CN103703008B - 作为双重活性的H1反向激动剂/5-HT2A拮抗剂的(噻吩并[2,3-b][1,5]苯并氧氮杂䓬-4-基)哌嗪-1-基化合物 - Google Patents

作为双重活性的H1反向激动剂/5-HT2A拮抗剂的(噻吩并[2,3-b][1,5]苯并氧氮杂䓬-4-基)哌嗪-1-基化合物 Download PDF

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Publication number
CN103703008B
CN103703008B CN201280031201.7A CN201280031201A CN103703008B CN 103703008 B CN103703008 B CN 103703008B CN 201280031201 A CN201280031201 A CN 201280031201A CN 103703008 B CN103703008 B CN 103703008B
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sleep
insomnia
compounds
pharmaceutically acceptable
compound
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CN103703008A (zh
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A.J.勒加德
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Eli Lilly and Co
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Eli Lilly and Co
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN201280031201.7A 2011-07-08 2012-07-02 作为双重活性的H1反向激动剂/5-HT2A拮抗剂的(噻吩并[2,3-b][1,5]苯并氧氮杂䓬-4-基)哌嗪-1-基化合物 Active CN103703008B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161505685P 2011-07-08 2011-07-08
US61/505,685 2011-07-08
US61/505685 2011-07-08
PCT/US2012/045254 WO2013009517A1 (en) 2011-07-08 2012-07-02 (THIENO[2,3-b][1,5]BENZOXAZEPIN-4-YL)PIPERAZIN-1-YL COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS

Publications (2)

Publication Number Publication Date
CN103703008A CN103703008A (zh) 2014-04-02
CN103703008B true CN103703008B (zh) 2015-11-25

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CN201280031201.7A Active CN103703008B (zh) 2011-07-08 2012-07-02 作为双重活性的H1反向激动剂/5-HT2A拮抗剂的(噻吩并[2,3-b][1,5]苯并氧氮杂䓬-4-基)哌嗪-1-基化合物

Country Status (22)

Country Link
US (1) US9481688B2 (enExample)
EP (1) EP2729474B1 (enExample)
JP (1) JP6050813B2 (enExample)
KR (1) KR101582429B1 (enExample)
CN (1) CN103703008B (enExample)
AU (1) AU2012283035B2 (enExample)
BR (1) BR112014000379A2 (enExample)
CA (1) CA2840217C (enExample)
DK (1) DK2729474T3 (enExample)
EA (1) EA023460B1 (enExample)
ES (1) ES2665035T3 (enExample)
HR (1) HRP20180475T1 (enExample)
HU (1) HUE037649T2 (enExample)
IN (1) IN2014MN00144A (enExample)
LT (1) LT2729474T (enExample)
MX (1) MX341132B (enExample)
NO (1) NO2729474T3 (enExample)
PL (1) PL2729474T3 (enExample)
PT (1) PT2729474T (enExample)
RS (1) RS57207B1 (enExample)
SI (1) SI2729474T1 (enExample)
WO (1) WO2013009517A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT2943498T (lt) 2013-01-14 2017-11-27 Eli Lilly And Company (tieno[2,3-b][1,5]benzoksazepin-4-il)piperazin-1-ilo junginiai kaip dvigubo aktyvumo h1 inversiniai agonistai / 5-ht2a antagonistai
TW201625644A (zh) 2014-04-29 2016-07-16 美國禮來大藥廠 作為選擇性５－ＨＴＡ反向促效劑之（噻吩并［２，３－ｂ］［１，５］苯并氧氮呯－４－基）哌嗪－１－基化合物
WO2018166855A1 (en) 2017-03-16 2018-09-20 Basf Se Heterobicyclic substituted dihydroisoxazoles
CN108371660B (zh) * 2017-12-14 2020-03-10 五邑大学 一种四氢环戊二烯并吡咯化合物及其衍生物的用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996018629A1 (en) * 1994-12-12 1996-06-20 Allelix Biopharmaceuticals Inc. 5-ht2 receptor ligands
CN1777613A (zh) * 2003-04-22 2006-05-24 埃吉斯药物工厂 奥氮平盐酸盐新的多晶型
WO2007022068A1 (en) * 2005-08-11 2007-02-22 Hypnion, Inc. Olanzapine analogs and methods of use thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2386092A1 (en) * 1999-09-29 2001-04-05 Yao-Chang Xu Piperidine derivatives
AU2008225014B2 (en) * 2007-03-15 2014-12-11 Protocell Therapeutics, Inc. Dibenzo(b,f)(1,4)oxazapine compounds
MX377802B (es) * 2008-05-27 2025-03-11 Intra Cellular Therapies Inc Metodos y composiciones para trastornos del sueño y otros trastornos.
GB0910009D0 (en) * 2009-06-10 2009-07-22 Glaxo Group Ltd Novel compounds
AR084867A1 (es) * 2011-02-07 2013-07-10 Lilly Co Eli Compuestos de acido [(5h-pirrolo[2,1-c][1,4]benzodiazepin-11-il)piperazin-1-il]-2,2-dimetilpropanoico sustituido como antagonistas de 5-ht/agonistas inversos de actividad dual
KR101596607B1 (ko) * 2011-08-30 2016-02-22 일라이 릴리 앤드 캄파니 이중 활성 H1 역 효능제/5-HT2A 길항제로서의 (티에노[2,3-b][1,5]벤족사제핀-4-일)피페라진-1-일 화합물

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996018629A1 (en) * 1994-12-12 1996-06-20 Allelix Biopharmaceuticals Inc. 5-ht2 receptor ligands
CN1777613A (zh) * 2003-04-22 2006-05-24 埃吉斯药物工厂 奥氮平盐酸盐新的多晶型
WO2007022068A1 (en) * 2005-08-11 2007-02-22 Hypnion, Inc. Olanzapine analogs and methods of use thereof

Also Published As

Publication number Publication date
EA023460B1 (ru) 2016-06-30
KR20140029512A (ko) 2014-03-10
US20140121199A1 (en) 2014-05-01
PL2729474T3 (pl) 2018-08-31
DK2729474T3 (en) 2018-05-22
NO2729474T3 (enExample) 2018-08-11
JP6050813B2 (ja) 2016-12-21
KR101582429B1 (ko) 2016-01-04
PT2729474T (pt) 2018-06-05
RS57207B1 (sr) 2018-07-31
EP2729474B1 (en) 2018-03-14
CN103703008A (zh) 2014-04-02
HUE037649T2 (hu) 2018-09-28
IN2014MN00144A (enExample) 2015-06-19
ES2665035T3 (es) 2018-04-24
BR112014000379A2 (pt) 2017-01-10
EA201391706A1 (ru) 2014-04-30
MX341132B (es) 2016-08-09
AU2012283035A1 (en) 2014-01-16
SI2729474T1 (en) 2018-04-30
EP2729474A1 (en) 2014-05-14
CA2840217C (en) 2016-03-22
MX2014000337A (es) 2014-11-13
US9481688B2 (en) 2016-11-01
JP2014518280A (ja) 2014-07-28
LT2729474T (lt) 2018-05-10
AU2012283035B2 (en) 2015-07-30
WO2013009517A1 (en) 2013-01-17
HRP20180475T1 (hr) 2018-06-15
CA2840217A1 (en) 2013-01-17

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