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PE20020927A1 - Uso de agonistas inversos de gaba a en combinacion con agonistas parciales del receptor de nicotina, estrogenos, moduladores selectivos de estrogenos o vitamina e, para el tratamiento de trastornos cognitivos - Google Patents

Uso de agonistas inversos de gaba a en combinacion con agonistas parciales del receptor de nicotina, estrogenos, moduladores selectivos de estrogenos o vitamina e, para el tratamiento de trastornos cognitivos

Info

Publication number
PE20020927A1
PE20020927A1 PE2002000157A PE2002000157A PE20020927A1 PE 20020927 A1 PE20020927 A1 PE 20020927A1 PE 2002000157 A PE2002000157 A PE 2002000157A PE 2002000157 A PE2002000157 A PE 2002000157A PE 20020927 A1 PE20020927 A1 PE 20020927A1
Authority
PE
Peru
Prior art keywords
alkyl
agonists
cycloalkyl
estrogens
estrogen
Prior art date
Application number
PE2002000157A
Other languages
English (en)
Inventor
Anabella Villalobos
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of PE20020927A1 publication Critical patent/PE20020927A1/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355Tocopherols, e.g. vitamin E
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Psychology (AREA)
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  • Tropical Medicine & Parasitology (AREA)
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  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE: a)AGONISTA INVERSO DEL RECEPTOR GABA A SUBTIPO O5 DE FORMULA I DONDE X ES H, HALOGENO, OR1, NR2R3, ALQUILO C1-C6, FENILO, NAFTILO, CARBOCICLO C3-C7, ENTRE OTROS; Y ES ALQUILO C1-C8, CARBOCICLO, ENTRE OTROS; R1 Y R4 SON H, ALQUILO C1-C6, CICLOALQUILO C3-C7 OPCIONALMENTE SUSTITUIDO CON OR4, NR5R6; R2, R3, R5 Y R6 SON H, ALQUILO OPCIONALMENTE SUSTITUIDO CON ALQUILO, ARILO, HALOGENO, ENTRE OTROS; R7 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C7; R8 ES ALQUILO C1-C6, CICLOALQUILO C3-C7; R8 ES ALQUILO C1-C6, CICLOALQUILO C3-C7, FENILO; SON COMPUESTOS PREFERIDOS N-n-BUTIL-6-CLORO-4-OXO-1,4-TETRAHIDRO-1,5-NAFTIRIDINA-3-CARBOXAMIDA; N-n-BUTIL-6-ETOXI-4-OXO-1,4-TETRAHIDRO-1,5-NAFTIRIDINA-3-CARBOXAMIDA, ENTRE OTROS; b)AGONISTA PARCIAL DEL RECEPTOR DE NICOTINA (NRPA) TAL COMO 9-BROMO-1,2,3,4,5,6-HEXAHIDRO-1,5-METANO-PIRIDO[1,2-a][1,5]DIAZOCIN-8-ONA; 9-CLORO-1,2,3,4,5,6-HEXAHIDRO-1,5-METANO-PIRIDO[1,2-a[1,5]DIAZOCIN-8-ONA, ENTRE OTROS, c)ESTROGENOS, d)MODULADORES SELECTIVOS DE ESTROGENOS O VITAMINA E. LA COMPOSICION POTENCIA LA COGNICION Y PUEDE SER UTIL PARA EL TRATAMIENTO DE ALZHEIMER, DETERIORO COGNITIVO LEVE, REDUCCION COGNITIVA RELACIONADA CON LA EDAD, DEMENCIA VASCULAR, PARKINSON, HUNTINGTON
PE2002000157A 2001-03-01 2002-02-26 Uso de agonistas inversos de gaba a en combinacion con agonistas parciales del receptor de nicotina, estrogenos, moduladores selectivos de estrogenos o vitamina e, para el tratamiento de trastornos cognitivos PE20020927A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US27256601P 2001-03-01 2001-03-01

Publications (1)

Publication Number Publication Date
PE20020927A1 true PE20020927A1 (es) 2002-10-30

