ATE383337T1 - 1-(1h-indol-1-yl)-3-(4-methylpiperazin-1-yl)-1- phenylpropan-2-olderivate und verwandte verbindungen als modulatoren der norepinephrin- (ne-) und der serotonin-(5-ht-) aktivität und der monoaminwiederaufnahme zur behandlung von vasomotorischen symptomen (vms) - Google Patents

1-(1h-indol-1-yl)-3-(4-methylpiperazin-1-yl)-1- phenylpropan-2-olderivate und verwandte verbindungen als modulatoren der norepinephrin- (ne-) und der serotonin-(5-ht-) aktivität und der monoaminwiederaufnahme zur behandlung von vasomotorischen symptomen (vms)

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Publication number
ATE383337T1
ATE383337T1 AT05730271T AT05730271T ATE383337T1 AT E383337 T1 ATE383337 T1 AT E383337T1 AT 05730271 T AT05730271 T AT 05730271T AT 05730271 T AT05730271 T AT 05730271T AT E383337 T1 ATE383337 T1 AT E383337T1
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AT
Austria
Prior art keywords
resubstitution
phenylpropane
vms
norepinephrine
methylpiperazine
Prior art date
Application number
AT05730271T
Other languages
English (en)
Inventor
Callain Kim
Paige Mahaney
Eugene Trybulski
Puwen Zhang
Eugene Terefenko
Casey Mccomas
Michael Marella
Richard Coghlan
Gavin Heffernan
Stephen Cohn
An Vu
Joseph Sabatucci
Fei Ye
Original Assignee
Wyeth Corp
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Publication date
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Publication of ATE383337T1 publication Critical patent/ATE383337T1/de

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/22Anxiolytics
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/42Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • C07D471/02Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AT05730271T 2004-03-30 2005-03-29 1-(1h-indol-1-yl)-3-(4-methylpiperazin-1-yl)-1- phenylpropan-2-olderivate und verwandte verbindungen als modulatoren der norepinephrin- (ne-) und der serotonin-(5-ht-) aktivität und der monoaminwiederaufnahme zur behandlung von vasomotorischen symptomen (vms) ATE383337T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55765104P 2004-03-30 2004-03-30
US56986304P 2004-05-11 2004-05-11
US11/091,885 US7517899B2 (en) 2004-03-30 2005-03-28 Phenylaminopropanol derivatives and methods of their use

Publications (1)

Publication Number Publication Date
ATE383337T1 true ATE383337T1 (de) 2008-01-15

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AT05730271T ATE383337T1 (de) 2004-03-30 2005-03-29 1-(1h-indol-1-yl)-3-(4-methylpiperazin-1-yl)-1- phenylpropan-2-olderivate und verwandte verbindungen als modulatoren der norepinephrin- (ne-) und der serotonin-(5-ht-) aktivität und der monoaminwiederaufnahme zur behandlung von vasomotorischen symptomen (vms)

Country Status (20)

Country Link
US (3) US7517899B2 (de)
EP (1) EP1732887B1 (de)
JP (1) JP2007531751A (de)
KR (1) KR20060134186A (de)
AR (1) AR048675A1 (de)
AT (1) ATE383337T1 (de)
AU (1) AU2005230900A1 (de)
BR (1) BRPI0509390A (de)
CA (1) CA2560967A1 (de)
CR (1) CR8639A (de)
DE (1) DE602005004268T2 (de)
DK (1) DK1732887T3 (de)
EC (1) ECSP066899A (de)
ES (1) ES2299025T3 (de)
IL (1) IL178185A0 (de)
NO (1) NO20064892L (de)
PE (1) PE20060288A1 (de)
PL (1) PL1732887T3 (de)
TW (1) TW200536532A (de)
WO (1) WO2005097744A1 (de)

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US7365076B2 (en) * 2003-10-14 2008-04-29 Wyeth Substituted aryl cycloalkanol derivatives and methods of their use
US7491723B2 (en) * 2003-10-14 2009-02-17 Wyeth Alkanol and cycloalkanol-amine derivatives and methods of their use
US7550485B2 (en) * 2003-10-14 2009-06-23 Wyeth Substituted N-heterocycle derivatives and methods of their use
US7531543B2 (en) * 2003-10-14 2009-05-12 Wyeth Phenylpiperazine cycloalkanol derivatives and methods of their use
US20050165082A1 (en) * 2003-12-16 2005-07-28 Wyeth Methods of treating vasomotor symptoms
US7414052B2 (en) * 2004-03-30 2008-08-19 Wyeth Phenylaminopropanol derivatives and methods of their use

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IL178185A0 (en) 2006-12-31
PE20060288A1 (es) 2006-05-23
ES2299025T3 (es) 2008-05-16
US20090093469A1 (en) 2009-04-09
EP1732887A1 (de) 2006-12-20
JP2007531751A (ja) 2007-11-08
PL1732887T3 (pl) 2008-05-30
AR048675A1 (es) 2006-05-17
DK1732887T3 (da) 2008-04-28
NO20064892L (no) 2006-12-13
AU2005230900A1 (en) 2005-10-20
BRPI0509390A (pt) 2007-09-18
ECSP066899A (es) 2006-11-24
CA2560967A1 (en) 2005-10-20
US20050222148A1 (en) 2005-10-06
TW200536532A (en) 2005-11-16
EP1732887B1 (de) 2008-01-09
DE602005004268T2 (de) 2009-01-02
CR8639A (es) 2007-06-08
WO2005097744A1 (en) 2005-10-20
KR20060134186A (ko) 2006-12-27
US20090099164A1 (en) 2009-04-16
US7517899B2 (en) 2009-04-14
DE602005004268D1 (de) 2008-02-21

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