EA201400183A1 - Фенил-3-азабицикло[3.1.0]гекс-3-илметаноны и их применение в качестве лекарственного средства - Google Patents
Фенил-3-азабицикло[3.1.0]гекс-3-илметаноны и их применение в качестве лекарственного средстваInfo
- Publication number
- EA201400183A1 EA201400183A1 EA201400183A EA201400183A EA201400183A1 EA 201400183 A1 EA201400183 A1 EA 201400183A1 EA 201400183 A EA201400183 A EA 201400183A EA 201400183 A EA201400183 A EA 201400183A EA 201400183 A1 EA201400183 A1 EA 201400183A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- application
- azabicyclo
- hex
- phenyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 4
- 102000010726 Glycine Plasma Membrane Transport Proteins Human genes 0.000 abstract 2
- 108010063380 Glycine Plasma Membrane Transport Proteins Proteins 0.000 abstract 2
- 230000001575 pathological effect Effects 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
- 208000028698 Cognitive impairment Diseases 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
- 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
В заявке описаны замещенные фенил-3-азабицикло[3,1,0]гекс-3-илметаноны общей формулы (I)в которой R, R, R, R, Rи Rявляются такими, как описано в настоящем изобретении, и их соли, предпочтительно их фармацевтически приемлемые соли. В заявке также описаны получение указанных соединений, фармацевтические композиции, содержащие соединения общей формулы (I), и применение указанных соединений для лечения различных патологических состояний, таких как патологические состояния, связанные с позитивными и негативными симптомами шизофрении, а также нарушений познавательной способности, связанных с шизофренией, болезнью Альцгеймера и другими неврологическими и психическими нарушениями. Соединения, предлагаемые в настоящем изобретении, обладают способностью ингибировать переносчик-1 глицина (GlyT1).
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 |
|---|---|
| EA201400183A1 true EA201400183A1 (ru) | 2014-06-30 |
| EA024933B1 EA024933B1 (ru) | 2016-11-30 |
Family
ID=46598566
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201400183A EA024933B1 (ru) | 2011-08-03 | 2012-08-02 | Фенил-3-азабицикло[3.1.0]гекс-3-илметаноны и их применение в качестве лекарственного средства |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US9012489B2 (ru) |
| EP (1) | EP2739615B1 (ru) |
| JP (1) | JP5850589B2 (ru) |
| KR (1) | KR101944686B1 (ru) |
| CN (2) | CN105837562B (ru) |
| AP (1) | AP2014007399A0 (ru) |
| AR (1) | AR087436A1 (ru) |
| AU (1) | AU2012292036C1 (ru) |
| BR (1) | BR112014001642B1 (ru) |
| CA (1) | CA2843805C (ru) |
| CL (1) | CL2014000246A1 (ru) |
| CO (1) | CO6870037A2 (ru) |
| CY (1) | CY1119326T1 (ru) |
| DK (1) | DK2739615T3 (ru) |
| EA (1) | EA024933B1 (ru) |
| EC (1) | ECSP14013221A (ru) |
| ES (1) | ES2623006T3 (ru) |
| GE (1) | GEP20166483B (ru) |
| HR (1) | HRP20170695T1 (ru) |
| HU (1) | HUE033134T2 (ru) |
| IL (1) | IL229962A (ru) |
| LT (1) | LT2739615T (ru) |
| MA (1) | MA35286B1 (ru) |
| ME (1) | ME02672B (ru) |
| MX (1) | MX347828B (ru) |
| MY (1) | MY167396A (ru) |
| PE (1) | PE20141352A1 (ru) |
| PH (1) | PH12014500276A1 (ru) |
| PL (1) | PL2739615T3 (ru) |
| PT (1) | PT2739615T (ru) |
| RS (1) | RS55927B1 (ru) |
| SI (1) | SI2739615T1 (ru) |
| TN (1) | TN2014000044A1 (ru) |
| TW (1) | TWI543974B (ru) |
| UA (1) | UA114405C2 (ru) |
| UY (1) | UY34239A (ru) |
| WO (1) | WO2013017657A1 (ru) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3151669T3 (pl) | 2014-06-06 | 2021-04-19 | Basf Se | Zastosowanie podstawionych oksadiazoli do zwalczania fitopatogennych grzybów |
| AR106679A1 (es) | 2015-11-13 | 2018-02-07 | Basf Se | Oxadiazoles sustituidos para combatir hongos fitopatógenos |
| EP3373735A1 (en) | 2015-11-13 | 2018-09-19 | Basf Se | Substituted oxadiazoles for combating phytopathogenic fungi |
| EA201891146A1 (ru) | 2015-11-19 | 2018-12-28 | Басф Се | Замещенные оксадиазолы для борьбы с фитопатогенными грибами |
| AU2017250397A1 (en) | 2016-04-11 | 2018-10-11 | Basf Se | Substituted oxadiazoles for combating phytopathogenic fungi |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| CN113784966B (zh) | 2019-05-01 | 2024-07-19 | 勃林格殷格翰国际有限公司 | Glyt1抑制剂的固体形式 |
| KR20220125326A (ko) | 2020-01-09 | 2022-09-14 | 디스크 메디슨, 인크. | 적혈구형성 프로토포르피린증, x-연계된 프로토포르피린증, 또는 선천성 적혈구 조혈포르피린증을 글리신 운반 억제제로 치료하는 방법 |
| CA3188340A1 (en) * | 2020-08-13 | 2022-02-17 | Boehringer Ingelheim International Gmbh | Treatment of cognitive impairement associated with schizophrenia |
| CA3195702A1 (en) | 2020-10-13 | 2022-04-21 | Boehringer Ingelheim International Gmbh | Process of reworking |
| MX2024006371A (es) * | 2021-11-24 | 2024-07-15 | Maplight Therapeutics Inc | Métodos para tratar trastornos neurológicos. |
| 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 |
| TW202348602A (zh) * | 2022-06-10 | 2023-12-16 | 大陸商成都百裕製藥股份有限公司 | 吡咯烷衍生物、藥物组合物及其製藥用途 |
| WO2024042043A1 (en) | 2022-08-24 | 2024-02-29 | Boehringer Ingelheim International Gmbh | A scalable process for the preparation of a glyt-1 inhibitor |
| CN121443286A (zh) * | 2023-05-25 | 2026-01-30 | 地图之光治疗股份有限公司 | 用于治疗神经障碍的组合物 |
| 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 |
|---|---|---|---|---|
| DE60313898T2 (de) | 2003-04-10 | 2008-01-17 | Ranbaxy Laboratories, Ltd. | Substituierte azabicyclo hexane derivate als muscarin rezeptor antagonisten |
| KR20060095865A (ko) | 2003-10-14 | 2006-09-04 | 화이자 프로덕츠 인크. | 글리신 수송 억제제로서의 비시클릭 [3.1.0] 유도체 |
| DE102004035280A1 (de) | 2004-07-21 | 2006-03-16 | Robert Bosch Gmbh | Kraftstoffinjektor mit direkter mehrstufiger Einspritzventilgliedansteuerung |
| CA2593453A1 (en) * | 2005-01-06 | 2006-07-13 | F. Hoffmann-La Roche Ag | Sulfanyl substituted phenyl methanones as glycine transporter 1 (glyt-1) inhibitors for the treatment of neurological and neuropsychiatric disorders |
| AU2005324024B2 (en) * | 2005-01-07 | 2011-02-17 | 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 |
| DE602006010665D1 (en) * | 2005-02-07 | 2010-01-07 | Hoffmann La Roche | Heterocyclsche substituierte phenylmethanone als inhibitoren des glycintransporters 1 |
| KR101072796B1 (ko) * | 2006-06-22 | 2011-10-14 | 에프. 호프만-라 로슈 아게 | 치환된 페닐 메탄온 유도체 |
| NZ573129A (en) | 2006-06-28 | 2011-06-30 | Amgen Inc | Piperazine acetic acid glycine transporter-1 inhibitors |
| CL2007003827A1 (es) * | 2006-12-28 | 2008-09-26 | Actelion Pharmaceuticals Ltd | Compuestos derivados de n-(2-aza-biciclo(3.1.0)hex-3-ilmetil)amida; y su uso para prevenir o tratar la depresion, neurosis, esquizofrenia, ansiedad, adicciones, epilepsia, dolor, enfermedades cardiacas, entre otras. |
| 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 |
| UA104611C2 (en) | 2009-01-27 | 2014-02-25 | Ф. Хоффманн-Ля Рош Аг | Aroylamino- and heteroaroylamino-substituted piperidines as glyt-1 inhibitors |
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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 PE PE2014000158A patent/PE20141352A1/es active IP Right Grant
- 2012-08-02 CN CN201610214305.1A patent/CN105837562B/zh active Active
- 2012-08-02 EA EA201400183A patent/EA024933B1/ru not_active IP Right Cessation
- 2012-08-02 WO PCT/EP2012/065140 patent/WO2013017657A1/en not_active Ceased
- 2012-08-02 CA CA2843805A patent/CA2843805C/en active Active
- 2012-08-02 AU AU2012292036A patent/AU2012292036C1/en active Active
- 2012-08-02 EP EP12741022.3A patent/EP2739615B1/en active Active
- 2012-08-02 AP AP2014007399A patent/AP2014007399A0/xx unknown
- 2012-08-02 KR KR1020147002515A patent/KR101944686B1/ko active Active
- 2012-08-02 RS RS20170472A patent/RS55927B1/sr unknown
- 2012-08-02 LT LTEP12741022.3T patent/LT2739615T/lt unknown
- 2012-08-02 ES ES12741022.3T patent/ES2623006T3/es active Active
- 2012-08-02 PT PT127410223T patent/PT2739615T/pt unknown
- 2012-08-02 BR BR112014001642-9A patent/BR112014001642B1/pt active IP Right Grant
- 2012-08-02 MX MX2014001252A patent/MX347828B/es active IP Right Grant
- 2012-08-02 UA UAA201402017A patent/UA114405C2/uk unknown
- 2012-08-02 GE GEAP201213402A patent/GEP20166483B/en unknown
- 2012-08-02 DK DK12741022.3T patent/DK2739615T3/en active
- 2012-08-02 MY MYPI2014000271A patent/MY167396A/en unknown
- 2012-08-02 CN CN201280042794.7A patent/CN103797005B/zh active Active
- 2012-08-02 HU HUE12741022A patent/HUE033134T2/en unknown
- 2012-08-02 JP JP2014523332A patent/JP5850589B2/ja active Active
- 2012-08-02 SI SI201230968A patent/SI2739615T1/sl unknown
- 2012-08-02 PH PH1/2014/500276A patent/PH12014500276A1/en unknown
- 2012-08-02 PL PL12741022T patent/PL2739615T3/pl unknown
- 2012-08-02 AR ARP120102828 patent/AR087436A1/es active IP Right Grant
- 2012-08-02 ME MEP-2017-92A patent/ME02672B/me unknown
- 2012-08-03 UY UY34239A patent/UY34239A/es unknown
-
2013
- 2013-12-17 IL IL229962A patent/IL229962A/en active IP Right Grant
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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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