UY25143A1 - Procedimiento para la preparacion de inhibidores de proteasas. - Google Patents

Procedimiento para la preparacion de inhibidores de proteasas.

Info

Publication number
UY25143A1
UY25143A1 UY25143A UY25143A UY25143A1 UY 25143 A1 UY25143 A1 UY 25143A1 UY 25143 A UY25143 A UY 25143A UY 25143 A UY25143 A UY 25143A UY 25143 A1 UY25143 A1 UY 25143A1
Authority
UY
Uruguay
Prior art keywords
alkyl
het
alkenyl
cysteine proteases
inhibitors
Prior art date
Application number
UY25143A
Other languages
English (en)
Inventor
F Veber Daniel
D Gribble Andrew
Witherington J
E Fenwick Ashley
Robert Marquis
Original Assignee
Smithkline Beecham Corp Y Smithkline Beecham P L C
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 Y Smithkline Beecham P L C filed Critical Smithkline Beecham Corp Y Smithkline Beecham P L C
Publication of UY25143A1 publication Critical patent/UY25143A1/es

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Classifications

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

Abstract

Procedimiento para preparar compuestos derivados n-sustituidos de 4-amino-tetrahidrofuran-3-ona, 4-aminotetrahidropiran-3-ona y 4-aminotetrahidrotiofen-3-ona utilizados como inhibidores de cisteína proteasas, particularmente catepsina k. Son útiles en el tratamiento de enfermedades caracterizadas por la pérdida excesiva de hueso o cartílago, por ejemplo osteoporosis, periodontitis y artritis, en las que están implicadas cisteína proteasas. Es un compuesto de fórmula l en que: R1 es R'', R''C(O), R''C(S), R''OC(O), CH(R6)C(O); R2 es H, alquilo, alquenilo, Ar-alquilo, o Het-alquilo; R3 es H, alquilo, alquenilo, alquinilo, cicloalquil, Het-alquilo; R4 es H, alquilo, alquenilo, Ar-alquilo, Het-alquilo; R5 en cada caso, es independientemente H, alquilo, alquenilo, Ar-alquilo, Het-alquilo; X es O o S; y nes 1,2 o 3; o una sal farmacéuticamente aceptables, que son inhibidores de cisteína proteasas. Ejemplo de un compuesto de fórmula l sería: 4-(R, S)-Amino-N-[(3,4-diclorobenzoil)-S-leucina]-tetrahidrofuran-3-ona.
UY25143A 1997-05-06 1998-08-17 Procedimiento para la preparacion de inhibidores de proteasas. UY25143A1 (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
UY25143A1 true UY25143A1 (es) 1998-11-27

Family

ID=21939723

Family Applications (1)

Application Number Title Priority Date Filing Date
UY25143A UY25143A1 (es) 1997-05-06 1998-08-17 Procedimiento para la preparacion de 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) NO995434L (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
AU1588901A (en) * 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
US20040024000A1 (en) * 2000-10-19 2004-02-05 Rajeshwar Singh Dihydropyrimidine derivatives as cysteine protease inhibitors
JP2004520439A (ja) * 2000-11-17 2004-07-08 メディヴィル・アクチボラグ システインプロテアーゼインヒビター
EP1345931A2 (en) * 2000-11-17 2003-09-24 Medivir UK Ltd Cysteine protease inhibitors
US7132449B2 (en) 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
EP1358176A2 (en) * 2001-01-17 2003-11-05 Amura Therapeutics Limited 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
WO2002057270A1 (en) * 2001-01-17 2002-07-25 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
JP2005508979A (ja) * 2001-10-29 2005-04-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド システインプロテアーゼの可逆性インヒビターとして有用な化合物
JP2006504651A (ja) * 2002-07-16 2006-02-09 アミュラ テラピューティクス リミテッド 生物活性化合物
KR100962972B1 (ko) 2002-07-26 2010-06-09 주식회사유한양행 1-페닐피페리딘-3-온 유도체 및 그의 제조방법
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
EP3431464A3 (en) 2003-08-06 2019-07-31 Senomyx Inc. Novel flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof
AU2005203972B2 (en) 2004-01-08 2010-11-18 Medivir Ab Cysteine protease inhibitors
JP4976394B2 (ja) * 2005-08-17 2012-07-18 シェーリング コーポレイション 新規な高親和性のキノリンベースのキナーゼリガンド
GB0614042D0 (en) 2006-07-14 2006-08-23 Amura Therapeutics Ltd Compounds
CL2008001724A1 (es) * 2007-06-13 2008-08-08 Bristol Myers Squibb Co Compuestos derivados de analogos dipeptidos, inhibidores del factor de coagulacion; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de un trastorno tromboembolico, infarto de miocardio, trombosis, ate
US7893067B2 (en) 2007-06-27 2011-02-22 Medivir Ab Cysteine protease inhibitors
EP2240491B1 (en) 2008-01-09 2015-07-15 Amura Therapeutics Limited TETRAHYDROFURO(2,3-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)

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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
CN1177293A (zh) * 1995-10-30 1998-03-25 史密丝克莱恩比彻姆公司 抑制组织蛋白酶k的方法
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
BR9809306A (pt) 2000-07-04
PL336856A1 (en) 2000-07-17
NO995434D0 (no) 1999-11-05
AR013079A1 (es) 2000-12-13
EP1003846A4 (en) 2002-11-13
CO4950618A1 (es) 2000-09-01
EP1003846A1 (en) 2000-05-31
CN1255161A (zh) 2000-05-31
CA2288868A1 (en) 1998-11-12
PE71599A1 (es) 1999-09-15
JP2001525804A (ja) 2001-12-11
WO1998050533A1 (en) 1998-11-12
NZ337889A (en) 2001-09-28
IL132088A0 (en) 2001-03-19
KR20010012256A (ko) 2001-02-15
ZA983762B (en) 1998-11-06
NO995434L (no) 1999-11-05
TR199902766T2 (xx) 2000-02-21
AU7562598A (en) 1998-11-27
HUP0002247A2 (hu) 2001-05-28
HUP0002247A3 (en) 2003-01-28

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Effective date: 20001213