MX2021003508A - Derivados de 5-azaindazol como antagonistas del receptor de adenosina. - Google Patents
Derivados de 5-azaindazol como antagonistas del receptor de adenosina.Info
- Publication number
- MX2021003508A MX2021003508A MX2021003508A MX2021003508A MX2021003508A MX 2021003508 A MX2021003508 A MX 2021003508A MX 2021003508 A MX2021003508 A MX 2021003508A MX 2021003508 A MX2021003508 A MX 2021003508A MX 2021003508 A MX2021003508 A MX 2021003508A
- Authority
- MX
- Mexico
- Prior art keywords
- sub
- receptor antagonists
- adenosine receptor
- azaindazole derivatives
- azaindazole
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- 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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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
- A61K9/08—Solutions
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- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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- 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
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
-
- 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
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (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)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se relaciona con nuevos derivados de 5-azaindazol de la fórmula (I), como se describe y define en la presente, y sus sales, solvatos y profármacos farmacéuticamente aceptables, así como composiciones farmacéuticas que comprenden tales compuestos. Se ha descubierto que los derivados de 5-azaindazol de acuerdo con la invención son antagonistas del receptor de adenosina duales A2A/A2B altamente eficaces y, por lo tanto, pueden usarse como agentes terapéuticos, particularmente en el tratamiento o prevención de enfermedades o trastornos hiperproliferativos o infecciosos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP18306390 | 2018-10-25 | ||
PCT/EP2019/078625 WO2020083856A1 (en) | 2018-10-25 | 2019-10-22 | 5-azaindazole derivatives as adenosine receptor antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2021003508A true MX2021003508A (es) | 2021-05-27 |
Family
ID=64267733
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2021003508A MX2021003508A (es) | 2018-10-25 | 2019-10-22 | Derivados de 5-azaindazol como antagonistas del receptor de adenosina. |
Country Status (13)
Country | Link |
---|---|
US (1) | US20210361669A1 (es) |
EP (1) | EP3870294A1 (es) |
JP (1) | JP2022505872A (es) |
KR (1) | KR20210083293A (es) |
CN (1) | CN112912142A (es) |
AU (1) | AU2019363657A1 (es) |
BR (1) | BR112021007727A2 (es) |
CA (1) | CA3117512A1 (es) |
IL (1) | IL282527A (es) |
MX (1) | MX2021003508A (es) |
SG (1) | SG11202104081XA (es) |
TW (1) | TW202043223A (es) |
WO (1) | WO2020083856A1 (es) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA3220380A1 (en) | 2021-06-07 | 2022-12-15 | Rinat ZAYNAGETDINOV | Combination treatment of cancer |
WO2022272313A1 (en) * | 2021-06-25 | 2022-12-29 | The Board Of Trustees Of The Leland Stanford Junior University | Modulators of histone acetyltransferase 1 and methods of treatment thereof |
WO2023169535A1 (en) * | 2022-03-10 | 2023-09-14 | Huahui Health Ltd. | Hepatitis b antiviral agents |
Family Cites Families (27)
Publication number | Priority date | Publication date | Assignee | Title |
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US4207554A (en) | 1972-08-04 | 1980-06-10 | Med-El Inc. | Method and apparatus for automated classification and analysis of cells |
US4125828A (en) | 1972-08-04 | 1978-11-14 | Med-El Inc. | Method and apparatus for automated classification and analysis of cells |
GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
AU1345697A (en) * | 1995-12-22 | 1997-07-17 | Du Pont Merck Pharmaceutical Company, The | Novel integrin receptor antagonists |
KR19990082463A (ko) | 1996-02-13 | 1999-11-25 | 돈 리사 로얄 | 혈관 내피 성장 인자 억제제로서의 퀴나졸린유도체 |
DK0885198T3 (da) | 1996-03-05 | 2002-03-25 | Astrazeneca Ab | 4-Anilinoquinazolinderivater |
GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
EP1054012B1 (en) | 1998-01-05 | 2003-06-11 | Eisai Co., Ltd. | Purine derivatives and adenosine a2 receptor antagonists serving as preventives/remedies for diabetes |
GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
GB9900752D0 (en) | 1999-01-15 | 1999-03-03 | Angiogene Pharm Ltd | Benzimidazole vascular damaging agents |
PT1221444E (pt) | 1999-07-02 | 2005-11-30 | Eisai Co Ltd | Derivados de imidazole condensados e medicamentos para a diabetes mellitus |
CA2406979A1 (en) | 2000-05-31 | 2001-12-06 | Astrazeneca Ab | Indole derivatives with vascular damaging activity |
RU2003103603A (ru) | 2000-07-07 | 2004-08-20 | Энджиоджен Фармасьютикалз Лимитед (Gb) | Производные колхинола в качестве ингибиторов ангиогенеза |
AU2001266233B2 (en) | 2000-07-07 | 2006-06-29 | Angiogene Pharmaceuticals Limited | Colchinol derivatives as vascular damaging agents |
WO2004089942A2 (en) | 2001-10-02 | 2004-10-21 | Acadia Pharmaceuticals Inc. | Benzimidazolidinone derivatives as muscarinic agents |
EP1465634B1 (en) | 2001-12-12 | 2014-10-22 | The Government of the United States of America, as represented by the Secretary Department of Health and Human Services | Methods for using adenosine receptor inhibitors to enhance immune response and inflammation |
US20080070932A1 (en) | 2003-04-09 | 2008-03-20 | Chi Vu | Triazolo[ 1,5-A] Pyrimidines And Pyrazolo[ 1,5-A] Pyrimidines And Methods Of Making And Using The Same |
ES2301991T3 (es) | 2003-05-19 | 2008-07-01 | F. Hoffmann-La Roche Ag | Derivados de benzotiazol como ligandos del receptor de adenosina. |
RU2006112847A (ru) | 2003-09-19 | 2007-11-10 | Ф. Хоффманн-Ля Рош Аг (Ch) | Производные тиазолопиридина в качестве лигандов аденозинового рецептора |
EP1773827B1 (en) | 2004-07-22 | 2010-02-17 | F.Hoffmann-La Roche Ag | Benzothiazole derivatives |
WO2008112695A2 (en) | 2007-03-12 | 2008-09-18 | Irm Llc | Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment |
EP2210891A1 (en) | 2009-01-26 | 2010-07-28 | Domain Therapeutics | New adenosine receptor ligands and uses thereof |
US8859566B2 (en) * | 2009-03-13 | 2014-10-14 | Advinus Therapeutics Private Limited | Substituted fused pyrimidine compounds |
WO2011055391A1 (en) * | 2009-11-09 | 2011-05-12 | Advinus Therapeutics Private Limited | Substituted fused pyrimidine compounds, its preparation and uses thereof |
MX2015004041A (es) | 2012-09-28 | 2015-07-06 | Merck Sharp & Dohme | Compuestos novedosos que son inhibidores de erk. |
CA2996018C (en) | 2015-08-20 | 2024-02-06 | Changzhou Jiekai Pharmatech Co., Ltd. | Pyrazolo fused heterocyclic compounds as erk inhibitors |
-
2019
- 2019-10-22 WO PCT/EP2019/078625 patent/WO2020083856A1/en unknown
- 2019-10-22 MX MX2021003508A patent/MX2021003508A/es unknown
- 2019-10-22 CN CN201980070446.2A patent/CN112912142A/zh active Pending
- 2019-10-22 AU AU2019363657A patent/AU2019363657A1/en active Pending
- 2019-10-22 KR KR1020217015638A patent/KR20210083293A/ko active Search and Examination
- 2019-10-22 EP EP19786996.9A patent/EP3870294A1/en active Pending
- 2019-10-22 JP JP2021522946A patent/JP2022505872A/ja active Pending
- 2019-10-22 CA CA3117512A patent/CA3117512A1/en active Pending
- 2019-10-22 SG SG11202104081XA patent/SG11202104081XA/en unknown
- 2019-10-22 US US17/288,164 patent/US20210361669A1/en active Pending
- 2019-10-22 BR BR112021007727-8A patent/BR112021007727A2/pt unknown
- 2019-10-24 TW TW108138338A patent/TW202043223A/zh unknown
-
2021
- 2021-04-21 IL IL282527A patent/IL282527A/en unknown
Also Published As
Publication number | Publication date |
---|---|
EP3870294A1 (en) | 2021-09-01 |
KR20210083293A (ko) | 2021-07-06 |
US20210361669A1 (en) | 2021-11-25 |
JP2022505872A (ja) | 2022-01-14 |
BR112021007727A2 (pt) | 2021-07-27 |
IL282527A (en) | 2021-06-30 |
SG11202104081XA (en) | 2021-05-28 |
WO2020083856A1 (en) | 2020-04-30 |
CA3117512A1 (en) | 2020-04-30 |
AU2019363657A1 (en) | 2021-06-03 |
CN112912142A (zh) | 2021-06-04 |
TW202043223A (zh) | 2020-12-01 |
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