AR072084A1 - Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim - Google Patents
Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pimInfo
- Publication number
- AR072084A1 AR072084A1 ARP090102077A ARP090102077A AR072084A1 AR 072084 A1 AR072084 A1 AR 072084A1 AR P090102077 A ARP090102077 A AR P090102077A AR P090102077 A ARP090102077 A AR P090102077A AR 072084 A1 AR072084 A1 AR 072084A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- optionally
- optionally mono
- heteroaryl
- mono
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
Abstract
Utilizacion en terapeutica para el tratamiento del c ncer y procedimientos de s¡ntesis. Se proveen adem s, composiciones farmaceuticas que las contienen e intermediarios para su preparacion. Reivindicacion 1: Compuestos de formula general (1) siguiente; en la que -R3, R4 pueden ser independientemente el uno del otro: 1. H; 2. halogeno; 3. CF3; 4. oxi sustituido; 5. alcoxi opcionalmente sustituido; 6. amino opcionalmente sustituido; 7. carbonilo sustituido; 8. carbonilo opcionalmente sustituido; 9. amida opcionalmente sustituida; 10. azufre con diferentes grados de oxidacion (II o IV o VI) tales como los sulfuros, sulfoxidos o sulfonas opcionalmente sustituidos; 11. alquilo C1-10 lineal, ramificado o c¡clico que contiene opcionalmente un hetero tomo opcionalmente sustituido; 12. alquenilo C2-7 lineal, ramificado o c¡clico opcionalmente sustituido; 13. alquinilo C2-6 lineal o ramificado opcionalmente sustituido; 14. arilo o heteroarilo opcionalmente sustituido; 15. heterociloalquilo opcionalmente sustituido; - siendo R6 un heteroarilo (5 o 6 eslabones con 1 a 4 hetero tomos elegidos entre N, S o O) unido al resto azacarbolina bien con un C bien con un N que pertenece a R6, estando R6 opcionalmente sustituido; pudiendo igualmente representar R6 C(O)NR1aR1b o un heterocicloalquilo opcionalmente sustituido o -C(O)heterocicloalquilo opcionalmente sustituido, tal que R1a y R1b pueden ser independientemente el uno del otro: 1. H; 2. alquilo C1-10 lineal o ramificado o c¡clico (C3-7) opcionalmente mono o di sustituido; 3. alquenilo C2-6 lineal o ramificado opcionalmente mono o di sustituido; 4. alquinilo C2-6 lineal o ramificado opcionalmente mono o di sustituido; 5. arilo opcionalmente mono o di sustituido; 6. heteroarilo opcionalmente mono o di sustituido; 7. bencilo opcionalmente mono o di sustituido; 8. COalquilo opcionalmente mono o di sustituido; 9. COarilo opcionalmente mono o di sustituido; 10. COheteroarilo opcionalmente mono o di sustituido; 11. CO2alquilo opcionalmente mono o di sustituido; 12. CO2arilo opcionalmente mono o di sustituido; 13. CO2heteroarilo opcionalmente mono o di sustituido; 14. CONH2; 15. CONHalquilo opcionalmente mono o di sustituido; 16. CONHarilo opcionalmente mono o di sustituido; 17. CONHheteroarilo opcionalmente mono o di sustituido; 18. CON(alquilo)2 opcionalmente mono o di sustituido; 19. CON(arilo)2 opcionalmente mono o di sustituido; 2. CON(heteroarilo)2 opcionalmente mono o di sustituido; estando dichos productos de formula 1 en el estado de base o de sal de adicion a un cido. Reivindicacion 15: Como productos industriales nuevos, los intermedios de s¡ntesis (2); en los que los sustituyentes R3, R4 tienen los significados indicados en una cualquiera de las reivindicaciones 1 a 5, y R representa los valores de R6 tales como se ha definido en una cualquiera de las reivindicaciones 1 a 5 y los valores siguiente: OH, OCH3, OS(O)2CF3, Cl, SCH3, CN. Reivindicacion 16: Como productos industriales nuevos, los intermedios de s¡ntesis (2); en los que el sustituyente R3 representa un tomo de fluor o un radical metoxi, y el sustituyente R4 representa un tomo de hidrogeno, eligiendose R entre los valores de R6 tales como se han definido en una cualquiera de las reivindicaciones 1 a 5 y los valores siguientes: OH, OCH3, OS(O)2CF3, Cl, SCH3, CN. Reivindicacion 17: Como productos industriales nuevos, los intermedios de s¡ntesis (3); en los que los sustituyentes R3 y R4 tienen los significados indicados en una cualquiera de las reivindicaciones 1 a 5 y R representa los valores siguientes: OH, OCH3, OS(O)2CF3, Cl, SCH3, CN.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0803262 | 2008-06-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072084A1 true AR072084A1 (es) | 2010-08-04 |
Family
ID=40445526
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102077A AR072084A1 (es) | 2008-06-12 | 2009-06-10 | Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US20110178053A1 (es) |
| EP (1) | EP2303882A2 (es) |
| JP (1) | JP2011522867A (es) |
| KR (1) | KR20110016998A (es) |
| CN (1) | CN102124007A (es) |
| AR (1) | AR072084A1 (es) |
| AU (1) | AU2009259114B2 (es) |
| BR (1) | BRPI0915204A2 (es) |
| CA (1) | CA2725093A1 (es) |
| CO (1) | CO6280536A2 (es) |
| CR (1) | CR11814A (es) |
| DO (1) | DOP2010000366A (es) |
| EA (1) | EA018945B1 (es) |
| EC (1) | ECSP10010670A (es) |
| IL (1) | IL209840A0 (es) |
| MA (1) | MA32460B1 (es) |
| MX (1) | MX2010013699A (es) |
| NI (1) | NI201000210A (es) |
| NZ (1) | NZ589839A (es) |
| PE (1) | PE20110122A1 (es) |
| SV (1) | SV2010003754A (es) |
| TW (1) | TW201002711A (es) |
| UA (1) | UA101668C2 (es) |
| UY (1) | UY31895A (es) |
| WO (1) | WO2009150381A2 (es) |
| ZA (1) | ZA201008387B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009151598A1 (en) | 2008-06-11 | 2009-12-17 | Genentech, Inc. | Diazacarbazoles and methods of use |
| EA018198B1 (ru) | 2008-06-12 | 2013-06-28 | Янссен Фармацевтика Нв | Диаминопиридиновые, пиримидиновые и пиридазиновые модуляторы гистаминового рецептора h |
| AR073431A1 (es) * | 2009-03-24 | 2010-11-03 | Sanofi Aventis | Derivados de azacarbolinas 9h- pirrolo (2,3-b:5,4-c) dipiridina , su preparacion y si utilizacion terapeutica |
| FR2950891B1 (fr) * | 2009-10-06 | 2012-11-09 | Sanofi Aventis | Derives d'azacarbolines 9h-pyrrolo[2,3-b:5,4-c']dipyridine, leur preparation et leur utilisation therapeutique |
| FR2953838B1 (fr) * | 2009-12-10 | 2012-02-24 | Sanofi Aventis | Derives de 9h-beta-carboline (ou 9h-pyridino[3,4-b]indole) trisubstitues, leur preparation et leur utilisation therapeutique |
| US20110183938A1 (en) * | 2009-12-16 | 2011-07-28 | Genentech, Inc. | 1,7-diazacarbazoles and methods of use |
| SI2861595T1 (sl) | 2012-06-13 | 2017-04-26 | Incyte Holdings Corporation | Substituirane triciklične spojine kot inhibitorji fgfr |
| CA2903463A1 (en) * | 2013-03-11 | 2014-10-09 | The Regents Of The University Of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| KR101652577B1 (ko) * | 2013-04-19 | 2016-08-30 | 영남대학교 산학협력단 | 아미도피리딘올 유도체 또는 이의 약제학적 허용가능한 염 및 이를 유효성분으로 함유하는 혈관신생으로 인한 질환의 예방 또는 치료용 약학조성물 |
| CN103408573B (zh) * | 2013-07-12 | 2015-12-23 | 上海工程技术大学 | 硼酸衍生物及其制备方法和应用 |
| WO2018137655A1 (zh) * | 2017-01-25 | 2018-08-02 | 江苏豪森药业集团有限公司 | 吡咯并吡啶类n-氧化衍生物及其制备方法和应用 |
| WO2019031990A1 (ru) * | 2017-08-07 | 2019-02-14 | Закрытое Акционерное Общество "Биокад" | Новые гетероциклические соединения как ингибиторы cdk8/19 |
| MX2020011639A (es) | 2018-05-04 | 2021-02-15 | Incyte Corp | Sales de un inhibidor de receptores de factor de crecimiento de fibroblastos (fgfr). |
| EP3860996A4 (en) | 2018-10-02 | 2022-08-31 | Northwestern University | BETA-CARBOLINES AS POSITIVE ALLOSTERIC MODULATORS OF HUMAN SEROTONIN RECEPTOR 2C (5-HT2C) |
| CR20220285A (es) | 2019-12-04 | 2022-10-27 | Incyte Corp | Derivados de un inhibidor de fgfr |
| CN116693449A (zh) | 2022-03-04 | 2023-09-05 | 上海致根医药科技有限公司 | 用作tyk2抑制剂的化合物、其制备方法及其在医药上的应用 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8119655B2 (en) * | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| WO2009151598A1 (en) * | 2008-06-11 | 2009-12-17 | Genentech, Inc. | Diazacarbazoles and methods of use |
-
2009
- 2009-06-10 AR ARP090102077A patent/AR072084A1/es not_active Application Discontinuation
- 2009-06-11 WO PCT/FR2009/051100 patent/WO2009150381A2/fr not_active Ceased
- 2009-06-11 EP EP09761932A patent/EP2303882A2/fr not_active Withdrawn
- 2009-06-11 PE PE2010001118A patent/PE20110122A1/es not_active Application Discontinuation
- 2009-06-11 NZ NZ589839A patent/NZ589839A/en not_active IP Right Cessation
- 2009-06-11 CA CA2725093A patent/CA2725093A1/fr not_active Abandoned
- 2009-06-11 MX MX2010013699A patent/MX2010013699A/es active IP Right Grant
- 2009-06-11 AU AU2009259114A patent/AU2009259114B2/en not_active Ceased
- 2009-06-11 UA UAA201100324A patent/UA101668C2/ru unknown
- 2009-06-11 JP JP2011513034A patent/JP2011522867A/ja not_active Ceased
- 2009-06-11 EA EA201170002A patent/EA018945B1/ru not_active IP Right Cessation
- 2009-06-11 KR KR1020117000721A patent/KR20110016998A/ko not_active Withdrawn
- 2009-06-11 BR BRPI0915204A patent/BRPI0915204A2/pt not_active IP Right Cessation
- 2009-06-11 CN CN2009801313693A patent/CN102124007A/zh active Pending
- 2009-06-11 US US12/997,326 patent/US20110178053A1/en not_active Abandoned
- 2009-06-12 UY UY0001031895A patent/UY31895A/es not_active Application Discontinuation
- 2009-06-12 TW TW098119820A patent/TW201002711A/zh unknown
-
2010
- 2010-11-23 ZA ZA2010/08387A patent/ZA201008387B/en unknown
- 2010-11-25 CR CR11814A patent/CR11814A/es not_active Application Discontinuation
- 2010-11-29 DO DO2010000366A patent/DOP2010000366A/es unknown
- 2010-12-03 EC EC2010010670A patent/ECSP10010670A/es unknown
- 2010-12-06 NI NI201000210A patent/NI201000210A/es unknown
- 2010-12-08 IL IL209840A patent/IL209840A0/en unknown
- 2010-12-09 SV SV2010003754A patent/SV2010003754A/es unknown
- 2010-12-09 CO CO10154614A patent/CO6280536A2/es active IP Right Grant
-
2011
- 2011-01-07 MA MA33499A patent/MA32460B1/fr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20110016998A (ko) | 2011-02-18 |
| EA201170002A1 (ru) | 2011-08-30 |
| MA32460B1 (fr) | 2011-07-03 |
| EP2303882A2 (fr) | 2011-04-06 |
| SV2010003754A (es) | 2011-03-15 |
| DOP2010000366A (es) | 2010-12-31 |
| UY31895A (es) | 2010-01-29 |
| WO2009150381A2 (fr) | 2009-12-17 |
| TW201002711A (en) | 2010-01-16 |
| AU2009259114B2 (en) | 2013-05-23 |
| CO6280536A2 (es) | 2011-05-20 |
| MX2010013699A (es) | 2011-02-23 |
| NZ589839A (en) | 2012-07-27 |
| IL209840A0 (en) | 2011-02-28 |
| JP2011522867A (ja) | 2011-08-04 |
| BRPI0915204A2 (pt) | 2019-01-15 |
| PE20110122A1 (es) | 2011-03-07 |
| UA101668C2 (ru) | 2013-04-25 |
| EA018945B1 (ru) | 2013-11-29 |
| US20110178053A1 (en) | 2011-07-21 |
| CA2725093A1 (fr) | 2009-12-17 |
| AU2009259114A1 (en) | 2009-12-17 |
| CR11814A (es) | 2011-01-10 |
| NI201000210A (es) | 2011-05-09 |
| ZA201008387B (en) | 2012-02-29 |
| CN102124007A (zh) | 2011-07-13 |
| ECSP10010670A (es) | 2011-01-31 |
| WO2009150381A3 (fr) | 2010-02-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |