JP7023876B2 - α5含有GABAA受容体アゴニストによる神経変性および神経精神障害における認知症状および気分症状の処置 - Google Patents
α5含有GABAA受容体アゴニストによる神経変性および神経精神障害における認知症状および気分症状の処置 Download PDFInfo
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- JP7023876B2 JP7023876B2 JP2018568186A JP2018568186A JP7023876B2 JP 7023876 B2 JP7023876 B2 JP 7023876B2 JP 2018568186 A JP2018568186 A JP 2018568186A JP 2018568186 A JP2018568186 A JP 2018568186A JP 7023876 B2 JP7023876 B2 JP 7023876B2
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- BGYVDFYYQYICIR-UHFFFAOYSA-N C#Cc(cc1)cc(C(c2ncccc2)=NC2)c1-[n]1c2c(C(N)=O)nc1 Chemical compound C#Cc(cc1)cc(C(c2ncccc2)=NC2)c1-[n]1c2c(C(N)=O)nc1 BGYVDFYYQYICIR-UHFFFAOYSA-N 0.000 description 2
- 0 CCc1n[o]c(-c(nc2)c(CN=C(c3c4)c5ccc(C**)cn5)[n]2-c3ccc4C#C)n1 Chemical compound CCc1n[o]c(-c(nc2)c(CN=C(c3c4)c5ccc(C**)cn5)[n]2-c3ccc4C#C)n1 0.000 description 2
- TUGXBMPGOAZFBE-UHFFFAOYSA-N C#Cc(cc1)cc(C(c(cccc2)c2I)=NC2)c1-[n]1c2c(C(N)=O)nc1 Chemical compound C#Cc(cc1)cc(C(c(cccc2)c2I)=NC2)c1-[n]1c2c(C(N)=O)nc1 TUGXBMPGOAZFBE-UHFFFAOYSA-N 0.000 description 1
- FFEOWAYXEZFOFE-GFCCVEGCSA-N CCOC(c(nc1)c2[n]1-c(ccc(Br)c1)c1C(C1=CC=CCN1)=N[C@@H]2C)=O Chemical compound CCOC(c(nc1)c2[n]1-c(ccc(Br)c1)c1C(C1=CC=CCN1)=N[C@@H]2C)=O FFEOWAYXEZFOFE-GFCCVEGCSA-N 0.000 description 1
- FFVVHHGTBSWVRT-LLVKDONJSA-N C[C@H](c1c(-c2nc(C)n[o]2)nc[n]1-c(cc1)c2cc1Br)N=C2c1ncccc1 Chemical compound C[C@H](c1c(-c2nc(C)n[o]2)nc[n]1-c(cc1)c2cc1Br)N=C2c1ncccc1 FFVVHHGTBSWVRT-LLVKDONJSA-N 0.000 description 1
- PIPOCLOMPZRSLC-CYBMUJFWSA-N C[C@H]1N=C(c(cccc2)c2F)c(cc(cc2)C#C)c2-[n]2c1c(C(NC)=O)nc2 Chemical compound C[C@H]1N=C(c(cccc2)c2F)c(cc(cc2)C#C)c2-[n]2c1c(C(NC)=O)nc2 PIPOCLOMPZRSLC-CYBMUJFWSA-N 0.000 description 1
- LNPOWXXHIUMIKI-CQSZACIVSA-N C[C@H]1N=C(c(cccc2)c2F)c2cc(C#C)ccc2-[n]2c1c(C(N(C)C)=O)nc2 Chemical compound C[C@H]1N=C(c(cccc2)c2F)c2cc(C#C)ccc2-[n]2c1c(C(N(C)C)=O)nc2 LNPOWXXHIUMIKI-CQSZACIVSA-N 0.000 description 1
- BDFZSOMNQYUCRC-UHFFFAOYSA-N Cc1n[o]c(-c(nc2)c3[n]2-c(ccc(C#C)c2)c2C(c2ncccc2)=NC3)n1 Chemical compound Cc1n[o]c(-c(nc2)c3[n]2-c(ccc(C#C)c2)c2C(c2ncccc2)=NC3)n1 BDFZSOMNQYUCRC-UHFFFAOYSA-N 0.000 description 1
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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022017827A JP7515526B2 (ja) | 2016-03-18 | 2022-02-08 | α5含有GABAA受容体アゴニストによる神経変性および神経精神障害における認知症状および気分症状の処置 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662310409P | 2016-03-18 | 2016-03-18 | |
| US62/310,409 | 2016-03-18 | ||
| PCT/US2017/023206 WO2017161370A1 (en) | 2016-03-18 | 2017-03-20 | Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022017827A Division JP7515526B2 (ja) | 2016-03-18 | 2022-02-08 | α5含有GABAA受容体アゴニストによる神経変性および神経精神障害における認知症状および気分症状の処置 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019509340A JP2019509340A (ja) | 2019-04-04 |
| JP7023876B2 true JP7023876B2 (ja) | 2022-02-22 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018568186A Active JP7023876B2 (ja) | 2016-03-18 | 2017-03-20 | α5含有GABAA受容体アゴニストによる神経変性および神経精神障害における認知症状および気分症状の処置 |
