AR071208A1 - Derivados de piridazinona - Google Patents
Derivados de piridazinonaInfo
- Publication number
- AR071208A1 AR071208A1 ARP090101359A ARP090101359A AR071208A1 AR 071208 A1 AR071208 A1 AR 071208A1 AR P090101359 A ARP090101359 A AR P090101359A AR P090101359 A ARP090101359 A AR P090101359A AR 071208 A1 AR071208 A1 AR 071208A1
- Authority
- AR
- Argentina
- Prior art keywords
- nhet
- hal
- atoms
- mono
- nhet1
- Prior art date
Links
- 125000004429 atom Chemical group 0.000 abstract 4
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 abstract 2
- FPYJSJDOHRDAMT-KQWNVCNZSA-N 1h-indole-5-sulfonamide, n-(3-chlorophenyl)-3-[[3,5-dimethyl-4-[(4-methyl-1-piperazinyl)carbonyl]-1h-pyrrol-2-yl]methylene]-2,3-dihydro-n-methyl-2-oxo-, (3z)- Chemical compound C=1C=C2NC(=O)\C(=C/C3=C(C(C(=O)N4CCN(C)CC4)=C(C)N3)C)C2=CC=1S(=O)(=O)N(C)C1=CC=CC(Cl)=C1 FPYJSJDOHRDAMT-KQWNVCNZSA-N 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 235000010290 biphenyl Nutrition 0.000 abstract 1
- 239000004305 biphenyl Substances 0.000 abstract 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000000169 tricyclic heterocycle group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Los compuestos de la formula (1) en donde R1 es H, A, Ar o Het; R2 es H, A, Hal, OR3, N(R3)2, N=CR3N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, Het, -[C(R3)2]nN(R3)2, -[C(R3)2]nHet, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet, S[C(R3)2]nN(R3)2, S[C(R3)2]nHet, -NR3[C(R3)2]nN(R3)2, -NR3[C(R3)2]nHet, NHCON(R3)2, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet, NHCO[C(R3)2]nN(R3)2, -NHCO[C(R3)2]nHet, CON(R3)2, CONR3[C(R3)2]nN(R3)2, CONR3[C(R3)2]nHet, COHet o COA; R3 es H o A; W es un heterociclo insaturado o aromático de cinco o seis miembros con 1 a 3 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal y/o A; D es un heterociclo insaturado o aromático de cinco o seis miembros con 1 a 3 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal y/o A; A es alquilo no ramificado o ramificado C1-10, en donde 1-7 átomos de H pueden estar reemplazados por OH, F Cl y/o Br, y/o en donde uno o dos grupos CH2 pueden estar reemplazados por O, NH, S, SO, SO2 y/o grupos CH=CH, o alquilo cíclico con 3-7 átomos de C; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2 y/o S(O)mA; Het es un heterociclo saturado, insaturado o aromático mono-, bi- o tricíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het1, Het1, [C(R3)2]nN(R3)2, [C(R3)2]nHet1, O(C(R3)2]nN(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1, CO-Het1, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo); Het1 es un heterociclo saturado monocíclico con 1 a 2 átomos de N y/u O, que puede estar mono- o disustituido con A, OA, OH, Hal y/u =O (oxígeno del carbonilo); Hal es F, Cl, Br o I; m es 0, 1 o 2, n es 1, 2, 3 o 4; así como sus sales, tautomeros y estereoisomeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de las tirosina quinasas, en especial de la Metquinasa, y pueden utilizarse, por ejemplo, para el tratamiento de tumores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102008019907A DE102008019907A1 (de) | 2008-04-21 | 2008-04-21 | Pyridazinonderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR071208A1 true AR071208A1 (es) | 2010-06-02 |
Family
ID=40639931
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090101359A AR071208A1 (es) | 2008-04-21 | 2009-04-17 | Derivados de piridazinona |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8604036B2 (es) |
| EP (1) | EP2280962B1 (es) |
| JP (1) | JP5576358B2 (es) |
| KR (1) | KR20100137564A (es) |
| CN (1) | CN102015694A (es) |
| AR (1) | AR071208A1 (es) |
| AU (1) | AU2009240346B2 (es) |
| BR (1) | BRPI0911161B8 (es) |
| CA (1) | CA2721858C (es) |
| CY (1) | CY1113443T1 (es) |
| DE (1) | DE102008019907A1 (es) |
| DK (1) | DK2280962T5 (es) |
| EA (1) | EA018362B1 (es) |
| ES (1) | ES2394147T3 (es) |
| HR (1) | HRP20120884T1 (es) |
| IL (1) | IL208336A (es) |
| MX (1) | MX2010011454A (es) |
| PL (1) | PL2280962T3 (es) |
| PT (1) | PT2280962E (es) |
| SI (1) | SI2280962T1 (es) |
| WO (1) | WO2009129905A1 (es) |
| ZA (1) | ZA201008330B (es) |
Families Citing this family (17)
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|---|---|---|---|---|
| DE102007026341A1 (de) | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
| DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102007038957A1 (de) * | 2007-08-17 | 2009-02-19 | Merck Patent Gmbh | 6-Thioxo-pyridazinderivate |
| DE102007061963A1 (de) * | 2007-12-21 | 2009-06-25 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102008019907A1 (de) | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102008028905A1 (de) * | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
| DE102008037790A1 (de) * | 2008-08-14 | 2010-02-18 | Merck Patent Gmbh | Bicyclische Triazolderivate |
| MY160526A (en) | 2008-12-22 | 2017-03-15 | Merck Patent Gmbh | Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof |
| CN102532126B (zh) * | 2012-02-10 | 2014-06-18 | 贵州大学 | 2-取代-4-氯-5-[5-取代胺基-2-(1,3,4-噻二唑基)-巯基]-3(2h)-哒嗪酮类衍生物及其制备方法和用途 |
| AU2017348186A1 (en) * | 2016-10-26 | 2019-05-16 | Proteostasis Therapeutics, Inc | Pyridazine derivatives, compositions and methods for modulating CFTR |
| ES2946551T3 (es) | 2017-10-17 | 2023-07-20 | Palau Pharma S L U | Síntesis de compuestos de 4-aminopirimidina |
| CN108752322A (zh) * | 2018-09-12 | 2018-11-06 | 广州新民培林医药科技有限公司 | 一种新型Tepotinib衍生物和制备方法及其在抗肿瘤药物中的应用 |
| AU2019376065B2 (en) | 2018-11-06 | 2025-03-06 | Edgewise Therapeutics, Inc. | Pyridazinone compounds and uses thereof |
| DK3877052T3 (da) | 2018-11-06 | 2023-09-25 | Edgewise Therapeutics Inc | Pyridazinonforbindelser og anvendelser deraf |
| WO2020097258A1 (en) | 2018-11-06 | 2020-05-14 | Edgewise Therapeutics, Inc. | Pyridazinone compounds and uses thereof |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| WO2021085550A1 (ja) | 2019-11-01 | 2021-05-06 | ユニマテック株式会社 | 含フッ素ピリミジン化合物およびその製造方法 |
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-
2008
- 2008-04-21 DE DE102008019907A patent/DE102008019907A1/de not_active Withdrawn
-
2009
- 2009-03-24 EP EP09734854A patent/EP2280962B1/de active Active
- 2009-03-24 EA EA201001648A patent/EA018362B1/ru not_active IP Right Cessation
- 2009-03-24 AU AU2009240346A patent/AU2009240346B2/en not_active Ceased
- 2009-03-24 US US12/988,666 patent/US8604036B2/en not_active Expired - Fee Related
- 2009-03-24 ES ES09734854T patent/ES2394147T3/es active Active
- 2009-03-24 CN CN2009801141150A patent/CN102015694A/zh active Pending
- 2009-03-24 BR BRPI0911161A patent/BRPI0911161B8/pt not_active IP Right Cessation
- 2009-03-24 DK DK09734854.4T patent/DK2280962T5/da active
- 2009-03-24 MX MX2010011454A patent/MX2010011454A/es active IP Right Grant
- 2009-03-24 PT PT97348544T patent/PT2280962E/pt unknown
- 2009-03-24 HR HRP20120884AT patent/HRP20120884T1/hr unknown
- 2009-03-24 JP JP2011505385A patent/JP5576358B2/ja not_active Expired - Fee Related
- 2009-03-24 CA CA2721858A patent/CA2721858C/en active Active
- 2009-03-24 WO PCT/EP2009/002137 patent/WO2009129905A1/de not_active Ceased
- 2009-03-24 KR KR1020107025412A patent/KR20100137564A/ko not_active Ceased
- 2009-03-24 PL PL09734854T patent/PL2280962T3/pl unknown
- 2009-03-24 SI SI200930411T patent/SI2280962T1/sl unknown
- 2009-04-17 AR ARP090101359A patent/AR071208A1/es not_active Application Discontinuation
-
2010
- 2010-09-21 IL IL208336A patent/IL208336A/en active IP Right Grant
- 2010-11-19 ZA ZA2010/08330A patent/ZA201008330B/en unknown
-
2012
- 2012-12-07 CY CY20121101191T patent/CY1113443T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0911161B1 (pt) | 2020-02-11 |
| ZA201008330B (en) | 2011-09-28 |
| CA2721858A1 (en) | 2009-10-29 |
| IL208336A (en) | 2016-07-31 |
| SI2280962T1 (sl) | 2013-01-31 |
| DE102008019907A1 (de) | 2009-10-22 |
| CY1113443T1 (el) | 2016-06-22 |
| US8604036B2 (en) | 2013-12-10 |
| DK2280962T3 (da) | 2012-11-19 |
| EP2280962B1 (de) | 2012-10-03 |
| WO2009129905A1 (de) | 2009-10-29 |
| DK2280962T5 (da) | 2013-09-16 |
| JP5576358B2 (ja) | 2014-08-20 |
| EA201001648A1 (ru) | 2011-06-30 |
| PT2280962E (pt) | 2012-12-17 |
| AU2009240346B2 (en) | 2013-10-10 |
| ES2394147T3 (es) | 2013-01-22 |
| HRP20120884T1 (hr) | 2012-11-30 |
| EA018362B1 (ru) | 2013-07-30 |
| IL208336A0 (en) | 2010-12-30 |
| KR20100137564A (ko) | 2010-12-30 |
| BRPI0911161A2 (pt) | 2015-10-06 |
| CN102015694A (zh) | 2011-04-13 |
| CA2721858C (en) | 2016-07-19 |
| AU2009240346A1 (en) | 2009-10-29 |
| JP2011518202A (ja) | 2011-06-23 |
| US20110034474A1 (en) | 2011-02-10 |
| EP2280962A1 (de) | 2011-02-09 |
| PL2280962T3 (pl) | 2013-02-28 |
| MX2010011454A (es) | 2010-12-21 |
| BRPI0911161B8 (pt) | 2021-05-25 |
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