MX347828B - Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento. - Google Patents
Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento.Info
- Publication number
- MX347828B MX347828B MX2014001252A MX2014001252A MX347828B MX 347828 B MX347828 B MX 347828B MX 2014001252 A MX2014001252 A MX 2014001252A MX 2014001252 A MX2014001252 A MX 2014001252A MX 347828 B MX347828 B MX 347828B
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- aza
- phenyl
- metanonas
- hex
- Prior art date
Links
- 229940126601 medicinal product Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 201000000980 schizophrenia Diseases 0.000 abstract 2
- OZGRFPZYTKHWMZ-UHFFFAOYSA-N 2-ethylpentanal Chemical class CCCC(CC)C=O OZGRFPZYTKHWMZ-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 239000004471 Glycine Substances 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
Abstract
Las presentes invenciones se refiere a fenil-3-aza-biciclo[3, 1 ,0]hex3-il-metanonas sustituidas de la fórmula general (I) (ver Fórmula) en donde R1, R2, R3, R4, R5 y R6 son como se describen en la presente o sus sales, con preferencia, sus sales farmacéuticamente aceptables. La invención también se refiere a la preparación de dichos compuestos, composiciones farmacéuticas que comprenden un compuesto de acuerdo con la fórmula general (I) y el uso de dichos compuestos para el tratamiento de diversas condiciones tales como condiciones referidas a síntomas positivos y negativos de esquizofrenia, así como las alteraciones cognitivas asociadas con esquizofrenia, enfermedad de Alzheimer y otros trastornos neurológicos y psiquiátricos. Los compuestos de la invención muestran propiedades inhibidoras del transportador de glicina 1 (GIyT1).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11176468 | 2011-08-03 | ||
| PCT/EP2012/065140 WO2013017657A1 (en) | 2011-08-03 | 2012-08-02 | Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2014001252A MX2014001252A (es) | 2014-05-13 |
| MX347828B true MX347828B (es) | 2017-05-15 |
Family
ID=46598566
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2014001252A MX347828B (es) | 2011-08-03 | 2012-08-02 | Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento. |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US9012489B2 (es) |
| EP (1) | EP2739615B1 (es) |
| JP (1) | JP5850589B2 (es) |
| KR (1) | KR101944686B1 (es) |
| CN (2) | CN105837562B (es) |
| AP (1) | AP2014007399A0 (es) |
| AR (1) | AR087436A1 (es) |
| AU (1) | AU2012292036C1 (es) |
| BR (1) | BR112014001642B1 (es) |
| CA (1) | CA2843805C (es) |
| CL (1) | CL2014000246A1 (es) |
| CO (1) | CO6870037A2 (es) |
| CY (1) | CY1119326T1 (es) |
| DK (1) | DK2739615T3 (es) |
| EA (1) | EA024933B1 (es) |
| EC (1) | ECSP14013221A (es) |
| ES (1) | ES2623006T3 (es) |
| GE (1) | GEP20166483B (es) |
| HR (1) | HRP20170695T1 (es) |
| HU (1) | HUE033134T2 (es) |
| IL (1) | IL229962A (es) |
| LT (1) | LT2739615T (es) |
| MA (1) | MA35286B1 (es) |
| ME (1) | ME02672B (es) |
| MX (1) | MX347828B (es) |
| MY (1) | MY167396A (es) |
| PE (1) | PE20141352A1 (es) |
| PH (1) | PH12014500276A1 (es) |
| PL (1) | PL2739615T3 (es) |
| PT (1) | PT2739615T (es) |
| RS (1) | RS55927B1 (es) |
| SI (1) | SI2739615T1 (es) |
| TN (1) | TN2014000044A1 (es) |
| TW (1) | TWI543974B (es) |
| UA (1) | UA114405C2 (es) |
| UY (1) | UY34239A (es) |
| WO (1) | WO2013017657A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106455572B (zh) | 2014-06-06 | 2020-01-14 | 巴斯夫欧洲公司 | 取代噁二唑在防除植物病原性真菌中的用途 |
| AR106679A1 (es) | 2015-11-13 | 2018-02-07 | Basf Se | Oxadiazoles sustituidos para combatir hongos fitopatógenos |
| US10492494B2 (en) | 2015-11-13 | 2019-12-03 | Basf Se | Substituted oxadiazoles for combating phytopathogenic fungi |
| BR112018008449B1 (pt) | 2015-11-19 | 2021-07-06 | Basf Se | Compostos de fórmula i, mistura, composição agroquímica e método para combater fungos nocivos fitopatogênicos |
| CN108884062A (zh) | 2016-04-11 | 2018-11-23 | 巴斯夫欧洲公司 | 用于防治植物病原性真菌的取代噁二唑类 |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| US11447474B2 (en) * | 2019-05-01 | 2022-09-20 | Boehringer Ingelheim International Gmbh | Solid forms of a GlyT1 inhibitor |
| CN115279372A (zh) | 2020-01-09 | 2022-11-01 | 迪斯克医药公司 | 用甘氨酸转运蛋白抑制剂治疗红细胞生成性原卟啉病、x连锁原卟啉病或先天性红细胞生成性卟啉病的方法 |
| EP4196118A1 (en) * | 2020-08-13 | 2023-06-21 | Boehringer Ingelheim International GmbH | Treatment of cognitive impairement associated with schizophrenia |
| JP2023545808A (ja) | 2020-10-13 | 2023-10-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 再加工方法 |
| EP4436564A4 (en) * | 2021-11-24 | 2025-10-22 | Maplight Therapeutics Inc | METHODS OF TREATMENT OF NEUROLOGICAL DISORDERS |
| CN114957087A (zh) * | 2022-04-13 | 2022-08-30 | 湖南复瑞生物医药技术有限责任公司 | 一种帕罗韦德中间体制备方法 |
| WO2023237103A1 (zh) * | 2022-06-10 | 2023-12-14 | 成都百裕制药股份有限公司 | 吡咯烷衍生物、药物组合物及其在医药上的应用 |
| AU2023328948A1 (en) | 2022-08-24 | 2025-01-16 | Boehringer Ingelheim International Gmbh | A scalable process for the preparation of a glyt-1 inhibitor |
| AU2024274586A1 (en) * | 2023-05-25 | 2026-01-15 | Maplight Therapeutics, Inc. | Compositions for treating neurological disorders |
| WO2025140479A1 (zh) * | 2023-12-29 | 2025-07-03 | 苏州科睿思制药有限公司 | Iclepertin的晶型及其制备方法和用途 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100406009C (zh) * | 2003-04-10 | 2008-07-30 | 兰贝克赛实验室有限公司 | 作为毒蕈碱受体拮抗剂的取代的氮杂双环己烷衍生物 |
| UA86037C2 (ru) * | 2003-10-14 | 2009-03-25 | Пфайзер Продактс Инк. | Бициклические [3.1.0] производные, как ингибиторы переносчика глицина |
| DE102004035280A1 (de) | 2004-07-21 | 2006-03-16 | Robert Bosch Gmbh | Kraftstoffinjektor mit direkter mehrstufiger Einspritzventilgliedansteuerung |
| JP2008526795A (ja) * | 2005-01-06 | 2008-07-24 | エフ．ホフマン−ラ ロシュ アーゲー | 神経障害および神経精神疾患を処置するためのグリシントランスポータ１（ｇｌｙｔ−１）阻害物質としての、スルファニル置換フェニルメタノン |
| CA2593463C (en) * | 2005-01-07 | 2013-10-08 | F. Hoffmann-La Roche Ag | [4-(heteroaryl) piperazin-1-yl]-(2,5-substituted -phenyl)methanone derivatives as glycine transporter 1 (glyt-1) inhibitors for the treatment of neurological and neuropsychiatric disorders |
| RU2405771C2 (ru) * | 2005-02-07 | 2010-12-10 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические замещенные фенилметаноны в качестве ингибиторов переносчика глицина 1 |
| EP2035371B1 (en) * | 2006-06-22 | 2013-03-06 | F. Hoffmann-La Roche AG | Substituted phenyl methanone derivatives and their use as glyt1 and glyt2 receptor inhibitors |
| KR101086589B1 (ko) | 2006-06-28 | 2011-11-23 | 암젠 인크 | 글리신 수송자-1 억제제 |
| AR064561A1 (es) * | 2006-12-28 | 2009-04-08 | Actelion Pharmaceuticals Ltd | Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina. |
| UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| WO2010078348A1 (en) * | 2008-12-29 | 2010-07-08 | Vanderbilt University | 3.1.0 bicyclic glyt1 inhibitors and methods of making and using same |
| BRPI1007410A2 (pt) | 2009-01-27 | 2016-02-16 | Hoffmann La Roche | piperidinas aroilamino- e heteroaroilamino-substituídas como inibidores de glyt-1 |
-
2012
- 2012-07-27 US US13/560,063 patent/US9012489B2/en active Active
- 2012-08-01 TW TW101127831A patent/TWI543974B/zh active
- 2012-08-02 HR HRP20170695TT patent/HRP20170695T1/hr unknown
- 2012-08-02 PL PL12741022T patent/PL2739615T3/pl unknown
- 2012-08-02 ES ES12741022.3T patent/ES2623006T3/es active Active
- 2012-08-02 WO PCT/EP2012/065140 patent/WO2013017657A1/en not_active Ceased
- 2012-08-02 RS RS20170472A patent/RS55927B1/sr unknown
- 2012-08-02 SI SI201230968A patent/SI2739615T1/sl unknown
- 2012-08-02 AR ARP120102828 patent/AR087436A1/es active IP Right Grant
- 2012-08-02 CA CA2843805A patent/CA2843805C/en active Active
- 2012-08-02 LT LTEP12741022.3T patent/LT2739615T/lt unknown
- 2012-08-02 DK DK12741022.3T patent/DK2739615T3/en active
- 2012-08-02 PT PT127410223T patent/PT2739615T/pt unknown
- 2012-08-02 UA UAA201402017A patent/UA114405C2/uk unknown
- 2012-08-02 EP EP12741022.3A patent/EP2739615B1/en active Active
- 2012-08-02 PE PE2014000158A patent/PE20141352A1/es active IP Right Grant
- 2012-08-02 GE GEAP201213402A patent/GEP20166483B/en unknown
- 2012-08-02 HU HUE12741022A patent/HUE033134T2/en unknown
- 2012-08-02 PH PH1/2014/500276A patent/PH12014500276A1/en unknown
- 2012-08-02 CN CN201610214305.1A patent/CN105837562B/zh active Active
- 2012-08-02 BR BR112014001642-9A patent/BR112014001642B1/pt active IP Right Grant
- 2012-08-02 MY MYPI2014000271A patent/MY167396A/en unknown
- 2012-08-02 AU AU2012292036A patent/AU2012292036C1/en active Active
- 2012-08-02 CN CN201280042794.7A patent/CN103797005B/zh active Active
- 2012-08-02 AP AP2014007399A patent/AP2014007399A0/xx unknown
- 2012-08-02 JP JP2014523332A patent/JP5850589B2/ja active Active
- 2012-08-02 ME MEP-2017-92A patent/ME02672B/me unknown
- 2012-08-02 KR KR1020147002515A patent/KR101944686B1/ko active Active
- 2012-08-02 EA EA201400183A patent/EA024933B1/ru not_active IP Right Cessation
- 2012-08-02 MX MX2014001252A patent/MX347828B/es active IP Right Grant
- 2012-08-03 UY UY34239A patent/UY34239A/es unknown
-
2013
- 2013-12-17 IL IL229962A patent/IL229962A/en active IP Right Grant
-
2014
- 2014-01-31 TN TNP2014000044A patent/TN2014000044A1/en unknown
- 2014-01-31 MA MA36719A patent/MA35286B1/fr unknown
- 2014-01-31 CL CL2014000246A patent/CL2014000246A1/es unknown
- 2014-02-03 CO CO14022058A patent/CO6870037A2/es active IP Right Grant
- 2014-02-26 EC ECSP14013221 patent/ECSP14013221A/es unknown
-
2017
- 2017-06-06 CY CY20171100591T patent/CY1119326T1/el unknown
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