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) | MX2019010595A (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 (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020154350A1 (en) | 2019-01-23 | 2020-07-30 | Theravance Biopharma R&D Ip, Llc | Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors |
| WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1183033T3 (da) | 1999-05-21 | 2006-06-06 | Bristol Myers Squibb Co | Pyrrolotriazininhibitorer af kinaser |
| 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 |
| JP5249776B2 (ja) | 2005-12-02 | 2013-07-31 | バイエル・ヘルスケア・エルエルシー | 過剰増殖性疾患および血管新生と関連する疾患を処置するために有用な置換された４−アミノ−ピロロトリアジン誘導体 |
| BRPI0707245A2 (pt) | 2006-01-23 | 2011-04-26 | Crystalgenomics Inc | derivados de imidazopiridina que inibem a atividade de proteìna quinase, método para a preparação destes e composição farmacêutica contendo os mesmos |
| US8354408B2 (en) * | 2007-11-15 | 2013-01-15 | Ym Biosciences Australia Pty Ltd | N-containing heterocyclic compounds |
| EP3311818A3 (en) | 2008-07-16 | 2018-07-18 | Pharmacyclics, LLC | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| US20110207736A1 (en) * | 2009-12-23 | 2011-08-25 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| RU2617405C2 (ru) | 2010-05-07 | 2017-04-25 | Джилид Коннектикут, Инк. | Пиридоновые и азапиридоновые соединения и способы применения |
| CA2847540C (en) * | 2011-09-22 | 2016-05-17 | Pfizer Inc. | Pyrrolopyrimidine and purine derivatives |
| EP2947084B8 (en) | 2013-01-18 | 2021-03-10 | Guangzhou Maxinovel Pharmaceuticals Co. | 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 |
| KR101879422B1 (ko) | 2013-09-18 | 2018-07-17 | 베이징 한미 파마슈티컬 컴퍼니 리미티드 | Btk 및/또는 jak3 키나제의 활성을 억제하는 화합물 |
| 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 IP Right Grant
-
2018
- 2018-03-19 MY MYPI2019004124A patent/MY189983A/en unknown
- 2018-03-19 JP JP2019571195A patent/JP6864124B2/ja active Active
- 2018-03-19 SG SG11201906467VA patent/SG11201906467VA/en unknown
- 2018-03-19 AU AU2018236672A patent/AU2018236672B2/en active Active
- 2018-03-19 US US16/478,920 patent/US11084823B2/en active Active
- 2018-03-19 CN CN201880006529.0A patent/CN110167943B/zh active Active
- 2018-03-19 WO PCT/KR2018/003140 patent/WO2018169373A1/en active Application Filing
- 2018-03-19 NZ NZ755298A patent/NZ755298A/en unknown
- 2018-03-19 RU RU2019123998A patent/RU2726632C1/ru active
- 2018-03-19 CA CA3049648A patent/CA3049648C/en active Active
- 2018-03-19 EP EP18766994.0A patent/EP3596081A4/en active Pending
- 2018-03-19 MX MX2019010595A patent/MX2019010595A/es unknown
- 2018-03-19 BR BR112019015428-0A patent/BR112019015428A2/pt 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 IP Right Grant
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