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)
  • 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

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) 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)

* 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
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
EP1003846A1 (en) 2000-05-31
CN1255161A (zh) 2000-05-31
CA2288868A1 (en) 1998-11-12
UY25143A1 (es) 1998-11-27
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

Similar Documents

Publication Publication Date Title
CO4950618A1 (es) Inhibidores de proteasas
PT91927A (pt) Processo para a preparacao de novos inibidores de peptidase
AR041729A1 (es) Compuesto de cefemo
ES2058091T3 (es) Derivados de acido 3-pirrolidiniltio-1-azabiciclo(3.2.0)hept-2-eno-2-carboxilico y procedimientos para su preparacion.
IE811566L (en) Steel articles protected against corrosion.
AR017164A1 (es) Derivados de la benzamidina, un procedimiento para prepararlos, el empleo de los mismos para preparar un medicamento, los medicamentos y laspreparaciones farmaceuticas que contienen estos derivados de la benzamidina, y un procedimiento para obtener estas preparaciones farmaceuticas.
AR045768A1 (es) Compuestos de cefem y sus sales farmaceuticamente aceptables
MXPA03000547A (es) Uso de derivados de amidas de acido valproico y de acido 2-valproenico, para el tratamiento de manias en trastornos bipolares.
HUP9702403A2 (hu) Eljárás vírusellenes proteáz inhibitorok intermedierjeinek előállítására
ATE141606T1 (de) Cephemverbindungen und verfahren zu ihrer herstellung
PT92540A (pt) Processo para a preparacao de derivados de anfotericina b
DK1347965T3 (da) Hidtil ukendte desloratidinsalte, fremgangsmåde til syntese deraf samt farmaceutiske præparater deraf
PT1292597E (pt) Derivados de podofilotoxina carbamato e tiocarbamato processo para a sua preparacao e as composicoes farmaceuticas que os contem
DK0619817T3 (da) Hidtil ukendte farmaceutisk aktive flaviliumforbindelser
AU1735397A (en) Pyridonecarboxylic acid derivatives and intermediates for the synthesis thereo
YU46183B (sh) Postupak za dobijanje peptida
AR010366A1 (es) Proceso para la produccion de compuestos de amina utiles como medicamentos.
AR004401A1 (es) Derivados de la tirosina, procedimiento para prepararlos y preparaciones farmaceuticas que los contienen.
MY155266A (en) Selective thrombin inhibitors