ES2157366T3 - Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos. - Google Patents

Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos.

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Publication number
ES2157366T3
ES2157366T3 ES96108493T ES96108493T ES2157366T3 ES 2157366 T3 ES2157366 T3 ES 2157366T3 ES 96108493 T ES96108493 T ES 96108493T ES 96108493 T ES96108493 T ES 96108493T ES 2157366 T3 ES2157366 T3 ES 2157366T3
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Prior art keywords
sub
rent
arilo
sup
heteroarilo
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Expired - Lifetime
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ES96108493T
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English (en)
Inventor
Gary W Bantle
Todd R Elworthy
Angel Guzman
Saul Jaime-Figueroa
Francisco J Lopez-Tapia
David J Morgans Jr
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members with 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
    • C07D253/075—Two hetero atoms, in positions 3 and 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 containing two hetero rings
    • C07D401/06—Heterocyclic 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 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A NUEVOS AGONISTAS AL SUB,3}-ADRENOCEPTORES DE LA FORMULA (I) EN LA CUAL: R{SUP,1} ES ACETILAMINO, AMINO, CIANO, TRIFLUOACETILAMINO, HALO, HIDRO, HIDROXI, NITRO, METILSULFONILAMINO, 2-PROPINILOXI, UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,1-6}), CICLOALQUILO(C{SUB,36}), ALQUIL(C{SUB,1-4})CICLOALQUILO(C{SUB,3-6}, ALQUILOXI(C{SUB,1-6}), CICLOALQUILOXI(C{SUB,3-6}, ALQUILOXI(C{SUB,1-4})CICLOALQUILO(C{SUB,3-6}) Y ALQUILTIO(C{SUB,1-4}) (CUYO GRUPO ESTA ADEMAS OPCIONALMENTE SUBSTITUIDO CON DE 1 A 3 ATOMOS DE HALO) O UN GRUPO SELECCIONADO DE ARILO, ALQUIL(C{SUB,1-4})ARILO, HETEROARILO, ALQUIL(C{SUB,14})HETEROARILO, ARILOXI, ALQUILOXI(C{SUB,1-4})ARILO, HETEROARILOXI Y ALQUILOXI(C{SUB,1-4})HETEROARILO (CUYO ARILO Y HETEROARILO ESTAN ADEMAS OPCIONALMENTE SUBSTITUIDOS CON DE 1 A 2 RADICALES INDEPENDIENTEMENTE SELECCIONADOS DE HALO Y CIANO); R{SUP,2} ES CIANO, HALO, HIDRO, HIDROXI O UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,1-6}) Y ALQUILOXI(C{SUB,1-6}) (CUYO GRUPO ESTA ADEMASOPCIONALMENTE SUBSTITUIDO CON DE 1 A 3 ATOMOS DE HALOGENO); R{SUP,3} Y R{SUP,4} SON AMBOS HIDRO O METILO O JUNTOS SON ETILENO; Y R{SUP,5} ES UN GRUPO SELECCIONADO DE LAS FORMULAS (A), (B), (C) Y (D): EN QUE: X ES C(O), CH{SUB,2} O CH(OH); Y ES CH{SUB,2} O CH(OH); Z ES N O C(R{SUP,9}), EN DONDE R{SUP,9} ES HIDRO, ALQUILO(C{SUB,1-6}) O HIDROXI; R{SUP,6} ES HIDRO, UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,1-6}), CICLOALQUILO(C{SUB,3-6}), ALQUIL(C{SUB,1-4})CICLOALQUILO(C{SUB,36}) (CUYO GRUPO ESTA OPCIONALMENTE SUBSTITUIDO CON DE 1 A 3 ATOMOS DE HALO) O UN GRUPO SELECCIONADO DE ARILO, HETEROARILO, ALQUIL(C{SUB,1-4})ARILO Y ALQUIL(C{SUB,1-4}HETEROARILO (CUYO ARILO Y HETEROARILO ESTAN ADEMAS OPCIONALMENTE SUBSTITUIDOS CON DE UNO A TRES RADICALES SELECCIONADOS DE HALO, CIANO, ALQUILOXI(C{SUB,1-6}), ALQUILO(C{SUB,1-6}) Y ARILO); R{SUP,7} ES ALCANOILO(C{SUB,1-6}), CARBAMOILO, CIANO, DIALQUILAMINO(C{SUB,1-6}), HALO, HIDRO, HIDROXI, HIDROXIIMINOMETILO, ALQUIL(C{SUB,1-6})-SULFONILO, ALQUILTIO(C{SUB,1-6}),UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,16}), CICLOALQUILO(C{SUB,3-6}), ALQUILOXI(C{SUB,1-6}) Y ALQUIL(C{SUB,1-4})ALQUILOXI(C{SUB,1-6}) (CUYO GRUPO ESTA OPCIONALMENTE SUBSTITUIDO CON DE UNO A TRES RADICALES SELECCIONADOS DE HALO, HIDROXI O ALQUILOXI(C{SUB,1-6})) O UN GRUPO SELECCIONADO DE ARILO, HETEROARILO, ALQUIL(C{SUB,1-4})ARILO Y ALQUIL(C{SUB,1-4})HETEROARILO (CUYO ARILO Y HETEROARILO ESTAN ADEMAS OPCIONALMENTE SUBSTITUIDOS CON DE UNO A TRES RADICALES SELECCIONADOS DE HALO, CIANO, ALQUILOXI(C{SUB,1-6}), ALQUILO(C{SUB,1-6}) Y ARILO) O R{SUP,7} Y R{SUP,9} JUNTOS SON TETRAMETILENO, Y CADA R{SUP,8} ES INDEPENDIENTEMENTE HIDRO, HIDROXI, METILO O ETILO; Y LAS SALES FARMACEUTICAMENTE ACEPTABLES Y N-OXIDOS DE LOS MISMOS.
ES96108493T 1995-06-09 1996-05-28 Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos. Expired - Lifetime ES2157366T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US48918395A 1995-06-09 1995-06-09

Publications (1)

Publication Number Publication Date
ES2157366T3 true ES2157366T3 (es) 2001-08-16

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ES96108493T Expired - Lifetime ES2157366T3 (es) 1995-06-09 1996-05-28 Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos.

Country Status (31)

Country Link
EP (1) EP0748800B1 (es)
JP (1) JP2721147B2 (es)
KR (1) KR100446877B1 (es)
CN (1) CN1118459C (es)
AR (1) AR003428A1 (es)
AT (1) ATE201016T1 (es)
AU (1) AU710754B2 (es)
BR (1) BR9602705A (es)
CA (1) CA2178548A1 (es)
CO (1) CO4700472A1 (es)
CZ (1) CZ290004B6 (es)
DE (1) DE69612698T2 (es)
DK (1) DK0748800T3 (es)
ES (1) ES2157366T3 (es)
GR (1) GR3036307T3 (es)
HU (1) HU223594B1 (es)
IL (1) IL118519A (es)
MA (1) MA23899A1 (es)
MY (1) MY113499A (es)
NO (1) NO309424B1 (es)
NZ (1) NZ286720A (es)
PE (1) PE46497A1 (es)
PL (1) PL188061B1 (es)
PT (1) PT748800E (es)
RU (1) RU2175322C2 (es)
SA (1) SA96170263B1 (es)
SG (1) SG45486A1 (es)
TR (1) TR970073A2 (es)
TW (1) TW340846B (es)
UY (1) UY24257A1 (es)
ZA (1) ZA964561B (es)

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CN1118459C (zh) 2003-08-20
JP2721147B2 (ja) 1998-03-04
GR3036307T3 (en) 2001-10-31
EP0748800A3 (en) 1996-12-27
EP0748800B1 (en) 2001-05-09
PE46497A1 (es) 1997-12-04
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RU2175322C2 (ru) 2001-10-27
IL118519A (en) 1999-12-22
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ATE201016T1 (de) 2001-05-15
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MA23899A1 (fr) 1996-12-31
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