PE20020062A1 - 5-AMINO-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA COMO ANTAGONISTAS RECEPTORES DE ADENOSINA A2a - Google Patents
5-AMINO-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA COMO ANTAGONISTAS RECEPTORES DE ADENOSINA A2aInfo
- Publication number
- PE20020062A1 PE20020062A1 PE2001000475A PE2001000475A PE20020062A1 PE 20020062 A1 PE20020062 A1 PE 20020062A1 PE 2001000475 A PE2001000475 A PE 2001000475A PE 2001000475 A PE2001000475 A PE 2001000475A PE 20020062 A1 PE20020062 A1 PE 20020062A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- phenyl
- halogen
- triazolo
- pyrazolo
- Prior art date
Links
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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (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
SE REFIERE A COMPUESTOS 5-AMINO-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA DE FORMULA I DONDE R ES R1-FURANILO, R1-TIENILO, R1-PIRIDILO, ENTRE OTROS; X ES ALQUILENO, COCH2; Y ES NR2CH2CH2NR3, OCH2CH2NR2, O, S, CH2S, (CH2)2NH, GRUPO a; m Y n SON 2-3; Q ES N, CH, COH, ENTRE OTROS; Z ES R5-FENILO, R5-FENILALQUILO, R5-HETEROARILO, DIFENILMETILO, GRUPO b, R6CO, ENTRE OTROS; Z E Y SON PIPERIDINILO, FENILO, GRUPO c; R1 ES H, ALQUILO C1-C6, CF3, HALOGENO, NO2; R2, Y R3 SON H, ALQUILO C1-C6; R4 ES H, ALQUILO C1-C6; R5 ES H, HALOGENO, ALQUILO C1-C6, OH, ALCOXI C1-C6, ENTRE OTROS; R6 ES ALQUILO C1-C6, R5-FENILO, TIENILO, ENTRE OTROS; R7 ES ALQUILO C1-C6, R5-FENILO, ENTRE OTROS; R8 ES H, ALQUILO C1-C6 O R7 Y R8 SON (CH2)p-A-(CH2)q; p Y q SON 2-3; A ES UN ENLACE, CH2, S, O; R9 ES H, ALQUILO C1-C6, OH, ALCOXI C1-C6, HALOGENO, ENTRE OTROS; R10 ES H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; R11 ES H, ALQUILO C1-C6, FENILO, ENTRE OTROS; R12 ES H, ALQUILO C1-C6; R13 ES ALQUILO C1-C6-CO, ALQUILO C1-C6-SO2. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS I SON ANTAGONISTAS DE RECEPTORES DE ADENOSINA A2a Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE DEPRESION, ENFERMEDADES COGNITIVAS, ENFERMEDADES NEURODEGENERATIVAS, APOPLEJIA, PARKINSON
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20714300P | 2000-05-26 | 2000-05-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20020062A1 true PE20020062A1 (es) | 2002-02-02 |
Family
ID=22769372
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2001000475A PE20020062A1 (es) | 2000-05-26 | 2001-05-24 | 5-AMINO-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA COMO ANTAGONISTAS RECEPTORES DE ADENOSINA A2a |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US6630475B2 (es) |
| EP (1) | EP1283839B1 (es) |
| JP (3) | JP4574112B2 (es) |
| KR (1) | KR100520907B1 (es) |
| CN (2) | CN1247588C (es) |
| AR (1) | AR028621A1 (es) |
| AT (1) | ATE293627T1 (es) |
| AU (2) | AU2001268089C1 (es) |
| BR (1) | BRPI0111015B8 (es) |
| CA (1) | CA2410237C (es) |
| CZ (1) | CZ303790B6 (es) |
| DE (1) | DE60110219T2 (es) |
| DK (1) | DK1283839T3 (es) |
| EC (1) | ECSP024364A (es) |
| ES (1) | ES2237576T3 (es) |
| HK (1) | HK1049007B (es) |
| HU (1) | HU230420B1 (es) |
| IL (3) | IL152726A0 (es) |
