CO5040090A1 - PROTEASE INHIBITORS - Google Patents

PROTEASE INHIBITORS

Info

Publication number
CO5040090A1
CO5040090A1 CO99036559A CO99036559A CO5040090A1 CO 5040090 A1 CO5040090 A1 CO 5040090A1 CO 99036559 A CO99036559 A CO 99036559A CO 99036559 A CO99036559 A CO 99036559A CO 5040090 A1 CO5040090 A1 CO 5040090A1
Authority
CO
Colombia
Prior art keywords
alkyl
group
cycloalkyl
het
alkynyl
Prior art date
Application number
CO99036559A
Other languages
Spanish (es)
Inventor
Andrew D Gribble
Jr Robert Wells Marquis
Jason Witherington
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 CO5040090A1 publication Critical patent/CO5040090A1/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/24—Oxygen or sulfur atoms
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Cosmetics (AREA)

Abstract

Un compuesto según la fórmula (I):en la que:X se selecciona del grupo formado por oxígeno, azufre, SO y SO2 ;Y se selecciona del grupo formado por H2 y oxígeno; donde, si Y es H2 , entonces el enlace ----- representa dos enlaces sencillos y donde si U es O, entonces el enlace ------ representa un enlace doble;R1 se selecciona del grupo formado por hidrógeno,alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo CO -C6 , Het-alquilo C0 -C6 , (CH2 )0-6 CO2 R", y (CH2 )O-6 Ar;R" se selecciona del grupo formado por hidrógeno,alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo C0 -C6 y Het-alquilo C0 -C6 ;R2 se selecciona del grupo formado por H, alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo CO -C6 , Ar-alquilo CO -C6 y Het-alquilo CO -C6 ;R3 se selecciona del grupo formado por H, alquilo C1 -C6 , alquenilo C2 -C6 , alquinilo C2 -C6 , cicloalquil C3 -C6 -alquilo C0 -C6 , Ar-alquilo C0 -C6 y Het-alquilo CO -C6 ;alquilo C1 -C6 se selecciona del grupo formado pormetilo, etilo, n-propilo, isopropilo, n-butilo, isobutilo, t-butilo, pentilo, n-pentilo, isopentilo, neopentilo y hexilo sustituidos o no sustituidos, y los isomeros alifáticos de los mismos; cicloalquilo C3 -C6 se selecciona del grupo formado por ciclopropano, ciclobutano, ciclopentano y ciclohexano sustituidos y no sustituidos; ...A compound according to formula (I): in which: X is selected from the group consisting of oxygen, sulfur, SO and SO2; Y is selected from the group consisting of H2 and oxygen; where, if Y is H2, then the bond ----- represents two single bonds and where if U is O, then the bond ------ represents a double bond; R1 is selected from the group consisting of hydrogen, alkyl C1-C6, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl-C0-C6 alkyl, Ar-CO-C6 alkyl, Het-C0-C6 alkyl, (CH2) 0-6 CO2 R ", and ( CH2) O-6 Ar; R "is selected from the group consisting of hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl-C0-C6 alkyl, Ar-C0-C6 alkyl and Het -C0-C6 alkyl; R2 is selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl-CO-C6 alkyl, Ar-CO-C6 alkyl and Het-alkyl CO-C6; R3 is selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl-C0-C6 alkyl, Ar-C0-C6 alkyl and Het-CO-alkyl C6; C1-C6 alkyl is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobut substituted or unsubstituted yl, t-butyl, pentyl, n-pentyl, isopentyl, neopentyl and hexyl, and the aliphatic isomers thereof; C3-C6 cycloalkyl is selected from the group consisting of substituted and unsubstituted cyclopropane, cyclobutane, cyclopentane and cyclohexane; ...

CO99036559A 1998-06-12 1999-06-10 PROTEASE INHIBITORS CO5040090A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US8905698P 1998-06-12 1998-06-12

Publications (1)

Publication Number Publication Date
CO5040090A1 true CO5040090A1 (en) 2001-05-29

Family

ID=22215426

Family Applications (1)

Application Number Title Priority Date Filing Date
CO99036559A CO5040090A1 (en) 1998-06-12 1999-06-10 PROTEASE INHIBITORS

Country Status (10)

Country Link
EP (1) EP1086083A4 (en)
JP (1) JP2002517485A (en)
AR (1) AR018652A1 (en)
AU (1) AU4564499A (en)
CA (1) CA2334652A1 (en)
CO (1) CO5040090A1 (en)
DZ (1) DZ2815A1 (en)
MA (1) MA24877A1 (en)
PE (1) PE20000725A1 (en)
WO (1) WO1999064399A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
US6534498B1 (en) 1999-11-10 2003-03-18 Smithkline Beecham Corporation Protease inhibitors
JP2003513972A (en) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
WO2001034599A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EA005893B1 (en) 2000-03-21 2005-06-30 Смитклайн Бичам Корпорейшн Protease inhibitors
US20020156063A1 (en) * 2001-04-06 2002-10-24 Setti Eduardo L. Arylacetamido-ketobenzoxazole as cysteine protease inhibitors
WO2003062192A1 (en) 2002-01-17 2003-07-31 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k 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
CN117940420A (en) 2021-09-14 2024-04-26 勃林格殷格翰国际有限公司 3-Phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives and their use as pharmaceuticals

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2175218A1 (en) * 1993-11-09 1995-05-18 Gregori J. Morriello Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
US5770573A (en) * 1993-12-06 1998-06-23 Cytel Corporation CS-1 peptidomimetics, compositions and methods of using the same
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase

Also Published As

Publication number Publication date
AR018652A1 (en) 2001-11-28
PE20000725A1 (en) 2000-09-28
DZ2815A1 (en) 2003-12-01
MA24877A1 (en) 1999-12-31
WO1999064399A1 (en) 1999-12-16
EP1086083A4 (en) 2001-09-26
EP1086083A1 (en) 2001-03-28
JP2002517485A (en) 2002-06-18
AU4564499A (en) 1999-12-30
CA2334652A1 (en) 1999-12-16

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