AR060010A1 - Piridopirazinas y su uso como moduladores de quinasas - Google Patents
Piridopirazinas y su uso como moduladores de quinasasInfo
- 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
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- 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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- A61K31/33—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61P9/12—Antihypertensives
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- 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
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- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
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.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73569805P | 2005-11-11 | 2005-11-11 | |
| EP05024693A EP1785423A1 (de) | 2005-11-11 | 2005-11-11 | Neue Pyridopyrazine und deren Verwendung als Modulatoren von Kinasen |
| US84976106P | 2006-10-06 | 2006-10-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR060010A1 true AR060010A1 (es) | 2008-05-21 |
Family
ID=37654792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104949A AR060010A1 (es) | 2005-11-11 | 2006-11-13 | Piridopirazinas y su uso como moduladores de quinasas |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1957487A1 (es) |
| JP (1) | JP5527972B2 (es) |
| KR (1) | KR101400905B1 (es) |
| AR (1) | AR060010A1 (es) |
| AU (1) | AU2006313701B2 (es) |
| CA (1) | CA2628039A1 (es) |
| IL (1) | IL191139A0 (es) |
| NO (1) | NO20082511L (es) |
| WO (1) | WO2007054556A1 (es) |
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 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| 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 (hr) | 2014-03-26 | 2021-04-30 | Astex Therapeutics Ltd. | Kombinacije inhibitora fgfr i inhibitora igf1r |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| RU2715236C2 (ru) | 2014-03-26 | 2020-02-26 | Астекс Терапьютикс Лтд | Комбинации |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| 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 (de) | 1995-03-28 | 1998-12-17 | Sumitomo Chemical Co., Ltd., Osaka | Verfahren zur Herstellung von Aminonitropyridinen |
| UA71555C2 (en) * | 1997-10-06 | 2004-12-15 | Zentaris Gmbh | Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives |
| ATE529109T1 (de) | 1997-12-22 | 2011-11-15 | Bayer Healthcare Llc | Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe |
| AU2180500A (en) | 1998-12-15 | 2000-07-03 | Warner-Lambert Company | Use of a mek inhibitor for preventing transplant rejection |
| 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 (ja) | 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 | ４−ヨードフェニルアミノベンズヒドロキサム酸の酸素化エステル |
| CN101851173A (zh) | 2001-09-14 | 2010-10-06 | 梅特希尔基因公司 | 组蛋白脱乙酰化酶抑制剂 |
| 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 | HEMMER OF ACT 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 (pt) * | 2003-05-23 | 2009-02-02 | Aeterna Zentaris Gmbh | Novas piridopirazinas e sua utilização como moduladores de cinases |
| DE10323345A1 (de) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
| EP1641777A1 (de) * | 2003-06-05 | 2006-04-05 | Zentaris GmbH | Indolderivate mit apoptose induzierender wirkung |
| 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 (de) * | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
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2006
- 2006-11-10 WO PCT/EP2006/068322 patent/WO2007054556A1/de not_active Ceased
- 2006-11-10 KR KR1020087014068A patent/KR101400905B1/ko not_active Expired - Fee Related
- 2006-11-10 AU AU2006313701A patent/AU2006313701B2/en not_active Ceased
- 2006-11-10 JP JP2008539443A patent/JP5527972B2/ja not_active Expired - Fee Related
- 2006-11-10 CA CA002628039A patent/CA2628039A1/en not_active Abandoned
- 2006-11-10 EP EP06819385A patent/EP1957487A1/de not_active Withdrawn
- 2006-11-13 AR ARP060104949A patent/AR060010A1/es unknown
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2008
- 2008-04-29 IL IL191139A patent/IL191139A0/en unknown
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| AU2006313701B2 (en) | 2012-05-31 |
| HK1126474A1 (en) | 2009-09-04 |
| WO2007054556A1 (de) | 2007-05-18 |
| JP5527972B2 (ja) | 2014-06-25 |
| CA2628039A1 (en) | 2007-05-18 |
| JP2009515853A (ja) | 2009-04-16 |
| IL191139A0 (en) | 2008-12-29 |
| NO20082511L (no) | 2008-06-24 |
| AU2006313701A1 (en) | 2007-05-18 |
| EP1957487A1 (de) | 2008-08-20 |
| KR20080068117A (ko) | 2008-07-22 |
| KR101400905B1 (ko) | 2014-05-29 |
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