AR074830A1 - Pirrolotriazinas como inhibidores de alk y jak2 - Google Patents
Pirrolotriazinas como inhibidores de alk y jak2Info
- Publication number
- AR074830A1 AR074830A1 ARP090105015A ARP090105015A AR074830A1 AR 074830 A1 AR074830 A1 AR 074830A1 AR P090105015 A ARP090105015 A AR P090105015A AR P090105015 A ARP090105015 A AR P090105015A AR 074830 A1 AR074830 A1 AR 074830A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- nr12r13
- nr24c
- nr14c
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, donde Q1 es -L1-A1-G1-X1-Z1; Q2 es -L2-A2-G2-X2-Z2; Q3 es -L3-A3-G3-X3-Z3; Q4 es -L4-A4-G4-X4-Z4; L1 es alquileno C1-6 opcionalmente sustituido por 1-12 R9, alquenileno C2-6 opcionalmente sustituido por 1-10 R9, alquinileno C2-6 opcionalmente sustituido por 1-8 R9, arileno C6-10 opcionalmente sustituido por 1-10 R9, arilalquileno C7-16 opcionalmente sustituido por 1-18 R9, cicloalquileno C3-11 opcionalmente sustituido por 1-20 R9, cicloalquilalquileno C4-17 opcionalmente sustituido por 1-31 R9, heterocicloalquileno de 3 a 15 miembros opcionalmente sustituido por 1-27 R9, heterocicloalquilalquileno de 4 a 21 miembros opcionalmente sustituido por 1-39 R9, heteroarileno de 5 a 15 miembros opcionalmente sustituido por 1-14 R9, heteroarilalquileno de 6 a 21 miembros opcionalmente sustituido por 1-26 R9, -alquil C0-3-C(=O)alquilo C0-3-, -alquil C0-3-C(=O)O-alquilo C0-3-, -alquil C0-3-C(=O)NR4-alquilo C0-3-, -alquil C0-3-C(=O)C(=O)alquilo C0-3-, -alquil C0-3-C(=NR5)alquilo C0-3-, -alquil C0-3-C(=NR5)NR4-alquilo C0-3-, -alquil C0-3-C(=NOH)NR4-alquilo C0-3-, -alquil C0-3-C(=NOR6)alquilo C0-3-, -alquil C0-3-C(=NNR2R3)alquilo C0-3-, -alquil C0-3-C(=NNR4C(=O)R1)alquilo C0-3-, -alquil C0-3-C(=NNR4C(=O)OR1)alquilo C0-3-, -alquil C0-3-C(=S)NR4-alquilo C0-3-, -alquil C0-3-NR4-alquilo C0-3-, -alquil C0-3-NR4NR4-alquilo C0-3-, -alquil C0-3-N=N-alquilo C0-3-, -alquil C0-3-NR4C(=O)alquilo C0-3-, -alquil C0-3-NR4C(=O)C(=O)alquilo C0-3-, -alquil C0-3-NR4C(=O)O-alquilo C0-3-, -alquil C0-3-NR4C(=O)C(=O)O-alquilo C0-3-, -alquil C0-3-NR4C(=O)NR4-alquilo C0-3-, -alquil C0-3-NR4C(=O)NR4C(=O)alquilo C0-3-, -alquil C0-3-NR4C(=O)NR4C(=O)O-alquilo C0-3-, -alquil C0-3-NR4C(=NR5)NR4-alquilo C0-3-, -alquil C0-3-NR4C(=O)C(=O)NR4-alquilo C0-3-, -alquil C0-3-NR4C(=S)alquilo C0-3-, -alquil C0-3-NR4C(=S)O-alquilo C0-3-, -alquil C0-3-NR4C(=S)NR4-alquilo C0-3-, -alquil C0-3-NR4S(=O)2alquilo C0-3-, -alquil C0-3-NR4S(=O)2NR4-alquilo C0-3-, -alquil C0-3O-alquilo C0-3-, -alquil C0-3-OC(=O)alquilo C0-3-, -alquil C0-3-OC(=O)NR4-alquilo C0-3-, -alquil C0-3-OC(=O)O-alquilo C0-3-, -alquil C0-3-OC(=NR5)NR4-alquilo C0-3-, -alquil C0-3-OS(=O)alquilo C0-3-, -alquil C0-3-OS(=O)2alquilo C0-3-, -alquil C0-3-OS(=O)2O-alquilo C0-3-, -alquil C0-3-OS(=O)2NR4-alquilo C0-3-, -alquil C0-3-S(=O)n-alquilo C0-3-, -alquil C0-3-S(=O)2O-alquilo C0-3-, -alquil C0-3-So3-alquilo C0-3-, -alquil C0-3-S(=O)2NR4-alquilo C0-3-, -alquil C0-3-S(=O)NR4-alquilo C0-3-, o ausente; A1 es alquilo C1-6 o alquileno C1-6 opcionalmente sustituido por 1-13 o 1-12 Ra, respectivamente, alquenilo C2-6 o alquenileno C2-6 opcionalmente sustituido por 1-11 o 1-10 Ra respectivamente, alquinilo C2-6 o alquinileno C2-6 opcionalmente sustituido por 1-9 o 1-8 Ra, respectivamente, arilo C6-10 o arileno C6-10 opcionalmente sustituido por 1-11 o 1-10 Ra, respectivamente, arilalquilo C7-16, o arilalquileno C7-16 opcionalmente sustituido por 1-19 o 1-18 Ra, respectivamente, cicloalquilo C3-11 o cicloalquileno C3-11 opcionalmente sustituido por 1-21 o 1-20 Ra, respectivamente, cicloalquilalquilo C4-17 o cicloalquilalquileno C4-17 opcionalmente sustituido por 1-32 o 1-31 Ra, respectivamente, heterocicloalquilo de 3 a 15 miembros o heterocicloalquileno de 3 a 15 miembros opcionalmente sustituido por 1-28 o 1-27 Ra, respectivamente, heterocicloalquilalquilo de 4 a 21 miembros o heterocicloalquilalquileno de 4 a 21 miembros opcionalmente sustituido por 1-40 ó 1-39 Ra, respectivamente, heteroarilo de 5 a 15 miembros o heteroarileno de 5 a 15 miembros opcionalmente sustituido por 1-15 o 1-14 Ra, respectivamente, o heteroarilalquilo de 6 a 21 miembros o heteroarilalquileno de 6 a 21 miembros opcionalmente sustituido por 1-27 o 1-26 Ra, respectivamente, donde cada Ra se selecciona independientemente de alquilo C1-6 opcionalmente sustituido por 1-13 R19, alquenilo C2-6 opcionalmente sustituido por 1-11 R19, alquinilo C2-6 opcionalmente sustituido por 1-9 R19, arilo C6-10 opcionalmente sustituido por 1-11 R19, arilalquilo C7-16 opcionalmente sustituido por 1-19 R19, cicloalquilo C3-11 opcionalmente sustituido por 1-21 R19, cicloalquilalquilo C4-17 opcionalmente sustituido por 1-32 R19, heterocicloalquilo de 3 a 15 miembros opcionalmente sustituido por 1-28 R19, heterocicloalquilalquilo de 4 a 21 miembros opcionalmente sustituido por 1-40 R19, heteroarilo de 5 a 15 miembros opcionalmente sustituido por 1-15 R19, heteroarilalquilo de 6 a 21 miembros opcionalmente sustituido por 1-27 R19, halógeno, -CN, -C(=O)R10, -C(=O)OR10, -C(=O)NR12R13, -C(=O)C(=O)R10, -C(=NR15)R10, -C(=NR85)R12R13, -C(NOH)NR12R13, -C(=NOR16)R10, -C(=NNR12R13)R10, -C(=NNR14C(=O)R11)R10, -C(=NNR14C(=O)OR11)R10, -C(=S)NR12R13, -NC, -NO2, -NR12R13, -NR14NR12R13, -N=NR14, =NR10, =NOR10, -NR14OR16, -NR14C(=O)R10, -NR14C(=O)C(=O)R10, -NR14C(=O)OR11, NR14C(=O)C(=O)OR11, -NR14C(=O)NR12R13, -NR14C(=O)NR14C(=O)R10, -NR14C(=O)NR14c(=o)oR10, -NR14C(=NR15)NR12R13, -NR14C(=O)C(=O)NR12R13, -NR14C(=S)R10, -NR14C(=S)OR10, -NR14C(=S)NR12R13, -NR14S(=O)2R11, -NR14S(=O)2NR12R13, -NR14P(=O)R18R18, -NR14P(=O)(NR12R13)(NR12R13), -NR14P(=O)(OR10)(OR10), -NR14P(=O)(SR10)(SR10), -OR10, =O, -OCN, -OC(=O)R10, -OC(=O)NR12R13, -OC(=O)OR10, -OC(=NR15)NR12R13, -OS(=O)R10, -OS(=O)2R10, -OS(=O)2OR10, -OS(=O)2NR12R13, -OP(=O)R18R18, OP(=O)(NR12R13)(NR12R13), -OP(=O)(OR10)(OR10), -OP(=O)(SR10)(SR10), -SCN, =S, -S(=O)nR10, -S(=O)2OR10, -so3R17, -S(=O)2NR12R13, -S(=O)NR12R13, -SP(=O)R18R18, -SP(=O)(NR12R13)(NR12R13), -SP(=O)(OR10)(OR10), -SP(=O)(SR10)(SR10), -P(=O)R18R18, -P(=O)(NR12R13)(NR12R13), -P(=O)(OR10)(OR10), y -P(=O)(SR10)(SR10); G1 es alquilo C1-6 o alquileno C1-6 opcionalmente sustituido por 1-13 ó 1-12 R29, respectivamente, alquenilo C2-6 o alquenileno C2-6 opcionalmente sustituido por 1-11 o 1-10 R29, respectivamente, alquinilo C2-6 o alquinileno C2-6 opcionalmente sustituido por 1-9 o 1-8 R29, respectivamente, arilo C6-10 o arilero C6-10 opcionalmente sustituido por 1-11 o 1-10 R29, respectivamente, arilalquilo C7-16 o arilalquileno C7-16 opcionalmente sustituido por 1-19 o 1-18 R29, respectivamente, cicloalquilo C3-11 o cicloalquileno C3-11 opcionalmente sustituido por 1-21 o 1-20 R29, cicloalquilalquilo C4-17 o cicloalquilalquileno C4-17 opcionalmente sustituido por 1-32 o 1-31 R29, respectivamente, heterocicloalquilo de 3 a 15 miembros o heterocicloalquileno de 3 a 15 miembros opcionalmente sustituido por 1-28 o 1-27 R29, respectivamente, heterocicloalquilalquilo de 4 a 21 miembros o heterocicloalquilalquileno de 4 a 21 miembros opcionalmente sustituido por 1-40 ó 1-39 R29, respectivamente, heteroarilo de 5 a 15 miembros o heteroarileno de 5 a 15 miembros opcionalmente sustituido por 1-15 o 1-14 R29, respectivamente, o heteroarilalquilo de 6 a 21 miembros o heteroarilalquileno de 6 a 21 miembros opcionalmente sustituido por 1-27 o 1-26 R29, respectivamente, -alquil C0-3-C(=O)alquilo C0-3-, -alquil C0-3-C(=O)O-alquilo C0-3-, -alquil C0-3-C(=O)NR24-alquilo C0-3-, -alquil C0-3-C(=O)C(=O)alquilo C0-3-, -alquil C0-3-C(=NR25)alquilo C0-3-, -alquil C0-3-C(=NR25)NR24-alquilo C0-3-, -alquil C0-3-C(=NOH)NR24-alquilo C0-3-, -alquil C0-3-C(=NOR26)alquilo C0-3-, -alquil C0-3-C(=NNR22R23)alquilo C0-3-, -alquil C0-3-C(=NNR24C(=O)R21)alquilo C0-3-, -alquil C0-3-C(=NNR24C(=O)OR21)alquilo C0-3-, -alquil C0-3-C(=S)NR24-alquilo C0-3-, -alquil C0-3-NR24-alquilo C0-3-, -alquil C0-3-NR24NR24-alquilo C0-3-, -alquil C0-3-N=N-alquilo C0-3-, -alquil C0-3-NR24C(=O)alquilo C0-3-, -alquil C0-3-NR24C(=O)C(=O)alquilo C0-3-, -alquil C0-3-NR24C(=O)O-alquilo C0-3-, -alquil C0-3-NR24C(=O)C(=O)O-alquilo C0-3-, -alquil C0-3-NR24C(=O)NR24-alquilo C0-3-, -alquil C0-3-NR24C(=O)NR24C(=O)alquilo C0-3-, -alquil C0-3-NR24C(=O)NR24C(=O)O-alquilo C0-3-, -alquil C0-3-NR24C(=NR25)NR24-alquilo C0-3-, -alquil C0-3-NR24C(=O)C(=O)NR24-alquilo C0-3-, -alquil C0-3-NR24C(=S)alquilo C0-3-, -alquil C0-3-NR24C(=S)O-alquilo C0-3-, -alquil C0-3-NR24C(=S)NR24-alquilo C0-3-, -alquil C0-3-NR24S(=O)2alquilo C0-3-, -alquil C0-3-NR24S(=O)2NR24-alquilo C0-3-, -alquil C0-3O-alquilo C0-3-, -alquil C0-3-OC(=O)alquilo C0-3-, -alquil C0-3-OC(=O)NR24-alquilo C0-3-, -alquil C0-3-OC(=O)O-alquilo C0-3-, -alquil C0-3-OC(=NR25)NR24-alquilo C0-3-, -alquil C0-3-OS(=O)alquilo C0-3-, -alquil C0-3-OS(=O)2alquilo C0-3-, -alquil C0-3-OS(=O)2O-alquilo C0-3-, -alquil C0-3-OS(=O)2NR24-alquilo C0-3-, -alquil C0-3-S(=O)n-alquilo C0-3-, -alquil C0-3-S(=O)2O-alquilo C0-3-, -alquil C0-3-So3-alquilo C0-3-, -alquil C0-3-S(=O)2NR24-alquilo C0-3-, -alquil C0-3-S(=O)NR24-alquilo C0-3-, o ausente; X1 es alquilo C1-6 o alquileno C1-6 opcionalmente sustituido por 1-13 o 1-12 R39 respectivamente, alquenilo C2-6 o alquenileno C2-6 opcionalmente sustituido por 1-11 o 1-10 R39, respectivamente, alquinilo C2-6 o alquinileno C2-6 opcionalmente sustituido por 1-9 o 1-8 R39, respectivamente, arilo C6-10 o arileno C6-10 opcionalmente sustituido por 1-11 o 1-10 R39, respectivamente, arilalquilo C7-16 o arilalquileno C7-16 opcionalmente sustituido por 1-19 o 1-18 R39, respectivamente, cicloalquilo C3-11 o cicloalquileno C3-11 opcionalmente sustituido por 1-21 o 1-20 R39, cicloalquilalquilo C4-17 o cicloalquilalquileno C4-17 opcionalmente sustituido por 1-32 o 1-31 R39, respectivamente, heterocicloalquilo de 3 a 15 miembros o heterocicloalquileno de 3 a 15 miembros opcionalmente sustituido por 1-28 o 1-27 R39, respectivamente, heterocicloalquilalquilo de 4 a 21 miembros o heterocicloalquilalquileno de 4 a 21 miembros opcionalmente sustituido por 1-40 ó 1-39 R39, respectivamente, heteroarilo de 5 a 15 miembros o heteroarileno de 5 a 15 miembros opcionalmente sustituido por 1-15 o 1-14 R39, respectivamente, o heteroarilalquilo de 6 a 21 miembros o heteroarilalquileno de 6 a 21 miembros opcionalmente sustituido por 1-27 o 1-26 R39, respectivamente, -alquil C0-3-C(=O)alquilo C0-3-, -alquil C0-3-C(=O)O-alquilo C0-3-, -alquil C0-3-C(=O)NR34-alquilo C0-3-, -alquil C0-3-C(=O)C(=O)alquilo C0-3-, -alquil C0
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13954508P | 2008-12-19 | 2008-12-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR074830A1 true AR074830A1 (es) | 2011-02-16 |
Family
ID=41683065
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090105015A AR074830A1 (es) | 2008-12-19 | 2009-12-21 | Pirrolotriazinas como inhibidores de alk y jak2 |
Country Status (7)
Country | Link |
---|---|
US (1) | US8471005B2 (es) |
EP (1) | EP2376491B1 (es) |
AR (1) | AR074830A1 (es) |
ES (1) | ES2539620T3 (es) |
HK (1) | HK1162520A1 (es) |
TW (1) | TW201035100A (es) |
WO (1) | WO2010071885A1 (es) |
Families Citing this family (57)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2671748T3 (es) | 2011-07-21 | 2018-06-08 | Tolero Pharmaceuticals, Inc. | Inhibidores heterocíclicos de proteína quinasas |
JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Pimキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
MX2015009057A (es) | 2013-01-15 | 2015-10-05 | Incyte Corp | Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de cinasa pim. |
EP2951590A1 (en) | 2013-02-04 | 2015-12-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
WO2014193932A1 (en) | 2013-05-29 | 2014-12-04 | Cephalon, Inc. | Pyrrolotriazines as alk inhibitors |
TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作pim激酶抑制劑之呋喃并-及噻吩并-吡啶甲醯胺化合物 |
US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
US10158988B2 (en) * | 2014-07-24 | 2018-12-18 | Qualcomm Incorporated | Multi-SIM based device auto configuration system and process |
EP3268006B1 (en) | 2015-03-12 | 2020-01-08 | Merck Sharp & Dohme Corp. | Pyrrolotriazine inhibitors of irak4 activity |
WO2016144844A1 (en) * | 2015-03-12 | 2016-09-15 | Merck Sharp & Dohme Corp. | Carboxamide inhibitors of irak4 activity |
WO2016183071A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Hetero-tricyclic compounds and their use for the treatment of cancer |
US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
US9708333B2 (en) | 2015-08-12 | 2017-07-18 | Incyte Corporation | Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors |
WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
WO2017070089A1 (en) | 2015-10-19 | 2017-04-27 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
MD3377488T2 (ro) | 2015-11-19 | 2023-02-28 | Incyte Corp | Compuși heterociclici ca imunomodulatori |
MX2018007774A (es) | 2015-12-22 | 2018-11-09 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores. |
PE20190175A1 (es) | 2016-03-28 | 2019-02-01 | Incyte Corp | Compuestos de pirrolotriazina como inhibidores de tam |
AR108396A1 (es) | 2016-05-06 | 2018-08-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
ES2905980T3 (es) | 2016-05-26 | 2022-04-12 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
CN109890819B (zh) | 2016-06-20 | 2022-11-22 | 因赛特公司 | 作为免疫调节剂的杂环化合物 |
EP3484866B1 (en) | 2016-07-14 | 2022-09-07 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
EP3504198B1 (en) | 2016-08-29 | 2023-01-25 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
CN110691782A (zh) * | 2016-12-01 | 2020-01-14 | 艾普托斯生物科学公司 | 作为brd4和jak2双重抑制剂的稠合的嘧啶化合物及其使用方法 |
PE20191532A1 (es) | 2016-12-22 | 2019-10-23 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores |
LT3558990T (lt) | 2016-12-22 | 2022-12-27 | Incyte Corporation | Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai |
ES2899402T3 (es) | 2016-12-22 | 2022-03-11 | Incyte Corp | Derivados de piridina como inmunomoduladores |
WO2018119236A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Triazolo[1,5-a]pyridine derivatives as immunomodulators |
CA3048376A1 (en) | 2016-12-27 | 2018-07-05 | Riken | Bmp-signal-inhibiting compound |
WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
EP3610264A1 (en) | 2017-04-13 | 2020-02-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
US11827616B2 (en) | 2017-05-04 | 2023-11-28 | Discovery Purchaser Corporation | Heterocyclic compounds as pesticides |
KR20200088308A (ko) | 2017-09-27 | 2020-07-22 | 인사이트 코포레이션 | Tam 억제제로서 유용한 피롤로트리아진 유도체의 염 |
AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
MX2020010321A (es) | 2018-03-30 | 2021-01-08 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores. |
US20210113562A1 (en) | 2018-04-13 | 2021-04-22 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
MX2020012045A (es) | 2018-05-11 | 2021-03-29 | Incyte Corp | Derivados de tetrahidro-imidazo[4,5-c]piridina como inmunomoduladores de ligando 1 de muerte programada (pd-l1). |
AR117600A1 (es) | 2018-06-29 | 2021-08-18 | Incyte Corp | Formulaciones de un inhibidor de axl / mer |
WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
CA3127502A1 (en) | 2019-02-12 | 2020-08-20 | Sumitomo Dainippon Pharma Oncology, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
CN112094272A (zh) * | 2019-06-18 | 2020-12-18 | 北京睿熙生物科技有限公司 | Cdk激酶抑制剂 |
KR20220042127A (ko) * | 2019-06-28 | 2022-04-04 | 상하이 파마슈티컬스 홀딩 컴퍼니 리미티드 | 피라졸로피리미딘 화합물, 그의 제조 방법 및 그의 응용 |
MX2022001671A (es) | 2019-08-09 | 2022-05-13 | Incyte Corp | Sales de un inhibidor de pd-1/pd-l1. |
AR120109A1 (es) | 2019-09-30 | 2022-02-02 | Incyte Corp | Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores |
CN114829366A (zh) | 2019-11-11 | 2022-07-29 | 因赛特公司 | Pd-1/pd-l1抑制剂的盐及结晶形式 |
US11780836B2 (en) | 2020-11-06 | 2023-10-10 | Incyte Corporation | Process of preparing a PD-1/PD-L1 inhibitor |
WO2022099071A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof |
US11760756B2 (en) | 2020-11-06 | 2023-09-19 | Incyte Corporation | Crystalline form of a PD-1/PD-L1 inhibitor |
CN115466264A (zh) * | 2021-06-11 | 2022-12-13 | 腾讯科技(深圳)有限公司 | 吡咯并[2,1-f][1,2,4]三嗪类衍生物及其应用 |
KR20230081667A (ko) | 2021-11-30 | 2023-06-07 | 연세대학교 산학협력단 | 단백질 키나아제 저해활성을 가지는 2, 7-치환된 피롤로[2,1-f][1,2,4]트라아진 화합물 |
CA3239668A1 (en) * | 2021-11-30 | 2023-06-08 | Tae Bo Sim | 2,7-substituted pyrrolo[2,1-f][1,2,4]triazine compound having protein kinase inhibitory activity |
WO2023147372A1 (en) * | 2022-01-25 | 2023-08-03 | Kinnate Biopharma Inc. | Inhibitors of cdk4/6 kinase |
TW202412758A (zh) * | 2022-06-29 | 2024-04-01 | 香港商英矽智能科技知識產權有限公司 | Fgfr2與fgfr3抑制劑及其用途 |
WO2024097653A1 (en) | 2022-10-31 | 2024-05-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (82)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4838925A (en) | 1986-04-25 | 1989-06-13 | E. I. Du Pont De Nemours And Company | Heterocyclic acyl sulfonamides |
WO1989000994A2 (en) | 1987-07-31 | 1989-02-09 | E.I. Du Pont De Nemours And Company | Herbicidal sulfonamides |
IT1269176B (it) | 1994-01-11 | 1997-03-21 | Isagro Srl | Eterobicicli ad attivita' fungicida |
SE9500051D0 (sv) | 1995-01-09 | 1995-01-09 | Frode Rise | Antioxidants, tissue- and/or neuroprotectants |
CA2373990C (en) | 1999-05-21 | 2007-05-08 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
WO2001014378A1 (fr) | 1999-08-23 | 2001-03-01 | Shionogi & Co., Ltd. | DERIVES DE PYRROLOTRIAZINE A ACTIVITES INHIBANT sPLA¿2? |
YU37903A (sh) | 2000-11-17 | 2006-05-25 | Bristol-Myers Squibb Company | POSTUPCI LEČENJA STANJA POVEZANIH SA p38 KINAZOM I JEDINJENJA PIROLOTRIAZINA KOJA SE KORISTE KAO INHIBITORI KINAZE |
US6867300B2 (en) | 2000-11-17 | 2005-03-15 | Bristol-Myers Squibb Company | Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors |
TW200300350A (en) | 2001-11-14 | 2003-06-01 | Bristol Myers Squibb Co | C-5 modified indazolylpyrrolotriazines |
US7388009B2 (en) | 2002-04-23 | 2008-06-17 | Bristol-Myers Squibb Company | Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors |
ATE418546T1 (de) | 2002-04-23 | 2009-01-15 | Bristol Myers Squibb Co | Als kinase inhibitoren geeignete arylketonpyrrolotriazin-verbindungen |
KR101025675B1 (ko) | 2002-04-23 | 2011-03-30 | 브리스톨-마이어스 스큅 컴퍼니 | 키나제 억제제로서 유용한 피롤로-트리아진 아닐린 화합물 |
TW200407143A (en) | 2002-05-21 | 2004-05-16 | Bristol Myers Squibb Co | Pyrrolotriazinone compounds and their use to treat diseases |
TWI329112B (en) | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
TWI272271B (en) | 2002-07-19 | 2007-02-01 | Bristol Myers Squibb Co | Process for preparing certain pyrrolotriazine compounds |
WO2004013145A1 (en) * | 2002-08-02 | 2004-02-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
KR20050088079A (ko) | 2002-11-15 | 2005-09-01 | 이데닉스 (케이만) 리미티드 | 2'-분지형 뉴클레오시드 및 플라비비리다에 돌연변이 |
TW200420565A (en) | 2002-12-13 | 2004-10-16 | Bristol Myers Squibb Co | C-6 modified indazolylpyrrolotriazines |
AU2004212435A1 (en) | 2003-02-05 | 2004-08-26 | Bristol-Myers Squibb Company | Process for preparing pyrrolotriazine kinase inhibitors |
TW200508224A (en) | 2003-02-12 | 2005-03-01 | Bristol Myers Squibb Co | Cyclic derivatives as modulators of chemokine receptor activity |
CA2520465A1 (en) | 2003-03-28 | 2004-10-14 | Scios Inc. | Bi-cyclic pyrimidine inhibitors of tgf.beta. |
AU2004259012C1 (en) | 2003-07-23 | 2012-08-02 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
DK1660458T3 (da) | 2003-08-15 | 2012-05-07 | Irm Llc | 2, 4-pyrimidindiaminer egnede i behandling af neoplastiske sygdomme, in-flammatoriske lidelser og lidelser i immunsystemet. |
US7163937B2 (en) | 2003-08-21 | 2007-01-16 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
US7378409B2 (en) | 2003-08-21 | 2008-05-27 | Bristol-Myers Squibb Company | Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity |
US7102001B2 (en) | 2003-12-12 | 2006-09-05 | Bristol-Myers Squibb Company | Process for preparing pyrrolotriazine |
US20060014741A1 (en) | 2003-12-12 | 2006-01-19 | Dimarco John D | Synthetic process, and crystalline forms of a pyrrolotriazine compound |
US7064203B2 (en) | 2003-12-29 | 2006-06-20 | Bristol Myers Squibb Company | Di-substituted pyrrolotriazine compounds |
MY145634A (en) | 2003-12-29 | 2012-03-15 | Bristol Myers Squibb Co | Pyrrolotriazine compounds as kinase inhibitors |
PT1713806E (pt) | 2004-02-14 | 2013-08-27 | Irm Llc | Compostos e composições como inibidores da proteína quinase |
US7306631B2 (en) | 2004-03-30 | 2007-12-11 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
WO2005097765A1 (en) | 2004-03-31 | 2005-10-20 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
UY28931A1 (es) | 2004-06-03 | 2005-12-30 | Bayer Pharmaceuticals Corp | Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis |
US7102002B2 (en) | 2004-06-16 | 2006-09-05 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
US7432373B2 (en) | 2004-06-28 | 2008-10-07 | Bristol-Meyers Squibb Company | Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors |
US7439246B2 (en) | 2004-06-28 | 2008-10-21 | Bristol-Myers Squibb Company | Fused heterocyclic kinase inhibitors |
US7173031B2 (en) | 2004-06-28 | 2007-02-06 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
US7253167B2 (en) | 2004-06-30 | 2007-08-07 | Bristol-Myers Squibb Company | Tricyclic-heteroaryl compounds useful as kinase inhibitors |
TW200600513A (en) | 2004-06-30 | 2006-01-01 | Bristol Myers Squibb Co | A method for preparing pyrrolotriazine compounds |
US7102003B2 (en) | 2004-07-01 | 2006-09-05 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds |
US7148348B2 (en) | 2004-08-12 | 2006-12-12 | Bristol-Myers Squibb Company | Process for preparing pyrrolotriazine aniline compounds useful as kinase inhibitors |
EP2364699A1 (en) | 2004-09-13 | 2011-09-14 | Eisai R&D Management Co., Ltd. | Joint use of sulfonamide based compound with angiogenesis inhibitor |
CA2577745C (en) | 2004-09-30 | 2012-11-27 | Tibotec Pharmaceuticals Ltd. | Hcv inhibiting bi-cyclic pyrimidines |
EP1812439B2 (en) | 2004-10-15 | 2017-12-06 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
US7151176B2 (en) | 2004-10-21 | 2006-12-19 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds |
TW200635927A (en) | 2004-12-22 | 2006-10-16 | Bristol Myers Squibb Co | Synthetic process |
US7456289B2 (en) | 2004-12-31 | 2008-11-25 | National Health Research Institutes | Anti-tumor compounds |
US7534882B2 (en) | 2005-04-06 | 2009-05-19 | Bristol-Myers Squibb Company | Method for preparing pyrrolotriazine compounds via in situ amination of pyrroles |
US20060235020A1 (en) | 2005-04-18 | 2006-10-19 | Soojin Kim | Process for preparing salts of 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide and novel stable forms produced therein |
US20110045459A1 (en) | 2005-04-21 | 2011-02-24 | Mischel Paul S | Molecular determinants of EGFR kinase inhibitor response in glioblastoma |
JO2787B1 (en) | 2005-04-27 | 2014-03-15 | امجين إنك, | Alternative amide derivatives and methods of use |
US20060257400A1 (en) | 2005-05-13 | 2006-11-16 | Bristol-Myers Squibb Company | Combination therapy |
US7393667B2 (en) | 2005-05-31 | 2008-07-01 | Bristol-Myers Squibb Company | Stereoselective reduction process for the preparation of pyrrolotriazine compounds |
US7619083B2 (en) | 2005-07-01 | 2009-11-17 | Bristol-Myers Squibb Company | Intermediates useful in preparing certain pyrrolotriazine compounds and process for making such intermediates |
US7405213B2 (en) | 2005-07-01 | 2008-07-29 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith |
US7402582B2 (en) | 2005-07-01 | 2008-07-22 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith |
JP5136945B2 (ja) | 2005-07-05 | 2013-02-06 | トヨタ自動車株式会社 | 燃料電池システム |
WO2007004731A1 (ja) | 2005-07-05 | 2007-01-11 | Sumitomo Chemical Company, Limited | 亜リン酸エステル類の結晶 |
US20100105031A1 (en) | 2005-08-01 | 2010-04-29 | Esai R & D Management Co., Ltd. | Method for prediction of the efficacy of vascularization inhibitor |
JP4989476B2 (ja) | 2005-08-02 | 2012-08-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 血管新生阻害物質の効果を検定する方法 |
JP2009511440A (ja) | 2005-09-27 | 2009-03-19 | ブリストル−マイヤーズ スクイブ カンパニー | [(1R),2S]−2−アミノプロピオン酸2−[4−(4−フルオロ−2−メチル−1H−インドール−5−イルオキシ)−5−メチルピロロ[2,1−f][1,2,4]トリアジン−6−イルオキシ]−1−メチルエチルエステルの結晶形 |
EP1945222B1 (en) | 2005-11-02 | 2012-12-26 | Bayer Pharma Aktiengesellschaft | Pyrrolo[2,1-f] [1,2,4]-triazin-4-ylamines as igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases |
US7514435B2 (en) | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
US7348325B2 (en) | 2005-11-30 | 2008-03-25 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
PE20070855A1 (es) | 2005-12-02 | 2007-10-14 | Bayer Pharmaceuticals Corp | Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas |
MX2008007103A (es) | 2005-12-02 | 2008-09-12 | Bayer Healthcare Llc | Derivados 4-amino-pirrolotriazina sustituidos, útiles para tratar trastornos hiperproliferativos y enfermedades asociadas con angiogenesis. |
CN101448506A (zh) | 2005-12-02 | 2009-06-03 | 拜尔健康护理有限责任公司 | 通过抑制有丝分裂酶激酶治疗癌症的吡咯并三嗪衍生物 |
CA2633211A1 (en) | 2005-12-15 | 2007-06-21 | Astrazeneca Ab | Combination of angiopoietin-2 antagonist and of vegf-a, kdr and/or flt1 antagonist for treating cancer |
US8063208B2 (en) | 2006-02-16 | 2011-11-22 | Bristol-Myers Squibb Company | Crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol |
CN101395158A (zh) | 2006-03-07 | 2009-03-25 | 百时美施贵宝公司 | 可作为激酶抑制剂的吡咯并三嗪苯胺前体药物化合物 |
CN101405278A (zh) | 2006-03-15 | 2009-04-08 | 4Sc股份公司 | 新颖的杂环NF-κB抑制剂 |
CA2650059A1 (en) | 2006-04-21 | 2007-11-01 | Bristol-Myers Squibb Company | Process for the preparation of [(1r), 2s]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester |
CA2657594C (en) | 2006-07-07 | 2012-01-17 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
ES2393410T3 (es) | 2006-08-09 | 2012-12-21 | Bristol-Myers Squibb Company | Pirrolotriazinas inhibidoras de quinasas |
US7531539B2 (en) | 2006-08-09 | 2009-05-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
CN101583357B (zh) | 2006-08-29 | 2013-03-20 | 新加坡国立癌症中心 | Mtor拮抗剂和血管生成抑制剂用于制备治疗癌症的药物的用途 |
WO2008057775A2 (en) | 2006-10-27 | 2008-05-15 | Bristol-Myers Squibb Company | Heterocyclic amide compounds useful as kinase inhibitors |
WO2008057863A1 (en) | 2006-11-01 | 2008-05-15 | Bristol-Myers Squibb Company | Therapeutic combination of a panher/vegfr2 kinase inhibitor and a platinum compound |
US7851623B2 (en) | 2006-11-02 | 2010-12-14 | Astrazeneca Ab | Chemical process |
US7982033B2 (en) | 2006-11-03 | 2011-07-19 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
US20100074897A1 (en) | 2006-12-01 | 2010-03-25 | University Of Utah Research Foundation | Methods and Compositions related to HIF-1 alpha |
-
2009
- 2009-12-21 AR ARP090105015A patent/AR074830A1/es unknown
- 2009-12-21 TW TW098143815A patent/TW201035100A/zh unknown
- 2009-12-21 EP EP09775073.1A patent/EP2376491B1/en active Active
- 2009-12-21 WO PCT/US2009/069006 patent/WO2010071885A1/en active Application Filing
- 2009-12-21 ES ES09775073.1T patent/ES2539620T3/es active Active
-
2011
- 2011-06-15 US US13/160,890 patent/US8471005B2/en not_active Expired - Fee Related
-
2012
- 2012-04-02 HK HK12103270.1A patent/HK1162520A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
ES2539620T3 (es) | 2015-07-02 |
US20120028919A1 (en) | 2012-02-02 |
EP2376491B1 (en) | 2015-03-04 |
HK1162520A1 (en) | 2012-08-31 |
EP2376491A1 (en) | 2011-10-19 |
TW201035100A (en) | 2010-10-01 |
US8471005B2 (en) | 2013-06-25 |
WO2010071885A1 (en) | 2010-06-24 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR074830A1 (es) | Pirrolotriazinas como inhibidores de alk y jak2 | |
AR060994A1 (es) | Derivados de triazolopirazina | |
PE20091096A1 (es) | Compuestos organicos | |
PE20142400A1 (es) | Compuestos novedosos | |
NO20073492L (no) | 2,4 (4,6) Pyrimidinderivater | |
AR049104A1 (es) | Pirimidinas como inhibidores de plk, composiciones farmaceuticas que las contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades proliferativas, inflamatorias y autoinmunes. | |
RU2004132192A (ru) | Арил-алкиновые срединения в качестве гербицидов | |
JP2010529961A5 (es) | ||
BR112014000465A2 (pt) | catalisadores | |
JP2010111691A5 (es) | ||
AR086828A1 (es) | Compuestos heterociclicos fusionados como moduladores del canal ionico | |
AR057776A1 (es) | Derivados de 1,4-benzotiazepinas para prevenir y tratar trastornos que in-volucran la modulacion de los receptores ryr; procesos de obtencion y composiciones farmaceuticas | |
AR042192A1 (es) | Derivados antivirales de nucleosidos de pirimidina | |
PE20121158A1 (es) | Derivados de feniletinilo como moduladores alostericos positivos (map) | |
AR078513A1 (es) | Pirimidinas y composiciones farmaceuticas que las comprenden | |
JP2009503172A5 (es) | ||
NO20073723L (no) | Ibandronatpolymorf A | |
SI2651902T1 (en) | Tricyclic pyrazolyl and pyrimidinylenones as antioxidant inflammatory modulators | |
PE20080856A1 (es) | Inhibidores de metaloproteasas de matriz | |
AR087148A1 (es) | Imidazopiridazinas | |
JP2013538683A5 (es) | ||
NO20081180L (no) | Oxazolidinone-quinolone hybrids as antibacterial compounds | |
AR056191A1 (es) | Anillo de nucleosidos de siete miembros como inhibidores de la replica viral, metodos para su sintesis, composiciones farmaceuticas que los contienen y su uso en el tratamiento de infecciones con virus de la familia flaviviridae | |
NO20073755L (no) | Ibandronatpolymorf B | |
PE20120113A1 (es) | Nuevos derivados de benzotiadiazepinas, su procedimiento de preparacion y composiciones farmaceuticas que los contienen |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |