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
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
- 239000001257 hydrogen Substances 0.000 abstract 13
- 229910052739 hydrogen Inorganic materials 0.000 abstract 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 13
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 8
- 125000001153 fluoro group Chemical group F* 0.000 abstract 8
- 239000000460 chlorine Chemical group 0.000 abstract 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 4
- -1 chloro, methoxy Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 abstract 1
- 101150019464 ARAF gene Proteins 0.000 abstract 1
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 abstract 1
- 101100381978 Mus musculus Braf gene Proteins 0.000 abstract 1
- 206010033128 Ovarian cancer Diseases 0.000 abstract 1
- 206010061535 Ovarian neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 102000001788 Proto-Oncogene Proteins c-raf Human genes 0.000 abstract 1
- 108010029869 Proto-Oncogene Proteins c-raf Proteins 0.000 abstract 1
- 208000024770 Thyroid neoplasm Diseases 0.000 abstract 1
- 201000009036 biliary tract cancer Diseases 0.000 abstract 1
- 208000020790 biliary tract neoplasm Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 201000002510 thyroid cancer Diseases 0.000 abstract 1
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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Hematology (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) | US8198273B2 (es) |
| EP (2) | EP2427462A1 (es) |
| JP (2) | JP2012526127A (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) | WO2010129570A1 (es) |
| ZA (1) | ZA201108124B (es) |
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| US8329724B2 (en) | 2009-08-03 | 2012-12-11 | Hoffmann-La Roche Inc. | Process for the manufacture of pharmaceutically active compounds |
| SG10201407129SA (en) | 2009-11-06 | 2014-12-30 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| MX2012005827A (es) | 2009-11-18 | 2012-06-19 | Plexxikon Inc | Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello. |
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| JP7300394B2 (ja) | 2017-01-17 | 2023-06-29 | ヘパリジェニックス ゲーエムベーハー | 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害 |
| WO2018175311A1 (en) | 2017-03-20 | 2018-09-27 | Plexxikon Inc. | Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1h- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain |
| WO2018226846A1 (en) | 2017-06-07 | 2018-12-13 | Plexxikon Inc. | Compounds and methods for kinase modulation |
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| EP3694855A1 (en) | 2017-10-13 | 2020-08-19 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
| CN112165958A (zh) | 2017-10-27 | 2021-01-01 | 普莱希科公司 | 调制激酶的化合物的制剂 |
| JP7395480B2 (ja) * | 2018-01-10 | 2023-12-11 | クラ セラピューティクス， エルエルシー | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
| WO2019149738A1 (en) | 2018-01-31 | 2019-08-08 | Heparegenix Gmbh | Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| EP3768666A1 (en) | 2018-03-20 | 2021-01-27 | Plexxikon Inc. | Compounds and methods for ido and tdo modulation, and indications therefor |
| US11731968B2 (en) | 2018-06-21 | 2023-08-22 | Heparegenix Gmbh | Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| CA3104246A1 (en) * | 2018-07-16 | 2020-01-23 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| PL4073065T3 (pl) | 2019-12-10 | 2025-05-19 | F. Hoffmann-La Roche Ag | Nowe pochodne metylochinazolinonu |
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| BR122012021252B8 (pt) | 2002-09-06 | 2021-05-25 | Cerulean Pharma Inc | polímeros à base de ciclodextrina para o fornecimento de agentes terapêuticos ligados a eles por covalência |
| PL1893612T3 (pl) * | 2005-06-22 | 2012-01-31 | Plexxikon Inc | Pochodne pirolo-[2,3-b]pirydyny jako inhibitory kinazy białkowej |
| DE102005034406A1 (de) | 2005-07-22 | 2007-02-01 | Ratiopharm Gmbh | Neue Salze von Rosiglitazon |
| 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 |
| WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| PE20121126A1 (es) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa |
| BRPI0814423B1 (pt) * | 2007-07-17 | 2022-04-19 | Plexxikon, Inc | Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos |
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2010
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- 2010-05-04 SG SG2011078979A patent/SG175810A1/en unknown
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- 2010-05-04 MA MA34424A patent/MA34042B1/fr unknown
- 2010-05-04 RU RU2011149485/02A patent/RU2011149485A/ru not_active Application Discontinuation
- 2010-05-04 WO PCT/US2010/033576 patent/WO2010129570A1/en not_active Ceased
- 2010-05-04 BR BRPI1013843A patent/BRPI1013843A2/pt not_active IP Right Cessation
- 2010-05-04 WO PCT/US2010/033571 patent/WO2010129567A1/en not_active Ceased
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- 2010-05-04 US US13/318,760 patent/US20120122860A1/en not_active Abandoned
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| CR20110562A (es) | 2012-02-09 |
| WO2010129567A1 (en) | 2010-11-11 |
| NI201100189A (es) | 2012-01-11 |
| CN102459262A (zh) | 2012-05-16 |
| AU2010246005A1 (en) | 2011-12-01 |
| EP2427462A1 (en) | 2012-03-14 |
| ECSP11011437A (es) | 2011-12-30 |
| ZA201108124B (en) | 2014-04-30 |
| JP2012526128A (ja) | 2012-10-25 |
| TW201041888A (en) | 2010-12-01 |
| WO2010129570A1 (en) | 2010-11-11 |
| RU2011149485A (ru) | 2013-06-20 |
| MA34042B1 (fr) | 2013-03-05 |
| IL215908A0 (en) | 2012-01-31 |
| BRPI1013843A2 (pt) | 2016-04-12 |
| SG175810A1 (en) | 2011-12-29 |
| EP2427433A1 (en) | 2012-03-14 |
| KR20140014386A (ko) | 2014-02-06 |
| CL2011002739A1 (es) | 2012-04-09 |
| US20120122860A1 (en) | 2012-05-17 |
| US8198273B2 (en) | 2012-06-12 |
| CA2759997A1 (en) | 2010-11-11 |
| PE20120518A1 (es) | 2012-05-24 |
| US20120245174A1 (en) | 2012-09-27 |
| NO20111508A1 (no) | 2011-12-02 |
| JP2012526127A (ja) | 2012-10-25 |
| US20100286142A1 (en) | 2010-11-11 |
| MX2011011737A (es) | 2011-12-08 |
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