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PE20190349A1 - Acido (s)-3-amino-4-(difluorometilenil) ciclopent-1-ene-1-carboxilico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adiccion y carcinoma hepatocelular - Google Patents

Acido (s)-3-amino-4-(difluorometilenil) ciclopent-1-ene-1-carboxilico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adiccion y carcinoma hepatocelular

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Publication number
PE20190349A1
PE20190349A1 PE2018000517A PE2018000517A PE20190349A1 PE 20190349 A1 PE20190349 A1 PE 20190349A1 PE 2018000517 A PE2018000517 A PE 2018000517A PE 2018000517 A PE2018000517 A PE 2018000517A PE 20190349 A1 PE20190349 A1 PE 20190349A1
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PE
Peru
Prior art keywords
cyclopent
addiction
epilepsy
ene
amino
Prior art date
Application number
PE2018000517A
Other languages
English (en)
Inventor
Richard B Silverman
Kenji Takaya
Hoang V Le
Jose I Juncosa
Original Assignee
Univ Northwestern
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Univ Northwestern filed Critical Univ Northwestern
Publication of PE20190349A1 publication Critical patent/PE20190349A1/es

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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)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Referido a un compuesto de formula (I), en el que cada uno de R1 y R2 se selecciona independientemente de H, F, Cl, Br, e I. Estos compuestos, Acido (s)-3-amino-4-(difluorometilenil) ciclopent-1-ene-1-carboxilico y compuestos relacionados son utilizados como inhibidores selectivos de acido gamma-aminobutirico aminotransferasa (GABA-AT). Tambien se refiere a metodos de preparacion de estos compuestos y sus usos para el tratamiento de epilepsia, convulsiones, adiccion, entre otros.
PE2018000517A 2015-10-09 2016-10-10 Acido (s)-3-amino-4-(difluorometilenil) ciclopent-1-ene-1-carboxilico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adiccion y carcinoma hepatocelular PE20190349A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562239330P 2015-10-09 2015-10-09

Publications (1)

Publication Number Publication Date
PE20190349A1 true PE20190349A1 (es) 2019-03-07

Family

ID=58488679

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018000517A PE20190349A1 (es) 2015-10-09 2016-10-10 Acido (s)-3-amino-4-(difluorometilenil) ciclopent-1-ene-1-carboxilico y compuestos relacionados como inactivadores de gaba aminotransferasa para el tratamiento de epilepsia, adiccion y carcinoma hepatocelular

Country Status (20)

Country Link
US (3) US9670141B2 (es)
EP (1) EP3341355B1 (es)
JP (1) JP6841821B2 (es)
KR (1) KR102745965B1 (es)
CN (1) CN108137484B (es)
AU (1) AU2016334396B2 (es)
BR (1) BR112018007026B1 (es)
CA (1) CA3001330A1 (es)
CL (1) CL2018000914A1 (es)
CO (1) CO2018003828A2 (es)
DK (1) DK3341355T3 (es)
ES (1) ES2825349T3 (es)
HU (1) HUE053429T2 (es)
IL (1) IL258516A (es)
LT (1) LT3341355T (es)
MX (1) MX380592B (es)
PE (1) PE20190349A1 (es)
PL (1) PL3341355T3 (es)
PT (1) PT3341355T (es)
WO (1) WO2017062942A2 (es)

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PT3183254T (pt) 2014-08-21 2019-08-29 Boehringer Ingelheim Int Novos compostos de espiro[3h-indole-3,2¿-pirrolidin]-2(1h)-ona e derivados como inibidores de mdm2-p53
PL3341355T3 (pl) * 2015-10-09 2021-03-08 Northwestern University Kwas (S)-3-amino-4-(difluorometylenylo)cyklopent-1-eno-1-karboksylowy i związki pokrewne jako dezaktywatory aminotransferazy GABA do leczenia padaczki, uzależnienia oraz raka wątrobowokomórkowego
SI3359542T1 (sl) 2015-10-09 2021-08-31 Boehringer Ingelheim International Gmbh Spojine in derivati spiro(3H-indol-3,2'-pirolidin)-2(1H)-ona kot MDM2-P53 inhibitorji
KR20240110989A (ko) 2017-02-08 2024-07-16 오비드 테라퓨틱스 인크. 프라더-윌리 증후군 및 발작 장애들을 치료하는 방법들
US10653652B2 (en) 2018-02-08 2020-05-19 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
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
CN112218628A (zh) * 2018-03-29 2021-01-12 奥维德医疗公司 (1s,3s)-3-氨基-4-(二氟亚甲基)环戊烷-1-甲酸和(s)-3-氨基-4-(二氟亚甲基)环戊-1-烯-1-甲酸在治疗眼紊乱中的用途
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
US10836708B2 (en) * 2018-05-25 2020-11-17 Northwestern University Process for the synthesis of (s) 3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid
JP7387179B2 (ja) 2018-06-07 2023-11-28 オービッド・セラピューティクス・インコーポレイテッド 発達障害の処置における(s)-3-アミノ-4-(ジフルオロメチレニル)シクロペンタ-1-エン-1-カルボン酸および関連化合物、(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-カルボン酸ならびにビガバトリンの使用
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
EP4551205A4 (en) * 2022-07-06 2025-11-12 Ovid Therapeutics Inc USE OF (S)-3-AMINO-4-(DIFLUOROMETHYLENYL) CYCLOPENT-1-ENE-1-CARBOXYLIC ACID IN CANCER TREATMENT
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
KR20250145688A (ko) * 2023-02-17 2025-10-13 오비드 테라퓨틱스 인크. 당뇨병 및 당뇨 전단계의 치료에 있어서 (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복시산의 용도
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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EP2542234A4 (en) * 2010-02-25 2013-07-31 Univ Northwestern PROCESS FOR USE OF (1S, 3S -) - 3-AMINO-4-DIFLUOROMETHYLENYL-1-CYCLOPENTANIC ACID
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PL3341355T3 (pl) * 2015-10-09 2021-03-08 Northwestern University Kwas (S)-3-amino-4-(difluorometylenylo)cyklopent-1-eno-1-karboksylowy i związki pokrewne jako dezaktywatory aminotransferazy GABA do leczenia padaczki, uzależnienia oraz raka wątrobowokomórkowego

Also Published As

Publication number Publication date
US20170239202A1 (en) 2017-08-24
CN108137484B (zh) 2021-02-12
US9993449B2 (en) 2018-06-12
PL3341355T3 (pl) 2021-03-08
CN108137484A (zh) 2018-06-08
HUE053429T2 (hu) 2021-07-28
AU2016334396A1 (en) 2018-04-19
IL258516A (en) 2018-05-31
US20180271816A1 (en) 2018-09-27
US9670141B2 (en) 2017-06-06
BR112018007026A2 (pt) 2018-10-16
WO2017062942A3 (en) 2018-03-01
BR112018007026B1 (pt) 2022-06-21
AU2016334396B2 (en) 2021-04-08
MX380592B (es) 2025-03-12
US20170101364A1 (en) 2017-04-13
EP3341355A2 (en) 2018-07-04
HK1253002A1 (zh) 2019-06-06
PT3341355T (pt) 2020-10-21
LT3341355T (lt) 2020-11-10
KR102745965B1 (ko) 2024-12-20
EP3341355A4 (en) 2019-04-10
CA3001330A1 (en) 2017-04-13
CO2018003828A2 (es) 2018-07-19
ES2825349T3 (es) 2021-05-17
EP3341355B1 (en) 2020-09-30
JP6841821B2 (ja) 2021-03-10
JP2018531941A (ja) 2018-11-01
KR20180052782A (ko) 2018-05-18
WO2017062942A2 (en) 2017-04-13
DK3341355T3 (da) 2020-10-26
MX2018004302A (es) 2018-11-09
CL2018000914A1 (es) 2018-08-31

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