JP2018531941A5 - - Google Patents
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- Publication number
- JP2018531941A5 JP2018531941A5 JP2018517734A JP2018517734A JP2018531941A5 JP 2018531941 A5 JP2018531941 A5 JP 2018531941A5 JP 2018517734 A JP2018517734 A JP 2018517734A JP 2018517734 A JP2018517734 A JP 2018517734A JP 2018531941 A5 JP2018531941 A5 JP 2018531941A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- substituent
- salt
- ammonium
- compound according
- 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
- 150000001875 compounds Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O ammonium group Chemical group [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims 2
- 150000003863 ammonium salts Chemical class 0.000 claims 2
- 150000007942 carboxylates Chemical group 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 150000002500 ions Chemical class 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
Claims (11)
- 式
ただしＲ１およびＲ２の少なくとも一方はＨではない〕
の化合物またはその塩。 - 前記アミノ置換基が（Ｓ）立体化学配置を有する、請求項１に記載の化合物。
- Ｒ１およびＲ２の少なくとも一方がＦである、請求項２に記載の化合物。
- アンモニウム置換基、カルボキシレート置換基およびそれらの組合せから選択される置換基を含む塩である、請求項１に記載の化合物。
- アンモニウム塩がプロトン酸の共役塩基である対イオンを有する、請求項４に記載の化合物。
- 薬学的に許容される担体成分を含む医薬組成物中の、請求項１に記載の化合物。
- 式
Ｒ１およびＲ２の各々は独立して、ＨおよびＦから選択され、
ただし、Ｒ１およびＲ２の少なくとも一方はＦである〕
の化合物またはその塩。 - Ｒ１およびＲ２の各々がＦである、請求項７に記載の化合物。
- アンモニウム置換基、カルボキシレート置換基およびそれらの組合せから選択される置換基を含む塩である、請求項７に記載の化合物。
- 前記アンモニウム塩がプロトン酸の共役塩基である対イオンを有する、請求項９に記載の化合物。
- 薬学的に許容される担体成分を含む医薬組成物中の、請求項７に記載の化合物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562239330P | 2015-10-09 | 2015-10-09 | |
| US62/239,330 | 2015-10-09 | ||
| PCT/US2016/056245 WO2017062942A2 (en) | 2015-10-09 | 2016-10-10 | (s)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid, and related compounds as gaba aminotransferase inactivators for the treatment of epilepsy, addiction and hepatocellular carcinoma |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018531941A JP2018531941A (ja) | 2018-11-01 |
| JP2018531941A5 true JP2018531941A5 (ja) | 2019-11-21 |
| JP6841821B2 JP6841821B2 (ja) | 2021-03-10 |
Family
ID=58488679
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018517734A Active JP6841821B2 (ja) | 2015-10-09 | 2016-10-10 | てんかん、嗜癖および肝細胞癌の処置のためのｇａｂａアミノトランスフェラーゼ不活性化剤としての（ｓ）−３−アミノ−４−（ジフルオロメチレニル）シクロペント−１−エン−１−カルボン酸および関連化合物 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US9670141B2 (ja) |
| EP (1) | EP3341355B1 (ja) |
| JP (1) | JP6841821B2 (ja) |
| KR (1) | KR20180052782A (ja) |
| CN (1) | CN108137484B (ja) |
| AU (1) | AU2016334396B2 (ja) |
| BR (1) | BR112018007026B1 (ja) |
| CA (1) | CA3001330A1 (ja) |
| CL (1) | CL2018000914A1 (ja) |
| CO (1) | CO2018003828A2 (ja) |
| DK (1) | DK3341355T3 (ja) |
| ES (1) | ES2825349T3 (ja) |
| HK (1) | HK1253002A1 (ja) |
| HU (1) | HUE053429T2 (ja) |
| IL (1) | IL258516A (ja) |
| LT (1) | LT3341355T (ja) |
| MX (1) | MX2018004302A (ja) |
| PE (1) | PE20190349A1 (ja) |
| PL (1) | PL3341355T3 (ja) |
| PT (1) | PT3341355T (ja) |
| WO (1) | WO2017062942A2 (ja) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112018007026B1 (pt) * | 2015-10-09 | 2022-06-21 | Northwestern University | Composto, composição farmacêutica, e usos do composto |
| US20200000757A1 (en) * | 2017-02-08 | 2020-01-02 | Ovid Therapeutics Inc. | Methods of treating seizure disorders and prader-willi syndrome |
| US11771671B2 (en) | 2018-02-08 | 2023-10-03 | Ovid Therapeutics Inc. | Use of (1S,3S)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid and (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid in the treatment of tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, attention deficit hyperactivity disorder and addiction |
| WO2019157273A1 (en) * | 2018-02-08 | 2019-08-15 | Ovid Therapeutics Inc. | Use of (1s,3s)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid and (s)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid in the treatment of tinnitus, acute sensorineural hearing loss, meniere's disease, tourette's syndrome, attention deficit hyperactivity disorder and addiction |
| WO2019191525A1 (en) * | 2018-03-29 | 2019-10-03 | Ovid Therapeutics Inc. | Use of (1s,3s)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid and (s)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid in the treatment of eye disorders |
| US10822301B2 (en) | 2018-04-12 | 2020-11-03 | Northwestern University | 3-carbon substituted 4-aminocyclopent-1-ene-1-carboxylic acid compounds as inhibitors of gamma-aminobutyric acid (GABA) aminotransferase |
| EP3784649A4 (en) * | 2018-05-25 | 2022-04-13 | Northwestern University | METHOD OF SYNTHESIS OF (S)-3-AMINO-4-(DIFLUORMETHYLENYL)CYCLOPENT-1-EN-1-CARBONIC ACID |
| ES2948263T3 (es) * | 2018-06-07 | 2023-09-07 | Ovid Therapeutics Inc | Uso del ácido (S)-3-amino-4-(difluorometilenil) ciclopent-1-eno-1-carboxílico y compuestos relacionados, ácido (1s,3s)-3-amino-4-(difluorometiliden) ciclopentano-1-carboxílico en el tratamiento del síndrome del X frágil o del síndrome de temblor/ataxia asociado al X frágil |
| WO2020176511A1 (en) | 2019-02-25 | 2020-09-03 | Northwestern University | Analogs of 3-amino-4-(propan-2-ylidene) cyclopentane-1-carboxylic acid and uses thereof for treating diseases and disorders associated with ornithine aminotransferase activity |
| WO2020206234A1 (en) | 2019-04-03 | 2020-10-08 | Northwestern University | 2-difluoro substituted 4-aminocyclopentanecarboxylic acids as inhibitors of gamma-aminobutyric acid aminotransferase and human ornithine aminotransferase |
| CN110935495B (zh) * | 2019-11-29 | 2021-02-23 | 中国科学院电子学研究所 | Gaba和电生理微纳同步传感检测芯片及其制备方法 |
| JP2024510422A (ja) * | 2021-03-03 | 2024-03-07 | ノースウェスタン ユニバーシティ | ヒトオルニチンアミノトランスフェラーゼの選択的不活化剤としての３－アミノ－４，４－ジハロシクロペンタ－１－エンカルボン酸 |
| WO2024010840A1 (en) * | 2022-07-06 | 2024-01-11 | Ovid Therapeutics Inc. | Use of (s)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid in the treatment of cancer |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6794413B1 (en) * | 2002-07-19 | 2004-09-21 | Northwestern University | Compounds and related methods for inhibition of γ-aminobutyric acid aminotransferase |
| IL177609A (en) * | 2006-08-21 | 2015-11-30 | Yaron Ilan | Use of gobacoline or its analogue to produce a drug to treat liver carcinoma |
| EP2542234A4 (en) * | 2010-02-25 | 2013-07-31 | Univ Northwestern | METHODS OF USING (1S, 3S) -3-AMINO-4-DIFLUOROMETHYLENYL-1-CYCLOPENTANOIC ACID |
| AR087700A1 (es) * | 2011-08-30 | 2014-04-09 | Gilead Sciences Inc | Inhibidores de aldh-2 en el tratamiento de adicciones |
| BR112018007026B1 (pt) * | 2015-10-09 | 2022-06-21 | Northwestern University | Composto, composição farmacêutica, e usos do composto |
-
2016
- 2016-10-10 BR BR112018007026-2A patent/BR112018007026B1/pt active IP Right Grant
- 2016-10-10 PL PL16854531T patent/PL3341355T3/pl unknown
- 2016-10-10 CN CN201680059069.9A patent/CN108137484B/zh active Active
- 2016-10-10 JP JP2018517734A patent/JP6841821B2/ja active Active
- 2016-10-10 WO PCT/US2016/056245 patent/WO2017062942A2/en active Application Filing
- 2016-10-10 HU HUE16854531A patent/HUE053429T2/hu unknown
- 2016-10-10 DK DK16854531.7T patent/DK3341355T3/da active
- 2016-10-10 PT PT168545317T patent/PT3341355T/pt unknown
- 2016-10-10 EP EP16854531.7A patent/EP3341355B1/en active Active
- 2016-10-10 AU AU2016334396A patent/AU2016334396B2/en active Active
- 2016-10-10 KR KR1020187013228A patent/KR20180052782A/ko not_active Application Discontinuation
- 2016-10-10 PE PE2018000517A patent/PE20190349A1/es unknown
- 2016-10-10 LT LTEP16854531.7T patent/LT3341355T/lt unknown
- 2016-10-10 ES ES16854531T patent/ES2825349T3/es active Active
- 2016-10-10 MX MX2018004302A patent/MX2018004302A/es unknown
- 2016-10-10 US US15/289,480 patent/US9670141B2/en active Active
- 2016-10-10 CA CA3001330A patent/CA3001330A1/en active Pending
-
2017
- 2017-05-04 US US15/586,730 patent/US9993449B2/en active Active
-
2018
- 2018-04-05 IL IL258516A patent/IL258516A/en active IP Right Grant
- 2018-04-09 CL CL2018000914A patent/CL2018000914A1/es unknown
- 2018-04-10 CO CONC2018/0003828A patent/CO2018003828A2/es unknown
- 2018-05-29 US US15/991,323 patent/US20180271816A1/en not_active Abandoned
- 2018-09-26 HK HK18112366.1A patent/HK1253002A1/zh unknown
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