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1. WO1996006068 - BENZENE COMPOUND AND MEDICINAL USE THEREOF

Publication Number WO/1996/006068
Publication Date 29.02.1996
International Application No. PCT/JP1995/001654
International Filing Date 22.08.1995
Chapter 2 Demand Filed 19.02.1996
IPC
C07C 215/28 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
215Compounds containing amino and hydroxy groups bound to the same carbon skeleton
02having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
22the carbon skeleton being unsaturated
28and containing six-membered aromatic rings
C07C 215/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
215Compounds containing amino and hydroxy groups bound to the same carbon skeleton
02having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
22the carbon skeleton being unsaturated
28and containing six-membered aromatic rings
30containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
C07C 215/56 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
215Compounds containing amino and hydroxy groups bound to the same carbon skeleton
46having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
56with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups
C07C 217/64 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
54having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
64with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
C07C 217/72 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
54having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
64with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
66with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain
72linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 219/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
219Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
02having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
20the carbon skeleton being unsaturated
22and containing six-membered aromatic rings
CPC
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 37/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
06Immunosuppressants, e.g. drugs for graft rejection
C07C 215/28
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
215Compounds containing amino and hydroxy groups bound to the same carbon skeleton
02having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
22the carbon skeleton being unsaturated
28and containing six-membered aromatic rings
C07C 215/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
215Compounds containing amino and hydroxy groups bound to the same carbon skeleton
02having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
22the carbon skeleton being unsaturated
28and containing six-membered aromatic rings
30containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
C07C 215/56
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
215Compounds containing amino and hydroxy groups bound to the same carbon skeleton
46having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
56with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups
C07C 217/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
54having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
64with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
Applicants
  • YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. [JP]/[JP] (AllExceptUS)
  • FUJITA, Tetsuro [JP]/[JP] (UsOnly)
  • ADACHI, Kunitomo [JP]/[JP] (UsOnly)
  • KOHARA, Toshiyuki [JP]/[JP] (UsOnly)
  • KIUCHI, Masatoshi [JP]/[JP] (UsOnly)
  • CHIBA, Kenji [JP]/[JP] (UsOnly)
  • TESHIMA, Koji [JP]/[JP] (UsOnly)
  • MISHINA, Tadashi [JP]/[JP] (UsOnly)
Inventors
  • FUJITA, Tetsuro
  • ADACHI, Kunitomo
  • KOHARA, Toshiyuki
  • KIUCHI, Masatoshi
  • CHIBA, Kenji
  • TESHIMA, Koji
  • MISHINA, Tadashi
Agents
  • TAKASHIMA, Hajime
Priority Data
6/19688822.08.1994JP
7/17254307.07.1995JP
7/8293407.04.1995JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) BENZENE COMPOUND AND MEDICINAL USE THEREOF
(FR) COMPOSE BENZENIQUE ET SON UTILISATION MEDICALE
Abstract
(EN)
A benzene compound represented by general formula (I) (wherein each symbol is as defined in the specification), an optical isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma, and pollinosis. It is useful also as an antifungal agent and hair growth stimulant.
(FR)
L'invention concerne un composé benzénique représenté par la formule générale (I), dans laquelle chaque symbole correspond à la définition donnée dans la description, un isomère optique ou un sel de ce composé, une composition médicinale le contenant, et un immunosuppresseur le contenant comme principe actif. Ledit composé, isomère ou sel a un excellent effet immunosuppresseur et peut être utilisé comme inhibiteur de la réaction de rejet se produisant lors de la greffe d'un organe ou de moelle osseuse et comme agent destiné à prévenir ou à soigner le rhumatisme articulaire, l'eczéma atopique (dermatite), le symdrome de Behçet, l'uvéite, le lupus érythèmateux aigu dissémimé , le syndrome de Sjögren, la sclérose en plaque, la myasthénie grave, le diabète de type I, l'ophtalmopathie endocrinienne, la cirrhose biliaire primitive, la maladie de Crohn, la glomérulonéphrite, la sarcoïdose, le psoriasis, le pemphigus, l'anémie aplasique, le purpura thrombocytopénique essentiel, l'allergie, la périartérite noueuse, la sclérodermie généralisée, la connectivite mixte, le syndrome de la crosse aortique, la polymyosite, la dermatomyosite, la granulomatose de Wegener, la colite ulcéreuse, l'hépatite chronique active, l'anémie hémolytique autoimmunue, le syndrome d'Evans, l'asthme bronchique et la pollinose. Un tel composé, isomère ou sel peut également être utilisé comme agent antifongique et comme stimulant de la pousse des cheveux.
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