AR089727A1 - Compuesto de pirazin-carboxamida - Google Patents
Compuesto de pirazin-carboxamidaInfo
- Publication number
- AR089727A1 AR089727A1 ARP130100118A ARP130100118A AR089727A1 AR 089727 A1 AR089727 A1 AR 089727A1 AR P130100118 A ARP130100118 A AR P130100118A AR P130100118 A ARP130100118 A AR P130100118A AR 089727 A1 AR089727 A1 AR 089727A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- lower alkyl
- alkylene
- egfr
- mutation
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 abstract 6
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 abstract 6
- 230000035772 mutation Effects 0.000 abstract 6
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 abstract 6
- -1 pyrazin-carboxamide compound Chemical class 0.000 abstract 6
- 125000002947 alkylene group Chemical group 0.000 abstract 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 3
- 201000011510 cancer Diseases 0.000 abstract 3
- 201000005202 lung cancer Diseases 0.000 abstract 3
- 208000020816 lung neoplasm Diseases 0.000 abstract 3
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 abstract 3
- 239000005483 tyrosine kinase inhibitor Substances 0.000 abstract 3
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 abstract 2
- 102000004169 proteins and genes Human genes 0.000 abstract 2
- 108090000623 proteins and genes Proteins 0.000 abstract 2
- 239000004576 sand Substances 0.000 abstract 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
- C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
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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
- C07D471/10—Spiro-condensed systems
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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
- C07D487/08—Bridged systems
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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
- C07D487/10—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Steroid Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
El compuesto de pirazin-carboxamida de la presente tiene una acción inhibidora sobre una quinasa con mutación T790M en el EGFR, y se puede usar como agente para prevenir y/o tratar el cáncer positivo con mutación T790M en el EGFR; en otra forma de realización, cáncer de pulmón positivo con mutación T790M en el EGRF; aún en otra forma de realización, cáncer de pulmón de células no pequeñas positivo con mutación T790M en el EGFR; también en otra forma de realización, cáncer de proteínas positivo con mutación T790M en el EGRF; en una forma de realización diferente, cáncer de pulmón de proteínas positivo con mutación T790M en el EGRF; aún en una forma de realización diferente, cáncer resistente al inhibidor de la tirosina quinasa en el EGFR; aún en una forma de realización diferente, cáncer de pulmón resistente al inhibidor de la tirosina quinasa en el EGFR; y también en otra forma de realización diferente, cáncer de pulmón de células no pequeñas resistente al inhibidor de la tirosina quinasa en el EGFR y similares. Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales, donde R¹ representa alquilo inferior que puede estar sustituido, -O-alquilo inferior que puede estar sustituido, -NH₂, -NH-alquilo inferior que puede estar sustituido, -N(alquilo inferior que puede estar sustituido)₂, -L⁴-cicloalquilo que puede estar sustituido, -L⁴-arilo que puede estar sustituido, -L⁴-grupo heterocíclico aromático que puede estar sustituido, o -L⁴-grupo heterocíclico no aromático que puede estar sustituido; el anillo A representa areno que puede estar sustituido o un heterociclo aromático que puede estar sustituido; L¹ representa -O- o -NH-; R² representa