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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (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 (23)
| 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 |
| MX2009002267A (es) * | 2006-08-28 | 2009-03-20 | Schering Corp | Procedimiento e intermediarios para la sintesis de derivados e intermediarios de (3-alquil-5-piperidin-1-il-3,3a-dihidro-pirazolo [1,5-a]pirimidin-7-il)-amino. |
| EP2271645A1 (de) * | 2008-04-07 | 2011-01-12 | Irm Llc | Verbindungen und zusammensetzungen als kinasehemmer |
| 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 |
| EP2501706B1 (de) | 2009-11-18 | 2014-08-06 | Council of Scientific & Industrial Research | Neues 3-substituiertes 7-imino-2-thioxo-3, 7-dihydro-2h-thiazolo [4,5-di pyrimidin-6-yl und herstellungsverfahren dafür |
| EP2539342B1 (de) * | 2010-02-26 | 2015-04-15 | Mitsubishi Tanabe Pharma Corporation | Pyrazolopyrimidinverbindungen und ihre verwendung als pde10-hemmer |
| HUE029196T2 (en) * | 2010-06-04 | 2017-02-28 | Hoffmann La Roche | Aminoprimidine derivatives as LRRK2 modulators |
| EP2768833A4 (de) * | 2011-10-20 | 2015-04-15 | Sirtris Pharmaceuticals Inc | Substituierte bicyclische aza-heterocyclen und analoga als sirtuin-modulatoren |
| EP2768509B1 (de) | 2011-10-20 | 2017-03-22 | Glaxosmithkline LLC | Substituierte bicyclische aza-heterocyclen und analoga als sirtuin-modulatoren |
| EP2970307B1 (de) * | 2013-03-13 | 2020-03-11 | Genentech, Inc. | Pyrazolverbindungen und verwendungen davon |
| 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 |
| WO2016130920A2 (en) * | 2015-02-13 | 2016-08-18 | Dana-Farber Cancer Institute, Inc. | Lrrk2 inhibitors and methods of making and using the same |
| MY210039A (en) | 2018-10-30 | 2025-08-22 | Kronos Bio Inc | Compounds, compositions, and methods for modulating cdk9 activity |
| EP3883576B1 (de) | 2018-11-20 | 2025-12-17 | Merck Sharp & Dohme LLC | Substituierte aminotriazolopyrimidine und amino-triazolopyrazin-adenosinrezeptor-antagonisten, pharmazeutische zusammensetzungen und deren verwendung |
| 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 |
| KR102653800B1 (ko) | 2018-11-30 | 2024-04-01 | 머크 샤프 앤드 돔 엘엘씨 | 아데노신 수용체 길항제로서의 9-치환된 아미노 트리아졸로 퀴나졸린 유도체, 제약 조성물 및 그의 용도 |
| CA3120331A1 (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 |
| 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 |
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 |
| CA2284737C (en) | 1997-03-24 | 2007-03-13 | 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 |
| EP1218381B1 (de) * | 1999-09-30 | 2006-12-06 | Neurogen Corporation | Amino-substituierte pyrazolo¬1,5-a|-1,5-pyrimidine und pyrazolo¬1,5-a|-1,3,5-triazine |
| CN1701073B (zh) | 2002-09-04 | 2011-06-22 | 先灵公司 | 作为细胞周期蛋白依赖激酶抑制剂的吡唑并[1,5-a]嘧啶 |
| EP1599482A4 (de) * | 2003-02-28 | 2008-10-01 | Teijin Pharma Ltd | Pyrazolo¬1,5-a pyrimidinderivate |
| EP1608652A1 (de) * | 2003-03-31 | 2005-12-28 | Vernalis (Cambridge) Limited | Pyrazolopyrimidinverbindungen und deren verwendung in der medizin |
| 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 WO PCT/US2005/045658 patent/WO2006068954A2/en not_active Ceased
- 2005-12-19 CN CNA2005800482380A patent/CN101119998A/zh active Pending
- 2005-12-19 CA CA002591125A patent/CA2591125A1/en not_active Abandoned
- 2005-12-19 EP EP05854388A patent/EP1836205B1/de not_active Expired - Lifetime
- 2005-12-19 ES ES05854388T patent/ES2327145T3/es not_active Expired - Lifetime
- 2005-12-19 DE DE602005014891T patent/DE602005014891D1/de not_active Expired - Lifetime
- 2005-12-19 JP JP2007548334A patent/JP2008524330A/ja active Pending
- 2005-12-19 US US11/311,195 patent/US7741318B2/en active Active
- 2005-12-19 AT AT05854388T patent/ATE433454T1/de not_active IP Right Cessation
- 2005-12-19 MX MX2007007604A patent/MX2007007604A/es active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| CA2591125A1 (en) | 2006-06-29 |
| DE602005014891D1 (de) | 2009-07-23 |
| WO2006068954A3 (en) | 2006-12-07 |
| JP2008524330A (ja) | 2008-07-10 |
| US20060135526A1 (en) | 2006-06-22 |
| CN101119998A (zh) | 2008-02-06 |
| WO2006068954A2 (en) | 2006-06-29 |
| ES2327145T3 (es) | 2009-10-26 |
| HK1108882A1 (en) | 2008-05-23 |
| US7741318B2 (en) | 2010-06-22 |
| EP1836205B1 (de) | 2009-06-10 |
| EP1836205A2 (de) | 2007-09-26 |
| MX2007007604A (es) | 2007-08-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |