JP6841821B2 - 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 - Google Patents

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 Download PDF

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JP6841821B2
JP6841821B2 JP2018517734A JP2018517734A JP6841821B2 JP 6841821 B2 JP6841821 B2 JP 6841821B2 JP 2018517734 A JP2018517734 A JP 2018517734A JP 2018517734 A JP2018517734 A JP 2018517734A JP 6841821 B2 JP6841821 B2 JP 6841821B2
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gaba
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JP2018531941A5 (OSRAM
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リチャード・ビー・シルバーマン
健二 高谷
健二 高谷
ホアン・ブイ・レー
ホセ・アイ・ジャンコーサ
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ノースウェスタン ユニバーシティ
ノースウェスタン ユニバーシティ
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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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  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2018517734A 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 Active JP6841821B2 (ja)

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

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JP2018531941A JP2018531941A (ja) 2018-11-01
JP2018531941A5 JP2018531941A5 (OSRAM) 2019-11-21
JP6841821B2 true JP6841821B2 (ja) 2021-03-10

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US (3) US9670141B2 (OSRAM)
EP (1) EP3341355B1 (OSRAM)
JP (1) JP6841821B2 (OSRAM)
KR (1) KR102745965B1 (OSRAM)
CN (1) CN108137484B (OSRAM)
AU (1) AU2016334396B2 (OSRAM)
BR (1) BR112018007026B1 (OSRAM)
CA (1) CA3001330A1 (OSRAM)
CL (1) CL2018000914A1 (OSRAM)
CO (1) CO2018003828A2 (OSRAM)
DK (1) DK3341355T3 (OSRAM)
ES (1) ES2825349T3 (OSRAM)
HU (1) HUE053429T2 (OSRAM)
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HRP20191414T1 (hr) 2014-08-21 2019-11-01 Boehringer Ingelheim Int Novi spojevi i derivati spiro[3h-indol-3,2'-pirolidin]-2(1h)-ona kao mdm1-p53-inhibitori
LT3341355T (lt) * 2015-10-09 2020-11-10 Northwestern University (s)-3-amino-4-(difluormetilenil)ciklopent-1-en-1-karboksirūgštis ir giminingi junginiai kaip gaba aminotransferazės inaktyvatoriai, skirti epilepsijos, priklausomybės ir kepenų ląstelių karcinomos gydymui
HUE054985T2 (hu) 2015-10-09 2021-11-29 Boehringer Ingelheim Int Spiro[3H-indol-3,2'-pirrolidin]-2(1H)-on vegyületek és számrazékok, mint MDM2-P53 inhibitorok
KR20240110989A (ko) 2017-02-08 2024-07-16 오비드 테라퓨틱스 인크. 프라더-윌리 증후군 및 발작 장애들을 치료하는 방법들
KR20240154700A (ko) * 2018-02-08 2024-10-25 오비드 테라퓨틱스 인크. 이명, 급성 감각신경성 난청, 메니에르병, 투렛 증후군, 주의력 결핍 과잉행동 장애 및 중독의 치료에 있어서 (1s,3s)-3-아미노-4-(디플루오로메틸리덴) 시클로펜탄-1-카르복시산 및 (s)-3-아미노-4-(디플루오로메틸리덴)시클로펜트-1-엔-1-카르복시산의 용도
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
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
CN117550990B (zh) * 2018-05-25 2025-09-16 西北大学 用于合成(s)-3-氨基-4-(二氟亚甲基)环戊-1-烯-1-甲酸的工艺
KR102744830B1 (ko) 2018-06-07 2024-12-19 오비드 테라퓨틱스 인크. 발달 장애 치료에 있어서, (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복실산 및 관련된 화합물들, (1s,3s)-3-아미노-4-(디플루오로메틸리덴) 사이클로펜탄 -1-카르복실산 및 비가바트린의 사용
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
EP4301724A4 (en) * 2021-03-03 2025-05-28 Northwestern University (S)-3-AMINO-4,4-DIHALOCYCLOPENT-1-CARBOXYLIC ACID AS SELECTIVE INACTIVATORS OF HUMAN ORNITHINE AMINOTRANSFERASE
CA3260997A1 (en) * 2022-07-06 2024-01-11 Ovid Therapeutics Inc. USE OF (S)-3-AMINO-4-(DIFLUOROMETHYLENYL) CYCLOPENT-1-ENE-1-CARBOXYLIC ACID IN CANCER TREATMENT
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
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
EP4648797A4 (en) * 2023-02-17 2025-12-24 Ovid Therapeutics Inc USE OF (S)-3-AMINO-4-(DIFLUOROMETHYLENYL)CYCLOPENT-1-ENE-1-CARBOXYLIC ACID IN THE TREATMENT OF MULTIPLE SCLEROSIS
EP4665324A1 (en) * 2023-02-17 2025-12-24 Ovid Therapeutics Inc. Use of (s)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid in the treatment of diabetes and pre-diabetes

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IL177609A (en) * 2006-08-21 2015-11-30 Yaron Ilan Use of gobacoline or its analogue to produce a drug to treat liver carcinoma
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LT3341355T (lt) * 2015-10-09 2020-11-10 Northwestern University (s)-3-amino-4-(difluormetilenil)ciklopent-1-en-1-karboksirūgštis ir giminingi junginiai kaip gaba aminotransferazės inaktyvatoriai, skirti epilepsijos, priklausomybės ir kepenų ląstelių karcinomos gydymui

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EP3341355A2 (en) 2018-07-04
KR102745965B1 (ko) 2024-12-20
BR112018007026A2 (pt) 2018-10-16
PE20190349A1 (es) 2019-03-07
JP2018531941A (ja) 2018-11-01
CN108137484B (zh) 2021-02-12
ES2825349T3 (es) 2021-05-17
US20180271816A1 (en) 2018-09-27
IL258516A (en) 2018-05-31
MX2018004302A (es) 2018-11-09
US9993449B2 (en) 2018-06-12
LT3341355T (lt) 2020-11-10
EP3341355B1 (en) 2020-09-30
US20170101364A1 (en) 2017-04-13
AU2016334396A1 (en) 2018-04-19
HK1253002A1 (zh) 2019-06-06
CL2018000914A1 (es) 2018-08-31
DK3341355T3 (da) 2020-10-26
KR20180052782A (ko) 2018-05-18
WO2017062942A3 (en) 2018-03-01
PT3341355T (pt) 2020-10-21
CO2018003828A2 (es) 2018-07-19
US9670141B2 (en) 2017-06-06
CN108137484A (zh) 2018-06-08
AU2016334396B2 (en) 2021-04-08
CA3001330A1 (en) 2017-04-13
BR112018007026B1 (pt) 2022-06-21
HUE053429T2 (hu) 2021-07-28
PL3341355T3 (pl) 2021-03-08
WO2017062942A2 (en) 2017-04-13
US20170239202A1 (en) 2017-08-24
MX380592B (es) 2025-03-12
EP3341355A4 (en) 2019-04-10

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