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1. WO1999028300 - SUBSTITUTED IMIDAZOLE DERIVATIVES HAVING AGONIST-LIKE ACTIVITY AT ALPHA 2B OR 2B/2C ADRENERGIC RECEPTORS

Publication Number WO/1999/028300
Publication Date 10.06.1999
International Application No. PCT/US1998/025669
International Filing Date 03.12.1998
Chapter 2 Demand Filed 28.06.1999
IPC
C07D 233/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
04having one double bond between ring members or between a ring member and a non-ring member
06with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
C07D 233/54 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
C07D 233/84 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
66with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
84Sulfur atoms
C07D 263/28 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
08having one double bond between ring members or between a ring member and a non-ring member
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
28Nitrogen atoms not forming part of a nitro radical
C07D 401/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
CPC
A61P 1/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
12Antidiarrhoeals
A61P 11/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
A61P 13/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
02of urine or of the urinary tract, e.g. urine acidifiers
A61P 21/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
A61P 21/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21Drugs for disorders of the muscular or neuromuscular system
02Muscle relaxants, e.g. for tetanus or cramps
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
Applicants
  • ALLERGAN SALES, INC. [US]/[US]
Inventors
  • CHOW, Ken
  • GIL, Daniel, W.
  • BURKE, James, A.
  • HARCOURT, Dale, A.
  • GARST, Michael, E.
  • WHEELER, Larry, A.
  • MUNK, Stephen, A.
Agents
  • HOCH, James, M.
Priority Data
08/985,34704.12.1997US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) SUBSTITUTED IMIDAZOLE DERIVATIVES HAVING AGONIST-LIKE ACTIVITY AT ALPHA 2B OR 2B/2C ADRENERGIC RECEPTORS
(FR) DERIVES IMIDAZOLES SUBSTITUES AYANT UNE ACTIVITE DE TYPE AGONISTE VIS A VIS DES RECEPTEURS ADRENERGIQUES ALPHA 2B OU 2B/2C
Abstract
(EN) Coumpounds having adrenergic activity which are selective agonists for one or both of the $g(a)2B and $g(a)2C adrenoceptor receptor subtypes in preference to the $g(a)2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having formula (I) wherein the dotted lines represent optional bonds provided that two double bonds may not share a common carbon atom; R is H or lower alkyl; X is S or C(H)R1, wherein R1 is H or lower alkyl, but R1 is absent when the bond between X and the ring represented by formula (a) is a double bond; Y is O, N, S, (CR12)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y1CH2-, wherein Y1 is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R2, R3 or R4 is bound to a saturated carbon atom and x is 2 when R2, R3 or R4 is bound to a saturated carbon atom; R2 is H, lower alkyl, halogen, hydroxy or lower alkoxy, or, when attached to a saturated carbon atom, R2 may be oxo; R3 and R4 are, each, H, lower alkyl, hydroxy, lower alkoxy, or phenyl or, together, are -(C(R2)x)z-; -Y1(C(R2)x)z'-; -Y1(C(R2)x)yY1-; -(C(R2)x)-Y1-(C(R2)x)-; -(C(R2)x)-Y1-(C(R2)x)-(C(R2)x)- and -Y1-(C(R2)x)-Y1-(C(R2)x)- wherein z is an integer of from 3 to 5, z' is an integer of from 2 to 4 and x and y are as defined above, and further either end of each of these divalent moieties may attach at either R3 or R4 to form a condensed ring structure and the rings formed may be totally unsaturated, partially unsaturated, or totally saturated; and being useful for treating muscle spasticity including hyperactive micturition, diarrhea, diuresis, withdrawal syndromes, pain including neuropathic pain, neurodegenerative diseases, memory and cognition deficits, psychoses including manic disorders and anxiety, hypertension, cardiac ischemia, congestive heart failure, and nasal congestion without sedating or cardiovascular side effects.
(FR) L'invention se rapporte à des composés dotés d'une activité adrénergique qui s'avèrent être des agonistes sélectifs vis à vis de l'un des deux, ou des deux, sous-types de récepteurs adrénergiques $g(a)2B et $g(a)2C, plutôt que vis à vis du sous-type de récepteur adrénergique $g(a)2A. Le composé actif est sélectionné dans le groupe constitué par des composés représentés par la formule (I) dans laquelle les lignes pointillées représentent des liaisons facultatives qui doivent être telles que deux doubles liaisons ne partagent pas un même atome de carbone; R est H ou alkyle inférieur; X est S ou C(H)R1, où R1 est H ou alkyle inférieur, mais R1 est absent lorsque la liaison entre X et le noyau représenté par la formule (a) est une liaison double; Y est O, N, S, (CR12)y, où y est un entier compris entre 1 et 3, -CH=CH- ou -Y1CH2-, où Y1 est O, N ou S; x est un entier égal à 1 ou 2, x valant 1 lorsque R2, R3 ou R4 est lié à un atome de carbone insaturé et x valant 2 lorsque R2, R3 ou R4 est lié à un atome de carbone saturé; R2 est H, alkyle inférieur, halogène, hydroxy ou alcoxy inférieur ou, lorsqu'il est fixé à un atome de carbone saturé, R2 peut être oxo; R3 et R4 sont chacun H, alkyle inférieur, hydroxy, alcoxy inférieur ou phényle ou, pris conjointement sont -(C(R2)x)z-; -Y1(C(R2)x)z'-; -Y1(C(R2)x)yY1-; -(C(R2)x)-Y1-(C(R2)x)-; -(C(R2)x)-Y1-(C(R2)x)-(C(R2)x)- et -Y1-(C(R2)x)-Y1-(C(R2)x)-, où z est un entier compris entre 3 et 5, z' est un entier compris entre 2 et 4 et x et y sont tels que définis ci-dessus, et de plus, chacune des extrémités de ces fractions divalentes peuvent se fixer soit sur R3 soit sur R4 pour former une structure en anneau condensée et les anneaux formés peuvent être totalement insaturés, partiellement insaturés ou totalement saturés. Ces composés s'avèrent utiles pour traiter la spasticité et notamment les troubles de type miction hyperactive, diarrhée, diurèse, syndromes de sevrage, douleurs du type douleurs neuropathiques, maladies neurodégénératives, troubles cognitifs et de la mémoire, psychoses telles que troubles maniaques et anxiété, hypertension, ischémie cardiaque, insuffisance cardiaque globale et congestion nasale sans effets secondaires cardio-vasculaires ou sédatifs.
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