ES2825349T3 - Acido (S)-3-amino-4-(difluorometilenil)ciclopent-1-eno-1-carboxílico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adicción y carcinoma hepatocelular - Google Patents

Acido (S)-3-amino-4-(difluorometilenil)ciclopent-1-eno-1-carboxílico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adicción y carcinoma hepatocelular Download PDF

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ES2825349T3
ES2825349T3 ES16854531T ES16854531T ES2825349T3 ES 2825349 T3 ES2825349 T3 ES 2825349T3 ES 16854531 T ES16854531 T ES 16854531T ES 16854531 T ES16854531 T ES 16854531T ES 2825349 T3 ES2825349 T3 ES 2825349T3
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compound
gaba
aminotransferase
activity
disorder
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Spanish (es)
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Richard Silverman
Kenji Takaya
Hoang Le
Jose Juncosa
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Northwestern University
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Northwestern University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46Compounds 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
    • C07C229/48Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
ES16854531T 2015-10-09 2016-10-10 Acido (S)-3-amino-4-(difluorometilenil)ciclopent-1-eno-1-carboxílico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adicción y carcinoma hepatocelular Active ES2825349T3 (es)

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
ES2825349T3 true ES2825349T3 (es) 2021-05-17

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ES16854531T Active ES2825349T3 (es) 2015-10-09 2016-10-10 Acido (S)-3-amino-4-(difluorometilenil)ciclopent-1-eno-1-carboxílico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adicción y carcinoma hepatocelular

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)

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EA038071B1 (ru) 2014-08-21 2021-07-01 Бёрингер Ингельхайм Интернациональ Гмбх СОЕДИНЕНИЕ СПИРО[3H-ИНДОЛ-3,2'-ПИРРОЛИДИН]-2(1H)-ОНА И ЕГО ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ MDM2-p53
EP3341355B1 (en) * 2015-10-09 2020-09-30 Northwestern University (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
MX377009B (es) 2015-10-09 2025-03-07 Boehringer Ingelheim Int Nuevos compuestos de espiro[3h-indol-3,2´-pirrolidin]-2(1h)-ona y derivados como inhibidores de mdm2-p53.
IL268212B2 (en) 2017-02-08 2024-06-01 Ovid Therapeutics Inc Methods for 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
JP2021512920A (ja) * 2018-02-08 2021-05-20 オービッド・セラピューティクス・インコーポレイテッドOvid Therapeutics Inc. 耳鳴、急性感音性難聴、メニエール病、トゥレット症候群、注意欠陥多動性障害、および嗜癖の治療における(1s,3s)−3−アミノ−4−(ジフルオロメチリデン)シクロペンタン−1−カルボン酸および(s)−3−アミノ−4−(ジフルオロメチルエニル)シクロペンタ−1−エン−1−カルボン酸の使用
EP3758693A4 (en) * 2018-03-29 2021-06-02 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 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
KR20250051780A (ko) * 2018-05-25 2025-04-17 노오쓰웨스턴 유니버시티 (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복실산의합성을 위한 공정
PL3813816T3 (pl) 2018-06-07 2023-07-31 Ovid Therapeutics Inc. Zastosowanie kwasu (s)-3-amino-4-(difluorometylenylo)cyklopentano-1-eno-1-karboksylowego i związków pokrewnych, kwasu (1s,3s)-3-amino-4-(difluorometylideno)cyklopentano-1-karboksylowego w leczeniu zespołu łamliwego chromosomu x lub zespołu drżenia/ataksji związanego z zespołem łamliwego chromosomu x
US11203596B2 (en) 2019-02-25 2021-12-21 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
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
US20240009160A1 (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
WO2024173747A1 (en) * 2023-02-17 2024-08-22 Ovid Therapeutics Inc. Use of (s)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid in the treatment of diabetes and pre-diabetes
KR20250149771A (ko) * 2023-02-17 2025-10-16 오비드 테라퓨틱스 인크. 위장관 장애의 치료 및 면역조절제로서의 (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복시산의 용도
CN120659624A (zh) * 2023-02-17 2025-09-16 奥维德医疗公司 (s)-3-氨基-4-(二氟亚甲基)环戊-1-烯-1-甲酸在治疗多发性硬化中的用途
US20240285563A1 (en) * 2023-02-17 2024-08-29 Ovid Therapeutics Inc. Use of (s)-3-amino-4-(difluoromethylenyl) cyclopent-1-ene-1-carboxylic acid in the treatment of rheumatoid arthritis

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US6794413B1 (en) * 2002-07-19 2004-09-21 Northwestern University Compounds and related methods for inhibition of γ-aminobutyric acid aminotransferase
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WO2011106692A2 (en) * 2010-02-25 2011-09-01 Northwestern University Methods of using (1s, 3s) -3-amino-4-difluoromethylenyl-1-cyclopentanoic acid
TWI468403B (zh) * 2011-08-30 2015-01-11 Gilead Sciences Inc 用於治療成癮之aldh-2抑制劑
EP3341355B1 (en) * 2015-10-09 2020-09-30 Northwestern University (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

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Publication number Publication date
MX380592B (es) 2025-03-12
US20180271816A1 (en) 2018-09-27
BR112018007026A2 (pt) 2018-10-16
WO2017062942A3 (en) 2018-03-01
KR20180052782A (ko) 2018-05-18
CN108137484A (zh) 2018-06-08
EP3341355A4 (en) 2019-04-10
LT3341355T (lt) 2020-11-10
HK1253002A1 (zh) 2019-06-06
BR112018007026B1 (pt) 2022-06-21
IL258516A (en) 2018-05-31
CL2018000914A1 (es) 2018-08-31
JP6841821B2 (ja) 2021-03-10
KR102745965B1 (ko) 2024-12-20
CN108137484B (zh) 2021-02-12
US20170101364A1 (en) 2017-04-13
CA3001330A1 (en) 2017-04-13
HUE053429T2 (hu) 2021-07-28
PT3341355T (pt) 2020-10-21
EP3341355A2 (en) 2018-07-04
US9993449B2 (en) 2018-06-12
PE20190349A1 (es) 2019-03-07
EP3341355B1 (en) 2020-09-30
DK3341355T3 (da) 2020-10-26
AU2016334396A1 (en) 2018-04-19
WO2017062942A2 (en) 2017-04-13
JP2018531941A (ja) 2018-11-01
US20170239202A1 (en) 2017-08-24
AU2016334396B2 (en) 2021-04-08
PL3341355T3 (pl) 2021-03-08
US9670141B2 (en) 2017-06-06
CO2018003828A2 (es) 2018-07-19
MX2018004302A (es) 2018-11-09

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