PE20060185A1 - ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA - Google Patents
ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINAInfo
- Publication number
- PE20060185A1 PE20060185A1 PE2005000428A PE2005000428A PE20060185A1 PE 20060185 A1 PE20060185 A1 PE 20060185A1 PE 2005000428 A PE2005000428 A PE 2005000428A PE 2005000428 A PE2005000428 A PE 2005000428A PE 20060185 A1 PE20060185 A1 PE 20060185A1
- Authority
- PE
- Peru
- Prior art keywords
- adenosine
- triazolo
- pyrimidine
- receptor antagonist
- alcoxyalkyl
- Prior art date
Links
- 229940123702 Adenosine A2a receptor antagonist Drugs 0.000 title 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- 239000002467 adenosine A2a receptor antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000007471 Adenosine A2A receptor Human genes 0.000 abstract 1
- 108010085277 Adenosine A2A receptor Proteins 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
-
- 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
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)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R ES R6-FENILO, R6-TIENILO, CICLOALQUENILO, ENTRE OTROS; R1, R2, R3, R4 Y R5 SON CADA UNO H, ALQUILO, ALCOXIALQUILO; R6 ES UNO A 3 SUSTITUYENTES SELECCIONADOS DE H, ALQUILO, -CF3, HALOGENO, -NO2, -CN, ALCOXI, ENTRE OTROS; Z ES ALQUENILO, ALCOXIALQUILO, R10-HETEROARILO, ENTRE OTROS; R10 ES 1-3 SUSTITUYENTES SELECCIONADOS ENTRE H, ALQUILO, HIDROXI, ALCOXIALQUILO, HIDROXIALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: A, B, ENTRE OTROS. SE REFIERE TAMBIEN A UN COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR A2a DE ADENOSINA UTILES EN EL TRATAMIENTO DE PARKINSON
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56391304P | 2004-04-21 | 2004-04-21 | |
| US60996604P | 2004-09-15 | 2004-09-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060185A1 true PE20060185A1 (es) | 2006-03-20 |
Family
ID=34966464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000428A PE20060185A1 (es) | 2004-04-21 | 2005-04-19 | ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US7709492B2 (es) |
| EP (1) | EP1745047B1 (es) |
| JP (2) | JP2007533754A (es) |
| KR (1) | KR20060135901A (es) |
| AR (1) | AR048617A1 (es) |
| AT (1) | ATE461932T1 (es) |
| AU (1) | AU2005236059B2 (es) |
| CA (1) | CA2563635A1 (es) |
| DE (1) | DE602005020127D1 (es) |
| ES (1) | ES2342082T3 (es) |
| IL (1) | IL178674A0 (es) |
| MX (1) | MXPA06012231A (es) |
| NZ (1) | NZ550591A (es) |
| PE (1) | PE20060185A1 (es) |
| TW (1) | TW200538118A (es) |
| WO (1) | WO2005103055A1 (es) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2237576T3 (es) * | 2000-05-26 | 2005-08-01 | Schering Corporation | Antagonistas del receptor a2a de adenosina. |
| US20060128694A1 (en) * | 2002-12-19 | 2006-06-15 | Michael Grzelak | Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| EA012241B1 (ru) | 2003-09-19 | 2009-08-28 | Янссен Фармацевтика, Н.В. | 4-((феноксиалкил)тио)феноксиуксусные кислоты и их аналоги |
| MY147518A (en) | 2004-09-15 | 2012-12-31 | Janssen Pharmaceutica Nv | 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs |
| CA2588595A1 (en) * | 2004-12-13 | 2006-06-22 | Arena Pharmaceuticals, Inc. | N-biaryl and n-arylheteroaryl piperazine derivatives as modulators of the 5ht2c receptor useful for the treatment of disorders related thereto |
| JPWO2006064780A1 (ja) * | 2004-12-14 | 2008-06-12 | 塩野義製薬株式会社 | 便秘治療剤 |
| JO3006B1 (ar) | 2005-09-14 | 2016-09-05 | Janssen Pharmaceutica Nv | املاح ليسين مبتكرة من مشتقات حامض 4-((فينوكسي الكيل)ثيو) فينوكسي الخليك |
| 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 |
| 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 |
| PE20080188A1 (es) | 2006-04-18 | 2008-03-10 | Janssen Pharmaceutica Nv | Derivados del acido benzoazepin-oxi-acetico como agonistas de ppar-delta usados para aumentar hdl-c, reducir ldl-c y reducir colesterol |
| 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 |
| CA2717172A1 (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 |
| US8153416B2 (en) * | 2008-12-10 | 2012-04-10 | Thesis Chemistry, Llc | Process for manufacture of optically active 2-(acyloxymethyl)-1,3-oxathiolanes using enzymatic resolution |
| EP2379556A1 (en) * | 2008-12-30 | 2011-10-26 | ArQule, Inc. | Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds |
| US8431699B2 (en) * | 2009-02-27 | 2013-04-30 | Vertichem Corporation | Method for manufacture of 2-oxoimidazolidines |
| ES2487616T3 (es) | 2009-03-10 | 2014-08-22 | Takeda Pharmaceutical Company Limited | Derivados de benzofurano |
| EP2414361A1 (en) * | 2009-03-31 | 2012-02-08 | ArQule, Inc. | Substituted heterocyclic compounds |
| CN102666508A (zh) * | 2009-10-08 | 2012-09-12 | 赛诺菲 | 作为前列腺素d合酶抑制剂的苯基噁二唑衍生物 |
| 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 |
| WO2012135084A1 (en) * | 2011-03-31 | 2012-10-04 | Merck Sharp & Dohme Corp. | METABOLITES OF 2-(FURAN-2-YL)-7-(2-(4-(4-(2-METHOXYETHOXY)PHENYL)PIPERAZIN-1-YL)ETHYL)-7H-PYRAZOLO[4,3-e][1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-5-AMINE AND THEIR UTILITY AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| MX353024B (es) * | 2011-12-27 | 2017-12-18 | Bio Pharm Solutions Co Ltd | Compuestos de fenil carbamato para uso en la prevencion o tratamiento de epilepsia. |
| KR102640927B1 (ko) * | 2017-03-30 | 2024-02-27 | 아이테오스 벨지움 에스에이 | A2a 억제제로서의 2-옥소-티아졸 유도체 및 암 치료에 사용하기 위한 화합물 |
| 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 |
| CN107935953A (zh) * | 2017-12-31 | 2018-04-20 | 佛山市赛维斯医药科技有限公司 | 含末端烯键和酰肼结构的comt抑制剂、制备方法及其用途 |
| CN108218796A (zh) * | 2017-12-31 | 2018-06-29 | 佛山市赛维斯医药科技有限公司 | 含酰肼结构的化合物、制备方法及其用途 |
| CN108148004A (zh) * | 2017-12-31 | 2018-06-12 | 佛山市赛维斯医药科技有限公司 | 一种含丙酰肼和嘧啶结构的化合物、制备方法及其用途 |
| CN108191775A (zh) * | 2017-12-31 | 2018-06-22 | 佛山市赛维斯医药科技有限公司 | 一种末端烯丙基丙酰肼结构化合物及其用途 |
| US11472811B2 (en) | 2018-04-08 | 2022-10-18 | Beigene, Ltd. | Pyrazolotriazolopyrimidine derivatives as A2A receptor antagonist |
| 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 |
| US11376255B2 (en) | 2018-09-11 | 2022-07-05 | iTeos Belgium SA | Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents |
| WO2020053263A1 (en) * | 2018-09-11 | 2020-03-19 | Iteos Therapeutics S.A. | Thiocarbamate derivatives as a2a inhibitors, pharmaceutical composition thereof and combinations with anticancer agents |
| BE1026615B1 (fr) * | 2018-09-27 | 2020-07-06 | Iteos Therapeutics S A | Combinaison d’un inhibiteur du récepteur a2a et d'un agent anticancéreux |
| BE1026758B1 (fr) * | 2018-09-11 | 2020-06-09 | Iteos Therapeutics S A | Composition pharmaceutique comprenant des dérivés de thiocarbamate inhibiteurs d’a2a |
| BE1026602B1 (fr) * | 2018-09-27 | 2020-06-18 | Iteos Therapeutics S A | Inhibiteurs d’a2a ne penetrant pas dans le cerveau et methodes d’utilisation dans le traitement de cancers |
| US11427594B2 (en) | 2018-09-27 | 2022-08-30 | iTeos Belgium SA | Non brain penetrant A2A inhibitors and methods for use in the treatment of cancers |
| US12414952B2 (en) | 2018-11-20 | 2025-09-16 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| EP3883575B1 (en) | 2018-11-20 | 2025-10-08 | Merck Sharp & Dohme LLC | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| PE20211768A1 (es) | 2018-11-30 | 2021-09-07 | Merck Sharp & Dohme | Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmaceuticas y su uso |
| KR20210097152A (ko) | 2018-11-30 | 2021-08-06 | 머크 샤프 앤드 돔 코포레이션 | 아데노신 수용체 길항제로서의 7-, 8- 및 10-치환된 아미노 트리아졸로 퀴나졸린 유도체, 제약 조성물 및 그의 용도 |
| WO2020227156A1 (en) * | 2019-05-03 | 2020-11-12 | Nektar Therapeutics | Adenosine 2 receptor antagonists |
| US20230024108A1 (en) * | 2019-07-17 | 2023-01-26 | Teon Therapeutics, Inc. | Adenosine a2a receptor antagonists |
Family Cites Families (9)
| 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 |
| ES2165393T3 (es) | 1993-07-27 | 2002-03-16 | Kyowa Hakko Kogyo Kk | Remedio contra la enfermedad de parkinson. |
| 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 |
| ES2237576T3 (es) * | 2000-05-26 | 2005-08-01 | Schering Corporation | Antagonistas del receptor a2a de adenosina. |
| GB0100624D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| 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 |
| DE60335294D1 (de) | 2002-12-19 | 2011-01-20 | Schering Corp | Dlung des extrapyramidalen syndroms |
| TWI375677B (en) | 2003-04-23 | 2012-11-01 | Schering Corp | 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine a2a receptor antagonists |
-
2005
- 2005-04-19 PE PE2005000428A patent/PE20060185A1/es not_active Application Discontinuation
- 2005-04-19 TW TW094112339A patent/TW200538118A/zh unknown
- 2005-04-19 AT AT05737774T patent/ATE461932T1/de not_active IP Right Cessation
- 2005-04-19 CA CA002563635A patent/CA2563635A1/en not_active Abandoned
- 2005-04-19 ES ES05737774T patent/ES2342082T3/es not_active Expired - Lifetime
- 2005-04-19 JP JP2007509594A patent/JP2007533754A/ja active Pending
- 2005-04-19 DE DE602005020127T patent/DE602005020127D1/de not_active Expired - Lifetime
- 2005-04-19 KR KR1020067021803A patent/KR20060135901A/ko not_active Ceased
- 2005-04-19 MX MXPA06012231A patent/MXPA06012231A/es active IP Right Grant
- 2005-04-19 NZ NZ550591A patent/NZ550591A/en unknown
- 2005-04-19 AU AU2005236059A patent/AU2005236059B2/en not_active Ceased
- 2005-04-19 US US11/108,916 patent/US7709492B2/en active Active
- 2005-04-19 WO PCT/US2005/013454 patent/WO2005103055A1/en not_active Ceased
- 2005-04-19 EP EP05737774A patent/EP1745047B1/en not_active Expired - Lifetime
- 2005-04-20 AR ARP050101559A patent/AR048617A1/es not_active Application Discontinuation
-
2006
- 2006-10-17 IL IL178674A patent/IL178674A0/en unknown
-
2008
- 2008-04-08 JP JP2008100773A patent/JP2008231111A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US7709492B2 (en) | 2010-05-04 |
| NZ550591A (en) | 2010-10-29 |
| ATE461932T1 (de) | 2010-04-15 |
| JP2008231111A (ja) | 2008-10-02 |
| MXPA06012231A (es) | 2006-12-15 |
| US20050239795A1 (en) | 2005-10-27 |
| IL178674A0 (en) | 2007-02-11 |
| AU2005236059A1 (en) | 2005-11-03 |
| HK1095818A1 (en) | 2007-05-18 |
| AR048617A1 (es) | 2006-05-10 |
| JP2007533754A (ja) | 2007-11-22 |
| ES2342082T3 (es) | 2010-07-01 |
| TW200538118A (en) | 2005-12-01 |
| WO2005103055A1 (en) | 2005-11-03 |
| DE602005020127D1 (de) | 2010-05-06 |
| EP1745047A1 (en) | 2007-01-24 |
| EP1745047B1 (en) | 2010-03-24 |
| KR20060135901A (ko) | 2006-12-29 |
| AU2005236059B2 (en) | 2009-01-15 |
| CA2563635A1 (en) | 2005-11-03 |
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