AR106297A1 - Compuestos macrocíclicos modificados como inhibidores selectivos de la quinasa cdk9 - Google Patents
Compuestos macrocíclicos modificados como inhibidores selectivos de la quinasa cdk9Info
- Publication number
- AR106297A1 AR106297A1 ARP160103078A ARP160103078A AR106297A1 AR 106297 A1 AR106297 A1 AR 106297A1 AR P160103078 A ARP160103078 A AR P160103078A AR P160103078 A ARP160103078 A AR P160103078A AR 106297 A1 AR106297 A1 AR 106297A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- acetylamino
- cycloalkyl
- heteroaryl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/02—Formic acid
- C07C53/06—Salts thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D515/08—Bridged systems
Abstract
Compuestos macrocíclicos modificados y métodos para su preparación, a su uso para el tratamiento y/o la prevención de trastornos, en particular de trastornos hiperproliferativos y/o enfermedades infecciosas viralmente inducidas y/o de enfermedades cardiovasculares. También se refiere a compuestos intermediarios útiles en la preparación de dichos compuestos. Reivindicación 1: Un compuesto de la fórmula general (1), en donde A representa un resto bivalente seleccionado del grupo que consiste en -S-, -S(=O)-, -S(=O)₂-, -S(=O)(=NR⁵)-; G, E representan, de modo independiente entre sí, un resto bivalente seleccionado del grupo que consiste en -O-, -N(RA)-, -CH₂-, -CH(alquilo C₁₋₆), -C(alquilo C₁₋₆)₂-, -S-, -S(=O)-, -S(=O)₂-, siempre que al menos uno de dichos restos bivalentes G y E sea diferente de -O-; L representa un resto de alquileno C₂₋₈, en donde dicho resto está opcionalmente sustituido con (i) un sustituyente seleccionado de hidroxi, -NR⁶R⁷, alquenilo C₂₋₃, alquinilo C₂₋₃, cicloalquilo C₃₋₄, hidroxi-alquilo C₁₋₃, -(CH₂)NR⁶R⁷, y/o (ii) uno o dos o tres o cuatro sustituyentes, iguales o diferentes, seleccionados de halógeno y alquilo C₁₋₃, o en donde un átomo de carbono de dicho resto de alquileno C₂₋₈ forma un anillo de tres o cuatro miembros junto con un resto bivalente al que está unido, en donde dicho resto bivalente se selecciona de -CH₂CH₂-, -CH₂CH₂CH₂-, -CH₂OCH₂-; X, Y representan CH o N siempre que uno de X e Y represente CH y uno de X e Y represente N; R¹ representa un grupo seleccionado de alquilo C₁₋₆, alquenilo C₃₋₆, alquinilo C₃₋₆, cicloalquilo C₃₋₇, heterociclilo, fenilo, heteroarilo, fenil-alquilo C₁₋₃ y heteroaril-alquilo C₁₋₃, en donde dicho grupo está opcionalmente sustituido con uno o dos o tres sustituyentes, iguales o diferentes, seleccionados del grupo que consiste en hidroxi, ciano, halógeno, alquilo C₁₋₆, halo-alquilo C₁₋₃, alcoxi C₁₋₆, fluoroalcoxi C₁₋₃, -NH₂, alquilamino, dialquilamino, acetilamino, N-metil-N-acetilamino, aminas cíclicas, -OP(=O)(OH)₂, -C(=O)OH, -C(=O)NH₂; R² representa un grupo seleccionado de un átomo de hidrógeno, un átomo de flúor, un átomo de cloro, un átomo de bromo, ciano, alquilo C₁₋₃, alcoxi C₁₋₃, halo-alquilo C₁₋₃, fluoroalcoxi C₁₋₃; R³, R⁴ representan, de modo independiente entre sí, un grupo seleccionado de un átomo de hidrógeno, un átomo de flúor, un átomo de cloro, un átomo de bromo, ciano, alquilo C₁₋₃, alcoxi C₁₋₃, halo-alquilo C₁₋₃, fluoroalcoxi C₁₋₃; R⁵ representa un grupo seleccionado de un átomo de hidrógeno, ciano, -C(=O)R⁸, -C(=O)OR⁸, -S(=O)₂R⁸, -C(=O)NR⁶R⁷, alquilo C₁₋₆, cicloalquilo C₃₋₇, heterociclilo, fenilo, heteroarilo, en donde dicho grupo alquilo C₁₋₆, cicloalquilo C₃₋₇, heterociclilo, fenilo o heteroarilo está opcionalmente sustituido con uno, dos o tres sustituyentes, iguales o diferentes, seleccionados del grupo que consiste en halógeno, hidroxi, ciano, alquilo C₁₋₃, alcoxi C₁₋₃, -NH₂, alquilamino, dialquilamino, acetilamino, N-metil-N-acetilamino, aminas cíclicas, halo-alquilo C₁₋₃, fluoroalcoxi C₁₋₃; R⁶, R⁷ representan, de modo independiente entre sí, un grupo seleccionado de un átomo de hidrógeno, alquilo C₁₋₆, cicloalquilo C₃₋₇, heterociclilo, fenilo, bencilo y heteroarilo, en donde dicho grupo alquilo C₁₋₆, cicloalquilo C₃₋₇, heterociclilo, fenilo, bencilo o heteroarilo está opcionalmente sustituido con uno, dos o tres sustituyentes, iguales o diferentes, seleccionados del grupo que consiste en halógeno, hidroxi, alquilo C₁₋₃, alcoxi C₁₋₃, -NH₂, alquilamino, dialquilamino, acetilamino, N-metil-N-acetilamino, aminas cíclicas, halo-alquilo C₁₋₃, fluoroalcoxi C₁₋₃, o R⁶ y R⁷, junto con el átomo de nitrógeno al que están unidos, forman una amina cíclica; R⁸ representa un grupo seleccionado de alquilo C₁₋₆, halo-alquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo, fenilo, bencilo y heteroarilo, en donde dicho grupo está opcionalmente sustituido con uno, dos o tres sustituyentes, iguales o diferentes, seleccionados del grupo que consiste en halógeno, hidroxi, alquilo C₁₋₃, alcoxi C₁₋₃, -NH₂, alquilamino, dialquilamino, acetilamino, N-metil-N-acetilamino, aminas cíclicas, halo-alquilo C₁₋₃, fluoroalcoxi C₁₋₃; RA representa un átomo de hidrógeno o un grupo alquilo C₁₋₆; o uno de sus enantiómeros, diastereómeros, sales, solvatos o sales de solvatos. Reivindicación 14: Un compuesto de la fórmula general (2) en donde R¹, R², R³, R⁴ y L son como se definen de acuerdo con cualquiera de las reivindicaciones 1 a 10 para el compuesto de la fórmula general (1), o uno de sus enantiómeros, diastereómeros, sales, solvatos o sales de solvatos. Reivindicación 15: Un compuesto de la fórmula general (3) en donde R¹, R², R³, R⁴, RA y L son como se definen de acuerdo con cualquiera de las reivindicaciones 1 a 10 para el compuesto de la fórmula general (1), o uno de sus enantiómeros, diastereómeros, sales, solvatos o sales de solvatos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP15188914 | 2015-10-08 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR106297A1 true AR106297A1 (es) | 2018-01-03 |
Family
ID=54288713
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160103078A AR106297A1 (es) | 2015-10-08 | 2016-10-07 | Compuestos macrocíclicos modificados como inhibidores selectivos de la quinasa cdk9 |
Country Status (10)
Country | Link |
---|---|
US (1) | US10214542B2 (es) |
EP (1) | EP3359544B1 (es) |
JP (1) | JP6888000B2 (es) |
CN (1) | CN108368129B (es) |
AR (1) | AR106297A1 (es) |
CA (1) | CA3001085A1 (es) |
ES (1) | ES2819869T3 (es) |
TW (1) | TW201718585A (es) |
UY (1) | UY36938A (es) |
WO (1) | WO2017060167A1 (es) |
Families Citing this family (7)
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US11254690B2 (en) | 2017-03-28 | 2022-02-22 | Bayer Pharma Aktiengesellschaft | PTEFb inhibiting macrocyclic compounds |
CA3057891A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
WO2020151682A1 (zh) * | 2019-01-23 | 2020-07-30 | 成都先导药物开发股份有限公司 | 一种大环类免疫调节剂 |
CN112321604A (zh) * | 2019-08-05 | 2021-02-05 | 华东理工大学 | 大环类jak2抑制剂及其应用 |
CN113603708B (zh) * | 2021-07-27 | 2023-08-11 | 中国药科大学 | 一种具有大环骨架结构的cdk9抑制剂的制备及其应用 |
WO2023229430A1 (ko) * | 2022-05-27 | 2023-11-30 | 보로노이 주식회사 | 헤테로아릴 유도체 화합물 및 이의 용도 |
CN117964628A (zh) * | 2022-10-24 | 2024-05-03 | 科辉智药生物科技(深圳)有限公司 | 作为cdk9抑制剂的大环类化合物及其应用 |
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2016
- 2016-09-30 JP JP2018517543A patent/JP6888000B2/ja active Active
- 2016-09-30 CN CN201680071824.5A patent/CN108368129B/zh active Active
- 2016-09-30 CA CA3001085A patent/CA3001085A1/en active Pending
- 2016-09-30 WO PCT/EP2016/073399 patent/WO2017060167A1/en active Application Filing
- 2016-09-30 US US15/764,289 patent/US10214542B2/en active Active
- 2016-09-30 EP EP16774683.3A patent/EP3359544B1/en active Active
- 2016-09-30 ES ES16774683T patent/ES2819869T3/es active Active
- 2016-10-05 TW TW105132216A patent/TW201718585A/zh unknown
- 2016-10-07 UY UY0001036938A patent/UY36938A/es not_active Application Discontinuation
- 2016-10-07 AR ARP160103078A patent/AR106297A1/es unknown
Also Published As
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CN108368129A (zh) | 2018-08-03 |
US10214542B2 (en) | 2019-02-26 |
EP3359544B1 (en) | 2020-08-12 |
EP3359544A1 (en) | 2018-08-15 |
JP6888000B2 (ja) | 2021-06-16 |
US20180282346A1 (en) | 2018-10-04 |
UY36938A (es) | 2017-05-31 |
CA3001085A1 (en) | 2017-04-13 |
TW201718585A (zh) | 2017-06-01 |
CN108368129B (zh) | 2021-08-17 |
ES2819869T3 (es) | 2021-04-19 |
JP2018532735A (ja) | 2018-11-08 |
WO2017060167A1 (en) | 2017-04-13 |
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