KR102745965B1 - 간질, 중독 및 간세포암종의 치료를 위한 gaba 아미노트랜스페라제 불활성화제들로서 (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복실산, 및 관련된 화합물들 - Google Patents

간질, 중독 및 간세포암종의 치료를 위한 gaba 아미노트랜스페라제 불활성화제들로서 (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복실산, 및 관련된 화합물들 Download PDF

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KR102745965B1
KR102745965B1 KR1020187013228A KR20187013228A KR102745965B1 KR 102745965 B1 KR102745965 B1 KR 102745965B1 KR 1020187013228 A KR1020187013228 A KR 1020187013228A KR 20187013228 A KR20187013228 A KR 20187013228A KR 102745965 B1 KR102745965 B1 KR 102745965B1
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리차드 비. 실버맨
켄지 타카야
브이 리 호안
요세 아이. 준코사
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노오쓰웨스턴 유니버시티
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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
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    • AHUMAN NECESSITIES
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    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
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    • A61P25/08Antiepileptics; Anticonvulsants
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    • 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
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    • 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
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    • 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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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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KR1020187013228A 2015-10-09 2016-10-10 간질, 중독 및 간세포암종의 치료를 위한 gaba 아미노트랜스페라제 불활성화제들로서 (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복실산, 및 관련된 화합물들 Active KR102745965B1 (ko)

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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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KR102745965B1 true KR102745965B1 (ko) 2024-12-20

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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.
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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
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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
ES2825349T3 (es) 2021-05-17
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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