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
Classifications
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- 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) | CN103797005B (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) |
| HK (1) | HK1193100A1 (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) |
| 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 (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3756464A1 (en) | 2014-06-06 | 2020-12-30 | Basf Se | Substituted oxadiazoles for combating phytopathogenic fungi |
| 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 |
| CA3003949A1 (en) | 2015-11-19 | 2017-05-26 | Basf Se | Substituted oxadiazoles for combating phytopathogenic fungi |
| RU2018138748A (ru) | 2016-04-11 | 2020-05-12 | Басф Се | Замещенные оксадиазолы для борьбы с фитопатогенными грибами |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| AU2020266566A1 (en) * | 2019-05-01 | 2021-11-11 | Boehringer Ingelheim International Gmbh | Solid forms of a GlyT1 inhibitor |
| AU2021205510A1 (en) | 2020-01-09 | 2022-07-21 | Disc Medicine, Inc. | Methods of treating erythropoietic protoporphyria, X-linked protoporphyria, or congenital erythropoietic porphyria with glycine transport inhibitors |
| WO2022034146A1 (en) | 2020-08-13 | 2022-02-17 | Boehringer Ingelheim International Gmbh | Treatment of cognitive impairement associated with schizophrenia |
| BR112023004774A2 (pt) | 2020-10-13 | 2023-04-25 | Boehringer Ingelheim Int | Processo de retrabalho |
| EP4436564A1 (en) * | 2021-11-24 | 2024-10-02 | MapLight Therapeutics, Inc. | Methods of treating 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 |
| WO2024042043A1 (en) | 2022-08-24 | 2024-02-29 | Boehringer Ingelheim International Gmbh | A scalable process for the preparation of a glyt-1 inhibitor |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE362364T1 (de) | 2003-04-10 | 2007-06-15 | Ranbaxy Lab 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 |
| EP1836178A1 (en) * | 2005-01-06 | 2007-09-26 | F. Hoffmann-Roche AG | Sulfanyl substituted phenyl methanones as glycine transporter 1 (glyt-1) inhibitors for the treatment of neurological and neuropsychiatric disorders |
| CN101137363B (zh) * | 2005-01-07 | 2010-09-15 | 弗·哈夫曼-拉罗切有限公司 | 作为甘氨酸转运体1(GlyT-1)抑制剂用于治疗神经学和神经精神病学障碍的[4-(杂芳基)哌嗪-1-基]-(2,5-取代的-苯基)甲酮衍生物 |
| DE602006010665D1 (en) * | 2005-02-07 | 2010-01-07 | Hoffmann La Roche | Heterocyclsche substituierte phenylmethanone als inhibitoren des glycintransporters 1 |
| RU2437872C2 (ru) * | 2006-06-22 | 2011-12-27 | Ф. Хоффманн-Ля Рош Аг | Замещенные производные фенилметанона |
| EP2041088B1 (en) | 2006-06-28 | 2014-01-08 | Amgen Inc. | Glycine transporter-1 inhibitors |
| TW200833328A (en) * | 2006-12-28 | 2008-08-16 | Actelion Pharmaceuticals Ltd | 2-aza-bicyclo[3.1.0]hexane derivatives |
| 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 |
| CN102271677A (zh) * | 2008-12-29 | 2011-12-07 | 凡德贝尔大学 | 3.1.0双环G1yT1抑制剂及其制备和使用方法 |
| MA32947B1 (fr) | 2009-01-27 | 2012-01-02 | Hoffmann La Roche | Piperidines substitues par aroylamino et heteroaroylamino comme inhibiteurs de glyt-1 |
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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 EA EA201400183A patent/EA024933B1/ru not_active IP Right Cessation
- 2012-08-02 KR KR1020147002515A patent/KR101944686B1/ko active IP Right Grant
- 2012-08-02 WO PCT/EP2012/065140 patent/WO2013017657A1/en active Application Filing
- 2012-08-02 MX MX2014001252A patent/MX347828B/es active IP Right Grant
- 2012-08-02 DK DK12741022.3T patent/DK2739615T3/en active
- 2012-08-02 MY MYPI2014000271A patent/MY167396A/en unknown
- 2012-08-02 HU HUE12741022A patent/HUE033134T2/en unknown
- 2012-08-02 ES ES12741022.3T patent/ES2623006T3/es active Active
- 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 SI SI201230968A patent/SI2739615T1/sl unknown
- 2012-08-02 AR ARP120102828 patent/AR087436A1/es active IP Right Grant
- 2012-08-02 JP JP2014523332A patent/JP5850589B2/ja active Active
- 2012-08-02 LT LTEP12741022.3T patent/LT2739615T/lt unknown
- 2012-08-02 AP AP2014007399A patent/AP2014007399A0/xx unknown
- 2012-08-02 ME MEP-2017-92A patent/ME02672B/me unknown
- 2012-08-02 GE GEAP201213402A patent/GEP20166483B/en unknown
- 2012-08-02 RS RS20170472A patent/RS55927B1/sr unknown
- 2012-08-02 UA UAA201402017A patent/UA114405C2/uk unknown
- 2012-08-02 CN CN201280042794.7A patent/CN103797005B/zh active Active
- 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 PL PL12741022T patent/PL2739615T3/pl unknown
- 2012-08-02 PT PT127410223T patent/PT2739615T/pt unknown
- 2012-08-02 BR BR112014001642-9A patent/BR112014001642B1/pt active IP Right Grant
- 2012-08-03 UY UY34239A patent/UY34239A/es unknown
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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
- 2014-07-02 HK HK14106631.6A patent/HK1193100A1/zh unknown
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2017
- 2017-05-10 HR HRP20170695TT patent/HRP20170695T1/hr unknown
- 2017-06-06 CY CY20171100591T patent/CY1119326T1/el unknown
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