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AR035795A1 - DERIVATIVES OF GLUTARAMIDE REPLACED WITH N-FENPROPILCICLOPENTILO AS INHIBITORS OF THE NEUTRAL ENDOPEPTIDASE ENZYME, USE OF THE SAME, PROCEDURES AND INTERMEDIARIES FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THESE INHIBITORS - Google Patents

DERIVATIVES OF GLUTARAMIDE REPLACED WITH N-FENPROPILCICLOPENTILO AS INHIBITORS OF THE NEUTRAL ENDOPEPTIDASE ENZYME, USE OF THE SAME, PROCEDURES AND INTERMEDIARIES FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THESE INHIBITORS

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Publication number
AR035795A1
AR035795A1 ARP020101114A ARP020101114A AR035795A1 AR 035795 A1 AR035795 A1 AR 035795A1 AR P020101114 A ARP020101114 A AR P020101114A AR P020101114 A ARP020101114 A AR P020101114A AR 035795 A1 AR035795 A1 AR 035795A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
carbocyclyl
heterocyclyl
halo
Prior art date
Application number
ARP020101114A
Other languages
Spanish (es)
Original Assignee
Pfizer
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 filed Critical Pfizer
Publication of AR035795A1 publication Critical patent/AR035795A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • 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
    • 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
    • A61K9/0019—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
    • 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
    • A61K9/0036—Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—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
    • 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
    • C07C323/40—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • C07D213/02—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
    • 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
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Reproductive Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gynecology & Obstetrics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Dispersion Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • 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)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Pyrane Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Quinoline Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

Un compuesto derivado de glutaramida sustituida con N-fenpropilciclopentilo de fórmula (1), una sal, solvato, poliformo o profármaco del mismo farmacéuticamente aceptables, donde: R1 es alquilo C1-6 que puede estar sustituido con uno o más sustituyentes, que pueden ser iguales o diferentes, seleccionados de la lista: halo, hidroxi, alcoxi C1-6, hidroxi-alcoxi C1-6, alcoxi C1-6-alcoxi C1-6, carbociclilo, carbocicliloxi, alcoxi C1-4-carbocicliloxi, heterociclilo, heterocicliloxi, -NR2R3, -NR4COR5, -NR4SO2R5, -CONR2R3, -S(O)pR6, -COR7 y CO2(alquilo C1-4); o R1 es carbociclilo o heterociclilo, cada uno de los cuales puede estar sustituido con uno o más sustituyentes de dicha lista, cuyos sustituyentes pueden ser iguales o diferentes, cuya lista incluye además alquilo C1-6, o R1 es hidrógeno, alcoxi C1-6, -NR2R3 o NR4SO2R5; en donde: R2 y R3, que pueden ser iguales o diferentes, son carbociclilo o heterociclilo (cada uno de los cuales puede estar sustituido con alquilo C1-4, hidroxi o alcoxi C1-4); o son hidrógeno o alquilo C1-4; o R2 y R3 junto con el nitrógeno al que están unidos forman un grupo pirrolidinilo, piperidino, morfolino, piperazinilo o N-(alquil C1-4) piperazinilo; R4 es hidrógeno o alquilo C1-4; R5 es alquilo C1-4, CF3, carbociclilo, (alquil C1-4) carbociclilo, (alcoxi C1-4) carbociclilo, heterociclilo, alcoxi C1-4 o -NR2R3; R6 es alquilo C1-4, carbociclilo, heterociclilo o NR2R3; y R7 es alquilo C1-4, carbociclilo o heterociclilo; p es 0, 1, 2 o 3; X es el enlace -(CH2)n- o -(CH2)q-O- (donde Y está unido al oxígeno), donde uno o más átomos de hidrógeno en el enlace X se pueden reemplazar, independientemente, por alcoxi C1-4; hidroxi, hidroxi(alquilo C1-3), cicloalquilo C3-7, carbociclilo, heterociclilo, o por alquilo C1-4 opcionalmente sustituido con uno o más grupos flúor o fenilo; n es 3, 4, 5, 6 o 7; y q es 2, 3, 4, 5 o 6; e Y es fenilo o piridilo, cada uno de os cuales puede estar sustituido con uno o más grupos R8 que pueden ser iguales o diferentes; donde R8 es hidroxi, mercapto, halógeno, ciano, acilo, amino, mono-alquilo C1-4-amino, di-alquil C1-4-amino, carbociclilo o heterociclilo (cada uno de los cuales está opcionalmente sustituido con alquilo C1-6, halo-alquilo C1-6, alcoxi C1-6, halo-alcoxi C1-6, alquiltio C1-6 o halógeno), alcoxi C1-6, fenoxi, alquiltio C1-6, feniltio, o alquilo opcionalmente sustituido con alcoxi C1-6, halo-alcoxi C1-6, alquiltio C1-6, halógeno o fenilo; o dos grupos R8 en los átomos de carbono adyacentes junto con los átomos de carbono que los interconectan pueden formar un anillo carbocíclico o heterocíclico, condensado, de 5 o 6 miembros, opcionalmente sustituido con alquilo C1-6, halo-alquilo C1-6, alcoxi C1-6, halo-alcoxi C1-6, alquiltio C1-6 o halógeno. También se dan a conocer: composiciones farmacéuticas que los contienen, su uso para la fabricación de un medicamento para inhibir la endopeptidasa neutra, procedimientos y compuestos necesarios para su preparación.A compound derived from glutaramide substituted with N-phepropylcyclopentyl of formula (1), a pharmaceutically acceptable salt, solvate, polymorph or prodrug thereof, wherein: R1 is C1-6 alkyl which may be substituted with one or more substituents, which may be same or different, selected from the list: halo, hydroxy, C1-6 alkoxy, C1-6 hydroxy-alkoxy, C1-6 alkoxy-C1-6 alkoxy, carbocyclyl, carbocyclyloxy, C1-4-carbocyclyloxy alkoxy, heterocyclyl, heterocyclyloxy, -NR2R3, -NR4COR5, -NR4SO2R5, -CONR2R3, -S (O) pR6, -COR7 and CO2 (C1-4 alkyl); or R1 is carbocyclyl or heterocyclyl, each of which may be substituted with one or more substituents of said list, whose substituents may be the same or different, whose list also includes C1-6 alkyl, or R1 is hydrogen, C1-6 alkoxy , -NR2R3 or NR4SO2R5; wherein: R2 and R3, which may be the same or different, are carbocyclyl or heterocyclyl (each of which may be substituted with C1-4alkyl, hydroxy or C1-4alkoxy); or are hydrogen or C1-4 alkyl; or R2 and R3 together with the nitrogen to which they are attached form a pyrrolidinyl, piperidino, morpholino, piperazinyl or N- (C1-4 alkyl) piperazinyl group; R4 is hydrogen or C1-4 alkyl; R5 is C1-4 alkyl, CF3, carbocyclyl, (C1-4 alkyl) carbocyclyl, (C1-4 alkoxy) carbocyclyl, heterocyclyl, C1-4 alkoxy or -NR2R3; R6 is C1-4 alkyl, carbocyclyl, heterocyclyl or NR2R3; and R7 is C1-4 alkyl, carbocyclyl or heterocyclyl; p is 0, 1, 2 or 3; X is the bond - (CH2) n- or - (CH2) q-O- (where Y is attached to oxygen), where one or more hydrogen atoms in the X bond can be replaced, independently, by C1-4 alkoxy; hydroxy, hydroxy (C1-3 alkyl), C3-7 cycloalkyl, carbocyclyl, heterocyclyl, or by C1-4 alkyl optionally substituted with one or more fluorine or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted with one or more R8 groups that may be the same or different; where R 8 is hydroxy, mercapto, halogen, cyano, acyl, amino, mono 1-4C-alkyl, di-C 1-4 alkyl, carbocyclyl or heterocyclyl (each of which is optionally substituted with C 1-6 alkyl , halo C1-6 alkyl, C1-6 alkoxy, halo C1-6 alkoxy, C1-6 alkylthio or halogen), C1-6 alkoxy, phenoxy, C1-6 alkylthio, phenylthio, or alkyl optionally substituted with C1- alkoxy 6, halo C1-6 alkoxy, C1-6 alkylthio, halogen or phenyl; or two R8 groups in the adjacent carbon atoms together with the interconnecting carbon atoms may form a condensed, 5- or 6-membered carbocyclic or heterocyclic ring, optionally substituted with C1-6 alkyl, halo- C1-6 alkyl, C1-6 alkoxy, halo- C1-6 alkoxy, C1-6 alkylthio or halogen. Also disclosed are: pharmaceutical compositions containing them, their use for the manufacture of a medicament for inhibiting neutral endopeptidase, procedures and compounds necessary for its preparation.

ARP020101114A 2001-03-28 2002-03-26 DERIVATIVES OF GLUTARAMIDE REPLACED WITH N-FENPROPILCICLOPENTILO AS INHIBITORS OF THE NEUTRAL ENDOPEPTIDASE ENZYME, USE OF THE SAME, PROCEDURES AND INTERMEDIARIES FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THESE INHIBITORS AR035795A1 (en)

Applications Claiming Priority (3)

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

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AR035795A1 true AR035795A1 (en) 2004-07-14

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EP (1) EP1373192A1 (en)
JP (1) JP4018545B2 (en)
KR (1) KR100564466B1 (en)
CN (1) CN1243723C (en)
AP (1) AP1689A (en)
AR (1) AR035795A1 (en)
BG (1) BG108130A (en)
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CA (1) CA2437113A1 (en)
CZ (1) CZ20032534A3 (en)
DO (1) DOP2002000364A (en)
EA (1) EA006154B1 (en)
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