AR076749A1 - Pirrolo[2, 3 - b]piridinas como inhibidores de las protein quinasas raf - Google Patents
Pirrolo[2, 3 - b]piridinas como inhibidores de las protein quinasas rafInfo
- Publication number
- AR076749A1 AR076749A1 ARP100101517A ARP100101517A AR076749A1 AR 076749 A1 AR076749 A1 AR 076749A1 AR P100101517 A ARP100101517 A AR P100101517A AR P100101517 A ARP100101517 A AR P100101517A AR 076749 A1 AR076749 A1 AR 076749A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- hydrogen
- fluoro
- cyano
- methyl
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se describen compuestos y sales de los mismos, formulaciones de los mismos, conjugados de los mismos, derivados de los mismos, formas de los mismos y usos de los mismos. En algunos aspectos y formas de realizacion, los compuestos descriptos o sales de los mismos, formulaciones de los mismos, conjugados de los mismos, derivados de los mismos y formas de los mismos son activos en cada una de las proteína quinasas BRaf y c-Raf-1, y también pueden ser activos en cualquiera, o ambas, de las proteínas quinasas A-Raf y B-Raf V600E. También se describe el uso de los mismos para tratar enfermedades y condiciones, incluyendo melanoma, cáncer colorrectal, cáncer de tiroides, cáncer ovárico y cáncer del tracto biliar. Reivindicacion 1: Un compuesto que tiene la estructura química de formula (1) o una sal, un profármaco o un tautomero del mismo, caracterizado porque R1 es seleccionado entre el grupo que consiste en formulas (2) a (9), en donde © indica el punto de union de R1 al S(O)2 mostrado en la formula (1); R2 es hidrogeno o fluoro; R3 es hidrogeno, cloro, metoxi o ciano; R4 es seleccionado entre el grupo que consiste en hidrogeno, cloro, metilo, metoxi, ciano, grupo de formulas (10) en donde © indica el punto de union de R4 a la posicion 5 del anillo de pirrolo[2,3-b]piridina mostrado en la formula (1) en donde cuando R1 es como en formula (2), R2 es fluoro y R3 es hidrogeno, R4 es seleccionado entre el grupo que consiste en formulas (11), cuando R1 es como en formula (2), R2 es H y R3 es H, R4 es como en formulas (a10)(b10), cuando R1 es formula (3), R2 es fluoro y R3 es hidrogeno, R4 es formula (c10), cuando R1 es formula (4), R3 es hidrogeno y R4 es ciano, R2 es hidrogeno o fluoro; cuando R1 es formula (5), R2 es fluoro y R3 es hidrogeno, R4 es metilo, metoxi, ciano, o como en formula (b10); cuando R2 es fluoro, R4 es hidrogeno y R3 es cloro, metoxi, o ciano, R1 es formula (5 a 9); cuando R2 es hidrogeno, R3 es hidrogeno y R4 es ciano, R1 es formulas (5 a 9); cuando R1 es formula (6), R2 es fluoro y R3 es hidrogeno, R4 es metilo como formula (b10); cuando R1 es formula (7), R2 es fluoro y R3 es hidrogeno, R4 es cloro, metilo o ciano o como formula (b10), cuando R1 es formula (8), R2 es F y R3 es H, R4 es Cl, metilo metoxi o formula (b10), y cuando R1 es formula (9) R2 es F y R3 es H, R4 es Cl, metilo o ciano.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17605409P | 2009-05-06 | 2009-05-06 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR076749A1 true AR076749A1 (es) | 2011-07-06 |
Family
ID=42236712
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100101517A AR076749A1 (es) | 2009-05-06 | 2010-05-05 | Pirrolo[2, 3 - b]piridinas como inhibidores de las protein quinasas raf |
Country Status (23)
Country | Link |
---|---|
US (3) | US20120122860A1 (es) |
EP (2) | EP2427462A1 (es) |
JP (2) | JP2012526128A (es) |
KR (1) | KR20140014386A (es) |
CN (1) | CN102459262A (es) |
AR (1) | AR076749A1 (es) |
AU (1) | AU2010246005A1 (es) |
BR (1) | BRPI1013843A2 (es) |
CA (1) | CA2759997A1 (es) |
CL (1) | CL2011002739A1 (es) |
CR (1) | CR20110562A (es) |
EC (1) | ECSP11011437A (es) |
IL (1) | IL215908A0 (es) |
MA (1) | MA34042B1 (es) |
MX (1) | MX2011011737A (es) |
NI (1) | NI201100189A (es) |
NO (1) | NO20111508A1 (es) |
PE (1) | PE20120518A1 (es) |
RU (1) | RU2011149485A (es) |
SG (1) | SG175810A1 (es) |
TW (1) | TW201041888A (es) |
WO (2) | WO2010129567A1 (es) |
ZA (1) | ZA201108124B (es) |
Families Citing this family (88)
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WO2007002433A1 (en) * | 2005-06-22 | 2007-01-04 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors |
WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
CN101808994B (zh) | 2007-07-17 | 2013-05-15 | 普莱希科公司 | 用于激酶调节的化合物和方法以及其适应症 |
WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
US9447089B2 (en) | 2009-04-03 | 2016-09-20 | Plexxikon Inc. | Compositions and uses thereof |
US8329724B2 (en) | 2009-08-03 | 2012-12-11 | Hoffmann-La Roche Inc. | Process for the manufacture of pharmaceutically active compounds |
UA105813C2 (uk) | 2009-11-06 | 2014-06-25 | Плексікон, Інк. | Сполуки-інгібітори кіназ та фармацевтична композиція (варіанти) |
MY156210A (en) | 2009-11-18 | 2016-01-29 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
BR112012015745A2 (pt) * | 2009-12-23 | 2016-05-17 | Plexxikon Inc | compostos e métodos para a modulação de quinase, e indicações dos mesmos |
TWI510487B (zh) | 2010-04-21 | 2015-12-01 | Plexxikon Inc | 用於激酶調節的化合物和方法及其適應症 |
GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
JP6112512B2 (ja) * | 2010-12-01 | 2017-04-12 | レクシ ファーマ インコーポレイテッド | 難治性癌を治療するための方法 |
US8889684B2 (en) * | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
WO2012106559A1 (en) * | 2011-02-02 | 2012-08-09 | Translational Genomics Research Institute | Biomarkers and methods of use thereof |
AU2012214762B2 (en) * | 2011-02-07 | 2015-08-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
TWI558702B (zh) * | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
CN103476943A (zh) | 2011-03-10 | 2013-12-25 | 普罗维克图斯药品公司 | 用于增强治疗癌症的局部和全身性免疫调节疗法的组合 |
WO2012138809A1 (en) * | 2011-04-05 | 2012-10-11 | Dawei Zhang | Heterocyclic compounds as kinase inhibitors |
BR112013029163A2 (pt) | 2011-05-17 | 2017-01-31 | Plexxikon Inc | modulação quinase e indicações dos mesmos |
CA2846574C (en) * | 2011-08-26 | 2020-07-07 | Neupharma, Inc. | Quinoxaline sulfonamide derivates for use as kinase inhibitors |
CN102993199A (zh) * | 2011-09-09 | 2013-03-27 | 山东轩竹医药科技有限公司 | 杂环取代的吡啶并吡咯激酶抑制剂 |
CA2848506C (en) | 2011-09-14 | 2020-07-21 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
WO2013043935A1 (en) | 2011-09-21 | 2013-03-28 | Neupharma, Inc. | Certain chemical entites, compositions, and methods |
WO2013049701A1 (en) | 2011-09-30 | 2013-04-04 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
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JP6013029B2 (ja) * | 2012-05-25 | 2016-10-25 | 千葉県 | 抗癌剤 |
GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
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KR102479696B1 (ko) | 2014-03-26 | 2022-12-22 | 아스텍스 테라퓨틱스 리미티드 | Fgfr 억제제 및 igf1r 억제제의 조합물 |
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CN107722013B (zh) * | 2016-08-11 | 2021-01-12 | 中国科学院上海药物研究所 | 去氮嘌呤类化合物及其药物组合物、制备方法和用途 |
TW201815766A (zh) | 2016-09-22 | 2018-05-01 | 美商普雷辛肯公司 | 用於ido及tdo調節之化合物及方法以及其適應症 |
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MXPA05002444A (es) | 2002-09-06 | 2005-09-30 | Insert Therapeutics Inc | Polimeros a base de ciclodextrina para el suministro de agentes terapeuticos. |
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WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
GB0624084D0 (en) * | 2006-12-01 | 2007-01-10 | Selamine Ltd | Ramipril amino acid salts |
PE20121126A1 (es) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
CN101808994B (zh) * | 2007-07-17 | 2013-05-15 | 普莱希科公司 | 用于激酶调节的化合物和方法以及其适应症 |
-
2010
- 2010-04-30 TW TW099113997A patent/TW201041888A/zh unknown
- 2010-05-04 CA CA2759997A patent/CA2759997A1/en not_active Abandoned
- 2010-05-04 EP EP10717408A patent/EP2427462A1/en not_active Withdrawn
- 2010-05-04 US US13/318,760 patent/US20120122860A1/en not_active Abandoned
- 2010-05-04 BR BRPI1013843A patent/BRPI1013843A2/pt not_active IP Right Cessation
- 2010-05-04 SG SG2011078979A patent/SG175810A1/en unknown
- 2010-05-04 JP JP2012509907A patent/JP2012526128A/ja active Pending
- 2010-05-04 KR KR1020117029018A patent/KR20140014386A/ko not_active Application Discontinuation
- 2010-05-04 EP EP10717980A patent/EP2427433A1/en not_active Withdrawn
- 2010-05-04 RU RU2011149485/02A patent/RU2011149485A/ru not_active Application Discontinuation
- 2010-05-04 JP JP2012509906A patent/JP2012526127A/ja active Pending
- 2010-05-04 US US12/773,798 patent/US8198273B2/en active Active
- 2010-05-04 CN CN2010800305090A patent/CN102459262A/zh active Pending
- 2010-05-04 MA MA34424A patent/MA34042B1/fr unknown
- 2010-05-04 AU AU2010246005A patent/AU2010246005A1/en not_active Abandoned
- 2010-05-04 MX MX2011011737A patent/MX2011011737A/es not_active Application Discontinuation
- 2010-05-04 WO PCT/US2010/033571 patent/WO2010129567A1/en active Application Filing
- 2010-05-04 WO PCT/US2010/033576 patent/WO2010129570A1/en active Application Filing
- 2010-05-04 PE PE2011001867A patent/PE20120518A1/es not_active Application Discontinuation
- 2010-05-05 AR ARP100101517A patent/AR076749A1/es not_active Application Discontinuation
-
2011
- 2011-10-25 IL IL215908A patent/IL215908A0/en unknown
- 2011-10-26 CR CR20110562A patent/CR20110562A/es unknown
- 2011-11-01 EC EC2011011437A patent/ECSP11011437A/es unknown
- 2011-11-03 CL CL2011002739A patent/CL2011002739A1/es unknown
- 2011-11-03 NO NO20111508A patent/NO20111508A1/no not_active Application Discontinuation
- 2011-11-03 NI NI201100189A patent/NI201100189A/es unknown
- 2011-11-04 ZA ZA2011/08124A patent/ZA201108124B/en unknown
-
2012
- 2012-06-07 US US13/491,480 patent/US20120245174A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
KR20140014386A (ko) | 2014-02-06 |
MA34042B1 (fr) | 2013-03-05 |
TW201041888A (en) | 2010-12-01 |
JP2012526127A (ja) | 2012-10-25 |
CN102459262A (zh) | 2012-05-16 |
SG175810A1 (en) | 2011-12-29 |
CL2011002739A1 (es) | 2012-04-09 |
ECSP11011437A (es) | 2011-12-30 |
WO2010129567A1 (en) | 2010-11-11 |
NI201100189A (es) | 2012-01-11 |
US20100286142A1 (en) | 2010-11-11 |
IL215908A0 (en) | 2012-01-31 |
MX2011011737A (es) | 2011-12-08 |
EP2427462A1 (en) | 2012-03-14 |
CR20110562A (es) | 2012-02-09 |
US8198273B2 (en) | 2012-06-12 |
JP2012526128A (ja) | 2012-10-25 |
US20120245174A1 (en) | 2012-09-27 |
RU2011149485A (ru) | 2013-06-20 |
PE20120518A1 (es) | 2012-05-24 |
NO20111508A1 (no) | 2011-12-02 |
BRPI1013843A2 (pt) | 2016-04-12 |
EP2427433A1 (en) | 2012-03-14 |
ZA201108124B (en) | 2014-04-30 |
WO2010129570A1 (en) | 2010-11-11 |
US20120122860A1 (en) | 2012-05-17 |
AU2010246005A1 (en) | 2011-12-01 |
CA2759997A1 (en) | 2010-11-11 |
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