AR106301A1 - Composiciones de pirrolpirimidina como inhibidores de quinasas - Google Patents
Composiciones de pirrolpirimidina como inhibidores de quinasasInfo
- Publication number
- AR106301A1 AR106301A1 ARP160103082A ARP160103082A AR106301A1 AR 106301 A1 AR106301 A1 AR 106301A1 AR P160103082 A ARP160103082 A AR P160103082A AR P160103082 A ARP160103082 A AR P160103082A AR 106301 A1 AR106301 A1 AR 106301A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- substituted
- halo
- hydroxyl
- Prior art date
Links
Classifications
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
- 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
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicación 1: Una composición farmacéutica caracterizada porque comprende: (a) un compuesto de la fórmula (1), en donde X¹ es O, NH, o S; R¹ y R² son cada uno, independientemente, hidrógeno, halo, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; R³ es halo, hidroxilo, C₁₋₆ alquilo, C₁₋₆ alcoxi, ciano, o nitro; n es 0, 1, 2, 3 ó 4; R⁴ es hidrógeno, C₁₋₆ alquilo, C₃₋₇ cicloalquilo, o -NR²²R²³; en donde el alquilo y el cicloalquilo no están sustituidos o están sustituidos con hidroxilo o amino; y R²² y R²³ son cada uno, independientemente, hidrógeno o C₁₋₆ alquilo; o R²² y R²³ tomados junto con el nitrógeno al que están unidos, forman un anillo heterocicloalquilo de entre 3 y 10 miembros; R⁵ es hidrógeno o C₁₋₄ alquilo; R⁶ y R⁷ son cada uno, independientemente, hidrógeno, halo, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₂₋₆ alcoxi, C₁₋₆ haloalcoxi, hidroxilo, ciano, o nitro; R⁸ es hidrógeno, halo, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ alcoxi, C₁₋₆ haloalcoxi, hidroxilo, ciano, o nitro; R¹¹ y R¹² son cada uno, independientemente, hidrógeno o C₁₋₆ alquilo; Q es CR⁹ o N; donde R⁹ es hidrógeno, halo, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ alcoxi, C₁₋₆ haloalcoxi, hidroxilo, ciano, o nitro; -NR¹⁸R¹⁹ es: (a) un compuesto de fórmula (2) ó (3); donde R¹⁰ se selecciona entre hidrógeno y C₁₋₆ alquilo; R¹⁵ es metilo no sustituido, o es C₂₋₄ alquilo no sustituido o sustituido con hidroxi, metoxi, o halo; y m es 1 ó 2; o (b) R¹⁹ y R⁹ se toman junto con los átomos a los que están unidos para formar un anillo heteroarilo de 5 ó 6 miembros, opcionalmente sustituido con C₁₋₆ alquilo, en donde el alquilo no está sustituido o está sustituido con amino, hidroxilo, halo, o un heterocicloalquilo conectado al N; y R¹⁸ es hidrógeno o C₁₋₆ alquilo, donde el alquilo no está sustituido o está sustituido con amino, o R¹⁸ está ausente para satisfacer la valencia del anillo heteroarilo; o Compuesto de fórmula (4), o una sal farmacéuticamente aceptable del compuesto de la fórmula (1) o Compuesto de fórmula (4); y (b) un agente de adsorción que reduce o suprime la formación de un dímero del compuesto, o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2015091536 | 2015-10-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR106301A1 true AR106301A1 (es) | 2018-01-03 |
Family
ID=58487279
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160103082A AR106301A1 (es) | 2015-10-09 | 2016-10-07 | Composiciones de pirrolpirimidina como inhibidores de quinasas |
Country Status (14)
Country | Link |
---|---|
US (1) | US10533011B2 (es) |
EP (1) | EP3359159B1 (es) |
JP (1) | JP6889494B2 (es) |
KR (1) | KR20180067584A (es) |
CN (1) | CN107949388B (es) |
AR (1) | AR106301A1 (es) |
AU (1) | AU2016334141B2 (es) |
BR (1) | BR112018006939A2 (es) |
CA (1) | CA3001744A1 (es) |
HK (1) | HK1253537A1 (es) |
MX (1) | MX2018004332A (es) |
RU (1) | RU2018115334A (es) |
TW (1) | TW201722431A (es) |
WO (1) | WO2017059702A1 (es) |
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KR102173433B1 (ko) | 2013-07-11 | 2020-11-04 | 에이시아 바이오사이언시스 인코포레이티드. | 키나아제 억제제로써의 피리미딘 유도체 |
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CN111212837A (zh) * | 2017-04-07 | 2020-05-29 | 艾森医药公司 | 吡咯并嘧啶激酶抑制剂的药用盐、物理形态和组合物及其制备方法 |
MA53388A (fr) | 2018-07-25 | 2021-06-02 | Novartis Ag | Inhibiteurs d'inflammasome nlrp3 |
AR119731A1 (es) | 2019-05-17 | 2022-01-05 | Novartis Ag | Inhibidores del inflamasoma nlrp3 |
CN110407840A (zh) * | 2019-08-15 | 2019-11-05 | 重庆化工职业学院 | 一种艾维替尼的制备方法 |
US11708366B2 (en) | 2020-08-14 | 2023-07-25 | Novartis Ag | Heteroaryl substituted spiropiperidinyl derivatives and pharmaceutical uses thereof |
CN111848631B (zh) * | 2020-08-28 | 2022-04-19 | 四川大学华西医院 | 一种靶向EGFR突变的吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途 |
CN114573591B (zh) * | 2022-04-16 | 2023-04-25 | 成都施贝康生物医药科技有限公司 | 一种取代的吡咯并嘧啶化合物及其应用 |
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2016
- 2016-06-30 WO PCT/CN2016/087857 patent/WO2017059702A1/en active Application Filing
- 2016-06-30 CA CA3001744A patent/CA3001744A1/en active Pending
- 2016-06-30 CN CN201680021771.6A patent/CN107949388B/zh active Active
- 2016-06-30 JP JP2018537705A patent/JP6889494B2/ja active Active
- 2016-06-30 RU RU2018115334A patent/RU2018115334A/ru not_active Application Discontinuation
- 2016-06-30 US US15/766,736 patent/US10533011B2/en active Active
- 2016-06-30 KR KR1020187012886A patent/KR20180067584A/ko not_active Application Discontinuation
- 2016-06-30 EP EP16853009.5A patent/EP3359159B1/en active Active
- 2016-06-30 BR BR112018006939A patent/BR112018006939A2/pt not_active IP Right Cessation
- 2016-06-30 AU AU2016334141A patent/AU2016334141B2/en active Active
- 2016-06-30 MX MX2018004332A patent/MX2018004332A/es unknown
- 2016-10-07 TW TW105132675A patent/TW201722431A/zh unknown
- 2016-10-07 AR ARP160103082A patent/AR106301A1/es unknown
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2018
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CN107949388B (zh) | 2021-10-26 |
CA3001744A1 (en) | 2017-04-13 |
KR20180067584A (ko) | 2018-06-20 |
RU2018115334A3 (es) | 2019-11-29 |
TW201722431A (zh) | 2017-07-01 |
BR112018006939A2 (pt) | 2018-10-16 |
JP6889494B2 (ja) | 2021-06-18 |
RU2018115334A (ru) | 2019-11-11 |
US10533011B2 (en) | 2020-01-14 |
AU2016334141A1 (en) | 2018-04-26 |
EP3359159A1 (en) | 2018-08-15 |
JP2018530610A (ja) | 2018-10-18 |
US20180312510A1 (en) | 2018-11-01 |
HK1253537A1 (zh) | 2019-06-21 |
AU2016334141B2 (en) | 2019-12-19 |
MX2018004332A (es) | 2019-01-10 |
WO2017059702A1 (en) | 2017-04-13 |
CN107949388A (zh) | 2018-04-20 |
EP3359159B1 (en) | 2023-06-07 |
EP3359159A4 (en) | 2019-06-05 |
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