DK3053923T3 - Triazolopyrazinderivater som tyrosin kinaseinhibitorer - Google Patents
Triazolopyrazinderivater som tyrosin kinaseinhibitorer Download PDFInfo
- Publication number
- DK3053923T3 DK3053923T3 DK13894061.4T DK13894061T DK3053923T3 DK 3053923 T3 DK3053923 T3 DK 3053923T3 DK 13894061 T DK13894061 T DK 13894061T DK 3053923 T3 DK3053923 T3 DK 3053923T3
- Authority
- DK
- Denmark
- Prior art keywords
- methyl
- mmol
- triazolo
- pyrazol
- pyrazin
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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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
- 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
- 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
Claims (9)
1. Triazolopyrazinderivat vist med den kemiske formel 1: kemisk formel 1
eller et farmaceutisk acceptabelt salt deraf, hvor: Ri til R3 er hver uafhængigt hydrogen, halogen, 5- til 6-leddet heterocycloalkyl, 5- til 6-leddet heterocycloalkenyl, C1-C3 alkoxy substitueret med 5- til 6-leddet heterocycloalkyl, C1-C5 alkyl substitueret med 5- til 6-leddet heterocycloalkyl, C1-C3 alkoxy substitueret med 5- til 6-leddet heterocycloalkyl, phenyl substitueret med halogen, acetylpiperazin, eller piperazinylcarbonyl, eller 5- til 6-leddet heteroaryl substitueret med 5- til 6-leddet heterocycloalkyl, hydroxy C1-C5 alkyl, eller C1-C5 alkyl; hvor mindst én af Ri til R3 ikke er hydrogen; R4 og R5 er hver uafhængigt hydrogen, 5- til 6-leddet heteroaryl usubstitueret eller substitueret med C1-C5 alkyl, eller phenyl substitueret med cyano, halogen, eller C1-C5 alkyl; hvor mindst én af R4 og Rs ikke er hydrogen; og X er oxygen eller carbon.
2. Triazolopyrazinderivat ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, hvor Ri til R3 er hver uafhængigt hydrogen; halogen; pyrazol substitueret med methyl, hydroxyethyl, piperidin, eller N-methylpiperidin; tetrahydropyridin usubstitueret eller substitueret med methyl eller hydroxyethyl; phenyl substitueret med halogen, morpholinoethoxy, piperazinylethoxy, piperazinylmethyl, morpholinomethyl, acetylpiperazin, eller piperazinylcarbonyl; morpholinoethoxy; piperazinylethoxy; eller piperidin usubstitueret eller substitueret med methyl eller hydroxyethyl, hvor to af Ri til R3 er hydrogen.
3. Triazolopyrazinderivat ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, hvor R4 og Rs er hver uafhængigt hydrogen; N-methylpyrazol; eller phenyl substitueret med cyano eller halogen, hvor én af R4 og Rs er hydrogen.
4. Triazolopyrazinderivat ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, hvor triazolopyrazinet vist med den kemiske formel 1 er valgt fra gruppen bestående af forbindelser vist med de kemiske formler 2 til 50 nedenfor: kemisk formel 2 kemisk formel 3
kemisk formel 4 kemisk formel 5
kemisk formel 6 kemisk formel 7
5. Triazolopyrazinderivat ifølge krav 4, eller et farmaceutisk acceptabelt salt deraf, hvor triazolopyrazinderivat er valgt fra gruppen bestående af forbindelser vist med de kemiske formler 6 til 9, 11 til 13, 17, 23, 24, 26 til 32, og 38.
6. Farmaceutisk sammensætning til anvendelse i inhibering af c-Met- tyrosinkinaseaktivitet, farmaceutisk sammensætning indeholdende, som aktiv bestanddel, triazolopyrazinderivat ifølge et af kravene 1 til 5, eller et farmaceutisk acceptabelt salt eller solvat deraf.
7. Farmaceutisk sammensætning til anvendelse i forebyggelse eller behandling af hyperproliferative sygdomme, farmaceutisk sammensætning indeholdende, som aktiv bestanddel, triazolopyrazinderivat ifølge et af kravene 1 til 5, eller et farmaceutisk acceptabelt salt eller solvat deraf.
8. Farmaceutisk sammensætning til anvendelse ifølge krav 7, hvor de hyperproliferative sygdomme er valgt fra gruppen bestående af cancer, diabetisk retinopati, retinopati af præmaturitet, corneal transplantatafstødning, neovaskulær glaucom, erythrosis, proliferativ retinopati, psoriasis, rheumatoid arthritis, osteoarthritis, autoimmune sygdomme, Crohn's sygdom, restenose, atherosclerose, entero-adhæsion, mavesår, cirrhosis, glomerulonephritis, diabetisk nefropati, malignant nephrosclerose, thrombotisk mikroangiopati, organ transplantatafstødning, og glomerulopati.
9. Farmaceutisk sammensætning til anvendelse ifølge krav 8, hvor canceren er lungecancer, gastrisk cancer, bugspytkirtelcancer, coloncancer, æggestokcancer, nyrecellecancer, prostatacancer, eller hjernetumor.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/KR2013/008740 WO2015046653A1 (ko) | 2013-09-30 | 2013-09-30 | 신규한 트리아졸로 피라진 유도체 및 그의 용도 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3053923T3 true DK3053923T3 (da) | 2018-07-23 |
Family
ID=52743772
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK13894061.4T DK3053923T3 (da) | 2013-09-30 | 2013-09-30 | Triazolopyrazinderivater som tyrosin kinaseinhibitorer |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9403831B2 (da) |
| EP (1) | EP3053923B1 (da) |
| JP (1) | JP6039095B2 (da) |
| CN (1) | CN104703988B (da) |
| AU (1) | AU2013402175B2 (da) |
| BR (1) | BR112016006444B1 (da) |
| CA (1) | CA2923533C (da) |
| DK (1) | DK3053923T3 (da) |
| ES (1) | ES2675355T3 (da) |
| MX (1) | MX368311B (da) |
| RU (1) | RU2643361C2 (da) |
| WO (1) | WO2015046653A1 (da) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190077A1 (ar) * | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| KR20180092096A (ko) | 2017-02-08 | 2018-08-17 | 에이비온 주식회사 | 트리아졸로 피라진 유도체의 신규한 다형체 및 이의 제조 방법 |
| CN108570053A (zh) * | 2017-03-13 | 2018-09-25 | 中国科学院上海药物研究所 | 五元并六元杂环化合物、制备方法、中间体、组合和应用 |
| CA3135555C (en) | 2019-04-02 | 2023-09-19 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| KR102267662B1 (ko) * | 2019-11-19 | 2021-06-22 | 한국화학연구원 | 벤즈아미드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| US20220235054A1 (en) * | 2021-01-27 | 2022-07-28 | Abion Inc | Novel maleate salts of triazolopyrazine derivatives, compositions, methods of use, and processes of manufacturing the same |
| US20230416255A1 (en) * | 2022-06-27 | 2023-12-28 | Abion Inc. | Mesylate salts of triazolopyrazine derivatives |
| US11964979B2 (en) * | 2022-06-27 | 2024-04-23 | Abion Inc. | Camsylate salts of triazolopyrazine derivatives |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2401330T3 (es) | 2003-02-26 | 2013-04-18 | Sugen, Inc. | Compuesto de heteroarilamino inhibidores de proteín quinasas |
| WO2006021886A1 (en) | 2004-08-26 | 2006-03-02 | Pfizer Inc. | Aminoheteroaryl compounds as protein tyrosine kinase inhibitors |
| DK1784396T3 (da) | 2004-08-26 | 2011-02-14 | Pfizer | Pyrazol-substituerede aminoheteroaryl-forbindelser som proteinkinase-inhibitorer |
| EP1871377A1 (en) * | 2005-02-25 | 2008-01-02 | Kudos Pharmaceuticals Ltd | 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors |
| CA2630884A1 (en) | 2005-11-30 | 2007-06-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-met and uses thereof |
| NL2000613C2 (nl) * | 2006-05-11 | 2007-11-20 | Pfizer Prod Inc | Triazoolpyrazinederivaten. |
| DE102008037790A1 (de) * | 2008-08-14 | 2010-02-18 | Merck Patent Gmbh | Bicyclische Triazolderivate |
| WO2011058478A1 (en) * | 2009-11-16 | 2011-05-19 | Pfizer Inc. | Substituted triazolopyrimidines as pde8 inhibitors |
| CN106432225B (zh) * | 2009-12-31 | 2019-02-19 | 和记黄埔医药（上海）有限公司 | 某些三唑并吡啶化合物和三唑并吡嗪化合物、其组合物和其使用方法 |
-
2013
- 2013-09-30 US US14/435,974 patent/US9403831B2/en active Active
- 2013-09-30 CA CA2923533A patent/CA2923533C/en active Active
- 2013-09-30 DK DK13894061.4T patent/DK3053923T3/da active
- 2013-09-30 BR BR112016006444-5A patent/BR112016006444B1/pt active IP Right Grant
- 2013-09-30 WO PCT/KR2013/008740 patent/WO2015046653A1/ko active Application Filing
- 2013-09-30 ES ES13894061.4T patent/ES2675355T3/es active Active
- 2013-09-30 AU AU2013402175A patent/AU2013402175B2/en active Active
- 2013-09-30 RU RU2016112963A patent/RU2643361C2/ru active
- 2013-09-30 MX MX2016003968A patent/MX368311B/es active IP Right Grant
- 2013-09-30 EP EP13894061.4A patent/EP3053923B1/en active Active
- 2013-09-30 JP JP2015539492A patent/JP6039095B2/ja active Active
- 2013-09-30 CN CN201380051661.0A patent/CN104703988B/zh active Active
Also Published As
| Publication number | Publication date |
|---|---|
| BR112016006444A2 (pt) | 2017-08-01 |
| RU2643361C2 (ru) | 2018-02-01 |
| BR112016006444B1 (pt) | 2021-01-19 |
| US20150259350A1 (en) | 2015-09-17 |
| EP3053923B1 (en) | 2018-04-11 |
| JP2015535242A (ja) | 2015-12-10 |
| EP3053923A1 (en) | 2016-08-10 |
| CN104703988B (zh) | 2017-04-12 |
| MX368311B (es) | 2019-09-27 |
| AU2013402175A1 (en) | 2016-04-28 |
| AU2013402175B2 (en) | 2017-09-07 |
| US9403831B2 (en) | 2016-08-02 |
| WO2015046653A1 (ko) | 2015-04-02 |
| MX2016003968A (es) | 2017-01-06 |
| CN104703988A (zh) | 2015-06-10 |
| ES2675355T3 (es) | 2018-07-10 |
| CA2923533A1 (en) | 2015-04-02 |
| CA2923533C (en) | 2019-08-06 |
| JP6039095B2 (ja) | 2016-12-07 |
| EP3053923A4 (en) | 2017-04-12 |
| RU2016112963A (ru) | 2017-11-09 |
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