NO332005B1 - Nye pyridopyraziner, anvendelse derav, medikament inneholdende minst en slik forbindelse og fremgangsmate for fremstilling av et slikt medikament - Google Patents
Nye pyridopyraziner, anvendelse derav, medikament inneholdende minst en slik forbindelse og fremgangsmate for fremstilling av et slikt medikament Download PDFInfo
- Publication number
- NO332005B1 NO332005B1 NO20056032A NO20056032A NO332005B1 NO 332005 B1 NO332005 B1 NO 332005B1 NO 20056032 A NO20056032 A NO 20056032A NO 20056032 A NO20056032 A NO 20056032A NO 332005 B1 NO332005 B1 NO 332005B1
- Authority
- NO
- Norway
- Prior art keywords
- pyrazin
- pyrido
- thiourea
- phenylpyrido
- allyl
- Prior art date
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- YEYHFKBVNARCNE-UHFFFAOYSA-N pyrido[2,3-b]pyrazine Chemical class N1=CC=NC2=CC=CN=C21 YEYHFKBVNARCNE-UHFFFAOYSA-N 0.000 title claims abstract description 24
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- 238000000034 method Methods 0.000 title claims description 33
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 11
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- 230000001575 pathological effect Effects 0.000 claims abstract description 8
- 230000003211 malignant effect Effects 0.000 claims abstract description 7
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims description 106
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 66
- -1 c-Abl Proteins 0.000 claims description 30
- 239000000203 mixture Substances 0.000 claims description 29
- 150000003839 salts Chemical class 0.000 claims description 15
- 229940079593 drug Drugs 0.000 claims description 12
- 208000035475 disorder Diseases 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
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- 125000001424 substituent group Chemical group 0.000 claims description 8
- 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 claims description 7
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- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims description 2
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- 125000004944 pyrazin-3-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims description 2
- UDJFFSGCRRMVFH-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine Chemical compound N1=CN=CC2=CC=CN=C21 UDJFFSGCRRMVFH-UHFFFAOYSA-N 0.000 claims description 2
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- NTOQMJIXQWHLML-UHFFFAOYSA-N 1-(2,3-dimethylpyrido[2,3-b]pyrazin-6-yl)-3-ethylurea Chemical compound N1=C(C)C(C)=NC2=NC(NC(=O)NCC)=CC=C21 NTOQMJIXQWHLML-UHFFFAOYSA-N 0.000 claims 1
- NNMVZBZBSISKNQ-UHFFFAOYSA-N 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-(3-phenylpyrido[2,3-b]pyrazin-6-yl)urea Chemical compound C1=C(Cl)C(C(F)(F)F)=CC(NC(=O)NC=2N=C3N=C(C=NC3=CC=2)C=2C=CC=CC=2)=C1 NNMVZBZBSISKNQ-UHFFFAOYSA-N 0.000 claims 1
- 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 claims 1
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Classifications
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- 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
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- 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10323345A DE10323345A1 (de) | 2003-05-23 | 2003-05-23 | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
| DE102004022383A DE102004022383A1 (de) | 2004-05-06 | 2004-05-06 | Neue Pyridopyrazine und deren Verwendung als Modulatoren von Kinasen |
| PCT/EP2004/005388 WO2004104003A1 (de) | 2003-05-23 | 2004-05-19 | Neue pyridopyrazine und deren verwendung als modulatoren von kinasen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO20056032L NO20056032L (no) | 2006-02-15 |
| NO332005B1 true NO332005B1 (no) | 2012-05-21 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20056032A NO332005B1 (no) | 2003-05-23 | 2005-12-19 | Nye pyridopyraziner, anvendelse derav, medikament inneholdende minst en slik forbindelse og fremgangsmate for fremstilling av et slikt medikament |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US7276507B2 (pt) |
| EP (1) | EP1636228B1 (pt) |
| JP (2) | JP4571944B2 (pt) |
| KR (1) | KR101111464B1 (pt) |
| AR (1) | AR045686A1 (pt) |
| AT (1) | ATE411992T1 (pt) |
| AU (1) | AU2004240747B2 (pt) |
| BR (1) | BRPI0410633A (pt) |
| CA (1) | CA2524525C (pt) |
| CY (1) | CY1108715T1 (pt) |
| DE (1) | DE502004008322D1 (pt) |
| DK (1) | DK1636228T3 (pt) |
| ES (1) | ES2316985T3 (pt) |
| HK (1) | HK1090643A1 (pt) |
| HR (1) | HRP20090036T3 (pt) |
| ME (1) | ME00541B (pt) |
| MX (1) | MXPA05012645A (pt) |
| NO (1) | NO332005B1 (pt) |
| NZ (1) | NZ544112A (pt) |
| PL (1) | PL1636228T3 (pt) |
| PT (1) | PT1636228E (pt) |
| RU (1) | RU2330851C9 (pt) |
| SI (1) | SI1636228T1 (pt) |
| TW (1) | TWI341839B (pt) |
| UA (1) | UA78929C2 (pt) |
| WO (1) | WO2004104003A1 (pt) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101115479A (zh) * | 2005-02-14 | 2008-01-30 | 默克公司 | Akt活性抑制剂 |
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| EP1785423A1 (de) * | 2005-11-11 | 2007-05-16 | Zentaris GmbH | Neue Pyridopyrazine und deren Verwendung als Modulatoren von Kinasen |
| KR101400905B1 (ko) | 2005-11-11 | 2014-05-29 | 아에테르나 젠타리스 게엠베하 | 신규한 피리도피라진 및 키나제의 조절제로서의 이의 용도 |
| EP1790342A1 (de) * | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| JO2985B1 (ar) | 2006-12-20 | 2016-09-05 | Takeda Pharmaceuticals Co | مثبطات كينازmapk/erk |
| EP1990342A1 (en) * | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| CN102869775A (zh) | 2009-09-30 | 2013-01-09 | 哈佛大学校长及研究员协会 | 通过调节自噬抑制基因产物调节自噬的方法 |
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| EP2508184A1 (en) | 2011-04-06 | 2012-10-10 | Æterna Zentaris GmbH | Pyridopyrazine derivatives and their use |
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| 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 |
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| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| JP6980385B2 (ja) | 2014-03-26 | 2021-12-15 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | Ｆｇｆｒ阻害剤とｉｇｆ１ｒ阻害剤の組合せ |
| HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
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| GB9413975D0 (en) * | 1994-07-11 | 1994-08-31 | Fujisawa Pharmaceutical Co | New heterobicyclic derivatives |
| TW274550B (pt) | 1992-09-26 | 1996-04-21 | Hoechst Ag | |
| US5700823A (en) * | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| UA71555C2 (en) * | 1997-10-06 | 2004-12-15 | Zentaris Gmbh | Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives |
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| AU2003223467B2 (en) | 2002-04-08 | 2007-10-04 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
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| WO2003084473A2 (en) * | 2002-04-08 | 2003-10-16 | Merck & Co., Inc. | Method of treating cancer |
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| US7208493B2 (en) | 2002-10-03 | 2007-04-24 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| DE10323345A1 (de) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
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