AR060010A1 - PIRIDOPIRAZINAS AND ITS USE AS KINASE MODULATORS - Google Patents
PIRIDOPIRAZINAS AND ITS USE AS KINASE MODULATORSInfo
- Publication number
- AR060010A1 AR060010A1 ARP060104949A ARP060104949A AR060010A1 AR 060010 A1 AR060010 A1 AR 060010A1 AR P060104949 A ARP060104949 A AR P060104949A AR P060104949 A ARP060104949 A AR P060104949A AR 060010 A1 AR060010 A1 AR 060010A1
- Authority
- AR
- Argentina
- Prior art keywords
- allergic
- kinases
- kinase
- enantiomers
- derivatives
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 4
- 102000020233 phosphotransferase Human genes 0.000 title abstract 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 2
- 102000001253 Protein Kinase Human genes 0.000 abstract 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 abstract 2
- 208000010668 atopic eczema Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 108060006633 protein kinase Proteins 0.000 abstract 2
- 101100226058 Dictyostelium discoideum erkB gene Proteins 0.000 abstract 1
- 208000001953 Hypotension Diseases 0.000 abstract 1
- 125000002842 L-seryl group Chemical group O=C([*])[C@](N([H])[H])([H])C([H])([H])O[H] 0.000 abstract 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 abstract 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 abstract 1
- 102000004278 Receptor Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000873 Receptor Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 230000000202 analgesic effect Effects 0.000 abstract 1
- 230000003266 anti-allergic effect Effects 0.000 abstract 1
- 230000003257 anti-anginal effect Effects 0.000 abstract 1
- 230000002456 anti-arthritic effect Effects 0.000 abstract 1
- 230000001088 anti-asthma Effects 0.000 abstract 1
- 230000003178 anti-diabetic effect Effects 0.000 abstract 1
- 230000036436 anti-hiv Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000002682 anti-psoriatic effect Effects 0.000 abstract 1
- 230000003356 anti-rheumatic effect Effects 0.000 abstract 1
- 239000000924 antiasthmatic agent Substances 0.000 abstract 1
- 239000003472 antidiabetic agent Substances 0.000 abstract 1
- 239000003435 antirheumatic agent Substances 0.000 abstract 1
- 230000001086 cytosolic effect Effects 0.000 abstract 1
- 239000000824 cytostatic agent Substances 0.000 abstract 1
- 230000001085 cytostatic effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 208000021822 hypotensive Diseases 0.000 abstract 1
- 230000001077 hypotensive effect Effects 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000324 neuroprotective effect Effects 0.000 abstract 1
- 230000001777 nootropic effect Effects 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- -1 pyrazin-6-yl Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000019491 signal transduction Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
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- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
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- Health & Medical Sciences (AREA)
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Abstract
Derivados de pirido[2,3]pirazina de las formulas generales (1) y (2) y sus sales, derivados o análogos, sus solvatos, hidratos, formas polimorficas y profármacos pueden estar presente en forma de sus racematos, en forma de sus enantiomeros y/o diastereomeros puros o en forma de mezclas de estos enantiomeros y/o diastereomeros o en forma de tautomeros; en donde los sustituyentes se definen en la descripcion. Estos compuestos presenta las siguientes actividades: citostática, antiinflamatoria, analgésica, anti-VIH, antirreumática, antiartrítica, nootropica, neuroprotectiva, antipsoriática, inmunosupresiva, vasotropica, antidiabética, nefrotropica, oftalmologica, antiasmática, antialérgica, antiarterioesclerotica, sobre el corazon, cerebroprotectivo, anoréctico, antianginal e hipotensivo. El mecanismo de accion actua modulando las rutas de transduccion de senales que involucran quinasas, particularmente receptores de tirosinquinasas, quinasas, Ser/Thr, Tyr citoplasmáticas o quinasas lipídicas. El compuesto 1-(3-ciclopropiletinil-pirido2,3-b]pirazin-6-il)-3-etil urea presento una IC50 contra la quinasa erk2 de 5, 8 mu M y contra la quinasa P13Kalpa de 16.8mu M.Pyrido derivatives [2,3] pyrazine of the general formulas (1) and (2) and their salts, derivatives or analogs, their solvates, hydrates, polymorphic forms and prodrugs may be present in the form of their racemates, in the form of their enantiomers and / or pure diastereomers or in the form of mixtures of these enantiomers and / or diastereomers or in the form of tautomers; wherein the substituents are defined in the description. These compounds have the following activities: cytostatic, anti-inflammatory, analgesic, anti-HIV, anti-rheumatic, antiarthritic, nootropic, neuroprotective, antipsoriatic, immunosuppressive, vasotropic, antidiabetic, nephrotropic, ophthalmological, anti-asthmatic, anti-allergic, anti-arterio-allergic, cerebral-allergic , antianginal and hypotensive. The mechanism of action acts by modulating signal transduction pathways that involve kinases, particularly tyrosine kinase receptors, kinases, Ser / Thr, Tyr cytoplasmic or lipid kinases. Compound 1- (3-cyclopropylethynyl-pyrido2,3-b] pyrazin-6-yl) -3-ethyl urea had an IC50 against erk2 kinase of 5.8 µM and against P13Kalpa kinase of 16.8mu M.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73569805P | 2005-11-11 | 2005-11-11 | |
| EP05024693A EP1785423A1 (en) | 2005-11-11 | 2005-11-11 | Pyridopyrazine derivatives and their use as kinase modulators |
| US84976106P | 2006-10-06 | 2006-10-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR060010A1 true AR060010A1 (en) | 2008-05-21 |
Family
ID=37654792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104949A AR060010A1 (en) | 2005-11-11 | 2006-11-13 | PIRIDOPIRAZINAS AND ITS USE AS KINASE MODULATORS |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1957487A1 (en) |
| JP (1) | JP5527972B2 (en) |
| KR (1) | KR101400905B1 (en) |
| AR (1) | AR060010A1 (en) |
| AU (1) | AU2006313701B2 (en) |
| CA (1) | CA2628039A1 (en) |
| IL (1) | IL191139A0 (en) |
| NO (1) | NO20082511L (en) |
| WO (1) | WO2007054556A1 (en) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| EP1790342A1 (en) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazine derivatives and their use as signal transduction modulators |
| EP1990342A1 (en) * | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| US20100130597A1 (en) * | 2007-07-06 | 2010-05-27 | The United State Of America, As Represented By The Secretary Of The Dept Of Health And Human Service | Dna-pkcs modulates energy regulation and brain function |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| US8846723B2 (en) | 2010-07-29 | 2014-09-30 | Eastman Chemical Company | Esters of O-substituted hydroxy carboxylic acids and preparations thereof |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| EP2508184A1 (en) | 2011-04-06 | 2012-10-10 | Æterna Zentaris GmbH | Pyridopyrazine derivatives and their use |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| 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 |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| HRP20210319T1 (en) | 2014-03-26 | 2021-04-30 | Astex Therapeutics Ltd. | COMBINATIONS OF FGFR INHIBITOR AND IGF1R INHIBITOR |
| JO3512B1 (en) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | Quinoxaline derivatives useful as fgfr kinase modulators |
| RU2715236C2 (en) | 2014-03-26 | 2020-02-26 | Астекс Терапьютикс Лтд | Combinations |
| TWI719960B (en) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | New compositions |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| US11155555B2 (en) | 2015-09-23 | 2021-10-26 | Janssen Pharmaceutica Nv | Compounds |
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| US3809695A (en) | 1967-04-19 | 1974-05-07 | Degussa | 2,6-dichloro-3-nitro-pyridine |
| US5700823A (en) * | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| DE69600385T2 (en) | 1995-03-28 | 1998-12-17 | Sumitomo Chemical Co., Ltd., Osaka | Process for the preparation of aminonitropyridines |
| UA71555C2 (en) * | 1997-10-06 | 2004-12-15 | Zentaris Gmbh | Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives |
| ATE529109T1 (en) | 1997-12-22 | 2011-11-15 | Bayer Healthcare Llc | INHIBITION OF P38 KINASE ACTIVITY BY SUBSTITUTED HETEROCYCLIC UREAS |
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| AP2001002175A0 (en) | 1998-12-22 | 2001-06-21 | Warner Lambert Co | Combination chemotherapy. |
| GEP20084317B (en) | 2000-04-25 | 2008-02-25 | Icos Corp | Inhibitors of human phosphatidyl-inositol 3-kinase delta |
| JP3811775B2 (en) | 2000-07-19 | 2006-08-23 | ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー | Oxygenated ester of 4-iodophenylaminobenzhydroxamic acid |
| CN101851173A (en) | 2001-09-14 | 2010-10-06 | 梅特希尔基因公司 | Inhibitors of histone deacetylase |
| US20040023961A1 (en) | 2002-02-11 | 2004-02-05 | Bayer Corporation | Aryl ureas with raf kinase and angiogenisis inhibiting activity |
| EP1496981A2 (en) | 2002-04-08 | 2005-01-19 | Merck & Co., Inc. | Method of treating cancer |
| EP1496906A4 (en) | 2002-04-08 | 2006-05-03 | Merck & Co Inc | INHIBITORS OF AKT ACTIVITY |
| US7223738B2 (en) | 2002-04-08 | 2007-05-29 | Merck & Co., Inc. | Inhibitors of Akt activity |
| US7718651B2 (en) | 2002-07-02 | 2010-05-18 | Southern Research Institute | Inhibitors of FtsZ and uses thereof |
| AU2003255845A1 (en) | 2002-08-22 | 2004-03-11 | Piramed Limited | Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents |
| PT1636228E (en) * | 2003-05-23 | 2009-02-02 | Aeterna Zentaris Gmbh | Novel pyridopyrazines and use thereof as kinase modulators |
| DE10323345A1 (en) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | New pyridopyrazines and their use as kinase inhibitors |
| EP1641777A1 (en) * | 2003-06-05 | 2006-04-05 | Zentaris GmbH | Indole derivatives with apoptosis-inducing effect |
| WO2005007099A2 (en) | 2003-07-10 | 2005-01-27 | Imclone Systems Incorporated | Pkb inhibitors as anti-tumor agents |
| US7592340B2 (en) | 2003-12-04 | 2009-09-22 | Vertex Pharmaceuticals Incorporated | Quinoxalines useful as inhibitors of protein kinases |
| EP1790342A1 (en) * | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazine derivatives and their use as signal transduction modulators |
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