IL258516A - (s)-3-Amino-4-(difluoromethylnyl)cyclopent-1-en-1-carboxylic acid and related compounds as GABA aminotransferase inhibitors for the treatment of epilepsy, addiction and hepatocellular carcinoma - Google Patents
(s)-3-Amino-4-(difluoromethylnyl)cyclopent-1-en-1-carboxylic acid and related compounds as GABA aminotransferase inhibitors for the treatment of epilepsy, addiction and hepatocellular carcinomaInfo
- Publication number
- IL258516A IL258516A IL258516A IL25851618A IL258516A IL 258516 A IL258516 A IL 258516A IL 258516 A IL258516 A IL 258516A IL 25851618 A IL25851618 A IL 25851618A IL 258516 A IL258516 A IL 258516A
- Authority
- IL
- Israel
- Prior art keywords
- difluoromethylenyl
- cyclopent
- addiction
- epilepsy
- ene
- Prior art date
Links
- 108010060511 4-Aminobutyrate Transaminase Proteins 0.000 title 1
- 102100035923 4-aminobutyrate aminotransferase, mitochondrial Human genes 0.000 title 1
- 206010012335 Dependence Diseases 0.000 title 1
- FBLNZOCTNRXJQD-YFKPBYRVSA-N N[C@H]1C=C(CC1=C(F)F)C(O)=O Chemical compound N[C@H]1C=C(CC1=C(F)F)C(O)=O FBLNZOCTNRXJQD-YFKPBYRVSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 206010015037 epilepsy Diseases 0.000 title 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 title 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 title 1
- 230000000937 inactivator Effects 0.000 title 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/46—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C229/48—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562239330P | 2015-10-09 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| IL258516A true IL258516A (en) | 2018-05-31 |
Family
ID=58488679
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL258516A IL258516A (en) | 2015-10-09 | 2018-04-05 | (s)-3-Amino-4-(difluoromethylnyl)cyclopent-1-en-1-carboxylic acid and related compounds as GABA aminotransferase inhibitors for the treatment of epilepsy, addiction and hepatocellular carcinoma |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US9670141B2 (enExample) |
| EP (1) | EP3341355B1 (enExample) |
| JP (1) | JP6841821B2 (enExample) |
| KR (1) | KR102745965B1 (enExample) |
| CN (1) | CN108137484B (enExample) |
| AU (1) | AU2016334396B2 (enExample) |
| BR (1) | BR112018007026B1 (enExample) |
| CA (1) | CA3001330A1 (enExample) |
| CL (1) | CL2018000914A1 (enExample) |
| CO (1) | CO2018003828A2 (enExample) |
| DK (1) | DK3341355T3 (enExample) |
| ES (1) | ES2825349T3 (enExample) |
| HU (1) | HUE053429T2 (enExample) |
| IL (1) | IL258516A (enExample) |
| LT (1) | LT3341355T (enExample) |
| MX (1) | MX380592B (enExample) |
| PE (1) | PE20190349A1 (enExample) |
| PL (1) | PL3341355T3 (enExample) |
| PT (1) | PT3341355T (enExample) |
| WO (1) | WO2017062942A2 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2739697T3 (es) | 2014-08-21 | 2020-02-03 | Boehringer Ingelheim Int | Nuevos compuestos y derivados de espiro[3H-indol-3,2-pirrolidin]-2(1H)-ona como inhibidores de MDM2-p53 |
| BR112018007026B1 (pt) * | 2015-10-09 | 2022-06-21 | Northwestern University | Composto, composição farmacêutica, e usos do composto |
| HRP20210960T1 (hr) | 2015-10-09 | 2021-09-03 | Boehringer Ingelheim International Gmbh | Spojevi i derivati spiro[3h-indol-3,2’-pirolidin]-2(1h)-ona kao inhibitori mdm2-p53 |
| IL310065A (en) * | 2017-02-08 | 2024-03-01 | Ovid Therapeutics Inc | Methods for treating seizure disorders and Prader-Willi syndrome |
| MX2020008359A (es) * | 2018-02-08 | 2020-11-24 | Ovid Therapeutics Inc | Uso de ácido (1s,3s)-3-amino-4-(difluorometiliden) ciclopentano-1-carboxílico y ácido (s)-3-amino-4-(difluorometileni l)ciclopent-1-eno-1-carboxílico en el tratamiento del tinnitus, pérdida de audición neurosensorial aguda, enfermedad de meniere, síndrome de tourette, trastorno por déficit de atención e hiperactividad y adicción. |
| 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 |
| US20190298674A1 (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 |
| KR102791742B1 (ko) * | 2018-05-25 | 2025-04-03 | 노오쓰웨스턴 유니버시티 | (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복실산의 합성을 위한 공정 |
| EP3813816B1 (en) * | 2018-06-07 | 2023-06-07 | Ovid Therapeutics Inc. | Use of (s)-3-amino-4-(difluoromethylenyl) cyclopent-1-ene-1-carboxylic acid and related compounds, (1s,3s)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid in the treatment of fragile x syndrome or fragile x-associated tremor/ataxia syndrome |
| 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 |
| US11993569B2 (en) | 2020-01-23 | 2024-05-28 | Northwestern University | 3-amino-4-halocyclopentene carboxylic acids as inactivators of aminotransferases |
| CN117321025A (zh) * | 2021-03-03 | 2023-12-29 | 西北大学 | 作为人鸟氨酸氨基转移酶的选择性灭活剂的(s)-3-氨基-4,4-二卤代环戊-1-烯甲酸 |
| WO2023164715A2 (en) * | 2022-02-27 | 2023-08-31 | Northwestern University | (3s,4r)-3-amino-4-(difluoromethyl)cyclopent-1-ene-1-carboxylic acid and related compounds as selective inactivators of ornithine aminotransferase |
| JP2025521898A (ja) * | 2022-07-06 | 2025-07-10 | オービッド・セラピューティクス・インコーポレイテッド | 癌の処置における（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－カルボン酸の使用 |
| EP4648757A4 (en) * | 2023-02-17 | 2026-01-07 | Ovid Therapeutics Inc | USE OF (S)-3-AMINO-4-(DIFLUOROMETHYLENYL)CYCLOPENT-1-ENE-1-CARBOXYLIC ACID FOR THE TREATMENT OF GASTROINTESTINAL TRACT DISORDERS AND AS AN IMMUNOMODULATING AGENT |
| CN120641130A (zh) * | 2023-02-17 | 2025-09-12 | 奥维德医疗公司 | (s)-3-氨基-4-(二氟亚甲基)环戊-1-烯-1-甲酸在治疗类风湿性关节炎中的用途 |
| IL322803A (en) * | 2023-02-17 | 2025-10-01 | Ovid Therapeutics Inc | Use of (s)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid in the treatment of diabetes and prediabetes |
| JP2026506097A (ja) * | 2023-02-17 | 2026-02-20 | オービッド・セラピューティクス・インコーポレイテッド | 多発性硬化症の処置における（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－カルボン酸の使用 |
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 |
| WO2011106692A2 (en) * | 2010-02-25 | 2011-09-01 | Northwestern University | 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 AU AU2016334396A patent/AU2016334396B2/en active Active
- 2016-10-10 CA CA3001330A patent/CA3001330A1/en active Pending
- 2016-10-10 PE PE2018000517A patent/PE20190349A1/es unknown
- 2016-10-10 MX MX2018004302A patent/MX380592B/es unknown
- 2016-10-10 LT LTEP16854531.7T patent/LT3341355T/lt unknown
- 2016-10-10 US US15/289,480 patent/US9670141B2/en active Active
- 2016-10-10 DK DK16854531.7T patent/DK3341355T3/da active
- 2016-10-10 ES ES16854531T patent/ES2825349T3/es active Active
- 2016-10-10 PT PT168545317T patent/PT3341355T/pt unknown
- 2016-10-10 KR KR1020187013228A patent/KR102745965B1/ko active Active
- 2016-10-10 JP JP2018517734A patent/JP6841821B2/ja active Active
- 2016-10-10 WO PCT/US2016/056245 patent/WO2017062942A2/en not_active Ceased
- 2016-10-10 HU HUE16854531A patent/HUE053429T2/hu unknown
- 2016-10-10 EP EP16854531.7A patent/EP3341355B1/en active Active
- 2016-10-10 CN CN201680059069.9A patent/CN108137484B/zh active Active
-
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
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed |