[go: up one dir, main page]

AR036875A1 - Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa - Google Patents

Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa

Info

Publication number
AR036875A1
AR036875A1 ARP020103499A ARP020103499A AR036875A1 AR 036875 A1 AR036875 A1 AR 036875A1 AR P020103499 A ARP020103499 A AR P020103499A AR P020103499 A ARP020103499 A AR P020103499A AR 036875 A1 AR036875 A1 AR 036875A1
Authority
AR
Argentina
Prior art keywords
crara1
substituted
nrara1
carbon atoms
time
Prior art date
Application number
ARP020103499A
Other languages
English (en)
Inventor
Gregory Ott
Xiao-Tao Chen
Jingwu Duan
Lu Zhonghui
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR036875A1 publication Critical patent/AR036875A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • A61P31/08—Antibacterial agents for leprosy
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compuestos que son útiles como inhibidores de las metaloproteinasas de matriz (MMP), enzima que convierte el TNF-a TACE, agrecanasa o una combinación de los mismos, composiciones farmacéuticas que contienen el mismo y métodos para usar el mismo. Reivindicación 1: Un compuesto de la fórmula (1) o un estereoisómero o una forma de sal farmacéuticamente aceptable del mismo; en donde el anillo B es un anillo heterocíclico o carbocíclico no aromático de 4-7 miembros que comprende: átomos de carbono, 0-3 grupos carbonilo, 0-3 enlaces dobles, y 0-2 heteroátomos de anillo seleccionados de O, N, NR1, y S(O)p, con la condición de que el anillo B contiene otros enlaces diferentes a S-S, O-O, ó S-O; R1 se selecciona de Q, alquileno C1-6-Q, alquenileno C2-6-Q, alquinileno C2-6-Q, (CRaRa1)qO(CRaRa1)s-Q, (CRaRa1)qNRa(CRaRa1)s-Q, (CRaRa1)rC(O)(CRaRa1)s-Q, (CRaRa1)rC(O)-alquenileno C2-6-Q, (CRaRa1)rC(O)O(CRaRa1)s-Q, (CRaRa1)rOC(O)O(CRaRa1)s-Q, (CRaRa1)rOC(O)NRa(CRaRa1)s-Q, (CRaRa1)rC(O)NRaRa1, (CRaRa1)rC(O)NRa(CRaRa1)s-Q, (CRaRa1)qNRaC(O)(CRaRa1)s-Q, (CRaRa1)qNRaC(O)O(CRaRa1)s-Q, (CRaRa1)qNRaC(O)NRa(CRaRa1)s-Q, (CRaRa1)rS(O)p(CRaRa1)s-Q, (CRaRa1)rNRaSO2(CRaRa1)s-Q, y (CRaRa1)rSO2NRa(CRaRa1)s-Q; R2 se selecciona de Q, alquileno C1-6-Q, alquenileno C2-6-Q, alquinileno C2-6-Q, (CRaRa1)rO (CRaRa1)s-Q, (CRaRa1)rNRa(CRaRa1)s-Q, (CRaRa1)rC(O)(CRaRa1)s-Q, (CRaRa1)rC(O)-alquenileno C2-6-Q, (CRaRa1)rC(O)O(CRaRa1)s-Q, (CRaRa1)rC(O)NRaRa1, (CRaRa1)rC(O)NRa(CRaRa1)s-Q, (CRaRa1)rNRaC(O)(CRaRa1)s-Q, (CRaRa1)rNRaC(O)O(CRaRa1)s-Q, (CRaRa1)rNRaC(O)NRa(CRaRa1)s-Q, (CRaRa1)rS(O)p(CRaRa1)s-Q, y (CRaRa1)rSO2NRa(CRaRa1)s-Q; Q se selecciona de H, un carbociclo C3-6 sustituido con 0-3 Rd, y un heterociclo de 5-10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituidos con 0-3 Rd; R3 se selecciona de Q1, Cl, F, alquileno C1-6-Q1, alquenileno C2-6-Q1, alquinileno C2-6-Q1, (CRaRa1)rO(CRaRa1)s-Q1, (CRaRa1)rNRa(CRaRa1)s-Q1, (CRaRa1)rNRaC(O)(CRaRa1)s-Q1, (CRaRa1)rC(O)NRa(CRaRa1)s-Q1, (CRaRa1)rC(O)(CRaRa1)s-Q1, (CRaRa1)rC(O)O(CRaRa1)s-Q1, (CRaRa12)rS(O)p(CRaRa1)s-Q1, y (CRaRa1)rSO2NRa(CRaRa1)s-Q1; Q1 se selecciona de H, fenilo sustituido con 0-3 Rd, naftilo sustituido con 0-3 Rd y un heterociclo de 5-10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-3 Rd; Za se selecciona de del grupo de fórmulas (2); X es S, SO, SO2, O, ó NR14; Y es N ó CR17; R11 y R12, cada vez que se presentan, se seleccionan independientemente de H, Rc, alquilo C1-6 sustituido con 0-3 Rc1, carbociclo C3-10 sustituido con 0-3 Rc1, y heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y sustituido con 0-3 Rc1 ; R13 y R13a cada vez que se presentan, se seleccionan independientemente de H, Rc, alquilo C1-6 sustituido con 0-3 Rc1, carbociclo C3-10 sustituido con 0-3 Rc1, y un heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-3 Rc1; alternativamente, cuando R13 y R13a se enlazan a átomos de carbono adyacentes, junto con los átomos de carbono a los cuales se enlazan, forman un anillo de 5-7 miembros que consiste de: átomos de carbono, 0-2 grupos carbonilo, 0-3 dobles enlaces, y 0-2 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-2 Rc1; R14, cada vez que se presenta, se selecciona independientemente de H, alquilo C1-4, fenilo, y bencilo; R15 y R16, cada vez que se presentan, se seleccionan independientemente de H, Rc1, alquilo C1-6 sustituido con 0-3 Rc1, carbociclo C3-10 sustituido con 0-3 Rc1, y un heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p, y sustituido con 0-3 Rc1; alternativamente, cuando R15 y R16 se enlazan a los átomos de carbono adyacentes, junto con los átomos de carbono a los cuales se enlazan, forman un anillo de 5-7 miembros, que consiste de: átomos de carbono, 0-2 grupos carbonilo, 0-3 dobles enlaces, 0-2 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p; este anillo está sustituido con 0-2 Rc1; alternativamente, cuando R15 y R16 se enlazan al mismo átomo de carbono, junto con el átomo de carbono al cual están enlazados, forman un anillo de 3-7 miembros que consiste de: átomos de carbono, 0-2 grupos carbonilo, 0-3 dobles enlaces, y 0-2 heteroátomos seleccionados de N, O, y S(O)p; este anillo está sustituido con 0-2 Rc1; R17 se selecciona de H, Cl, F, y alquilo C1-4; Ra, cada vez que se presenta, se selecciona independientemente de H, alquilo C1-4, fenilo, y bencilo; Ra1, cada vez que se presenta, se selecciona independientemente de H y alquilo C1-4; Ra2, cada vez que se presenta, se selecciona independientemente de alquilo C1-4, fenilo, y bencilo; Rc, cada vez que se presenta, se selecciona independientemente de alquilo C1-6, ORa, Cl, F, Br, I, -CN, NO2, NRaRa1, C(O)Ra, C(O)ORa, C(O)NRaRa1, RaNC(O)NRaRa1, OC(O)NRaRa1, RaNC(O)ORa, S(O)2NRaRa1, NRaS(O)2Ra2, NRaS(O)2NRaRa1, OS(O)2NRaRa1, NRaS(O)2Ra2, S(O)pRa2, CF3, OCF3, CF2CF3, CH2F, y CHF2; Rc1, cada vez que se presenta, se selecciona independientemente de alquilo C1-6, ORa, Cl, F, Br, I, =O, -CN, NO2, NRaRa1, C(O)Ra, C(O)ORa, C(O)NRaRa1, RaNC(O)NRaRa1, OC(O)NRaRa1, RaNC(O)ORa, S(O)2NRaRa1, NRaS(O)2Ra2, NRaS(O)2NRaRa1, OS(O)2NRaRa1, NRaS(O)2Ra2, S(O)pRa2, CF3, OCF3, CF2CF3, CH2F, y CHF2; Rd, cada vez que se presenta, se selecciona independientemente de alquilo C1-6, ORa, Cl, F, Br, I, =O, -CN, NO2, NRaRa1, C(O)Ra, C(O)ORa, C(O)NRaRa1, RaNC(O)NRaRa1, OC(O)NRaRa1, RaNC(O)O, S(O)2NRaRa1, NRaS(O)2Ra2, NRaS(O)2NRaRa1, OS(O)2NRaRa1, NRaS(O)2Ra2, S(O)pRa2, CF3, OCF3, CF2CF3, carbociclo C3-10, y un heterociclo de 5-14 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados del grupo que consiste de N, O, y S(O)p; p, cada vez que se presenta, se selecciona de 0, 1, y 2; q, cada vez que se presenta, se selecciona de 1, 2, 3, y 4; r, cada vez que se presenta, se selecciona de 0, 1, 2, 3, y 4; y, s, cada vez que se presenta, se selecciona de 0, 1, 2, 3, y 4.
ARP020103499A 2001-09-17 2002-09-17 Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa AR036875A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US32263001P 2001-09-17 2001-09-17

