AU2012283035B2 - (thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists - Google Patents

(thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists Download PDF

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Publication number
AU2012283035B2
AU2012283035B2 AU2012283035A AU2012283035A AU2012283035B2 AU 2012283035 B2 AU2012283035 B2 AU 2012283035B2 AU 2012283035 A AU2012283035 A AU 2012283035A AU 2012283035 A AU2012283035 A AU 2012283035A AU 2012283035 B2 AU2012283035 B2 AU 2012283035B2
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AU
Australia
Prior art keywords
sleep
insomnia
pharmaceutically acceptable
compound
acceptable salt
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Ceased
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AU2012283035A
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English (en)
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AU2012283035A1 (en
Inventor
Andrew James Ledgard
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Eli Lilly and Co
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Eli Lilly and Co
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Publication of AU2012283035B2 publication Critical patent/AU2012283035B2/en
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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)
AU2012283035A 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 Ceased AU2012283035B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161505685P 2011-07-08 2011-07-08
US61/505,685 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
AU2012283035A1 AU2012283035A1 (en) 2014-01-16
AU2012283035B2 true AU2012283035B2 (en) 2015-07-30

Family

ID=46513872

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012283035A Ceased AU2012283035B2 (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

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
ES2647523T3 (es) * 2013-01-14 2017-12-22 Eli Lilly And Company Compuestos de (tieno[2,3-b][1,5]benzoxazepin-4-il)piperazin-1-ilo de doble actividad como agonistas inversos de H1/antagonistas de 5-HT2A
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007022068A1 (en) * 2005-08-11 2007-02-22 Hypnion, Inc. Olanzapine analogs and methods of use thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5602124A (en) * 1994-12-12 1997-02-11 Allelix Biopharmaceuticals, Inc. 5-HT2 receptor ligands
CN1149212C (zh) * 1999-09-29 2004-05-12 伊莱利利公司 用作再摄入抑制剂的哌啶衍生物
HU226410B1 (en) * 2003-04-22 2008-11-28 Egis Gyogyszergyar Nyilvanosan Novel polymorphous forms of olanzapine hydrochlorides, process for producing them, use thereof and pharmaceutical compositions containing them
BRPI0808828A8 (pt) * 2007-03-15 2017-11-28 Aryx Therapeutics Inc Compostos de dibenzo[b,f][1,4]oxazapina
WO2009145900A1 (en) * 2008-05-27 2009-12-03 Intra-Cellular Therapies, Inc. Methods and compositions for sleep disorders and other disorders
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
CN103958523B (zh) * 2011-08-30 2016-07-27 伊莱利利公司 作为双重活性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*-4-基)哌嗪-1-基化合物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007022068A1 (en) * 2005-08-11 2007-02-22 Hypnion, Inc. Olanzapine analogs and methods of use thereof

Also Published As

Publication number Publication date
CN103703008A (zh) 2014-04-02
EP2729474B1 (en) 2018-03-14
MX2014000337A (es) 2014-11-13
PL2729474T3 (pl) 2018-08-31
LT2729474T (lt) 2018-05-10
EA023460B1 (ru) 2016-06-30
RS57207B1 (sr) 2018-07-31
US9481688B2 (en) 2016-11-01
EA201391706A1 (ru) 2014-04-30
EP2729474A1 (en) 2014-05-14
HRP20180475T1 (hr) 2018-06-15
ES2665035T3 (es) 2018-04-24
KR101582429B1 (ko) 2016-01-04
WO2013009517A1 (en) 2013-01-17
US20140121199A1 (en) 2014-05-01
NO2729474T3 (enExample) 2018-08-11
JP6050813B2 (ja) 2016-12-21
CN103703008B (zh) 2015-11-25
IN2014MN00144A (enExample) 2015-06-19
CA2840217C (en) 2016-03-22
DK2729474T3 (en) 2018-05-22
PT2729474T (pt) 2018-06-05
KR20140029512A (ko) 2014-03-10
SI2729474T1 (en) 2018-04-30
MX341132B (es) 2016-08-09
BR112014000379A2 (pt) 2017-01-10
CA2840217A1 (en) 2013-01-17
HUE037649T2 (hu) 2018-09-28
AU2012283035A1 (en) 2014-01-16
JP2014518280A (ja) 2014-07-28

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired