BR112021009078A8 - Antagonistas substituídos de receptor de adenosina de aminotriazolopirimidina e aminotriazolopirazina, composições farmacêuticas e seus usos - Google Patents
Antagonistas substituídos de receptor de adenosina de aminotriazolopirimidina e aminotriazolopirazina, composições farmacêuticas e seus usosInfo
- Publication number
- BR112021009078A8 BR112021009078A8 BR112021009078A BR112021009078A BR112021009078A8 BR 112021009078 A8 BR112021009078 A8 BR 112021009078A8 BR 112021009078 A BR112021009078 A BR 112021009078A BR 112021009078 A BR112021009078 A BR 112021009078A BR 112021009078 A8 BR112021009078 A8 BR 112021009078A8
- Authority
- BR
- Brazil
- Prior art keywords
- adenosine receptor
- aminotriazolopyrazine
- aminotriazolopyrimidine
- pharmaceutical compositions
- receptor antagonists
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (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)
Abstract
ANTAGONISTAS SUBSTITUÍDOS DE RECEPTOR DE ADENOSINA DE AMINOTRIAZOLOPIRIMIDINA E AMINOTRIAZOLOPIRAZINA, COMPOSIÇÕES FARMACÊUTICAS E SEUS USOS. Em suas muitas modalidades, a presente invenção fornece certos compostos substituídos de aminotriazolopirimidina e aminotriazolopirazina de Fórmula (IA) e Fórmula (IB) ou e sais farmaceuticamente aceitáveis dos mesmos, em que, R1, R2, e R3 são como definidos na presente invenção, composições farmacêuticas compreendendo um ou mais de tais compostos (sozinhos e em combinação com um ou mais outros agentes terapeuticamente ativos), e métodos para a sua preparação e uso, sozinhos e em combinação com outros agentes terapêuticos, como antagonistas de A2a e/ou receptores A2b, e seu uso no tratamento de uma variedade de doenças, condições ou distúrbios que são mediados, pelo menos em parte, pelo receptor de adenosina A2a e/ou receptor de adenosina A2b.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862769843P | 2018-11-20 | 2018-11-20 | |
US62/769,843 | 2018-11-20 | ||
PCT/US2019/061622 WO2020106558A1 (en) | 2018-11-20 | 2019-11-15 | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112021009078A2 BR112021009078A2 (pt) | 2021-08-10 |
BR112021009078A8 true BR112021009078A8 (pt) | 2023-02-07 |
Family
ID=70774154
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112021009078A BR112021009078A8 (pt) | 2018-11-20 | 2019-11-15 | Antagonistas substituídos de receptor de adenosina de aminotriazolopirimidina e aminotriazolopirazina, composições farmacêuticas e seus usos |
Country Status (11)
Country | Link |
---|---|
US (1) | US20210395255A1 (pt) |
EP (1) | EP3883575A4 (pt) |
JP (1) | JP2022507734A (pt) |
KR (1) | KR20210093964A (pt) |
CN (1) | CN113015530A (pt) |
AU (1) | AU2019383948A1 (pt) |
BR (1) | BR112021009078A8 (pt) |
CA (1) | CA3119774A1 (pt) |
MA (1) | MA55142A (pt) |
MX (1) | MX2021005839A (pt) |
WO (1) | WO2020106558A1 (pt) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MX2021006329A (es) | 2018-11-30 | 2021-08-11 | Merck Sharp & Dohme Llc | Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmaceuticas y su uso. |
WO2021041360A1 (en) * | 2019-08-26 | 2021-03-04 | Incyte Corporation | Triazolopyrimidines as a2a / a2b inhibitors |
WO2023201267A1 (en) | 2022-04-13 | 2023-10-19 | Gilead Sciences, Inc. | Combination therapy for treating trop-2 expressing cancers |
Family Cites Families (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2284737C (en) | 1997-03-24 | 2007-03-13 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]triazolo[1,5-c]pyrimidine derivatives |
KR20040038899A (ko) * | 2001-09-28 | 2004-05-08 | 교와 핫꼬 고교 가부시끼가이샤 | 수용체 길항제 |
PE20030739A1 (es) * | 2001-11-30 | 2003-08-28 | Schering Corp | Antagonistas del receptor de adenosina a2a |
AU2003211993A1 (en) | 2002-02-15 | 2003-09-04 | Kyowa Hakko Kogyo Co., Ltd. | (1,2,4)TRIAZOLO(1,5-c)PYRIMIDINE DERIVATIVES |
ATE481985T1 (de) | 2002-07-03 | 2010-10-15 | Ono Pharmaceutical Co | Immunpotenzierende zusammensetzungen |
JPWO2004029056A1 (ja) * | 2002-09-24 | 2006-01-26 | 協和醗酵工業株式会社 | [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体 |
AU2003288675B2 (en) | 2002-12-23 | 2010-07-22 | Medimmune Limited | Antibodies against PD-1 and uses therefor |
WO2004072286A1 (ja) | 2003-01-23 | 2004-08-26 | Ono Pharmaceutical Co., Ltd. | ヒトpd−1に対し特異性を有する物質 |
EP1615931A1 (en) * | 2003-04-09 | 2006-01-18 | Biogen Idec MA Inc. | Triazolopyrazines and methods of making and using the same |
PT2161336E (pt) | 2005-05-09 | 2013-10-03 | Ono Pharmaceutical Co | Anticorpos monoclonais humanos para morte programada 1 (pd-1) e métodos de tratamento do cancro utilizando anticorpos anti- pd-1 sozinhos ou em combinação com outros agentes imunoterapêuticos¿ |
KR101607288B1 (ko) | 2005-07-01 | 2016-04-05 | 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. | 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체 |
ES2616355T3 (es) | 2007-06-18 | 2017-06-12 | Merck Sharp & Dohme B.V. | Anticuerpos para el receptor humano de muerte programada PD-1 |
US8168757B2 (en) | 2008-03-12 | 2012-05-01 | Merck Sharp & Dohme Corp. | PD-1 binding proteins |
DE102008023801A1 (de) * | 2008-05-15 | 2009-11-19 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Imidazo- und Triazolopyrimidine, Imidazo- und Pyrazolopyrazine und Imidazotriazine |
GB0906579D0 (en) * | 2009-04-16 | 2009-05-20 | Vernalis R&D Ltd | Pharmaceuticals, compositions and methods of making and using the same |
AU2009288289B2 (en) | 2008-08-25 | 2012-11-08 | Amplimmune, Inc. | PD-1 antagonists and methods of use thereof |
SI2342226T1 (sl) | 2008-09-26 | 2016-11-30 | Dana-Farber Cancer Institute Inc. | Humana protitelesa proti PD-1, PD-L1 in PD-L2 in njihove uporabe |
EP3929216A1 (en) | 2008-12-09 | 2021-12-29 | F. Hoffmann-La Roche AG | Anti-pd-l1 antibodies and their use to enhance t-cell function |
JP2013512251A (ja) | 2009-11-24 | 2013-04-11 | アンプリミューン、インコーポレーテッド | Pd−l1/pd−l2の同時阻害 |
PE20190262A1 (es) | 2011-08-01 | 2019-02-25 | Genentech Inc | Metodos para tratar el cancer por el uso de antagonistas de union al eje pd-1 e inhibidores de mek |
TW201803871A (zh) * | 2016-06-24 | 2018-02-01 | 英塞特公司 | 作為PI3K-γ抑制劑之雜環化合物 |
EP3611174B1 (en) | 2017-04-07 | 2022-06-08 | Medshine Discovery Inc. | [1,2,4]triazolo[1,5-c]pyrimidine derivative as a2a receptor inhibitor |
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 |
CN117903140A (zh) | 2018-02-27 | 2024-04-19 | 因赛特公司 | 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶 |
-
2019
- 2019-11-15 KR KR1020217018498A patent/KR20210093964A/ko unknown
- 2019-11-15 CA CA3119774A patent/CA3119774A1/en active Pending
- 2019-11-15 EP EP19886307.8A patent/EP3883575A4/en active Pending
- 2019-11-15 US US17/292,511 patent/US20210395255A1/en active Pending
- 2019-11-15 BR BR112021009078A patent/BR112021009078A8/pt not_active Application Discontinuation
- 2019-11-15 MA MA055142A patent/MA55142A/fr unknown
- 2019-11-15 JP JP2021527186A patent/JP2022507734A/ja active Pending
- 2019-11-15 AU AU2019383948A patent/AU2019383948A1/en not_active Abandoned
- 2019-11-15 CN CN201980076511.2A patent/CN113015530A/zh active Pending
- 2019-11-15 MX MX2021005839A patent/MX2021005839A/es unknown
- 2019-11-15 WO PCT/US2019/061622 patent/WO2020106558A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
CN113015530A (zh) | 2021-06-22 |
JP2022507734A (ja) | 2022-01-18 |
CA3119774A1 (en) | 2020-05-28 |
BR112021009078A2 (pt) | 2021-08-10 |
KR20210093964A (ko) | 2021-07-28 |
WO2020106558A1 (en) | 2020-05-28 |
MX2021005839A (es) | 2021-07-15 |
EP3883575A1 (en) | 2021-09-29 |
MA55142A (fr) | 2022-02-23 |
EP3883575A4 (en) | 2022-06-15 |
AU2019383948A1 (en) | 2021-05-20 |
US20210395255A1 (en) | 2021-12-23 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B25A | Requested transfer of rights approved |
Owner name: MERCK SHARP AND DOHME LLC (US) |
|
B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |