AR067236A1 - PROTEASE INHIBITORS - Google Patents

PROTEASE INHIBITORS

Info

Publication number
AR067236A1
AR067236A1 ARP080101172A ARP080101172A AR067236A1 AR 067236 A1 AR067236 A1 AR 067236A1 AR P080101172 A ARP080101172 A AR P080101172A AR P080101172 A ARP080101172 A AR P080101172A AR 067236 A1 AR067236 A1 AR 067236A1
Authority
AR
Argentina
Prior art keywords
formula
alkyl
methyl
compound
clause
Prior art date
Application number
ARP080101172A
Other languages
Spanish (es)
Inventor
Kevin Parkes
Urszula Grabowska
Vladimir Ivanov
Tony Johnson
Lourdes Oden
Christian Sun
Jussi Kangasmetsa
Pia Kahnberg
Magnus Nilsson
Matt Tozer
Original Assignee
Medivir Ab
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 GB0705213A external-priority patent/GB0705213D0/en
Priority claimed from GB0712182A external-priority patent/GB0712182D0/en
Application filed by Medivir Ab filed Critical Medivir Ab
Publication of AR067236A1 publication Critical patent/AR067236A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders

Abstract

Compuestos de la formula (1) en donde R2 es la cadena lateral de leucina, isoleucina, ciclohexilglicina, O-metilo treonina, 4-fluoroleucina o 3-metoxivalina; R3 es H, metilo o fluoro; R4 es alquilo C1-6; E es un enlace o tiazolilo, opcionalmente sustituido con metilo o fluoro; n es 0 o 1; o una sal, N-oxido o hidrato aceptable para uso farmacéutico del mismo; que son de utilidad en el tratamiento de trastornos caracterizados por una expresion o activacion inapropiada de catepsina K, tales como osteoporosis, osteoartritis, artritis reumatoide o metástasis osea. Reivindicacion 30: Un compuesto, caracterizado porque es de la formula (2) en donde los grupos Rb definen un cetal, tal como el bis-metilcetal, o juntos definen un cetal cíclico, tal como 1,3-dioxolano, o un derivado N-protegido del mismo. Reivindicacion 31: Un compuesto de acuerdo con la cláusula 30 caracterizado porque es de formula (3). Reivindicacion 32: Un compuesto, caracterizado porque es de la formula (4) en donde R4 representa aIquiIo C1-6, o una sal o éster de alquilo inferior (por ejemplo alquilo C1-6) del mismo. Reivindicacion 33: Un compuesto de acuerdo con la cláusula 32, caracterizado porque es e formula (5).Compounds of the formula (1) wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxivaline; R3 is H, methyl or fluoro; R4 is C1-6 alkyl; E is a bond or thiazolyl, optionally substituted with methyl or fluoro; n is 0 or 1; or a salt, N-oxide or hydrate acceptable for pharmaceutical use thereof; which are useful in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastasis. Claim 30: A compound, characterized in that it is of the formula (2) wherein the Rb groups define a ketal, such as bis-methylketal, or together define a cyclic ketal, such as 1,3-dioxolane, or a derivative N -protected from it. Claim 31: A compound according to clause 30 characterized in that it is of formula (3). Claim 32: A compound, characterized in that it is of the formula (4) wherein R4 represents C1-6 alkyl, or a lower alkyl salt or ester (for example C1-6 alkyl) thereof. Claim 33: A compound according to clause 32, characterized in that it is e formula (5).

ARP080101172A 2007-03-19 2008-03-19 PROTEASE INHIBITORS AR067236A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0705213A GB0705213D0 (en) 2007-03-19 2007-03-19 Protease inhibitors
GB0712182A GB0712182D0 (en) 2007-06-25 2007-06-25 Protease inhabitors
EP07123740 2007-12-20

Publications (1)

Publication Number Publication Date
AR067236A1 true AR067236A1 (en) 2009-10-07

Family

ID=39472105

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080101172A AR067236A1 (en) 2007-03-19 2008-03-19 PROTEASE INHIBITORS

Country Status (3)

Country Link
AR (1) AR067236A1 (en)
TW (1) TW200906392A (en)
WO (1) WO2008114054A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0817424D0 (en) 2008-09-24 2008-10-29 Medivir Ab Protease inhibitors

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7425562B2 (en) * 2001-01-17 2008-09-16 Amura Therapeutics Ltd. Inhibitors of cruzipain and other cysteine proteases
ATE461200T1 (en) * 2004-01-08 2010-04-15 Medivir Ab CYSTEIN PROTEASE INHIBITORS

Also Published As

Publication number Publication date
TW200906392A (en) 2009-02-16
WO2008114054A1 (en) 2008-09-25

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