AU2003230754B2 - Anxiolytic agents with reduced sedative and ataxic effects - Google Patents

Anxiolytic agents with reduced sedative and ataxic effects Download PDF

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Publication number
AU2003230754B2
AU2003230754B2 AU2003230754A AU2003230754A AU2003230754B2 AU 2003230754 B2 AU2003230754 B2 AU 2003230754B2 AU 2003230754 A AU2003230754 A AU 2003230754A AU 2003230754 A AU2003230754 A AU 2003230754A AU 2003230754 B2 AU2003230754 B2 AU 2003230754B2
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compound
cyclopropyl
salt
mixture
substituted
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AU2003230754A
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AU2003230754A1 (en
Inventor
James M Cook
Dongmei Han
Xiaohui He
Qi Huang
Xiaoyan Li
Jianming Yu
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WiSys
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WiSys
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Publication of AU2003230754B2 publication Critical patent/AU2003230754B2/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/12—1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2003230754A 2002-03-28 2003-03-28 Anxiolytic agents with reduced sedative and ataxic effects Ceased AU2003230754B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2007221890A AU2007221890A1 (en) 2002-03-28 2007-10-09 Anxiolytic agents with reduced sedative and ataxic effects

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36840802P 2002-03-28 2002-03-28
US60/368,408 2002-03-28
PCT/US2003/009587 WO2003082832A2 (en) 2002-03-28 2003-03-28 Anxiolytic agents with reduced sedative and ataxic effects

Related Child Applications (1)

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AU2007221890A Division AU2007221890A1 (en) 2002-03-28 2007-10-09 Anxiolytic agents with reduced sedative and ataxic effects

Publications (2)

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AU2003230754A1 AU2003230754A1 (en) 2003-10-13
AU2003230754B2 true AU2003230754B2 (en) 2007-10-25

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AU2003230754A Ceased AU2003230754B2 (en) 2002-03-28 2003-03-28 Anxiolytic agents with reduced sedative and ataxic effects

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US (6) US7119196B2 (enExample)
EP (1) EP1490344B1 (enExample)
JP (1) JP2005525392A (enExample)
KR (2) KR100865410B1 (enExample)
CN (1) CN1642924A (enExample)
AT (1) ATE389640T1 (enExample)
AU (1) AU2003230754B2 (enExample)
BR (1) BR0308918A (enExample)
CA (1) CA2480869A1 (enExample)
DE (1) DE60319812T2 (enExample)
DK (1) DK1490344T3 (enExample)
ES (1) ES2300576T3 (enExample)
IL (1) IL163958A0 (enExample)
MX (1) MXPA04009332A (enExample)
NZ (1) NZ535517A (enExample)
WO (1) WO2003082832A2 (enExample)

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USRE47475E1 (en) * 2002-03-28 2019-07-02 Wisys Technology Foundation, Inc. Selective agents for pain suppression
AU2005260650A1 (en) 2004-06-30 2006-01-12 Wisys Technology Foundation, Inc. Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects
US8119629B2 (en) * 2007-10-03 2012-02-21 Bristol-Meyers Squibb Company Carboxamide GABAA α2 modulators
US7709522B2 (en) * 2008-01-22 2010-05-04 Eli Lilly And Company Kappa selective opioid receptor antagonist
US20100261711A1 (en) * 2009-03-20 2010-10-14 Wisys Technology Foundation Selective anticonvulsant agents and their uses
JP2013209292A (ja) * 2010-07-23 2013-10-10 Nippon Chemiphar Co Ltd Ｐ２ｘ４受容体拮抗剤
US9006233B2 (en) 2011-04-28 2015-04-14 Uwm Research Foundation, Inc. Gabaergic receptor subtype selective ligands and their uses
US20150374705A1 (en) 2012-02-14 2015-12-31 Shanghai Institues for Biological Sciences Substances for treatment or relief of pain
CA2885148A1 (en) 2012-09-21 2014-03-27 Uwm Research Foundation, Inc. Novel gabaa agonists and methods of using to control airway hyperresponsiveness and inflammation in asthma
FR3010785B1 (fr) * 2013-09-18 2015-08-21 Snecma Procede de controle de la densite d'energie d'un faisceau laser par analyse d'image et dispositif correspondant
BR112018015386A2 (pt) 2016-01-27 2019-03-19 Universität Zürich uso de moduladores de receptor gabaa para tratamento de prurido
EP4129297A1 (en) 2016-03-18 2023-02-08 UWM Research Foundation, Inc. Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists
AU2017313753B2 (en) 2016-08-16 2022-01-27 The Trustees Of Columbia University In The City Of New York GABA(A) receptor modulators and methods to control airway hyperresponsiveness and inflammation in asthma
JP7139323B2 (ja) * 2016-11-01 2022-09-20 エフ．ホフマン－ラ ロシュ アーゲー Ｃｎｓ関連疾患を処置するための１，３－ジヒドロ－１，４－ベンゾジアゼピン－２－チオン
CN107056760A (zh) * 2017-01-22 2017-08-18 苏州楚凯药业有限公司 5,7位取代的1H‑苯并[e][1,4]二氮杂‑2(3H)‑酮衍生物的制备方法
CN107325101B (zh) * 2017-06-29 2019-03-26 上海合全药物研发有限公司 6-羟甲基-6,7-二氢-5h,9h-咪唑并二氮杂卓-8-羧酸叔丁酯的合成方法
CN107216332B (zh) * 2017-06-29 2019-04-30 上海药明康德新药开发有限公司 叔丁基-7-羟甲基-7,8-二氢4h吡唑并二氮杂卓5(6h)甲酸基酯的合成方法
WO2019070910A1 (en) 2017-10-03 2019-04-11 Uwm Research Foundation, Inc. NEW POLYTHERAPY FOR ANXIETY, EPILEPSY AND PAIN DISORDERS
TWI878507B (zh) 2020-03-31 2025-04-01 瑞士商赫孚孟拉羅股份公司 作為 GABA A γ1 PAM 的新穎苯并二氮呯衍生物
US12161622B2 (en) 2021-05-04 2024-12-10 Janssen Pharmaceuticals, Inc. Compositions and methods for the treatment of depression
AR127127A1 (es) * 2021-09-24 2023-12-20 Hoffmann La Roche NUEVOS DERIVADOS DE PIRIDODIAZEPINAS COMO PAM DE GABAA g1
JP2024537773A (ja) 2021-09-29 2024-10-16 エフ． ホフマン－ラ ロシュ アーゲー ＧＡＢＡ Ａγ１ ＰＡＭとしての新規ベンゾジアゼピン誘導体
WO2023057415A1 (en) 2021-10-06 2023-04-13 F. Hoffmann-La Roche Ag Benzodiazepine derivatives as positive allosteric modulators of the gaba a gamma1 receptor
CN119156211A (zh) 2022-03-07 2024-12-17 杨森制药公司 用于治疗重性抑郁障碍的多晶型形式的阿替卡普兰
CA3254546A1 (en) 2022-03-07 2023-09-14 Janssen Pharmaceuticals, Inc. COMPOSITIONS CONTAINING ATICAPRANT
WO2024030535A2 (en) * 2022-08-03 2024-02-08 The Johns Hopkins University Peripherally restricted gaba positive allosteric modulators for the treatment of irritable bowel syndrome and other ailments of the peripheral nervous system

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Also Published As

Publication number Publication date
US20070054881A1 (en) 2007-03-08
US7235656B2 (en) 2007-06-26
US20080108605A1 (en) 2008-05-08
WO2003082832A3 (en) 2004-04-08
WO2003082832A2 (en) 2003-10-09
CA2480869A1 (en) 2003-10-09
KR20040098029A (ko) 2004-11-18
CN1642924A (zh) 2005-07-20
US20070299058A1 (en) 2007-12-27
IL163958A0 (en) 2005-12-18
US7119196B2 (en) 2006-10-10
US20100130481A1 (en) 2010-05-27
DE60319812T2 (de) 2009-04-23
AU2003230754A1 (en) 2003-10-13
MXPA04009332A (es) 2005-12-12
ATE389640T1 (de) 2008-04-15
NZ535517A (en) 2007-02-23
DK1490344T3 (da) 2008-06-16
EP1490344A2 (en) 2004-12-29
US20040082573A1 (en) 2004-04-29
DE60319812D1 (de) 2008-04-30
ES2300576T3 (es) 2008-06-16
US20070049580A1 (en) 2007-03-01
KR100865410B1 (ko) 2008-10-24
KR20080060286A (ko) 2008-07-01
JP2005525392A (ja) 2005-08-25
EP1490344B1 (en) 2008-03-19
BR0308918A (pt) 2005-01-04

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