WO2001025219A3 - Piperazine compounds - Google Patents

Piperazine compounds Download PDF

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Publication number
WO2001025219A3
WO2001025219A3 PCT/EP2000/009722 EP0009722W WO0125219A3 WO 2001025219 A3 WO2001025219 A3 WO 2001025219A3 EP 0009722 W EP0009722 W EP 0009722W WO 0125219 A3 WO0125219 A3 WO 0125219A3
Authority
WO
WIPO (PCT)
Prior art keywords
group
alkyl
represents hydrogen
integer
nitrogen
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2000/009722
Other languages
French (fr)
Other versions
WO2001025219A2 (en
Inventor
Giuseppe Alvaro
Fabio Romano Di
Riccardo Giovannini
Giuseppe Guercio
Yves St-Denis
Antonella Ursini
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glaxo Group Ltd
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to EP00969414A priority Critical patent/EP1218359B1/en
Priority to DK04076632T priority patent/DK1460066T3/en
Priority to DE60012031T priority patent/DE60012031T2/en
Priority to JP2001528165A priority patent/JP4776844B2/en
Priority to NZ518144A priority patent/NZ518144A/en
Priority to AT00969414T priority patent/ATE270664T1/en
Priority to DK00969414T priority patent/DK1218359T3/en
Priority to AU79139/00A priority patent/AU768780B2/en
Priority to BR0014541-6A priority patent/BR0014541A/en
Priority to HU0203136A priority patent/HUP0203136A3/en
Priority to US10/089,964 priority patent/US6951861B1/en
Priority to SI200030492T priority patent/SI1218359T1/en
Priority to MXPA02003515A priority patent/MXPA02003515A/en
Priority to CA2386515A priority patent/CA2386515C/en
Priority to PL356261A priority patent/PL201191B1/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Priority to DK04076650T priority patent/DK1454901T3/en
Priority to IL14896400A priority patent/IL148964A0/en
Priority to HK03104740.2A priority patent/HK1052506B/en
Publication of WO2001025219A2 publication Critical patent/WO2001025219A2/en
Publication of WO2001025219A3 publication Critical patent/WO2001025219A3/en
Priority to IL148964A priority patent/IL148964A/en
Priority to NO20021637A priority patent/NO323776B1/en
Anticipated expiration legal-status Critical
Priority to US10/637,825 priority patent/US7071196B2/en
Priority to AU2004201361A priority patent/AU2004201361B2/en
Priority to US10/958,744 priority patent/USRE39921E1/en
Priority to US11/334,267 priority patent/US7345041B2/en
Priority to US11/955,847 priority patent/US7625904B2/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • 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
    • A61K31/495—Heterocyclic 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

The present invention relates to piperazine derivatives of formula (I) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents hydrogen or a C1-4 alkyl group; R2 represents hydrogen, a C1-4 alkyl, C2-6 alkenyl or a C3-7 cycloalkyl group; or R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5-6 membered heterocyclic group; R3 represents a trifluoromethyl, a C1-4 alkyl, a C1-4 alkoxy, a trifluoromethoxy or a halogen group; R4 represents hydrogen, a (CH2)qR7 or a (CH2)rCO(CH2)pR7 group; R5 represents hydrogen, a C1-4 alkyl or a COR6 group; R6 represents hydrogen, hydroxy, amino, methylamino, dimethylamino a 5 membered heteroaryl group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen or a 6 membered heteroaryl group containing 1 to 3 nitrogen atoms; R7 represents hydrogen, hydroxy or NR8R9 wherein R8 and R9 represent independently hydrogen or C1-4 alkyl optionally substituted by hydroxy, or by amino; R10 represents hydrogen, a C1-4 alkyl I group or R10 together with R2 represents a C3-7 cycloalkyl group; m is zero or an integer from 1 to 3; n is zero or an integer from 1 to 3; both p and r are independently zero or an integer from 1 to 4; q is an integer from 1 to 4; provided that, when R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5 to 6 membered heterocyclic group, i) m is 1 or 2; ii) when m is 1, R is not fluorine and iii) when m is 2, the two substituents R are not both fluorine,and pharmaceutically acceptable salts and solvates thereof.
PCT/EP2000/009722 1999-10-07 2000-10-05 Piperazine compounds Ceased WO2001025219A2 (en)

Priority Applications (25)

Application Number Priority Date Filing Date Title
PL356261A PL201191B1 (en) 1999-10-07 2000-10-05 Piperazine compounds
DE60012031T DE60012031T2 (en) 1999-10-07 2000-10-05 PIPERAZIN COMPOUNDS AS TACHYKININE ANTAGONISTS
JP2001528165A JP4776844B2 (en) 1999-10-07 2000-10-05 Compound
NZ518144A NZ518144A (en) 1999-10-07 2000-10-05 Piperazine Compounds
AT00969414T ATE270664T1 (en) 1999-10-07 2000-10-05 PIPERAZINE COMPOUNDS AS TACHYKININ ANTAGONISTS
DK00969414T DK1218359T3 (en) 1999-10-07 2000-10-05 Piperazine compounds as tachykinin antagonists
AU79139/00A AU768780B2 (en) 1999-10-07 2000-10-05 Piperazine compounds
BR0014541-6A BR0014541A (en) 1999-10-07 2000-10-05 Chemical compounds
HU0203136A HUP0203136A3 (en) 1999-10-07 2000-10-05 Piperazine compounds, process for their preparation, pharmaceutical compositions containing them and their use
US10/089,964 US6951861B1 (en) 1999-10-07 2000-10-05 Chemical compounds
SI200030492T SI1218359T1 (en) 1999-10-07 2000-10-05 Piperazine compounds as tachykinins antagonists
MXPA02003515A MXPA02003515A (en) 1999-10-07 2000-10-05 Piperazine compounds.
CA2386515A CA2386515C (en) 1999-10-07 2000-10-05 Piperazine derivatives
EP00969414A EP1218359B1 (en) 1999-10-07 2000-10-05 Piperazine compounds as tachykinins antagonists
DK04076650T DK1454901T3 (en) 1999-10-07 2000-10-05 Pharmaceutical compositions comprising tachykinin antagonists and a serotonin reuptake inhibitor
DK04076632T DK1460066T3 (en) 1999-10-07 2000-10-05 Piperazine compound as tachykinin inhibitors
IL14896400A IL148964A0 (en) 1999-10-07 2000-10-05 Piperazine compounds
HK03104740.2A HK1052506B (en) 1999-10-07 2000-10-05 Compound
IL148964A IL148964A (en) 1999-10-07 2002-04-01 Piperazine compounds
NO20021637A NO323776B1 (en) 1999-10-07 2002-04-05 Piperazine derivatives, processes for the preparation of the same, pharmaceutical composition including the same and the use of the same for the preparation of the drug
US10/637,825 US7071196B2 (en) 1999-10-07 2003-08-08 Chemical compounds
AU2004201361A AU2004201361B2 (en) 1999-10-07 2004-03-31 Piperazine compounds
US10/958,744 USRE39921E1 (en) 1999-10-07 2004-10-05 Chemical compounds
US11/334,267 US7345041B2 (en) 1999-10-07 2006-01-18 Chemical compounds
US11/955,847 US7625904B2 (en) 1999-10-07 2007-12-13 Methods for the treatment of sleep disorders

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9923748.9A GB9923748D0 (en) 1999-10-07 1999-10-07 Chemical compounds
GB9923748.9 1999-10-07

Related Child Applications (4)

Application Number Title Priority Date Filing Date
US10/089,964 A-371-Of-International US6951861B1 (en) 1999-10-07 2000-10-05 Chemical compounds
US10089964 A-371-Of-International 2000-10-05
US10/190,170 Continuation US6642240B2 (en) 1999-10-07 2002-07-03 Treating emesis in a mammal
US10/838,838 Continuation US20040209893A1 (en) 1999-10-07 2004-05-04 Chemical compounds

Publications (2)

Publication Number Publication Date
WO2001025219A2 WO2001025219A2 (en) 2001-04-12
WO2001025219A3 true WO2001025219A3 (en) 2001-12-13

Family

ID=10862304

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/009722 Ceased WO2001025219A2 (en) 1999-10-07 2000-10-05 Piperazine compounds

Country Status (33)

Country Link
US (6) US6951861B1 (en)
EP (3) EP1218359B1 (en)
JP (1) JP4776844B2 (en)
KR (2) KR100817373B1 (en)
CN (1) CN100413850C (en)
AR (2) AR025975A1 (en)
AT (3) ATE270664T1 (en)
AU (1) AU768780B2 (en)
BR (1) BR0014541A (en)
CA (1) CA2386515C (en)
CO (1) CO5251467A1 (en)
CY (2) CY1110172T1 (en)
CZ (1) CZ302340B6 (en)
DE (3) DE60042501D1 (en)
DK (3) DK1454901T3 (en)
ES (3) ES2312917T3 (en)
GB (1) GB9923748D0 (en)
HK (1) HK1052506B (en)
HU (1) HUP0203136A3 (en)
IL (2) IL148964A0 (en)
MX (1) MXPA02003515A (en)
MY (1) MY130907A (en)
NO (1) NO323776B1 (en)
NZ (2) NZ531127A (en)
PE (1) PE20010741A1 (en)
PL (1) PL201191B1 (en)
PT (3) PT1460066E (en)
SI (3) SI1454901T1 (en)
TN (1) TNSN00194A1 (en)
TR (1) TR200200936T2 (en)
TW (1) TWI225485B (en)
WO (1) WO2001025219A2 (en)
ZA (1) ZA200202589B (en)

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