UA114405C2 - Феніл-3-азабіцикло[3.1.0]гекс-3-илметанони та їх застосування як лікарського засобу - Google Patents
Феніл-3-азабіцикло[3.1.0]гекс-3-илметанони та їх застосування як лікарського засобуInfo
- Publication number
- UA114405C2 UA114405C2 UAA201402017A UAA201402017A UA114405C2 UA 114405 C2 UA114405 C2 UA 114405C2 UA A201402017 A UAA201402017 A UA A201402017A UA A201402017 A UAA201402017 A UA A201402017A UA 114405 C2 UA114405 C2 UA 114405C2
- Authority
- UA
- Ukraine
- Prior art keywords
- compounds
- hex
- schizophrenia
- general formula
- phenyl
- Prior art date
Links
- 229940126601 medicinal product Drugs 0.000 title 1
- 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
- 150000003839 salts Chemical class 0.000 abstract 2
- 201000000980 schizophrenia Diseases 0.000 abstract 2
- PZWNQSJXMXNUAT-UHFFFAOYSA-N 3-azabicyclo[3.1.0]hexan-3-yl(phenyl)methanone Chemical class C1C2CC2CN1C(=O)C1=CC=CC=C1 PZWNQSJXMXNUAT-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
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 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
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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
У заявці описані заміщені феніл-3-азабіцикло[3.1.0]гекс-3-илметанони загальної формули (І) EMBED ISISServer , (I) в якій R1, R2, R3, R4, R5 i R6 є такими, як описано в даному винаході, і їх солі, краще їх фармацевтично прийнятні солі. У заявці також описані отримання зазначених сполук, фармацевтичні композиції, що містять сполуки загальної формули (І), і застосування зазначених сполук для лікування різних патологічних станів, таких як патологічні стани, пов'язані з позитивними і негативними симптомами шизофренії, а також порушень пізнавальної здатності, пов'язаних із шизофренією, хворобою Альцгеймера і іншими неврологічними і психічними порушеннями. Сполуки, запропоновані в даному винаході, мають здатність інгібувати переносник-1 гліцину (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 (1)
| Publication Number | Publication Date |
|---|---|
| UA114405C2 true UA114405C2 (uk) | 2017-06-12 |
Family
ID=46598566
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA201402017A UA114405C2 (uk) | 2011-08-03 | 2012-08-02 | Феніл-3-азабіцикло[3.1.0]гекс-3-илметанони та їх застосування як лікарського засобу |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US9012489B2 (uk) |
| EP (1) | EP2739615B1 (uk) |
| JP (1) | JP5850589B2 (uk) |
| KR (1) | KR101944686B1 (uk) |
| CN (2) | CN105837562B (uk) |
| AP (1) | AP2014007399A0 (uk) |
| AR (1) | AR087436A1 (uk) |
| AU (1) | AU2012292036C1 (uk) |
| BR (1) | BR112014001642B1 (uk) |
| CA (1) | CA2843805C (uk) |
| CL (1) | CL2014000246A1 (uk) |
| CO (1) | CO6870037A2 (uk) |
| CY (1) | CY1119326T1 (uk) |
| DK (1) | DK2739615T3 (uk) |
| EA (1) | EA024933B1 (uk) |
| EC (1) | ECSP14013221A (uk) |
| ES (1) | ES2623006T3 (uk) |
| GE (1) | GEP20166483B (uk) |
| HR (1) | HRP20170695T1 (uk) |
| HU (1) | HUE033134T2 (uk) |
| IL (1) | IL229962A (uk) |
| LT (1) | LT2739615T (uk) |
| MA (1) | MA35286B1 (uk) |
| ME (1) | ME02672B (uk) |
| MX (1) | MX347828B (uk) |
| MY (1) | MY167396A (uk) |
| PE (1) | PE20141352A1 (uk) |
| PH (1) | PH12014500276A1 (uk) |
| PL (1) | PL2739615T3 (uk) |
| PT (1) | PT2739615T (uk) |
| RS (1) | RS55927B1 (uk) |
| SI (1) | SI2739615T1 (uk) |
| TN (1) | TN2014000044A1 (uk) |
| TW (1) | TWI543974B (uk) |
| UA (1) | UA114405C2 (uk) |
| UY (1) | UY34239A (uk) |
| WO (1) | WO2013017657A1 (uk) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112016027983B1 (pt) | 2014-06-06 | 2021-11-03 | Basf Se | Uso dos compostos, composição agroquímica e método para o combate dos fungos fitopatogênicos |
| 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 |
| WO2017085100A1 (en) | 2015-11-19 | 2017-05-26 | Basf Se | Substituted oxadiazoles for combating phytopathogenic fungi |
| BR112018069897B1 (pt) | 2016-04-11 | 2023-01-17 | Basf Se | Composto de fórmula i, composição agroquímica, processo para a preparação de compostos de fórmula i, uso não terapêutico de compostos e método para o combate de fungos fitopatogênicos nocivos |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| AU2020266566B2 (en) * | 2019-05-01 | 2025-11-06 | Boehringer Ingelheim International Gmbh | Solid forms of a GlyT1 inhibitor |
| US11813257B2 (en) | 2020-01-09 | 2023-11-14 | Disc Medicine, Inc. | Methods of treating erythropoietic protoporphyria, X-linked protoporphyria, or congenital erythropoietic porphyria with glycine transport inhibitors |
| US12059408B2 (en) * | 2020-08-13 | 2024-08-13 | Boehringer Ingelheim International Gmbh | Treatment of cognitive impairment associated with schizophrenia |
| WO2022078927A1 (en) | 2020-10-13 | 2022-04-21 | Boehringer Ingelheim International Gmbh | Process of reworking |
| 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 |
| WO2024243600A2 (en) * | 2023-05-25 | 2024-11-28 | 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 |
|---|---|---|---|---|
| CA2521788A1 (en) * | 2003-04-10 | 2004-10-21 | Ranbaxy Laboratories Limited | Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists |
| ES2634841T3 (es) | 2003-10-14 | 2017-09-29 | Pfizer Products Inc. | Derivados bicíclicos [3.1.0] como inhibidores del transportador de glicina |
| 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 |
| BRPI0519794A2 (pt) * | 2005-01-07 | 2009-03-17 | Hoffmann La Roche | derivados de [4-(heteroaril)piperazin-1-il]-(fenil 2,5-substituìdo)metanona como inibidores de transportador de glicina 1 (glyt-1) para o tratamento de distúrbios neurológicos e neuropsiquiátricos |
| DK1848694T3 (da) * | 2005-02-07 | 2010-01-25 | Hoffmann La Roche | Heterocykliske substituerede phenylmethanoner som inhibitorer af glycintransporter |
| ES2406085T3 (es) * | 2006-06-22 | 2013-06-05 | F. Hoffmann-La Roche Ag | Derivados de fenil-metanona sustituida y su empleo como inhibidores de receptores de GlyT1 y GlyT2 |
| JP5179486B2 (ja) | 2006-06-28 | 2013-04-10 | アムジエン・インコーポレーテツド | グリシン輸送体−１阻害剤 |
| 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 |
| RU2011124709A (ru) * | 2008-12-29 | 2013-02-10 | Вандербилт Юниверсити | ДВУЯДЕРНЫЕ ИНГИБИТОРЫ GlyT1 И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
| RU2517701C2 (ru) | 2009-01-27 | 2014-05-27 | Ф. Хоффманн-Ля Рош Аг | Ароиламино- и гетероароиламино-замещенные пиперидины в качестве ингибиторов 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 AR ARP120102828 patent/AR087436A1/es active IP Right Grant
- 2012-08-02 ES ES12741022.3T patent/ES2623006T3/es active Active
- 2012-08-02 UA UAA201402017A patent/UA114405C2/uk unknown
- 2012-08-02 PH PH1/2014/500276A patent/PH12014500276A1/en unknown
- 2012-08-02 PT PT127410223T patent/PT2739615T/pt unknown
- 2012-08-02 DK DK12741022.3T patent/DK2739615T3/en active
- 2012-08-02 PE PE2014000158A patent/PE20141352A1/es active IP Right Grant
- 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 LT LTEP12741022.3T patent/LT2739615T/lt unknown
- 2012-08-02 PL PL12741022T patent/PL2739615T3/pl unknown
- 2012-08-02 SI SI201230968A patent/SI2739615T1/sl unknown
- 2012-08-02 AU AU2012292036A patent/AU2012292036C1/en active Active
- 2012-08-02 MY MYPI2014000271A patent/MY167396A/en unknown
- 2012-08-02 EP EP12741022.3A patent/EP2739615B1/en active Active
- 2012-08-02 JP JP2014523332A patent/JP5850589B2/ja active Active
- 2012-08-02 HU HUE12741022A patent/HUE033134T2/en unknown
- 2012-08-02 MX MX2014001252A patent/MX347828B/es active IP Right Grant
- 2012-08-02 CN CN201610214305.1A patent/CN105837562B/zh active Active
- 2012-08-02 AP AP2014007399A patent/AP2014007399A0/xx unknown
- 2012-08-02 KR KR1020147002515A patent/KR101944686B1/ko active Active
- 2012-08-02 BR BR112014001642-9A patent/BR112014001642B1/pt active IP Right Grant
- 2012-08-02 GE GEAP201213402A patent/GEP20166483B/en unknown
- 2012-08-02 ME MEP-2017-92A patent/ME02672B/me unknown
- 2012-08-02 CN CN201280042794.7A patent/CN103797005B/zh active Active
- 2012-08-02 HR HRP20170695TT patent/HRP20170695T1/hr unknown
- 2012-08-02 RS RS20170472A patent/RS55927B1/sr unknown
- 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 MA MA36719A patent/MA35286B1/fr unknown
- 2014-01-31 CL CL2014000246A patent/CL2014000246A1/es unknown
- 2014-01-31 TN TNP2014000044A patent/TN2014000044A1/en unknown
- 2014-02-03 CO CO14022058A patent/CO6870037A2/es active IP Right Grant
- 2014-02-26 EC ECSP14013221 patent/ECSP14013221A/es unknown
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2017
- 2017-06-06 CY CY20171100591T patent/CY1119326T1/el unknown
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