HUP0203136A2 - Piperazinszármazékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Piperazinszármazékok, eljárás az előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP0203136A2
HUP0203136A2 HU0203136A HUP0203136A HUP0203136A2 HU P0203136 A2 HUP0203136 A2 HU P0203136A2 HU 0203136 A HU0203136 A HU 0203136A HU P0203136 A HUP0203136 A HU P0203136A HU P0203136 A2 HUP0203136 A2 HU P0203136A2
Authority
HU
Hungary
Prior art keywords
atom
alkyl
group
hydrogen
compounds
Prior art date
Application number
HU0203136A
Other languages
English (en)
Inventor
Giuseppe Alvaro
Romano Di Fabio
Riccardo Giovannini
Giuseppe Guercio
Yves St-Denis
Antonella Ursini
Original Assignee
Glaxo Group Limited
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
Application filed by Glaxo Group Limited filed Critical Glaxo Group Limited
Publication of HUP0203136A2 publication Critical patent/HUP0203136A2/hu
Publication of HUP0203136A3 publication Critical patent/HUP0203136A3/hu

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    • 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
    • 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
    • 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
    • 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
    • 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

Abstract

A találmány (I) általános képletű piperazinszármazékokra - amelynekképletében R halogénatom vagy alkilcsoport; R1 hidrogénatom vagyalkilcsoport; R2 hidrogénatom, alkil-, alkenil- vagycikloalkilcsoport; vagy R1 és R2 a nitrogén- és szénatommal együtt egyöt- vagy hattagú heterociklusos csoportot képez; R3 trifluor-metil-,alkil-, alkoxi-, trifluor-metoxi-csoport vagy halogénatom; R4hidrogénatom, -(CH2)qR7 vagy -(CH2)rCO(CH2)pR7 csoport; R5hidrogénatom, alkil- vagy -COR6 csoport; R10 hidrogénatom,alkilcsoport; vagy R10 és R2 együtt cikloalkilcsoportot képez; mértéke 0, 1, 2 vagy 3; n értéke 0, 1, 2 vagy 3; azzal a megkötéssel,hogy ha R1 és R2 azzal a nitrogénatommal és szénatommal együtt,amelyhez kapcsolódik, egy öt- vagy hattagú heterociklusos csoportotképez, i) m értéke 1 vagy 2; ii) ha m értéke 1, akkor R jelentésefluoratomtól eltérő, és iii) ha m értéke 2, akkor a két Rszubsztituens legalább egyikének a jelentése fluoratomtól eltérő, valamint gyógyászatilag elfogadható sóikra és szolvátjaikravonatkozik. A találmány kiterjed a találmány szerinti vegyületekelőállítási eljárásaira, a vegyületeket tartalmazógyógyszerkészítményekre és a vegyületek gyógyászati készítményekelőállítására vonatkozó felhasználására is. A találmány szerintivegyületek a tachykininek, köztük a P anyag (substance P) és másneurokininek antagonistái. Ó
HU0203136A 1999-10-07 2000-10-05 Piperazine compounds, process for their preparation, pharmaceutical compositions containing them and their use HUP0203136A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9923748.9A GB9923748D0 (en) 1999-10-07 1999-10-07 Chemical compounds
PCT/EP2000/009722 WO2001025219A2 (en) 1999-10-07 2000-10-05 Piperazine compounds

Publications (2)

Publication Number Publication Date
HUP0203136A2 true HUP0203136A2 (hu) 2003-02-28
HUP0203136A3 HUP0203136A3 (en) 2003-03-28

Family

ID=10862304

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0203136A HUP0203136A3 (en) 1999-10-07 2000-10-05 Piperazine compounds, process for their preparation, pharmaceutical compositions containing them and their use

Country Status (33)

Country Link
US (6) US6951861B1 (hu)
EP (3) EP1454901B1 (hu)
JP (1) JP4776844B2 (hu)
KR (2) KR100857671B1 (hu)
CN (1) CN100413850C (hu)
AR (2) AR025975A1 (hu)
AT (3) ATE407125T1 (hu)
AU (1) AU768780B2 (hu)
BR (1) BR0014541A (hu)
CA (1) CA2386515C (hu)
CO (1) CO5251467A1 (hu)
CY (2) CY1110172T1 (hu)
CZ (1) CZ302340B6 (hu)
DE (3) DE60042501D1 (hu)
DK (3) DK1454901T3 (hu)
ES (3) ES2329130T3 (hu)
GB (1) GB9923748D0 (hu)
HK (3) HK1052506B (hu)
HU (1) HUP0203136A3 (hu)
IL (2) IL148964A0 (hu)
MX (1) MXPA02003515A (hu)
MY (1) MY130907A (hu)
NO (1) NO323776B1 (hu)
NZ (2) NZ518144A (hu)
PE (1) PE20010741A1 (hu)
PL (1) PL201191B1 (hu)
PT (3) PT1454901E (hu)
SI (3) SI1460066T1 (hu)
TN (1) TNSN00194A1 (hu)
TR (1) TR200200936T2 (hu)
TW (1) TWI225485B (hu)
WO (1) WO2001025219A2 (hu)
ZA (1) ZA200202589B (hu)

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