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
- 150000002678 macrocyclic compounds Chemical class 0.000 title abstract 2
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 title 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 title 1
- 229940124639 Selective inhibitor Drugs 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 12
- -1 -NR6R7 Chemical group 0.000 abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 150000001875 compounds Chemical class 0.000 abstract 6
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 6
- 239000012453 solvate Chemical class 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 4
- 125000003282 alkyl amino group Chemical group 0.000 abstract 4
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 2
- 229910052794 bromium Inorganic materials 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 abstract 1
- 125000006593 (C2-C3) alkynyl group Chemical group 0.000 abstract 1
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Catalysts (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3601236A1 (en) | 2017-03-28 | 2020-02-05 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| US11254690B2 (en) | 2017-03-28 | 2022-02-22 | Bayer Pharma Aktiengesellschaft | 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 |
| CN120417944A (zh) | 2022-11-28 | 2025-08-01 | 诺华股份有限公司 | Pcta衍生物、其缀合物及其用途 |
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| JP5982490B2 (ja) | 2011-09-16 | 2016-08-31 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 二置換５−フルオロ−ピリミジン |
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-
2016
- 2016-09-30 CA CA3001085A patent/CA3001085A1/en active Pending
- 2016-09-30 ES ES16774683T patent/ES2819869T3/es active Active
- 2016-09-30 WO PCT/EP2016/073399 patent/WO2017060167A1/en not_active Ceased
- 2016-09-30 CN CN201680071824.5A patent/CN108368129B/zh not_active Expired - Fee Related
- 2016-09-30 EP EP16774683.3A patent/EP3359544B1/en active Active
- 2016-09-30 US US15/764,289 patent/US10214542B2/en active Active
- 2016-09-30 JP JP2018517543A patent/JP6888000B2/ja not_active Expired - Fee Related
- 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
| Publication number | Publication date |
|---|---|
| JP2018532735A (ja) | 2018-11-08 |
| EP3359544B1 (en) | 2020-08-12 |
| CA3001085A1 (en) | 2017-04-13 |
| ES2819869T3 (es) | 2021-04-19 |
| UY36938A (es) | 2017-05-31 |
| WO2017060167A1 (en) | 2017-04-13 |
| TW201718585A (zh) | 2017-06-01 |
| EP3359544A1 (en) | 2018-08-15 |
| CN108368129B (zh) | 2021-08-17 |
| JP6888000B2 (ja) | 2021-06-16 |
| US20180282346A1 (en) | 2018-10-04 |
| CN108368129A (zh) | 2018-08-03 |
| US10214542B2 (en) | 2019-02-26 |
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