PE20230372A1 - Triazolopirimidinas como inhibidores de a2a/a2b - Google Patents
Triazolopirimidinas como inhibidores de a2a/a2bInfo
- Publication number
- PE20230372A1 PE20230372A1 PE2022000278A PE2022000278A PE20230372A1 PE 20230372 A1 PE20230372 A1 PE 20230372A1 PE 2022000278 A PE2022000278 A PE 2022000278A PE 2022000278 A PE2022000278 A PE 2022000278A PE 20230372 A1 PE20230372 A1 PE 20230372A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrimidin
- triazolo
- benzonitrile
- amino
- methyl
- Prior art date
Links
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
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente solicitud se refiere a compuestos especificos derivados de triazolopirimidina, los cuales tienen en comun la estructura quimica de Formula (I), en donde: R2 es L-W y L-W'-Z; Cy1 es cianofenilo o cianofluorofenilo; y Cy2 es un heteroarilo de 5-6 miembros sustituido. Entre los compuestos especificos definidos en la presente solicitud tenemos los siguientes: 3-(5-amino-2-((5-(3-aminofenil)-1H-tetrazol-1-il)metil)-8-(pirimidin-4-il)-[1,2,4]triazolo[1,5-c]pirimidin-7-il)benzonitrilo; 3-(2-((5-(1H-pirazol-1-il)-1H-tetrazol-1-il)metil)-5-amino-8-(1-metil-6-oxo-1,6-dihidropiridin-3- il)-[1,2,4]triazolo[1,5-c]pirimidin-7-il)benzonitrilo; 3-(5-amino-2-((3-metilpiridin-2-il)metoxi)-8-(3-metilpiridin-4-il)-[1,2,4]triazolo[1,5-c]pirimidin-7- il)benzonitrilo; entre otros. Estos compuestos modulan la actividad de los receptores de adenosina, tales como los subtipos A2A y A2B, y son utiles para el tratamiento de enfermedades relacionadas con la actividad de los receptores de adenosina, que incluyen, por ejemplo, cancer, enfermedades inflamatorias, enfermedades cardiovasculares y enfermedades neurodegenerativas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962891685P | 2019-08-26 | 2019-08-26 | |
| PCT/US2020/047714 WO2021041360A1 (en) | 2019-08-26 | 2020-08-25 | Triazolopyrimidines as a2a / a2b inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230372A1 true PE20230372A1 (es) | 2023-03-06 |
Family
ID=72422275
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022000278A PE20230372A1 (es) | 2019-08-26 | 2020-08-25 | Triazolopirimidinas como inhibidores de a2a/a2b |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US20210061809A1 (es) |
| EP (1) | EP4021907A1 (es) |
| JP (1) | JP7631317B2 (es) |
| KR (1) | KR20220066074A (es) |
| CN (1) | CN114585625A (es) |
| AR (1) | AR119822A1 (es) |
| AU (1) | AU2020337350A1 (es) |
| BR (1) | BR112022003408A2 (es) |
| CA (1) | CA3150766A1 (es) |
| CL (1) | CL2022000457A1 (es) |
| CO (1) | CO2022003457A2 (es) |
| CR (1) | CR20220124A (es) |
| EC (1) | ECSP22022322A (es) |
| IL (1) | IL290529A (es) |
| MX (1) | MX2022002219A (es) |
| PE (1) | PE20230372A1 (es) |
| PH (1) | PH12022550470A1 (es) |
| TW (1) | TW202115082A (es) |
| WO (1) | WO2021041360A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2019227607C1 (en) | 2018-02-27 | 2023-07-20 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors |
| MX2020012376A (es) | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
| US11161850B2 (en) | 2018-07-05 | 2021-11-02 | Incyte Corporation | Fused pyrazine derivatives as A2A / A2B inhibitors |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| WO2021138467A1 (en) | 2020-01-03 | 2021-07-08 | Incyte Corporation | Anti-cd73 antibodies and uses thereof |
| MX2022007573A (es) | 2020-01-03 | 2022-09-23 | Incyte Corp | Terapia de combinación de inhibidor de grupo de diferenciación 73 (cd73) e inhibidor del receptor de adenosina a2a/a2b. |
| CA3236342A1 (en) | 2021-11-19 | 2023-05-25 | Crossignal Therapeutics, Inc. | Adenosine receptor antagonists |
| CA3256033A1 (en) | 2022-04-13 | 2023-10-19 | Arcus Biosciences, Inc. | POLYTHERAPY FOR THE TREATMENT OF CANCERS EXPRESSING TOO MUCH-2 |
| KR20250026469A (ko) | 2023-08-17 | 2025-02-25 | 김택민 | 오염된 공기를 맑고 깨끗한 공기가 되도록 가공하거나 또는 방사능 오염수 또는 각종 슬러지와 쓰레기 또는 음식물 쓰레기 또는 축분이나 인분을 액비로 가공하는 자연친화적인 친환경 공법에 적용되는 친환경 물질분자 가공 시스템 |
| CN120022278A (zh) * | 2023-11-22 | 2025-05-23 | 英诺湖医药(杭州)有限公司 | 用于治疗癌症的化合物 |
| US20250230168A1 (en) | 2023-12-22 | 2025-07-17 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| ATE257156T1 (de) * | 1997-03-24 | 2004-01-15 | Kyowa Hakko Kogyo Kk | (1,2,4)triazolo(1,5-c)pyrimidin-derivate |
| BR9912938B1 (pt) | 1998-08-11 | 2011-06-28 | derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos. | |
| US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| NZ522783A (en) | 2000-06-28 | 2004-07-30 | Smithkline Beecham P | Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant |
| WO2003024967A2 (en) | 2001-09-19 | 2003-03-27 | Aventis Pharma S.A. | Indolizines as kinase protein inhibitors |
| MXPA04004137A (es) | 2001-10-30 | 2005-01-25 | Novartis Ag | Derivados de estauroesporina como inhibidores de la actividad de cinasa de tirosina del receptor flt3. |
| PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| DK3611174T3 (da) * | 2017-04-07 | 2022-07-04 | Medshine Discovery Inc | [1,2,4]triazolo[1,5-c]pyrimidinderivat som a2a-receptorinhibitor |
| CN109535161B (zh) * | 2017-09-22 | 2021-09-03 | 江苏恒瑞医药股份有限公司 | 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| AU2019227607C1 (en) | 2018-02-27 | 2023-07-20 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors |
| DK3766884T3 (da) * | 2018-04-28 | 2022-03-28 | Medshine Discovery Inc | Krystalform og salttype af triazolopyrimidinforbindelse og fremstillingsfremgangsmåde dertil |
| MX2020012376A (es) * | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
| AR116315A1 (es) * | 2018-09-12 | 2021-04-21 | Dizal Jiangsu Pharmaceutical Co Ltd | Compuestos de triazolo-pirimidina y usos de los mismos |
| CN113015530A (zh) * | 2018-11-20 | 2021-06-22 | 默沙东公司 | 取代的氨基三唑并嘧啶和氨基三唑并吡嗪腺苷受体拮抗剂、药物组合物及其用途 |
| US12414952B2 (en) * | 2018-11-20 | 2025-09-16 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
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2020
- 2020-08-25 PE PE2022000278A patent/PE20230372A1/es unknown
- 2020-08-25 CA CA3150766A patent/CA3150766A1/en active Pending
- 2020-08-25 WO PCT/US2020/047714 patent/WO2021041360A1/en not_active Ceased
- 2020-08-25 EP EP20768191.7A patent/EP4021907A1/en active Pending
- 2020-08-25 PH PH1/2022/550470A patent/PH12022550470A1/en unknown
- 2020-08-25 CN CN202080068863.6A patent/CN114585625A/zh active Pending
- 2020-08-25 TW TW109128933A patent/TW202115082A/zh unknown
- 2020-08-25 CR CR20220124A patent/CR20220124A/es unknown
- 2020-08-25 KR KR1020227009865A patent/KR20220066074A/ko active Pending
- 2020-08-25 MX MX2022002219A patent/MX2022002219A/es unknown
- 2020-08-25 US US17/002,045 patent/US20210061809A1/en not_active Abandoned
- 2020-08-25 AU AU2020337350A patent/AU2020337350A1/en active Pending
- 2020-08-25 JP JP2022513216A patent/JP7631317B2/ja active Active
- 2020-08-25 AR ARP200102383A patent/AR119822A1/es unknown
- 2020-08-25 BR BR112022003408A patent/BR112022003408A2/pt unknown
-
2022
- 2022-02-10 IL IL290529A patent/IL290529A/en unknown
- 2022-02-24 CL CL2022000457A patent/CL2022000457A1/es unknown
- 2022-03-24 CO CONC2022/0003457A patent/CO2022003457A2/es unknown
- 2022-03-24 EC ECSENADI202222322A patent/ECSP22022322A/es unknown
- 2022-12-08 US US18/077,610 patent/US20230124485A1/en not_active Abandoned
-
2024
- 2024-06-27 US US18/755,824 patent/US20250034153A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20230124485A1 (en) | 2023-04-20 |
| US20250034153A1 (en) | 2025-01-30 |
| IL290529A (en) | 2022-04-01 |
| CR20220124A (es) | 2022-06-15 |
| EP4021907A1 (en) | 2022-07-06 |
| CL2022000457A1 (es) | 2022-10-21 |
| CO2022003457A2 (es) | 2022-05-20 |
| AU2020337350A1 (en) | 2022-03-10 |
| WO2021041360A1 (en) | 2021-03-04 |
| JP7631317B2 (ja) | 2025-02-18 |
| MX2022002219A (es) | 2022-06-14 |
| CA3150766A1 (en) | 2021-03-04 |
| TW202115082A (zh) | 2021-04-16 |
| JP2022545923A (ja) | 2022-11-01 |
| US20210061809A1 (en) | 2021-03-04 |
| KR20220066074A (ko) | 2022-05-23 |
| CN114585625A (zh) | 2022-06-03 |
| BR112022003408A2 (pt) | 2022-05-17 |
| AR119822A1 (es) | 2022-01-12 |
| PH12022550470A1 (en) | 2023-02-27 |
| ECSP22022322A (es) | 2022-05-31 |
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