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AR002726A1 - Un compuesto que inhibe la transferasa de proteina farnesilada, una composicion farmaceutica que lo comprende y el uso del mismo para lamanufactura de un medicamento. - Google Patents

Un compuesto que inhibe la transferasa de proteina farnesilada, una composicion farmaceutica que lo comprende y el uso del mismo para lamanufactura de un medicamento.

Info

Publication number
AR002726A1
AR002726A1 ARP960101942A AR10194296A AR002726A1 AR 002726 A1 AR002726 A1 AR 002726A1 AR P960101942 A ARP960101942 A AR P960101942A AR 10194296 A AR10194296 A AR 10194296A AR 002726 A1 AR002726 A1 AR 002726A1
Authority
AR
Argentina
Prior art keywords
aryl
substituted
alkyl
heterocycle
protein
Prior art date
Application number
ARP960101942A
Other languages
English (en)
Original Assignee
Merck & Co 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 US08/600,728 external-priority patent/US5856326A/en
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR002726A1 publication Critical patent/AR002726A1/es

Links

Classifications

    • 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
    • C07D233/64—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 substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • C07D401/14—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
    • C07D403/06—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
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

La presente invención está dirigida a compuestos de fórmula (I) que inhiben a la transferasa de proteína farnesilada (FTasa) y a la farnesilación de laproteína del oncogén Ras. La invención está dirigida también a medicamentos que contienen estoscompuestos; donde R es -C: O-Y y Z; R1a y R1b son a)H,arilo, cicloalquilo, alquenilo, alquinilo R10O-, R11S(O)m-, R10C(O)NR10-, (R10)2N-C:0-, -CN, -NO2, (R10)2N-C(NR10)2-, R10C:O-, R10OC:0-, N3, -(NR10)2 oR11OC:ONR10-; b) alquilo sustituido onó con arilo, a su vez sustituido o nó por los mismos sustituyentes exceptuando el arilo.R2 y R3 son alquilo saturadoo nó, arilo, heterociclilo todos pueden estar sustituidos, carboxilo esterificado por alquilo, arilo,heteroaroilo,hetero- o arilsulfonil entre otrosamido, o amido sustituidos en el N por F carbamatos, heterociclos, N3, arilos o alquilos entre otros. R2 y R3 pueden formar un puente alquileno sustituidoo nó por: S(O)m, -NC:O-. R4 y R5 son H ó CH3; R8 puede ser entreotros H, perfluoroalquil cianofenil, F, Cl, Br, además de lo definido para R1a y R1b,exceptuando los alquilos cíclicos o no insaturados o nó; R9 es H, perfluoralquil y los radicales mencionados para R1a y R1b en a) o bienalquilosustituido o nó por los ya definidos para R9; R10 es alquilo, bencilo, arilo; R11 es alquilo, arilo; A y A2 son un enlace simple, doble o tripleademás de -C:O-, -C:ONR10-, -NR10C:0-, O, S(O)m, -S(O)2NR10-, -NR10S(O2)-; C es H ó O; V es H, aril, heterociclo, alquenil, alquil sustituido o nó por O, S,N; W es un heterociclo; X es metileno, -C:O-, -S(:O)m-; Y es arilo o heterociclo sustituidos o nó; Z es arilo, heteroarilo, arilmetil, heteroarilmetil, arilsulfonil, heteroarilsulfonilsustituidos o nó.
ARP960101942A 1995-03-29 1996-03-27 Un compuesto que inhibe la transferasa de proteina farnesilada, una composicion farmaceutica que lo comprende y el uso del mismo para lamanufactura de un medicamento. AR002726A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41282995A 1995-03-29 1995-03-29
US47069095A 1995-06-06 1995-06-06
US08/600,728 US5856326A (en) 1995-03-29 1996-03-01 Inhibitors of farnesyl-protein transferase

Publications (1)

Publication Number Publication Date
AR002726A1 true AR002726A1 (es) 1998-04-29

Family

ID=27410959

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP960101942A AR002726A1 (es) 1995-03-29 1996-03-27 Un compuesto que inhibe la transferasa de proteina farnesilada, una composicion farmaceutica que lo comprende y el uso del mismo para lamanufactura de un medicamento.

Country Status (21)

Country Link
EP (1) EP0820445A1 (es)
JP (1) JP3043815B2 (es)
CN (1) CN1195340A (es)
AR (1) AR002726A1 (es)
AU (1) AU710672B2 (es)
BG (1) BG101973A (es)
BR (1) BR9607953A (es)
CA (1) CA2216707A1 (es)
CZ (1) CZ306297A3 (es)
EE (1) EE9700314A (es)
HR (1) HRP960143A2 (es)
HU (1) HUP9801883A3 (es)
IL (1) IL117580A0 (es)
IS (1) IS4568A (es)
MX (1) MX9707459A (es)
NO (1) NO974457L (es)
NZ (1) NZ305254A (es)
PL (1) PL322549A1 (es)
SK (1) SK129297A3 (es)
TR (1) TR199701056T1 (es)
WO (1) WO1996030343A1 (es)

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