda Pharmaceuticals Co | Compuestos de heteroarilo utiles como inhibidores de enzima activadora de sumo. |
| EP3212650B1 (en) * | 2014-10-29 | 2021-02-17 | 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 |
| MA54092A (fr) | 2018-10-30 | 2021-09-08 | Kronos Bio Inc | Composés, compositions et procédés de modulation de l'activité de cdk9 |
| 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 |
|---|---|---|---|---|
| WO2003073989A2 (en) | 2002-02-28 | 2003-09-12 | Biota, Inc. | Nucleoside 5'-monophosphate mimics and their prodrugs |
| 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 |
| US7196092B2 (en) | 2002-09-04 | 2007-03-27 | Schering Corporation | N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| 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 |
| 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 |
| 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 |
| EP1758873A1 (en) | 2004-06-22 | 2007-03-07 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| SI1848718T1 (sl) | 2005-02-04 | 2012-12-31 | Millennium Pharmaceuticals, Inc. | Inhibitorji E1 aktivacijskih enzimov |
| AR055206A1 (es) | 2005-10-06 | 2007-08-08 | Schering Corp | Pirazolo[1, 5 - a]pirimidinas como inhibidoras de proteina quinasa, composiciones farmaceuticas y combinaciones con agentes citostaticos que las comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer. |
| SI1989206T1 (sl) * | 2006-02-02 | 2012-11-30 | Millennium Pharm Inc | Inhibitorji e aktivirajočih enzimov |
| WO2007099021A1 (en) * | 2006-02-28 | 2007-09-07 | Sez Ag | Device and method for liquid treating disc-like articles |
| KR20150036358A (ko) * | 2006-08-08 | 2015-04-07 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｅ１ 활성화 효소의 억제제로서 유용한 헤테로아릴 화합물 |
| US8008307B2 (en) | 2006-08-08 | 2011-08-30 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as inhibitors of E1 activating enzymes |
| CA2691987C (en) | 2007-06-12 | 2016-08-16 | Achaogen, Inc. | Antibacterial agents |
| TW201434851A (zh) * | 2007-08-02 | 2014-09-16 | Millennium Pharm Inc | 合成ｅ１活化酶抑制劑之方法 |
| WO2009082691A1 (en) | 2007-12-21 | 2009-07-02 | 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 |
| WO2010132110A1 (en) | 2009-05-14 | 2010-11-18 | Millennium Pharmaceuticals, 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 |
| US8809356B2 (en) | 2011-08-24 | 2014-08-19 | Millennium Pharmaceuticals, Inc. | Inhibitors of NEDD8-activating enzyme |
| UA116534C2 (uk) | 2012-02-17 | 2018-04-10 | Мілленніум Фармасьютікалз, Інк. | Піразолопіримідинілові інгібітори убіквітинактивуючого ферменту |
| CN104684559A (zh) | 2012-08-03 | 2015-06-03 | 米伦纽姆医药公司 | 针对Uba6的吲哚取代的吡咯并嘧啶基抑制剂 |
| EP3016934B1 (en) | 2013-07-02 | 2018-01-10 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as inhibitors of sumo activating enzyme |
| MX376054B (es) | 2014-07-01 | 2025-03-07 | Takeda Pharmaceuticals Co | Compuestos de heteroarilo utiles como inhibidores de enzima activadora de sumo. |
-
2013
- 2013-02-14 UA UAA201409297A patent/UA116534C2/uk unknown
- 2013-02-14 CA CA2864672A patent/CA2864672C/en active Active
- 2013-02-14 JP JP2014557765A patent/JP6122877B2/ja not_active Expired - Fee Related
- 2013-02-14 SG SG10201606581RA patent/SG10201606581RA/en unknown
- 2013-02-14 EP EP13748707.0A patent/EP2814791A4/en not_active Withdrawn
- 2013-02-14 KR KR1020147025556A patent/KR20140123104A/ko not_active Ceased
- 2013-02-14 BR BR112014020365-2A patent/BR112014020365B1/pt not_active IP Right Cessation
- 2013-02-14 MX MX2014009944A patent/MX352963B/es active IP Right Grant
- 2013-02-14 EP EP16205139.5A patent/EP3173413B1/en active Active
- 2013-02-14 US US13/767,314 patent/US9290500B2/en active Active
- 2013-02-14 CN CN201380009784.8A patent/CN104136399B/zh active Active
- 2013-02-14 EA EA201400831A patent/EA035020B1/ru not_active IP Right Cessation
- 2013-02-14 SG SG11201404757WA patent/SG11201404757WA/en unknown
- 2013-02-14 GE GEAP201313560A patent/GEP201706687B/en unknown
- 2013-02-14 NZ NZ628969A patent/NZ628969A/en not_active IP Right Cessation
- 2013-02-14 EP EP19170607.6A patent/EP3536692B1/en active Active
- 2013-02-14 HK HK15102227.4A patent/HK1201817A1/xx unknown
- 2013-02-14 PE PE2014001278A patent/PE20142244A1/es active IP Right Grant
- 2013-02-14 WO PCT/US2013/026113 patent/WO2013123169A1/en not_active Ceased
- 2013-02-14 ES ES16205139T patent/ES2739150T3/es active Active
- 2013-02-15 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
-
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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20142244A1 (es) | Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina | |
| EA201691428A1 (ru) | Бициклические гетероциклические производные в качестве ингибиторов irak4 | |
| EA201300250A1 (ru) | Оксадиазольные ингибиторы продуцирования лейкотриена | |
| MX352672B (es) | Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer. | |
| EA201491012A1 (ru) | Гетероциклические ингибиторы глютаминазы | |
| PE20171057A1 (es) | Derivados espirodiamina como inhibidores de la aldosterona sintasa | |
| EA201201161A1 (ru) | Пирролопиримидины в качестве ингибиторов cdk4/6 | |
| EA201290980A1 (ru) | Производные 1-амино-2-циклопропилэтилбороновой кислоты | |
| EA201391752A1 (ru) | Спиро-[1,3]-оксазины и спиро-[1,4]-оксазепины в качестве ингибиторов bace1 и/или bace2 | |
| EA201391670A1 (ru) | 1,3-оксазины в качестве ингибиторов bace1 и/или bace2 | |
| CO6382125A2 (es) | Inhibidores de proteína quinasa | |
| EA201500298A1 (ru) | Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы | |
| MA37405A1 (fr) | Composés hétérocyclyle | |
| EA201891553A1 (ru) | Ингибиторы syk | |
| EA201101583A1 (ru) | Ингибиторы pi3 киназы или mtor | |
| CY1118478T1 (el) | Παραγωγα τυπου αζαϊνδαζολιου ή διαζαϊνδαζολιου για τη θεραπεια του πονου | |
| EA201400412A1 (ru) | ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ | |
| AR050952A1 (es) | Derivados de indazolona; procesos para su obtencion; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la enzima 11beta - hsd1. | |
| EA201400333A1 (ru) | Бензонитрильные производные в качестве ингибиторов киназ | |
| EA201291356A1 (ru) | Пиперидиноновые производные как ингибиторы mdm2 для лечения рака | |
| EA201500544A1 (ru) | НОВЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ АНТИБАКТЕРИАЛЬНЫХ АГЕНТОВ И ИНГИБИТОРОВ β-ЛАКТАМАЗ | |
| EA201170508A1 (ru) | Производные 1-амино-2-циклобутилэтилбороновой кислоты | |
| MX2016006336A (es) | Compuestos pirazolopirimidina. | |
| EA201370166A1 (ru) | Содержащие диарилацетиленгидразид ингибиторы тирозинкиназы | |
| EA201490493A1 (ru) | Пирано[3,2-d][1,3]тиазол в качестве ингибиторов гликозидазы |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |