AR092797A1 - Inhibidores de pirazolopirimidinilo de enzima activadora de ubicuitina - Google Patents
Inhibidores de pirazolopirimidinilo de enzima activadora de ubicuitinaInfo
- Publication number
- AR092797A1 AR092797A1 ARP130100480A ARP130100480A AR092797A1 AR 092797 A1 AR092797 A1 AR 092797A1 AR P130100480 A ARP130100480 A AR P130100480A AR P130100480 A ARP130100480 A AR P130100480A AR 092797 A1 AR092797 A1 AR 092797A1
- Authority
- AR
- Argentina
- Prior art keywords
- case
- independently
- alkyl
- halo
- formula
- Prior art date
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
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- 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)
- 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
Las entidades químicas útiles para tratar trastornos, particularmente trastornos de proliferación celular, incluidos cánceres. Reivindicación 1: Una entidad química que comprende un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: W es -N(R*³)-; Y es un compuesto de formula (2); cada uno de RY¹, RY² y RY³ se selecciona independientemente de -H, (a) halo, (b1) alifático C₁₋₃, (b2) R#²⁻¹, (c) -OR*³, (d) -N(R*³)₂, (e) -SR⁺³, (f) haloalquilo C₁₋₂ y (g) haloalcoxi C₁₋₂; Z es [1] arilo opcionalmente sustituido: de la formula (3), en donde el anillo Ar representa el grupo arilo; [2] arilo fusionado opcionalmente sustituido: de la formula (4), en donde el anillo Ar representa el grupo arilo, y el anillo Cyc/Het representa el carbociclo o heterociclo; [3] heteroarilo opcionalmente sustituido: de la formula (5), en donde el anillo HetAr representa el grupo heteroarilo; o [4] un compuesto de formula (6), en donde X⁴ es -O-, -N(R*³)-, -S- o -C(O)-; y cada uno de n1 y n2 es independientemente 0, 1 ó 2, siempre que n1 + n2 = 0, 1 ó 2; cada caso de RS¹ se selecciona independientemente de -H, (a) halo, (c) -OR*², (d) -N(R*²)₂ y (e) -SR⁺²; cada caso de RS² se selecciona independientemente de -H, (a) halo, (c) -OR*⁴, (d) -N(R*⁴)₂, (e) -SR⁺⁴, (h) -NO₂, (i) -CN, (j) -C(O)-R⁺⁴, (k) -C(O)-OR*⁴, (l) -C(O)-N(R*⁴)₂, (m) -O-C(O)-R⁺⁴, (n) -N(R*⁴)-C(O)-R⁺⁴, (o) -O-C(O)-OR*⁴, (p) -O-C(O)-N(R*⁴)₂, (q) -N(R*⁴)-C(O)-OR*⁴ y (r) -N(R*⁴)-C(O)-N(R*⁴)₂; cada caso de RS⁴ se selecciona independientemente de -H, (a) halo, (b1) alifático C₁₋₄, (b2) R#⁴⁻², (c) -OR*⁴, (d) -N(R*⁴)₂ y (e) -SR⁺⁴; cada caso de RS⁵ se selecciona independientemente de -H, (a) halo, (b1) alifático C₁₋₄, (b2) R^⁴⁻², (c) -OR*⁴, (d) -N(R*⁴)₂, (e) -SR⁺⁴, (f) haloalquilo C₁₋₃, (h) -NO₂, (i) -CN, (j) -C(O)-R⁺⁴, (k) -C(O)-OR*⁴, (l) -C(O)-N(R*⁴)₂, (m) -O-C(O)-R⁺⁴, (n) -N(R*⁴)-C(O)-R⁺⁴, (o) -O-C(O)-OR*⁴, (p) -O-C(O)-N(R*⁴)₂, (q) -N(R*⁴)-C(O)-OR*⁴ y (r) -N(R*⁴)-C(O)-N(R*⁴)₂; cada caso de RS⁷ se selecciona independientemente de -H, (a) halo, (b1) alifático C₁₋₄, (b2) R#⁴⁻², (c) -OR*⁴, (d) -N(R*⁴)₂ y (e) -SR⁺⁴; cada caso de RS⁸ se selecciona independientemente de -H, (a) halo, (b1) alifático C₁₋₄, (b2) R^⁴⁻², (c) OR*⁴, (d) -N(R*⁴)₂, (e) -SR⁺⁴, (f) haloalquilo C₁₋₃, (g1) haloalcoxi C₁₋₃, (g2) haloalquiltio C₁₋₃, (h) -NO₂, (i) -CN, (j) -C(O)-R⁺⁴, (k) -C(O)-OR*⁴, (l) -C(O)-N(R*⁴)₂, (m) -O-C(O)-R⁺⁴, (n) -N(R*⁴)-C(O)-R⁺⁴, (o) -O-C(O)-OR*⁴, (p) -O-C(O)-N(R*⁴)₂, (q) -N(R*⁴)-C(O)-OR*⁴ y (r) -N(R*⁴)-C(O)-N(R*⁴)₂; cada caso de RS⁹ se selecciona independientemente de -H, (a) halo, (b1) alifático C₁₋₆, (b2) R^⁶⁻³, (c) -OR*⁶, (d) -N(R*⁶)₂, (e) -SR⁺⁶, (f) haloalquilo C₁₋₃, (g1) haloalcoxi C₁₋₃, (g2) haloalquiltio C₁₋₃, (h) -NO₂, (i) -CN, (j) -C(O)-R⁺⁶, (k) -C(O)-OR*⁶, (l) -C(O)-N(R*⁶)₂, (m) -O-C(O)-R⁺⁶, (n) -N(R*⁶)-C(O)-R⁺⁶, (o) -O-C(O)-OR*⁶, (p) -O-C(O)-N(R*⁶)₂ (q) -N(R*⁶)-C(O)-OR*⁶, (r) -N(R*⁶)-C(O)-N(R*⁶)₂, (s) -Si(R⁺²)₃, (aa) carbociclilo C₃₋₈, (bb) -A-(carbociclilo C₃₋₈), (cc) heterociclilo de 5 a 10 miembros, (dd) -A-(heterociclilo de 5 a 10 miembros), (ee) arilo C₆₋₁₀, (ff) -A-(arilo C₆₋₁₀), (gg) heteroarilo de 5 a 10 miembros y (hh) -A-(heteroarilo de 5 a 10 miembros); en donde cada caso de A se selecciona independientemente de alquileno C₁₋₃, heteroalquileno C₀₋₃, -O-, -S-, -N(R*¹)- y -C(O)-; y en donde cada uno de (aa) - (dd) se sustituye opcionalmente por 1 - 3 grupos seleccionados independientemente de (a) halo, (b1) alifático C₁₋₂, (b2) R#²⁻¹, (c) -OR*², (d) -N(R*²)₂ y (e) -SR⁺²; y en donde cada uno de (ee) - (hh) se sustituye opcionalmente por 1 - 3 grupos seleccionados independientemente de (a) halo, (b1) alifático C₁₋₄, (b2) R#⁴⁻², (c) -OR*⁴, (d) -N(R*⁴)₂ y (e) -SR⁺⁴; cada caso de R*⁶ es independientemente -H o alquilo C₁₋₆; cada caso de R*⁴ es independientemente -H o alquilo C₁₋₄; cada caso de R*³ es independientemente -H o alquilo C₁₋₃; cada caso de R*² es independientemente -H o alquilo C₁₋₂; cada caso de R*¹ es independientemente -H o metilo; casa caso de R⁺⁶ es independientemente alquilo C₁₋₆; casa caso de R⁺⁴ es independientemente alquilo C₁₋₄; casa caso de R⁺³ es independientemente alquilo C₁₋₃; casa caso de R⁺² es independientemente alquilo C₁₋₂; cada caso de R^⁶⁻³ es independientemente un resto de fórmula (7), en donde Alk representa alquilo C₁₋₆; y cada uno de m1, m2 y m3 es independientemente 0 ó 1; cada caso de R^⁴⁻² es independientemente un resto de fórmula (8), en donde Alk representa alquilo C₁₋₄; y cada uno de m1 y m2 es independientemente 0 ó 1; cada caso de R#⁴⁻² es independientemente un resto de fórmula (9), en donde Alk representa alquilo C₁₋₄; y cada uno de m1 y m2 es independientemente 0 ó 1; y cada caso de R#²⁻¹ es independientemente un resto de fórmula (10), en donde Alk representa alquilo C₁₋₂; y m1 es 0 ó 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261600070P | 2012-02-17 | 2012-02-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092797A1 true AR092797A1 (es) | 2015-05-06 |
Family
ID=48982730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130100480A AR092797A1 (es) | 2012-02-17 | 2013-02-15 | Inhibidores de pirazolopirimidinilo de enzima activadora de ubicuitina |
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 (9)
| 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 |
| BR112014020365B1 (pt) | 2012-02-17 | 2023-02-23 | Takeda Pharmaceutical Company Limited | Inibidores de pirazolopirimidinila de enzima de ativação de ubiquitina |
| 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 |
| US9695154B2 (en) | 2013-07-02 | 2017-07-04 | Millennium Pharmaceuticals, Inc. | Heteroaryl inhibitors of sumo activating enzyme |
| UY36198A (es) | 2014-07-01 | 2016-01-29 | Millennium Pharm Inc | Compuestos de heteroarilo útiles como inhibidores de enzima activadora de sumo |
| WO2016069392A1 (en) | 2014-10-29 | 2016-05-06 | Millennium Pharmaceuticals, Inc. | Administration of ubiquitin-activating enzyme inhibitor and chemotherapeutic agents |
| WO2016069393A1 (en) | 2014-10-29 | 2016-05-06 | Millennium Pharmaceuticals, Inc. | Administration of ubiquitin-activating enzyme inhibitor and radiation |
| MX2021004769A (es) | 2018-10-30 | 2021-08-24 | Kronos Bio Inc | Compuestos, composiciones, y metodos para modular la actividad cdk9. |
| 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 |
| 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 |
| EP1608652A1 (en) | 2003-03-31 | 2005-12-28 | 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 |
| EP1758873A1 (en) | 2004-06-22 | 2007-03-07 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| JP5048520B2 (ja) | 2005-02-04 | 2012-10-17 | 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 | Ｅ１活性化酵素の阻害剤 |
| WO2007044426A2 (en) | 2005-10-06 | 2007-04-19 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| EP2402334B1 (en) | 2006-02-02 | 2016-06-29 | Millennium Pharmaceuticals, Inc. | Inhibitors of E1 Activating Enzymes |
| EP1992008A1 (en) * | 2006-02-28 | 2008-11-19 | Sez Ag | Device and method for liquid treating disc-like articles |
| MY157177A (en) | 2006-08-08 | 2016-05-13 | Millennium Pharm 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 |
| CN107021895A (zh) | 2007-06-12 | 2017-08-08 | 尔察祯有限公司 | 抗菌剂 |
| ES2758027T3 (es) * | 2007-08-02 | 2020-05-04 | Millennium Pharm Inc | Intermedios para la síntesis de inhibidores de enzimas activadoras de actividad E1 |
| 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 |
| 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 |
| BR112014004239A2 (pt) | 2011-08-24 | 2017-03-21 | Millennium Pharm Inc | inibidores de enzima ativadora de nedd8 |
| BR112014020365B1 (pt) | 2012-02-17 | 2023-02-23 | Takeda Pharmaceutical Company Limited | Inibidores de pirazolopirimidinila de enzima de ativação de ubiquitina |
| 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 |
| US9695154B2 (en) | 2013-07-02 | 2017-07-04 | Millennium Pharmaceuticals, Inc. | Heteroaryl inhibitors of sumo activating enzyme |
| UY36198A (es) | 2014-07-01 | 2016-01-29 | Millennium Pharm Inc | Compuestos de heteroarilo útiles como inhibidores de enzima activadora de sumo |
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2013
- 2013-02-14 BR BR112014020365-2A patent/BR112014020365B1/pt active IP Right Grant
- 2013-02-14 CN CN201380009784.8A patent/CN104136399B/zh active Active
- 2013-02-14 SG SG10201606581RA patent/SG10201606581RA/en unknown
- 2013-02-14 SG SG11201404757WA patent/SG11201404757WA/en unknown
- 2013-02-14 JP JP2014557765A patent/JP6122877B2/ja active Active
- 2013-02-14 EA EA201400831A patent/EA035020B1/ru not_active IP Right Cessation
- 2013-02-14 WO PCT/US2013/026113 patent/WO2013123169A1/en active Application Filing
- 2013-02-14 EP EP13748707.0A patent/EP2814791A4/en not_active Withdrawn
- 2013-02-14 EP EP16205139.5A patent/EP3173413B1/en active Active
- 2013-02-14 UA UAA201409297A patent/UA116534C2/uk unknown
- 2013-02-14 KR KR1020147025556A patent/KR20140123104A/ko not_active Application Discontinuation
- 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 ES ES16205139T patent/ES2739150T3/es active Active
- 2013-02-14 CA CA2864672A patent/CA2864672C/en active Active
- 2013-02-14 GE GEAP201313560A patent/GEP201706687B/en unknown
- 2013-02-14 EP EP19170607.6A patent/EP3536692B1/en active Active
- 2013-02-14 US US13/767,314 patent/US9290500B2/en active Active
- 2013-02-14 PE PE2014001278A patent/PE20142244A1/es active IP Right Grant
- 2013-02-15 UY UY0001034629A patent/UY34629A/es not_active Application Discontinuation
- 2013-02-15 AR ARP130100480A patent/AR092797A1/es unknown
- 2013-02-18 TW TW102105676A patent/TWI593688B/zh not_active IP Right Cessation
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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
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2015
- 2015-03-05 HK HK15102227.4A patent/HK1201817A1/xx unknown
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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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