PE20001486A1 - ANNULAR ETEREO COMPOUNDS FROM 7 TO 14 MEMBERS AS PROTEASE INHIBITORS - Google Patents

ANNULAR ETEREO COMPOUNDS FROM 7 TO 14 MEMBERS AS PROTEASE INHIBITORS

Info

Publication number
PE20001486A1
PE20001486A1 PE2000000128A PE0001282000A PE20001486A1 PE 20001486 A1 PE20001486 A1 PE 20001486A1 PE 2000000128 A PE2000000128 A PE 2000000128A PE 0001282000 A PE0001282000 A PE 0001282000A PE 20001486 A1 PE20001486 A1 PE 20001486A1
Authority
PE
Peru
Prior art keywords
alkyl
het
compounds
cycloalkyl
etereo
Prior art date
Application number
PE2000000128A
Other languages
Spanish (es)
Inventor
Wells Marquis Robert
Frank Veber Daniel
Original Assignee
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 Corp filed Critical Smithkline Beecham Corp
Publication of PE20001486A1 publication Critical patent/PE20001486A1/en

Links

Classifications

    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • C07D313/16—Eight-membered rings
    • C07D313/18—Eight-membered rings not condensed with other rings
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS ETER ANULAR DE 7-14 MIEMBROS DE FORMULA I, DONDE A ES CO, CH(OH); R1 ES R3-N(R`)-C(R2)-C(=O)-; R' ES H, ALQUILO C1-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R'' ES H, ALQUILO C1-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R''' ES H, ALQUILO C1-C6, CICLOALQUIL C3-C6-ALQUILO C0-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R2 ES H, ALQUENILO C2-C6, ALQUINILO C2-C6, HET, Ar, ALQUILO C1-C6 CON OR6, R6NC(O)OR5, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, CICLOALQUIL C3-C6-ALQUILO C0-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6, R4C(O)-, R4R7NC(O)-, ENTRE OTROS; R4 ES ALQUILO C1-C6, CICLOALQUIL C3-C6-ALQUILO C0-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R5 ES H, ALQUILO C1-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; R6 Y R7 SON H, ALQUILO C1-C6, Ar-ALQUILO C0-C6, HET-ALQUILO C0-C6; M ES HC=CH, H2C-CH2, H(OR2)C-C(OR2)H, H(OR2)C-CH2, H(NR2H)C-C(NR2H)H, ENTRE OTROS; n ES 1-7; l ES 0-1. SON COMPUESTOS PREFERIDOS [(S)-3-METIL-1-(3-OXO-3,4,5,8-TETRAHIDRO-2H-OXOCIN-4-ILCARBAMOIL)-BUTIL]-AMIDA DE ACIDO NAFTILENO-2-CARBOXILICO; [(S)-3-METIL-1((S)-3-OXO-3,4,5,8-TETRAHIDRO-2H-OXOCIN-4-ILCARBAMOIL)-BUTIL]-AMIDA DE ACIDO BENZO[b]TIOFEN-2-CARBOXILICO, ENTRE OTROS. EL COMPUESTO DE FORMULA I ES UN INHIBIDOR DE CISTEINA Y SERINA PROTEASA Y PUEDE SER UTIL PARA EL TRATAMIENTO OSTEOPOROSIS, PERIODONTITIS, ARTRITIS, GINGIVITIS, OSTEOARTRITISREFERS TO 7-14 MEMBER RING ETHER COMPOUNDS OF FORMULA I, WHERE A IS CO, CH (OH); R1 IS R3-N (R`) -C (R2) -C (= O) -; R 'IS H, C1-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; R '' IS H, C1-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; R '' 'IS H, C1-C6 ALKYL, C3-C6 CYCLOALKYL-C0-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; R2 IS H, C2-C6 ALKENYL, C2-C6 ALKYNYL, HET, Ar, C1-C6 ALKYL WITH OR6, R6NC (O) OR5, AMONG OTHERS; R3 IS H, C1-C6 ALKYL, C3-C6 CYCLOALKYL-C0-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL, R4C (O) -, R4R7NC (O) -, AMONG OTHERS; R4 IS C1-C6 ALKYL, C3-C6 CYCLOALKYL-C0-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; R5 IS H, C1-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; R6 AND R7 ARE H, C1-C6 ALKYL, Ar-C0-C6 ALKYL, HET-C0-C6 ALKYL; M IS HC = CH, H2C-CH2, H (OR2) C-C (OR2) H, H (OR2) C-CH2, H (NR2H) C-C (NR2H) H, AMONG OTHERS; n IS 1-7; l IS 0-1. PREFERRED COMPOUNDS ARE [(S) -3-METHYL-1- (3-OXO-3,4,5,8-TETRAHYDRO-2H-OXOCIN-4-ILCARBAMOYL) -BUTYL] -NAPHTHYLENE-2-CARBOXYL ACID AMIDE; [(S) -3-METHYL-1 ((S) -3-OXO-3,4,5,8-TETRAHYDRO-2H-OXOCIN-4-ILCARBAMOYL) -BUTIL] -BENZO [b] THIOFEN- ACID AMIDE- 2-CARBOXYL, AMONG OTHERS. THE FORMULA I COMPOUND IS AN INHIBITOR OF CYSTEINE AND SERINE PROTEASE AND MAY BE USEFUL FOR THE TREATMENT OF OSTEOPOROSIS, PERIODONTITIS, ARTHRITIS, GINGIVITIS, OSTEOARTHRITIS

PE2000000128A 1999-02-19 2000-02-18 ANNULAR ETEREO COMPOUNDS FROM 7 TO 14 MEMBERS AS PROTEASE INHIBITORS PE20001486A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12069999P 1999-02-19 1999-02-19

Publications (1)

Publication Number Publication Date
PE20001486A1 true PE20001486A1 (en) 2001-02-08

Family

ID=22392011

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000128A PE20001486A1 (en) 1999-02-19 2000-02-18 ANNULAR ETEREO COMPOUNDS FROM 7 TO 14 MEMBERS AS PROTEASE INHIBITORS

Country Status (8)

Country Link
EP (1) EP1153022A4 (en)
JP (1) JP2002537297A (en)
AU (1) AU3235100A (en)
CO (1) CO5271679A1 (en)
DZ (1) DZ3083A1 (en)
HK (1) HK1042695A1 (en)
PE (1) PE20001486A1 (en)
WO (1) WO2000049011A1 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7168084B1 (en) 1992-12-09 2007-01-23 Sedna Patent Services, Llc Method and apparatus for targeting virtual objects
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
WO2001034599A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034600A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
US6534498B1 (en) 1999-11-10 2003-03-18 Smithkline Beecham Corporation Protease inhibitors
AU2001243441B2 (en) 2000-03-21 2004-11-25 Smithkline Beecham Corporation Protease inhibitors
EP1358183B1 (en) * 2000-11-17 2006-04-12 Medivir Ab Cysteine protease inhibitors
IL155961A0 (en) * 2000-11-17 2003-12-23 Medivir Uk Ltd Cysteine protease inhibitors
ATE338803T1 (en) * 2003-05-27 2006-09-15 Merck Patent Gmbh PYRANDERIVATIVES WITH EXOCYCLIC DOUBLE BOND
ATE340836T1 (en) 2003-05-27 2006-10-15 Merck Patent Gmbh PYRAND DERIVATIVES
EP1757284A1 (en) * 2005-08-25 2007-02-28 Santhera Pharmaceuticals (Schweiz) AG Use of N-(dibenz(b,f)oxepin-10ylmethyl)-N-methyl-N-prop-2-ynylamine (omigapil) for the prophylaxis and/or treatment of muscular dystrophy

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5021432A (en) * 1988-04-26 1991-06-04 Yoshitomi Pharmaceutical Industries, Ltd. Benzopyran compound and its pharmaceutical use
JPH09503994A (en) * 1993-03-03 1997-04-22 イーライ・リリー・アンド・カンパニー Balanoid
US5612370A (en) * 1995-06-07 1997-03-18 Bristol-Myers Squibb Company Phenylglycine and phenylalaninen amido benzopyran derivatives
AR013079A1 (en) * 1997-05-06 2000-12-13 Smithkline Beecham Corp SUBSTITUTED DERIVATIVES OF TETRAHIDROFURANO-3-ONAS, TETRAHIDROPIRANO-3- ONAS AND TETRAHIDROTIOFEN-3-ONAS, A PROCEDURE FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION OF A MEDICINAL PRODUCT USEFUL AS INTERMEDIATE PROTEIN INHIBITORS

Also Published As

Publication number Publication date
JP2002537297A (en) 2002-11-05
WO2000049011A1 (en) 2000-08-24
EP1153022A1 (en) 2001-11-14
AU3235100A (en) 2000-09-04
HK1042695A1 (en) 2002-08-23
EP1153022A4 (en) 2002-03-27
DZ3083A1 (en) 2004-06-02
CO5271679A1 (en) 2003-04-30

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