| JP2022017827A Active JP7515526B2 (ja) | 2016-03-18 | 2022-02-08 | α5含有GABAA受容体アゴニストによる神経変性および神経精神障害における認知症状および気分症状の処置 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022017827A Active JP7515526B2 (ja) | 2016-03-18 | 2022-02-08 | α5含有GABAA受容体アゴニストによる神経変性および神経精神障害における認知症状および気分症状の処置 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10906909B2 (https=) |
| EP (2) | EP3439665B1 (https=) |
| JP (2) | JP7023876B2 (https=) |
| AU (2) | AU2017235665B2 (https=) |
| CA (1) | CA3016491A1 (https=) |
| CY (1) | CY1125576T1 (https=) |
| DK (1) | DK3439665T3 (https=) |
| ES (1) | ES2926918T3 (https=) |
| HR (1) | HRP20221098T1 (https=) |
| HU (1) | HUE059774T2 (https=) |
| LT (1) | LT3439665T (https=) |
| PL (1) | PL3439665T3 (https=) |
| PT (1) | PT3439665T (https=) |
| RS (1) | RS63674B1 (https=) |
| SI (1) | SI3439665T1 (https=) |
| SM (1) | SMT202200372T1 (https=) |
| WO (1) | WO2017161370A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7013446B2 (ja) | 2016-08-16 | 2022-02-15 | ユーダブリューエム・リサーチ・ファウンデーション,インコーポレーテッド | Gaba(a)受容体モジュレーター、及び、喘息における気道過敏及び炎症を抑制するための方法 |
| US20220105106A1 (en) * | 2019-02-13 | 2022-04-07 | Centre For Addiction And Mental Health | Compositions and methods relating to use of agonists of alpha5-containing gabaa receptors |
| SG11202109526PA (en) * | 2019-03-18 | 2021-10-28 | Neurocycle Therapeutics Inc | Use of gabaa receptor modulators for treatment of pain |
| TWI901650B (zh) | 2020-03-26 | 2025-10-21 | 匈牙利商羅特格登公司 | 啶及吡啶并〔3,4-c〕嗒衍生物 |
| US20240374612A1 (en) * | 2021-09-08 | 2024-11-14 | Uwm Research Foundation, Inc. | Imidazobenzodiazepines for treatment of cognitive and mood symptoms |
| HU231691B1 (hu) | 2021-09-29 | 2025-10-28 | Richter Gedeon Nyrt | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
| AU2022359461A1 (en) * | 2021-10-07 | 2024-05-02 | Pantherics Incorporated | Methods and compounds for treating inflammation |
| WO2024077061A2 (en) * | 2022-10-04 | 2024-04-11 | Uwm Research Foundation, Inc. | Gaba(a) receptor modulators and methods to control smooth muscle contraction and inflammation |
| IT202400001089A1 (it) * | 2024-01-22 | 2025-07-22 | Fondazione St Italiano Tecnologia | Composti e composizioni per l'uso nel ripristino di deficit cognitivi e comportamentali e nel miglioramento della memoria di individui nati pretermine |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090093466A1 (en) | 2007-10-03 | 2009-04-09 | Bristol-Myers Squibb Company | Carboxamide GABAa ALPHA2 Modulators |
| US20100004226A1 (en) | 2004-06-30 | 2010-01-07 | Cook James M | Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects |
| US20100317619A1 (en) | 2002-03-28 | 2010-12-16 | James Cook | Selective Agents for Pain Suppression |
| US20150258128A1 (en) | 2011-04-28 | 2015-09-17 | Uwm Research Foundation, Inc. | Gabaergic receptor subtype selective ligands and their uses |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA755418B (en) * | 1974-09-11 | 1977-06-29 | Hoffmann La Roche | Diazepine derivatives |
| US4226768A (en) | 1979-05-29 | 1980-10-07 | Hoffmann-La Roche Inc. | Process for the preparation of imidazobenzodiazepines |
| US20030176456A1 (en) | 2001-12-21 | 2003-09-18 | June Harry L. | Methods for reducing alcohol cravings in chronic alcoholics |
| USRE47475E1 (en) | 2002-03-28 | 2019-07-02 | Wisys Technology Foundation, Inc. | Selective agents for pain suppression |
| DE60319812T2 (de) | 2002-03-28 | 2009-04-23 | Wisys Technology Foundation, Inc., Madison | Angstlösende wirkstoffe mit verminderten beruhigenden und ataktischen nebenwirkungen |
| US20100130479A1 (en) | 2005-05-16 | 2010-05-27 | Cook James M | Gabaergic Agents to Treat Memory Deficits |
| EP1888594A2 (en) | 2005-05-16 | 2008-02-20 | Wisys Technology Foundation, Inc. | Gabaergic agents to treat memory deficits |
| WO2007042544A2 (en) | 2005-10-14 | 2007-04-19 | Neurosearch A/S | Imidazole derivatives and their use for modulating the gabaa receptor complex |
| DE102006023554A1 (de) | 2006-05-19 | 2007-11-22 | Zf Friedrichshafen Ag | Ermittlung der Drehzahl einer Getriebewelle |
| EP2364571B1 (en) | 2008-10-02 | 2012-08-22 | Telefonaktiebolaget L M Ericsson (PUBL) | Wireless communication system and method for assigning a channel in said wireless communication system |
| US20100261711A1 (en) | 2009-03-20 | 2010-10-14 | Wisys Technology Foundation | Selective anticonvulsant agents and their uses |
| CA2885148A1 (en) | 2012-09-21 | 2014-03-27 | Uwm Research Foundation, Inc. | Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma |
| CA2979701C (en) | 2015-03-20 | 2023-01-03 | Uwm Research Foundation, Inc. | Oxazole substituted benzimidazodiazepines and their uses as gabaergic ligands |
-
2017
- 2017-03-20 DK DK17767701.0T patent/DK3439665T3/da active
- 2017-03-20 PT PT177677010T patent/PT3439665T/pt unknown
- 2017-03-20 HR HRP20221098TT patent/HRP20221098T1/hr unknown
- 2017-03-20 CA CA3016491A patent/CA3016491A1/en active Pending
- 2017-03-20 RS RS20220892A patent/RS63674B1/sr unknown
- 2017-03-20 AU AU2017235665A patent/AU2017235665B2/en active Active
- 2017-03-20 WO PCT/US2017/023206 patent/WO2017161370A1/en not_active Ceased
- 2017-03-20 SI SI201731230T patent/SI3439665T1/sl unknown
- 2017-03-20 PL PL17767701.0T patent/PL3439665T3/pl unknown
- 2017-03-20 ES ES17767701T patent/ES2926918T3/es active Active
- 2017-03-20 US US16/086,053 patent/US10906909B2/en active Active
- 2017-03-20 JP JP2018568186A patent/JP7023876B2/ja active Active
- 2017-03-20 EP EP17767701.0A patent/EP3439665B1/en active Active
- 2017-03-20 EP EP22181243.1A patent/EP4129297A1/en active Pending
- 2017-03-20 SM SM20220372T patent/SMT202200372T1/it unknown
- 2017-03-20 LT LTEPPCT/US2017/023206T patent/LT3439665T/lt unknown
- 2017-03-20 HU HUE17767701A patent/HUE059774T2/hu unknown
-
2020
- 2020-12-15 US US17/122,745 patent/US11753412B2/en active Active
-
2022
- 2022-02-08 JP JP2022017827A patent/JP7515526B2/ja active Active
- 2022-09-27 CY CY20221100636T patent/CY1125576T1/el unknown
- 2022-11-23 AU AU2022275446A patent/AU2022275446B2/en active Active
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2023
- 2023-08-02 US US18/363,933 patent/US12180216B2/en active Active
-
2024
- 2024-11-12 US US18/944,947 patent/US20250179080A1/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US20100317619A1 (en) | 2002-03-28 | 2010-12-16 | James Cook | Selective Agents for Pain Suppression |
| US20100004226A1 (en) | 2004-06-30 | 2010-01-07 | Cook James M | Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects |
| US20090093466A1 (en) | 2007-10-03 | 2009-04-09 | Bristol-Myers Squibb Company | Carboxamide GABAa ALPHA2 Modulators |
| US20150258128A1 (en) | 2011-04-28 | 2015-09-17 | Uwm Research Foundation, Inc. | Gabaergic receptor subtype selective ligands and their uses |
Non-Patent Citations (4)
| Title |
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| Namjoshi, Ojas A. et al ,Search for α3β2/3γ2 subtype selective ligands that are stable on human liver microsomes,Bioorganic & Medicinal Chemistry,2013年,21(1),,93-101 |
| Poe, Michael M. et al,Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy,Journal of Medicinal Chemistry ,2016年,59(23),,10800-10806 |
| REGISTRY(STN)[online],2009年,CAS登録番号 1141017-14-2 |
| Stamenic, Tamara Timic et al,Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABAA receptors containing the α5 subunit,European Journal of Pharmacology,2016年,791,,433-443 |
Also Published As
| Publication number | Publication date |
|---|---|
| LT3439665T (lt) | 2022-10-10 |
| PT3439665T (pt) | 2022-09-27 |
| US12180216B2 (en) | 2024-12-31 |
| HRP20221098T1 (hr) | 2022-11-25 |
| AU2017235665B2 (en) | 2022-12-08 |
| WO2017161370A1 (en) | 2017-09-21 |
| EP3439665A1 (en) | 2019-02-13 |
| DK3439665T3 (da) | 2022-09-26 |
| JP2019509340A (ja) | 2019-04-04 |
| AU2022275446B2 (en) | 2025-01-02 |
| RS63674B1 (sr) | 2022-11-30 |
| AU2022275446A1 (en) | 2023-01-05 |
| EP3439665A4 (en) | 2019-11-27 |
| JP2022065035A (ja) | 2022-04-26 |
| SMT202200372T1 (it) | 2022-11-18 |
| PL3439665T3 (pl) | 2023-01-16 |
| CA3016491A1 (en) | 2017-09-21 |
| SI3439665T1 (sl) | 2023-05-31 |
| US11753412B2 (en) | 2023-09-12 |
| EP4129297A1 (en) | 2023-02-08 |
| EP3439665B1 (en) | 2022-06-29 |
| US20210309662A1 (en) | 2021-10-07 |
| JP7515526B2 (ja) | 2024-07-12 |
| ES2926918T3 (es) | 2022-10-31 |
| CY1125576T1 (el) | 2026-02-25 |
| US10906909B2 (en) | 2021-02-02 |
| US20200181146A1 (en) | 2020-06-11 |
| US20240083905A1 (en) | 2024-03-14 |
| WO2017161370A8 (en) | 2018-09-27 |
| HUE059774T2 (hu) | 2023-01-28 |
| US20250179080A1 (en) | 2025-06-05 |
| AU2017235665A1 (en) | 2018-09-27 |
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