ES2153118T3 - Analogos heterociclicos de 1,2,4-triazolo 1,5-c)pirimidina que tienen una actividad antagonista sobre los receptores de adenosina a 2a?. - Google Patents

Analogos heterociclicos de 1,2,4-triazolo 1,5-c)pirimidina que tienen una actividad antagonista sobre los receptores de adenosina a 2a?.

Info

Publication number
ES2153118T3
ES2153118T3 ES96924840T ES96924840T ES2153118T3 ES 2153118 T3 ES2153118 T3 ES 2153118T3 ES 96924840 T ES96924840 T ES 96924840T ES 96924840 T ES96924840 T ES 96924840T ES 2153118 T3 ES2153118 T3 ES 2153118T3
Authority
ES
Spain
Prior art keywords
triazol
pirimidine
heterociclic
analogs
antagonist activity
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
Application number
ES96924840T
Other languages
English (en)
Inventor
Pier Giovanni Baraldi
Barbara Cacciari
Monica Viziano
Silvio Dionisotti
Ennio Ongini
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme Corp
Original Assignee
Schering Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Application granted granted Critical
Publication of ES2153118T3 publication Critical patent/ES2153118T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-condensed systems

Abstract

LOS COMPUESTOS DE FORMULA GENERAL (I), EN LA CUAL A ES UN ANILLO PIRAZOL, IMIDAZOL O TRIAZOL, R TIENE LA FORMULA (II), EN LA QUE R 1 Y R 2 , QUE SON IGUALES O DIFERENTES, SON H, OH, HALOGENO, GRUPOS ALCOXI C 1-4 , ALQUILO C 1.4 , NITRO, AMINO, CIANO, HALOALQUILO C 1-4 , HALOALCOXI C 14 , CARBOXI, CARBOXAMIDO; ADEMAS EL GRUPO OH JUNTO CON UNO DE R 1 O R 2 O R 1 Y R 2 PUEDEN FORMAR EL GRUPO METILENDIOXI O - CH 2 - O; N ES UN NUMERO ENTERO ENTRE 0 Y 4, SON UTILES COMO AGENTES TERAPEUTICOS.
ES96924840T 1995-07-28 1996-07-02 Analogos heterociclicos de 1,2,4-triazolo 1,5-c)pirimidina que tienen una actividad antagonista sobre los receptores de adenosina a 2a?. Expired - Lifetime ES2153118T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT95MI001671A IT1277392B1 (it) 1995-07-28 1995-07-28 Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina

Publications (1)

Publication Number Publication Date
ES2153118T3 true ES2153118T3 (es) 2001-02-16

Family

ID=11372092

Family Applications (1)

Application Number Title Priority Date Filing Date
ES96924840T Expired - Lifetime ES2153118T3 (es) 1995-07-28 1996-07-02 Analogos heterociclicos de 1,2,4-triazolo 1,5-c)pirimidina que tienen una actividad antagonista sobre los receptores de adenosina a 2a?.

Country Status (11)

Country Link
US (1) US5935964A (es)
EP (1) EP0856003B1 (es)
AT (1) ATE198334T1 (es)
CA (1) CA2227991C (es)
DE (1) DE69611377T2 (es)
DK (1) DK0856003T3 (es)
ES (1) ES2153118T3 (es)
GR (1) GR3035309T3 (es)
IT (1) IT1277392B1 (es)
PT (1) PT856003E (es)
WO (1) WO1997005138A1 (es)

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US7160890B2 (en) 1999-12-02 2007-01-09 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
DK1246623T3 (da) 1999-12-02 2006-11-13 Osi Pharm Inc Forbindelser, som er specifikke for adenosin A1-, A2a- og A3-receptor og anvendelser deraf
US6680322B2 (en) 1999-12-02 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
ATE293627T1 (de) * 2000-05-26 2005-05-15 Schering Corp Adenosin a2a rezeptor antagonisten
US6680324B2 (en) * 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US6673802B2 (en) 2000-12-01 2004-01-06 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
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EP1453836B1 (en) 2001-11-30 2007-03-28 Schering Corporation BICYCLIC [1,2,4] -TRIAZOLE ADENOSINE A2a RECEPTOR ANTAGONISTS
DE60234951D1 (de) 2001-11-30 2010-02-11 Schering Corp Adenosin a2a rezeptor antagonisten
EP1450811B1 (en) * 2001-11-30 2009-10-21 OSI Pharmaceuticals, Inc. Compounds specific to adenosine A1 and A3 receptors and uses thereof
AR038366A1 (es) 2001-11-30 2005-01-12 Schering Corp Compuestos de 1,2,4-triazolo [1,5-c] pirimidinas sustituidas, antagonistas del receptor de adenosina a2a, composiciones farmaceuticas, el uso de dichos compuestos para la manufactura de un medicamento para el tratamiento de enfermedades del sistema nervioso central y un kit que comprende combinacion
CN1620294A (zh) 2001-12-20 2005-05-25 Osi药物公司 嘧啶a2b选择性拮抗剂化合物,它们的合成及用途
CN1816551A (zh) 2001-12-20 2006-08-09 Osi药物公司 吡咯并嘧啶A2b选择性拮抗剂化合物,它们的合成及用途
US7205403B2 (en) * 2002-02-01 2007-04-17 King Pharmaceuticals Research And Development, Inc. 8-Heteroaryl xanthine adenosine A2B receptor antagonists
KR20040111324A (ko) 2002-05-30 2004-12-31 킹 파머슈티칼스 리서치 앤드 디벨로프먼트 아이엔씨 트리사이클릭 파이라졸로트리아졸로피리미딘 링 구조를지닌 약제학적 활성화합물 및 사용 방법
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
CN100415217C (zh) * 2002-12-19 2008-09-03 先灵公司 腺苷A2a受体拮抗剂的应用
MY139344A (en) 2003-04-23 2009-09-30 Schering Corp 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine a2a receptor antagonists
US7709492B2 (en) 2004-04-21 2010-05-04 Schering Corporation Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
EP1934227B1 (en) 2005-09-19 2011-12-21 Schering Corporation 2-HETEROARYL-PYRAZOLO-[4, 3-e]-1, 2, 4-TRIAZOLO-[1,5-c]-PYRIMIDINE AS ADENOSINE A2a RECEPTOR ANTAGONISTS
PE20070521A1 (es) 2005-09-23 2007-07-13 Schering Corp 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
ES2273599B1 (es) 2005-10-14 2008-06-01 Universidad De Barcelona Compuestos para el tratamiento de la fibrilacion auricular.
US9255099B2 (en) 2006-06-06 2016-02-09 Intra-Cellular Therapies, Inc. Pyrazolo[3,4-D]pyrimidine-4,6(5H,7H)-diones as phosphodiesterase 1 inhibitors
US7723343B2 (en) * 2007-03-30 2010-05-25 King Pharmaceuticals Research And Development, Inc. Adenosine A2A receptor antagonists
KR20100094551A (ko) 2007-12-06 2010-08-26 인트라-셀룰라 써래피스, 인코퍼레이티드. 유기 화합물
EP2262811B1 (en) 2008-03-04 2016-04-27 Merck Sharp & Dohme Corp. 1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo [4,3-e]-1,2,4-triazolo [4,3-c]pyrimidin-3-one compounds for use as adenosine a2a receptor antagonists
EP2367431B1 (en) 2008-12-06 2015-08-05 Intra-Cellular Therapies, Inc. Organic compounds
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BRPI0922809A2 (pt) 2008-12-06 2018-05-29 Intracellular Therapies Inc compostos orgânicos
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US9434730B2 (en) 2010-05-31 2016-09-06 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
US9371327B2 (en) 2010-05-31 2016-06-21 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
AU2011306358B2 (en) * 2010-09-24 2014-08-14 Impetis Biosciences Ltd. Fused tricyclic compounds as adenosine receptor antagonist
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
US9546175B2 (en) 2014-08-07 2017-01-17 Intra-Cellular Therapies, Inc. Organic compounds
US10472347B2 (en) 2014-11-18 2019-11-12 Merck Sharp & Dohme Corp. Aminopyrazine compounds with A2A antagonist properties
WO2016126570A1 (en) 2015-02-06 2016-08-11 Merck Sharp & Dohme Corp. Aminoquinazoline compounds as a2a antagonist
US10688082B2 (en) 2015-06-11 2020-06-23 Merck Sharp & Dohme Corp. Aminopyrazine compounds with A2A antagonist properties
WO2017008205A1 (en) 2015-07-10 2017-01-19 Merck Sharp & Dohme Corp. Substituted aminoquinazoline compounds as a2a antagonist
EP3723754A4 (en) 2017-12-13 2021-05-19 Merck Sharp & Dohme Corp. IMIDAZO [1,2-C] QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
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
CN111072676B (zh) * 2019-12-12 2021-07-16 广东东阳光药业有限公司 含氮稠合三环衍生物及其用途

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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
WO1995003806A1 (fr) * 1993-07-27 1995-02-09 Kyowa Hakko Kogyo Co., Ltd. Remede contre la maladie de parkinson

Also Published As

Publication number Publication date
PT856003E (pt) 2001-04-30
CA2227991A1 (en) 1997-02-13
ATE198334T1 (de) 2001-01-15
IT1277392B1 (it) 1997-11-10
ITMI951671A1 (it) 1997-01-28
DE69611377T2 (de) 2001-04-26
WO1997005138A1 (en) 1997-02-13
ITMI951671A0 (it) 1995-07-28
DE69611377D1 (de) 2001-02-01
EP0856003B1 (en) 2000-12-27
EP0856003A1 (en) 1998-08-05
GR3035309T3 (en) 2001-04-30
DK0856003T3 (da) 2001-01-22
US5935964A (en) 1999-08-10
CA2227991C (en) 2001-09-11

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