CO5280093A1 - TREATMENT METHODS - Google Patents

TREATMENT METHODS

Info

Publication number
CO5280093A1
CO5280093A1 CO01029288A CO01029288A CO5280093A1 CO 5280093 A1 CO5280093 A1 CO 5280093A1 CO 01029288 A CO01029288 A CO 01029288A CO 01029288 A CO01029288 A CO 01029288A CO 5280093 A1 CO5280093 A1 CO 5280093A1
Authority
CO
Colombia
Prior art keywords
alkyl
group
het
cycloalkyl
alkynyl
Prior art date
Application number
CO01029288A
Other languages
Spanish (es)
Inventor
Robert Well
Danbiel Frank Veber
Ru-Maxwell Yu
Scott Kevon Thompson
Dennis Shinji Yamashita
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 CO5280093A1 publication Critical patent/CO5280093A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un método para inhibir la catepsina L, que comprende administrar, a un paciente que lo necesite, una cantidad eficaz de un compuesto de Fórmula I: <EMI FILE="01029288_1" ID="1" IMF=JPEG >en la que:R1 seleccionado del grupo que consiste en:<EMI FILE="01029288_2" ID="2" IMF=JPEG > R2 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6 -alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, R9C(O)-, R9C(S)-, R9SO2-, R9OC(O)-, R9R11NC(O)-,R9R11NC(S)-, R9(R11)NSO2-, R3 es seleccionado del grupo que consiste en: H, alquilo Cl-6, cicloalquil C3-6-alquilo C0-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6, y Ar-alquilo C0-6;R3 y R' pueden estar unidos para formar un anillo de pirrolidina, piperidina o morfolina;R4 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, R5C(O)-, R5C(S)-, R5SO2-, R5OC(O), R5R13NC(O)-, y R5R13NC(S)-; - 2 -R5 es seleccionado del grupo que consiste en: H, alquilo C1-6 alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R6 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6 alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R7 es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, R10C(O)-, R10C(S)-, - R10SO2-, R10OC(O)-, R10R14N-C(O)-, y R10 R14NC(S)-;R8 es seleccionado del grupo que consiste en: H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6 y Ar-alquilo C0-6; R9 es seleccionado del grupo que consiste en: alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6, R10 seleccionado del grupo que consiste en: alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R11 es seleccionado del grupo que consiste en: H, alquilo C1-6 Ar-alquilo C0-6 y Het-alquilo C0-6; R12 es seleccionado del grupo que consiste en: H, alquilo Cl-6 Ar-alquilo C0-6 y Het-alquilo C0-6, R13 es seleccionado del grupo que consiste en: H, alquilo C1-6 Ar-alquilo C0-6 y Het-alquilo C0-6; R14 es seleccionado del grupo que consiste en: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6;R´ es seleccionado del grupo que consiste en: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R" es seleccionado del grupo que consiste en: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6, R"' es seleccionado del grupo que consiste en: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; X es seleccionado del grupo que consiste en: CH2, S y O; yZ es seleccionado del grupo que consiste en: C(O) y CH2; y sales, hidratos y solvatos farmacéuticamente aceptables del mismo.A method for inhibiting cathepsin L, which comprises administering, to a patient in need, an effective amount of a compound of Formula I: <EMI FILE = "01029288_1" ID = "1" MFI = JPEG> in which: R1 selected from the group consisting of: <EMI FILE = "01029288_2" ID = "2" MFI = JPEG> R2 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar -C0-6 alkyl, Het-C0-6 alkyl, R9C (O) -, R9C (S) -, R9SO2-, R9OC (O) -, R9R11NC (O) -, R9R11NC (S) -, R9 (R11) NSO2-, R3 is selected from the group consisting of: H, Cl-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Het-C0-6 alkyl, and Ar-alkyl C0-6; R3 and R 'may be linked to form a pyrrolidine, piperidine or morpholine ring; R4 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar- C0-6 alkyl, Het-C0-6 alkyl, R5C (O) -, R5C (S) -, R5SO2-, R5OC (O), R5R13NC (O) -, and R5R13NC (S) -; - 2 -R5 is selected from the group consisting of: H, C1-6 alkyl C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0 alkyl -6; R6 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; R7 is selected from the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, R10C (O) -, R10C (S) -, - R10SO2-, R10OC (O) -, R10R14N-C (O) -, and R10 R14NC (S) -; R8 is selected from the group consisting of: H, C1-6 alkyl, C2-6 alkenyl, alkynyl C2-6, Het-C0-6 alkyl and Ar-C0-6 alkyl; R9 is selected from the group consisting of: C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R10 selected from the group consisting of: C1-6 alkyl , C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R11 is selected from the group consisting of: H, C1-6 alkyl Ar-C0-6 alkyl and Het-C0-6 alkyl; R12 is selected from the group consisting of: H, Cl-6 alkyl Ar-C0-6 alkyl and Het-C0-6 alkyl, R13 is selected from the group consisting of: H, C1-6 alkyl Ar-C0-6 alkyl and Het-C0-6 alkyl; R14 is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R 'is selected from the group consisting of: H, C1-6 alkyl, Ar-alkyl C0-6 and Het-C0-6 alkyl; R "is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R" 'is selected from the group consisting of: H, C1-6 alkyl, cycloalkyl C3-6-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; X is selected from the group consisting of: CH2, S and O; and Z is selected from the group consisting of: C (O) and CH2; and pharmaceutically acceptable salts, hydrates and solvates thereof.

CO01029288A 2000-04-18 2001-04-16 TREATMENT METHODS CO5280093A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19771700P 2000-04-18 2000-04-18

Publications (1)

Publication Number Publication Date
CO5280093A1 true CO5280093A1 (en) 2003-05-30

Family

ID=22730469

Family Applications (1)

Application Number Title Priority Date Filing Date
CO01029288A CO5280093A1 (en) 2000-04-18 2001-04-16 TREATMENT METHODS

Country Status (5)

Country Link
EP (1) EP1303281A4 (en)
JP (1) JP2003531122A (en)
AU (1) AU2001253560A1 (en)
CO (1) CO5280093A1 (en)
WO (1) WO2001078734A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1401453A4 (en) * 2001-05-17 2005-04-06 Smithkline Beecham Corp Protease inhibitors
EP1551823A1 (en) * 2002-10-08 2005-07-13 Merck Frosst Canada Inc. 4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ511710A (en) * 1998-12-23 2003-12-19 Smithkline Beecham Corp 4-Amino-azepan-3-one derivatives useful as protease inhibitors
JP2003513956A (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
WO2001034160A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
AU1474601A (en) * 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
US6534498B1 (en) * 1999-11-10 2003-03-18 Smithkline Beecham Corporation Protease inhibitors
EP1229912A4 (en) * 1999-11-10 2003-05-07 Smithkline Beecham Corp Protease inhibitors
JP2003513926A (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
JP2003533432A (en) * 1999-11-10 2003-11-11 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
CN1416346A (en) * 2000-03-21 2003-05-07 史密丝克莱恩比彻姆公司 Peotease inhibitors

Also Published As

Publication number Publication date
EP1303281A1 (en) 2003-04-23
EP1303281A4 (en) 2006-02-15
AU2001253560A1 (en) 2001-10-30
WO2001078734A1 (en) 2001-10-25
JP2003531122A (en) 2003-10-21

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