PE20030665A1 - ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a - Google Patents
ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2aInfo
- Publication number
- PE20030665A1 PE20030665A1 PE2002001143A PE2002001143A PE20030665A1 PE 20030665 A1 PE20030665 A1 PE 20030665A1 PE 2002001143 A PE2002001143 A PE 2002001143A PE 2002001143 A PE2002001143 A PE 2002001143A PE 20030665 A1 PE20030665 A1 PE 20030665A1
- Authority
- PE
- Peru
- Prior art keywords
- aryl
- inhibitors
- adenosine
- azepanil
- piperidinyl
- Prior art date
Links
- 229940123702 Adenosine A2a receptor antagonist Drugs 0.000 title 1
- 239000002467 adenosine A2a receptor antagonist Substances 0.000 title 1
- -1 PIPERIDINYL Chemical class 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- KEUDMLLLHGLIGH-UHFFFAOYSA-N 1h-pyrazole;pyrimidine Chemical compound C=1C=NNC=1.C1=CN=CN=C1 KEUDMLLLHGLIGH-UHFFFAOYSA-N 0.000 abstract 1
- 102000007471 Adenosine A2A receptor Human genes 0.000 abstract 1
- 108010085277 Adenosine A2A receptor Proteins 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102000010909 Monoamine Oxidase Human genes 0.000 abstract 1
- 108010062431 Monoamine oxidase Proteins 0.000 abstract 1
- 206010039966 Senile dementia Diseases 0.000 abstract 1
- 150000003973 alkyl amines Chemical class 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 239000003543 catechol methyltransferase inhibitor Substances 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 239000000534 dopa decarboxylase inhibitor Substances 0.000 abstract 1
- 229940052760 dopamine agonists Drugs 0.000 abstract 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 abstract 1
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
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
- A61P25/14—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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurosurgery (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
SE REFIERE A COMPUESTO CONDENSADO TRIAZO PIRIMIDIN PIRAZOL DE FORMULA I DONDE R ES R1-FURANILO, R1-TIENILO, R1-PIRIDILO, R1-OXAZOLILO, R1-PIRROLILO, R2-ARILO; X ES (CH2)n, Y ES PIPERIDINILO, PIRROLIDINILO, AZEPANILO, CON UNA PORCION ARILO O HETEROARILO FUSIONADA A DOS ATOMOS DE CARBONO ADYACENTE EN Y, X ESTA UNIDO AL ATOMO DE N DEL PIPERIDINILO, PIRROLIDINILO, AZEPANILO; Q ES H, CICLOALQUILO, CICLOHETEROALQUILO, AMINO, ARILO, ARALQUILO, HETEROARILO, ENTRE OTROS; n ES 1-4; R1 ES H, ALQUILO, CF3, HALOGENO, NO2; R2 ES H, ALQUILO, CF3, HALOGENO, NO2, ALCOXI, ACILOXI, ALQUILAMINO, ACILAMINO, ALQUILSULFONLO, HIDROXILO. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS AGONISTAS DOPAMINERGICOS, INHIBIDORES DE MAO-B, INHIBIDORES DE DOPA DESCARBOXILASA, INHIBIDORES DE COMT. LOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE ENFERMEDAD DEL SISTEMA NERVIOSO CENTRAL, APOPLEJIA, ENFERMEDAD COGNITIVA, NEURODEGENERATIVA, PARKINSON, DEMENCIA SENIL
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33434201P | 2001-11-30 | 2001-11-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20030665A1 true PE20030665A1 (es) | 2003-08-08 |
Family
ID=23306779
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2002001143A PE20030665A1 (es) | 2001-11-30 | 2002-11-27 | ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US6916811B2 (es) |
| EP (1) | EP1448565B1 (es) |
| JP (2) | JP4284182B2 (es) |
| KR (1) | KR20050044593A (es) |
| CN (1) | CN1692116A (es) |
| AR (1) | AR037680A1 (es) |
| AT (1) | ATE453647T1 (es) |
| AU (1) | AU2002346503A1 (es) |
| CA (1) | CA2468649C (es) |
| DE (1) | DE60234951D1 (es) |
| ES (1) | ES2336435T3 (es) |
| HU (1) | HUP0402018A3 (es) |
| IL (1) | IL161716A0 (es) |
| MX (1) | MXPA04005209A (es) |
| PE (1) | PE20030665A1 (es) |
| TW (1) | TW200306837A (es) |
| WO (1) | WO2003048165A1 (es) |
| ZA (1) | ZA200404161B (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU6808901A (en) * | 2000-05-26 | 2001-12-11 | Schering Corp | Adenosine a2a receptor antagonists |
| US6964288B2 (en) * | 2001-07-06 | 2005-11-15 | Ksaria Corporation | Apparatus and method for automated preparation of an optical fiber |
| MXPA04003474A (es) | 2001-10-15 | 2004-07-30 | Schering Corp | Imidazo (4,3-e)-1,2,4-triazolo(1,5-c) pirimidinas como antagonistas del receptor de adenosina a2a. |
| BR0304963A (pt) * | 2002-05-30 | 2004-09-28 | King Pharmaceuticals Res & Dev | Compostos, composição farmacêutica, e, métodos para modular a atividade de adenosina em um mamìfero, e para tratar um mamìfero sofrendo de ou suscetìvel às doenças |
| ES2354875T3 (es) | 2002-12-19 | 2011-03-18 | Schering Corporation | Uso de antagonistas del receptor a2a de la adenosina para el tratamiento o prevención del síndrome extrapiramidal. |
| CA2541989C (en) * | 2003-10-24 | 2013-10-01 | Exelixis, Inc. | P70s6 kinase modulators and method of use |
| HRP20070063T3 (hr) * | 2003-10-28 | 2007-04-30 | Schering Corporation | POSTUPAK DOBIVANJA SUPSTITUIRANIH 5-AMINOPIRAZOLO[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA |
| US20060009504A1 (en) * | 2003-12-19 | 2006-01-12 | Schering Corporation | Pharmaceutical compositions |
| 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 |
| ES2273599B1 (es) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | Compuestos para el tratamiento de la fibrilacion auricular. |
| PE20080145A1 (es) | 2006-03-21 | 2008-02-11 | Janssen Pharmaceutica Nv | Tetrahidro-pirimidoazepinas como moduladores de trpv1 |
| US7723343B2 (en) * | 2007-03-30 | 2010-05-25 | King Pharmaceuticals Research And Development, Inc. | Adenosine A2A receptor antagonists |
| US8288397B2 (en) | 2007-12-17 | 2012-10-16 | Janssen Pharmaceutica Nv | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1 |
| US12246013B2 (en) | 2008-08-01 | 2025-03-11 | Eye Therapies Llc | Vasoconstriction compositions and methods of use |
| PT2320911E (pt) | 2008-08-01 | 2014-11-11 | Eye Therapies Llc | Composições de vasoconstrição e métodos de utilização |
| US8952011B2 (en) | 2008-08-01 | 2015-02-10 | Eye Therapies Llc | Compositions and methods for the treatment of nasal conditions |
| US20100203165A1 (en) | 2008-08-01 | 2010-08-12 | Gerald Horn | Compositions and methods for treatment of disorders or conditions of the eye |
| AU2009335019A1 (en) | 2008-12-30 | 2011-08-18 | Arqule, Inc. | Substituted 1H-pyrazolo[3,4-d]pyrimidine-6-amine compounds |
| WO2010114894A1 (en) | 2009-03-31 | 2010-10-07 | Arqule, Inc. | Substituted heterocyclic compounds |
| US8987270B2 (en) | 2009-07-27 | 2015-03-24 | Eye Therapies Llc | Formulations of selective alpha-2 agonists and methods of use thereof |
| CA2782872A1 (en) * | 2009-12-17 | 2011-06-23 | Alpha Synergy Development, Inc. | Compositions and methods for ophthalmic delivery of nasal decongestants |
| US8445526B2 (en) | 2011-02-03 | 2013-05-21 | Glaucoma & Nasal Therapies Llc | Compositions and methods for treatment of glaucoma |
| US8999938B2 (en) | 2013-06-21 | 2015-04-07 | Gnt Llc | Ophthalmic lipophilic drug delivery vehicle formulations |
| 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 |
| WO2020106560A1 (en) | 2018-11-20 | 2020-05-28 | Merck Sharp & Dohme Corp. | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| 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 |
| CA3120862C (en) | 2018-11-30 | 2024-05-07 | Merck Sharp & Dohme Corp. | 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| WO2020112706A1 (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 |
| 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 |
| EP3999513A4 (en) * | 2019-07-17 | 2022-12-21 | Teon Therapeutics, Inc. | ADENOSIN A2A RECEPTOR ANTAGONISTS AND USES THEREOF |
| 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 |
| CN112625050B (zh) | 2019-07-30 | 2021-10-01 | 杭州阿诺生物医药科技有限公司 | 一种a2a和/或a2b受体抑制剂的制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU7237294A (en) * | 1993-07-27 | 1995-02-28 | Kyowa Hakko Kogyo Co. Ltd. | Remedy for parkinson's disease |
| 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 |
| US6448253B1 (en) * | 1998-09-16 | 2002-09-10 | King Pharmaceuticals Research And Development, Inc. | Adenosine A3 receptor modulators |
| US6921825B2 (en) * | 1998-09-16 | 2005-07-26 | King Pharmaceuticuals Research & Development, Inc. | Adenosine A3 receptor modulators |
| AU6808901A (en) * | 2000-05-26 | 2001-12-11 | Schering Corp | Adenosine a2a receptor antagonists |
| BR0304963A (pt) * | 2002-05-30 | 2004-09-28 | King Pharmaceuticals Res & Dev | Compostos, composição farmacêutica, e, métodos para modular a atividade de adenosina em um mamìfero, e para tratar um mamìfero sofrendo de ou suscetìvel às doenças |
| MY139344A (en) * | 2003-04-23 | 2009-09-30 | Schering Corp | 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine a2a receptor antagonists |
-
2002
- 2002-11-26 WO PCT/US2002/037710 patent/WO2003048165A1/en not_active Ceased
- 2002-11-26 AT AT02784568T patent/ATE453647T1/de not_active IP Right Cessation
- 2002-11-26 KR KR1020047007876A patent/KR20050044593A/ko not_active Withdrawn
- 2002-11-26 JP JP2003549355A patent/JP4284182B2/ja not_active Expired - Fee Related
- 2002-11-26 CA CA002468649A patent/CA2468649C/en not_active Expired - Fee Related
- 2002-11-26 US US10/304,931 patent/US6916811B2/en not_active Expired - Lifetime
- 2002-11-26 AU AU2002346503A patent/AU2002346503A1/en not_active Abandoned
- 2002-11-26 HU HU0402018A patent/HUP0402018A3/hu unknown
- 2002-11-26 IL IL16171602A patent/IL161716A0/xx unknown
- 2002-11-26 CN CNA02823782XA patent/CN1692116A/zh active Pending
- 2002-11-26 MX MXPA04005209A patent/MXPA04005209A/es active IP Right Grant
- 2002-11-26 ES ES02784568T patent/ES2336435T3/es not_active Expired - Lifetime
- 2002-11-26 DE DE60234951T patent/DE60234951D1/de not_active Expired - Lifetime
- 2002-11-26 EP EP02784568A patent/EP1448565B1/en not_active Expired - Lifetime
- 2002-11-27 AR ARP020104561A patent/AR037680A1/es unknown
- 2002-11-27 TW TW091134471A patent/TW200306837A/zh unknown
- 2002-11-27 PE PE2002001143A patent/PE20030665A1/es not_active Application Discontinuation
-
2004
- 2004-05-27 ZA ZA200404161A patent/ZA200404161B/en unknown
-
2008
- 2008-06-04 JP JP2008147306A patent/JP2008260776A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| ATE453647T1 (de) | 2010-01-15 |
| HK1063780A1 (en) | 2005-01-14 |
| HUP0402018A2 (hu) | 2005-02-28 |
| JP2005511699A (ja) | 2005-04-28 |
| CA2468649A1 (en) | 2003-06-12 |
| HUP0402018A3 (en) | 2008-06-30 |
| CA2468649C (en) | 2009-03-10 |
| ES2336435T3 (es) | 2010-04-13 |
| DE60234951D1 (de) | 2010-02-11 |
| EP1448565A1 (en) | 2004-08-25 |
| AU2002346503A1 (en) | 2003-06-17 |
| AR037680A1 (es) | 2004-12-01 |
| JP2008260776A (ja) | 2008-10-30 |
| MXPA04005209A (es) | 2004-08-19 |
| WO2003048165A1 (en) | 2003-06-12 |
| US20030212059A1 (en) | 2003-11-13 |
| JP4284182B2 (ja) | 2009-06-24 |
| EP1448565B1 (en) | 2009-12-30 |
| KR20050044593A (ko) | 2005-05-12 |
| CN1692116A (zh) | 2005-11-02 |
| ZA200404161B (en) | 2005-11-30 |
| IL161716A0 (en) | 2004-09-27 |
| TW200306837A (en) | 2003-12-01 |
| US6916811B2 (en) | 2005-07-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |