IT1264901B1 - HETEROCYCLIC ANALOGUES OF 1,2,4-TRIAZOLE(15-C)PYRIMIDINES WITH ANTAGONIST ACTIVITY FOR THE ADENOSINE A2 RECEPTOR - Google Patents
HETEROCYCLIC ANALOGUES OF 1,2,4-TRIAZOLE(15-C)PYRIMIDINES WITH ANTAGONIST ACTIVITY FOR THE ADENOSINE A2 RECEPTORInfo
- Publication number
- IT1264901B1 IT1264901B1 IT93MI001396A ITMI931396A IT1264901B1 IT 1264901 B1 IT1264901 B1 IT 1264901B1 IT 93MI001396 A IT93MI001396 A IT 93MI001396A IT MI931396 A ITMI931396 A IT MI931396A IT 1264901 B1 IT1264901 B1 IT 1264901B1
- Authority
- IT
- Italy
- Prior art keywords
- adenosine
- receptor
- pyrimidines
- triazole
- antagonist activity
- Prior art date
Links
- 102000000506 Adenosine A2 Receptors Human genes 0.000 title abstract 2
- 108010041368 Adenosine A2 Receptors Proteins 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title abstract 2
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical class C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 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
I composti di formula I, dove R e A hanno i significati dati nella descrizione, sono dotati di selettiva attività antagonista sul recettore A2 dell'adenosina.The compounds of formula I, where R and A have the meanings given in the description, are endowed with selective antagonist activity on the adenosine A2 receptor.
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT93MI001396A IT1264901B1 (en) | 1993-06-29 | 1993-06-29 | HETEROCYCLIC ANALOGUES OF 1,2,4-TRIAZOLE(15-C)PYRIMIDINES WITH ANTAGONIST ACTIVITY FOR THE ADENOSINE A2 RECEPTOR |
AU70723/94A AU7072394A (en) | 1993-06-29 | 1994-06-22 | 1,2,4-triazolo(1,5-c)pyrimidine heterocyclic analogues having antagonistic activity on adenosine a2 receptor |
PCT/EP1994/002031 WO1995001356A1 (en) | 1993-06-29 | 1994-06-22 | 1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE HETEROCYCLIC ANALOGUES HAVING ANTAGONISTIC ACTIVITY ON ADENOSINE A2 RECEPTOR |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT93MI001396A IT1264901B1 (en) | 1993-06-29 | 1993-06-29 | HETEROCYCLIC ANALOGUES OF 1,2,4-TRIAZOLE(15-C)PYRIMIDINES WITH ANTAGONIST ACTIVITY FOR THE ADENOSINE A2 RECEPTOR |
Publications (3)
Publication Number | Publication Date |
---|---|
ITMI931396A0 ITMI931396A0 (en) | 1993-06-29 |
ITMI931396A1 ITMI931396A1 (en) | 1994-12-29 |
IT1264901B1 true IT1264901B1 (en) | 1996-10-17 |
Family
ID=11366495
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IT93MI001396A IT1264901B1 (en) | 1993-06-29 | 1993-06-29 | HETEROCYCLIC ANALOGUES OF 1,2,4-TRIAZOLE(15-C)PYRIMIDINES WITH ANTAGONIST ACTIVITY FOR THE ADENOSINE A2 RECEPTOR |
Country Status (3)
Country | Link |
---|---|
AU (1) | AU7072394A (en) |
IT (1) | IT1264901B1 (en) |
WO (1) | WO1995001356A1 (en) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IT1277392B1 (en) * | 1995-07-28 | 1997-11-10 | Schering Plough S P A | HEROCYCLIC ANALOGS OF 1,2,4-TRIAZOLE (1,5-C] PYRIMIDINE WITH ANTAGONIST ACTIVITY FOR THE A2A RECEPTOR OF ADENOSINE |
DE19629378A1 (en) * | 1996-07-20 | 1998-01-29 | Boehringer Ingelheim Kg | New triazolopurines, process for their preparation and their use as medicaments |
US6448253B1 (en) * | 1998-09-16 | 2002-09-10 | King Pharmaceuticals Research And Development, Inc. | Adenosine A3 receptor modulators |
US6921825B2 (en) | 1998-09-16 | 2005-07-26 | King Pharmaceuticuals Research & Development, Inc. | Adenosine A3 receptor modulators |
AU4343500A (en) | 1999-04-16 | 2000-11-02 | Schering Corporation | Use of azetidinone compounds |
CZ303790B6 (en) | 2000-05-26 | 2013-05-09 | Merck Sharp & Dohme Corp. | Pyrimidine derivatives, process of their preparation and pharmaceutical preparation containing them |
WO2003028732A1 (en) * | 2001-09-28 | 2003-04-10 | Kyowa Hakko Kogyo Co., Ltd. | Receptor antagonist |
WO2003032996A1 (en) * | 2001-10-15 | 2003-04-24 | Schering Corporation | Imidazo (4,3-e)-1,2,4-triazolo(1,5-c) pyrimidines as adenosine a2a receptor antagonists |
CN1692116A (en) | 2001-11-30 | 2005-11-02 | 先灵公司 | Adenosine A2A receptor antagonists |
TW200300686A (en) | 2001-11-30 | 2003-06-16 | Schering Corp | Adenosine A2a receptor antagonists |
JP4429724B2 (en) | 2001-11-30 | 2010-03-10 | シェーリング コーポレイション | [1,2,4] -Triazole bicyclic adenosine A2a receptor antagonist |
EP1549319A2 (en) * | 2002-05-30 | 2005-07-06 | King Pharmaceuticals Research and Development Inc. | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
ES2354875T3 (en) | 2002-12-19 | 2011-03-18 | Schering Corporation | USE OF ADENOSINE A2A RECEIVER ANTAGONISTS FOR THE TREATMENT OR PREVENTION OF EXTRAPIRAMIDAL SYNDROME. |
PE20050141A1 (en) | 2003-04-23 | 2005-04-01 | Schering Corp | DERIVATIVES OF 2-ALKINYL-AND 2-ALKENYL-PIRAZOLO- [4,3-e] -1,2,4-TRIAZOLO- [1,5-c] -PYRIDINE AS ANTAGONISTS OF THE A2a ADENOSINE RECEPTOR |
SI1678182T1 (en) | 2003-10-28 | 2007-06-30 | Schering Corp | PROCESS FOR PREPARING SUBSTITUTED 5-AMINO-PYRAZOLO- ?á4,3-E?å-1,2,4-TRIAZOLO ?á1,5-C?åPYRIMIDINES |
JP2007513091A (en) | 2003-12-01 | 2007-05-24 | シェーリング コーポレイション | Process for the preparation of substituted 5-amino-pyrazolo- [4,3-e] -1,2,4-triazolo [1,5-c] pyrimidines |
DE602005020127D1 (en) | 2004-04-21 | 2010-05-06 | Schering Corp | PYRAZOLOÄ4,3-EÜ-1,2,4-TRIAZOLOÄ1,5-CÜPYRIMIDINE AS ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR |
US7465740B2 (en) | 2005-09-19 | 2008-12-16 | Schering Corporation | 2-heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists |
PE20070521A1 (en) | 2005-09-23 | 2007-07-13 | Schering Corp | 7- [2- [4- (6-FLUORO-3-METHYL-1,2-BENZYSOXAZOL-5-IL) -1-PIPERAZINYL] ETHYL] -2- (1-PROPINYL) -7H-PIRAZOLE- [4, 3-E] - [1,2,4] -TRIAZOL- [1,5-C] -PYRIMIDIN-5-AMINE AS ANTAGONIST OF THE ADENOSINE A2a RECEPTOR |
ES2273599B1 (en) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | COMPOUNDS FOR THE TREATMENT OF HEADPHONE FIBRILATION. |
US7691869B2 (en) | 2007-03-30 | 2010-04-06 | King Pharmaceuticals Research And Development, Inc. | Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity |
AU2009222047A1 (en) | 2008-03-04 | 2009-09-11 | Schering Corporation | 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 |
CA2812378C (en) * | 2010-09-24 | 2016-11-29 | Advinus Therapeutics Limited | 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 |
EP3220910B1 (en) | 2014-11-18 | 2020-01-15 | Merck Sharp & Dohme Corp. | Aminopyrazine compounds with a2a antagonist properties |
US10138212B2 (en) | 2015-02-06 | 2018-11-27 | Merck Sharp & Dohme Corp. | Aminoquinazoline compounds as A2A antagonist |
EP3307067B1 (en) | 2015-06-11 | 2022-11-02 | Merck Sharp & Dohme LLC | Aminopyrazine compounds with a2a antagonist properties |
WO2017008205A1 (en) | 2015-07-10 | 2017-01-19 | Merck Sharp & Dohme Corp. | Substituted aminoquinazoline compounds as a2a antagonist |
US11498923B2 (en) | 2017-12-13 | 2022-11-15 | Merck Sharp & Dohme Llc | Substituted imidazo[1,2-c]quinazolines as A2A antagonists |
CN108864114B (en) | 2018-06-04 | 2020-11-06 | 应世生物科技(南京)有限公司 | Selectivity A2AReceptor antagonists |
DE102019116986A1 (en) | 2019-06-24 | 2020-12-24 | Helmholtz-Zentrum Dresden-Rossendorf E. V. | Deuterated 7- (3- (4- (2 - ([18F] fluoro) ethoxy) phenyl) propyl) -2- (furan-2-yl) -7H-pyrazolo [4,3-e] [1,2, 4] triazolo [1,5-c] pyrimidin-5-amine derivatives |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4713383A (en) * | 1984-10-01 | 1987-12-15 | Ciba-Geigy Corporation | Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses |
EP0217748B1 (en) * | 1985-09-30 | 1991-02-06 | Ciba-Geigy Ag | 2-Substituted-e-fused-[1,2,4,]triazolo-[1,5-c]pyrimidines pharmaceutical compositions and uses thereof |
WO1988002370A1 (en) * | 1986-09-30 | 1988-04-07 | Ciba-Geigy Ag | 2-substituted-e-fused-[1,2,4]triazolo[1,5-c]pyrimidines pharmaceutical compositions and uses thereof |
-
1993
- 1993-06-29 IT IT93MI001396A patent/IT1264901B1/en active IP Right Grant
-
1994
- 1994-06-22 AU AU70723/94A patent/AU7072394A/en not_active Abandoned
- 1994-06-22 WO PCT/EP1994/002031 patent/WO1995001356A1/en active Application Filing
Also Published As
Publication number | Publication date |
---|---|
AU7072394A (en) | 1995-01-24 |
WO1995001356A1 (en) | 1995-01-12 |
ITMI931396A1 (en) | 1994-12-29 |
ITMI931396A0 (en) | 1993-06-29 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
0001 | Granted | ||
TA | Fee payment date (situation as of event date), data collected since 19931001 |
Effective date: 19970530 |