PE20070521A1 - 7-[2-[4-(6-FLUORO-3-METIL-1,2-BENCISOXAZOL-5-IL)-1-PIPERAZINIL]ETIL]-2-(1-PROPINIL)-7H-PIRAZOL-[4,3-E]-[1,2,4]-TRIAZOL-[1,5-C]-PIRIMIDIN-5-AMINA COMO ANTAGONISTA DEL RECEPTOR DE ADENOSINA A2a - Google Patents
7-[2-[4-(6-FLUORO-3-METIL-1,2-BENCISOXAZOL-5-IL)-1-PIPERAZINIL]ETIL]-2-(1-PROPINIL)-7H-PIRAZOL-[4,3-E]-[1,2,4]-TRIAZOL-[1,5-C]-PIRIMIDIN-5-AMINA COMO ANTAGONISTA DEL RECEPTOR DE ADENOSINA A2aInfo
- Publication number
- PE20070521A1 PE20070521A1 PE2006001140A PE2006001140A PE20070521A1 PE 20070521 A1 PE20070521 A1 PE 20070521A1 PE 2006001140 A PE2006001140 A PE 2006001140A PE 2006001140 A PE2006001140 A PE 2006001140A PE 20070521 A1 PE20070521 A1 PE 20070521A1
- Authority
- PE
- Peru
- Prior art keywords
- benzysoxazol
- propinyl
- triazol
- pyrimidin
- adenosine
- Prior art date
Links
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 title abstract 2
- 102000007471 Adenosine A2A receptor Human genes 0.000 title 1
- 108010085277 Adenosine A2A receptor Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 102100028116 Amine oxidase [flavin-containing] B Human genes 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 229940123702 Adenosine A2a receptor antagonist Drugs 0.000 abstract 1
- 101710185931 Amine oxidase [flavin-containing] B Proteins 0.000 abstract 1
- 208000027776 Extrapyramidal disease Diseases 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 abstract 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 239000002467 adenosine A2a receptor antagonist Substances 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003954 decarboxylase inhibitor Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms 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
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- C07D487/12—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
- 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
-
- 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
-
- 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
- A61P25/24—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
-
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
REFERIDA AL COMPUESTO ANTAGONISTA DEL RECEPTOR DE ADENOSINA A2a, 7-[2-[4-(6-FLUORO-3-METIL-1,2-BENCISOXAZOL-5-IL)-1-PIPERAZINIL]ETIL]-2-(1-PROPINIL)-7H-PIRAZOL-[4,3-E]-[1,2,4]-TRIAZOL-[1,5-C]-PIRIMIDIN-5-AMINA DE FORMULA (I) O UNA SAL FARMACEUTICAMENTE ACEPTABLE DEL MISMO Y A UNA COMPOSICION FARMACEUTICA QUE LO COMPRENDE. DICHA COMPOSICION PUEDE CONTENER OTROS AGENTES TALES COMO L-DOPA, AGONISTAS DOPAMINERGICOS, INHIBIDORES DE LA MONOAMINAOXIDASA TIPO B (MAO-B), INHIBIDORES DE LA DOPA DECARBOXILASA (DCI) E INHIBIDORES DE LA CATECOL-METILTRANSFERASA (COMT) Y ES UTIL PARA EL TRATAMIENTO DE ENFERMEDADES DEL SISTEMA NERVIOSO CENTRAL TALES COMO ENFERMEDAD DE PARKINSON, SINDROME EXTRA-PIRAMIDAL, ENFERMEDAD DE HUNTINGTON, ENTRE OTRAS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72002705P | 2005-09-23 | 2005-09-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070521A1 true PE20070521A1 (es) | 2007-07-13 |
Family
ID=37487759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006001140A PE20070521A1 (es) | 2005-09-23 | 2006-09-20 | 7-[2-[4-(6-FLUORO-3-METIL-1,2-BENCISOXAZOL-5-IL)-1-PIPERAZINIL]ETIL]-2-(1-PROPINIL)-7H-PIRAZOL-[4,3-E]-[1,2,4]-TRIAZOL-[1,5-C]-PIRIMIDIN-5-AMINA COMO ANTAGONISTA DEL RECEPTOR DE ADENOSINA A2a |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US7572802B2 (es) |
| EP (1) | EP1937687B1 (es) |
| JP (1) | JP4808779B2 (es) |
| KR (1) | KR101396614B1 (es) |
| CN (2) | CN101273045B (es) |
| AR (1) | AR056080A1 (es) |
| AT (1) | ATE503759T1 (es) |
| AU (1) | AU2006294633B8 (es) |
| BR (1) | BRPI0616264B8 (es) |
| CA (1) | CA2623047C (es) |
| CY (1) | CY1111921T1 (es) |
| DE (1) | DE602006021042D1 (es) |
| DK (1) | DK1937687T3 (es) |
| EC (1) | ECSP088297A (es) |
| ES (1) | ES2361856T3 (es) |
| HR (1) | HRP20110466T1 (es) |
| IL (1) | IL190275A (es) |
| MY (1) | MY146429A (es) |
| NO (1) | NO341760B1 (es) |
| NZ (1) | NZ566737A (es) |
| PE (1) | PE20070521A1 (es) |
| PL (1) | PL1937687T3 (es) |
| PT (1) | PT1937687E (es) |
| RS (1) | RS51702B (es) |
| RU (1) | RU2417997C2 (es) |
| SG (1) | SG165419A1 (es) |
| SI (1) | SI1937687T1 (es) |
| TW (1) | TWI335329B (es) |
| WO (1) | WO2007038284A1 (es) |
| ZA (1) | ZA200802550B (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ527142A (en) | 2003-07-23 | 2006-03-31 | Douglas Pharmaceuticals Ltd | A stable suspension formulation |
| 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 |
| AU2010222289B2 (en) | 2009-03-13 | 2013-07-11 | Advinus Therapeutics Private Limited | Substituted fused pyrimidine compounds |
| 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 |
| WO2011101861A1 (en) | 2010-01-29 | 2011-08-25 | Msn Laboratories Limited | Process for preparation of dpp-iv 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 |
| WO2012135083A1 (en) * | 2011-03-31 | 2012-10-04 | Merck Sharp & Dohme Corp. | METABOLITES OF 7-(2-(4-(6-FLUORO-3-METHYLBENZO[d]ISOXAZOL-5-YL)PIPERAZIN-1-YL)ETHYL)-2-(PROP-1-YNYL)-7H-PYRAZOLO[4,3-e][1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-5-AMINE AND THEIR UTILITY AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| WO2014101113A1 (en) * | 2012-12-28 | 2014-07-03 | Merck Sharp & Dohme Corp. | Piperazine-substituted 7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
| 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 |
| WO2014128882A1 (ja) * | 2013-02-21 | 2014-08-28 | 医療法人 和楽会 | 不安うつ病の治療薬 |
| WO2015027431A1 (en) * | 2013-08-29 | 2015-03-05 | Merck Sharp & Dohme Corp. | 2,2-difluorodioxolo a2a receptor antagonists |
| MX390081B (es) * | 2014-11-03 | 2025-03-20 | Iomet Pharma Ltd | Compuesto farmacéutico. |
| WO2016089796A1 (en) * | 2014-12-04 | 2016-06-09 | Merck Sharp & Dohme Corp. | Formulation inhibiting effects of low acid environment |
| CN106543095B (zh) * | 2016-09-23 | 2019-03-05 | 江苏大学 | 一种基于2-羟基苯乙酮肟及其衍生物一锅制备苯并异噁唑的方法 |
| 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 |
| 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 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE462170B (sv) | 1987-10-27 | 1990-05-14 | Aahlstrom Corp | Avlaegsnande av loesta och kolloidala makromolekylaera organiska aemnen ur effluenter |
| 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. |
| IT1275420B (it) | 1995-06-02 | 1997-08-05 | Schering Plough S P A | Metodo per misurare l'affinita' di legame al recettore a2a dell'adenosina di componenti di interesse farmacologico mediante l'uso del ligando triziato (3h)-sch 58261 |
| 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 |
| DE19604919A1 (de) * | 1996-02-01 | 1997-08-07 | Schering Ag | Neue 2,3-Benzodiazepinderivate, deren Herstellung und Verwendung als Arzneimittel |
| 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. |
| GB0100624D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| 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 |
| DE60335294D1 (de) * | 2002-12-19 | 2011-01-20 | Schering Corp | Dlung des extrapyramidalen syndroms |
| 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 |
| 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 |
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2006
- 2006-09-20 AR ARP060104110A patent/AR056080A1/es active IP Right Grant
- 2006-09-20 PE PE2006001140A patent/PE20070521A1/es active IP Right Grant
- 2006-09-21 AU AU2006294633A patent/AU2006294633B8/en not_active Ceased
- 2006-09-21 DE DE602006021042T patent/DE602006021042D1/de active Active
- 2006-09-21 PT PT06804036T patent/PT1937687E/pt unknown
- 2006-09-21 RU RU2008115239/04A patent/RU2417997C2/ru active
- 2006-09-21 SI SI200631017T patent/SI1937687T1/sl unknown
- 2006-09-21 BR BRPI0616264A patent/BRPI0616264B8/pt not_active IP Right Cessation
- 2006-09-21 CN CN2006800352004A patent/CN101273045B/zh not_active Expired - Fee Related
- 2006-09-21 AT AT06804036T patent/ATE503759T1/de active
- 2006-09-21 WO PCT/US2006/037003 patent/WO2007038284A1/en not_active Ceased
- 2006-09-21 CA CA2623047A patent/CA2623047C/en not_active Expired - Fee Related
- 2006-09-21 US US11/525,065 patent/US7572802B2/en active Active
- 2006-09-21 PL PL06804036T patent/PL1937687T3/pl unknown
- 2006-09-21 DK DK06804036.9T patent/DK1937687T3/da active
- 2006-09-21 EP EP06804036A patent/EP1937687B1/en active Active
- 2006-09-21 MY MYPI20080750A patent/MY146429A/en unknown
- 2006-09-21 CN CN201110394181.7A patent/CN102716131B/zh not_active Expired - Fee Related
- 2006-09-21 NZ NZ566737A patent/NZ566737A/en not_active IP Right Cessation
- 2006-09-21 SG SG201006970-6A patent/SG165419A1/en unknown
- 2006-09-21 ES ES06804036T patent/ES2361856T3/es active Active
- 2006-09-21 HR HR20110466T patent/HRP20110466T1/hr unknown
- 2006-09-21 TW TW095134895A patent/TWI335329B/zh not_active IP Right Cessation
- 2006-09-21 JP JP2008532422A patent/JP4808779B2/ja not_active Expired - Fee Related
- 2006-09-21 KR KR1020087007052A patent/KR101396614B1/ko not_active Expired - Fee Related
- 2006-09-21 RS RS20110262A patent/RS51702B/sr unknown
-
2008
- 2008-03-18 IL IL190275A patent/IL190275A/en active IP Right Grant
- 2008-03-19 ZA ZA200802550A patent/ZA200802550B/xx unknown
- 2008-03-19 EC EC2008008297A patent/ECSP088297A/es unknown
- 2008-04-22 NO NO20081924A patent/NO341760B1/no not_active IP Right Cessation
-
2009
- 2009-07-06 US US12/498,013 patent/US8389532B2/en active Active
-
2011
- 2011-06-28 CY CY20111100618T patent/CY1111921T1/el unknown
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