AU2005229505B2 - 4- (sulfanyl-pyrimidin-4-ylmethyl) -morpholine derivatives and related compounds as GABA receptor ligands for the treatment of anxiety, depression and epilepsy - Google Patents

4- (sulfanyl-pyrimidin-4-ylmethyl) -morpholine derivatives and related compounds as GABA receptor ligands for the treatment of anxiety, depression and epilepsy Download PDF

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Publication number
AU2005229505B2
AU2005229505B2 AU2005229505A AU2005229505A AU2005229505B2 AU 2005229505 B2 AU2005229505 B2 AU 2005229505B2 AU 2005229505 A AU2005229505 A AU 2005229505A AU 2005229505 A AU2005229505 A AU 2005229505A AU 2005229505 B2 AU2005229505 B2 AU 2005229505B2
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formula
compounds
methyl
ylmethyl
compound
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AU2005229505A
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AU2005229505A1 (en
Inventor
Pari Malherbe
Raffaello Masciadri
Eric Prinssen
Will Spooren
Andrew William Thomas
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/38One sulfur atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • 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
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2005229505A 2004-03-02 2005-02-22 4- (sulfanyl-pyrimidin-4-ylmethyl) -morpholine derivatives and related compounds as GABA receptor ligands for the treatment of anxiety, depression and epilepsy Ceased AU2005229505B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP04100830 2004-03-02
EP04100830.1 2004-03-02
PCT/EP2005/001814 WO2005094828A1 (en) 2004-03-02 2005-02-22 4- (sulfanyl-pyrimidin-4-ylmethyl) -morpholine derivatives and related compounds as gaba receptor ligands for the treatment of anxiety, depression and epilepsy

Publications (2)

Publication Number Publication Date
AU2005229505A1 AU2005229505A1 (en) 2005-10-13
AU2005229505B2 true AU2005229505B2 (en) 2010-07-15

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AU2005229505A Ceased AU2005229505B2 (en) 2004-03-02 2005-02-22 4- (sulfanyl-pyrimidin-4-ylmethyl) -morpholine derivatives and related compounds as GABA receptor ligands for the treatment of anxiety, depression and epilepsy

Country Status (14)

Country Link
US (1) US7351700B2 (https=)
EP (1) EP1725239B1 (https=)
JP (1) JP4563447B2 (https=)
KR (1) KR100802863B1 (https=)
CN (1) CN1925859B (https=)
AT (1) ATE367163T1 (https=)
AU (1) AU2005229505B2 (https=)
BR (1) BRPI0508310A (https=)
CA (1) CA2557719A1 (https=)
DE (1) DE602005001696T2 (https=)
ES (1) ES2290885T3 (https=)
PL (1) PL1725239T3 (https=)
RU (1) RU2382033C2 (https=)
WO (1) WO2005094828A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2353619C2 (ru) 2007-06-28 2009-04-27 Общество С Ограниченной Ответственностью "Бионика" Новые соединения, обладающие функцией антикоагулянтов, фармацевтические композиции на их основе для лечения тромботических состояний и плазмозамещающий раствор для коррекции гиперкоагуляционных нарушений при гемодилюции
RU2354647C2 (ru) * 2007-06-28 2009-05-10 Общество С Ограниченной Ответственностью "Бионика" Новые соединения, обладающие функцией ингибиторов тромбина, и фармацевтические композиции на их основе
CA2692945A1 (en) * 2007-07-09 2009-01-15 Astrazeneca Ab Compounds - 945
TW201623257A (zh) 2014-05-09 2016-07-01 奧利安公司 藥理活性之喹唑啉二酮衍生物
KR102269132B1 (ko) 2014-06-10 2021-06-25 삼성디스플레이 주식회사 반방향족성 화합물 및 이를 포함하는 유기 발광 소자
US10084141B2 (en) 2014-06-13 2018-09-25 Samsung Display Co., Ltd. Antiaromatic compound and organic light-emitting device including the same
HU231058B1 (hu) 2017-03-13 2020-04-28 Richter Gedeon Nyrt. Gyógyászatilag hatékony aliciklusos-szubsztituált pirazolo[1,5-a]pirimidin származékok
TWI907472B (zh) 2020-08-05 2025-12-11 匈牙利商羅特格登公司 具藥理活性之經雜環取代的吡唑并〔1,5-a〕嘧啶衍生物
GB202414197D0 (en) 2024-09-27 2024-11-13 Addex Pharmaceuticals Sa Novel compounds
GB202414199D0 (en) 2024-09-27 2024-11-13 Addex Pharmaceuticals Sa Novel Compounds
GB202414200D0 (en) 2024-09-27 2024-11-13 Addex Pharmaceuticals Sa Novel compounds
GB202414193D0 (en) 2024-09-27 2024-11-13 Addex Pharmaceuticals Sa Novel compounds
GB202414192D0 (en) 2024-09-27 2024-11-13 Addex Pharmaceuticals Sa Novel compounds

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6313146B1 (en) 1991-08-23 2001-11-06 Nps Pharmaceuticals, Inc. Calcium receptor-active molecules
RU2153494C2 (ru) * 1993-10-12 2000-07-27 Дзе Дюпон Мерк Фармасьютикал Компани 1-n-алкил-n-арилпиримидинамины, способ лечения заболеваний, фармацевтическая композиция
WO2001056990A2 (en) 2000-02-03 2001-08-09 Eli Lilly And Company Pyridine derivates as potentiators of glutamate receptors
CA2444148A1 (en) * 2001-04-11 2002-10-24 Queen's University At Kingston Pyrimidine compounds as anti-ictogenic and/or anti-epileptogenic agents
GB0209481D0 (en) 2002-04-24 2002-06-05 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
KR100802863B1 (ko) 2008-02-12
WO2005094828A1 (en) 2005-10-13
KR20060116240A (ko) 2006-11-14
EP1725239B1 (en) 2007-07-18
RU2006134632A (ru) 2008-04-10
EP1725239A1 (en) 2006-11-29
DE602005001696D1 (de) 2007-08-30
US20050197337A1 (en) 2005-09-08
CN1925859B (zh) 2010-11-24
AU2005229505A1 (en) 2005-10-13
BRPI0508310A (pt) 2007-07-24
DE602005001696T2 (de) 2008-04-10
CA2557719A1 (en) 2005-10-13
JP4563447B2 (ja) 2010-10-13
PL1725239T3 (pl) 2007-12-31
ES2290885T3 (es) 2008-02-16
US7351700B2 (en) 2008-04-01
JP2007526266A (ja) 2007-09-13
CN1925859A (zh) 2007-03-07
RU2382033C2 (ru) 2010-02-20
ATE367163T1 (de) 2007-08-15

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