CO6260060A2 - 2-anilinopurin-8-onas como inhibidores de ttk/mps1 para el tratamiento de trastornos proliferativos - Google Patents
2-anilinopurin-8-onas como inhibidores de ttk/mps1 para el tratamiento de trastornos proliferativosInfo
- Publication number
- CO6260060A2 CO6260060A2 CO10033946A CO10033946A CO6260060A2 CO 6260060 A2 CO6260060 A2 CO 6260060A2 CO 10033946 A CO10033946 A CO 10033946A CO 10033946 A CO10033946 A CO 10033946A CO 6260060 A2 CO6260060 A2 CO 6260060A2
- Authority
- CO
- Colombia
- Prior art keywords
- 3alkyl
- cyclopropyl
- optionally substituted
- fluoro
- cyano
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 230000002062 proliferating effect Effects 0.000 title 1
- -1 chloro, bromo, cyano, methoxy, ethoxy, trifluoromethoxy, methyl Chemical group 0.000 abstract 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 5
- 125000001153 fluoro group Chemical group F* 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 125000003725 azepanyl group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 abstract 1
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 abstract 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000005678 ethenylene group Chemical group [H]C([*:1])=C([H])[*:2] 0.000 abstract 1
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000003551 oxepanyl group Chemical group 0.000 abstract 1
- 125000003566 oxetanyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 1
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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
1.- Un compuesto de fórmula (I):donde:R1 se selecciona entre C1-4alquilo, ciclopropilo, ciclopropilmetilo y ciclobutilo; donde dicho ciclopropilo puede estar opcionalmente sustituido por metilo; y donde R1 puede estar opcionalmente sustituido por uno o más R5; m es 0 ó 1; R2 se selecciona entre C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C3-6cicloalquilo, ciclopentenilo, ciclohexenilo, oxetanilo, tetrahidropiranilo, tetrahidrofuranilo, oxepanilo, azetidinilo, pirrolidinilo, piperidinilo y azepanilo; donde R2 puede estar opcionalmente sustituido en un carbono por uno o más R6; y donde si R2 contiene un resto -NH- en el anillo, dicho nitrógeno puede estar opcionalmente sustituido por R7;R3 se selecciona independientemente entre fluoro, cloro, bromo, ciano, metoxi, etoxi, trifluorometoxi, metilo, etilo, trifluorometilo, etenilo, etinilo, ciclopropilo, metiltio, etiltio, N-metilamino, N,N-dimetilamino, amino y metilsulfoniloxi; n es un número entero seleccionado entre 0 y 3; donde los valores de R3 pueden ser los mismos o diferentes; R4 es -L-R8 o R9; L se selecciona entre etinileno, etenileno, ciclopropilo y -X-C1-2alquileno-; donde X es un enlace directo, -O, -S-, -NH-, -OS(O)2-, -N(CH3)- o -N(CH2R10)-; y donde L puede estar opcionalmente sustituido en un carbono por uno o más fluoro; R5 es ciano o fluoro; R6 se selecciona entre C1-3alquilo, C1-3alcoxi, N-(C1-3alquil)amino, N,N-(C1-3alquil)2amino, hidroxi, amino, fluoro y ciano; R7 se selecciona entre C1-3alquilo, ciclopropilo, C1-3alcanoílo y C1-3alquilsulfonilo;R8 y R10 se seleccionan cada uno independientemente entre cloro, bromo, yodo, ciano, ...
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95750807P | 2007-08-23 | 2007-08-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6260060A2 true CO6260060A2 (es) | 2011-03-22 |
Family
ID=39951669
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO10033946A CO6260060A2 (es) | 2007-08-23 | 2010-03-23 | 2-anilinopurin-8-onas como inhibidores de ttk/mps1 para el tratamiento de trastornos proliferativos |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20110118238A1 (es) |
| EP (1) | EP2212326A1 (es) |
| JP (1) | JP2010536841A (es) |
| KR (1) | KR20100057650A (es) |
| CN (1) | CN103298814A (es) |
| AU (1) | AU2008290330A1 (es) |
| BR (1) | BRPI0815709A2 (es) |
| CA (1) | CA2696200A1 (es) |
| CO (1) | CO6260060A2 (es) |
| CR (1) | CR11295A (es) |
| DO (1) | DOP2010000064A (es) |
| EA (1) | EA201000341A1 (es) |
| EC (1) | ECSP10010034A (es) |
| MX (1) | MX2010002115A (es) |
| NI (1) | NI201000032A (es) |
| NZ (1) | NZ584138A (es) |
| SV (1) | SV2010003491A (es) |
| WO (1) | WO2009024824A1 (es) |
| ZA (1) | ZA201001193B (es) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080119496A1 (en) * | 2006-11-16 | 2008-05-22 | Pharmacopeia Drug Discovery, Inc. | 7-Substituted Purine Derivatives for Immunosuppression |
| TW201107329A (en) | 2009-07-30 | 2011-03-01 | Oncotherapy Science Inc | Fused imidazole derivative having ttk inhibitory action |
| EP2343294A1 (en) * | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Substituted triazolopyridines |
| EP2343295A1 (en) * | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridine derivates |
| EP2343297A1 (en) * | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridines |
| FR2955109B1 (fr) | 2010-01-08 | 2012-09-07 | Sanofi Aventis | Derives de 5-oxo-5,8-dihydro-pyrido[2, 3-d]pyrimidine, leur preparation et leur application en therapeutique |
| UY33452A (es) | 2010-06-16 | 2012-01-31 | Bayer Schering Pharma Ag | Triazolopiridinas sustituidas |
| UY33539A (es) * | 2010-08-02 | 2012-02-29 | Astrazeneca Ab | Compuestos químicos alk |
| EP2651946B1 (en) * | 2010-12-17 | 2015-05-27 | Bayer Intellectual Property GmbH | 2-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| US9284317B2 (en) * | 2010-12-17 | 2016-03-15 | Bayer Intellectual Property Gmbh | Substituted imidazo[1,2-a]pyrazines as MPS-1 inhibitors |
| EP2651948A1 (en) * | 2010-12-17 | 2013-10-23 | Bayer Intellectual Property GmbH | Imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment hyperproliferative disorders |
| EP2651950A1 (en) * | 2010-12-17 | 2013-10-23 | Bayer Intellectual Property GmbH | 6 substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| EP2651945A1 (en) * | 2010-12-17 | 2013-10-23 | Bayer Intellectual Property GmbH | 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| WO2012080228A1 (en) * | 2010-12-17 | 2012-06-21 | Bayer Pharma Aktiengesellschaft | 6-thio-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| EA023766B1 (ru) | 2011-04-21 | 2016-07-29 | Байер Интеллектчуал Проперти Гмбх | Триазолопиридины |
| WO2012160029A1 (en) | 2011-05-23 | 2012-11-29 | Bayer Intellectual Property Gmbh | Substituted triazolopyridines |
| UA112096C2 (uk) | 2011-12-12 | 2016-07-25 | Байєр Інтеллектуал Проперті Гмбх | Заміщені триазолопіридини та їх застосування як інгібіторів ttk |
| CN104284896B (zh) | 2012-03-14 | 2016-06-01 | 拜耳知识产权有限责任公司 | 取代的咪唑并哒嗪 |
| JP6238979B2 (ja) | 2012-07-10 | 2017-11-29 | バイエル・ファルマ・アクティエンゲゼルシャフト | 置換トリアゾロピリジンを調製する方法 |
| WO2014020043A1 (en) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer |
| EP3004092B1 (en) * | 2013-06-07 | 2017-03-22 | Bayer Pharma Aktiengesellschaft | Substituted triazolopyridines |
| AP2015008898A0 (en) | 2013-06-11 | 2015-12-31 | Bayer Pharma AG | Prodrug derivatives of substituted triazolopyridines |
| GB201403536D0 (en) * | 2014-02-28 | 2014-04-16 | Cancer Rec Tech Ltd | Inhibitor compounds |
| HUE064630T2 (hu) | 2015-04-17 | 2024-04-28 | Crossfire Oncology Holding B V | Prognosztikai biomarkerek TTK-inhibitoros kemoterápiához |
| PL3558997T3 (pl) | 2016-12-20 | 2021-07-19 | Astrazeneca Ab | Związki amino-triazolopirydyny i ich zastosowanie w leczeniu nowotworu złośliwego |
| ES2909234T3 (es) * | 2016-12-21 | 2022-05-05 | Ono Pharmaceutical Co | Compuestos de 6-amino-7,9-dihidro-8H-purin-8-ona como inhibidores de Brk |
| TWI820146B (zh) * | 2018-06-15 | 2023-11-01 | 瑞典商阿斯特捷利康公司 | 嘌呤酮化合物及其在治療癌症中之用途 |
| BR112021017829A2 (pt) * | 2019-03-13 | 2021-11-30 | Voronoi Inc | Composto, e, composição farmacêutica para uso em prevenir ou tratar câncer |
