CO5180541A1 - Inhibidores de proteasa del tipo de 1,3-diaminocetonas con anillo de 8-14 miembros - Google Patents

Inhibidores de proteasa del tipo de 1,3-diaminocetonas con anillo de 8-14 miembros

Info

Publication number
CO5180541A1
CO5180541A1 CO99078651A CO99078651A CO5180541A1 CO 5180541 A1 CO5180541 A1 CO 5180541A1 CO 99078651 A CO99078651 A CO 99078651A CO 99078651 A CO99078651 A CO 99078651A CO 5180541 A1 CO5180541 A1 CO 5180541A1
Authority
CO
Colombia
Prior art keywords
alkyl
group
het
cycloalkyl
mfi
Prior art date
Application number
CO99078651A
Other languages
English (en)
Inventor
Jr Robert Wells Marquis
Daniel Frank Veber
Original Assignee
Smithkline Beechman 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 Beechman Corp filed Critical Smithkline Beechman Corp
Publication of CO5180541A1 publication Critical patent/CO5180541A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D225/00Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
    • C07D225/02Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom not condensed with other rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto de fórmula I:<EMI FILE="99078651_1" ID="1" IMF=JPEG >en la que:A se selecciona entre el grupo que consta de: C(O) y CH(OH);R1 se selecciona entre el grupo que consta de:<EMI FILE="99078651_2" ID="2" IMF=JPEG >R2 se selecciona entre el grupo que consta de: 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)-, R9R12NC(O)-, R9R12NC(S)-, R12HNCH(R12)C(O)-, R9OC(O)NR12CH(R12)C(O)-, adamantil-C(O)-, o<EMI FILE="99078651_3" ID="3" IMF=JPEG >R" se selecciona entre el grupo que consta de: H, alquilo C1-6, Ar-alquilo C0-6, y Het-alquilo C0-6.R"´ se selecciona entre el grupo que consta de: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6,R3 y R8 se seleccionan independientemente entre el grupo que consta de: H, alquenilo C2-6, alquinilo C2-6, Het, Ar o alquilo C1-6 opcionalmenre sustituido con OR13, SR13, NR132, R13NC(O)OR5, CO2R13, CO2NR132, N(C=NH)NH2, Het y Ar;R4 se selecciona entre el grupo que consta de: 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)-, R5R14NC(O)-, R5R14NC(S)-, R14HNCH(R14)C(O)- y R5OC(O)NR14CH(R14)C(O)-;R5, R9 y R10 se seleccionan independientemente entre el grupo que consta de:alquilo C1-6, cicloalquiI C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6 ;R6 se selecciona entre el grupo que consta de: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6 ;R7 se selecciona entre el grupo que consta de: 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)-, R10R15NC(O)-, R10R15NC(S)-, R15HNCH(R15)C(O)- y R10OC(O)NR15CH(R15)C(O)-;oR6 y R7 se conectan para formar un anillo de pirrolidina, piperidina o morfolina; ...
CO99078651A 1998-12-23 1999-12-16 Inhibidores de proteasa del tipo de 1,3-diaminocetonas con anillo de 8-14 miembros CO5180541A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11414398P 1998-12-23 1998-12-23

Publications (1)

Publication Number Publication Date
CO5180541A1 true CO5180541A1 (es) 2002-07-30

Family

ID=22353596

Family Applications (1)

Application Number Title Priority Date Filing Date
CO99078651A CO5180541A1 (es) 1998-12-23 1999-12-16 Inhibidores de proteasa del tipo de 1,3-diaminocetonas con anillo de 8-14 miembros

Country Status (9)

Country Link
EP (1) EP1140897A4 (es)
JP (1) JP2002533452A (es)
AR (1) AR021970A1 (es)
AU (1) AU2713100A (es)
CO (1) CO5180541A1 (es)
DZ (1) DZ2976A1 (es)
HK (1) HK1041690A1 (es)
PE (1) PE20001355A1 (es)
WO (1) WO2000039115A1 (es)

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
WO2001034599A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EP1232154A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
AU1474801A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
CN1416346A (zh) 2000-03-21 2003-05-07 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
US7087604B2 (en) 2002-03-08 2006-08-08 Bristol-Myers Squibb Company Cyclic derivatives as modulators of chemokine receptor activity
WO2006029154A2 (en) * 2004-09-07 2006-03-16 Smithkline Beecham Corporation Novel compounds
CN101137412B (zh) 2005-01-13 2012-11-07 布里斯托尔-迈尔斯·斯奎布公司 用作凝血因子XIa抑制剂的取代的二芳基化合物

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DZ2285A1 (fr) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
TR199902752T2 (xx) * 1997-05-08 2000-06-21 Smithkline Beecham Corporation Proteaz inhibit�rleri.

