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1. WO1999002520 - DIAMINE DERIVATIVES AND PHARMACEUTICAL CONTAINING THE SAME

Publication Number WO/1999/002520
Publication Date 21.01.1999
International Application No. PCT/JP1998/003054
International Filing Date 07.07.1998
IPC
C07D 215/227 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
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
20Oxygen atoms
22attached in position 2 or 4
227only one oxygen atom which is attached in position 2
C07D 401/12 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
12linked by a chain containing hetero atoms as chain links
C07D 403/12 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
12linked by a chain containing hetero atoms as chain links
C07D 417/12 2006.1
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 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 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
A61P 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
A61P 37/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
08Antiallergic agents
Applicants
  • KOWA CO., LTD. [JP]/[JP] (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, JP, KR, LU, MC, NL, PT, SE)
  • TIMMERMAN, Henk [NL]/[NL] (UsOnly)
  • ZANG, Mingqiang [NL]/[GB] (UsOnly)
  • ONOGI, Kazuhiro [JP]/[JP] (UsOnly)
  • TAMURA, Masahiro [JP]/[JP] (UsOnly)
  • TOHMA, Tsutomu [JP]/[JP] (UsOnly)
  • WADA, Yasushi [JP]/[JP] (UsOnly)
Inventors
  • TIMMERMAN, Henk
  • ZANG, Mingqiang
  • ONOGI, Kazuhiro
  • TAMURA, Masahiro
  • TOHMA, Tsutomu
  • WADA, Yasushi
Agents
  • ARUGA, Mitsuyuki
Priority Data
9/18119607.07.1997JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) DIAMINE DERIVATIVES AND PHARMACEUTICAL CONTAINING THE SAME
(FR) DERIVES DE DIAMINE ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
Abstract
(EN) Diamine derivatives represented by general formula (1) or salts thereof wherein R1 represents H, OH, an aralkyloxy group, or a halogen atom; R2 represents H or a lower alkyl group; A represents -C(R3)=CH-, -CH=N-, -N(R4)- (wherein R3 represents H or OH and R4 represents a lower alkyl group or an alkoxyalkyl group), -O-, or -S-; B represents a single bond, -C(R5)(R6)-(CH2)k- (wherein R5 and R6 represent each H or a lower alkyl group and k is 0 to 2), -S(O)qCH(R7)-, or -CH=CH-; E represents a single bond or -(CH2)3-; W and Y represent each -CH2- or -CO-; Z represents O or S; m is 2 or 3; and n is 1 to 4, provided that when B represents a single bond, E represents -(CH2)3-, while when B represents a group other than a single bond, E represents a single bond. The diamine derivatives or salts thereof have both antileukotriene and antihistaminic activities and are reduced in intracranal migration, thus being useful as pharmaceuticals, such as prophylactic and therapeutic agents for asthma.
(FR) Dérivés de diamine de formule générale (1), ou sels desdits dérivés. Dans ladite formule, R1 est H, OH, un groupe aralkyloxy, ou un atome d'halogène; R2 est H ou un groupe alkyle inférieur; A est -C(R3)=CH-, -CH=N-, -N(R4)- (dans lesquelles R3 est H ou OH et R4 est un groupe alkyle inférieur ou un groupe acoxyalkyle), -O-, ou -S-; B est une liaison simple, -C(R5)(R6)-(CH2)k- (dans laquelle R5 et R6 sont chacun H ou un groupe alkyle inférieur et k est 0 à 2), -S(O)qCH(R7)-, ou -CH=CH-; E est une liaison simple ou -(CH2)3; W et Y sont chacun -CH2- ou -CO-; Z est O ou S; m est 2 ou 3; et n est 1 à 4, à condition que lorsque B est une liaison simple, E soit -(CH2)3-, tandis que lorsque B est un groupe autre qu'une liaison simple, E est une liaison simple. Lesdits dérivés d'amine ou sels desdits dérivés possèdent une activité antileucémique et antihistaminique et présentent une migration intracranienne réduite, ce qui les rend utiles comme substances pharmaceutiques, telles que des agents prophylactiques et thérapeutiques contre l'asthme.
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