AR052568A1 - Derivados de pirazolo -pirimidina como antagonstas de mglur2 - Google Patents
Derivados de pirazolo -pirimidina como antagonstas de mglur2Info
- Publication number
- AR052568A1 AR052568A1 ARP060100412A ARP060100412A AR052568A1 AR 052568 A1 AR052568 A1 AR 052568A1 AR P060100412 A ARP060100412 A AR P060100412A AR P060100412 A ARP060100412 A AR P060100412A AR 052568 A1 AR052568 A1 AR 052568A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- halogen
- haloalkyl
- cycloalkyl
- Prior art date
Links
- 101150016175 Grm2 gene Proteins 0.000 title 1
- 102100036837 Metabotropic glutamate receptor 2 Human genes 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000006413 ring segment Chemical group 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 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
- C07D487/02—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 two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P25/18—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
- A61P25/28—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
- A61P35/00—Antineoplastic agents
-
- 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)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto que se ajusta a la formula (1) en la que a se elige entre el grupo formado por las formulas (2), Ra es H, halogeno o alquilo C1-6; R1 es H, halogeno, alcoxi C1-6, alquilo C1-6, haloalquilo C1-6, haloalcoxi c1-6; R2 es halogeno, haloalquilo C1-6; R3 es alquilo c1-6 opcionalmente sustituido por hidroxi; o es NRbRc, en el que Rb y Rc se eligen con independencia entre sí entre el grupo formado por: H, cicloalquilo C3-8, arilo, heteroarilo que tiene de 5 a 12 átomos en el anillo y alquilo C1-6 que está opcionalmente sustituido por uno o varios sustituyentes elegidos entre el grupo formado por halogeno, hidroxi, cicloalquilo C3-8, arilo, heteroarilo que tiene de 5 a 12 átomos en el anillo y -NRbRc, en el que Rb y Rc se eligen con independencia entre sí entre el grupo formado por H y alquilo C1-6; o Rb y Rc junto con el átomo de N al que están unidos pueden formar un grupo heterocíclico opcionalmente sustituido que contiene de 5 a 12 átomos en el anillo, en el que los sustituyentes se eligen entre el grupo formado por halogeno, hidroxi, alquilo C1-6 y haloalquilo C1-6; R4 es H, alquilo C1-6 lineal, haloalquilo C1-6 o cicloalquilo C3-4; así como las sales farmacéuticamente aceptables del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05101027 | 2005-02-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR052568A1 true AR052568A1 (es) | 2007-03-21 |
Family
ID=36090752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060100412A AR052568A1 (es) | 2005-02-11 | 2006-02-06 | Derivados de pirazolo -pirimidina como antagonstas de mglur2 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7361659B2 (es) |
| EP (1) | EP1851225B1 (es) |
| JP (1) | JP4708438B2 (es) |
| KR (1) | KR100968291B1 (es) |
| CN (1) | CN101115755B (es) |
| AR (1) | AR052568A1 (es) |
| AT (1) | ATE512966T1 (es) |
| AU (1) | AU2006212457B2 (es) |
| BR (1) | BRPI0607927A2 (es) |
| CA (1) | CA2597608C (es) |
| ES (1) | ES2365406T3 (es) |
| IL (1) | IL184712A (es) |
| MX (1) | MX2007009106A (es) |
| NO (1) | NO20073876L (es) |
| RU (1) | RU2402553C2 (es) |
| TW (1) | TW200716120A (es) |
| WO (1) | WO2006084634A1 (es) |
| ZA (1) | ZA200706353B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2085398A1 (en) * | 2008-02-01 | 2009-08-05 | Merz Pharma GmbH & Co. KGaA | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| EP2268645B1 (en) * | 2008-03-06 | 2014-11-12 | Sanofi | Substituted dihydro, trihydro and tetrahydro cycloalkyloxazolopyrimidinones, preparation and use thereof as allosteric modulators of mglur |
| US8207181B2 (en) | 2008-03-06 | 2012-06-26 | Sanofi | Substituted dihydro, trihydro and tetrahydro cycloalkyloxazolopyrimidinones, preparation and use thereof |
| US20130137865A1 (en) | 2010-08-11 | 2013-05-30 | Taisho Pharmaceutical Co., Ltd. | Heteroaryl-pyrazole derivative |
| US9447099B2 (en) * | 2011-10-04 | 2016-09-20 | Hoffmann-La Roche Inc. | Methods for the preparation of 5-[2-[7 (trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo [1,5-A]pyrimidin-3-yl[ethynyl]-2-pyridinamine |
| US9957271B2 (en) | 2011-10-20 | 2018-05-01 | Glaxosmithkline Llc | Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators |
| EP2666775A1 (en) | 2012-05-21 | 2013-11-27 | Domain Therapeutics | Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors |
| EP2925292A1 (en) | 2012-10-23 | 2015-10-07 | F. Hoffmann-La Roche AG | Mglu2/3 antagonists for the treatment of autistic disorders |
| RU2016144702A (ru) | 2014-04-23 | 2018-05-24 | Ф. Хоффманн-Ля Рош Аг | Антагонисты mglu2/3 для лечения интеллектуальной недостаточности |
| JOP20150179B1 (ar) * | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| EP3000814A1 (en) | 2014-09-26 | 2016-03-30 | Domain Therapeutics | Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors |
| WO2016073889A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| SI3215511T1 (sl) | 2014-11-06 | 2024-07-31 | Bial-R&D Investments, S. A. | Substituirani pirazolo(1,5-a)pirimidini in njihova uporaba pri zdravljenju zdravstvenih motenj |
| WO2016073891A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| AU2015357169B2 (en) | 2014-12-03 | 2021-03-04 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
| PL236355B1 (pl) * | 2015-04-02 | 2021-01-11 | Celon Pharma Spolka Akcyjna | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3 |
| US11045562B2 (en) | 2015-12-18 | 2021-06-29 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| JP6927974B2 (ja) | 2015-12-18 | 2021-09-01 | ヤンセン ファーマシューティカ エヌ．ベー． | 放射性標識ｍＧｌｕＲ２／３ＰＥＴリガンド |
| BR112018070586A8 (pt) * | 2016-04-06 | 2023-03-14 | Lysosomal Therapeutics Inc | Compostos de pirazol[1,5-a]pirimidinil carboxamida e seu uso no tratamento de distúrbios médicos |
| EP3440081A4 (en) | 2016-04-06 | 2019-09-18 | Lysosomal Therapeutics Inc. | PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER |
| WO2017176961A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| BR112018072552A8 (pt) | 2016-05-05 | 2023-03-14 | Lysosomal Therapeutics Inc | Compostos de imidazo [1,2-b]piridazinas e imidazo [1,5-b] piridazinas substituídas, composição farmacêutica que os compreende e seu uso no tratamento de distúrbios médicos |
| CN110225781B (zh) * | 2017-01-09 | 2022-05-17 | 辉诺生物医药科技（杭州）有限公司 | 噻唑衍生物及其应用 |
| AU2018373464B2 (en) | 2017-11-24 | 2022-12-08 | Sumitomo Pharma Co., Ltd. | 6,7-dihydropyrazolo[1,5-a] pyrazinone derivative and medical use thereof |
| AU2019297214B2 (en) * | 2018-07-06 | 2022-07-07 | Phaeno Therapeutics Co., Ltd. | Crystal forms of thiazole compound and application thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1090189C (zh) | 1996-02-07 | 2002-09-04 | 詹森药业有限公司 | 吡唑并嘧啶类化合物 |
| DK0891978T3 (da) | 1997-07-18 | 2002-07-01 | Hoffmann La Roche | 5H-Thiazol(3,2-a)pyrimidinderivativer |
| WO2000059908A2 (en) | 1999-04-06 | 2000-10-12 | Du Pont Pharmaceuticals Company | Pyrazolopyrimidines as crf antagonists |
| HUP0400851A3 (en) * | 2001-04-12 | 2010-03-29 | Hoffmann La Roche | Dihydro-benzo[b][1,4]diazepin-2-one derivatives as mglur2 antagonists ii, process for their preparation and pharmaceutical compositions containing them |
| JP2006523707A (ja) * | 2003-04-15 | 2006-10-19 | アストラゼネカ アクツィエボラーグ | 治療化合物 |
| US7329662B2 (en) * | 2003-10-03 | 2008-02-12 | Hoffmann-La Roche Inc. | Pyrazolo-pyridine |
| JP4608542B2 (ja) * | 2004-06-21 | 2011-01-12 | エフ．ホフマン−ラ ロシュ アーゲー | ピラゾロピリミジン誘導体 |
-
2006
- 2006-02-03 WO PCT/EP2006/000940 patent/WO2006084634A1/en not_active Ceased
- 2006-02-03 CA CA2597608A patent/CA2597608C/en not_active Expired - Fee Related
- 2006-02-03 AT AT06706609T patent/ATE512966T1/de active
- 2006-02-03 RU RU2007128624/04A patent/RU2402553C2/ru not_active IP Right Cessation
- 2006-02-03 ES ES06706609T patent/ES2365406T3/es not_active Expired - Lifetime
- 2006-02-03 MX MX2007009106A patent/MX2007009106A/es active IP Right Grant
- 2006-02-03 AU AU2006212457A patent/AU2006212457B2/en not_active Ceased
- 2006-02-03 BR BRPI0607927-0A patent/BRPI0607927A2/pt not_active IP Right Cessation
- 2006-02-03 EP EP06706609A patent/EP1851225B1/en not_active Expired - Lifetime
- 2006-02-03 KR KR1020077018345A patent/KR100968291B1/ko not_active Expired - Fee Related
- 2006-02-03 CN CN2006800046579A patent/CN101115755B/zh not_active Expired - Fee Related
- 2006-02-03 JP JP2007554484A patent/JP4708438B2/ja not_active Expired - Fee Related
- 2006-02-06 US US11/348,105 patent/US7361659B2/en not_active Expired - Fee Related
- 2006-02-06 AR ARP060100412A patent/AR052568A1/es not_active Application Discontinuation
- 2006-02-08 TW TW095104260A patent/TW200716120A/zh unknown
-
2007
- 2007-07-19 IL IL184712A patent/IL184712A/en not_active IP Right Cessation
- 2007-07-24 NO NO20073876A patent/NO20073876L/no not_active Application Discontinuation
- 2007-07-31 ZA ZA200706353A patent/ZA200706353B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP1851225A1 (en) | 2007-11-07 |
| MX2007009106A (es) | 2007-09-11 |
| US20060183756A1 (en) | 2006-08-17 |
| ZA200706353B (en) | 2009-09-30 |
| CA2597608A1 (en) | 2006-08-17 |
| EP1851225B1 (en) | 2011-06-15 |
| NO20073876L (no) | 2007-09-10 |
| ES2365406T3 (es) | 2011-10-04 |
| RU2402553C2 (ru) | 2010-10-27 |
| ATE512966T1 (de) | 2011-07-15 |
| JP4708438B2 (ja) | 2011-06-22 |
| AU2006212457A1 (en) | 2006-08-17 |
| IL184712A (en) | 2013-05-30 |
| JP2008530042A (ja) | 2008-08-07 |
| TW200716120A (en) | 2007-05-01 |
| KR100968291B1 (ko) | 2010-07-07 |
| WO2006084634A1 (en) | 2006-08-17 |
| AU2006212457B2 (en) | 2011-04-14 |
| CA2597608C (en) | 2013-12-24 |
| IL184712A0 (en) | 2007-12-03 |
| US7361659B2 (en) | 2008-04-22 |
| RU2007128624A (ru) | 2009-03-20 |
| CN101115755A (zh) | 2008-01-30 |
| CN101115755B (zh) | 2013-01-16 |
| KR20070104592A (ko) | 2007-10-26 |
| BRPI0607927A2 (pt) | 2009-10-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |