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
Links
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical compound C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 title 1
- 102000009346 Adenosine receptors Human genes 0.000 title 1
- 108050000203 Adenosine receptors Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical group C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 abstract 1
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 1
- -1 NITRO, AMINO Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 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
- C07D487/12—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
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.
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) |
Families Citing this family (51)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1069126B1 (en) * | 1998-04-03 | 2003-05-28 | Otsuka Pharmaceutical Factory, Inc. | Triazolopurine derivatives, medicinal composition containing the derivatives, adenosine a3 receptor compatibilizing agent, and asthmatic remedy |
US6878716B1 (en) | 1998-06-02 | 2005-04-12 | Osi Pharmaceuticals, Inc. | Compounds specific to adenosine A1 receptor and uses thereof |
MXPA00011889A (es) | 1998-06-02 | 2003-04-25 | Osi Pharm Inc | Composiciones de pirrolo (2,3d) piridina y su uso. |
US6686366B1 (en) | 1998-06-02 | 2004-02-03 | Osi Pharmaceuticals, Inc. | Compounds specific to adenosine A3 receptor and uses thereof |
US6921825B2 (en) | 1998-09-16 | 2005-07-26 | King Pharmaceuticuals Research & Development, Inc. | Adenosine A3 receptor modulators |
US6448253B1 (en) * | 1998-09-16 | 2002-09-10 | King Pharmaceuticals Research And Development, Inc. | Adenosine A3 receptor modulators |
KR20020046285A (ko) * | 1999-09-28 | 2002-06-20 | 고마즈 교우이찌 | 트리아조로푸린 유도체,그 유도체를 함유하는 의약 조성물및 아데노신 에이 3 수용체 친화제 |
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 |
CA2459304A1 (en) * | 2001-09-13 | 2003-03-20 | Schering Corporation | Combination of an adenosine a2a receptor antagonist and an antidepressant or anxiolytic |
IL160878A0 (en) | 2001-10-15 | 2004-08-31 | Schering Corp | Imidazo (4,3-e)-1,2,4-triazolo (1,5-c) pyrimidines as adenosine a2a receptor antagonists |
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 |
SG171777A1 (en) | 2008-12-06 | 2011-07-28 | Intra Cellular Therapies Inc | Organic compounds |
BRPI0922809A2 (pt) | 2008-12-06 | 2018-05-29 | Intracellular Therapies Inc | compostos orgânicos |
WO2011101861A1 (en) | 2010-01-29 | 2011-08-25 | Msn Laboratories Limited | Process for preparation of dpp-iv inhibitors |
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 |
Family Cites Families (2)
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 |
WO1995003806A1 (fr) * | 1993-07-27 | 1995-02-09 | Kyowa Hakko Kogyo Co., Ltd. | Remede contre la maladie de parkinson |
-
1995
- 1995-07-28 IT IT95MI001671A patent/IT1277392B1/it active IP Right Grant
-
1996
- 1996-07-02 DE DE69611377T patent/DE69611377T2/de not_active Expired - Fee Related
- 1996-07-02 PT PT96924840T patent/PT856003E/pt unknown
- 1996-07-02 DK DK96924840T patent/DK0856003T3/da active
- 1996-07-02 WO PCT/EP1996/002881 patent/WO1997005138A1/en active IP Right Grant
- 1996-07-02 CA CA002227991A patent/CA2227991C/en not_active Expired - Fee Related
- 1996-07-02 US US09/006,698 patent/US5935964A/en not_active Expired - Fee Related
- 1996-07-02 ES ES96924840T patent/ES2153118T3/es not_active Expired - Lifetime
- 1996-07-02 EP EP96924840A patent/EP0856003B1/en not_active Expired - Lifetime
- 1996-07-02 AT AT96924840T patent/ATE198334T1/de not_active IP Right Cessation
-
2001
- 2001-01-26 GR GR20010400134T patent/GR3035309T3/el not_active IP Right Cessation
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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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG2A | Definitive protection |
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