AR099138A1 - Piridinas fusionadas como inhibidores del complejo p97 - Google Patents
Piridinas fusionadas como inhibidores del complejo p97Info
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- AR099138A1 AR099138A1 ARP150100150A ARP150100150A AR099138A1 AR 099138 A1 AR099138 A1 AR 099138A1 AR P150100150 A ARP150100150 A AR P150100150A AR P150100150 A ARP150100150 A AR P150100150A AR 099138 A1 AR099138 A1 AR 099138A1
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- independently
- group
- hydrogen
- optionally substituted
- ring
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
Abstract
La presente se refiere a ciertas pirimidinas fusionadas que tienen un anillo homo- o hetero-ciclopentilo, ciclohexilo o cicloheptilo como par de fusión de la pirimidina; que tienen un grupo aminobencilo o aminobencilo sustituido en la posición 4 del anillo pirimidina; y un anillo heterobiciclo 5:6 con al menos un N, O ó S en la posición 2 del anillo pirimidina. Estos compuestos son útiles para el tratamiento del cáncer por inhibición del complejo p97. Reivindicación 1: Un compuesto de pirimidina fusionada de fórmula (1), en donde: Y es CR⁴, NH, NR⁵, O ó S y C cuando CR⁴ es un átomo sp³; m y n son cada uno independientemente un número entero de 0 a 4, y la suma de m y n es un número entero de 2, 3 ó 4; Ar es un grupo arilo opcionalmente sustituido; A, D y E son cada uno independientemente C o N, en donde C es un carbono sp² sustituido por hidrógeno o alquilo de 1 a 4 carbonos cuando una de las valencias de C no está designada de otro modo; Z y B son cada uno independientemente CR⁶, N, NR⁷, O ó S, en donde C como CR⁶ es un carbono sp²; R¹, R², R³, R⁴, R⁵, R⁶ y R⁷ se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, un grupo alifático opcionalmente sustituido, un grupo aromático opcionalmente sustituido y un grupo funcional opcionalmente sustituido; con la condición de que; a) al menos uno de D y E sea C; b) al menos uno de A, D, E, Z y B sea distinto de C; c) Z y B no pueden ser ambos simultáneamente cualquiera de NR⁷, O ó S; d) cuando uno de D y E es N y A es C, entonces Z y B son cada uno independientemente CR⁶, N o NR⁷; e) cuando ambos D y E son C y A es N, Z y B son cada uno independientemente CR⁶ o N, pero cuando Y es carbono y R³ es hidrógeno, entonces Z y B no pueden ser ambos CR⁶ y B no puede ser N; f) cuando ambos D y E son C y A es N, Z y B son cada uno independientemente CR⁶ o N, pero cuando ni m ni n es cero y R³ es hidrógeno, entonces Z y B no pueden ser ambos CR⁶ y B no puede ser N; g) cuando D, E y A son todos C, entonces Z y B son cada uno independientemente CR⁶, N, NR⁷, O ó S; h) cuando uno de Z y B es O ó S, entonces el otro es CR⁶ o N, y A, D y E son todos C; i) cuando uno de Z y B es NR⁷, entonces el otro es N o CR⁶, A, D y E son todos C.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201461929382P | 2014-01-20 | 2014-01-20 |
Publications (1)
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AR099138A1 true AR099138A1 (es) | 2016-06-29 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP150100150A AR099138A1 (es) | 2014-01-20 | 2015-01-20 | Piridinas fusionadas como inhibidores del complejo p97 |
Country Status (19)
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US (2) | US9828363B2 (es) |
EP (1) | EP3097092B1 (es) |
JP (1) | JP6387111B2 (es) |
KR (1) | KR101922317B1 (es) |
CN (1) | CN106458996B (es) |
AR (1) | AR099138A1 (es) |
AU (1) | AU2015206292B2 (es) |
BR (1) | BR112016016421B1 (es) |
CA (1) | CA2936559C (es) |
CL (1) | CL2016001840A1 (es) |
EA (1) | EA031317B1 (es) |
ES (1) | ES2819867T3 (es) |
IL (1) | IL246692B (es) |
MX (1) | MX2016009465A (es) |
NZ (1) | NZ722624A (es) |
SG (1) | SG11201605699QA (es) |
TW (1) | TWI640516B (es) |
WO (1) | WO2015109285A1 (es) |
ZA (1) | ZA201605107B (es) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2015089218A1 (en) | 2013-12-10 | 2015-06-18 | David Wustrow | Monocyclic pyrimidine/pyridine compounds as inhibitors of p97 complex |
WO2015109285A1 (en) | 2014-01-20 | 2015-07-23 | Cleave Biosciences, Inc. | FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX |
CR20190338A (es) * | 2016-12-22 | 2019-09-09 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso |
JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
US20210230170A1 (en) * | 2018-08-31 | 2021-07-29 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
SG11202112855WA (en) | 2019-05-21 | 2021-12-30 | Amgen Inc | Solid state forms |
CN110078749B (zh) * | 2019-06-04 | 2021-01-01 | 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) | 3a,3a′-双呋喃[2,3-b]吲哚啉类化合物、制备方法、药物组合物及应用 |
CN110872291B (zh) * | 2019-11-26 | 2021-06-25 | 五邑大学 | 一种四氢吡啶并嘧啶类化合物及其制备方法和应用 |
EP4149934A4 (en) * | 2020-05-11 | 2024-05-15 | Cleave Therapeutics Inc | CRYSTALLINE FORMS AND FORMULATIONS OF A VCP/P97 INHIBITOR |
CN115916779A (zh) * | 2020-05-11 | 2023-04-04 | 克立弗治疗学股份有限公司 | 用于治疗癌症的VCP/p97抑制剂 |
GB202111193D0 (en) * | 2021-08-03 | 2021-09-15 | Phoremost Ltd | Pharmaceutical compounds |
WO2023086419A1 (en) * | 2021-11-10 | 2023-05-19 | Cleave Therapeutics, Inc. | Vcp/p97 inhibitor for the treatment of cancer |
CN116178374A (zh) * | 2023-01-13 | 2023-05-30 | 河北医科大学 | 小电导钙激活钾离子通道激动剂及其合成和应用 |
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SG11201605699QA (en) | 2016-08-30 |
CN106458996A (zh) | 2017-02-22 |
KR20160110506A (ko) | 2016-09-21 |
EA201691472A1 (ru) | 2017-05-31 |
EP3097092B1 (en) | 2020-08-26 |
JP2017505812A (ja) | 2017-02-23 |
US9828363B2 (en) | 2017-11-28 |
AU2015206292A1 (en) | 2016-08-18 |
CL2016001840A1 (es) | 2017-04-17 |
EA031317B1 (ru) | 2018-12-28 |
JP6387111B2 (ja) | 2018-09-05 |
CA2936559C (en) | 2019-03-12 |
TW201605833A (zh) | 2016-02-16 |
CN106458996B (zh) | 2020-11-03 |
EP3097092A1 (en) | 2016-11-30 |
US20180044325A1 (en) | 2018-02-15 |
IL246692A0 (en) | 2016-08-31 |
US10174005B2 (en) | 2019-01-08 |
AU2015206292B2 (en) | 2018-02-15 |
BR112016016421A2 (es) | 2017-08-08 |
IL246692B (en) | 2019-05-30 |
NZ722624A (en) | 2017-09-29 |
US20160332990A1 (en) | 2016-11-17 |
BR112016016421B1 (pt) | 2022-10-18 |
CA2936559A1 (en) | 2015-07-23 |
MX2016009465A (es) | 2016-12-02 |
ES2819867T3 (es) | 2021-04-19 |
WO2015109285A1 (en) | 2015-07-23 |
TWI640516B (zh) | 2018-11-11 |
ZA201605107B (en) | 2017-09-27 |
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