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PE2002000157A PE20020927A1 (es) 2001-03-01 2002-02-26 Uso de agonistas inversos de gaba a en combinacion con agonistas parciales del receptor de nicotina, estrogenos, moduladores selectivos de estrogenos o vitamina e, para el tratamiento de trastornos cognitivos

Country Status (33)

Country Link
US (2) US20020193360A1 (es)
EP (1) EP1363606A1 (es)
JP (1) JP2004527500A (es)
KR (1) KR20030076717A (es)
CN (1) CN1494422A (es)
AP (1) AP2002002465A0 (es)
AR (1) AR033425A1 (es)
BG (1) BG108131A (es)
BR (1) BR0207802A (es)
CA (1) CA2439581A1 (es)
CR (1) CR7059A (es)
CZ (1) CZ20032338A3 (es)
DO (1) DOP2002000345A (es)
EA (1) EA200300854A1 (es)
EC (1) ECSP034759A (es)
EE (1) EE200300422A (es)
GT (1) GT200200039A (es)
HU (1) HUP0303448A3 (es)
IL (1) IL157465A0 (es)
IS (1) IS6905A (es)
MA (1) MA26999A1 (es)
MX (1) MXPA03007834A (es)
NO (1) NO20033821L (es)
NZ (1) NZ527397A (es)
OA (1) OA12554A (es)
PA (1) PA8540701A1 (es)
PE (1) PE20020927A1 (es)
PL (1) PL364081A1 (es)
SK (1) SK10752003A3 (es)
TN (1) TNSN02018A1 (es)
UY (1) UY27188A1 (es)
WO (1) WO2002069948A1 (es)
ZA (1) ZA200306193B (es)

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US20080004332A1 (en) * 2002-03-07 2008-01-03 Alkon Daniel L Methods for alzheimer's disease treatment and cognitive enhancement
US20050065205A1 (en) * 2002-03-07 2005-03-24 Daniel Alkon Methods for Alzheimer's disease treatment and cognitive enhance
US6825229B2 (en) 2002-03-07 2004-11-30 Blanchette Rockefeller Neurosciences Institute Methods for Alzheimer's Disease treatment and cognitive enhancement
US8030300B2 (en) 2003-06-10 2011-10-04 Georgetown University Ligands for nicotinic acetylcholine receptors, and methods of making and using them
TW201206425A (en) 2004-05-18 2012-02-16 Brni Neurosciences Inst Treatment of depressive disorders
US8510055B2 (en) 2005-08-03 2013-08-13 The Johns Hopkins University Methods for characterizing and treating cognitive impairment in aging and disease
EP2682481A3 (en) * 2005-08-03 2014-09-17 The Johns-Hopkins University Methods for characterizing and treating cognitive impairment in aging and disease
EP3050562A1 (en) 2006-05-22 2016-08-03 The Board of Trustees of the Leland Stanford Junior University Pharmacological treatment of cognitive impairment using gabaa receptor antagonists
US10954231B2 (en) 2006-10-16 2021-03-23 Bionomics Limited Anxiolytic compounds
AU2013202426B2 (en) * 2006-10-16 2015-08-06 Bionomics Limited Novel anxiolytic compounds
AU2007312936B2 (en) * 2006-10-16 2013-09-26 Bionomics Limited Novel anxiolytic compounds
EP3332797A3 (en) 2007-02-09 2018-08-01 Blanchette Rockefeller Neurosciences Institute Therapeutic effects of bryostatins, bryologs and other related substances on head trauma-induced memory impairment and brain injury
US8039620B2 (en) * 2008-05-22 2011-10-18 Teva Pharmaceutical Industries Ltd. Varenicline tosylate, an intermediate in the preparation process of varenicline L-tartrate
US20090318695A1 (en) * 2008-06-19 2009-12-24 Vinod Kumar Kansal Processes for the preparation of varenicline and intermediates thereof
US20100010221A1 (en) * 2008-07-10 2010-01-14 Revital Lifshitz-Liron Processes for purifying varenicline l-tartrate salt and preparing crystalline forms of varenicline l-tartrate salt
US10206921B2 (en) * 2009-06-03 2019-02-19 The Regents Of The University Of California Methods and compositions for treating a subject for central nervous system (CNS) injury
RU2012102052A (ru) * 2009-06-22 2013-11-20 Тева Фармасьютикал Индастриз Лтд. Твердые формы солей варениклина и способы их получения
CN103313712B (zh) 2010-11-15 2016-10-26 艾吉因生物股份有限公司 用于治疗认知障碍的哒嗪衍生物、组合物和方法
AU2012222874B2 (en) 2011-03-02 2015-04-16 Bionomics Limited Novel small-molecules as therapeutics
AU2012222869B2 (en) * 2011-03-02 2015-08-13 Bionomics Limited Methods of treating a disease or condition of the central nervous system
WO2012151640A1 (en) 2011-05-12 2012-11-15 Bionomics Limited Methods for preparing naphthyridines
US10329301B2 (en) 2013-12-20 2019-06-25 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
CN113264939A (zh) 2015-06-19 2021-08-17 艾吉因生物股份有限公司 用于治疗认知损害的苯并二氮杂环庚三烯衍生物、组合物和方法
US20180170941A1 (en) 2016-12-19 2018-06-21 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
BR112019012821A2 (pt) 2016-12-19 2019-11-26 Agenebio, Inc. derivados de benzodiazepina, composições e métodos para o tratamento do comprometimento cognitivo
EA202190076A1 (ru) 2018-06-19 2021-09-22 Эйджинбайо, Инк. Производные бензодиазепина, композиции и способы лечения когнитивных нарушений
CN116008442B (zh) * 2023-03-27 2023-06-30 上海赛默罗生物科技有限公司 α5-GABAA受体调节剂的合成中间体的杂质检测方法
CN116077459B (zh) * 2023-04-10 2023-07-07 上海赛默罗生物科技有限公司 α5-GABAA受体调节剂的胶囊剂及其制备方法

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IL134291A0 (en) * 1997-08-25 2001-04-30 Neurogen Corp Substituted 4-oxo-napthyridine-3- carboxamides as gaba brain receptor ligands
AU5289600A (en) * 1999-05-25 2000-12-12 Neurogen Corporation 4h-1,4-benzothiazine-2-carboxamides and their use as gaba brain receptor ligands

Also Published As

Publication number Publication date
ECSP034759A (es) 2003-10-28
MXPA03007834A (es) 2003-12-08
US20040082555A1 (en) 2004-04-29
EA200300854A1 (ru) 2004-02-26
AP2002002465A0 (en) 2002-06-30
EP1363606A1 (en) 2003-11-26
US20020193360A1 (en) 2002-12-19
IS6905A (is) 2003-08-07
GT200200039A (es) 2002-11-21
HUP0303448A3 (en) 2005-05-30
EE200300422A (et) 2004-02-16
UY27188A1 (es) 2002-10-31
MA26999A1 (fr) 2004-12-20
CN1494422A (zh) 2004-05-05
CR7059A (es) 2004-03-10
ZA200306193B (en) 2004-08-11
IL157465A0 (en) 2004-03-28
PL364081A1 (en) 2004-12-13
HUP0303448A2 (hu) 2004-01-28
PA8540701A1 (es) 2002-09-30
BG108131A (en) 2004-09-30
NZ527397A (en) 2005-05-27
TNSN02018A1 (fr) 2005-12-23
KR20030076717A (ko) 2003-09-26
NO20033821D0 (no) 2003-08-28
WO2002069948A1 (en) 2002-09-12
NO20033821L (no) 2003-09-10
OA12554A (en) 2006-06-07
JP2004527500A (ja) 2004-09-09
SK10752003A3 (sk) 2004-08-03
CZ20032338A3 (cs) 2004-08-18
DOP2002000345A (es) 2002-12-15
AR033425A1 (es) 2003-12-17
CA2439581A1 (en) 2002-09-12
BR0207802A (pt) 2004-03-09

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