H, halógeno, -OH, -NR⁵R⁶, -CONH₂, -CN, -L⁴-cicloalquilo que puede estar sustituido, -L⁴-arilo que puede estar sustituido, -L⁴-grupo heterocíclico aromático que puede estar sustituido, -L⁴-grupo heterocíclico no aromático que puede estar sustituido, alquilo inferior que puede estar sustituido, alquenilo inferior que puede estar sustituido, o alquinilo inferior que puede estar sustituido; L² representa -O-, -S(O)ₚ-, -NH-, -N(CH₃)-, -NHCH₂-, -NHCH₂CH₂-, -OCH₂- o una unión; Y representa anillo X o una unión; el anillo X representa cicloalcano que puede estar sustituido, areno que puede estar sustituido, un heterociclo aromático que puede estar sustituido, o un heterociclo no aromático que puede estar sustituido; L³ representa -O-, -NH-, -N(alquilo inferior que puede estar sustituido)-, -N(cicloalquilo que puede estar sustituido), -alquileno inferior que puede estar sustituido-, -alquileno inferior que puede estar sustituido-NH-, -NH-alquileno inferior que puede estar sustituido-, -alquileno inferior que puede estar sustituido-N(alquilo inferior que puede estar sustituido)-, -N(alquilo inferior que puede estar sustituido)-alquileno inferior que puede estar sustituido- o una unión; M representa -C(O)- o -S(O)₂-; R³ representa H o alquilo inferior que puede estar sustituido; R⁴ representa alquilo inferior que puede estar sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste de -OH, halógeno, -NH₂, -NH-(alquilo inferior que puede estar sustituido), -N(alquilo inferior que puede estar sustituido)₂, y un grupo heterocíclico no aromático que puede estar sustituido, o H; R⁵ y R⁶ son iguales o diferentes entre sí, y representan H o alquilo inferior que puede estar sustituido; L⁴s son iguales o diferentes entre sí, y representan alquileno inferior que puede estar sustituido-, -NH-, -O-, -O-alquileno inferior que puede estar sustituido-, -alquileno inferior que puede estar sustituido-O- o una unión; y p representa 0, 1 ó 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012007525 | 2012-01-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089727A1 true AR089727A1 (es) | 2014-09-10 |
Family
ID=48799179
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130100118A AR089727A1 (es) | 2012-01-17 | 2013-01-15 | Compuesto de pirazin-carboxamida |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US9085540B2 (es) |
| EP (1) | EP2805940B1 (es) |
| JP (1) | JP5532366B2 (es) |
| KR (1) | KR101985050B1 (es) |
| CN (1) | CN104080774B (es) |
| AR (1) | AR089727A1 (es) |
| AU (1) | AU2013210438B2 (es) |
| BR (1) | BR112014017466A8 (es) |
| CA (1) | CA2860765C (es) |
| CY (1) | CY1118644T1 (es) |
| DK (1) | DK2805940T3 (es) |
| EA (1) | EA026353B1 (es) |
| ES (1) | ES2613399T3 (es) |
| HR (1) | HRP20170226T1 (es) |
| HU (1) | HUE033177T2 (es) |
| IL (1) | IL233437A (es) |
| LT (1) | LT2805940T (es) |
| ME (1) | ME02648B (es) |
| MX (1) | MX355434B (es) |
| PH (1) | PH12014501456A1 (es) |
| PL (1) | PL2805940T3 (es) |
| PT (1) | PT2805940T (es) |
| RS (1) | RS55704B1 (es) |
| SI (1) | SI2805940T1 (es) |
| SM (2) | SMT201700094T1 (es) |
| TW (1) | TWI532727B (es) |
| UA (1) | UA111010C2 (es) |
| WO (1) | WO2013108754A1 (es) |
| ZA (1) | ZA201405045B (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014163161A1 (ja) * | 2013-04-04 | 2014-10-09 | 武田薬品工業株式会社 | 複素環化合物 |
| HUE044683T2 (hu) * | 2013-10-21 | 2019-11-28 | Merck Patent Gmbh | Heteroaril vegyületek mint BTK inhibitorok és alkalmazásuk |
| RU2646758C2 (ru) * | 2013-12-05 | 2018-03-07 | Ф. Хоффманн-Ля Рош Аг | Гетероарил пиридоны и азапиридоны с электрофильной функциональностью |
| AU2014360446A1 (en) | 2013-12-05 | 2016-06-09 | Pharmacyclics, Llc | Inhibitors of Bruton's tyrosine kinase |
| TW201622744A (zh) | 2014-03-04 | 2016-07-01 | 美國禮來大藥廠 | 癌症之組合療法 |
| AU2015266552A1 (en) * | 2014-05-28 | 2016-12-01 | Astellas Pharma Inc. | Pharmaceutical composition comprising pyrazine carboxamide compound as active ingredient |
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技(上海)有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| WO2016121777A1 (ja) * | 2015-01-28 | 2016-08-04 | アステラス製薬株式会社 | ピラジンカルボキサミド化合物の製造方法及びその合成中間体 |
| EP3290036A4 (en) * | 2015-04-27 | 2019-01-02 | Astellas Pharma Inc. | Stabilized pharmaceutical composition |
| JP2018104290A (ja) * | 2015-04-28 | 2018-07-05 | アステラス製薬株式会社 | ピラジンカルボキサミド化合物を有効成分とする医薬組成物 |
| EP3310776A4 (en) * | 2015-06-02 | 2019-01-16 | Pharmacyclics LLC | BRUTON TYROSINE KINASE HEMMER |
| JP6878316B2 (ja) * | 2015-06-19 | 2021-05-26 | ノバルティス アーゲー | Shp2の活性を阻害するための化合物および組成物 |
| JP2019014653A (ja) * | 2015-11-27 | 2019-01-31 | アステラス製薬株式会社 | がん免疫を介したがん治療方法 |
| KR20180094923A (ko) * | 2015-12-24 | 2018-08-24 | 교와 핫꼬 기린 가부시키가이샤 | α, β 불포화 아미드 화합물 |
| WO2017176565A1 (en) | 2016-04-07 | 2017-10-12 | Eli Lilly And Company | Combinations of an anti-b7-h1 antibody and a cxcr4 peptide antagonist for treating a solid tumor |
| WO2018013597A1 (en) * | 2016-07-12 | 2018-01-18 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| JPWO2018079570A1 (ja) * | 2016-10-26 | 2019-09-19 | アステラス製薬株式会社 | 安定な医薬組成物 |
| WO2018103663A1 (zh) * | 2016-12-09 | 2018-06-14 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的吡嗪甲酰胺类化合物及包含该化合物的组合物及其用途 |
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| TWI798334B (zh) * | 2018-01-31 | 2023-04-11 | 大陸商迪哲(江蘇)醫藥股份有限公司 | Erbb/btk抑制劑 |
| CN112839930B (zh) | 2018-09-30 | 2022-03-15 | 南京明德新药研发有限公司 | 作为flt3和axl抑制剂的3,9-二氮杂螺[5,5]十一烷类化合物 |
| CN112062728A (zh) * | 2019-05-25 | 2020-12-11 | 上海鑫凯化学科技有限公司 | 一种3,5-二氯-6-乙基吡嗪甲酰胺的合成方法 |
| CN114728905B (zh) * | 2019-11-13 | 2025-08-01 | 基因泰克公司 | 治疗性化合物及使用方法 |
| CN111266090B (zh) * | 2020-02-19 | 2022-11-15 | 渤海大学 | 一种快速吸附和选择性分离阳离子染料污染物的吸附分离材料及其应用 |
| US20230167099A1 (en) * | 2020-06-01 | 2023-06-01 | Wigen Biomedicine Technology (shanghai) Co., Ltd. | New pyrazine compound |
| CN113943288A (zh) * | 2020-07-17 | 2022-01-18 | 微境生物医药科技(上海)有限公司 | 5,6-二氢吡嗪并[2,3-c]异喹啉化合物 |
| MX2023003731A (es) * | 2020-09-30 | 2023-04-24 | Beigene Ltd | Compuestos de 3-[(1h-pirazol-4-il)oxi]pirazin-2-amina como inhibidores de hpk1, y uso de los mismos. |
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| US7019012B2 (en) | 2000-12-20 | 2006-03-28 | Boehringer Ingelheim International Pharma Gmbh & Co. Kg | Quinazoline derivatives and pharmaceutical compositions containing them |
| DE10063435A1 (de) | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| AU2003304497B2 (en) | 2003-09-15 | 2010-06-24 | Wyeth Llc | Substituted quinolines as protein tyrosine kinase enzyme inhibitors |
| SI1746999T1 (sl) | 2004-05-06 | 2012-01-31 | Warner Lambert Co | 4-fenilamino-kinazolin-6-il-amidi |
| WO2008117050A1 (en) | 2007-03-27 | 2008-10-02 | Astrazeneca Ab | Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer |
| TWI377944B (en) | 2007-06-05 | 2012-12-01 | Hanmi Holdings Co Ltd | Novel amide derivative for inhibiting the growth of cancer cells |
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| CA2960692C (en) * | 2008-04-16 | 2019-09-24 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| TWI458721B (zh) | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Egfr 억제제 및 질환 치료방법 |
| DK2428508T3 (en) | 2009-05-08 | 2016-02-01 | Astellas Pharma Inc | Diamino heterocyclic carboxamide COMPOUND |
| WO2011140338A1 (en) | 2010-05-05 | 2011-11-10 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
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