| MX (1) | MXPA02011625A (es) |
| MY (1) | MY132006A (es) |
| NO (1) | NO325008B1 (es) |
| NZ (1) | NZ522326A (es) |
| PE (1) | PE20020062A1 (es) |
| PL (1) | PL218764B1 (es) |
| PT (1) | PT1283839E (es) |
| RU (1) | RU2315053C2 (es) |
| SI (1) | SI1283839T1 (es) |
| SK (1) | SK287748B6 (es) |
| TW (1) | TWI288137B (es) |
| WO (1) | WO2001092264A1 (es) |
| ZA (1) | ZA200208898B (es) |
Families Citing this family (88)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2237576T3 (es) * | 2000-05-26 | 2005-08-01 | Schering Corporation | Antagonistas del receptor a2a de adenosina. |
| CA2459304A1 (en) * | 2001-09-13 | 2003-03-20 | Schering Corporation | Combination of an adenosine a2a receptor antagonist and an antidepressant or anxiolytic |
| JP4545437B2 (ja) | 2001-10-15 | 2010-09-15 | シェーリング コーポレイション | アデノシンa2a受容体アンタゴニストとしてのイミダゾ(4,3−e)−1,2,4−トリアゾロ(1,5−c)ピリミジン |
| FR2832405B1 (fr) * | 2001-11-19 | 2004-12-10 | Sanofi Synthelabo | Tetrahydropyridyl-alkyl-heterocycles azotes, procede pour leur preparation et compositions pharmaceutiques les contenant |
| KR20050044600A (ko) | 2001-11-30 | 2005-05-12 | 쉐링 코포레이션 | [1,2,4]-트리아졸 바이사이클릭 아데노신 A2a 수용체길항제 |
| PE20030739A1 (es) | 2001-11-30 | 2003-08-28 | Schering Corp | Antagonistas del receptor de adenosina a2a |
| HUP0402018A3 (en) | 2001-11-30 | 2008-06-30 | Schering Corp | 5-amino-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives, their use and pharmaceutical compositions containing them |
| EP2260850B1 (en) | 2002-01-28 | 2018-07-04 | Kyowa Hakko Kogyo Co., Ltd | A2A receptor antagonists for use in the treatment of movement disorders |
| IL160133A0 (en) * | 2002-05-30 | 2004-06-20 | King Pharmaceuticals Res & Dev | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
| US20060106040A1 (en) * | 2002-12-19 | 2006-05-18 | Michael Grzelak | Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| DE60335294D1 (de) | 2002-12-19 | 2011-01-20 | Schering Corp | Dlung des extrapyramidalen syndroms |
| WO2004092172A2 (en) | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolo[1,5-c]pyrimidines and pyrazolo[1,5-c]pyrimidines useful as a2a adenosin e receptor antagonists |
| TWI375677B (en) * | 2003-04-23 | 2012-11-01 | Schering Corp | 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine a2a receptor antagonists |
| EP1631294B1 (en) * | 2003-06-10 | 2010-09-15 | Kyowa Hakko Kirin Co., Ltd. | A method of treating an anxiety disorder |
| JP2006527212A (ja) * | 2003-06-12 | 2006-11-30 | ノボ ノルディスク アクティーゼルスカブ | ホルモン感受性リパーゼの阻害剤として使用するための、置換ピペラジンカルバメート |
| AU2004283751B2 (en) * | 2003-10-24 | 2011-05-19 | Exelixis, Inc. | p70S6 kinase modulators and method of use |
| SI1678182T1 (sl) | 2003-10-28 | 2007-06-30 | Schering Corp | Postopek priprave substituiranih 5-amino-pirazolo- (4,3-e)-1,2,4-triazolo(1,5-)pirimidinov |
| JP2007513091A (ja) * | 2003-12-01 | 2007-05-24 | シェーリング コーポレイション | 置換された5−アミノ−ピラゾロ−[4,3−e]−1,2,4−トリアゾロ[1,5−c]ピリミジンを調製するための方法 |
| AU2004303425C1 (en) * | 2003-12-19 | 2010-02-18 | Schering Corporation | Pharmaceutical compositions |
| PE20060185A1 (es) * | 2004-04-21 | 2006-03-20 | Schering Corp | ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA |
| JPWO2006132275A1 (ja) * | 2005-06-07 | 2009-01-08 | 協和醗酵工業株式会社 | 運動障害の予防および/または治療剤 |
| EP1934227B1 (en) * | 2005-09-19 | 2011-12-21 | Schering Corporation | 2-HETEROARYL-PYRAZOLO-[4, 3-e]-1, 2, 4-TRIAZOLO-[1,5-c]-PYRIMIDINE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| AR056080A1 (es) * | 2005-09-23 | 2007-09-19 | Schering Corp | 7-[2-[4-(6-fluoro-3-metil-1,2-benciosoxazol-5-il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c] -pirimidin-5-amine |
| ES2273599B1 (es) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | Compuestos para el tratamiento de la fibrilacion auricular. |
| WO2008008398A2 (en) * | 2006-07-14 | 2008-01-17 | Shionogi & Co., Ltd. | Oxime compounds and the use thereof |
| TW200840566A (en) * | 2006-12-22 | 2008-10-16 | Esteve Labor Dr | Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments |
| US7691869B2 (en) | 2007-03-30 | 2010-04-06 | King Pharmaceuticals Research And Development, Inc. | Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity |
| WO2009110955A2 (en) * | 2008-02-29 | 2009-09-11 | Albert Einstein College Of Medicine Of Yeshiva University | Ketoconazole-derivative antagonists of human pregnane x receptor and uses thereof |
| CA2717172A1 (en) | 2008-03-04 | 2009-09-11 | Schering Corporation | 1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo [4,3-e] -1,2,4-triazolo [4,3-c] pyrimidin-3-one compounds for use as adenosine a2a receptor antagonists |
| EP2274007B1 (en) | 2008-03-10 | 2016-12-14 | Cornell University | Modulation of blood brain barrier permeability |
| TWI473614B (zh) * | 2008-05-29 | 2015-02-21 | Kyowa Hakko Kirin Co Ltd | Anti-analgesic inhibitors |
| NZ590793A (en) * | 2008-07-23 | 2012-07-27 | Kyowa Hakko Kirin Co Ltd | Therapeutic agent for migraine |
| US20100093702A1 (en) * | 2008-10-13 | 2010-04-15 | Barbay J Kent | METHYLENE AMINES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| EP2379556A1 (en) | 2008-12-30 | 2011-10-26 | ArQule, Inc. | Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds |
| US20120053182A1 (en) | 2009-01-20 | 2012-03-01 | Schering Corporation | Methods of alleviating or treating signs and/or symptoms associated with moderate to severe parkinson's disease |
| WO2010084160A1 (en) | 2009-01-21 | 2010-07-29 | Oryzon Genomics S.A. | Phenylcyclopropylamine derivatives and their medical use |
| AU2010222289B2 (en) | 2009-03-13 | 2013-07-11 | Advinus Therapeutics Private Limited | Substituted fused pyrimidine compounds |
| EP2414361A1 (en) | 2009-03-31 | 2012-02-08 | ArQule, Inc. | Substituted heterocyclic compounds |
| US8537177B2 (en) * | 2009-06-15 | 2013-09-17 | Marvell World Trade Ltd. | System and methods for gamut bounded saturation adaptive color enhancement |
| EP2462144B1 (en) | 2009-08-07 | 2017-09-20 | Merck Sharp & Dohme Corp. | PROCESS FOR PREPARING A 2-ALKYNYL SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE |
| EP2480528B1 (en) | 2009-09-25 | 2018-08-29 | Oryzon Genomics, S.A. | Lysine specific demethylase-1 inhibitors and their use |
| WO2011042217A1 (en) | 2009-10-09 | 2011-04-14 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| WO2011101861A1 (en) | 2010-01-29 | 2011-08-25 | Msn Laboratories Limited | Process for preparation of dpp-iv inhibitors |
| WO2011106574A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
| WO2011106573A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| WO2011131697A1 (en) | 2010-04-19 | 2011-10-27 | Oryzon Genomics S.A. | Lysine specific demethylase-1 inhibitors and their use |
| CN104892525A (zh) | 2010-07-29 | 2015-09-09 | 奥瑞泽恩基因组学股份有限公司 | Lsd1的基于芳基环丙胺的脱甲基酶抑制剂及其医疗用途 |
| US9006449B2 (en) | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| CN103261202B (zh) * | 2010-09-24 | 2016-01-20 | 阿迪维纳斯疗法有限公司 | 作为腺苷受体拮抗剂的稠合三环化合物 |
| WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| WO2012107498A1 (en) | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| WO2012127472A1 (en) * | 2011-03-22 | 2012-09-27 | Mapi Pharma Ltd. | Process and intermediates for the preparation of preladenant and related compounds |
| WO2012129381A1 (en) * | 2011-03-22 | 2012-09-27 | Concert Pharmaceuticals Inc. | Deuterated preladenant |
| WO2013024474A1 (en) * | 2011-08-18 | 2013-02-21 | Mapi Phrarma Ltd. | Polymorphs of preladenant |
| IN2014CN03337A (es) | 2011-10-20 | 2015-07-03 | Oryzon Genomics Sa | |
| EP2768805B1 (en) | 2011-10-20 | 2020-03-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| WO2014071512A1 (en) * | 2012-11-06 | 2014-05-15 | Universite Laval | Combination therapy and methods for the treatment of respiratory diseases |
| WO2014101120A1 (en) * | 2012-12-28 | 2014-07-03 | Merck Sharp & Dohme Corp. | Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
| CA2967944C (en) | 2014-11-18 | 2020-11-17 | Merck Sharp & Dohme Corp. | Aminopyrazine compounds with a2a antagonist properties |
| EP3253390B1 (en) | 2015-02-06 | 2022-04-13 | Merck Sharp & Dohme Corp. | Aminoquinazoline compounds as a2a antagonist |
| EP3307067B1 (en) | 2015-06-11 | 2022-11-02 | Merck Sharp & Dohme LLC | Aminopyrazine compounds with a2a antagonist properties |
| WO2017008205A1 (en) | 2015-07-10 | 2017-01-19 | Merck Sharp & Dohme Corp. | Substituted aminoquinazoline compounds as a2a antagonist |
| US9687475B1 (en) | 2016-03-24 | 2017-06-27 | Ezra Pharma Llc | Extended release pharmaceutical formulations with controlled impurity levels |
| US9675585B1 (en) | 2016-03-24 | 2017-06-13 | Ezra Pharma | Extended release pharmaceutical formulations |
| KR102640927B1 (ko) * | 2017-03-30 | 2024-02-27 | 아이테오스 벨지움 에스에이 | A2a 억제제로서의 2-옥소-티아졸 유도체 및 암 치료에 사용하기 위한 화합물 |
| TWI801372B (zh) * | 2017-03-30 | 2023-05-11 | 比利時商艾特歐斯比利時有限公司 | 作為a2a抑制劑的硫胺甲酸酯衍生物以及用於癌症治療的方法 |
| EP3723754A4 (en) | 2017-12-13 | 2021-05-19 | Merck Sharp & Dohme Corp. | IMIDAZO [1,2-C] QUINAZOLINE-5-AMINE COMPOUNDS WITH PROPERTIES OF A2A ANTAGONIST |
| US11407758B2 (en) | 2018-01-04 | 2022-08-09 | Impetis Biosciences Ltd. | Tricyclic compounds, compositions and medicinal applications thereof |
| CR20200441A (es) | 2018-02-27 | 2021-03-15 | Incyte Corp | Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b |
| CN108276345A (zh) * | 2018-03-22 | 2018-07-13 | 重庆奥舍生物化工有限公司 | 一种药物中间体嘧啶-5-甲醛的制备方法 |
| US11472811B2 (en) * | 2018-04-08 | 2022-10-18 | Beigene, Ltd. | Pyrazolotriazolopyrimidine derivatives as A2A receptor antagonist |
| MX2020012376A (es) | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
| CN108864114B (zh) | 2018-06-04 | 2020-11-06 | 应世生物科技(南京)有限公司 | 选择性a2a受体拮抗剂 |
| IL279829B2 (en) | 2018-07-05 | 2025-05-01 | Incyte Holdings Corp | Fused pyrazine derivatives as A2A/A2B inhibitors |
| CN110742893B (zh) * | 2018-07-23 | 2024-04-05 | 百济神州(北京)生物科技有限公司 | A2a受体拮抗剂治疗癌症的方法 |
| PE20211768A1 (es) | 2018-11-30 | 2021-09-07 | Merck Sharp & Dohme | Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmaceuticas y su uso |
| BR112021011948A2 (pt) | 2018-12-20 | 2021-09-08 | Incyte Corporation | Compostos de imidazopiridazina e imidazopiridina e usos dos mesmos |
| 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 |
| WO2020227156A1 (en) * | 2019-05-03 | 2020-11-12 | Nektar Therapeutics | Adenosine 2 receptor antagonists |
| DE102019116986A1 (de) | 2019-06-24 | 2020-12-24 | Helmholtz-Zentrum Dresden-Rossendorf E. V. | Deuterierte 7-(3-(4-(2-([18F]Fluor)ethoxy)phenyl)propyl)-2-(furan-2-yl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amin-Derivate |
| US20230024108A1 (en) * | 2019-07-17 | 2023-01-26 | Teon Therapeutics, Inc. | Adenosine a2a receptor antagonists |
| CN112479956A (zh) | 2019-07-30 | 2021-03-12 | 杭州阿诺生物医药科技有限公司 | 一种用于制备腺苷受体抑制剂中间体的方法 |
| CN112592354B (zh) | 2019-07-30 | 2022-05-27 | 厦门宝太生物科技股份有限公司 | 一种异噁唑并嘧啶类杂环化合物的制备方法 |
| CN111072675A (zh) * | 2019-12-12 | 2020-04-28 | 广东东阳光药业有限公司 | 含氮稠合三环衍生物及其用途 |
| CN113773327B (zh) * | 2021-09-13 | 2022-07-15 | 八叶草健康产业研究院(厦门)有限公司 | 一种吡唑并嘧啶并三唑环类化合物的制备方法 |
| CN118812539B (zh) * | 2024-06-19 | 2025-11-28 | 苏州大学 | 一种5-氨基三唑并嘧啶衍生物及其制备方法 |
| CN118812544A (zh) * | 2024-06-19 | 2024-10-22 | 厦门大学 | 一种腺苷a2ar靶向小分子化合物、核素标记探针及其制备方法、应用和药物组合物 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0217748B1 (en) | 1985-09-30 | 1991-02-06 | Ciba-Geigy Ag | 2-Substituted-e-fused-[1,2,4,]triazolo-[1,5-c]pyrimidines pharmaceutical compositions and uses thereof |
| SU1739850A3 (ru) * | 1987-08-31 | 1992-06-07 | Такеда Кемикал Индастриз, Лтд (Фирма) | Способ получени конденсированных производных пиразоло[3,4- @ ]пиримидина |
| IT1264901B1 (it) * | 1993-06-29 | 1996-10-17 | Schering Plough S P A | Analoghi eterociclici di 1,2,4-triazolo(15-c)pirimidine ad attivita' antagonista per il recettore a2 dell'adenosina |
| ES2165393T3 (es) | 1993-07-27 | 2002-03-16 | Kyowa Hakko Kogyo Kk | Remedio contra la enfermedad de parkinson. |
| IT1277392B1 (it) | 1995-07-28 | 1997-11-10 | Schering Plough S P A | Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina |
| IT1291372B1 (it) * | 1997-05-21 | 1999-01-07 | Schering Plough S P A | Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie |
| ES2237576T3 (es) * | 2000-05-26 | 2005-08-01 | Schering Corporation | Antagonistas del receptor a2a de adenosina. |
| HUP0402018A3 (en) * | 2001-11-30 | 2008-06-30 | Schering Corp | 5-amino-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives, their use and pharmaceutical compositions containing them |
