CN1642924A - 减少了镇静与共济失调效果的抗焦虑剂 - Google Patents

减少了镇静与共济失调效果的抗焦虑剂 Download PDF

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Publication number
CN1642924A
CN1642924A CNA038073439A CN03807343A CN1642924A CN 1642924 A CN1642924 A CN 1642924A CN A038073439 A CNA038073439 A CN A038073439A CN 03807343 A CN03807343 A CN 03807343A CN 1642924 A CN1642924 A CN 1642924A
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substituted
thienyl
phenyl
cyclopropyl
ring
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Chinese (zh)
Inventor
J·M·库克
黄琦
贺晓晖
李晓燕
于建明
韩冬梅
S·勒拉斯
J·F·麦塞尔洛伊
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WiSys Technology Foundation Inc
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WiSys Technology Foundation Inc
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic 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
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic 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
    • C07D243/121,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic 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
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic 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
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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
    • C07D495/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
CNA038073439A 2002-03-28 2003-03-28 减少了镇静与共济失调效果的抗焦虑剂 Pending CN1642924A (zh)

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US36840802P 2002-03-28 2002-03-28
US60/368,408 2002-03-28

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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)
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN107216332A (zh) * 2017-06-29 2017-09-29 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
CN107325101A (zh) * 2017-06-29 2017-11-07 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

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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
NZ586225A (en) * 2008-01-22 2012-05-25 Lilly Co Eli 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
WO2014047413A1 (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
EP3407886A1 (en) 2016-01-27 2018-12-05 Universität Zürich Use of gabaa receptor modulators for treatment of itch
WO2017161370A1 (en) 2016-03-18 2017-09-21 Uwm Reseach Foundation, Inc. Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists
CN109790170B (zh) 2016-08-16 2022-08-02 Uwm研究基金会有限公司 Gaba(a)受体调节剂和控制哮喘中气道高反应性和炎症的方法
CN109906220A (zh) * 2016-11-01 2019-06-18 豪夫迈·罗氏有限公司 用于治疗cns相关疾病的1,3-二氢-1,4-苯并二氮杂*-2-硫酮化合物
WO2019070910A1 (en) 2017-10-03 2019-04-11 Uwm Research Foundation, Inc. NEW POLYTHERAPY FOR ANXIETY, EPILEPSY AND PAIN DISORDERS
CA3167543A1 (en) 2020-03-31 2021-10-07 F. Hoffmann-La Roche Ag Benzodiazepine derivatives as gaba a gamma1 pams
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
CN118019742A (zh) 2021-09-29 2024-05-10 豪夫迈·罗氏有限公司 作为GABA A γ1 PAM的新颖苯并二氮杂䓬衍生物
KR20240073892A (ko) 2021-10-06 2024-05-27 에프. 호프만-라 로슈 아게 Gaba a gamma1 수용체의 양성 알로스테릭 조절인자로서의 벤조디아제핀 유도체
IL315415A (en) 2022-03-07 2024-11-01 Janssen Pharmaceuticals Inc The compositions containing eticarpant
CA3254365A1 (en) 2022-03-07 2023-09-14 Janssen Pharmaceuticals, Inc. POLYMORPHIC FORMS OF ATICAPRANT INTENDED FOR USE IN THE TREATMENT OF MAJOR DEPRESSION

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN107216332A (zh) * 2017-06-29 2017-09-29 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
CN107325101A (zh) * 2017-06-29 2017-11-07 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
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

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US20070049580A1 (en) 2007-03-01
US20070299058A1 (en) 2007-12-27
US20070054881A1 (en) 2007-03-08
EP1490344A2 (en) 2004-12-29
WO2003082832A3 (en) 2004-04-08
CA2480869A1 (en) 2003-10-09
KR20080060286A (ko) 2008-07-01
US20080108605A1 (en) 2008-05-08
AU2003230754B2 (en) 2007-10-25
KR100865410B1 (ko) 2008-10-24
DK1490344T3 (da) 2008-06-16
DE60319812T2 (de) 2009-04-23
NZ535517A (en) 2007-02-23
DE60319812D1 (de) 2008-04-30
EP1490344B1 (en) 2008-03-19
US7235656B2 (en) 2007-06-26
US20100130481A1 (en) 2010-05-27
JP2005525392A (ja) 2005-08-25
BR0308918A (pt) 2005-01-04
US20040082573A1 (en) 2004-04-29
AU2003230754A1 (en) 2003-10-13
ATE389640T1 (de) 2008-04-15
WO2003082832A2 (en) 2003-10-09
KR20040098029A (ko) 2004-11-18
IL163958A0 (en) 2005-12-18
US7119196B2 (en) 2006-10-10
ES2300576T3 (es) 2008-06-16
MXPA04009332A (es) 2005-12-12

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