AR050858A1 - Compuesto de heteroaril-nitrilo sustituido, su uso para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para la preparacion del mismo - Google Patents

Compuesto de heteroaril-nitrilo sustituido, su uso para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para la preparacion del mismo

Info

Publication number
AR050858A1
AR050858A1 ARP050103711A ARP050103711A AR050858A1 AR 050858 A1 AR050858 A1 AR 050858A1 AR P050103711 A ARP050103711 A AR P050103711A AR P050103711 A ARP050103711 A AR P050103711A AR 050858 A1 AR050858 A1 AR 050858A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
heteroaryl
heterocyclyl
alkylene
Prior art date
Application number
ARP050103711A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR050858A1 publication Critical patent/AR050858A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Un compuesto de heteroaril-nitrilo sustituido de formula (1): en donde: R1 representa alquilo C1-8, -alquilen C1-8-NRERF, -alquilen C1-8-NRGC(O)O-alquilo C1-6, -alquilen C1-8NRGC(O)-alquilo C1-6 o -alquilen C1-8-cicloalquilo; R3 representa H o alquilo C1-6; R4 representa H o alquilo C1-6; y a) X representa NR5 y A representa C(O) y i) R2 representa R2a en donde R2a representa -NRH-arilo, -NRH-heteroarilo, -NRH-aril-heteroarilo o -NRH-heteroaril-arilo; y R2b representa -alquilen C1-6-RA, arilo, biarilo, -aril-heteroarilo, -heteroaril-arilo, -aril-heterociclilo, -aril-alquilen C1-3-heterociclilo, -aril-O-alquilen C1-3-heterociclilo, aril-alquilen C1-3-heteroarilo, -aril-heteroaril-alquilen C1-3-heterociclilo, -heteroaril-aril- alquilen C1-3-heterociclilo, ariloxi, heteroarilo, cicloalquilo, -cicloalquil-arilo, cicloalquiloxi, heterociclilo, -NRH-aril-heterociclilo, -NRH-cicloalquilo, -NRB-alquilen C1-6-RC, -O-alquilen C1-6RD o -O-alquenilo C1-6; -aril-alquilen C1-3- heterociclil-RJ, -aril-alquilen C1-3-heteroaril-RK, alquilen C1-3(NH2)-arilo; y R5 representa H, alquilo C1-6, alquenilo C1-6, -C(O)R2a, -alquilen C1-8-heterociclilo, -alquilen C1-8-NRGC(O)-alquilo C1-6, -alquilen C1-8NRGC(O)O-alquilo C1-6, - alquilen C1-8NRERF, N-ftalidimido-alquilen C1-8- o -C(O)-alquilo C1-6; o ii) R2 y R5 junto con los átomos de C y N a los que están respectivamente unidos forman un grupo seleccionado de los restos de formulas (2), o b) X representa NR5 y A representa -SO2- y R2 representa alquilo C1-6 o aralquilo C1-6; y R5 representa H, alquilo C1-6, alquenilo C1-6, -alquilen C1-8-heterociclilo, -alquilen C1-8-NRGC(O)-alquilo C1-6, -alquilen C1-8NRGC(O)O-alquilo C1-6, -alquilen C1-8NRERF, N- ftalidimido-alquilen C1-8- o -C(O)-alquilo C1-6; o c) X representa CH2 y A representa C(O) y R2 representa -NRH-arilo, -NRH-heteroarilo, -NRH-aralquilo C1-6, -NRH-alquilen C1-6-heteroarilo, -NRH-aril-heteroarilo, -NRH-aril-heterociclilo o -O- aralquilo C1-6; en la que RA, RC y RD independientemente representan H, halogeno, -NRERF, ciano, CCl3, -C(O)-alquilo C1-6, alquilo C1-3, cicloalquilo, heterociclilo, arilo, biarilo, -aril-heteroarilo, -aril-alquilen C1-3-heterociclilo, -aril-O- alquilen C1-3-heterociclilo, -alquenil C1-3-arilo, heteroarilo, aralquilo C1-6, -NHC(O)-alquilo C1-6, -NHC(O)O-alquilo C1-6, -NHC(O)-aralquilo C1-6 o -NHC(O)O-aralquilo C1-6; RB representa H o alquilo C1-8; Re y RF independientemente representan H o alquilo C1-3; o RE representa cicloalquilo y RF representa H; o RE y RF junto con el átomo de N al que están unidos forman un anillo heterocíclico de 5 o 6 miembros; RG representa H o alquilo C1-3; RH representa H, alquilo C1-6, -alquilen C1-6- NHC(O)-alquilo C1-4, -alquilen C1-6-NHC(O)O-alquilo C1-4 o -alquilen C1-6-NRERF; RJ representa arilo, heteroarilo, heterociclilo, -alquilen C1-3(arilo)2, -alquilen C1-3-heteroarilo, -aralquilo C1-3, -alquilen C1-3-oxo-heterociclilo, -O-C(O)-alquilen C1-3-arilo; RK representa uno o dos sustituyentes arilo; y sus sales y solvatos. Composicion farmacéutica que comprende dicho compuesto y su uso para la preparacion de dicha composicion util para el tratamiento de afecciones susceptibles de mediacion por un inhibidor de cistaína proteasa, como malaria o enfermedades oseas, de cartílagos o articulaciones. Procedimiento para la preparacion de dicho compuesto.
ARP050103711A 2004-09-07 2005-09-05 Compuesto de heteroaril-nitrilo sustituido, su uso para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para la preparacion del mismo AR050858A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP04381032 2004-09-07

Publications (1)

Publication Number Publication Date
AR050858A1 true AR050858A1 (es) 2006-11-29

Family

ID=34931921

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050103711A AR050858A1 (es) 2004-09-07 2005-09-05 Compuesto de heteroaril-nitrilo sustituido, su uso para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para la preparacion del mismo

Country Status (4)

Country Link
AR (1) AR050858A1 (es)
PE (1) PE20060718A1 (es)
TW (1) TW200624429A (es)
WO (1) WO2006027211A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0713320A2 (pt) 2006-06-20 2012-02-07 Wyeth Corp inibidores de canal de potássio imidazola kvl.5
EP2030621A1 (en) * 2007-08-21 2009-03-04 Glaxo Group Limited Novel substituted pyrimidines as cysteine protease inhibitors
EP1918284A1 (en) * 2006-10-30 2008-05-07 Glaxo Group Hydrazinopyrimidines as cysteine protease inhibitors
TW200825058A (en) * 2006-10-30 2008-06-16 Glaxo Group Ltd Cysteine protease inhibitors
EP1972630A1 (en) * 2007-03-02 2008-09-24 Glaxo Group Limited Purines as cysteine protease inhibitors
CN101675050A (zh) * 2007-03-02 2010-03-17 葛兰素集团有限公司 作为半胱氨酸蛋白酶抑制剂的嘌呤
DE102008063561A1 (de) * 2008-12-18 2010-08-19 Bayer Cropscience Ag Hydrazide, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Insektizide

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR036375A1 (es) * 2001-08-30 2004-09-01 Novartis Ag Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos
UY27813A1 (es) * 2002-05-31 2003-12-31 Smithkline Beecham Corp Inhibidores de la peptido-desformilasa
GB0220187D0 (en) * 2002-08-30 2002-10-09 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
PE20060718A1 (es) 2006-10-04
WO2006027211A1 (en) 2006-03-16
TW200624429A (en) 2006-07-16

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