AR037680A1 - Antagonistas del receptor de adenosina a2a de 5-amino-pirazolo-[4,3-e]-1,2,4-triazolo[1,5-c]-pirimidinas sustituidas, composiciones farmaceuticas que los comprenden, el uso de dichos compuestos, solos o en combinacion para la elaboracion de un medicamento utiles para el tratamiento de enfermedades d - Google Patents
Antagonistas del receptor de adenosina a2a de 5-amino-pirazolo-[4,3-e]-1,2,4-triazolo[1,5-c]-pirimidinas sustituidas, composiciones farmaceuticas que los comprenden, el uso de dichos compuestos, solos o en combinacion para la elaboracion de un medicamento utiles para el tratamiento de enfermedades dInfo
- Publication number
- AR037680A1 AR037680A1 ARP020104561A ARP020104561A AR037680A1 AR 037680 A1 AR037680 A1 AR 037680A1 AR P020104561 A ARP020104561 A AR P020104561A AR P020104561 A ARP020104561 A AR P020104561A AR 037680 A1 AR037680 A1 AR 037680A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- amino
- substituents
- aryl
- halogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 title 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 title 1
- 229960005305 adenosine Drugs 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 6
- 125000004442 acylamino group Chemical group 0.000 abstract 4
- 125000004423 acyloxy group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000003282 alkyl amino group Chemical group 0.000 abstract 4
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000003725 azepanyl group Chemical group 0.000 abstract 4
- 125000004472 dialkylaminosulfonyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000003386 piperidinyl group Chemical group 0.000 abstract 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 3
- 125000005083 alkoxyalkoxy group Chemical group 0.000 abstract 2
- 125000005422 alkyl sulfonamido group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 210000003169 central nervous system Anatomy 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 150000003230 pyrimidines Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
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)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Veterinary Medicine (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (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 |
|---|---|
| AR037680A1 true AR037680A1 (es) | 2004-12-01 |
Family
ID=23306779
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020104561A AR037680A1 (es) | 2001-11-30 | 2002-11-27 | Antagonistas del receptor de adenosina a2a de 5-amino-pirazolo-[4,3-e]-1,2,4-triazolo[1,5-c]-pirimidinas sustituidas, composiciones farmaceuticas que los comprenden, el uso de dichos compuestos, solos o en combinacion para la elaboracion de un medicamento utiles para el tratamiento de enfermedades d |
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 |
|---|---|---|---|---|
| SI1283839T1 (https=) * | 2000-05-26 | 2005-08-31 | Schering Corp | |
| US6964288B2 (en) * | 2001-07-06 | 2005-11-15 | Ksaria Corporation | Apparatus and method for automated preparation of an optical fiber |
| 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 |
| 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 |
| JP2006514697A (ja) * | 2002-12-19 | 2006-05-11 | シェーリング コーポレイション | アデノシンＡ２ａレセプターアンタゴニストの使用 |
| JP4800216B2 (ja) * | 2003-10-24 | 2011-10-26 | エグゼリクシス， インコーポレイテッド | ｐ７０Ｓ６キナーゼモジュレーターおよび使用方法 |
| CN1898246B (zh) * | 2003-10-28 | 2010-10-27 | 先灵公司 | 制备取代的5-氨基-吡唑并[4，3-e]-1，2，4-三唑并[1，5-c]嘧啶的方法 |
| WO2005060981A2 (en) * | 2003-12-19 | 2005-07-07 | Schering Corporation | Pharmaceutical compositions |
| EP1902716A4 (en) * | 2005-06-07 | 2009-05-13 | Kyowa Hakko Kirin Co Ltd | PROPHYLACTIC AND / OR THERAPEUTIC AGENT FOR MOTOR TROUBLESHOOTING |
| 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 |
| 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 |
| 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 |
