PE20211768A1 - Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmaceuticas y su uso - Google Patents
Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmaceuticas y su usoInfo
- Publication number
- PE20211768A1 PE20211768A1 PE2021000757A PE2021000757A PE20211768A1 PE 20211768 A1 PE20211768 A1 PE 20211768A1 PE 2021000757 A PE2021000757 A PE 2021000757A PE 2021000757 A PE2021000757 A PE 2021000757A PE 20211768 A1 PE20211768 A1 PE 20211768A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- antagonists
- substituted
- triazolo
- quinazoline
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- WOOIBJWFHSHPJN-UHFFFAOYSA-N 2h-triazolo[4,5-h]quinazoline Chemical compound C1=CC2=NNN=C2C2=NC=NC=C21 WOOIBJWFHSHPJN-UHFFFAOYSA-N 0.000 title 1
- 102000009346 Adenosine receptors Human genes 0.000 title 1
- 108050000203 Adenosine receptors Proteins 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- -1 9-substituted amino triazolo quinazoline Chemical class 0.000 abstract 1
- 108010085277 Adenosine A2A receptor Proteins 0.000 abstract 1
- 101150078577 Adora2b gene Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
Classifications
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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
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
- C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invencion se refiere a un compuesto de formula estructural (I), o una sal farmaceuticamente aceptable del mismo, en donde: R1 es F, Cl, alquilo C1-C6 y O(alquilo C1-C6); R2 es H, F, Cl, alquilo C1-C6 y O(alquilo C1-C6); el anillo A es i), ii), iii), entre otros; R3 es pirazolilo, triazolilo y piridinilo sustituidos con grupos R3A, donde R3A es alquilo C1-C6, O(alquilo C1-C6), entre otros; RA1 es H y alquilo C1-C4; RA2 y RA3 son H, F y alquilo C1-C4. Son compuestos preferidos los compuestos a), b), c), entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son derivados de amino triazolo quinazolina 9-sustituidos y antagonistas de los receptores A2a y/o A2b de adenosina, siendo utiles en el tratamiento del cancer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862774077P | 2018-11-30 | 2018-11-30 | |
| PCT/US2019/063136 WO2020112700A1 (en) | 2018-11-30 | 2019-11-26 | 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211768A1 true PE20211768A1 (es) | 2021-09-07 |
Family
ID=69005832
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000757A PE20211768A1 (es) | 2018-11-30 | 2019-11-26 | Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmaceuticas y su uso |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US11312719B2 (es) |
| EP (1) | EP3886988A1 (es) |
| JP (1) | JP7241871B2 (es) |
| KR (1) | KR102653800B1 (es) |
| CN (1) | CN113329791A (es) |
| AR (1) | AR117164A1 (es) |
| AU (1) | AU2019385905B2 (es) |
| BR (1) | BR112021010427B1 (es) |
| CA (1) | CA3120862C (es) |
| CL (1) | CL2021001406A1 (es) |
| CO (1) | CO2021006888A2 (es) |
| CR (1) | CR20210271A (es) |
| DO (1) | DOP2021000104A (es) |
| EA (1) | EA202191498A1 (es) |
| EC (1) | ECSP21036982A (es) |
| IL (1) | IL283334A (es) |
| JO (2) | JOP20210117A1 (es) |
| MA (1) | MA54298A (es) |
| MX (1) | MX2021006329A (es) |
| NI (1) | NI202100043A (es) |
| PE (1) | PE20211768A1 (es) |
| PH (1) | PH12021551196A1 (es) |
| SG (1) | SG11202105180PA (es) |
| TW (1) | TW202039496A (es) |
| WO (1) | WO2020112700A1 (es) |
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| KR101562580B1 (ko) | 2007-06-18 | 2015-10-22 | 머크 샤프 앤 도메 비.브이. | 사람 프로그램된 사멸 수용체 pd-1에 대한 항체 |
| US11466017B2 (en) | 2011-03-10 | 2022-10-11 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| CN109475531B (zh) | 2016-05-31 | 2021-08-17 | 得克萨斯州立大学董事会 | Ptpn11的杂环抑制剂 |
| JP7297871B2 (ja) | 2018-05-02 | 2023-06-26 | ナビール ファーマ,インコーポレイティド | Ptpn11の置換されたヘテロ環式インヒビター |
| EP4356973A3 (en) | 2018-08-10 | 2024-06-26 | Navire Pharma, Inc. | 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer |
| MA55142A (fr) | 2018-11-20 | 2022-02-23 | Merck Sharp & Dohme | Amino-triazolopyrimidine et amino-triazolopyrazine substitués antagoniste du récepteur de l'adénosine, compositions pharmaceutiques et leur utilisation |
| EP3883576B1 (en) | 2018-11-20 | 2025-12-17 | Merck Sharp & Dohme LLC | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| CA3121500A1 (en) | 2018-11-30 | 2020-06-04 | Comet Therapeutics, Inc. | Cyclic pantetheine derivatives and uses thereof |
| CA3120331A1 (en) * | 2018-11-30 | 2020-06-04 | Merck Sharp & Dohme Corp. | 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| EP4185297A4 (en) * | 2020-07-24 | 2024-08-28 | Merck Sharp & Dohme LLC | Adenosine a2a and a2b receptor dual antagonists for immuno-oncology |
| EP4185296A4 (en) * | 2020-07-24 | 2025-03-05 | Merck Sharp & Dohme LLC | DUAL ADENOSINE A2A RECEPTOR AND A2B RECEPTOR ANTAGONISTS FOR IMMUNO-ONCOLOGY |
| EP4479056A4 (en) * | 2022-02-16 | 2026-02-18 | Merck Sharp & Dohme Llc | Adenosine receptor antagonists, pharmaceutical compositions and their use |
| WO2023201267A1 (en) | 2022-04-13 | 2023-10-19 | Gilead Sciences, Inc. | Combination therapy for treating trop-2 expressing cancers |
| WO2024118460A1 (en) * | 2022-11-29 | 2024-06-06 | Merck Sharp & Dohme Llc | Adenosine a2a and a2b receptor antagonists, pharmaceutical compositions and use thereof |
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| AR117200A1 (es) | 2018-11-30 | 2021-07-21 | Syngenta Participations Ag | Derivados de tiazol microbiocidas |
| US10870663B2 (en) | 2018-11-30 | 2020-12-22 | Glaxosmithkline Intellectual Property Development Limited | Compounds useful in HIV therapy |
| CA3120331A1 (en) | 2018-11-30 | 2020-06-04 | Merck Sharp & Dohme Corp. | 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
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2019
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2022
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