MX2020007869A - Derivados de piperazina condensados con triazol, imidazol y pirrol y su uso como moduladores de receptores mglu5. - Google Patents
Derivados de piperazina condensados con triazol, imidazol y pirrol y su uso como moduladores de receptores mglu5.Info
- Publication number
- MX2020007869A MX2020007869A MX2020007869A MX2020007869A MX2020007869A MX 2020007869 A MX2020007869 A MX 2020007869A MX 2020007869 A MX2020007869 A MX 2020007869A MX 2020007869 A MX2020007869 A MX 2020007869A MX 2020007869 A MX2020007869 A MX 2020007869A
- Authority
- MX
- Mexico
- Prior art keywords
- triazole
- imidazole
- modulators
- piperazine derivatives
- pyrrole
- Prior art date
Links
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 title abstract 5
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title abstract 4
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 title abstract 2
- 150000003852 triazoles Chemical class 0.000 title abstract 2
- 101001032845 Homo sapiens Metabotropic glutamate receptor 5 Proteins 0.000 title 1
- RAXXELZNTBOGNW-UHFFFAOYSA-O Imidazolium Chemical compound C1=C[NH+]=CN1 RAXXELZNTBOGNW-UHFFFAOYSA-O 0.000 title 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 title 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 230000003281 allosteric effect Effects 0.000 abstract 3
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 abstract 2
- 208000010877 cognitive disease Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000004064 dysfunction Effects 0.000 abstract 2
- 229930195712 glutamate Natural products 0.000 abstract 2
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 abstract 1
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 230000006999 cognitive decline Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 230000007170 pathology Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000004885 piperazines Chemical class 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 201000000980 schizophrenia Diseases 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61P25/28—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
Abstract
Se divulgan derivados de piperazina condensados con triazol, imidazol y pinol, y sus usos corno moduladores alostéricos de la actividad del receptor mGlu5, composiciones farmacéuticas que comprenden tales compuestos, y métodos de tratamiento con los mismos. Los compuestos de la invención pueden usarse para el tratamiento y/o la prevención de trastornos neurológicos y psiquiátricos asociados con la disfunción del glutamato, tales como esquizofrenia o deterioro cognitivo, demencia o deficiencia cognitiva, u otras patologías que pueden estar relacionadas directamente o indirectamente con la disfunción del glutamato, es decir, trastornos tratables por modulación alostérica positiva (PAM) o por modulación alostérica negativa (NAM) de mGluR5.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862622379P | 2018-01-26 | 2018-01-26 | |
| PCT/EP2019/051134 WO2019145214A1 (en) | 2018-01-26 | 2019-01-17 | TRIAZOLE, IMIDAZOLE AND PYRROLE CONDENSED PIPERAZINE DERIVATIVES AND THEIR USE AS MODULATORS OF mGlu5 RECEPTORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2020007869A true MX2020007869A (es) | 2021-01-08 |
Family
ID=65351993
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020007869A MX2020007869A (es) | 2018-01-26 | 2019-01-17 | Derivados de piperazina condensados con triazol, imidazol y pirrol y su uso como moduladores de receptores mglu5. |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US11591337B2 (es) |
