PE20191715A1 - Derivados de pirrolotriazina como inhibidor de cinasas - Google Patents
Derivados de pirrolotriazina como inhibidor de cinasasInfo
- Publication number
- PE20191715A1 PE20191715A1 PE2019001453A PE2019001453A PE20191715A1 PE 20191715 A1 PE20191715 A1 PE 20191715A1 PE 2019001453 A PE2019001453 A PE 2019001453A PE 2019001453 A PE2019001453 A PE 2019001453A PE 20191715 A1 PE20191715 A1 PE 20191715A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compounds
- triazin
- pyrrolo
- oxy
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000003921 pyrrolotriazines Chemical class 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 abstract 2
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 abstract 2
- 102000015617 Janus Kinases Human genes 0.000 abstract 2
- 108010024121 Janus Kinases Proteins 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 229910052736 halogen Chemical group 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- SUPXSFXAMJPEPH-UHFFFAOYSA-N 5h-pyrrolo[3,2-d]triazine Chemical compound N1=NC=C2NC=CC2=N1 SUPXSFXAMJPEPH-UHFFFAOYSA-N 0.000 abstract 1
- VBVJXWLONOIZSB-UHFFFAOYSA-N N-[3-[2-[(1-cyclopropylpyrazol-4-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-4-yl]oxy-4-fluorophenyl]prop-2-enamide Chemical compound C1(CC1)N1N=CC(=C1)NC1=NN2C(C(=N1)OC=1C=C(C=CC=1F)NC(C=C)=O)=CC=C2 VBVJXWLONOIZSB-UHFFFAOYSA-N 0.000 abstract 1
- OYBHTCNVFPRUMK-UHFFFAOYSA-N N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]pyrrolo[2,1-f][1,2,4]triazin-4-yl]oxyphenyl]prop-2-enamide Chemical compound CN1CCN(CC1)C1=CC=C(NC2=NN3C=CC=C3C(OC3=CC=CC(NC(=O)C=C)=C3)=N2)C=C1 OYBHTCNVFPRUMK-UHFFFAOYSA-N 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invencion se refiere a compuestos derivados de pirrolotriazina de Formula Quimica 1 o una sal farmaceuticamente aceptable de los mismos, donde: X es O, o NH; A es un anillo aromatico C6-10 divalente, o un anillo heteroaromatico C2-10 divalente; R1 es H o alquilo C1-4 no sustituido o sustituido; R2 es hidrogeno, alquilo C1-4 o halogeno; y R3 es alquilo C1-4 sustituido con halogeno, ciano, entre otros. Son compuestos preferidos: N- (3-((2-((1-ciclopropil-1H-pirazol-4-il)amino)pirrolo[2,1-f][1,2,4] triazin-4-il)oxi)-4-fluorofenil) acrilamida; N-(3-((2-((4-(4-metilpiperazin-1-il)fenil)amino)pirrolo[2,1-f][1,2,4]triazin-4-il)oxi) fenil)acrilamida, entre otros. Dichos compuestos son inhibidores de cinasas JAK (Janus cinasa) y/o BTK (Tirosin cinasa de Bruton), siendo utiles en el tratamiento o prevencion de enfermedades inflamatorias, autoinmunes, proliferativas, cancer o tumor, entre otros. Tambien se refiere a composiciones que los contiene.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020170034059A KR102398659B1 (ko) | 2017-03-17 | 2017-03-17 | 카이네이즈 저해제로서의 피롤로트리아진 유도체 |
| PCT/KR2018/003140 WO2018169373A1 (en) | 2017-03-17 | 2018-03-19 | Pyrrolotriazine derivatives as kinase inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20191715A1 true PE20191715A1 (es) | 2019-12-05 |
Family
ID=63522428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019001453A PE20191715A1 (es) | 2017-03-17 | 2018-03-19 | Derivados de pirrolotriazina como inhibidor de cinasas |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US11084823B2 (es) |
| EP (1) | EP3596081A4 (es) |
| JP (1) | JP6864124B2 (es) |
| KR (2) | KR102398659B1 (es) |
| CN (1) | CN110167943B (es) |
| AU (1) | AU2018236672B2 (es) |
| BR (1) | BR112019015428A2 (es) |
| CA (1) | CA3049648C (es) |
| CL (1) | CL2019002025A1 (es) |
| CO (1) | CO2019007836A2 (es) |
| DO (1) | DOP2019000194A (es) |
| EC (1) | ECSP19051377A (es) |
| IL (1) | IL269144B2 (es) |
| MX (1) | MX394038B (es) |
| MY (1) | MY189983A (es) |
| NZ (1) | NZ755298A (es) |
| PE (1) | PE20191715A1 (es) |
| PH (1) | PH12019502046A1 (es) |
| RU (1) | RU2726632C1 (es) |
| SA (1) | SA519402114B1 (es) |
| SG (1) | SG11201906467VA (es) |
| WO (1) | WO2018169373A1 (es) |
| ZA (1) | ZA201904554B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12156523B2 (en) | 2017-03-17 | 2024-12-03 | Mmag Co., Ltd. | Plant disease control agent |
| CN113498352A (zh) | 2019-01-23 | 2021-10-12 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪 |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000071129A1 (en) | 1999-05-21 | 2000-11-30 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| US7102002B2 (en) * | 2004-06-16 | 2006-09-05 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| MX2008007103A (es) | 2005-12-02 | 2008-09-12 | Bayer Healthcare Llc | Derivados 4-amino-pirrolotriazina sustituidos, útiles para tratar trastornos hiperproliferativos y enfermedades asociadas con angiogenesis. |
| CN101379065A (zh) * | 2006-01-23 | 2009-03-04 | 克里斯特尔吉诺密斯株式会社 | 抑制蛋白质激酶活性的咪唑并吡啶衍生物、其制备方法和包含它的药物组合物 |
| SI2215094T1 (sl) * | 2007-11-15 | 2016-05-31 | Ym Biosciences Australia Pty Ltd | N vsebujoče heterociklične spojine |
| MX2011000661A (es) | 2008-07-16 | 2011-05-25 | Pharmacyclics Inc | Inhibidores de tirosina cinasa de bruton para el tratamiento de tumores solidos. |
| WO2011079231A1 (en) * | 2009-12-23 | 2011-06-30 | Gatekeeper Pharmaceutical, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| EP2566869B1 (en) * | 2010-05-07 | 2016-03-02 | Gilead Connecticut, Inc. | Pyridone and aza-pyridone compounds and methods of use |
| CN103814030A (zh) | 2011-09-22 | 2014-05-21 | 辉瑞大药厂 | 吡咯并嘧啶及嘌呤衍生物 |
| US9745320B2 (en) | 2013-01-18 | 2017-08-29 | Guangzhou Maxinovel Pharmaceuticals Co., Ltd. | Five-and-six-membered heterocyclic compound, and preparation method, pharmaceutical composition and use thereof |
| US9206188B2 (en) | 2013-04-18 | 2015-12-08 | Arrien Pharmaceuticals Llc | Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors |
| CN104311573B (zh) | 2013-09-18 | 2017-12-15 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| CN104974163B (zh) * | 2014-04-14 | 2017-11-07 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| CN104829610B (zh) | 2014-06-20 | 2017-03-15 | 中国科学院合肥物质科学研究院 | 一种新型布鲁顿酪氨酸激酶抑制剂 |
| CN105837572B (zh) | 2015-02-02 | 2019-04-19 | 四川大学 | N-取代苯基酰胺衍生物及其制备方法和用途 |
| CN105646497B (zh) * | 2016-02-01 | 2019-06-04 | 南京格亚医药科技有限公司 | 吡咯并三嗪酮衍生物 |
| CN106432249B (zh) * | 2016-09-30 | 2018-12-04 | 陕西科技大学 | 一类吡咯并[2，1-f][1，2，4]三嗪母核化合物的合成及其医药用途 |
-
2017
- 2017-03-17 KR KR1020170034059A patent/KR102398659B1/ko active Active
-
2018
- 2018-03-19 MX MX2019010595A patent/MX394038B/es unknown
- 2018-03-19 MY MYPI2019004124A patent/MY189983A/en unknown
- 2018-03-19 US US16/478,920 patent/US11084823B2/en active Active
- 2018-03-19 BR BR112019015428-0A patent/BR112019015428A2/pt not_active Application Discontinuation
- 2018-03-19 EP EP18766994.0A patent/EP3596081A4/en active Pending
- 2018-03-19 NZ NZ755298A patent/NZ755298A/en unknown
- 2018-03-19 RU RU2019123998A patent/RU2726632C1/ru active
- 2018-03-19 AU AU2018236672A patent/AU2018236672B2/en active Active
- 2018-03-19 JP JP2019571195A patent/JP6864124B2/ja active Active
- 2018-03-19 WO PCT/KR2018/003140 patent/WO2018169373A1/en not_active Ceased
- 2018-03-19 CN CN201880006529.0A patent/CN110167943B/zh active Active
- 2018-03-19 CA CA3049648A patent/CA3049648C/en active Active
- 2018-03-19 SG SG11201906467VA patent/SG11201906467VA/en unknown
- 2018-03-19 PE PE2019001453A patent/PE20191715A1/es unknown
-
2019
- 2019-07-08 SA SA519402114A patent/SA519402114B1/ar unknown
- 2019-07-11 ZA ZA2019/04554A patent/ZA201904554B/en unknown
- 2019-07-17 EC ECSENADI201951377A patent/ECSP19051377A/es unknown
- 2019-07-19 CL CL2019002025A patent/CL2019002025A1/es unknown
- 2019-07-22 CO CONC2019/0007836A patent/CO2019007836A2/es unknown
- 2019-07-24 DO DO2019000194A patent/DOP2019000194A/es unknown
- 2019-09-05 IL IL269144A patent/IL269144B2/en unknown
- 2019-09-09 PH PH12019502046A patent/PH12019502046A1/en unknown
-
2022
- 2022-04-18 KR KR1020220047811A patent/KR102428882B1/ko active Active
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