AR032622A1 - Compuestos de 4-amino-azepan-3-ona, composiciones farmaceuticas que los comprenden, intermediarios utiles en la sintesis de tales compuestos, procedimiento para la sintesis de dichos compuestos, y uso de tales compuestos en la fabricacion de medicamentos - Google Patents

Compuestos de 4-amino-azepan-3-ona, composiciones farmaceuticas que los comprenden, intermediarios utiles en la sintesis de tales compuestos, procedimiento para la sintesis de dichos compuestos, y uso de tales compuestos en la fabricacion de medicamentos

Info

Publication number
AR032622A1
AR032622A1 ARP010102840A ARP010102840A AR032622A1 AR 032622 A1 AR032622 A1 AR 032622A1 AR P010102840 A ARP010102840 A AR P010102840A AR P010102840 A ARP010102840 A AR P010102840A AR 032622 A1 AR032622 A1 AR 032622A1
Authority
AR
Argentina
Prior art keywords
compounds
alkyl
synthesis
het
azepan
Prior art date
Application number
ARP010102840A
Other languages
English (en)
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 AR032622A1 publication Critical patent/AR032622A1/es

Links

Classifications

    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/12—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D405/14—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 three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (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)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Epoxy Compounds (AREA)

Abstract

Compuestos de 4-amino-azepan-3-ona y sales, hidratos y solvatos farmacéuticamente aceptables de los mismos, que son inhibidores de proteasas, particularmente de cisteína- y serina-proteasas, y por lo tanto son utiles en el tratamiento de enfermedades en las cuales están implicadas dichas proteasas, especialmente trastornos de pérdida excesiva de hueso o cartílago. Dichos compuestos de 4-amino-azepan-3-ona tienen la formula (1), en la que: R1 se selecciona del grupo constituido por las formulas (2), (3) y (4); R2 se selecciona del grupo constituido por alquilo C1-6, Ar-alquilo C0-6, Het-alquilo C0-6, R9C(O)-, R9C(S)-, R9SO2-, R9R11NC(O)-, y R9SO2R11NC(O)-; R3 es alquilo C1-6; R4 es R5C(O)-; R5 es Het-alquilo C0-6; R9 se selecciona del grupo constituido por alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R11 se selecciona del grupo constituido por H, alquilo C1-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R' es H; R'' es H; R''' es H; R'''' se selecciona del grupo constituido por alquilo C1-6, cicloalquil C3-6-alquilo C0-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6, y Ar-alquilo C0-6; n es un numero entero de 1 a 5. Además, se dan a conocer: composiciones farmacéuticas que comprenden dichos compuestos, intermediarios utiles en la síntesis de tales compuestos, un procedimiento para la síntesis de dichos compuestos, y el uso de tales compuestos en la fabricacion de medicamentos.
ARP010102840A 2000-06-14 2001-06-14 Compuestos de 4-amino-azepan-3-ona, composiciones farmaceuticas que los comprenden, intermediarios utiles en la sintesis de tales compuestos, procedimiento para la sintesis de dichos compuestos, y uso de tales compuestos en la fabricacion de medicamentos AR032622A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US59384500A 2000-06-14 2000-06-14

Publications (1)

Publication Number Publication Date
AR032622A1 true AR032622A1 (es) 2003-11-19

Family

ID=24376433

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010102840A AR032622A1 (es) 2000-06-14 2001-06-14 Compuestos de 4-amino-azepan-3-ona, composiciones farmaceuticas que los comprenden, intermediarios utiles en la sintesis de tales compuestos, procedimiento para la sintesis de dichos compuestos, y uso de tales compuestos en la fabricacion de medicamentos

Country Status (25)

Country Link
EP (1) EP1307204A4 (es)
JP (1) JP2004503502A (es)
KR (1) KR20030008220A (es)
CN (1) CN1444481A (es)
AP (1) AP2002002671A0 (es)
AR (1) AR032622A1 (es)
AU (1) AU2001268407A1 (es)
BG (1) BG107327A (es)
BR (1) BR0111693A (es)
CA (1) CA2412353A1 (es)
CZ (1) CZ20024086A3 (es)
EA (1) EA200300018A1 (es)
EC (1) ECSP024388A (es)
HU (1) HUP0301231A2 (es)
IL (1) IL153421A0 (es)
MA (1) MA25758A1 (es)
MX (1) MXPA02012442A (es)
NO (1) NO20025786L (es)
NZ (1) NZ522965A (es)
OA (1) OA12288A (es)
PE (1) PE20011374A1 (es)
PL (1) PL360508A1 (es)
SK (1) SK17592002A3 (es)
WO (1) WO2001095911A1 (es)
ZA (1) ZA200209808B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034159A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
PL366232A1 (en) * 2000-11-22 2005-01-24 Smithkline Beecham Corporation Protease inhibitors
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
US7723366B2 (en) 2001-02-20 2010-05-25 Chugai Seiyaku Kabushiki Kaisha Azole compounds as malonyl-CoA decarboxylase inhibitors for treating metabolic diseases
AU2002342682A1 (en) * 2001-05-17 2002-11-25 Smithkline Beecham Corporation Protease inhibitors
CA2533747C (en) 2003-08-01 2012-11-13 Chugai Seiyaku Kabushiki Kaisha Heterocyclic compounds useful as malonyl-coa decarboxylase inhibitors
ES2314491T3 (es) 2003-08-01 2009-03-16 Chugai Seiyaku Kabushiki Kaisha Compuestos azol basados en cianoguanidina utiles como inhibidores de la manonil-coa descaraboxilasa.
US7449482B2 (en) 2003-08-01 2008-11-11 Chugai Seiyaku Kabushiki Kaisha Piperidine compounds useful as malonyl-CoA decarboxylase inhibitors
JP5587790B2 (ja) 2008-01-09 2014-09-10 アミュラ セラピューティクス リミティド 化合物
CN103275070A (zh) * 2013-05-10 2013-09-04 郑彪 调节单核细胞增殖的四环化合物及其应用
US9427441B2 (en) 2014-02-19 2016-08-30 Indiana University Research And Technology Corporation Targeting primary cilia to treat glaucoma

Family Cites Families (7)

* 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.
AU768565B2 (en) * 1998-12-23 2003-12-18 Smithkline Beecham Corporation Protease inhibitors
WO2001034158A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034565A2 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
JP2004509083A (ja) * 2000-09-01 2004-03-25 スミスクライン・ビーチャム・コーポレイション 治療方法
PL366232A1 (en) * 2000-11-22 2005-01-24 Smithkline Beecham Corporation Protease inhibitors
AU2002342682A1 (en) * 2001-05-17 2002-11-25 Smithkline Beecham Corporation Protease inhibitors

Also Published As

Publication number Publication date
NO20025786D0 (no) 2002-12-02
MA25758A1 (fr) 2003-04-01
ECSP024388A (es) 2003-02-06
JP2004503502A (ja) 2004-02-05
PE20011374A1 (es) 2002-04-07
PL360508A1 (en) 2004-09-06
EP1307204A4 (en) 2004-06-02
IL153421A0 (en) 2003-07-06
EP1307204A1 (en) 2003-05-07
SK17592002A3 (sk) 2003-05-02
WO2001095911A1 (en) 2001-12-20
BG107327A (bg) 2003-07-31
CN1444481A (zh) 2003-09-24
AP2002002671A0 (en) 2002-12-31
KR20030008220A (ko) 2003-01-24
AU2001268407A1 (en) 2001-12-24
NO20025786L (no) 2003-02-12
ZA200209808B (en) 2004-07-09
OA12288A (en) 2003-12-12
HUP0301231A2 (hu) 2003-08-28
NZ522965A (en) 2004-06-25
EA200300018A1 (ru) 2003-06-26
MXPA02012442A (es) 2003-04-25
BR0111693A (pt) 2004-04-06
CA2412353A1 (en) 2001-12-20
CZ20024086A3 (cs) 2003-05-14

Similar Documents

Publication Publication Date Title
AR032877A1 (es) Inhibidores alquil c(1-6)-4-amino-azepan-3-onicos de proteasas, composiciones farmaceuticas que los comprenden, intermediarios utiles en la preparacion de tales compuestos, procedimiento para la sintesis de dichos inhibidores, y uso de dichos inhibidores en la fabricacion de medicamentos
AR024060A1 (es) Nuevos compuestos farmaceuticamente activos
AR041566A1 (es) Derivados de indol utiles para el tratamiento de enfermedades
AR037517A1 (es) Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
ECSP034732A (es) Derivado de fenetanolamina para el tratamiento de enfermedades respiratorias
DOP2001000271A (es) Compuestos de imidazol condensado con arilo o heteroarilo como agentes antiinflamatorios y analgésicos.
BR0111263A (pt) Derivados de 2-aminocarbonil-9h-purina
MEP9509A (en) Pharmaceutical compositions containing azetidine derivatives, novel azetidine derivatives and preparation thereof
ECSP066383A (es) Derivados de 5-fenil-4-metil-tiazol-2-il-amina como inhibidores de enzimas de cinasa fosfatidilinositol 3 (pi3) para el tratamiento de enfermedades inflamatorias de las vías respiratorias
PA8547701A1 (es) Nucleosidos 4 substituidos.
AR035792A1 (es) Compuestos de n-(4-quinazolinil)-n-(1h-indazol-5-il) amina, inhibidor de la rho-quinasa, su uso para la fabricacion de un medicamento y metodo para prepararlo
SE0104332D0 (sv) Therapeutic agents
AR034268A1 (es) Compuestos derivados de piperidina, su uso en preparacion de medicamentos, composicion farmaceutica, metodo de tratamiento y proceso para su preparacion
HUP0303084A2 (hu) Gyulladásgátló hatású 17béta-karbotioát-17alfa-arilkarboniloxiloxi androsztán-származékok, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
DE60132309D1 (de) Amin-derivate zur behandlung von apoptosis
PT1263724E (pt) Novos compostos
PA8529501A1 (es) Nuevos tiadiazoles y oxadiazoles y su uso como inhibidores de fosfodiesterasa -7."
HUP0402225A2 (hu) Makrolid-vegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
ES2123039T3 (es) Nuevas 3-(hidroxi-bencilidenil)-indolin-2-onas, su procedimiento de preparacion y composiciones farmaceuticas que las contienen.
AR003440A1 (es) Nuevos derivados de aminoacidos, formulacion farmaceutica que los contiene, uso de dichos derivados para preparar medicamentos y procedimiento para la preparacion de dichos derivados.
AR029150A1 (es) Un derivado de piperidina, su empleo, un procedimiento para prepararlo y una composicin farmaceutica que lo comprende.
AR032622A1 (es) Compuestos de 4-amino-azepan-3-ona, composiciones farmaceuticas que los comprenden, intermediarios utiles en la sintesis de tales compuestos, procedimiento para la sintesis de dichos compuestos, y uso de tales compuestos en la fabricacion de medicamentos
CR7956A (es) Oxazolidinonas de indolona antibacterial intermedios para su preparacion y composiciones farmaceuticas que contienen los mismos
PA8495101A1 (es) Derivados de 13-metileritromicina
NO20025641D0 (no) Substituerte 1-aminoalkyl-laktamer og deres anvendelse som muscarin-reseptor-antagonister

Legal Events

Date Code Title Description
FA Abandonment or withdrawal