| US20100028266A1 (en) | 2008-08-01 | 2010-02-04 | Alpha Synergy Development. Inc. | Composition and methods for treating allergic response |
| US20100203165A1 (en) | 2008-08-01 | 2010-08-12 | Gerald Horn | Compositions and methods for treatment of disorders or conditions of the eye |
| US8952011B2 (en) | 2008-08-01 | 2015-02-10 | Eye Therapies Llc | Compositions and methods for the treatment of nasal conditions |
| WO2010078430A1 (en) | 2008-12-30 | 2010-07-08 | Arqule, Inc. | Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds |
| TW201100427A (en) | 2009-03-31 | 2011-01-01 | 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 |
| 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 |
| KR20210093964A (ko) | 2018-11-20 | 2021-07-28 | 머크 샤프 앤드 돔 코포레이션 | 치환된 아미노 트리아졸로피리미딘 및 아미노 트리아졸로피라진 아데노신 수용체 길항제, 제약 조성물 및 그의 용도 |
| TW202039496A (zh) | 2018-11-30 | 2020-11-01 | 美商默沙東藥廠 | 做為腺苷受體拮抗劑之9-經取代胺基三唑喹唑啉衍生物、醫藥組合物及其用途 |
| JP2022511778A (ja) | 2018-11-30 | 2022-02-01 | メルク・シャープ・アンド・ドーム・コーポレーション | アデノシン受容体拮抗薬としての７－、８－及び１０－置換されたアミノトリアゾロキナゾリン誘導体、医薬組成物及びそれらの使用 |
| 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 |
| CN114667287A (zh) * | 2019-07-17 | 2022-06-24 | 泰昂治疗公司 | 腺苷a2a受体拮抗剂及其用途 |
| CN112592346B (zh) | 2019-07-30 | 2022-04-26 | 厦门宝太生物科技股份有限公司 | 一种a2a和/或a2b抑制剂中间体的制备方法 |
| CN111825698B (zh) | 2019-07-30 | 2021-10-15 | 杭州阿诺生物医药科技有限公司 | 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 |
| EP0666079B1 (en) * | 1993-07-27 | 2001-11-07 | 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 |
| SI1283839T1 (https=) * | 2000-05-26 | 2005-08-31 | Schering Corp | |
| 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 |
| CL2004000847A1 (es) * | 2003-04-23 | 2005-03-11 | Schering Corp | Compuestos derivados de 2-alquinil o 2-alquenil-5amino-pirazolo-[4,3-e]-1,2,4-triazolo[1,5-]pirimidina; composicion farmaceutica, y uso en el tratamiento de enfermedades del sistema nervioso central o un accidente cerebrovascular tal como depresion, |
-
2002
- 2002-11-26 CA CA002468649A patent/CA2468649C/en not_active Expired - Fee Related
- 2002-11-26 ES ES02784568T patent/ES2336435T3/es not_active Expired - Lifetime
- 2002-11-26 MX MXPA04005209A patent/MXPA04005209A/es active IP Right Grant
- 2002-11-26 EP EP02784568A patent/EP1448565B1/en not_active Expired - Lifetime
- 2002-11-26 DE DE60234951T patent/DE60234951D1/de not_active Expired - Lifetime
- 2002-11-26 AT AT02784568T patent/ATE453647T1/de not_active IP Right Cessation
- 2002-11-26 JP JP2003549355A patent/JP4284182B2/ja not_active Expired - Fee Related
- 2002-11-26 AU AU2002346503A patent/AU2002346503A1/en not_active Abandoned
- 2002-11-26 IL IL16171602A patent/IL161716A0/xx unknown
- 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 HU HU0402018A patent/HUP0402018A3/hu unknown
- 2002-11-26 CN CNA02823782XA patent/CN1692116A/zh active Pending
- 2002-11-26 US US10/304,931 patent/US6916811B2/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 |
|---|---|
| MXPA04005209A (es) | 2004-08-19 |
| US6916811B2 (en) | 2005-07-12 |
| HUP0402018A2 (hu) | 2005-02-28 |
| JP4284182B2 (ja) | 2009-06-24 |
| JP2005511699A (ja) | 2005-04-28 |
| TW200306837A (en) | 2003-12-01 |
| ZA200404161B (en) | 2005-11-30 |
| CN1692116A (zh) | 2005-11-02 |
| EP1448565A1 (en) | 2004-08-25 |
| HK1063780A1 (en) | 2005-01-14 |
| CA2468649C (en) | 2009-03-10 |
| DE60234951D1 (de) | 2010-02-11 |
| AU2002346503A1 (en) | 2003-06-17 |
| ATE453647T1 (de) | 2010-01-15 |
| EP1448565B1 (en) | 2009-12-30 |
| PE20030665A1 (es) | 2003-08-08 |
| ES2336435T3 (es) | 2010-04-13 |
| HUP0402018A3 (en) | 2008-06-30 |
| KR20050044593A (ko) | 2005-05-12 |
| JP2008260776A (ja) | 2008-10-30 |
| IL161716A0 (en) | 2004-09-27 |
| WO2003048165A1 (en) | 2003-06-12 |
| US20030212059A1 (en) | 2003-11-13 |
| CA2468649A1 (en) | 2003-06-12 |
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| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |