BRPI0111015B8 - composto antagonista de receptor a2a de adenosina, composição farmacêutica compreendendo o mesmo, seu uso e processos para a preparação de compostos intermediários - Google Patents
composto antagonista de receptor a2a de adenosina, composição farmacêutica compreendendo o mesmo, seu uso e processos para a preparação de compostos intermediáriosInfo
- Publication number
- BRPI0111015B8 BRPI0111015B8 BRPI0111015A BRPI0111015B8 BR PI0111015 B8 BRPI0111015 B8 BR PI0111015B8 BR PI0111015 A BRPI0111015 A BR PI0111015A BR PI0111015 B8 BRPI0111015 B8 BR PI0111015B8
- Authority
- BR
- Brazil
- Prior art keywords
- adenosine
- processes
- optionally substituted
- phenyl
- same
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229940123702 Adenosine A2a receptor antagonist Drugs 0.000 title 1
- 239000002467 adenosine A2a receptor antagonist Substances 0.000 title 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 208000018737 Parkinson disease Diseases 0.000 abstract 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical class [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 229960005305 adenosine Drugs 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 229910052799 carbon Chemical class 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 150000002829 nitrogen Chemical class 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 150000003839 salts 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
-
- 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
- A61P25/24—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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20714300P | 2000-05-26 | 2000-05-26 | |
| US60/207,143 | 2000-05-26 | ||
| PCT/US2001/016954 WO2001092264A1 (en) | 2000-05-26 | 2001-05-24 | Adenosine a2a receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BR0111015A BR0111015A (pt) | 2005-01-11 |
| BRPI0111015B1 BRPI0111015B1 (pt) | 2017-11-07 |
| BRPI0111015B8 true BRPI0111015B8 (pt) | 2021-05-25 |
Family
ID=22769372
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0111015-2 BRPI0111015B8 (pt) | 2000-05-26 | 2001-05-24 | composto antagonista de receptor a2a de adenosina, composição farmacêutica compreendendo o mesmo, seu uso e processos para a preparação de compostos intermediários |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US6630475B2 (enExample) |
| EP (1) | EP1283839B1 (enExample) |
| JP (3) | JP4574112B2 (enExample) |
| KR (1) | KR100520907B1 (enExample) |
| CN (2) | CN100384847C (enExample) |
| AR (1) | AR028621A1 (enExample) |
| AT (1) | ATE293627T1 (enExample) |
| AU (2) | AU2001268089C1 (enExample) |
| BR (1) | BRPI0111015B8 (enExample) |
| CA (1) | CA2410237C (enExample) |
| CZ (1) | CZ303790B6 (enExample) |
| DE (1) | DE60110219T2 (enExample) |
| DK (1) | DK1283839T3 (enExample) |
| EC (1) | ECSP024364A (enExample) |
| ES (1) | ES2237576T3 (enExample) |
| HK (1) | HK1049007B (enExample) |
| HU (1) | HU230420B1 (enExample) |
| IL (3) | IL152726A0 (enExample) |
| MX (1) | MXPA02011625A (enExample) |
| MY (1) | MY132006A (enExample) |
| NO (1) | NO325008B1 (enExample) |
| NZ (1) | NZ522326A (enExample) |
| PE (1) | PE20020062A1 (enExample) |
| PL (1) | PL218764B1 (enExample) |
| PT (1) | PT1283839E (enExample) |
| RU (1) | RU2315053C2 (enExample) |
| SI (1) | SI1283839T1 (enExample) |
| SK (1) | SK287748B6 (enExample) |
| TW (1) | TWI288137B (enExample) |
| WO (1) | WO2001092264A1 (enExample) |
| ZA (1) | ZA200208898B (enExample) |
Families Citing this family (89)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1283839E (pt) * | 2000-05-26 | 2005-08-31 | Schering Corp | Antagonistas do receptor a2a da adenosina |
| EP1425017A1 (en) * | 2001-09-13 | 2004-06-09 | Schering Corporation | Combination of an adenosine a2a receptor antagonist and an antidepressant or anxiolytic |
| JP4545437B2 (ja) | 2001-10-15 | 2010-09-15 | シェーリング コーポレイション | アデノシンａ２ａ受容体アンタゴニストとしてのイミダゾ（４，３−ｅ）−１，２，４−トリアゾロ（１，５−ｃ）ピリミジン |
| FR2832405B1 (fr) * | 2001-11-19 | 2004-12-10 | Sanofi Synthelabo | Tetrahydropyridyl-alkyl-heterocycles azotes, procede pour leur preparation et compositions pharmaceutiques les contenant |
| AU2002346503A1 (en) * | 2001-11-30 | 2003-06-17 | Schering Corporation | Adenosine A2a receptor antagonists |
| CA2468658C (en) | 2001-11-30 | 2009-04-14 | Schering Corporation | [1,2,4]-triazole bicyclic adenosine a2a receptor antagonists |
| TW200300686A (en) | 2001-11-30 | 2003-06-16 | Schering Corp | Adenosine A2a receptor antagonists |
| ES2716404T3 (es) | 2002-01-28 | 2019-06-12 | Kyowa Hakko Kogyo Kk | Antagonistas de receptores A2A para su uso en el tratamiento de trastornos del movimiento |
| MXPA04000908A (es) * | 2002-05-30 | 2004-03-26 | King Pharmaceuticals Res & Dev | Compuestos farmaceuticamente activos que tienen estructura de anillo de pirazolotriazolopirimidina triciclica y metodos de uso. |
| MXPA05006790A (es) * | 2002-12-19 | 2005-09-08 | Schering Corp | Usos de antagonistas del receptor adenosina a2a. |
| 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 |
| EP1618109A2 (en) | 2003-04-09 | 2006-01-25 | Biogen Idec MA Inc. | Triazolo[1,5-c]pyrimidines and pyrazolo[1,5-c]pyrimidines useful as a2a adenosine receptor antagonists |
| EP1622912B1 (en) * | 2003-04-23 | 2009-05-27 | Schering Corporation | 2-alkynyl-and 2-alkenyl-pyrazolo- [4,3-e ] -1,2,4-triazolo- [1,5-c] -pyrimidine adenosine a2a receptor antagonists |
| EA200501924A1 (ru) * | 2003-06-10 | 2006-06-30 | Киова Хакко Когио Ко., Лтд. | Способ лечения тревожного расстройства |
| JP2006527212A (ja) * | 2003-06-12 | 2006-11-30 | ノボ ノルディスク アクティーゼルスカブ | ホルモン感受性リパーゼの阻害剤として使用するための、置換ピペラジンカルバメート |
| US7816353B2 (en) * | 2003-10-24 | 2010-10-19 | Exelixis, Inc. | P70S6 kinase modulators and method of use |
| DK1678182T3 (da) | 2003-10-28 | 2007-06-04 | Schering Corp | Fremgangsmåde til fremstilling af substituerede 5-amino-pyrazolo[4,3-E]-1,2,4-triazolo-[1,5-C]pyrimidiner |
| ATE377599T1 (de) * | 2003-12-01 | 2007-11-15 | Schering Corp | Verfahren zur herstellung von substituierten 5- aminopyrazolo(4,3-e)-1,2,4-triazolo(1,5- c)pyrimidinen |
| CA2550071A1 (en) * | 2003-12-19 | 2005-07-07 | Schering Corporation | Pharmaceutical compositions |
| ATE461932T1 (de) * | 2004-04-21 | 2010-04-15 | Schering Corp | Pyrazoloä4,3-eü-1,2,4-triazoloä1,5-cüpyrimidine als antagonisten des adenosin-a2a-rezeptors |
| JPWO2006132275A1 (ja) * | 2005-06-07 | 2009-01-08 | 協和醗酵工業株式会社 | 運動障害の予防および／または治療剤 |
| AR057817A1 (es) * | 2005-09-19 | 2007-12-19 | Schering Corp | Antagonistas del receptor a2a de 2-heteroaril-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidin adenosina. composiciones farmaceuticas |
| AR056080A1 (es) * | 2005-09-23 | 2007-09-19 | Schering Corp | 7-[2-[4-(6-fluoro-3-metil-1,2-benciosoxazol-5-il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c] -pirimidin-5-amine |
| ES2273599B1 (es) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | Compuestos para el tratamiento de la fibrilacion auricular. |
| EP2040698A4 (en) * | 2006-07-14 | 2011-08-10 | Shionogi & Co | OXIM CONNECTIONS AND ITS USE |
| TW200840566A (en) * | 2006-12-22 | 2008-10-16 | Esteve Labor Dr | Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments |
| 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 |
| WO2009110955A2 (en) * | 2008-02-29 | 2009-09-11 | Albert Einstein College Of Medicine Of Yeshiva University | Ketoconazole-derivative antagonists of human pregnane x receptor and uses thereof |
| JP2011513417A (ja) | 2008-03-04 | 2011-04-28 | シェーリング コーポレイション | アデノシンＡ２ａ受容体アンタゴニストとして使用するための１，２，４−トリアゾロ［４，３−ｃ］ピリミジン−３−オンおよびピラゾロ［４，３−ｅ］−１，２，４−トリアゾロ［４，３−ｃ］ピリミジン−３−オン化合物 |
| US20110064671A1 (en) | 2008-03-10 | 2011-03-17 | Cornell University | Modulation of blood brain barrier permeability |
| TWI473614B (zh) * | 2008-05-29 | 2015-02-21 | Kyowa Hakko Kirin Co Ltd | Anti-analgesic inhibitors |
| NZ590793A (en) * | 2008-07-23 | 2012-07-27 | Kyowa Hakko Kirin Co Ltd | Therapeutic agent for migraine |
| US20100093702A1 (en) * | 2008-10-13 | 2010-04-15 | Barbay J Kent | METHYLENE AMINES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| TW201036614A (en) | 2008-12-30 | 2010-10-16 | Arqule Inc | Substituted 1H-pyrazolo[3,4-d]pyrimidine-6-amine compounds |
| AU2010207004A1 (en) | 2009-01-20 | 2011-07-28 | Merck Sharp & Dohme Corp. | Methods of alleviating or treating signs and/or symptoms associated with moderate to severe Parkinson's disease |
| US8993808B2 (en) | 2009-01-21 | 2015-03-31 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
| BRPI1009398A2 (pt) | 2009-03-13 | 2016-03-08 | Advinus Therapeutics Private Ltd | compostos de pirimidina fundida substituída |
| EP2414361A1 (en) | 2009-03-31 | 2012-02-08 | ArQule, Inc. | Substituted heterocyclic compounds |
| WO2010147941A1 (en) | 2009-06-15 | 2010-12-23 | Marvell World Trade Ltd. | System and methods for gamut bounded saturation adaptive color enhancement |
| EP2462144B1 (en) | 2009-08-07 | 2017-09-20 | Merck Sharp & Dohme Corp. | PROCESS FOR PREPARING A 2-ALKYNYL SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE |
| WO2011035941A1 (en) | 2009-09-25 | 2011-03-31 | Oryzon Genomics S.A. | Lysine specific demethylase-1 inhibitors and their use |
| US8946296B2 (en) | 2009-10-09 | 2015-02-03 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use |
| WO2011101861A1 (en) | 2010-01-29 | 2011-08-25 | Msn Laboratories Limited | Process for preparation of dpp-iv inhibitors |
| WO2011106106A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| WO2011106574A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
| RS55348B1 (sr) | 2010-04-19 | 2017-03-31 | Oryzon Gnomics S A | Inhibitori lizin specifične demetilaze-1 i njihova upotreba |
| DK2598482T3 (en) | 2010-07-29 | 2018-06-14 | Oryzon Genomics Sa | ARYLCYCLOPROPYLAMINE-BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE |
| EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| CN103261202B (zh) * | 2010-09-24 | 2016-01-20 | 阿迪维纳斯疗法有限公司 | 作为腺苷受体拮抗剂的稠合三环化合物 |
| WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| EP2712315B1 (en) | 2011-02-08 | 2021-11-24 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| WO2012129381A1 (en) * | 2011-03-22 | 2012-09-27 | Concert Pharmaceuticals Inc. | Deuterated preladenant |
| WO2012127472A1 (en) * | 2011-03-22 | 2012-09-27 | Mapi Pharma Ltd. | Process and intermediates for the preparation of preladenant and related compounds |
| WO2013024474A1 (en) * | 2011-08-18 | 2013-02-21 | Mapi Phrarma Ltd. | Polymorphs of preladenant |
| US9469597B2 (en) | 2011-10-20 | 2016-10-18 | Oryzon Genomics S.A. | (Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors |
| AU2012324803B9 (en) | 2011-10-20 | 2017-08-24 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as LSD1 inhibitors |
| WO2014071512A1 (en) * | 2012-11-06 | 2014-05-15 | Universite Laval | Combination therapy and methods for the treatment of respiratory diseases |
| 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 |
| AU2015350315B2 (en) | 2014-11-18 | 2020-06-25 | 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 |
| 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 |
| US9687475B1 (en) | 2016-03-24 | 2017-06-27 | Ezra Pharma Llc | Extended release pharmaceutical formulations with controlled impurity levels |
| US9675585B1 (en) | 2016-03-24 | 2017-06-13 | Ezra Pharma | Extended release pharmaceutical formulations |
| TWI801372B (zh) * | 2017-03-30 | 2023-05-11 | 比利時商艾特歐斯比利時有限公司 | 作為a2a抑制劑的硫胺甲酸酯衍生物以及用於癌症治療的方法 |
| AU2018246355B2 (en) * | 2017-03-30 | 2021-12-09 | iTeos Belgium SA | 2-oxo-thiazole derivatives as A2A inhibitors and compounds for use in the treatment of cancers |
| US11498923B2 (en) | 2017-12-13 | 2022-11-15 | Merck Sharp & Dohme Llc | Substituted imidazo[1,2-c]quinazolines as A2A antagonists |
| AU2019205661B2 (en) | 2018-01-04 | 2022-06-30 | Impetis Biosciences Ltd. | Tricyclic compounds, compositions and medicinal applications thereof |
| AU2019227607C1 (en) | 2018-02-27 | 2023-07-20 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors |
| CN108276345A (zh) * | 2018-03-22 | 2018-07-13 | 重庆奥舍生物化工有限公司 | 一种药物中间体嘧啶-5-甲醛的制备方法 |
| KR20200140849A (ko) * | 2018-04-08 | 2020-12-16 | 베이진 엘티디 | A2a 수용체 길항제로서의 피라졸로트리아졸로피리미딘 유도체 |
| EP3810610A1 (en) | 2018-05-18 | 2021-04-28 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| CN108864114B (zh) | 2018-06-04 | 2020-11-06 | 应世生物科技(南京)有限公司 | 选择性a2a受体拮抗剂 |
| CN117304191A (zh) | 2018-07-05 | 2023-12-29 | 因赛特公司 | 作为a2a/a2b抑制剂的稠合吡嗪衍生物 |
| CN110742893B (zh) * | 2018-07-23 | 2024-04-05 | 百济神州(北京)生物科技有限公司 | A2a受体拮抗剂治疗癌症的方法 |
| AR117164A1 (es) | 2018-11-30 | 2021-07-14 | Merck Sharp & Dohme | Derivados de amino-triazoloquinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmacéuticas y su uso para el tratamiento de diversos tipos de cáncer |
| JP7414827B2 (ja) | 2018-12-20 | 2024-01-16 | インサイト・コーポレイション | アクチビン受容体様キナーゼ－２の阻害剤としてのイミダゾピリダジン及びイミダゾピリジン化合物 |
| 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 |
| US12325708B2 (en) | 2019-05-03 | 2025-06-10 | Nektar Therapeutics | Adenosine 2 receptor antagonists |
| 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 |
| WO2021011670A1 (en) * | 2019-07-17 | 2021-01-21 | Teon Therapeutics, Inc. | Adenosine a2a receptor antagonists and uses thereof |
| CN112592354B (zh) | 2019-07-30 | 2022-05-27 | 厦门宝太生物科技股份有限公司 | 一种异噁唑并嘧啶类杂环化合物的制备方法 |
| CN112608316B (zh) | 2019-07-30 | 2022-10-21 | 厦门宝太生物科技股份有限公司 | 一种吡唑并三嗪类腺苷受体拮抗剂 |
| CN111072675A (zh) * | 2019-12-12 | 2020-04-28 | 广东东阳光药业有限公司 | 含氮稠合三环衍生物及其用途 |
| CN113773327B (zh) * | 2021-09-13 | 2022-07-15 | 八叶草健康产业研究院(厦门)有限公司 | 一种吡唑并嘧啶并三唑环类化合物的制备方法 |
| CN117946123B (zh) * | 2024-01-26 | 2026-06-30 | 北京脑重大疾病研究院 | 放射性三氮唑并嘧啶基衍生物及其制备方法和应用 |
| CN118812544B (zh) * | 2024-06-19 | 2026-06-16 | 厦门大学 | 一种腺苷a2ar靶向小分子化合物、核素标记探针及其制备方法、应用和药物组合物 |
| CN118812539B (zh) * | 2024-06-19 | 2025-11-28 | 苏州大学 | 一种5-氨基三唑并嘧啶衍生物及其制备方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3677445D1 (de) | 1985-09-30 | 1991-03-14 | Ciba Geigy Ag | 2-substituierte-e-kondensierte(1,5-c)-pyrimidine, pharmazeutische zubereitungen und ihre verwendung. |
| SU1739850A3 (ru) * | 1987-08-31 | 1992-06-07 | Такеда Кемикал Индастриз, Лтд (Фирма) | Способ получени конденсированных производных пиразоло[3,4- @ ]пиримидина |
| 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 |
| US5565460A (en) | 1993-07-27 | 1996-10-15 | Kyowa Hakko Koygo Co., Ltd. | Therapeutic purine agents for parkinson's disease |
| 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 |
| 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 |
| PT1283839E (pt) * | 2000-05-26 | 2005-08-31 | Schering Corp | Antagonistas do receptor a2a da adenosina |
| AU2002346503A1 (en) * | 2001-11-30 | 2003-06-17 | Schering Corporation | Adenosine A2a receptor antagonists |
| MXPA05006790A (es) * | 2002-12-19 | 2005-09-08 | Schering Corp | Usos de antagonistas del receptor adenosina a2a. |
| DK1678182T3 (da) * | 2003-10-28 | 2007-06-04 | Schering Corp | Fremgangsmåde til fremstilling af substituerede 5-amino-pyrazolo[4,3-E]-1,2,4-triazolo-[1,5-C]pyrimidiner |
| ATE377599T1 (de) * | 2003-12-01 | 2007-11-15 | Schering Corp | Verfahren zur herstellung von substituierten 5- aminopyrazolo(4,3-e)-1,2,4-triazolo(1,5- c)pyrimidinen |
| ATE461932T1 (de) * | 2004-04-21 | 2010-04-15 | Schering Corp | Pyrazoloä4,3-eü-1,2,4-triazoloä1,5-cüpyrimidine als antagonisten des adenosin-a2a-rezeptors |
| AR057817A1 (es) * | 2005-09-19 | 2007-12-19 | Schering Corp | Antagonistas del receptor a2a de 2-heteroaril-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidin adenosina. composiciones farmaceuticas |
-
2001
- 2001-05-24 PT PT01945991T patent/PT1283839E/pt unknown
- 2001-05-24 AT AT01945991T patent/ATE293627T1/de active
- 2001-05-24 ES ES01945991T patent/ES2237576T3/es not_active Expired - Lifetime
- 2001-05-24 CN CNB2006100049297A patent/CN100384847C/zh not_active Expired - Lifetime
- 2001-05-24 AR ARP010102483A patent/AR028621A1/es active IP Right Grant
- 2001-05-24 KR KR10-2002-7015699A patent/KR100520907B1/ko not_active Expired - Lifetime
- 2001-05-24 EP EP01945991A patent/EP1283839B1/en not_active Expired - Lifetime
- 2001-05-24 BR BRPI0111015-2 patent/BRPI0111015B8/pt not_active IP Right Cessation
- 2001-05-24 WO PCT/US2001/016954 patent/WO2001092264A1/en not_active Ceased
- 2001-05-24 AU AU2001268089A patent/AU2001268089C1/en not_active Expired
- 2001-05-24 NZ NZ522326A patent/NZ522326A/xx not_active IP Right Cessation
- 2001-05-24 SK SK1671-2002A patent/SK287748B6/sk not_active IP Right Cessation
- 2001-05-24 TW TW090112461A patent/TWI288137B/zh not_active IP Right Cessation
- 2001-05-24 JP JP2002500877A patent/JP4574112B2/ja not_active Expired - Lifetime
- 2001-05-24 IL IL15272601A patent/IL152726A0/xx unknown
- 2001-05-24 HK HK03101315.3A patent/HK1049007B/en not_active IP Right Cessation
- 2001-05-24 DK DK01945991T patent/DK1283839T3/da active
- 2001-05-24 MX MXPA02011625A patent/MXPA02011625A/es active IP Right Grant
- 2001-05-24 AU AU6808901A patent/AU6808901A/xx active Pending
- 2001-05-24 PE PE2001000475A patent/PE20020062A1/es active IP Right Grant
- 2001-05-24 CN CNB018134491A patent/CN1247588C/zh not_active Expired - Lifetime
- 2001-05-24 HU HU0600239A patent/HU230420B1/hu unknown
- 2001-05-24 MY MYPI20012466A patent/MY132006A/en unknown
- 2001-05-24 US US09/865,071 patent/US6630475B2/en not_active Ceased
- 2001-05-24 CA CA002410237A patent/CA2410237C/en not_active Expired - Lifetime
- 2001-05-24 PL PL360472A patent/PL218764B1/pl unknown
- 2001-05-24 DE DE60110219T patent/DE60110219T2/de not_active Expired - Lifetime
- 2001-05-24 CZ CZ20023886A patent/CZ303790B6/cs not_active IP Right Cessation
- 2001-05-24 RU RU2002135620/04A patent/RU2315053C2/ru active
- 2001-05-24 SI SI200130336T patent/SI1283839T1/xx unknown
-
2002
- 2002-11-01 ZA ZA200208898A patent/ZA200208898B/en unknown
- 2002-11-10 IL IL152726A patent/IL152726A/en active IP Right Grant
- 2002-11-25 NO NO20025651A patent/NO325008B1/no not_active IP Right Cessation
- 2002-11-25 EC EC2002004364A patent/ECSP024364A/es unknown
-
2003
- 2003-05-30 US US10/448,854 patent/US6897216B2/en not_active Expired - Lifetime
-
2004
- 2004-08-06 US US10/912,834 patent/US7067655B2/en not_active Expired - Lifetime
-
2006
- 2006-05-02 JP JP2006128415A patent/JP4938348B2/ja not_active Expired - Lifetime
-
2007
- 2007-03-16 JP JP2007069618A patent/JP2007145875A/ja not_active Withdrawn
-
2012
- 2012-04-06 US US13/441,140 patent/USRE44205E1/en not_active Expired - Lifetime
- 2012-06-04 IL IL220174A patent/IL220174A/en active IP Right Grant
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BR0111015A (pt) | Antagonistas de receptor a2a de adenosina | |
| BR0010060A (pt) | Esteróides 3<244>-hidroxi-3<225>-metoximetil-21-heterocìclo substituìdos com atividade anestésica | |
| BRPI0215312B8 (pt) | composto, uso de um composto, composição farmacêutica, e processo para a preparação de um composto | |
| BR9814747A (pt) | Derivados pleuromutilina atuando comoantimicrobianos | |
| BR0317524A (pt) | Compostos derivados de pirrolopirimidina, composição farmacêutica, processo para as suas preparações e respectivo uso | |
| AR025756A1 (es) | Un compuesto de acido sustituido, composiciones y combinaciones farmaceuticas que lo comprenden y su uso para la preparacion de medicamentos | |
| BR9911482A (pt) | Composto, composição farmacêutica, uso do composto, e, processos para o tratamento ou profilaxia de doenças inflamatórias, e para a preparação de um composto | |
| TR200100241T2 (tr) | Nosiseptin reseptörü ORL-1 için yüksek çekim gücü olan ligandlar | |
| BR0209939A (pt) | Composto ou seu sal, éster ou prodroga farmaceuticamente aceitável, formulação farmacêutica, uso do composto ou de seu sal, éster ou prodroga farmaceuticamente aceitável, e, método para tratar câncer | |
| BG107171A (bg) | Производни на пурин | |
| BR0110521A (pt) | Carbamatos azabicìclicos e seu uso como agonistas de receptores de alfa-7 acetilcolina nicotìnico | |
| DK2041133T3 (da) | Derivater af imadazol [1,2-A] pyridine-2-carboxamider, fremstilling deraf og anvendelse deraf i terapeutik | |
| BR0102083A (pt) | Uso de derivados de alfa-cetoenamina como ingredientes | |
| BR0316948A (pt) | Composto, formulação farmacêutica, e, uso de um composto | |
| LT2001119A (en) | Pharmaceutical formulations comprising intranasal morphine and use thereof | |
| ES2149305T3 (es) | Compuestos de dibenzoxazepina sustituidos, composiciones farmaceuticas y procedimientos de uso. | |
| BR0315777A (pt) | Uso de derivados de piperazina como antagonistas ccr1 | |
| BRPI0511532A (pt) | composto, uso do mesmo, composição farmacêutica, e, métodos para a terapia de distúrbios gastrointestinais funcionais e de sìndrome do intestino irritável em um animal de sangue quente, e para a preparação de um composto | |
| BR0116481A (pt) | Compostos de heterociclilalquilindol ou azaindol como ligandos de 5-hidroxitriptamina-6 | |
| IL195818A0 (en) | Derivatives of 2-benzoyl-imidazopyridines, preparation ,method thereof and use of same in therapeutics | |
| GEP20094697B (en) | Condensed purine derivatives as a1 adenosine receptor antagonists | |
| BR0315958A (pt) | Composto, composição farmacêutica, processo para a preparação de um composto, novos intermediários e uso do composto | |
| BR0016217A (pt) | Composto, processo para prepará-lo, composição farmacêutica, e, uso do composto | |
| BRPI0012475A (pt) | composto derivado de titânio, seu processo de preparação e utilização, bem como composição para uso oral compreendendo o mesmo. | |
| BR0213907A (pt) | Derivados de heteroarila como ligandos superiores para receptor de nociceptina orl-1 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B25D | Requested change of name of applicant approved |
Owner name: MERCK SHARP AND DOHME CORP. (US) |
|
| B25G | Requested change of headquarter approved |
Owner name: MERCK SHARP AND DOHME CORP. (US) |
|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 12A ANUIDADE |
|
| B08G | Application fees: restoration [chapter 8.7 patent gazette] | ||
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 07/11/2017, OBSERVADAS AS CONDICOES LEGAIS. |
|
| B16C | Correction of notification of the grant [chapter 16.3 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 24/05/2001 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF |
|
| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 22A ANUIDADE. |
|
| B21H | Decision of lapse of a patent or of a certificate of addition of invention cancelled [chapter 21.8 patent gazette] |
Free format text: ANULADA A PUBLICACAO CODIGO 21.6 NA RPI NO 2724 DE 21/03/2023 POR TER SIDO INDEVIDA. |
|
| B21A | Patent or certificate of addition expired [chapter 21.1 patent gazette] |
Free format text: PATENTE EXTINTA EM 24/05/2021 |