ATE433454T1 - Pyrazoloä1,5-aüpyrimidine als antagonisten des adenosin-a2a-rezeptors - Google Patents
Pyrazoloä1,5-aüpyrimidine als antagonisten des adenosin-a2a-rezeptorsInfo
- Publication number
- ATE433454T1 ATE433454T1 AT05854388T AT05854388T ATE433454T1 AT E433454 T1 ATE433454 T1 AT E433454T1 AT 05854388 T AT05854388 T AT 05854388T AT 05854388 T AT05854388 T AT 05854388T AT E433454 T1 ATE433454 T1 AT E433454T1
- Authority
- AT
- Austria
- Prior art keywords
- optionally substituted
- alkyl
- cycloalkyl
- hydrogen
- halo
- Prior art date
Links
- 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
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 208000018737 Parkinson disease Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000000732 arylene group Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002993 cycloalkylene group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 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
- C07D487/02—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 two hetero rings
- C07D487/04—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
- A61P25/22—Anxiolytics
-
- 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 Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63802804P | 2004-12-21 | 2004-12-21 | |
| PCT/US2005/045658 WO2006068954A2 (en) | 2004-12-21 | 2005-12-19 | PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE433454T1 true ATE433454T1 (de) | 2009-06-15 |
Family
ID=36602229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT05854388T ATE433454T1 (de) | 2004-12-21 | 2005-12-19 | Pyrazoloä1,5-aüpyrimidine als antagonisten des adenosin-a2a-rezeptors |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US7741318B2 (de) |
| EP (1) | EP1836205B1 (de) |
| JP (1) | JP2008524330A (de) |
| CN (1) | CN101119998A (de) |
| AT (1) | ATE433454T1 (de) |
| CA (1) | CA2591125A1 (de) |
| DE (1) | DE602005014891D1 (de) |
| ES (1) | ES2327145T3 (de) |
| MX (1) | MX2007007604A (de) |
| WO (1) | WO2006068954A2 (de) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7196078B2 (en) * | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US20060128694A1 (en) * | 2002-12-19 | 2006-06-15 | Michael Grzelak | Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| WO2008027220A2 (en) * | 2006-08-28 | 2008-03-06 | Schering Corporation | Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3, 3a-dihydropyrazol0 [1, 5-a] pyrimidin-7-yl) -amino derivatives |
| JP5214799B2 (ja) * | 2008-04-07 | 2013-06-19 | アイアールエム・リミテッド・ライアビリティ・カンパニー | キナーゼ阻害剤としての化合物および組成物 |
| US20100093721A1 (en) * | 2008-10-13 | 2010-04-15 | Barbay J Kent | PHENYL AND HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| EP2210891A1 (de) | 2009-01-26 | 2010-07-28 | Domain Therapeutics | Neue Adenosin-Rezeptorliganden und Verwendungen davon |
| WO2010140339A1 (ja) * | 2009-06-01 | 2010-12-09 | 武田薬品工業株式会社 | 複素環化合物 |
| CN101906105B (zh) * | 2009-06-08 | 2013-01-16 | 河北医科大学 | 吡唑并[1,5-a]嘧啶酮衍生物及其药物组合物以及其用途 |
| WO2011061754A1 (en) * | 2009-11-18 | 2011-05-26 | Council Of Scientific & Industrial Research | A novel 3-substituted 7-imino-2-thioxo-3, 7-dihydro-2h-thiazolo [4,5-di pyrimidin-6-yl - and process for preparation thereof |
| PH12012501643A1 (en) * | 2010-02-26 | 2017-07-19 | Mitsubishi Tanabe Pharma Corp | Pyrazolopyrimidine compounds and their use as pde 10 inhibitors |
| AU2011260323A1 (en) * | 2010-06-04 | 2012-11-15 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as LRRK2 modulators |
| US20140288052A1 (en) * | 2011-10-20 | 2014-09-25 | GlaxoSmithKline, LLC | Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators |
| KR20140077963A (ko) | 2011-10-20 | 2014-06-24 | 글락소스미스클라인 엘엘씨 | 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체 |
| RU2015143517A (ru) * | 2013-03-13 | 2017-04-19 | Дженентек, Инк. | Пиразолсодержащие соединения и их применения |
| CN103626776B (zh) * | 2013-12-05 | 2017-02-15 | 北京师范大学 | 吡唑并[1,5‑a]嘧啶氮芥衍生物及其制备方法和肿瘤治疗应用 |
| US10913744B2 (en) * | 2015-02-13 | 2021-02-09 | Dana-Farber Cancer Institute, Inc. | LRRK2 inhibitors and methods of making and using the same |
| KR20250174699A (ko) | 2018-10-30 | 2025-12-12 | 크로노스 바이오, 인코포레이티드 | Cdk9 활성을 조절하기 위한 화합물, 조성물 및 방법 |
| 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 |
| JP2022507734A (ja) | 2018-11-20 | 2022-01-18 | メルク・シャープ・アンド・ドーム・コーポレーション | 置換アミノトリアゾロピリミジン及びアミノトリアゾロピラジンアデノシン受容体アンタゴニスト、医薬組成物及びそれらの使用 |
| AR117164A1 (es) | 2018-11-30 | 2021-07-14 | Merck Sharp & Dohme | Derivados de amino-triazoloquinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmacéuticas y su uso para el tratamiento de diversos tipos de cáncer |
| 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 |
| CN112921405B (zh) * | 2019-12-05 | 2023-06-27 | 成都先导药物开发股份有限公司 | 一种合成On-DNA吡唑并[1,5-a]嘧啶化合物的方法 |
| WO2022166796A1 (zh) * | 2021-02-05 | 2022-08-11 | 上海齐鲁制药研究中心有限公司 | 嘧啶或吡啶并杂环类腺苷受体抑制剂及其制备方法和用途 |
| WO2026089952A1 (en) * | 2024-10-21 | 2026-04-30 | International Flavors & Fragrances Inc. | Novel flavor modulating compounds |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2057089A1 (en) * | 1990-12-07 | 1992-06-08 | Eric E. Allen | Substituted pyrazolopyrimidines and imidazopyridazines as angiotensin ii antagonists |
| US5571813A (en) * | 1993-06-10 | 1996-11-05 | Beiersdorf-Lilly Gmbh | Fused pyrimidine compounds and their use as pharmaceuticals |
| WO1998042711A1 (en) * | 1997-03-24 | 1998-10-01 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES |
| US6355653B1 (en) * | 1999-09-06 | 2002-03-12 | Hoffmann-La Roche Inc. | Amino-triazolopyridine derivatives |
| YU23602A (sh) * | 1999-09-30 | 2004-09-03 | Neurogen Corporation | Amino supstituisani pirazolo /1,5/a/-1,5-pirimidini i pirazolo /1,5-a/-1,3,5-triazini |
| DE60313872T2 (de) * | 2002-09-04 | 2008-01-17 | Schering Corp. | Pyrazoloä1,5-aüpyrimidine als hemmstoffe cyclin-abhängiger kinasen |
| JP4564485B2 (ja) * | 2003-02-28 | 2010-10-20 | 帝人ファーマ株式会社 | ピラゾロ[1,5−a]ピリミジン誘導体 |
| WO2004087707A1 (en) * | 2003-03-31 | 2004-10-14 | Vernalis (Cambridge) Limited | Pyrazolopyrimidine compounds and their use in medicine |
| WO2004092171A2 (en) | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]pyrimidines useful as a2a adenosin e receptor antagonists |
-
2005
- 2005-12-19 CN CNA2005800482380A patent/CN101119998A/zh active Pending
- 2005-12-19 US US11/311,195 patent/US7741318B2/en not_active Expired - Lifetime
- 2005-12-19 WO PCT/US2005/045658 patent/WO2006068954A2/en not_active Ceased
- 2005-12-19 CA CA002591125A patent/CA2591125A1/en not_active Abandoned
- 2005-12-19 AT AT05854388T patent/ATE433454T1/de not_active IP Right Cessation
- 2005-12-19 ES ES05854388T patent/ES2327145T3/es not_active Expired - Lifetime
- 2005-12-19 JP JP2007548334A patent/JP2008524330A/ja active Pending
- 2005-12-19 EP EP05854388A patent/EP1836205B1/de not_active Expired - Lifetime
- 2005-12-19 DE DE602005014891T patent/DE602005014891D1/de not_active Expired - Lifetime
- 2005-12-19 MX MX2007007604A patent/MX2007007604A/es active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| US7741318B2 (en) | 2010-06-22 |
| US20060135526A1 (en) | 2006-06-22 |
| EP1836205A2 (de) | 2007-09-26 |
| DE602005014891D1 (de) | 2009-07-23 |
| CA2591125A1 (en) | 2006-06-29 |
| EP1836205B1 (de) | 2009-06-10 |
| JP2008524330A (ja) | 2008-07-10 |
| WO2006068954A2 (en) | 2006-06-29 |
| WO2006068954A3 (en) | 2006-12-07 |
| HK1108882A1 (en) | 2008-05-23 |
| MX2007007604A (es) | 2007-08-02 |
| ES2327145T3 (es) | 2009-10-26 |
| CN101119998A (zh) | 2008-02-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |