FI111841B - Kondenserade pyridazinföreningar och användning av desamma vid framställning av medikament - Google Patents

Kondenserade pyridazinföreningar och användning av desamma vid framställning av medikament Download PDF

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FI111841B
FI111841B FI961510A FI961510A FI111841B FI 111841 B FI111841 B FI 111841B FI 961510 A FI961510 A FI 961510A FI 961510 A FI961510 A FI 961510A FI 111841 B FI111841 B FI 111841B
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group
prepared
chloro
amino
nmr
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FI961510A
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FI961510A0 (sv
FI961510A (sv
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Hideyuki Adachi
Kazutoshi Miyake
Yasuhiro Kabasawa
Fumihiro Ozaki
Keiji Ishibashi
Shigeru Souda
Masayuki Matsukura
Hiroki Ishihara
Nobuhisa Watanabe
Yasutaka Takase
Kazuki Miyazaki
Kohtaro Kodama
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Eisai Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
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    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (9)

1. Kondenserad pyridazinförening som representeras av den allmänna formeln (I) eller ett farmakologiskt lämpligt sait 5 därav: _ T T ]-r13 i i R väri n är ett heltal 0-4, 10 R1 betecknar en halogenatom, en nitrogrupp, en aminogrupp, en syanogrupp, eller en 4-hydroxipiperidin-l-ylgrupp, R12, R1J och R14 betecknar envar oberoende av varandra väte, 15 halogen, möjligen substituerad lägre alkyl eller möjligen substituerad lägre alkoxi, eller alternativt kan tvä av grupperna R12, R13 och R14, som är bundna tili närliggande kolatomer vara förenade tili bildande av metylendioxi eller etylendioxi), 20 --- betecknar en enkelbindning eller en dubbelbindning, och (1) när ovan nämnda bindning är en dubbelbindning, sä betecknar X en kväveatom och Y betecknar en grupp =C-B, väri B betecknar v ' en halogenatom, en grupp med formeln NRVR8, väri R7 betecknar väte eller lägre alkyl och R8 betecknar lägre alkyl möjligen j ' : 25 substituerad med hydroxi, karboxi eller pyridyl, eller ; alternativt bildar R' och R8 tillsammans med kväveatomen som de är bundna tili, en ring, som kan vara substituerad, en lägre alkoxigrupp eller en lägre hydroxialkoxigrupp, » , ;·. (2) när ovan nämnda bindning är en enkelbindning, sä betecknar
2. Kondenserad pyridazinförening som representeras av den allmänna formeln (II) eller ett farinakologiskt lämpligt sait därav: 10 ΗΝ''<ΟΗ2)1-3\^γ/Κ12 R1^W^ kkR,3 i R II (lR1)rv' y väri R‘° betecknar halogen, en nitrogrupp, en aminogrupp, en syanogrupp eller 4-hydroxipiperidin-l-ylgrupp, 15 R1, R12 och Ru är envar säsom definierats i patentkrav 1, y är =C-B, där B är säsom definierats i patentkrav, och : : 2 0 n är heltal 1-3. t : : : 3. Kondenserad pyridazinförening som representeras av den allmänna formeln (V) eller ett f armakologiskt lämpligt sait därav: :v. 25 ,R12 :'V: hn- (Il ΐ r14 V . y '··' väri R1’ och Y envar är säsom definierats ovan, och R12, R13 och R14 betecknar envar oberoende av varandra halogen, 30 metoxi eller etoxi. si 111841
3. X en grupp -NR5-, väri Rs betecknar väte eller lägre alkyl möjligen substituerad med en hydroxylgrupp, en karboxylgrupp, 90 111841 en acylgrupp eller en tetrahydropyranylgrupp, och Y betecknar en karbonylgrupp, förutsatt att B icke är Cl, när R1 är 7- eller 8-nitro och R12 5 och R13 är 3,4-metylendioxi och R14 är väte.
4. Kondenserad pyridazinförening, som representeras av den allmänna formeln (VI) eller ett farmakologiskt lämpligt sait därav: 5 /R12 ^lli r14 v| där Rla och Y envar är säsom definierats ovan, och R12, R13 och R14 betecknar envar oberoende av varandra väte, 10 metoxi eller etoxi.
5. Kondenserad pyridazinförening enligt patentkrav 1 eller 2, väri -(CH2),_.f- är -CH2-.
6. Andvändning av en kondenserad pyridazinförening enligt nägot av patentkraven 1-5 vid framställning av ett medikament för behandling eller profylax av pulmonal hypertension.
7. Andvändning av en kondenserad pyridazinförening enligt nägot ‘ 2 0 av patentkraven 1-5 vid f ramställning av ett medikament för behandling eller profylax av angina pectoris.
8. Andvändning av en kondenserad pyridazinförening enligt nägot av patentkraven 1-5 vid framställning av ett medikament för ·'; 2 5 behandling eller profylax av sjukdomar för vilka en cyklisk GMP-fosfodiesteras-inhiberande verkning är effektiv.
: 9. Andvändning av en kondenserad pyridazinförening enligt nägot av patentkraven 1-5 vid framställning av ett medikament för 30 behandling eller profylax av sjukdomar för vilka en anti-blodplätte-verkning är effektiv.
FI961510A 1994-08-09 1996-04-03 Kondenserade pyridazinföreningar och användning av desamma vid framställning av medikament FI111841B (sv)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
JP18712894 1994-08-09
JP18712894 1994-08-09
JP31633794 1994-12-20
JP31633794 1994-12-20
PCT/JP1995/001575 WO1996005176A1 (fr) 1994-08-09 1995-08-08 Compose de pyridazine condense
JP9501575 1995-08-08

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FI961510A0 FI961510A0 (sv) 1996-04-03
FI961510A FI961510A (sv) 1996-05-29
FI111841B true FI111841B (sv) 2003-09-30

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US (2) US5849741A (sv)
EP (1) EP0722936B1 (sv)
KR (1) KR100189865B1 (sv)
CN (1) CN1151136C (sv)
AT (1) ATE267174T1 (sv)
AU (1) AU705229B2 (sv)
CA (1) CA2173493C (sv)
DE (1) DE69533057T2 (sv)
ES (1) ES2224130T3 (sv)
FI (1) FI111841B (sv)
HU (1) HU219864B (sv)
MX (1) MX9601310A (sv)
NO (1) NO309378B1 (sv)
NZ (1) NZ290952A (sv)
WO (1) WO1996005176A1 (sv)

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NO309378B1 (no) 2001-01-22
NZ290952A (en) 1998-05-27
CN1135210A (zh) 1996-11-06
ATE267174T1 (de) 2004-06-15
FI961510A0 (sv) 1996-04-03
EP0722936A1 (en) 1996-07-24
NO961397L (no) 1996-06-06
HU9600933D0 (en) 1996-07-29
NO961397D0 (no) 1996-04-09
CA2173493A1 (en) 1996-02-22
US5849741A (en) 1998-12-15
AU705229B2 (en) 1999-05-20
HU219864B (hu) 2001-08-28
CN1151136C (zh) 2004-05-26
EP0722936B1 (en) 2004-05-19
HUT76067A (en) 1997-06-30
FI961510A (sv) 1996-05-29
ES2224130T3 (es) 2005-03-01
DE69533057T2 (de) 2005-06-16
MX9601310A (es) 1998-11-30
WO1996005176A1 (fr) 1996-02-22
KR100189865B1 (ko) 1999-06-01
AU3191995A (en) 1996-03-07
US6218392B1 (en) 2001-04-17
KR960704854A (ko) 1996-10-09
CA2173493C (en) 2008-03-25
EP0722936A4 (en) 1996-12-11

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