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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (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)
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 (https=) |
| EP (1) | EP1448565B1 (https=) |
| JP (2) | JP4284182B2 (https=) |
| KR (1) | KR20050044593A (https=) |
| CN (1) | CN1692116A (https=) |
| AR (1) | AR037680A1 (https=) |
| AT (1) | ATE453647T1 (https=) |
| AU (1) | AU2002346503A1 (https=) |
| CA (1) | CA2468649C (https=) |
| DE (1) | DE60234951D1 (https=) |
| ES (1) | ES2336435T3 (https=) |
| HU (1) | HUP0402018A3 (https=) |
| IL (1) | IL161716A0 (https=) |
| MX (1) | MXPA04005209A (https=) |
| PE (1) | PE20030665A1 (https=) |
| TW (1) | TW200306837A (https=) |
| WO (1) | WO2003048165A1 (https=) |
| ZA (1) | ZA200404161B (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60110219T2 (de) * | 2000-05-26 | 2006-03-09 | Schering Corp. | Adenosin a2a rezeptor antagonisten |
| US6964288B2 (en) * | 2001-07-06 | 2005-11-15 | Ksaria Corporation | Apparatus and method for automated preparation of an optical fiber |
| KR100687954B1 (ko) | 2001-10-15 | 2007-02-27 | 쉐링 코포레이션 | 아데노신 Ａ2ａ 수용체 길항제로서의이미다조（4,3-ｅ）-1,2,4-트리아졸로（1,5-ｃ） 피리미딘 |
| AU2003245380A1 (en) * | 2002-05-30 | 2003-12-19 | King Pharmaceuticals Research & Development, Inc. | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
| TWI331036B (en) | 2002-12-19 | 2010-10-01 | Schering Corp | Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| WO2005039506A2 (en) * | 2003-10-24 | 2005-05-06 | Exelixis, Inc. | P70s6 kinase modulators and method of use |
| ES2278353T3 (es) * | 2003-10-28 | 2007-08-01 | Schering Corporation | Procedimiento para preparar 5-amino-pirazolo-(4,3-e)-1,2,4-triazolo(1,5-c)pirimidinas sustituidas. |
| CA2550071A1 (en) * | 2003-12-19 | 2005-07-07 | Schering Corporation | Pharmaceutical compositions |
| EP2258372B8 (en) * | 2005-06-07 | 2012-12-19 | Kyowa Hakko Kirin Co., Ltd. | A2A antagonists for use in the treatment of motor disorders |
| 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 |
| WO2009078999A1 (en) | 2007-12-17 | 2009-06-25 | Janssen Pharmaceutica N.V. | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1 |
| US12246013B2 (en) | 2008-08-01 | 2025-03-11 | Eye Therapies Llc | Vasoconstriction compositions and methods of use |
| 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 |
| HRP20141047T1 (hr) | 2008-08-01 | 2015-01-02 | Eye Therapies Llc | Pripravci za sužavanje krvnih žila i metode njihove uporabe |
| US8273754B2 (en) | 2008-12-30 | 2012-09-25 | Arqule, Inc. | Substituted 1H-pyrazolo[3,4-D]pyrimidine-6-amine compounds |
| US8343961B2 (en) | 2009-03-31 | 2013-01-01 | 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 |
| US20110152271A1 (en) * | 2009-12-17 | 2011-06-23 | Gerald Horn | 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 |
| 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 |
| AU2019383948A1 (en) | 2018-11-20 | 2021-05-20 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| WO2020112700A1 (en) | 2018-11-30 | 2020-06-04 | Merck Sharp & Dohme Corp. | 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| AU2019388872A1 (en) | 2018-11-30 | 2021-05-27 | Merck Sharp & Dohme Llc | 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 |
| JP2022540583A (ja) * | 2019-07-17 | 2022-09-16 | テオン セラピューティクス，インク． | アデノシンａ２ａ受容体アンタゴニスト及びその使用 |
| 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 |
| CN112028891B (zh) | 2019-07-30 | 2022-07-05 | 厦门宝太生物科技股份有限公司 | 腺苷受体拮抗剂 |
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 |
| WO1995003806A1 (en) * | 1993-07-27 | 1995-02-09 | 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 |
| US6921825B2 (en) * | 1998-09-16 | 2005-07-26 | King Pharmaceuticuals Research & Development, Inc. | Adenosine A3 receptor modulators |
| US6448253B1 (en) * | 1998-09-16 | 2002-09-10 | King Pharmaceuticals Research And Development, Inc. | Adenosine A3 receptor modulators |
| DE60110219T2 (de) * | 2000-05-26 | 2006-03-09 | Schering Corp. | Adenosin a2a rezeptor antagonisten |
| AU2003245380A1 (en) * | 2002-05-30 | 2003-12-19 | King Pharmaceuticals Research & Development, Inc. | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
| EP1622912B1 (en) * | 2003-04-23 | 2009-05-27 | Schering Corporation | 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 IL IL16171602A patent/IL161716A0/xx unknown
- 2002-11-26 EP EP02784568A patent/EP1448565B1/en not_active Expired - Lifetime
- 2002-11-26 KR KR1020047007876A patent/KR20050044593A/ko not_active Withdrawn
- 2002-11-26 WO PCT/US2002/037710 patent/WO2003048165A1/en not_active Ceased
- 2002-11-26 AU AU2002346503A patent/AU2002346503A1/en not_active Abandoned
- 2002-11-26 HU HU0402018A patent/HUP0402018A3/hu unknown
- 2002-11-26 MX MXPA04005209A patent/MXPA04005209A/es active IP Right Grant
- 2002-11-26 DE DE60234951T patent/DE60234951D1/de not_active Expired - Lifetime
- 2002-11-26 JP JP2003549355A patent/JP4284182B2/ja not_active Expired - Fee Related
- 2002-11-26 US US10/304,931 patent/US6916811B2/en not_active Expired - Lifetime
- 2002-11-26 AT AT02784568T patent/ATE453647T1/de not_active IP Right Cessation
- 2002-11-26 CN CNA02823782XA patent/CN1692116A/zh active Pending
- 2002-11-26 ES ES02784568T patent/ES2336435T3/es not_active Expired - Lifetime
- 2002-11-26 CA CA002468649A patent/CA2468649C/en not_active Expired - Fee Related
- 2002-11-27 AR ARP020104561A patent/AR037680A1/es unknown
- 2002-11-27 PE PE2002001143A patent/PE20030665A1/es not_active Application Discontinuation
- 2002-11-27 TW TW091134471A patent/TW200306837A/zh unknown
-
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 |
| IL161716A0 (en) | 2004-09-27 |
| HUP0402018A3 (en) | 2008-06-30 |
| CA2468649C (en) | 2009-03-10 |
| WO2003048165A1 (en) | 2003-06-12 |
| JP2005511699A (ja) | 2005-04-28 |
| MXPA04005209A (es) | 2004-08-19 |
| CN1692116A (zh) | 2005-11-02 |
| JP2008260776A (ja) | 2008-10-30 |
| DE60234951D1 (de) | 2010-02-11 |
| US6916811B2 (en) | 2005-07-12 |
| JP4284182B2 (ja) | 2009-06-24 |
| AU2002346503A1 (en) | 2003-06-17 |
| ZA200404161B (en) | 2005-11-30 |
| HK1063780A1 (en) | 2005-01-14 |
| KR20050044593A (ko) | 2005-05-12 |
| HUP0402018A2 (hu) | 2005-02-28 |
| AR037680A1 (es) | 2004-12-01 |
| CA2468649A1 (en) | 2003-06-12 |
| EP1448565B1 (en) | 2009-12-30 |
| US20030212059A1 (en) | 2003-11-13 |
| EP1448565A1 (en) | 2004-08-25 |
| ES2336435T3 (es) | 2010-04-13 |
| TW200306837A (en) | 2003-12-01 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20030665A1 (es) | ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a | |
| PE20030477A1 (es) | ANTAGONISTAS DEL RECEPTOR DE ADENOSINA A2a | |
| PE20060873A1 (es) | Compuestos de quinolina heteroaromaticos | |
| PE20060570A1 (es) | Compuestos de quinazolina e isoquinolina piperidilo sustituidos como inhibidores de fosfodiesterasa pde-10 | |
| CY1114022T1 (el) | Φαρμακα με δραση υποδοχεα ημ74α | |
| BRPI0507065B8 (pt) | derivados de quinolina, composição que os compreende, seu processo de preparação e seu uso como inibidores micobacterianos | |
| PE20040155A1 (es) | Derivados aminoinazoles, procedimiento de preparacion e intermedios de este procedimiento a titulo de medicamentos y composiciones farmaceuticas que los contienen | |
| BRPI0518459A2 (pt) | composto ou um sal farmaceuticamente aceitÁvel do mesmo, composiÇço farmacÊutica, uso de um composto, e, processo para preparar o composto ou um sal farmaceuticamente aceitÁvel do mesmo | |
| PE20120224A1 (es) | Derivados de 1h-imidazo-[4,5-c]-quinolinona | |
| PE20060334A1 (es) | Derivados de piridina como antagonistas del receptor a2b de adenosina | |
| GT200400092A (es) | Preparacion y uso de derivados de alquilarilo para el tratamiento de la obesidad | |
| CO5570667A2 (es) | Compuestos azabiciclico sustituidos condensados con heteroarilo para el tratamiento de enfermedades | |
| PE20080059A1 (es) | Quinazolinas para la inhibicion de pdk1 | |
| DE60235396D1 (de) | 3-amido-1,2-benzisoxazolderivate, herstellungsverfahren und deren verwendung | |
| BR0206433A (pt) | Composto, composição farmacêutica, processo para a prepapação de um composto, e, uso de um composto | |
| DE60318583D1 (de) | N-äphenyl(piperidin-2-yl)methylübenzamid-derivate, verfahren zu deren herstellung und ihre therapeutische verwendung | |
| ATE325796T1 (de) | Derivate von triazolyl-imidazopyridine und von triazolylpurine als ligande des adenosine a2a rezeptoren und ihre verwendung als medicamente | |
| PA8581401A1 (es) | Compuestos de imedazopiridina como agonistas del receptor 5-ht4 | |
| TW200508359A (en) | Quinoxaline derivatives, and light emitting element using thereof | |
| PA8676301A1 (es) | Metodos para sintetizar derivados de 6-alquilaminoquinolina | |
| PA8575001A1 (es) | Fluorobenzamidas como inhibidores de maob | |
| BR0317284A (pt) | Inibidores aminocianopiridina de proteìna quinase-2 ativada com proteìna quinase ativada com mitógeno | |
| PE20061378A1 (es) | INHIBIDORES DE LA ACTIVIDAD DE Akt | |
| PE20051095A1 (es) | DERIVADOS 1H-TIENO[2,3-c] PIRAZOL UTILES COMO INHIBIDORES DE QUINASA | |
| RU2008115239A (ru) | 7-[2-[4-(6-фтор-3-метил-1, 2-бензизоксазол-5-ил)-1-пиперазинил]этил]-2-(пропинил)-7h-пиразоло-[4,3-е]-[1,2,4]-триазоло-[1,5-с]пиримидин-5-амин |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |