PE20142244A1 - Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina - Google Patents

Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina

Info

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
Application number
PE2014001278A
Other languages
English (en)
Inventor
Roushan Afroze
Indu T Bharathan
Jeffrey P Ciavarri
Paul E Fleming
Jeffrey L Gaulin
Mario Girard
Steven P Langston
Francois R Soucy
Tzu-Tshin Wong
Yingchun Ye
Original Assignee
Millennium Pharm 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 Pharm Inc filed Critical Millennium Pharm Inc
Publication of PE20142244A1 publication Critical patent/PE20142244A1/es

Links

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)
  • 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

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.
PE2014001278A 2012-02-17 2013-02-14 Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina PE20142244A1 (es)

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) EP3536692B1 (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) SG11201404757WA (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 (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
EA201400831A1 (ru) 2014-12-30
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
CL2014002181A1 (es) 2014-12-12
TW201345909A (zh) 2013-11-16
EP2814791A4 (en) 2015-08-19

Similar Documents

Publication Publication Date Title
PE20142244A1 (es) Inhibidores de pirazolopirimidinilo de enzima activadora de ubiquitina
EA201891917A1 (ru) Бициклические гетероциклические производные в качестве ингибиторов irak4
PE20171057A1 (es) Derivados espirodiamina como inhibidores de la aldosterona sintasa
MX352672B (es) Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer.
EA201491012A1 (ru) Гетероциклические ингибиторы глютаминазы
CY1118478T1 (el) Παραγωγα τυπου αζαϊνδαζολιου ή διαζαϊνδαζολιου για τη θεραπεια του πονου
RS54030B1 (en) PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR CANCER TREATMENT
EA201300250A1 (ru) Оксадиазольные ингибиторы продуцирования лейкотриена
EA201201161A1 (ru) Пирролопиримидины в качестве ингибиторов cdk4/6
EA201391752A1 (ru) Спиро-[1,3]-оксазины и спиро-[1,4]-оксазепины в качестве ингибиторов bace1 и/или bace2
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201391670A1 (ru) 1,3-оксазины в качестве ингибиторов bace1 и/или bace2
CO6382125A2 (es) Inhibidores de proteína quinasa
EA201891553A1 (ru) Ингибиторы syk
MA37405A1 (fr) Composés hétérocyclyle
EA201391786A1 (ru) Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и/или bace2
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.
MX2015012427A (es) Compuestos de morfolinona de acido heteroarilo como inhibidores mdm2 para el tratamiento de cancer.
EA201500298A1 (ru) Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
EA201101583A1 (ru) Ингибиторы pi3 киназы или mtor
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201400333A1 (ru) Бензонитрильные производные в качестве ингибиторов киназ
EA201500544A1 (ru) НОВЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ АНТИБАКТЕРИАЛЬНЫХ АГЕНТОВ И ИНГИБИТОРОВ β-ЛАКТАМАЗ
EA201490493A1 (ru) Пирано[3,2-d][1,3]тиазол в качестве ингибиторов гликозидазы
EA201170508A1 (ru) Производные 1-амино-2-циклобутилэтилбороновой кислоты

Legal Events

Date Code Title Description
FG Grant, registration