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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (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 |
|---|---|---|---|---|
| SI1283839T1 (es) * | 2000-05-26 | 2005-08-31 | Schering Corp | |
| 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 |
| PT1667964E (pt) | 2003-09-19 | 2009-09-02 | Janssen Pharmaceutica Nv | Ácidos 4-((fenoxialquil)tio)-fenoxiacéticos e análogos |
| 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 |
| TW200633721A (en) * | 2004-12-14 | 2006-10-01 | Shionogi & Co | A pharmaceutical composition for treating constipation |
| JO3006B1 (ar) | 2005-09-14 | 2016-09-05 | Janssen Pharmaceutica Nv | املاح ليسين مبتكرة من مشتقات حامض 4-((فينوكسي الكيل)ثيو) فينوكسي الخليك |
| ATE538123T1 (de) * | 2005-09-19 | 2012-01-15 | Schering Corp | 2-heteroarylpyrazoloä4,3-eü-1, 2, 4-triazolo-ä1,5-cü-pyrimidine als antagonisten des adenosin-a2a- rezeptors |
| 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 |
| 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 |
| 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 |
| WO2010078430A1 (en) * | 2008-12-30 | 2010-07-08 | 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 |
| CN102421767B (zh) | 2009-03-10 | 2014-06-18 | 武田药品工业株式会社 | 苯并呋喃衍生物 |
| CA2756871A1 (en) * | 2009-03-31 | 2010-10-07 | Arqule, Inc. | Substituted heterocyclic compounds |
| CN107875155A (zh) * | 2009-10-08 | 2018-04-06 | 赛诺菲 | 苯基噁二唑衍生物在制备治疗变应性或炎性疾病的药物中的用途 |
| JP5843869B2 (ja) * | 2010-09-24 | 2016-01-13 | アドヴィナス・セラピューティックス・リミテッド | アデノシン受容体拮抗薬としての縮合三環化合物 |
| 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 |
| EP2797878B1 (en) * | 2011-12-27 | 2017-08-16 | Bio-Pharm Solutions Co., Ltd. | Phenyl carbamate compounds for use in preventing or treating stroke |
| WO2018178338A1 (en) * | 2017-03-30 | 2018-10-04 | Iteos Therapeutics | 2-oxo-thiazole derivatives as a2a inhibitors and compounds for use in the treatment of cancers |
| EP3601296B1 (en) * | 2017-03-30 | 2022-05-25 | iTeos Belgium SA | 2-oxo-thiazole derivatives as a2a inhibitors and compounds for use in the treatment of cancers |
| 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 |
| 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 |
| 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 |
| 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 |
| SG11202009706VA (en) | 2018-04-08 | 2020-10-29 | 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 |
| BE1026758B1 (fr) * | 2018-09-11 | 2020-06-09 | Iteos Therapeutics S A | Composition pharmaceutique comprenant des dérivés de thiocarbamate inhibiteurs d’a2a |
| BE1026615B1 (fr) * | 2018-09-27 | 2020-07-06 | Iteos Therapeutics S A | Combinaison d’un inhibiteur du récepteur a2a et d'un agent anticancéreux |
| 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 |
| 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 |
| MX2021005839A (es) | 2018-11-20 | 2021-07-15 | Merck Sharp & Dohme Llc | Antagonistas del receptor de adenosina aminotriazolopirimidina y aminotriazolopirazina sustituidos, composiciones farmaceuticas y su uso. |
| 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 |
| TW202039496A (zh) | 2018-11-30 | 2020-11-01 | 美商默沙東藥廠 | 做為腺苷受體拮抗劑之9-經取代胺基三唑喹唑啉衍生物、醫藥組合物及其用途 |
| CA3120331A1 (en) | 2018-11-30 | 2020-06-04 | Merck Sharp & Dohme Corp. | 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| US12325708B2 (en) | 2019-05-03 | 2025-06-10 | 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 |
| ATE208199T1 (de) * | 1993-07-27 | 2001-11-15 | Kyowa Hakko Kogyo Kk | Arzneimittel gegen parkinsonsche krankheit |
| 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 |
| SI1283839T1 (es) * | 2000-05-26 | 2005-08-31 | Schering Corp | |
| GB0100624D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| US6653315B2 (en) * | 2001-10-15 | 2003-11-25 | Schering Corporation | Adenosine A2a receptor antagonists |
| TWI331036B (en) | 2002-12-19 | 2010-10-01 | Schering Corp | Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| KR100831107B1 (ko) * | 2003-04-23 | 2008-05-20 | 쉐링 코포레이션 | 2-알키닐- 및 2-알케닐-피라졸로-[4,3-e]-1,2,4-트리아졸로-[1,5-c]-피리미딘 아데노신 A2a 수용체 길항제 및 이를 포함하는 약제학적 조성물 |
-
2005
- 2005-04-19 DE DE602005020127T patent/DE602005020127D1/de not_active Expired - Lifetime
- 2005-04-19 PE PE2005000428A patent/PE20060185A1/es not_active Application Discontinuation
- 2005-04-19 CA CA002563635A patent/CA2563635A1/en not_active Abandoned
- 2005-04-19 KR KR1020067021803A patent/KR20060135901A/ko not_active Ceased
- 2005-04-19 ES ES05737774T patent/ES2342082T3/es not_active Expired - Lifetime
- 2005-04-19 TW TW094112339A patent/TW200538118A/zh unknown
- 2005-04-19 US US11/108,916 patent/US7709492B2/en active Active
- 2005-04-19 JP JP2007509594A patent/JP2007533754A/ja active Pending
- 2005-04-19 AT AT05737774T patent/ATE461932T1/de not_active IP Right Cessation
- 2005-04-19 NZ NZ550591A patent/NZ550591A/en unknown
- 2005-04-19 WO PCT/US2005/013454 patent/WO2005103055A1/en not_active Ceased
- 2005-04-19 AU AU2005236059A patent/AU2005236059B2/en not_active Ceased
- 2005-04-19 EP EP05737774A patent/EP1745047B1/en not_active Expired - Lifetime
- 2005-04-19 MX MXPA06012231A patent/MXPA06012231A/es active IP Right Grant
- 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 |
|---|---|
| TW200538118A (en) | 2005-12-01 |
| WO2005103055A1 (en) | 2005-11-03 |
| MXPA06012231A (es) | 2006-12-15 |
| DE602005020127D1 (de) | 2010-05-06 |
| AU2005236059A1 (en) | 2005-11-03 |
| US7709492B2 (en) | 2010-05-04 |
| AR048617A1 (es) | 2006-05-10 |
| EP1745047B1 (en) | 2010-03-24 |
| ATE461932T1 (de) | 2010-04-15 |
| AU2005236059B2 (en) | 2009-01-15 |
| CA2563635A1 (en) | 2005-11-03 |
| EP1745047A1 (en) | 2007-01-24 |
| NZ550591A (en) | 2010-10-29 |
| ES2342082T3 (es) | 2010-07-01 |
| JP2008231111A (ja) | 2008-10-02 |
| KR20060135901A (ko) | 2006-12-29 |
| HK1095818A1 (en) | 2007-05-18 |
| JP2007533754A (ja) | 2007-11-22 |
| US20050239795A1 (en) | 2005-10-27 |
| IL178674A0 (en) | 2007-02-11 |
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