| DE60335294D1 (de) * | 2002-12-19 | 2011-01-20 | Schering Corp | Dlung des extrapyramidalen syndroms |
| SI1678182T1 (sl) * | 2003-10-28 | 2007-06-30 | Schering Corp | Postopek priprave substituiranih 5-amino-pirazolo- (4,3-e)-1,2,4-triazolo(1,5-)pirimidinov |
| JP2007513091A (ja) * | 2003-12-01 | 2007-05-24 | シェーリング コーポレイション | 置換された5−アミノ−ピラゾロ−[4,3−e]−1,2,4−トリアゾロ[1,5−c]ピリミジンを調製するための方法 |
| PE20060185A1 (es) * | 2004-04-21 | 2006-03-20 | Schering Corp | ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA |
| EP1934227B1 (en) * | 2005-09-19 | 2011-12-21 | Schering Corporation | 2-HETEROARYL-PYRAZOLO-[4, 3-e]-1, 2, 4-TRIAZOLO-[1,5-c]-PYRIMIDINE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
-
2001
- 2001-05-24 ES ES01945991T patent/ES2237576T3/es not_active Expired - Lifetime
- 2001-05-24 TW TW090112461A patent/TWI288137B/zh not_active IP Right Cessation
- 2001-05-24 HU HU0600239A patent/HU230420B1/hu unknown
- 2001-05-24 MY MYPI20012466A patent/MY132006A/en unknown
- 2001-05-24 PT PT01945991T patent/PT1283839E/pt unknown
- 2001-05-24 AT AT01945991T patent/ATE293627T1/de active
- 2001-05-24 SI SI200130336T patent/SI1283839T1/xx unknown
- 2001-05-24 SK SK1671-2002A patent/SK287748B6/sk not_active IP Right Cessation
- 2001-05-24 EP EP01945991A patent/EP1283839B1/en not_active Expired - Lifetime
- 2001-05-24 JP JP2002500877A patent/JP4574112B2/ja not_active Expired - Lifetime
- 2001-05-24 HK HK03101315.3A patent/HK1049007B/en not_active IP Right Cessation
- 2001-05-24 CZ CZ20023886A patent/CZ303790B6/cs not_active IP Right Cessation
- 2001-05-24 AU AU2001268089A patent/AU2001268089C1/en not_active Expired
- 2001-05-24 BR BR0111015-2 patent/BRPI0111015B8/pt not_active IP Right Cessation
- 2001-05-24 PL PL360472A patent/PL218764B1/pl unknown
- 2001-05-24 WO PCT/US2001/016954 patent/WO2001092264A1/en not_active Ceased
- 2001-05-24 NZ NZ522326A patent/NZ522326A/xx not_active IP Right Cessation
- 2001-05-24 KR KR10-2002-7015699A patent/KR100520907B1/ko not_active Expired - Lifetime
- 2001-05-24 PE PE2001000475A patent/PE20020062A1/es active IP Right Grant
- 2001-05-24 CA CA002410237A patent/CA2410237C/en not_active Expired - Lifetime
- 2001-05-24 RU RU2002135620/04A patent/RU2315053C2/ru active
- 2001-05-24 AR ARP010102483A patent/AR028621A1/es active IP Right Grant
- 2001-05-24 AU AU6808901A patent/AU6808901A/xx active Pending
- 2001-05-24 CN CNB018134491A patent/CN1247588C/zh not_active Expired - Lifetime
- 2001-05-24 US US09/865,071 patent/US6630475B2/en not_active Ceased
- 2001-05-24 DE DE60110219T patent/DE60110219T2/de not_active Expired - Lifetime
- 2001-05-24 IL IL15272601A patent/IL152726A0/xx unknown
- 2001-05-24 CN CNB2006100049297A patent/CN100384847C/zh not_active Expired - Lifetime
- 2001-05-24 MX MXPA02011625A patent/MXPA02011625A/es active IP Right Grant
- 2001-05-24 DK DK01945991T patent/DK1283839T3/da active
-
2002
- 2002-11-01 ZA ZA200208898A patent/ZA200208898B/en unknown
- 2002-11-10 IL IL152726A patent/IL152726A/en active IP Right Grant
- 2002-11-25 NO NO20025651A patent/NO325008B1/no not_active IP Right Cessation
- 2002-11-25 EC EC2002004364A patent/ECSP024364A/es unknown
-
2003
- 2003-05-30 US US10/448,854 patent/US6897216B2/en not_active Expired - Lifetime
-
2004
- 2004-08-06 US US10/912,834 patent/US7067655B2/en not_active Expired - Lifetime
-
2006
- 2006-05-02 JP JP2006128415A patent/JP4938348B2/ja not_active Expired - Lifetime
-
2007
- 2007-03-16 JP JP2007069618A patent/JP2007145875A/ja not_active Withdrawn
-
2012
- 2012-04-06 US US13/441,140 patent/USRE44205E1/en not_active Expired - Lifetime
- 2012-06-04 IL IL220174A patent/IL220174A/en active IP Right Grant
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20020062A1 (es) | 5-AMINO-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA COMO ANTAGONISTAS RECEPTORES DE ADENOSINA A2a | |
| PE20030477A1 (es) | ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a | |
| PE20060185A1 (es) | ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA | |
| PE20051039A1 (es) | [1,8] naftiridin-2-onas y compuestos relacionados | |
| CO5700778A2 (es) | Administracion combinada de una indolinona con un agente quimioterapeutico para trastornos de proliferacion celular | |
| PE20020366A1 (es) | Derivados de piperazina como ligandos del receptor 5ht2 | |
| PE20030739A1 (es) | Antagonistas del receptor de adenosina a2a | |
| AR004516A1 (es) | Derivados de pirimidina, su uso, procedimientos para prepararlos y medicamentos que los contienen | |
| PE20081192A1 (es) | Tratamiento del dolor | |
| PE20010629A1 (es) | Derivados de triazolpiridinamina como ligandos de receptores de adenosina | |
| PE20130012A1 (es) | Derivados de pirazol como inhibidores de jak | |
| PE20030129A1 (es) | Imidazotriazinas | |
| PE46899A1 (es) | Derivados de n-fenil-sulfonamida | |
| PE20040197A1 (es) | Pirazolopiridinas sustituidas con carbamato | |
| PE20010964A1 (es) | Derivados de tiazolilamida | |
| PE20091068A1 (es) | Compuestos pirrolo[3,2-d]pirimidina y su uso como inhibidores de quinasa pi3 y quinasa mtor | |
| AR072756A2 (es) | Intermediarios para la preparacion; derivados de triazolo[4,5-d]pirimidina, utiles como antitromboticos | |
| PE20020406A1 (es) | 7-OXO-PIRIDO[2,3-d]PIRIMIDINAS 2,6-DISUSTITUIDAS COMO INHIBIDORES DE LAS PROTEINAS CINASAS | |
| PE20030727A1 (es) | 17OALQUIL-17ß-OXI-ESTRATRIENOS, PRODUCTOS INTERMEDIARIOS PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN | |
| AR035068A1 (es) | Compuestos de pirimidinona, composiciones farmaceuticas que los comprenden, uso de tales compuestos en la fabricacion de medicamentos y proceso para la preparacion de dichos compuestos | |
| AR065863A1 (es) | Derivados de imidazolidinona | |
| PE109598A1 (es) | Pirrolcarboxamidas condensadas, utiles como ligandos de receptores cerebrales gaba | |
| PE20030761A1 (es) | Derivados del 7-amino-benzotiazol | |
| PE20030653A1 (es) | COMPUESTOS BICICLICOS[1,2,4]-TRIAZOL COMO ANTAGONISTAS DE RECEPTORES DE ADENOSINA A2a | |
| PE20020844A1 (es) | Derivados de imidazolilo como inhibidores del factor de liberacion de la corticotropina |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |