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AR050786A1 - Compuestos y composiciones utiles como inhibidores de catepsina-s - Google Patents

Compuestos y composiciones utiles como inhibidores de catepsina-s

Info

Publication number
AR050786A1
AR050786A1 ARP050103494A ARP050103494A AR050786A1 AR 050786 A1 AR050786 A1 AR 050786A1 AR P050103494 A ARP050103494 A AR P050103494A AR P050103494 A ARP050103494 A AR P050103494A AR 050786 A1 AR050786 A1 AR 050786A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
alkyl
halogen
denotes
Prior art date
Application number
ARP050103494A
Other languages
English (en)
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR050786A1 publication Critical patent/AR050786A1/es

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    • 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
    • C07D239/34—One oxygen atom
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen 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
    • C07D401/02—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
    • 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
    • C07D403/12—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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere al uso de un compuesto de 2-ciano-pirimidina de la formula (1), en donde: R1, R2, R3 y X son como se definen en la memoria descriptiva y en las reivindicaciones, en forma libre o en forma de sal, y donde sea posible, en forma tautomérica, como un inhibidor de la actividad de la catepsina S. Reivindicacion 1: Una 2-ciano-pirimidina de la formula (1), R1 denota un radical de la formula (2), en donde A, E, y G, independientemente unos de otros, representan O, S, o CH2, con la condicion de que cuando menos uno de A y E represente CH2; T es O, S, o un enlace, si G es CH2, y T es un enlace si G es O o S; Ra, Rb, y Rc, independientemente uno de otros, representan hidrogeno o alquilo C1-4; s es 0, 1 o 2, t es 1, 2, 3, o 4, y p es 0, 1, o 2; R2 denota halogeno, alquilo C1-4, arilo insustituido o sustituido, heterociclilo de 5 o 6 miembros -C(O)NR4R5, -NHC(O)R4, o CH2NHC(O)R4, en donde: R4 representa: a) alquilo C1-7 que está insustituido o sustituido por halogeno; amino, el cual está mono- o di-sustituido por cicloalquilo C3-5 o alquilo C1-6, que en cada caso están insustituidos o mono-, di-, o tri-sustituidos por halogeno; heterociclilo alifático C4-8 insustituido o sustituido, que comprende cuando menos un átomo de nitrogeno; arilo insustituido o sustituido; hetarilo insustituido o sustituido; espiro[4.5]decano insustituido o sustituido, el cual comprende uno o dos heteroátomos seleccionados a partir de oxígeno, nitrogeno, y azufre; cicloalquilo C3-6 insustituido o sustituido; o 1-aza-bicicloalquiloC5-8; b) N-alquiloC1-4-piperidinilo o N-cicloalquiloC4-6-piperidinilo insustituido o sustituido; c) arilo sustituido o sustituido; d) cicloalquilo C3-6 insustituido o sustituido; o e) hetarilo de 5 o 6 miembros insustituido o sustituido que contiene un átomo de nitrogeno; y R5 representa hidrogeno o alquilo C1-4; o R4 y R5, junto con el nitrogeno con el que están unidos, representan heterociclilo alifático C4-8 insustituido o sustituido, que comprende cuando menos un átomo de nitrogeno; o R2 denota -N(R9)SO2R10; R9 representa hidrogeno o alquilo C1-4; y R10 representa alquilo C1-4, el cual está insustituido o sustituido por arilo; o R9 y R10 forman juntos un radical -(CRR')m-, en donde m es un entero desde e incluyendo 2 y hasta e incluyendo 5, y R y R' representan ambos, independientemente uno del otro, hidrogeno o alquilo C1-4; R3 denota hidrogeno, halogeno, fenilo, piridilo, que está insustituido o mono-, di-, o tri-sustituido por halogeno, Y-R6, o NR7R8, en donde: Y representa O, CH2, S, SO, SO2, o NRN, en donde RN denota hidrogeno o alquilo C1-4 que está insustituido o sustituido por alcoxilo C1-4; R6 representa alquilo C1-6, fenilo, nitrogeno de 5 o 6 miembros que contiene hetarilo-(CO2)q-, en donde q es un entero de 0 a 4, o heterociclilo alifático de 5 o 6 miembros-(CH2)n-, en donde n es un entero de 0 a 4 y la fraccion de heterociclilo comprende cuando menos un átomo de nitrogeno del anillo, cuyos radicales en cada caso pueden estar insustituidos o sustituidos; R7 y R8, junto con el nitrogeno con el que están unidos, representan heterociclilo alifático de 5 o 6 miembros insustituido o sustituido, en donde la fraccion de heterociclilo comprende cuando menos un átomo de nitrogeno; X denota O, HN, alquiloC1-4-N, S, SO, SO2, O(CH2)gNH, en donde g es 1 o 2, (CH2)h, en donde h es 1 o 2, o arilo que está insustituido o mono-, di-, o tri-sustituido por halogeno, alquilo C1-4, o alcoxilo C1-4; o un tautomero y/o sal de esta 2-ciano-pirimidina.
ARP050103494A 2004-08-17 2005-08-19 Compuestos y composiciones utiles como inhibidores de catepsina-s AR050786A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0418353.9A GB0418353D0 (en) 2004-08-17 2004-08-17 Organic compounds

Publications (1)

Publication Number Publication Date
AR050786A1 true AR050786A1 (es) 2006-11-22

Family

ID=33042203

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050103494A AR050786A1 (es) 2004-08-17 2005-08-19 Compuestos y composiciones utiles como inhibidores de catepsina-s

Country Status (16)

Country Link
US (1) US7704996B2 (es)
EP (1) EP1781623A1 (es)
JP (1) JP2008509959A (es)
KR (1) KR20070036183A (es)
CN (2) CN101035768A (es)
AR (1) AR050786A1 (es)
AU (1) AU2005274319A1 (es)
BR (1) BRPI0514383A (es)
CA (1) CA2575826A1 (es)
GB (1) GB0418353D0 (es)
GT (1) GT200500220A (es)
MX (1) MX2007001952A (es)
PE (1) PE20060647A1 (es)
RU (1) RU2007109650A (es)
TW (1) TW200621727A (es)
WO (1) WO2006018284A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007097720A2 (en) * 2006-02-21 2007-08-30 Agency For Science, Technology And Research Method and reagents for treating hepatic fibrosis and inflammation
EP2202228B1 (en) 2007-10-15 2014-12-10 Takeda Pharmaceutical Company Limited Amide compounds and use of the same
US20110230660A1 (en) * 2008-12-04 2011-09-22 Method for Preparing a Spiroindoline Method for preparing a spiroindoline and a precursor thereof
TWI402072B (zh) * 2010-10-19 2013-07-21 Lilly Co Eli 組織蛋白酶ｓ抑制劑化合物
WO2020201572A1 (en) 2019-04-05 2020-10-08 Université De Bretagne Occidentale Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0201976D0 (sv) * 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
GB0220187D0 (en) 2002-08-30 2002-10-09 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
EP1781623A1 (en) 2007-05-09
US7704996B2 (en) 2010-04-27
JP2008509959A (ja) 2008-04-03
CN101671310A (zh) 2010-03-17
CA2575826A1 (en) 2006-02-23
KR20070036183A (ko) 2007-04-02
CN101035768A (zh) 2007-09-12
TW200621727A (en) 2006-07-01
US20090048230A1 (en) 2009-02-19
PE20060647A1 (es) 2006-08-11
MX2007001952A (es) 2007-05-09
GB0418353D0 (en) 2004-09-22
GT200500220A (es) 2006-03-29
BRPI0514383A (pt) 2008-06-10
WO2006018284A1 (en) 2006-02-23
AU2005274319A1 (en) 2006-02-23
RU2007109650A (ru) 2008-09-27

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