DE60209251T2 - Adenosine a2a receptor antagonisten - Google Patents
Adenosine a2a receptor antagonisten Download PDFInfo
- Publication number
- DE60209251T2 DE60209251T2 DE60209251T DE60209251T DE60209251T2 DE 60209251 T2 DE60209251 T2 DE 60209251T2 DE 60209251 T DE60209251 T DE 60209251T DE 60209251 T DE60209251 T DE 60209251T DE 60209251 T2 DE60209251 T2 DE 60209251T2
- Authority
- DE
- Germany
- Prior art keywords
- alkyl
- alkoxy
- group
- mmol
- heteroaryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 0 C[*-](C)C1CN(*)CC1 Chemical compound C[*-](C)C1CN(*)CC1 0.000 description 12
- OLHTUBJRPJSFJU-UHFFFAOYSA-N CC(CC1)=CCC11OCCO1 Chemical compound CC(CC1)=CCC11OCCO1 OLHTUBJRPJSFJU-UHFFFAOYSA-N 0.000 description 1
- WBRMEWIAKUOSCK-UHFFFAOYSA-N CCC(NCNC1=CC=C=C1)=O Chemical compound CCC(NCNC1=CC=C=C1)=O WBRMEWIAKUOSCK-UHFFFAOYSA-N 0.000 description 1
- RXIVPHKQVZJLGC-UHFFFAOYSA-N CCc1c(NS(C)C)[nH]c2c1cccc2 Chemical compound CCc1c(NS(C)C)[nH]c2c1cccc2 RXIVPHKQVZJLGC-UHFFFAOYSA-N 0.000 description 1
- LCMBITYKSYWPRU-UHFFFAOYSA-N CN1CC(c2ccs(C)cc2)=CC1 Chemical compound CN1CC(c2ccs(C)cc2)=CC1 LCMBITYKSYWPRU-UHFFFAOYSA-N 0.000 description 1
- VWBYKVSNDIXTSS-UHFFFAOYSA-N Nc1nc(-c2cc(N(CC3)CCN3C(CCl)=O)ccc2)cc2nc(-c3ccc[o]3)n[n]12 Chemical compound Nc1nc(-c2cc(N(CC3)CCN3C(CCl)=O)ccc2)cc2nc(-c3ccc[o]3)n[n]12 VWBYKVSNDIXTSS-UHFFFAOYSA-N 0.000 description 1
- GSSYNDKOMGUCMI-UHFFFAOYSA-N Nc1nc(-c2cccc(N(CC3)CCN3C(CN3CCCCC3)=O)c2)cc2nc(-c3ccc[o]3)n[n]12 Chemical compound Nc1nc(-c2cccc(N(CC3)CCN3C(CN3CCCCC3)=O)c2)cc2nc(-c3ccc[o]3)n[n]12 GSSYNDKOMGUCMI-UHFFFAOYSA-N 0.000 description 1
- MQAJFAGHNPJXCS-UHFFFAOYSA-N Nc1nc(-c2cccc(N3CCNCC3)c2)cc2nc(-c3ccc[o]3)n[n]12 Chemical compound Nc1nc(-c2cccc(N3CCNCC3)c2)cc2nc(-c3ccc[o]3)n[n]12 MQAJFAGHNPJXCS-UHFFFAOYSA-N 0.000 description 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurosurgery (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33429301P | 2001-11-30 | 2001-11-30 | |
| US334293P | 2001-11-30 | ||
| PCT/US2002/038134 WO2003048164A2 (en) | 2001-11-30 | 2002-11-26 | Adenosine a2a receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60209251D1 DE60209251D1 (de) | 2006-04-20 |
| DE60209251T2 true DE60209251T2 (de) | 2006-11-09 |
Family
ID=23306533
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60209251T Expired - Lifetime DE60209251T2 (de) | 2001-11-30 | 2002-11-26 | Adenosine a2a receptor antagonisten |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7041666B2 (enExample) |
| EP (1) | EP1453835B1 (enExample) |
| JP (2) | JP4284181B2 (enExample) |
| KR (1) | KR20050044607A (enExample) |
| CN (1) | CN1596258A (enExample) |
| AR (1) | AR038366A1 (enExample) |
| AT (1) | ATE317844T1 (enExample) |
| AU (1) | AU2002346572A1 (enExample) |
| CA (1) | CA2468681C (enExample) |
| DE (1) | DE60209251T2 (enExample) |
| ES (1) | ES2258164T3 (enExample) |
| HU (1) | HUP0402270A3 (enExample) |
| IL (1) | IL161572A0 (enExample) |
| MX (1) | MXPA04005156A (enExample) |
| PE (1) | PE20030739A1 (enExample) |
| TW (1) | TW200300686A (enExample) |
| WO (1) | WO2003048164A2 (enExample) |
| ZA (1) | ZA200404160B (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1544200A1 (en) * | 2002-09-24 | 2005-06-22 | Kyowa Hakko Kogyo Co., Ltd. | 1,2,4 -TRIAZOLO 1,5-c PYRIMIDINE DERIVATIVE |
| US20060106040A1 (en) | 2002-12-19 | 2006-05-18 | Michael Grzelak | Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| CN101310724A (zh) | 2002-12-19 | 2008-11-26 | 先灵公司 | 腺苷A2a受体拮抗剂的应用 |
| US20070010522A1 (en) * | 2003-04-09 | 2007-01-11 | Chi Vu | Triazolo[1,5-c]pyrimidines and pyrazolo[1,5-c]pyrimidines useful as a2a adenosine receptor antagonists |
| CA2541989C (en) * | 2003-10-24 | 2013-10-01 | Exelixis, Inc. | P70s6 kinase modulators and method of use |
| AR050926A1 (es) * | 2004-09-03 | 2006-12-06 | Astrazeneca Ab | Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac) |
| WO2006129626A1 (ja) * | 2005-05-30 | 2006-12-07 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]トリアゾロ[1,5-c]ピリミジン誘導体の製造法 |
| ES2273599B1 (es) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | Compuestos para el tratamiento de la fibrilacion auricular. |
| US8835631B2 (en) * | 2007-05-24 | 2014-09-16 | Mitsubishi Tanabe Pharma Corporation | Therapeutic agent for cerebral infarction |
| CA2690748A1 (en) * | 2007-06-25 | 2008-12-31 | Neurogen Corporation | Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues |
| US20100093764A1 (en) * | 2008-10-13 | 2010-04-15 | Devraj Chakravarty | AMINES AND SULFOXIDES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| US20100093756A1 (en) * | 2008-10-13 | 2010-04-15 | Berbay J Kent | HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| WO2010061696A1 (ja) | 2008-11-25 | 2010-06-03 | 日産自動車株式会社 | 導電部材及びこれを用いた固体高分子形燃料電池 |
| EP2424840B1 (en) * | 2009-04-27 | 2014-08-06 | Boehringer Ingelheim International GmbH | Cxcr3 receptor antagonists |
| WO2011084985A1 (en) | 2010-01-07 | 2011-07-14 | Boehringer Ingelheim International Gmbh | Cxcr3 receptor antagonists |
| JP5843869B2 (ja) * | 2010-09-24 | 2016-01-13 | アドヴィナス・セラピューティックス・リミテッド | アデノシン受容体拮抗薬としての縮合三環化合物 |
| WO2012127472A1 (en) * | 2011-03-22 | 2012-09-27 | Mapi Pharma Ltd. | Process and intermediates for the preparation of preladenant and related compounds |
| JP7065113B2 (ja) * | 2017-04-07 | 2022-05-11 | 南京明徳新薬研発有限公司 | Ａ２Ａ受容体阻害剤としての［１，２，４］トリアゾロ［１，５－ｃ］ピリミジン誘導体 |
| CA3092470A1 (en) * | 2018-02-27 | 2019-09-06 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors |
| CN112105617B (zh) * | 2018-04-28 | 2022-04-05 | 南京明德新药研发有限公司 | 一种三唑并嘧啶类化合物的晶型、盐型及其制备方法 |
| JP7391046B2 (ja) * | 2018-05-18 | 2023-12-04 | インサイト・コーポレイション | Ａ２ａ／ａ２ｂ阻害剤としての縮合ピリミジン誘導体 |
| JP7490631B2 (ja) | 2018-07-05 | 2024-05-27 | インサイト・コーポレイション | Ａ２ａ／ａ２ｂ阻害剤としての縮合ピラジン誘導体 |
| TWI820209B (zh) | 2018-09-12 | 2023-11-01 | 大陸商迪哲（江蘇）醫藥股份有限公司 | 三唑并－嘧啶化合物及其用途 |
| 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 |
| US12466831B2 (en) * | 2018-11-20 | 2025-11-11 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine 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 |
| EA202191498A1 (ru) | 2018-11-30 | 2021-08-20 | Мерк Шарп энд Доум Корп. | 9-замещенные производные аминотриазолохиназолина в качестве антагонистов аденозиновых рецепторов, фармацевтические композиции и их применение |
| BR112021011948A2 (pt) | 2018-12-20 | 2021-09-08 | Incyte Corporation | Compostos de imidazopiridazina e imidazopiridina e usos dos mesmos |
| WO2020128036A1 (en) * | 2018-12-21 | 2020-06-25 | Ryvu Therapeutics S.A. | Modulators of the adenosine a2a receptor |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU622330B2 (en) | 1989-06-23 | 1992-04-02 | Takeda Chemical Industries Ltd. | Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides |
| 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 |
| DE69428977T2 (de) | 1993-07-27 | 2002-07-11 | Kyowa Hakko Kogyo Co., Ltd. | Arzneimittel gegen Parkinsonsche Krankheit |
| 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 |
| AU743910B2 (en) | 1997-03-24 | 2002-02-07 | Kyowa Hakko Kirin Co., Ltd. | {1,2,4}triazolo{1,5-c}pyrimidine derivatives |
| 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 |
| CN1328560A (zh) | 1998-09-22 | 2001-12-26 | 协和发酵工业株式会社 | [1,2,4]三唑并[1,5－c]嘧啶衍生物 |
| DE60110219T2 (de) | 2000-05-26 | 2006-03-09 | Schering Corp. | Adenosin a2a rezeptor antagonisten |
| WO2002079204A1 (en) * | 2001-03-28 | 2002-10-10 | Kyowa Hakko Kogyo Co., Ltd. | 8-thiazolyl[1,2,4]triazolo[1,5-c]pyrimidine derivative |
| WO2003048163A1 (en) | 2001-11-30 | 2003-06-12 | Schering Corporation | [1,2,4]-TRIAZOLE BICYCLIC ADENOSINE A2a RECEPTOR ANTAGONISTS |
-
2002
- 2002-11-25 TW TW091134178A patent/TW200300686A/zh unknown
- 2002-11-25 AR ARP020104528A patent/AR038366A1/es unknown
- 2002-11-25 PE PE2002001128A patent/PE20030739A1/es not_active Application Discontinuation
- 2002-11-26 KR KR1020047008031A patent/KR20050044607A/ko not_active Withdrawn
- 2002-11-26 US US10/304,504 patent/US7041666B2/en not_active Expired - Lifetime
- 2002-11-26 DE DE60209251T patent/DE60209251T2/de not_active Expired - Lifetime
- 2002-11-26 AT AT02784641T patent/ATE317844T1/de not_active IP Right Cessation
- 2002-11-26 JP JP2003549354A patent/JP4284181B2/ja not_active Expired - Fee Related
- 2002-11-26 IL IL16157202A patent/IL161572A0/xx unknown
- 2002-11-26 EP EP02784641A patent/EP1453835B1/en not_active Expired - Lifetime
- 2002-11-26 MX MXPA04005156A patent/MXPA04005156A/es active IP Right Grant
- 2002-11-26 WO PCT/US2002/038134 patent/WO2003048164A2/en not_active Ceased
- 2002-11-26 CA CA2468681A patent/CA2468681C/en not_active Expired - Fee Related
- 2002-11-26 CN CNA028239229A patent/CN1596258A/zh active Pending
- 2002-11-26 ES ES02784641T patent/ES2258164T3/es not_active Expired - Lifetime
- 2002-11-26 HU HU0402270A patent/HUP0402270A3/hu unknown
- 2002-11-26 AU AU2002346572A patent/AU2002346572A1/en not_active Abandoned
-
2004
- 2004-05-27 ZA ZA200404160A patent/ZA200404160B/en unknown
-
2008
- 2008-06-04 JP JP2008147394A patent/JP2008303217A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP1453835A2 (en) | 2004-09-08 |
| WO2003048164A2 (en) | 2003-06-12 |
| ES2258164T3 (es) | 2006-08-16 |
| TW200300686A (en) | 2003-06-16 |
| KR20050044607A (ko) | 2005-05-12 |
| HUP0402270A3 (en) | 2008-09-29 |
| IL161572A0 (en) | 2004-09-27 |
| CA2468681C (en) | 2011-01-25 |
| DE60209251D1 (de) | 2006-04-20 |
| CA2468681A1 (en) | 2003-06-12 |
| HK1064100A1 (en) | 2005-01-21 |
| CN1596258A (zh) | 2005-03-16 |
| MXPA04005156A (es) | 2004-08-11 |
| PE20030739A1 (es) | 2003-08-28 |
| JP2005511698A (ja) | 2005-04-28 |
| HUP0402270A2 (hu) | 2005-02-28 |
| JP4284181B2 (ja) | 2009-06-24 |
| ATE317844T1 (de) | 2006-03-15 |
| US7041666B2 (en) | 2006-05-09 |
| WO2003048164A3 (en) | 2003-10-16 |
| EP1453835B1 (en) | 2006-02-15 |
| JP2008303217A (ja) | 2008-12-18 |
| AU2002346572A1 (en) | 2003-06-17 |
| AR038366A1 (es) | 2005-01-12 |
| US20030212080A1 (en) | 2003-11-13 |
| ZA200404160B (en) | 2005-04-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition |