PE20000725A1 - ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORS - Google Patents

ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORS

Info

Publication number
PE20000725A1
PE20000725A1 PE1999000518A PE00051899A PE20000725A1 PE 20000725 A1 PE20000725 A1 PE 20000725A1 PE 1999000518 A PE1999000518 A PE 1999000518A PE 00051899 A PE00051899 A PE 00051899A PE 20000725 A1 PE20000725 A1 PE 20000725A1
Authority
PE
Peru
Prior art keywords
alkyl
compounds
het
alcoxypyrrolidinone
preferred
Prior art date
Application number
PE1999000518A
Other languages
Spanish (es)
Inventor
Andrew D Gribble
Ashley E Fenwick
Marquis
Jason Witherington
Original Assignee
Smithkline Beecham Plc
Smithkline Beecham Corp
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 Plc, Smithkline Beecham Corp filed Critical Smithkline Beecham Plc
Publication of PE20000725A1 publication Critical patent/PE20000725A1/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

SE REFIERE A COMPUESTOS ALCOXIPIRROLIDINONA DE FORMULA I, DONDE X ES O, S, SO, SO2; Y ES H2, O; R1 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, (CH2)(0-6)CO2R", DE PREFERENCIA GRUPO a, b; R" ES H, ALQUILO C1-C6, ALQUENILO C2-C6, Ar-ALQUILO C0-C6, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, HET-ALQUILO C0-C6, DE PREFERENCIA ISOBUTILO, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, DE PREFERENCIA GRUPO c, d; Ar ES FENILO, NAFTILO, OPCIONALMENTE SUSTITUIDO CON Ph-ALQUILO C0-C6, HET-ALQUILO C0-C6, O(CH2)(1-6)NR`R', ENTRE OTROS; R' ES H, ALQUILO C1-C6, ENTRE OTROS; HET ES UN ANILLO HETEROCICLICO BICICLICO DE 7-10 MIEMBROS, ANILLO MONICICLICO DE 5-7 MIEMBROS OPCIONALMENTE SUSTITUIDO CON OR', N(R')2, SR'CF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 3-BENCILOXI-1-(N-CARBOBENCILOXI-L-LEUCINIL)PIRROLIDIN-4-ONA, 1-[2-(BENCILOXICARBONILAMINO)-4-METILPENTIL]-3-BENCILTIO-4-HIDROXIPIRROLIDINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA CONVERTIR 3-BENCILOXI-4-HIDROXI-1-(N-CARBOBENCILOXI-L-LEUCINIL)PIRROLIDONA, ENTRE OTROS EN UN COMPUESTO DE FORMULA I. EL COMPUESTO I ES UN INHIBIDOR DE CISTEINA-PROTEASAS (CATEPSINA K) POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DE ENFERMEDADES RELACIONADAS CON UNA EXCESIVA DEGRADACION DE HUESO O CARTILAGO COMO OSTEOPOROSIS, PERIODONTITIS, ARTRITIS, ENFERMEDAD GINGIVAL O PERIODONTALREFERS TO ALCOXYPYRROLIDINONE COMPOUNDS OF FORMULA I, WHERE X IS O, S, SO, SO2; Y IS H2, O; R1 IS H, C1-C6 ALKYL, C2-C6 ALKENYL, (CH2) (0-6) CO2R ", PREFERRED GROUP a, b; R" IS H, C1-C6 ALKYL, C2-C6 ALKENYL, Ar-ALKYL C0-C6, AMONG OTHERS; R2 IS H, C1-C6 ALKYL, HET-C0-C6 ALKYL, PREFERRED ISOBUTYL, AMONG OTHERS; R3 IS H, C1-C6 ALKYL, C2-C6 ALKYL, C2-C6 ALKYNYL, PREFERRED GROUP c, d; Ar IS PHENYL, NAPHTHYL, OPTIONALLY SUBSTITUTED WITH Ph-ALKYL C0-C6, HET-ALKYL C0-C6, O (CH2) (1-6) NR`R ', AMONG OTHERS; R 'IS H, C1-C6 ALKYL, AMONG OTHERS; HET IS A 7-10 MEMBER HETERO CYCLIC BICYCLE RING, 5-7 MEMBER MONICYCLE RING OPTIONALLY SUBSTITUTED WITH OR ', N (R') 2, SR'CF3, AMONG OTHERS. PREFERRED COMPOUNDS ARE 3-BENZYLLOXY-1- (N-CARBOBENZYLOXY-L-LEUKINYL) PYRROLIDIN-4-ONA, 1- [2- (BENZYLOXYCARBONYLAMINE) -4-METHYLPENTIL] -3-BENZYLTHI-4-HYDROXYPYRROLIDINE, BETWEEN. IT ALSO REFERS TO A PROCEDURE TO CONVERT 3-BENZYLOXY-4-HYDROXY-1- (N-CARBOBENZYLOXY-L-LEUKINYL) PYRROLIDONE, AMONG OTHERS, INTO A COMPOUND OF FORMULA I. COMPOUND I IS A CYSTEIN PROTEIN-PROTEIN INHIBITOR K) SO IT MAY BE USEFUL FOR THE TREATMENT OF DISEASES RELATED TO EXCESSIVE DEGRADATION OF THE BONE OR CARTILAGE SUCH AS OSTEOPOROSIS, PERIODONTITIS, ARTHRITIS, GINGIVAL OR PERIODONTAL DISEASE

PE1999000518A 1998-06-12 1999-06-11 ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORS PE20000725A1 (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
PE20000725A1 true PE20000725A1 (en) 2000-09-28

Family

ID=22215426

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1999000518A PE20000725A1 (en) 1998-06-12 1999-06-11 ALCOXYPYRROLIDINONE COMPOUNDS AS 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
DZ2815A1 (en) 2003-12-01
CO5040090A1 (en) 2001-05-29
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

Similar Documents

Publication Publication Date Title
PE20001340A1 (en) 4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS
PE20060777A1 (en) INDOLINONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES
PE20010696A1 (en) ADENOSINE A3 RECEPTOR AGONIST COMPOUNDS FOR THE TREATMENT OF ISCHEMIA
PE2799A1 (en) LACTAMS AND HETERO-CYCLIC IMIDES OF ARALQUILO AND ARALQUILIDENO
DZ3482A1 (en) SECRETAGOGUES OF THE GROWTH HORMONE
PE71599A1 (en) PROTEASE INHIBITORS
BRPI0411268A (en) process for the preparation of a substituted 3-aryl butyl amine compound
EA200400815A1 (en) CONTROLLED SYNTHESIS OF ZIPRAZIDONA AND ITS COMPOSITIONS
IS6859A (en) Crystalline form of atorvastatin
CY1107228T1 (en) Sodium channel blockers
HUP0203186A2 (en) Resolution of intermediates in the synthesis of substantially pure bicalutamide
PE20040672A1 (en) DERIVATIVES OF PHENYL OR HETEROARYL AMINO ALKANE
NO20013220L (en) Thrombin inhibitors
PE20050012A1 (en) BENZOPYRANE COMPOUNDS AS CYCLOOXYGENASE-2 INHIBITORS
PE20000725A1 (en) ALCOXYPYRROLIDINONE COMPOUNDS AS PROTEASE INHIBITORS
BR0317005A (en) Process for the preparation of optically pure active compounds
DK0657422T3 (en) Naphthyloxyacetic acid derivatives such as PEG2 agonists and antagonists
PE20040531A1 (en) DERIVATIVES OF ISOINDOLONE, PREPARATION PROCESS, INTERMEDIATE COMPOUNDS OF THIS PROCESS AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM
PE20090548A1 (en) AZA-BICYCLOHEXANE COMPOUNDS AS THROMBIN INHIBITORS
DE60330758D1 (en) CERTAIN PHARMACEUTICALLY VALUABLE SUBSTITUTED AMINO ALKYL HETEROCYCLES
AR031356A1 (en) LACTA MICO COMPOUND
NO20002589D0 (en) Bifenylamidinderivater
PE20001237A1 (en) PROTEASE INHIBITORS
AR053560A1 (en) ANTIBACTERIAL COMPOUNDS OF 3,3 'DIALCOXI-2,2' -DIHIDROXI -1,1 '-BIFENILO 5,5' DISUSTITUTED AND RELATED METHODS
PE20011374A1 (en) 4-AMINO-AZEPAN-3-ONA AS PROTEASE INHIBITORS

Legal Events

Date Code Title Description
FC Refusal