JP2020511515A5 - - Google Patents
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- Publication number
- JP2020511515A5 JP2020511515A5 JP2019552238A JP2019552238A JP2020511515A5 JP 2020511515 A5 JP2020511515 A5 JP 2020511515A5 JP 2019552238 A JP2019552238 A JP 2019552238A JP 2019552238 A JP2019552238 A JP 2019552238A JP 2020511515 A5 JP2020511515 A5 JP 2020511515A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrrole
- ethyl
- hexahydropyrrolo
- diethyl
- dihydrofuran
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 98
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims description 72
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 44
- 229910052739 hydrogen Inorganic materials 0.000 claims description 34
- 150000001875 compounds Chemical class 0.000 claims description 33
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 24
- -1 hexahydropyrrolo [3,4-c] pyrrole-2 (1H) -yl Chemical group 0.000 claims description 24
- 125000003545 alkoxy group Chemical group 0.000 claims description 22
- 239000001257 hydrogen Substances 0.000 claims description 22
- 125000001188 haloalkyl group Chemical group 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 17
- 150000002431 hydrogen Chemical class 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 14
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 10
- 208000035475 disorder Diseases 0.000 claims description 10
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 10
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 208000002193 Pain Diseases 0.000 claims description 8
- 229940002612 prodrug Drugs 0.000 claims description 8
- 239000000651 prodrug Substances 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 201000000980 schizophrenia Diseases 0.000 claims description 8
- 239000012453 solvate Substances 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 7
- 102100039126 5-hydroxytryptamine receptor 7 Human genes 0.000 claims description 6
- 101710150237 5-hydroxytryptamine receptor 7 Proteins 0.000 claims description 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 6
- 230000008482 dysregulation Effects 0.000 claims description 6
- 230000000694 effects Effects 0.000 claims description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 6
- HDGPAUBLUJEGSY-HRTMPFAESA-N (3R)-3-[2-[5-(2-propan-2-ylphenyl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-2-yl]ethyl]-2-oxaspiro[4.5]decan-1-one Chemical compound C(C)(C)C1=C(C=CC=C1)N1CC2C(C1)CN(C2)CC[C@@H]1OC(C2(C1)CCCCC2)=O HDGPAUBLUJEGSY-HRTMPFAESA-N 0.000 claims description 4
- HDGPAUBLUJEGSY-LZBANZJXSA-N (3S)-3-[2-[5-(2-propan-2-ylphenyl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-2-yl]ethyl]-2-oxaspiro[4.5]decan-1-one Chemical compound C(C)(C)C1=C(C=CC=C1)N1CC2C(C1)CN(C2)CC[C@H]1OC(C2(C1)CCCCC2)=O HDGPAUBLUJEGSY-LZBANZJXSA-N 0.000 claims description 4
- RBXFBWXIVPJFAU-QLOJAFMTSA-N (5R)-3,3-diethyl-5-[2-(5-phenyl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-2-yl)ethyl]oxolan-2-one Chemical compound C(C)C1(C(O[C@H](C1)CCN1CC2CN(CC2C1)C1=CC=CC=C1)=O)CC RBXFBWXIVPJFAU-QLOJAFMTSA-N 0.000 claims description 4
- RBXFBWXIVPJFAU-AFMYVXGZSA-N (5S)-3,3-diethyl-5-[2-(5-phenyl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-2-yl)ethyl]oxolan-2-one Chemical compound C(C)C1(C(O[C@@H](C1)CCN1CC2CN(CC2C1)C1=CC=CC=C1)=O)CC RBXFBWXIVPJFAU-AFMYVXGZSA-N 0.000 claims description 4
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 4
- 208000020925 Bipolar disease Diseases 0.000 claims description 4
- 208000017164 Chronobiology disease Diseases 0.000 claims description 4
- 208000027534 Emotional disease Diseases 0.000 claims description 4
- 206010020772 Hypertension Diseases 0.000 claims description 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 4
- 208000026139 Memory disease Diseases 0.000 claims description 4
- 208000019695 Migraine disease Diseases 0.000 claims description 4
- 208000007920 Neurogenic Inflammation Diseases 0.000 claims description 4
- 208000018262 Peripheral vascular disease Diseases 0.000 claims description 4
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 claims description 4
- 206010036618 Premenstrual syndrome Diseases 0.000 claims description 4
- 208000029061 Temperature regulation disease Diseases 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims description 4
- 208000022804 avoidant personality disease Diseases 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 230000000971 hippocampal effect Effects 0.000 claims description 4
- 150000004677 hydrates Chemical class 0.000 claims description 4
- 201000003723 learning disability Diseases 0.000 claims description 4
- 206010027599 migraine Diseases 0.000 claims description 4
- 210000005036 nerve Anatomy 0.000 claims description 4
- 230000002093 peripheral effect Effects 0.000 claims description 4
- 208000022821 personality disease Diseases 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 206010036596 premature ejaculation Diseases 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 230000001932 seasonal effect Effects 0.000 claims description 4
- 230000011664 signaling Effects 0.000 claims description 4
- 208000019116 sleep disease Diseases 0.000 claims description 4
- 208000020685 sleep-wake disease Diseases 0.000 claims description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 239000001301 oxygen Substances 0.000 claims description 2
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023174457A JP7705909B2 (ja) | 2017-03-21 | 2023-10-06 | ５－ヒドロキシトリプタミン受容体７調節物質および治療剤としてのその使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762474280P | 2017-03-21 | 2017-03-21 | |
| US62/474,280 | 2017-03-21 | ||
| PCT/US2018/022581 WO2018175190A1 (en) | 2017-03-21 | 2018-03-15 | 5-hydroxytryptamine receptor 7 modulators and their use as therapeutic agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023174457A Division JP7705909B2 (ja) | 2017-03-21 | 2023-10-06 | ５－ヒドロキシトリプタミン受容体７調節物質および治療剤としてのその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020511515A JP2020511515A (ja) | 2020-04-16 |
| JP2020511515A5 true JP2020511515A5 (enExample) | 2021-04-22 |
| JP7365238B2 JP7365238B2 (ja) | 2023-10-19 |
Family
ID=63585688
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019552238A Active JP7365238B2 (ja) | 2017-03-21 | 2018-03-15 | ５－ヒドロキシトリプタミン受容体７調節物質および治療剤としてのその使用 |
| JP2023174457A Active JP7705909B2 (ja) | 2017-03-21 | 2023-10-06 | ５－ヒドロキシトリプタミン受容体７調節物質および治療剤としてのその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023174457A Active JP7705909B2 (ja) | 2017-03-21 | 2023-10-06 | ５－ヒドロキシトリプタミン受容体７調節物質および治療剤としてのその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (3) | US11220505B2 (enExample) |
| EP (1) | EP3600289A4 (enExample) |
| JP (2) | JP7365238B2 (enExample) |
| MA (1) | MA49017A (enExample) |
| WO (1) | WO2018175190A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2970223B1 (en) | 2013-03-11 | 2020-04-15 | Temple University Of The Commonwealth System Of Higher Education | Novel 5-hydroxytryptamine receptor 7 activity modulators and their method of use |
| WO2016040554A1 (en) | 2014-09-10 | 2016-03-17 | Temple University-Of The Commonwealth System Of Higher Education | Novel 5-hydroxytryptamine receptor 7 activity modulators and their method of use |
| WO2018093818A1 (en) | 2016-11-15 | 2018-05-24 | Temple University-Of The Commonwealth System Of Higher Education | Novel modulators of the 5-hydroxytryptamine receptor 7 and their method of use |
| EP3600289A4 (en) | 2017-03-21 | 2020-08-05 | Temple University - Of The Commonwealth System of Higher Education | 5-HYDROXYTRYPTAMINE RECEPTOR 7 MODULATORS AND THE USE OF THESE AS THERAPEUTIC AGENTS |
| EP3600290B1 (en) * | 2017-03-21 | 2025-06-04 | Temple University - Of The Commonwealth System of Higher Education | Novel modulators of the sigma-2 receptor and their method of use |
| KR20210020182A (ko) * | 2018-05-11 | 2021-02-23 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 5-히드록시트립타민 수용체 7의 조절자로서의 신규한 기능화된 락탐 및 이의 사용 방법 |
| GB201809295D0 (en) * | 2018-06-06 | 2018-07-25 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| WO2020239073A1 (zh) * | 2019-05-30 | 2020-12-03 | 中国科学院上海药物研究所 | 一种并环化合物、其制备方法和用途 |
| WO2021097116A1 (en) * | 2019-11-13 | 2021-05-20 | Temple University-Of The Commonwealth System Of Higher Education | Novel functionalized lactams as modulators of the 5-hydroxytryptamine receptor 7 and their method of use |
| MX2022005819A (es) * | 2019-11-13 | 2022-08-16 | Univ Temple | Nuevas lactonas funcionalizadas como moduladores del receptor 7 de 5-hidroxitriptamina y su método de uso. |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1592772A2 (en) | 2003-01-31 | 2005-11-09 | Pfizer Products Incorporated | 5ht7 antagonists and inverse agonists |
| AU2005219438B2 (en) | 2004-03-03 | 2011-02-17 | Chemocentryx, Inc. | Bicyclic and bridged nitrogen heterocycles |
| GB0419192D0 (en) | 2004-08-27 | 2004-09-29 | Merck Sharp & Dohme | Therapeutic agents |
| EP1875899A1 (en) | 2006-06-29 | 2008-01-09 | Laboratorios Del Dr. Esteve, S.A. | Use of 5HT7 receptor agonists for the treatment of pain |
| KR20090112627A (ko) | 2006-11-13 | 2009-10-28 | 킹 파머슈티칼스 리서치 앤드 디벨로프먼트 아이엔씨 | 에이1 아데노신 수용체의 알로스테릭 조절제 |
| ES2380756T3 (es) | 2007-10-12 | 2012-05-18 | Eli Lilly And Company | Antagonistas del receptor 5-HT7 |
| US8148408B2 (en) | 2008-05-09 | 2012-04-03 | Abbott Laboratories | Selective substituted pyridine ligands for neuronal nicotinic receptors |
| CA2735934C (en) | 2008-09-05 | 2014-01-07 | Supernus Pharmaceuticals, Inc. | Method of treatment of attention deficit/hyperactivity disorder (adhd) |
| WO2012058769A1 (en) | 2010-11-03 | 2012-05-10 | Mcmaster University | Method of treating mucosal inflammation |
| US8697888B2 (en) | 2012-01-06 | 2014-04-15 | Vanderbilt University | Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors |
| US9464062B2 (en) | 2012-11-28 | 2016-10-11 | Temple University—Of the Commonwealth System of Higher Education | Disubstituted oxazolidin-2-ones 5-hydroxytryptamine receptor 2B activity modulators |
| DK2928474T3 (en) * | 2012-12-07 | 2019-02-11 | Chemocentryx Inc | Diazollactamer |
| EP2970223B1 (en) | 2013-03-11 | 2020-04-15 | Temple University Of The Commonwealth System Of Higher Education | Novel 5-hydroxytryptamine receptor 7 activity modulators and their method of use |
| MX2016008130A (es) | 2013-12-20 | 2016-10-13 | Esteve Labor Dr | Derivados de piperidina con actividad multimodal contra el dolor. |
| WO2016040554A1 (en) | 2014-09-10 | 2016-03-17 | Temple University-Of The Commonwealth System Of Higher Education | Novel 5-hydroxytryptamine receptor 7 activity modulators and their method of use |
| AR103297A1 (es) * | 2014-12-30 | 2017-05-03 | Forma Therapeutics Inc | Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina |
| US20180221365A1 (en) | 2015-05-12 | 2018-08-09 | Temple University-Of The Commonwealth System Of Higher Education | Novel sigma-2 receptor binders and their method of use |
| WO2018093818A1 (en) | 2016-11-15 | 2018-05-24 | Temple University-Of The Commonwealth System Of Higher Education | Novel modulators of the 5-hydroxytryptamine receptor 7 and their method of use |
| EP3600289A4 (en) * | 2017-03-21 | 2020-08-05 | Temple University - Of The Commonwealth System of Higher Education | 5-HYDROXYTRYPTAMINE RECEPTOR 7 MODULATORS AND THE USE OF THESE AS THERAPEUTIC AGENTS |
| EP3600290B1 (en) | 2017-03-21 | 2025-06-04 | Temple University - Of The Commonwealth System of Higher Education | Novel modulators of the sigma-2 receptor and their method of use |
| KR20210020182A (ko) | 2018-05-11 | 2021-02-23 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 5-히드록시트립타민 수용체 7의 조절자로서의 신규한 기능화된 락탐 및 이의 사용 방법 |
-
2018
- 2018-03-15 EP EP18772184.0A patent/EP3600289A4/en active Pending
- 2018-03-15 US US16/496,065 patent/US11220505B2/en active Active
- 2018-03-15 MA MA049017A patent/MA49017A/fr unknown
- 2018-03-15 JP JP2019552238A patent/JP7365238B2/ja active Active
- 2018-03-15 WO PCT/US2018/022581 patent/WO2018175190A1/en not_active Ceased
-
2021
- 2021-12-03 US US17/541,682 patent/US11807642B2/en active Active
-
2023
- 2023-09-27 US US18/475,749 patent/US12338245B2/en active Active
- 2023-10-06 JP JP2023174457A patent/JP7705909B2/ja active Active
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