CO4950618A1 - Inhibidores de proteasas - Google Patents

Inhibidores de proteasas

Info

Publication number
CO4950618A1
CO4950618A1 CO98024945A CO98024945A CO4950618A1 CO 4950618 A1 CO4950618 A1 CO 4950618A1 CO 98024945 A CO98024945 A CO 98024945A CO 98024945 A CO98024945 A CO 98024945A CO 4950618 A1 CO4950618 A1 CO 4950618A1
Authority
CO
Colombia
Prior art keywords
alkyl
het
alkenyl
formula
compound
Prior art date
Application number
CO98024945A
Other languages
English (en)
Inventor
Andrew D Gribble
Jason Witherington
Edward Fenwick Ashley
Robert W Marquis
Original Assignee
Smithkline Beecham Corp
Smithkline Beecham Plc
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 Smithkline Beecham Corp, Smithkline Beecham Plc filed Critical Smithkline Beecham Corp
Publication of CO4950618A1 publication Critical patent/CO4950618A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/99—Enzyme inactivation by chemical treatment
    • 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
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D307/32—Oxygen atoms
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06—Anabolic agents
    • 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
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/22—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/83—Oxygen atoms
    • 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
    • C07D307/86—Benzo [b] furans; Hydrogenated benzo [b] furans with an oxygen atom directly attached in position 7
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Genetics & Genomics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto según la fórmula (I):en la que:R1 es R", R"C(O), R"C(S), R"SO2 , R"OC(O), R"R´NC(O), o R"OC(O)NR´CH(R6 )C(O);R2 es H, alquilo C1 -C6 , alquenilo C2 -C6 , Ar-alquilo C0 -C6 , o Het-alquilo C0 -C6 ; R3 es H, alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo C0 -C6 , o Het-alquilo C0 -C6 ;R4 es H, alquilo C1 -C6 , alquenilo C2 -C6 , Ar-alquilo C0 -C6 , o Het-alquilo C0 -C6 ;R5 , en cada caso, es independientemente H, alquilo C1 -C6 , alquenilo C2 -C6 , Ar-alquilo C0 -C6 , o Het-alquilo C0 -C6 ;R6 es H, alquilo C1 -C6 , alquenilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo C0 -C6 o Het-alquilo C0 -C6 ;R´ es H, alquilo C1 -C6 , alquenilo C2 -C6 , Ar-alquilo C0 -C6 , o Het-alquilo C0 -C6 ;R" es alquilo C1 -C6 , Ar-alquilo C0 -C6 , Het-alquilo C0 -C6 , Ar-alquenilo C2 -C6 , o Het-alquenilo C2 -C6 ;X es O o S; yn es 1, 2 ó 3;o una de sus sales farmacéuticamente aceptables.3Un procedimiento para preparar un compuesto defórmula (I) según la reivindicación 1, procedimiento que comprende:(i) hacer reaccionar un compuesto de fórmula (III): - 2 -en la que R1 , R2 , R3 , R4 , R5 y n son como se definen para la fórmula (I) de la reivindicación 1, con todos sus grupos funcionales reactivos protegidos, con un agente oxidante; o(ii) descarboxilar un compuesto de fórmula (IV):en la que R1 , R2 , R3 , R4 , R5 y n son como se definen para la fórmula (I) de la reivindicación 1, con todos sus grupos funcionales reactivos protegidos; o(iii) hacer reaccionar un compuesto de fórmula (V):en la que R1 , R3 , R4 , R5 y n son como se definen para la fórmula (I) de la reivindicación 1, con todos sus grupos funcionales reactivos protegidos, con un ácido;y, después de ello, eliminar cualquier grupo protector y opcionalmente formar una sal farmacéuticamente aceptable.
CO98024945A 1997-05-06 1998-05-06 Inhibidores de proteasas CO4950618A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4575897P 1997-05-06 1997-05-06

Publications (1)

Publication Number Publication Date
CO4950618A1 true CO4950618A1 (es) 2000-09-01

Family

ID=21939723

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98024945A CO4950618A1 (es) 1997-05-06 1998-05-06 Inhibidores de proteasas

Country Status (19)

Country Link
EP (1) EP1003846A4 (es)
JP (1) JP2001525804A (es)
KR (1) KR20010012256A (es)
CN (1) CN1255161A (es)
AR (1) AR013079A1 (es)
AU (1) AU7562598A (es)
BR (1) BR9809306A (es)
CA (1) CA2288868A1 (es)
CO (1) CO4950618A1 (es)
HU (1) HUP0002247A3 (es)
IL (1) IL132088A0 (es)
NO (1) NO995434D0 (es)
NZ (1) NZ337889A (es)
PE (1) PE71599A1 (es)
PL (1) PL336856A1 (es)
TR (1) TR199902766T2 (es)
UY (1) UY25143A1 (es)
WO (1) WO1998050533A1 (es)
ZA (1) ZA983762B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5150165A1 (es) * 1998-11-13 2002-04-29 Smithkline Beecham Plc Inhibidores de proteasa: tipo catepsina k
DZ3083A1 (fr) * 1999-02-19 2004-06-02 Smithkline Beecham Corp Composés nouveaux inhibiteurs de protéases, procédé pour leur préparation et compositions pharmaceutiques les conentant.
GB9911417D0 (en) * 1999-05-18 1999-07-14 Peptide Therapeutics Ltd Furanone derivatives as inhibitors of cathepsin s
US6596715B1 (en) * 1999-11-10 2003-07-22 Smithkline Beecham Corporation Protease inhibitors
US20040024000A1 (en) * 2000-10-19 2004-02-05 Rajeshwar Singh Dihydropyrimidine derivatives as cysteine protease inhibitors
EP1345931A2 (en) * 2000-11-17 2003-09-24 Medivir UK Ltd Cysteine protease inhibitors
DE60118793T2 (de) * 2000-11-17 2007-04-26 Medivir Ab Cystein protease inhibitoren
US7132449B2 (en) 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
IL156776A0 (en) * 2001-01-17 2004-02-08 Amura Therapeutics Ltd Inhibitors of cruzipain and other cysteine proteases
NZ526914A (en) * 2001-01-17 2005-02-25 Amura Therapeutics Ltd Cyclic 2-carbonylaminoketones as inhibitors of cruzipain and other cysteine proteases
NZ526913A (en) * 2001-01-17 2004-12-24 Amura Therapeutics Ltd Inhibitors of cruzipain and other cysteine proteases
WO2003037892A1 (en) * 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
AU2003255711B2 (en) * 2002-07-16 2008-11-13 Amura Therapeutics Limited Biologically active compounds
KR100962972B1 (ko) 2002-07-26 2010-06-09 주식회사유한양행 1-페닐피페리딘-3-온 유도체 및 그의 제조방법
RU2006106920A (ru) 2003-08-06 2007-09-20 Синомикс Инк. (Us) Гетеро-олигомерные вкусовые рецепторы t1r, клеточные линии, которые экспрессируют указанные рецепторы и вкусовые соединения
AU2016206281B2 (en) * 2003-08-06 2017-11-30 Senomyx, Inc. Novel flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof
CA2552739A1 (en) * 2004-01-08 2005-07-21 Medivir Ab Cysteine protease inhibitors
CN101287727A (zh) * 2005-08-17 2008-10-15 先灵公司 新的高亲和力喹啉基激酶配体
GB0614042D0 (en) 2006-07-14 2006-08-23 Amura Therapeutics Ltd Compounds
US8367709B2 (en) * 2007-06-13 2013-02-05 Bristol-Myers Squibb Company Dipeptide analogs as coagulation factor inhibitors
US7893067B2 (en) 2007-06-27 2011-02-22 Medivir Ab Cysteine protease inhibitors
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
GB0817424D0 (en) * 2008-09-24 2008-10-29 Medivir Ab Protease inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3190431B2 (ja) * 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
JPH05140063A (ja) * 1991-11-19 1993-06-08 Suntory Ltd ジペプチド誘導体及びそれを有効成分とする骨疾患の予防及び治療剤
CA2111930A1 (en) * 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
JP2848232B2 (ja) * 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
JP3599287B2 (ja) * 1993-04-28 2004-12-08 三菱化学株式会社 スルホンアミド誘導体
US5403952A (en) * 1993-10-08 1995-04-04 Merck & Co., Inc. Substituted cyclic derivatives as novel antidegenerative agents
PL328877A1 (en) * 1995-10-30 1999-03-01 Smithkline Beecham Corp Method of inhibiting cathepsin k
TW448172B (en) * 1996-03-08 2001-08-01 Pharmacia & Upjohn Co Llc Novel hydroxamic acid derivatives useful for the treatment of diseases related to connective tissue degradation
WO1998004539A1 (fr) * 1996-07-29 1998-02-05 Mitsubishi Chemical Corporation Derives heterocycliques oxygenes

Also Published As

Publication number Publication date
NO995434L (no) 1999-11-05
WO1998050533A1 (en) 1998-11-12
ZA983762B (en) 1998-11-06
KR20010012256A (ko) 2001-02-15
UY25143A1 (es) 1998-11-27
TR199902766T2 (xx) 2000-02-21
EP1003846A1 (en) 2000-05-31
CA2288868A1 (en) 1998-11-12
BR9809306A (pt) 2000-07-04
IL132088A0 (en) 2001-03-19
HUP0002247A3 (en) 2003-01-28
NO995434D0 (no) 1999-11-05
AU7562598A (en) 1998-11-27
AR013079A1 (es) 2000-12-13
CN1255161A (zh) 2000-05-31
EP1003846A4 (en) 2002-11-13
HUP0002247A2 (hu) 2001-05-28
PE71599A1 (es) 1999-09-15
NZ337889A (en) 2001-09-28
PL336856A1 (en) 2000-07-17
JP2001525804A (ja) 2001-12-11

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