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1. WO2000043387 - NEW BENZIMIDAZOLE COMPOUNDS FOR USE AS ACTIVE THERAPEUTIC SUBSTANCES, PROCESS FOR THE PREPARATION OF THESE COMPOUDNS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM

Publication Number WO/2000/043387
Publication Date 27.07.2000
International Application No. PCT/SE2000/000144
International Filing Date 24.01.2000
Chapter 2 Demand Filed 08.06.2000
IPC
C07D 403/12 2006.01
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
12linked by a chain containing hetero atoms as chain links
C07D 417/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
A61P 15/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
08for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61P 15/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
14for lactation disorders, e.g. galactorrhoea
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
A61P 19/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
A61P 21/04
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
04for myasthenia gravis
C07D 403/12
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 C07D401/00
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • PHARMACIA AB [SE/SE]; S-112 87 Stockholm, SE (AllExceptUS)
  • HEDGECOCK, Charles [GB/SE]; SE (UsOnly)
  • DESARBRE, Eric [FR/SE]; SE (UsOnly)
  • KURZ, Guido [DE/SE]; SE (UsOnly)
  • NORIN, Martin [SE/SE]; SE (UsOnly)
  • LUTHMAN, Marguerite [SE/SE]; SE (UsOnly)
  • WIDERSTÅHL, Cathrin [SE/SE]; SE (UsOnly)
Inventors
  • HEDGECOCK, Charles; SE
  • DESARBRE, Eric; SE
  • KURZ, Guido; SE
  • NORIN, Martin; SE
  • LUTHMAN, Marguerite; SE
  • WIDERSTÅHL, Cathrin; SE
Agents
  • TANNERFELDT, Agneta; Pharmacia AB S-112 87 Stockholm, SE
Priority Data
9900211-525.01.1999SE
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NEW BENZIMIDAZOLE COMPOUNDS FOR USE AS ACTIVE THERAPEUTIC SUBSTANCES, PROCESS FOR THE PREPARATION OF THESE COMPOUDNS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
(FR) NOUVEAUX COMPOSES DE BENZIMIDAZOLE POUVANT ETRE UTILISES COMME PRINCIPES ACTIFS THERAPEUTIQUES, PROCEDE PERMETTANT DE LES PREPARER ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
Abstract
(EN)
The present invention relates to new benzimidazole compounds with general structure (I): in which Y-X is $m(g)C = X when X is NR8, O, or S and R2 is H, alkyl, substituted alkylaryl or substituted aryl; or Y-X is $m(g)C-X when X is H, alkyl, substituted alkyl, aryl, substituted aryl, OR9 or NHR9 and R2 is a bond to Y; Z = O, S or NR12; R1 is H, alkyl, substituted alkyl, aryl or substituted aryl; R3 is H, alkyl, substituted alkyl, aryl or substituted aryl, OR9 or NHR9; R4, R5, R6, R7 are H, halogen, OR10, NR10, R11, NO2, CF3, CN, COR8, COOR8, CONHR8 and/or N3 in any combination and/or two adjacent R4, R5, R6 or R7 form a carbocyclic or heterocyclic ring; R8, R9, R10, R11, R12 and R13 are H, alkyl, substituted alkylaryl, aryl and/or substituted aryl in any combination. These compounds are useful as a human Growth Hormone (hGH) mimetic, which trigger GH agonist effects in animals and especially as an orally availabel human Growth Hormone (hGH).
(FR)
L'invention concerne de nouveaux composés de benzimidazole de structure générale (I), dans laquelle Y-X est > C=X quand X est NR8, O ou S et R2 est H, alkyle, alkylaryle substitué ou aryle substitué; ou bien Y-X est > C-X quand X est H, alkyle, alkyle substitué, aryle, aryle substitué, OR9 ou NHR9 et R2 est une liaison avec Y; Z = O, S ou NR12; R1 est H, alkyle, alkyle substitué, aryle or aryle substitué; R3 est H, alkyle, alkyle substitué, aryle ou aryle substitué, OR9 ou NHR9; R4, R5, R6, R7 sont H, halogène, OR10, NR10, R11, NO2, CF3, CN, COR8, COOR8, CONHR8 et/ou N3 dans n'importe quelle combinaison et/ou deux R4, R5, R6 ou R7 adjacents forment un noyau carbocyclique or hétérocyclique; et R8, R9, R10, R11, R12 et R13 sont H, alkyle, alkylaryle substitué, aryle et/ou aryle substitué dans n'importe quelle combinaison. Ces composés, utiles comme mimétiques de l'hormone de croissance humaine (hGH), déclenchent des effets agonistes de GH chez l'animal. Ils peuvent donc notamment être utilisés chez l'homme comme hormone de croissance à administration orale (hGH).
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