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1. WO1991000729 - BIS-DIOXOPIPERAZINES, AND THEIR USE AS PROTECTING AGENTS

Publication Number WO/1991/000729
Publication Date 24.01.1991
International Application No. PCT/GB1990/001079
International Filing Date 13.07.1990
IPC
A61K 31/495 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/535 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
C07D 241/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
241Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02not condensed with other rings
06having one or two double bonds between ring members or between ring members and non-ring members
08with oxygen atoms directly attached to ring carbon atoms
CPC
A61K 31/495
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
A61K 31/535
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
A61K 31/70
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
C07D 241/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
241Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02not condensed with other rings
06having one or two double bonds between ring members or between ring members and non-ring members
08with oxygen atoms directly attached to ring carbon atoms
Applicants
  • NATIONAL RESEARCH DEVELOPMENT CORPORATION [GB/GB]; 101 Newington Causeway London SE1 6BU, GB (AllExceptUS)
  • CREIGHTON, Andrew, Malcolm [GB/GB]; GB (UsOnly)
Inventors
  • CREIGHTON, Andrew, Malcolm; GB
Agents
  • STEPHENSON, Gerald, Frederick; Patent Department National Research Development Corporation 101 Newington Causeway London SE1 6BU, GB
Priority Data
8916072.513.07.1989GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BIS-DIOXOPIPERAZINES, AND THEIR USE AS PROTECTING AGENTS
(FR) BIS-DIOXOPIPERAZINES, ET LEUR UTILISATION EN TANT QU'AGENTS DE PROTECTION
Abstract
(EN)
Compounds of formula (II), wherein n is 0, 1 or 2, R1, R2, R3 and R4 are each separately selected from hydrogen, unsubstituted acyclic aliphatic hydrocarbon groups having a maximum of six carbon atoms and C1-6 alkyl groups substituted by a hydroxy group or a C1-6 alkoxy group, or one of R1 and R2 and one of R3 and R4 is hydrogen and the others are a trimethylene, tetramethylene or pentamethylene bridging group, and R5 is hydrogen or an unsubstituted acyclic aliphatic hydrocarbon group having a maximum of six carbon atoms, but with the provisos that (a) when n is 0 the combinations R1 = R2 = R3 = R4 = R5 = H and R1 = R2 = R3 = R5 = H, R4 = methyl are excluded, and (b) when n is 0, R1, R3 and R5 are each hydrogen, and each of R2 and R4 is other than hydrogen the compound is in other than the $i(meso) or $i(erythro) configuration, or a salt thereof formed with a physiologically acceptable inorganic or organic acid, are of use in therapy, particularly as cardioprotective agents.
(FR)
L'invention se rapporte à des composés représentés par la formule (II); où n est égal à 0, à 1 ou à 2; R1, R2, R3 et R4 sont chacun choisis séparément parmi l'hydrogène, des groupes d'hydrocarbures aliphatiques acycliques non substitués ayant un maximum de six atomes de carbone et des groupes alkyle de 1 à 6 atomes de carbone substitués par un groupe hydroxy ou un groupe alkoxy de 1 à 6 atomes de carbone, ou l'un des éléments R1 et R2 et l'un des éléments R3 et R4 représentent l'hydrogène et les autres représentent un groupe de liaison en pont triméthylène, tétraméthylène ou pentaméthylène; et R5 représente l'hydrogène ou un groupe d'hydrocarbure aliphatique acyclique non substitué ayant un maximum de six atomes de carbone; à condition, toutefois, que: (a) lorsque n est égal à 0, les combinaisons R1 = R2 = R3 = R4 = R5 = H et R1 = R2 = R3 = R5 = H, R4 = méthyle sont exclues, et (b) lorsque n est égal à 0, que R1, R3 et R5 représentent chacun l'hydrogène et chacun des éléments R2 R4 est autre que l'hydrogène, le composé présente une configuration autre que la configuration $i(méso) ou $i(érythro); ou à un sel d'un tel composé formé avec un acide inorganique ou organique physiologiquement acceptable, ledit composé ou son sel ayant une utilité thérapeutique, notamment comme agents cardioprotecteurs.
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