| EP (1) | EP3743429A1 (es) |
| JP (1) | JP7447020B2 (es) |
| KR (1) | KR20200120915A (es) |
| CN (1) | CN112041319A (es) |
| AU (1) | AU2019212093A1 (es) |
| BR (1) | BR112020015230A2 (es) |
| CA (1) | CA3088288A1 (es) |
| EA (1) | EA202091787A1 (es) |
| IL (1) | IL276223B2 (es) |
| MX (1) | MX2020007869A (es) |
| PH (1) | PH12020500600A1 (es) |
| SG (1) | SG11202006622VA (es) |
| WO (1) | WO2019145214A1 (es) |
| ZA (1) | ZA202004768B (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3088288A1 (en) * | 2018-01-26 | 2019-08-01 | Recordati Industria Chimica E Farmaceutica S.P.A | Triazole, imidazole and pyrrole condensed piperazine derivatives and their use as modulators of mglu5 receptors |
| CN113861203B (zh) * | 2021-11-09 | 2023-08-08 | 安徽大学 | 4-芳香炔基取代的7H-吡咯并[2,3-d]嘧啶酰胺类化合物及其制备方法和用途 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1294358T1 (en) | 2000-06-28 | 2004-12-31 | Smithkline Beecham Plc | Wet milling process |
| TW200538108A (en) * | 2004-02-19 | 2005-12-01 | Astrazeneca Ab | Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists |
| TW200801005A (en) * | 2005-08-15 | 2008-01-01 | Astrazeneca Ab | Acetylenic piperazines as metabotropic glutamate receptor antagonists |
| KR20080042158A (ko) | 2005-08-31 | 2008-05-14 | 셀진 코포레이션 | 이소인돌-이미드 화합물과 이를 포함하는 조성물 및 이를이용한 방법 |
| EP2085398A1 (en) * | 2008-02-01 | 2009-08-05 | Merz Pharma GmbH & Co. KGaA | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| EP2090576A1 (en) | 2008-02-01 | 2009-08-19 | Merz Pharma GmbH & Co.KGaA | 6-halo-pyrazolo[1,5-a]pyridines, a process for their preparation and their use as metabotropic glutamate receptor (mGluR) modulators |
| US8455477B2 (en) | 2008-08-05 | 2013-06-04 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| WO2010125102A1 (en) * | 2009-04-29 | 2010-11-04 | Glaxo Group Limited | 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS |
| CN102906093B (zh) | 2010-04-02 | 2016-01-13 | 欧洲筛选有限公司 | Nk-3受体选择性拮抗剂化合物、药物组合物以及在nk-3受体介导的疾病中的使用方法 |
| CN102372716A (zh) | 2010-08-09 | 2012-03-14 | 江苏恒瑞医药股份有限公司 | 酞嗪酮类衍生物、其制备方法及其在医药上的应用 |
| US9539298B2 (en) | 2010-11-29 | 2017-01-10 | Osaka City University | Lissencephaly therapeutic agent |
| WO2012172093A1 (en) * | 2011-06-17 | 2012-12-20 | Merz Pharma Gmbh & Co. Kgaa | Dihydroindolizine derivate as metabotropic glutamate receptor modulators |
| 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 |
| CN106146391A (zh) * | 2015-04-15 | 2016-11-23 | 中国科学院上海药物研究所 | 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 |
| CA3088288A1 (en) * | 2018-01-26 | 2019-08-01 | Recordati Industria Chimica E Farmaceutica S.P.A | Triazole, imidazole and pyrrole condensed piperazine derivatives and their use as modulators of mglu5 receptors |
-
2019
- 2019-01-17 CA CA3088288A patent/CA3088288A1/en active Pending
- 2019-01-17 WO PCT/EP2019/051134 patent/WO2019145214A1/en active Search and Examination
- 2019-01-17 CN CN201980021802.1A patent/CN112041319A/zh active Pending
- 2019-01-17 SG SG11202006622VA patent/SG11202006622VA/en unknown
- 2019-01-17 AU AU2019212093A patent/AU2019212093A1/en active Pending
- 2019-01-17 EA EA202091787A patent/EA202091787A1/ru unknown
- 2019-01-17 US US16/964,337 patent/US11591337B2/en active Active
- 2019-01-17 KR KR1020207024536A patent/KR20200120915A/ko not_active Application Discontinuation
- 2019-01-17 BR BR112020015230-7A patent/BR112020015230A2/pt unknown