| BR112022020962A2 (pt) * | 2020-04-17 | 2022-12-06 | Chengdu Baiyu Pharmaceutical Co Ltd | Derivados de imidazolidinona e uso médico dos mesmos |
| KR102409595B1 (ko) * | 2020-06-29 | 2022-06-17 | 한국과학기술연구원 | 단백질 카이네이즈 csf-1r 억제제로서의 신규 퓨리논 유도체 |
| CZ309356B6 (cs) * | 2020-09-15 | 2022-09-28 | Ústav experimentální botaniky AV ČR, v. v. i | Substituované purinové sloučeniny jako inhibitory proteinkináz, jejich použití jako léčiva a farmaceutické přípravky obsahující tyto deriváty |
| TW202241901A (zh) * | 2020-12-21 | 2022-11-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 嘌呤酮衍生物、其製備方法及其在醫藥上的應用 |
| WO2022199547A1 (zh) * | 2021-03-22 | 2022-09-29 | 成都赜灵生物医药科技有限公司 | 一种7,9-二氢嘌呤衍生物及其制药用途 |
| WO2023025160A1 (zh) * | 2021-08-23 | 2023-03-02 | 成都百裕制药股份有限公司 | 一种咪唑啉酮衍生物的制备工艺及其中间体 |
| MX2024003693A (es) * | 2021-09-23 | 2024-04-09 | Chengdu Baiyu Pharmaceutical Co Ltd | Forma cristalina del derivado de imidazolinona. |
| CN120129524A (zh) * | 2022-07-13 | 2025-06-10 | 成都百裕制药股份有限公司 | 咪唑啉酮衍生物在联合放疗治疗肿瘤中的应用 |
| CN120129526A (zh) * | 2022-07-20 | 2025-06-10 | 成都百裕制药股份有限公司 | 咪唑啉酮衍生物联合多柔比星在治疗肿瘤中的应用 |
| IL321403A (en) * | 2022-12-13 | 2025-08-01 | Kangbaida Sichuan Biotechnology Co Ltd | Pharmaceutical preparation of imidazolinone compound, preparation method therefor, and use thereof |
| TW202513059A (zh) * | 2023-09-21 | 2025-04-01 | 大陸商成都百裕製藥股份有限公司 | 咪唑啉酮衍生物在製備用於聯合放療治療腫瘤的藥物中的應用及治療方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006205851A1 (en) * | 2005-01-14 | 2006-07-20 | Janssen Pharmaceutica N.V. | 5-membered annelated heterocyclic pyrimidines as kinase inhibitors |
| WO2006091737A1 (en) * | 2005-02-24 | 2006-08-31 | Kemia, Inc. | Modulators of gsk-3 activity |
| JO3235B1 (ar) * | 2006-05-26 | 2018-03-08 | Astex Therapeutics Ltd | مركبات بيررولوبيريميدين و استعمالاتها |
-
2008
- 2008-08-20 NZ NZ584138A patent/NZ584138A/en not_active IP Right Cessation
- 2008-08-20 WO PCT/GB2008/050724 patent/WO2009024824A1/en not_active Ceased
- 2008-08-20 EP EP08788695A patent/EP2212326A1/en not_active Withdrawn
- 2008-08-20 EA EA201000341A patent/EA201000341A1/ru unknown
- 2008-08-20 MX MX2010002115A patent/MX2010002115A/es not_active Application Discontinuation
- 2008-08-20 AU AU2008290330A patent/AU2008290330A1/en not_active Abandoned
- 2008-08-20 KR KR1020107006059A patent/KR20100057650A/ko not_active Withdrawn
- 2008-08-20 JP JP2010521487A patent/JP2010536841A/ja active Pending
- 2008-08-20 CA CA2696200A patent/CA2696200A1/en not_active Abandoned
- 2008-08-20 CN CN200880113474XA patent/CN103298814A/zh active Pending
- 2008-08-20 BR BRPI0815709A patent/BRPI0815709A2/pt not_active IP Right Cessation
- 2008-08-20 US US12/674,749 patent/US20110118238A1/en not_active Abandoned
-
2010
- 2010-02-18 ZA ZA201001193A patent/ZA201001193B/xx unknown
- 2010-02-23 DO DO2010000064A patent/DOP2010000064A/es unknown
- 2010-02-23 CR CR11295A patent/CR11295A/es not_active Application Discontinuation
- 2010-02-23 NI NI201000032A patent/NI201000032A/es unknown
- 2010-02-23 SV SV2010003491A patent/SV2010003491A/es not_active Application Discontinuation
- 2010-03-12 EC EC2010010034A patent/ECSP10010034A/es unknown
- 2010-03-23 CO CO10033946A patent/CO6260060A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009024824A1 (en) | 2009-02-26 |
| MX2010002115A (es) | 2010-06-01 |
| JP2010536841A (ja) | 2010-12-02 |
| ZA201001193B (en) | 2010-10-27 |
| EA201000341A1 (ru) | 2010-10-29 |
| CR11295A (es) | 2010-05-28 |
| DOP2010000064A (es) | 2010-03-31 |
| KR20100057650A (ko) | 2010-05-31 |
| US20110118238A1 (en) | 2011-05-19 |
| NI201000032A (es) | 2010-12-07 |
| EP2212326A1 (en) | 2010-08-04 |
| NZ584138A (en) | 2011-10-28 |
| AU2008290330A1 (en) | 2009-02-26 |
| CA2696200A1 (en) | 2009-02-26 |
| ECSP10010034A (es) | 2010-04-30 |
| CN103298814A (zh) | 2013-09-11 |
| BRPI0815709A2 (pt) | 2017-06-13 |
| SV2010003491A (es) | 2010-07-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Application withdrawn |