AR048617A1 - Antagonistas del receptor a2a de la adenosina con estructura de pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina. - Google Patents
Antagonistas del receptor a2a de la adenosina con estructura de pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina.Info
- Publication number
- AR048617A1 AR048617A1 ARP050101559A ARP050101559A AR048617A1 AR 048617 A1 AR048617 A1 AR 048617A1 AR P050101559 A ARP050101559 A AR P050101559A AR P050101559 A ARP050101559 A AR P050101559A AR 048617 A1 AR048617 A1 AR 048617A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- hydroxyalkyl
- group
- alkoxyalkyl
- Prior art date
Links
- 229940123702 Adenosine A2a receptor antagonist Drugs 0.000 title abstract 2
- 239000002467 adenosine A2a receptor antagonist Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 18
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 12
- 125000003545 alkoxy group Chemical group 0.000 abstract 10
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 8
- 125000001424 substituent group Chemical group 0.000 abstract 7
- -1 -NR7R8 Chemical group 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000006413 ring segment Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000005081 alkoxyalkoxyalkyl group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005159 cyanoalkoxy group Chemical group 0.000 abstract 2
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 2
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 2
- GWRWCCQBSHBLSN-UHFFFAOYSA-N 8h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine Chemical group N1=CN2NC=NC2=C2C=NN=C21 GWRWCCQBSHBLSN-UHFFFAOYSA-N 0.000 abstract 1
- 125000005083 alkoxyalkoxy group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
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- 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
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- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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
La presente se refiere a antagonistas del receptor A2A de la adenosina con estructura de pirazolo-[4,3-E]-1,2,4-triazolo-[1,5-C]-pirimidina, y composiciones farmacéuticas que los contienen y usos. Reivindicacion 1: Un compuesto que tiene la formula estructural (1) o una sal aceptable para uso farmacéutico del mismo, donde R es R6-fenilo, R6-furanilo, R6-tienilo, R6-piridilo, R6-piridilo N-oxido, R6-oxazolilo, R6-pirrolilo o cicloalquenilo; R1, R2, R3, R4 y R5 se seleccionan independientemente del grupo integrado por H, alquilo y alcoxialquilo; R6 es 1 a 3 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, -CF3, halogeno, -NO2, -CN, -NR7R8, alcoxi, alquiltio, alquilsulfinilo y alquilsulfonilo; R7 es H o alquilo; R8 es H, alquilo, alquilC(O)- o alquil-SO2-; Z es R9, R10-arilo o R9,R10-heteroarilo; R9 es alquenilo, hidroxialquilo, alcoxialquilo, alcoxi-alcoxi-alquilo-, (di-alcoxi)-alquilo, (hidroxi)-alcoxialquilo, R15-cicloalquilo, R15- cicloalquilalquilo, cicloalquil-oxi, cicloalquil-O-alcoxi, cianoalquilo, -C(O)R13, -N(R11)(R12), N(R11)(R12)-alquilo-, -C(O)N(R13)(R16), -alquilen-C(O)-N(R11)2, -C(O)-(R15-heterocicloalquilo), R15-heterocicloalquil-alquilo, R15-heterocicloalquil- alcoxi, R19-heteroarilo, CF3-alquilen-O-alquilo, CF3-hidroxialquilo, (CF3)(hidroxi)alcoxi, ciano-alcoxi, -alquilen-C(O)-O-alquilo, -SO2-N(alquilo)2, (cicloalquil)hidroxialquilo, (hidroxialquil)alcoxi, (dihidroxi)alquilo, (dihidroxi)alcoxi o - C(=NOR17)-CF3; R10 es 1 a 3 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, alquenilo, hidroxi, alcoxi, hidroxialquilo, hidroxialcoxi, alcoxialquilo, alcoxialcoxi, alcoxi-alcoxi-alquilo-, (di-alcoxi)-alquilo, (hidroxi)-alcoxialquilo, R15-cicloalquilo, R15-cicloalquilalquilo, cicloalquil-oxi, cicloalquil-O-alcoxi, alquil-SO2-, alquil-SO-, halo, -CN, cianoalquilo, -CHF2, -CF3, -OCHF2, -OCF3, -C(O)R13, -O-alquilen-C(O)OR13, -C(O)O-alquilo, -N(R11)(R12), N(R11)(R12)-alquilo, N(R11)(R12)-alcoxi, -C(O)N(R13)(R16), R19-heteroarilo, R15-heterocicloalquilo, R15-heterocicloalquil-alquilo, R15-heterocicloalquil-alcoxi, R15-heterocicloalquil-oxi, CF3-alquilen-O-alquilo, CF3-hidroxialquilo, (CF3)(hidroxi)alcoxi, ciano-alcoxi, -alquilen-C(O)-O-alquilo, -SO2-N(alquilo)2, (cicloalquil)hidroxialquilo, (hidroxialquil)alcoxi, (dihidroxi)alquilo, (dihidroxi)alcoxi, -C(=NOR17)-alquilo y -C(=NOR17)-CF3; o un grupo R9 y un grupo R10 en átomos de anillos de C adyacentes juntos forman -O-(CH2)2-O-, -CH2-O-(CH2)2-O-, -O-(CH2)2-, -(CH2)3-O-, -O-(CH2)3-O-, -(CH2)3- o -CH2-CH=CH-, done el anillo formado por los sustituyentes R9 y R10 y los átomos de C del anillo al cual están unidos están sustituidos con R16; o un grupo R9 y un grupo R10 en átomos de anillos de C adyacentes juntos forman -N(R11)-C(O)-O-, -N(R11)-C(O)-S- o -N(R12)-(CH2)2-; o un grupo R9 y un grupo R10 en átomos de anillos de C adyacentes juntos forman -(CH2)2CH(OR18)- , -CH2CH(OR18)CH2-, -(CH2)3CH(OR18)-, -(CH2)2CH(OR18)CH2-, -(CH2)2C(O)-, -CH2C(O)CH2-, -(CH2)3C(O)-, -(CH2)2C(O)CH2-, -O(CH2)2CH(OR18)- o -OCH2CH(OR18)CH2-, donde el anillo formado por los sustituyentes R9 y R10 y los átomos de C del anillo al cual están unidos está sustituido opcionalmente en un átomo de C con hidroxialquilo o alcoxialquilo; cada R11 se selecciona independientemente del grupo integrado por H y alquilo; cada R12 se selecciona independientemente del grupo integrado por H, alquilo, cicloalquilo, hidroxialquilo, alcoxialquilo, -C(O)-alquilo, -C(O)O-alquilo, (alcoxi)hidroxialquilo, alcoxialquil-C(O)-, -SO2alquilo, -alquilen-C(O)alquilo y -alquilen-C(O)O-alquilo; R13 es H, alquilo o -CF3, R15 es 1 a 3 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, -OH, alcoxi, alcoxialquilo e hidroxialquilo, o dos sustituyentes R15, tomados junto con el C al cual están unidos, forman un grupo -C(=O)-, R16 es H, alquilo, alcoxialquilo, OH o hidroxialquilo; R17 es H o alquilo; R18 es H o alquilo, y R19 es 1 o 2 sustituyentes independientemente seleccionados del grupo integrado por H, alquilo, hidroxialquilo, alcoxialquilo, -C(O)N(R11)(R12) y -N(R11)2.
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 |
|---|---|
| AR048617A1 true AR048617A1 (es) | 2006-05-10 |
Family
ID=34966464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050101559A AR048617A1 (es) | 2004-04-21 | 2005-04-20 | Antagonistas 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 |
|---|---|---|---|---|
| SK287748B6 (sk) * | 2000-05-26 | 2011-08-04 | Schering Corporation | Substituované 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo[1,5- c]pyrimidíny, spôsob ich výroby, farmaceutický prostriedok s ich obsahom a ich použitie |
| 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 |
| DK1667964T3 (da) | 2003-09-19 | 2009-10-26 | Janssen Pharmaceutica Nv | 4-((Phenoxyalkyl)thio)-phenoxyeddikesyrer og analoger |
| 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 |
| EP1844792A4 (en) * | 2004-12-14 | 2008-05-21 | Shionogi & Co | THERAPEUTIC AGENT AGAINST OBSTIPATION |
| JO3006B1 (ar) | 2005-09-14 | 2016-09-05 | Janssen Pharmaceutica Nv | املاح ليسين مبتكرة من مشتقات حامض 4-((فينوكسي الكيل)ثيو) فينوكسي الخليك |
| WO2007035542A1 (en) * | 2005-09-19 | 2007-03-29 | 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 |
| 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 |
| US7723343B2 (en) | 2007-03-30 | 2010-05-25 | King Pharmaceuticals Research And Development, Inc. | Adenosine A2A receptor antagonists |
| 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 |
| 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 |
| BRPI1009252A2 (pt) | 2009-03-10 | 2016-03-15 | Takeda Pharmaceutical | composto, pró-droga, composição farmacêutica, métodos para prevenir ou tratar doenças do sistema nervoso central, e mal de alzheimer, e, uso do composto ou de uma pró-droga do mesmo |
| TW201100427A (en) * | 2009-03-31 | 2011-01-01 | Arqule Inc | Substituted heterocyclic compounds |
| EP2486024B1 (en) * | 2009-10-08 | 2015-04-22 | Sanofi | Phenyloxadiazole derivatives as pgds inhibitors |
| 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 |
| ES2716832T3 (es) * | 2011-12-27 | 2019-06-17 | Bio Pharm Solutions Co Ltd | Compuestos carbamatos de fenilo para su uso en el alivio o el tratamiento del dolor y el dolor neuropático |
| 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 |
| CA3058260A1 (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 |
| 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 |
| 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 |
| 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 |
| 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 |
| JP2022500496A (ja) * | 2018-09-11 | 2022-01-04 | アイテオ ベルギウム エスエー | A2a阻害剤としてのチオカルバメート誘導体、その医薬組成物、及び抗がん剤との組み合わせ |
| US11376255B2 (en) | 2018-09-11 | 2022-07-05 | iTeos Belgium SA | 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 |
| 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 |
| WO2020106558A1 (en) | 2018-11-20 | 2020-05-28 | Merck Sharp & Dohme Corp. | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| WO2020106560A1 (en) | 2018-11-20 | 2020-05-28 | Merck Sharp & Dohme Corp. | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| JP2022511778A (ja) | 2018-11-30 | 2022-02-01 | メルク・シャープ・アンド・ドーム・コーポレーション | アデノシン受容体拮抗薬としての7-、8-及び10-置換されたアミノトリアゾロキナゾリン誘導体、医薬組成物及びそれらの使用 |
| JOP20210116A1 (ar) | 2018-11-30 | 2023-01-30 | Merck Sharp & Dohme | مشتقات أمينو ترايازولو كوينازولين بها استبدال في الموضع-9 كمضادات مستقبل أدينوزين، تركيبات صيدلانية واستخدامها |
| 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 |
| 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 |
| SK287748B6 (sk) * | 2000-05-26 | 2011-08-04 | Schering Corporation | Substituované 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo[1,5- c]pyrimidíny, spôsob ich výroby, farmaceutický prostriedok s ich obsahom a ich použitie |
| GB0100624D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| EP1435960B1 (en) | 2001-10-15 | 2014-07-30 | Merck Sharp & Dohme Corp. | Imidazo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as adenosine a2a receptor antagonists |
| NZ540493A (en) | 2002-12-19 | 2008-04-30 | Schering Corp | Uses of adenosine A2a receptor antagonists |
| TWI355381B (en) * | 2003-04-23 | 2012-01-01 | Schering Corp | 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-tri |
-
2005
- 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 PE PE2005000428A patent/PE20060185A1/es not_active Application Discontinuation
- 2005-04-19 DE DE602005020127T patent/DE602005020127D1/de not_active Expired - Lifetime
- 2005-04-19 MX MXPA06012231A patent/MXPA06012231A/es active IP Right Grant
- 2005-04-19 EP EP05737774A patent/EP1745047B1/en not_active Expired - Lifetime
- 2005-04-19 JP JP2007509594A patent/JP2007533754A/ja active Pending
- 2005-04-19 US US11/108,916 patent/US7709492B2/en active Active
- 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 ES ES05737774T patent/ES2342082T3/es not_active Expired - Lifetime
- 2005-04-19 TW TW094112339A patent/TW200538118A/zh unknown
- 2005-04-19 KR KR1020067021803A patent/KR20060135901A/ko not_active Ceased
- 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 |
|---|---|
| EP1745047A1 (en) | 2007-01-24 |
| MXPA06012231A (es) | 2006-12-15 |
| AU2005236059A1 (en) | 2005-11-03 |
| PE20060185A1 (es) | 2006-03-20 |
| NZ550591A (en) | 2010-10-29 |
| US20050239795A1 (en) | 2005-10-27 |
| JP2007533754A (ja) | 2007-11-22 |
| EP1745047B1 (en) | 2010-03-24 |
| WO2005103055A1 (en) | 2005-11-03 |
| US7709492B2 (en) | 2010-05-04 |
| AU2005236059B2 (en) | 2009-01-15 |
| ES2342082T3 (es) | 2010-07-01 |
| JP2008231111A (ja) | 2008-10-02 |
| HK1095818A1 (en) | 2007-05-18 |
| CA2563635A1 (en) | 2005-11-03 |
| ATE461932T1 (de) | 2010-04-15 |
| IL178674A0 (en) | 2007-02-11 |
| TW200538118A (en) | 2005-12-01 |
| DE602005020127D1 (de) | 2010-05-06 |
| KR20060135901A (ko) | 2006-12-29 |
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