- 2019-01-17 JP JP2020562833A patent/JP7447020B2/ja active Active
- 2019-01-17 IL IL276223A patent/IL276223B2/en unknown
- 2019-01-17 MX MX2020007869A patent/MX2020007869A/es unknown
- 2019-01-17 EP EP19703949.8A patent/EP3743429A1/en active Pending
-
2020
- 2020-07-09 PH PH12020500600A patent/PH12020500600A1/en unknown
- 2020-07-31 ZA ZA2020/04768A patent/ZA202004768B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL276223B2 (en) | 2024-03-01 |
| BR112020015230A2 (pt) | 2021-01-26 |
| AU2019212093A1 (en) | 2020-09-10 |
| IL276223A (en) | 2020-09-30 |
| KR20200120915A (ko) | 2020-10-22 |
| PH12020500600A1 (en) | 2021-05-17 |
| EP3743429A1 (en) | 2020-12-02 |
| JP7447020B2 (ja) | 2024-03-11 |
| CA3088288A1 (en) | 2019-08-01 |
| US20210047331A1 (en) | 2021-02-18 |
| IL276223B1 (en) | 2023-11-01 |
| ZA202004768B (en) | 2021-08-25 |
| US11591337B2 (en) | 2023-02-28 |
| CN112041319A (zh) | 2020-12-04 |
| WO2019145214A1 (en) | 2019-08-01 |
| JP2021512942A (ja) | 2021-05-20 |
| SG11202006622VA (en) | 2020-08-28 |
| EA202091787A1 (ru) | 2020-11-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MX2022005827A (es) | Derivados de pirazol como inhibidores de malt1. | |
| MX2021010198A (es) | Indoles n-sustituidos y otros heterociclos para el tratamiento de trastornos cerebrales. | |
| CR20200358A (es) | Compuestos para el tratamiento de trastornos dependientes de cinasas | |
| MX2022002877A (es) | Antagonistas de cinasa progenitora hematopoyetica 1 (hpk1) y sus usos. | |
| PH12020550881A1 (en) | Substituted bicyclic heterocyclic compounds as prmt5 inhibitors | |
| MX2022003166A (es) | Moduladores de il-17a y usos de los mismos. | |
| MX2017014189A (es) | Sulfonas triciclicas como moduladores del receptor huerfano relacionado con retinoide gamma (ror gamma). | |
| CR20200355A (es) | Compuestos para el tratamiento de trastornos dependientes de cinasas | |
| PH12020552207A1 (en) | Pyrazole derivatives as malt1 inhibitors | |
| PH12020552206A1 (en) | Pyrazole derivatives as malt1 inhibitors | |
| PH12020500600A1 (en) | Triazole, imidazole and pyrrole condensed piperazine derivatives and their use as modulators of mglu5 receptors | |
| MX2021000759A (es) | Derivados de triazolquinoxalina adicionalmente sustituidos. | |
| SG10201806809QA (en) | 1-heterocyclyl isochromanyl compounds and analogs for treating cns disorders | |
| CR20200509A (es) | Moduladores alostéricos de espiropiperidina receptores nicotínicos de acetilcolina | |
| MX2020012900A (es) | Potentes inhibidores de d-aminoacido oxidasa (daao) y sus usos. | |
| MX2021000762A (es) | Derivados de triazoloquinoxalina sustituida. | |
| MX2020008746A (es) | Compuestos de sulfonimidoilpurinona 7-sustituidos y sus derivados para el tratamiento y prevencion del cancer de higado. | |
| MX2022005084A (es) | Formas sólidas de un modulador del receptor s1p a. | |
| AU2020288559A8 (en) | Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists | |
| PH12019550251A1 (en) | HETEROCYCLYLMETHYLIDENE DERIVATIVES AND THEIR USE AS MODULATORS OF mGluR5 RECEPTORS | |
| MX2023001906A (es) | Diarilureas como moduladores alostericos de cannabinoide cb1. | |
| MX2020003185A (es) | Nuevos compuestos heterociclicos. | |
| PH12017501209A1 (en) | Heterocyclylalkyne derivatives and their use as modulators of mglur5 receptors | |
| EA202091790A1 (ru) | Соединения для лечения киназозависимых расстройств | |
| MX2021014582A (es) | Derivados de diazepinona como moduladores del ensamblaje de la capside. |