Also Published As

Publication number Publication date
PE20001355A1 (es) 2001-01-28
EP1140897A1 (en) 2001-10-10
AU2713100A (en) 2000-07-31
JP2002533452A (ja) 2002-10-08
AR021970A1 (es) 2002-09-04
DZ2976A1 (fr) 2004-03-15
EP1140897A4 (en) 2002-04-03
HK1041690A1 (zh) 2002-07-19
WO2000039115A1 (en) 2000-07-06

Similar Documents

Publication Publication Date Title
AR045782A2 (es) Derivados de piperidina que tienen actividad farmaceutica
CO5261626A1 (es) Glutarimidas sustituidas, su preparacion, medicamentos que las contienen, y uso de las mismas para la fabricacion de medicamentos, especialemente inmunomoduladores, como asi tambien inhibidores de angiopatias y/o enfermedades hematologicas/oncologica
AR029216A1 (es) Compuestos inhibidores no peptidicos de la union celular dependiente de vla-4 utiles en el tratamiento de enfermedades inflamatorias, autoinmunes y respiratorias; composicion farmaceutica y procedimiento de tratamiento
ES2141174T3 (es) 4-arilmetiloximetil piperidinas como antagonistas de taquiquinina.
YU108791A (sh) Pirazolopirimidinon antianginalna jedinjenja
PT1140916E (pt) Acetais heteroarilo ciclicos
AR068413A2 (es) Derivados 8-amino, metodos de preparacion, composiciones farmaceuticas y su uso en terapia
NZ511394A (en) N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
CO4650042A1 (es) Derivados de 6-fenilpiridil-2-amina
DE60322877D1 (de) Tetrahydropyranylcyclopentyltetrahydroisochino-linmodulatoren der chemokinrezeptoraktivität
HRP20070286T3 (en) Substituted diketopiperazines and their use as oxytocyn antagonists
HK1079191A1 (en) Pleuromutilin derivatives as antimicrobbials
CO4920225A1 (es) 2-amino-6-(4-fenoxi-2-sustituido)-piridinas sustituidas
DE69507293D1 (de) Benzamid-derivate als vasopressin-antagonisten
BR9707767A (pt) Composto analgésico composição farmaceuticamente aceitável compreendendo o mesmo e utilização de um composto analgésico
BR0004535A (pt) Compostos, e, uso dos mesmos.
CO5180541A1 (es) Inhibidores de proteasa del tipo de 1,3-diaminocetonas con anillo de 8-14 miembros
DE60318826D1 (de) Alkoxypyridinderivate
CO4950553A1 (es) Compuestos de 7-tetrahidroisoquinolinas y procedimiento para su preparacion
CO4990965A1 (es) Derivados de 1,3,8-triazaspiro(4,5)decan-4-ona to que los contiene y un proceso para la preparacion de es- tos derivados
PE20040750A1 (es) Derivados de n-(1-acetilpiperidin-4-il)-4-benzidril-2-isopropilpiperazin-1-carboxamida como inhibidores de 17beta-hidroxiesteroide deshidrogenasa de tipo 3
AR035451A1 (es) Derivados de beta-carbolina, su uso para la fabricacion de un medicamento para el tratamiento de la depresion, ansiedad y desordenes bipolares, una composicion farmaceutica y una combinacion.
TR200200360T2 (tr) Antibakteriyel aktif maddeler.
ATE333457T1 (de) Zyklische gmp-spezifische phosphodiesteraseinhibitoren
CO5140099A1 (es) Ciertas caprolactamas sustituidas, composiciones farmaceuticas que las contienen, y su uso en el tratamiento de tumores

Legal Events

Date Code Title Description
FA Application withdrawn