CU20170029A7 - Indazoles sustituidos con bencilo en calidad de inhibidores de bub1, útiles para el tratamiento o profilaxis de una enfermedad hiperproliferativa y/o un trastorno que responde a la inducción de la muerte celular, un procedimiento para la preparación de estos compuestos, y compuestos intermediarios - Google Patents
Indazoles sustituidos con bencilo en calidad de inhibidores de bub1, útiles para el tratamiento o profilaxis de una enfermedad hiperproliferativa y/o un trastorno que responde a la inducción de la muerte celular, un procedimiento para la preparación de estos compuestos, y compuestos intermediariosInfo
- Publication number
- CU20170029A7 CU20170029A7 CUP2017000029A CU20170029A CU20170029A7 CU 20170029 A7 CU20170029 A7 CU 20170029A7 CU P2017000029 A CUP2017000029 A CU P2017000029A CU 20170029 A CU20170029 A CU 20170029A CU 20170029 A7 CU20170029 A7 CU 20170029A7
- Authority
- CU
- Cuba
- Prior art keywords
- composition
- preparation
- disorder
- induction
- useful
- Prior art date
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 4
- 238000002360 preparation method Methods 0.000 title abstract 3
- 230000030833 cell death Effects 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title abstract 2
- 230000003463 hyperproliferative effect Effects 0.000 title abstract 2
- 230000006698 induction Effects 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 238000011282 treatment Methods 0.000 title abstract 2
- 101000896657 Homo sapiens Mitotic checkpoint serine/threonine-protein kinase BUB1 Proteins 0.000 title 1
- 102100021691 Mitotic checkpoint serine/threonine-protein kinase BUB1 Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 101100326430 Caenorhabditis elegans bub-1 gene Proteins 0.000 abstract 1
- 206010013710 Drug interaction Diseases 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
Classifications
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
<p>Se describen compuestos de fórmula (I)</p> <p>ESPACIO PARA FÓRMULA</p> <p>útiles para el tratamiento o profilaxis de una enfermedad hiperproliferativa y/o un trastorno que responde a la inducción de la muerte celular tal como un tumor hematológico, un tumor sólido y/o metástasis de los mismos. Tambien se describe un procedimiento para la preparación de estos compuestos, y los compuestos intermedios que se utilizan en dicho procedimiento de preparación. Los nuevos compuestos de la invención presentan propiedades farmacológicas mejoradas, en particular una potencia mejorada de la inhibición del objetivo Bub1, una inhibición más potente de la proliferación y/o interacciones fármaco reducidas cuando se utilizan en combinación con otros fármacos.</p>
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14185604 | 2014-09-19 | ||
| EP15176903 | 2015-07-15 | ||
| PCT/EP2015/071340 WO2016042084A1 (en) | 2014-09-19 | 2015-09-17 | Benzyl substituted indazoles as bub1 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CU20170029A7 true CU20170029A7 (es) | 2017-08-08 |
Family
ID=54140475
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CUP2017000029A CU20170029A7 (es) | 2014-09-19 | 2015-09-17 | Indazoles sustituidos con bencilo en calidad de inhibidores de bub1, útiles para el tratamiento o profilaxis de una enfermedad hiperproliferativa y/o un trastorno que responde a la inducción de la muerte celular, un procedimiento para la preparación de estos compuestos, y compuestos intermediarios |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US10350206B2 (es) |
| EP (1) | EP3194379A1 (es) |
| JP (1) | JP6664385B2 (es) |
| KR (1) | KR20170049604A (es) |
| CN (1) | CN107001331A (es) |
| AP (1) | AP2017009803A0 (es) |
| AU (1) | AU2015316796A1 (es) |
| BR (1) | BR112017005444A2 (es) |
| CA (1) | CA2961589A1 (es) |
| CL (1) | CL2017000654A1 (es) |
| CO (1) | CO2017002532A2 (es) |
| CR (1) | CR20170100A (es) |
| CU (1) | CU20170029A7 (es) |
| DO (1) | DOP2017000078A (es) |
| EA (1) | EA032401B1 (es) |
| EC (1) | ECSP17016797A (es) |
| IL (1) | IL251071A0 (es) |
| MA (1) | MA39484A (es) |
| MX (1) | MX2017003664A (es) |
| NI (1) | NI201700034A (es) |
| PE (1) | PE20170697A1 (es) |
| PH (1) | PH12017500509A1 (es) |
| SG (1) | SG11201702082VA (es) |
| TN (1) | TN2017000092A1 (es) |
| TW (1) | TW201615636A (es) |
| UY (1) | UY36311A (es) |
| WO (1) | WO2016042084A1 (es) |
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| UA111754C2 (uk) | 2011-10-06 | 2016-06-10 | Байєр Фарма Акцієнгезелльшафт | Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| US9745285B2 (en) | 2013-06-21 | 2017-08-29 | Bayer Pharma Aktiengesellschaft | Heteroaryl substituted pyrazoles |
| WO2014202590A1 (en) | 2013-06-21 | 2014-12-24 | Bayer Pharma Aktiengesellschaft | Substituted benzylpyrazoles |
| CN105764893A (zh) | 2013-10-30 | 2016-07-13 | 拜耳制药股份公司 | 杂芳基取代的吡唑 |
| RU2685230C2 (ru) | 2014-02-06 | 2019-04-17 | Хептарес Терапьютикс Лимитед | Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов |
| TW201613886A (en) | 2014-06-17 | 2016-04-16 | Bayer Pharma AG | 3-amino-1,5,6,7-tetrahydro-4h-indol-4-ones |
| WO2016042084A1 (en) | 2014-09-19 | 2016-03-24 | Bayer Pharma Aktiengesellschaft | Benzyl substituted indazoles as bub1 inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| WO2018122168A1 (en) | 2016-12-29 | 2018-07-05 | Bayer Pharma Aktiengesellschaft | Combinations of bub1 kinase and parp inhibitors |
| WO2018158175A1 (en) | 2017-02-28 | 2018-09-07 | Bayer Pharma Aktiengesellschaft | Combination of bub1 inhibitors |
| KR102615821B1 (ko) | 2017-04-11 | 2023-12-21 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 불소-치환된 인다졸 화합물 및 이의 용도 |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| WO2018215282A1 (en) | 2017-05-26 | 2018-11-29 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and pi3k inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| MX2022006691A (es) | 2019-12-04 | 2022-09-19 | Incyte Corp | Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr). |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
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2015
- 2015-09-17 WO PCT/EP2015/071340 patent/WO2016042084A1/en not_active Ceased
- 2015-09-17 SG SG11201702082VA patent/SG11201702082VA/en unknown
- 2015-09-17 AP AP2017009803A patent/AP2017009803A0/en unknown
- 2015-09-17 MA MA039484A patent/MA39484A/fr unknown
- 2015-09-17 US US15/512,494 patent/US10350206B2/en not_active Expired - Fee Related
- 2015-09-17 CN CN201580062951.4A patent/CN107001331A/zh active Pending
- 2015-09-17 EA EA201790649A patent/EA032401B1/ru not_active IP Right Cessation
- 2015-09-17 TN TN2017000092A patent/TN2017000092A1/en unknown
- 2015-09-17 EP EP15763619.2A patent/EP3194379A1/en not_active Withdrawn
- 2015-09-17 KR KR1020177010425A patent/KR20170049604A/ko not_active Withdrawn
- 2015-09-17 CU CUP2017000029A patent/CU20170029A7/es unknown
- 2015-09-17 MX MX2017003664A patent/MX2017003664A/es unknown
- 2015-09-17 CR CR20170100A patent/CR20170100A/es unknown
- 2015-09-17 AU AU2015316796A patent/AU2015316796A1/en not_active Abandoned
- 2015-09-17 BR BR112017005444A patent/BR112017005444A2/pt not_active IP Right Cessation
- 2015-09-17 CA CA2961589A patent/CA2961589A1/en not_active Abandoned
- 2015-09-17 JP JP2017514825A patent/JP6664385B2/ja not_active Expired - Fee Related
- 2015-09-17 PE PE2017000480A patent/PE20170697A1/es unknown
- 2015-09-18 UY UY0001036311A patent/UY36311A/es not_active Application Discontinuation
- 2015-09-18 TW TW104131025A patent/TW201615636A/zh unknown
-
2017
- 2017-03-09 IL IL251071A patent/IL251071A0/en unknown
- 2017-03-16 PH PH12017500509A patent/PH12017500509A1/en unknown
- 2017-03-17 NI NI201700034A patent/NI201700034A/es unknown
- 2017-03-17 DO DO2017000078A patent/DOP2017000078A/es unknown
- 2017-03-17 CL CL2017000654A patent/CL2017000654A1/es unknown
- 2017-03-17 EC ECIEPI201716797A patent/ECSP17016797A/es unknown
- 2017-03-17 CO CONC2017/0002532A patent/CO2017002532A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN107001331A (zh) | 2017-08-01 |
| US10350206B2 (en) | 2019-07-16 |
| MA39484A (fr) | 2016-03-24 |
| KR20170049604A (ko) | 2017-05-10 |
| EA201790649A1 (ru) | 2017-09-29 |
| CR20170100A (es) | 2017-04-24 |
| PH12017500509A1 (en) | 2017-08-30 |
| AP2017009803A0 (en) | 2017-03-31 |
| US20170273980A1 (en) | 2017-09-28 |
| TN2017000092A1 (en) | 2018-07-04 |
| BR112017005444A2 (pt) | 2018-04-24 |
| WO2016042084A1 (en) | 2016-03-24 |
| CL2017000654A1 (es) | 2017-12-11 |
| EA032401B1 (ru) | 2019-05-31 |
| SG11201702082VA (en) | 2017-04-27 |
| IL251071A0 (en) | 2017-04-30 |
| JP2017530962A (ja) | 2017-10-19 |
| UY36311A (es) | 2016-04-29 |
| CA2961589A1 (en) | 2016-03-24 |
| PE20170697A1 (es) | 2017-06-24 |
| ECSP17016797A (es) | 2017-05-31 |
| DOP2017000078A (es) | 2017-06-30 |
| MX2017003664A (es) | 2017-07-13 |
| NI201700034A (es) | 2017-06-16 |
| TW201615636A (zh) | 2016-05-01 |
| JP6664385B2 (ja) | 2020-03-13 |
| AU2015316796A1 (en) | 2017-03-30 |
| CO2017002532A2 (es) | 2017-07-11 |
| EP3194379A1 (en) | 2017-07-26 |
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