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HUP0303624A2 - NEP inhibitor hatású N-fenpropil-ciklopentil-csoporttal szubsztituált glutáramid származékok és ezeket tartalmazó gyógyászati készítmények és eljárás a vegyületek előállítására - Google Patents

NEP inhibitor hatású N-fenpropil-ciklopentil-csoporttal szubsztituált glutáramid származékok és ezeket tartalmazó gyógyászati készítmények és eljárás a vegyületek előállítására

Info

Publication number
HUP0303624A2
HUP0303624A2 HU0303624A HUP0303624A HUP0303624A2 HU P0303624 A2 HUP0303624 A2 HU P0303624A2 HU 0303624 A HU0303624 A HU 0303624A HU P0303624 A HUP0303624 A HU P0303624A HU P0303624 A2 HUP0303624 A2 HU P0303624A2
Authority
HU
Hungary
Prior art keywords
group
heterocyclyl
carbocyclyl
alkyl
groups
Prior art date
Application number
HU0303624A
Other languages
English (en)
Inventor
Stephen Challenger
Andrew Simon Cook
Adam Thomas Gillmore
Donald Stuart Middleton
David Cameron Pryde
Alan Stobie
Original Assignee
Pfizer Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0107750A external-priority patent/GB0107750D0/en
Priority claimed from GB0113112A external-priority patent/GB0113112D0/en
Priority claimed from GB0120152A external-priority patent/GB0120152D0/en
Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of HUP0303624A2 publication Critical patent/HUP0303624A2/hu
Publication of HUP0303624A3 publication Critical patent/HUP0303624A3/hu

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    • C07—ORGANIC CHEMISTRY
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    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/82—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
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    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • A61K9/0036—Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A—HUMAN NECESSITIES
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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    • C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having 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
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having 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 with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/74—Benzo[b]pyrans, hydrogenated in the carbocyclic ring
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    • C07—ORGANIC CHEMISTRY
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    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
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  • Bioinformatics & Cheminformatics (AREA)
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  • Urology & Nephrology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)

Abstract

A találmány tárgyát N-fenpropil-ciklopentil-csoporttal szubsztituáltglutáramid-származékok, valamint ezeket tartalmazó gyógyászatikészítmények és egy vagy több további hatóanyagot tartalmazókombinációk képezik; e vegyületek a neutrális endopeptidáz enzim (MEP)inhibitoraiként viselkednek, a találmány tárgyához tartozik az (I)általános képletű vegyületek előállítására szolgáló eljárás is. Az (l)általános képletben a szubsztituensek jelentése igen sokféle, ígypéldául R1 jelentése alkilcsoport, amely egy vagy több szubsztituensthordozhat, ahol a szubsztituensek lehetnek például halogénatom,hidroxil-, alkoxi-, karbociklil-, heterociklil-, -NR2R3, -NR4COR5, -NR4SO2R5, -CONR2R3, -S(O)pR6, -COR7 vagy CO2 csoport; vagy R1jelentése karbociklil- vagy heterociklilcsoport, amely csoportokmindegyike egy vagy több szubsztituenst hordozhat: vagy R1 jelentésehidrogénatom, 1-6 szénatomos alkoxicsoport, -NR2R3 vagy -NR4SO2R5;ahol R2 és R3 jelentése karbociklil- vagy heterociklilcsoport, amelycsoportok mindegyike alkil-, hidroxil- vagy alkoxicsoporttal lehetszubsztituálva; vagy hidrogénatom vagy alkilcsoport; vagy R2 és R3 anitrogénatommal együtt, amelyhez kapcsolódnak pirrolidinil-,piperidino-, morfolino-, piperazinil- vagy N-piperazinil-csoportotképeznek; R4 jelentése hidrogénatom vagy alkilcsoport; R5 jelentésepéldául alkil-, -CF3, karbociklil-, heterociklil-, alkoxicsoport vagy-NR2R3; R6 jelentése alkil-, karbociklil-, heterociklilcsoport vagy -NR2R3; és R7 jelentése alkil-, karbociklil- vagy heterociklilcsoport;p értéke 0, 1, 2 vagy 3; X jelentése -(CH2)n- vagy -CH2)qO- kapcsolócsoport, ahol az Y csoport az oxigénatomhoz kapcsolódik; ahol akapcsoló csoportokban lévő egy vagy több hidrogénatom helyettegymástól függetlenül állhat például alkoxi-, hidroxil-, hidroxil-alkil-, cikloalkil-, heterociklilcsoport; n értéke 3, 4, 5, 6 vagy 7;továbbá q értéke 2, 3, 4, 5 vagy 6; továbbá Y jelentése fenil- vagypiridilcsoport, amely csoportok bármelyike egy vagy több R8 csoporttallehet szubsztituálva, ahol az R8 csoport lehet azonos vagy egymástóleltérő, ahol R8 jelentése például hidroxil-, merkaptocsoport, ciano-,acil-, amino-, karbociklil- vagy heterociklilcsoport - amely csoportokadott esetben szubsztituálva lehetnek; vagy a szomszédos szénatomokonlévő két R8 csoport a kapcsolódó szénatomokkal együtt 5- vagy 6 tagúkondenzált karbociklil- vagy heterociklil gyűrűt képezhetnek. Atalálmány szerinti vegyületek eredményesen alkalmazhatók a nőiszexuális diszfunkció és a férfi erekciós diszfunkció kezelésére. Ó
HU0303624A 2001-03-28 2002-03-18 N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad and process for preparation of the compounds HUP0303624A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0107750A GB0107750D0 (en) 2001-03-28 2001-03-28 Novel pharmaceuticals
GB0113112A GB0113112D0 (en) 2001-05-30 2001-05-30 Novel pharmaceuticals
GB0120152A GB0120152D0 (en) 2001-08-17 2001-08-17 Novel pharmaceuticals
PCT/IB2002/000807 WO2002079143A1 (en) 2001-03-28 2002-03-18 N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad

Publications (2)

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HUP0303624A2 true HUP0303624A2 (hu) 2004-03-01
HUP0303624A3 HUP0303624A3 (en) 2005-06-28

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HU0303624A HUP0303624A3 (en) 2001-03-28 2002-03-18 N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad and process for preparation of the compounds

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EP (1) EP1373192A1 (hu)
JP (1) JP4018545B2 (hu)
KR (1) KR100564466B1 (hu)
CN (1) CN1243723C (hu)
AP (1) AP1689A (hu)
AR (1) AR035795A1 (hu)
BG (1) BG108130A (hu)
BR (1) BR0208455A (hu)
CA (1) CA2437113A1 (hu)
CZ (1) CZ20032534A3 (hu)
DO (1) DOP2002000364A (hu)
EA (1) EA006154B1 (hu)
EE (1) EE200300469A (hu)
GE (1) GEP20063783B (hu)
HK (1) HK1060724A1 (hu)
HR (1) HRP20030751A2 (hu)
HU (1) HUP0303624A3 (hu)
IL (1) IL157009A0 (hu)
IS (1) IS6877A (hu)
MA (1) MA26996A1 (hu)
MX (1) MXPA03006597A (hu)
MY (1) MY134081A (hu)
NO (1) NO20034299L (hu)
NZ (1) NZ527012A (hu)
OA (1) OA12553A (hu)
PA (1) PA8542401A1 (hu)
PE (1) PE20021014A1 (hu)
PL (1) PL365101A1 (hu)
RS (1) RS75303A (hu)
SK (1) SK11822003A3 (hu)
TN (1) TNSN02032A1 (hu)
TW (1) TWI254038B (hu)
UY (1) UY27227A1 (hu)
WO (1) WO2002079143A1 (hu)

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