Publications (1)

Publication Number Publication Date
AR036875A1 true AR036875A1 (es) 2004-10-13

Family

ID=23255712

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020103499A AR036875A1 (es) 2001-09-17 2002-09-17 Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa

Country Status (5)

Country Link
US (1) US6740649B2 (es)
EP (1) EP1427408A4 (es)
AR (1) AR036875A1 (es)
AU (1) AU2002341715A1 (es)
WO (1) WO2003024899A2 (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20030701A1 (es) 2001-12-20 2003-08-21 Schering Corp Compuestos para el tratamiento de trastornos inflamatorios
WO2003077914A1 (en) * 2002-03-13 2003-09-25 Array Biopharma, Inc N3 alkylated benzimidazole derivatives as mek inhibitors
JP2006516548A (ja) 2002-12-30 2006-07-06 アンジオテック インターナショナル アクツィエン ゲゼルシャフト 迅速ゲル化ポリマー組成物からの薬物送達法
MXPA06000091A (es) 2003-07-02 2006-04-07 Sugen Inc Arilmetiltriazolo e imidazopirazinas como inhibidores de c-met.
EP1651631A1 (en) 2003-08-01 2006-05-03 Genelabs Technologies, Inc. Bicyclic imidazol derivatives against flaviviridae
US20050080075A1 (en) * 2003-08-25 2005-04-14 Nichols M. James Formulations, conjugates, and combinations of drugs for the treatment of neoplasms
DE10348044A1 (de) * 2003-10-15 2005-05-19 Imtm Gmbh Duale Alanyl-Aminopeptidase- und Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
GB0505969D0 (en) 2005-03-23 2005-04-27 Novartis Ag Organic compounds
CA2608890C (en) * 2005-05-20 2011-08-02 Alantos-Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20070155738A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
WO2007016597A2 (en) * 2005-07-29 2007-02-08 The Regents Of The University Of California Targeting tnf-alpha converting enzyme (tace)-dependent growth factor shedding in cancer therapy
TWI387592B (zh) 2005-08-30 2013-03-01 Novartis Ag 經取代之苯并咪唑及其作為與腫瘤形成相關激酶之抑制劑之方法
WO2007053499A2 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
WO2007053495A2 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
WO2007053498A1 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
EP2420491B1 (en) 2005-12-30 2013-07-03 Novartis AG 3 , 5-substitued piperidine compounds as renin inhibitors
US7875636B2 (en) * 2006-04-12 2011-01-25 Merck Sharp & Dohme Corp. Pyridyl amide T-type calcium channel antagonists
BRPI0813900A2 (pt) 2007-06-25 2014-12-30 Novartis Ag Derivados de n5-(2-etoxietil)-n3-(2-piridinil)-3,5-piperidinodicarboxa mida para uso como inibidores de renina
JP5506776B2 (ja) 2008-03-25 2014-05-28 アフェクティス ファーマシューティカルズ アーゲー 新規ｐ２ｘ７ｒ拮抗薬及びその使用法
US8640466B2 (en) 2008-06-03 2014-02-04 Bsst Llc Thermoelectric heat pump
WO2010118921A1 (en) 2009-04-14 2010-10-21 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
JP5827627B2 (ja) * 2009-11-07 2015-12-02 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ＴＧＦ−β受容体キナーゼ阻害剤としてのヘテロアリールアミノキノリン
US20130331378A1 (en) * 2011-01-26 2013-12-12 Kissei Pharmaceutical Co., Ltd. Pyrazolopyridine derivative or pharmacologically acceptable salt thereof
WO2012110190A1 (en) 2011-02-17 2012-08-23 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
WO2012163456A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
WO2012163792A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
SMT201800613T1 (it) * 2011-12-16 2019-01-11 Poseida Therapeutics Inc Modulatori di trpc4 per uso nel trattamento o nella prevenzione del dolore
GB201321739D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
JP6483697B2 (ja) * 2013-12-09 2019-03-13 ユーシービー バイオファルマ エスピーアールエル Ｔｎｆ活性のモジュレーターとしての縮合二環式ヘテロ芳香族誘導体
UY36838A (es) * 2015-08-03 2017-01-31 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Compuestos heterocíclicos moduladores de la señalización de tnf alfa y composiciones farmacéuticas que los contienen
RS65335B1 (sr) 2018-10-05 2024-04-30 Annapurna Bio Inc Jedinjenja i kompozicije za lečenje stanja povezanih sa aktivnošću receptora apj
CN109439606B (zh) * 2018-11-14 2022-06-28 中国科学院青岛生物能源与过程研究所 一种提高间苯三酚产量的基因工程菌及其构建方法与应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5210079A (en) * 1988-01-07 1993-05-11 E. I. Du Pont De Nemours And Company Treatment of chronic renal failure with imidazole angiotensin-II receptor antagonists
DE4036706A1 (de) * 1990-11-17 1992-05-21 Hoechst Ag Verfahren zur behandlung der cardialen sowie der vasculaeren hypertrophie und hyperplasie
WO1995026188A1 (en) * 1994-03-29 1995-10-05 Merck & Co., Inc. Treatment of atherosclerosis with angiotensin ii receptor blocking imidazoles
GB9929979D0 (en) * 1999-12-17 2000-02-09 Darwin Discovery Ltd Hydroxamic acid derivatives
CZ20023033A3 (cs) 2000-03-17 2003-01-15 Bristol-Myers Squibb Pharma Company Deriváty cyklických beta-aminokyselin jako inhibitory matrixových metaloproteáz a TNF-alfa
EP1373199A4 (en) 2001-03-15 2004-04-07 Bristol Myers Squibb Pharma Co SPIROCYCLIC BETA-AMINOACID DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEINASES AND THE CONVERSION ENZYME OF TNF-ALPHA (TAGE)

Also Published As

Publication number Publication date
AU2002341715A1 (en) 2003-04-01
US20030139388A1 (en) 2003-07-24
EP1427408A4 (en) 2005-10-26
EP1427408A2 (en) 2004-06-16
WO2003024899A3 (en) 2003-11-27
US6740649B2 (en) 2004-05-25
WO2003024899A2 (en) 2003-03-27

Similar Documents

Publication Publication Date Title
AR036875A1 (es) Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa
RU2397168C2 (ru) Производные тиофена в качестве ингибиторов снк 1
AR052866A1 (es) Fenil-metanonas monociclicas sustituidas
AR073369A1 (es) Derivados de 2-carboxamida-cicloamino-urea como inhibidores de pi-3
AR057244A1 (es) Compuestos agonistas,antagonistas o agonistas inversos de receptores cb2,composiciones farmaceuticas que los contienen, metodos de preparacion y usos para tratar enfermedades inflamatorias y/o autoinmunes.
AR058077A1 (es) Derivados de acidos fenoxiaceticos
AR041260A1 (es) Piperazinas sustituidas por heterociclos para el tratamiento de la esquizofrenia
AR066043A1 (es) Derivados de benzamida sustituida como inhibidores de la 11-beta-hidroxi esteroide deshidrogenasa tipo 1(11betahsd1)
EA201000805A1 (ru) Бис-(сульфониламино)производные в терапии 066
UY30603A1 (es) Derivados de 2-aril-6-fenil-imidazo[1, 2-a]piridinas, su preparacion y su aplicacion en terapéutica
PE20091005A1 (es) N-(2-(hetaril)aril)arilsulfonamidas y n-(2-(hetaril)hetaril)arilsulfonamidas
AR086319A1 (es) Compuestos heterociclicos fusionados como moduladores de canal ionico
AR083367A1 (es) Compuestos de tipo quinazolinona como antagonistas de crth
EA201100482A1 (ru) Кристаллические формы 2-тиазолил-4-хинолинилоксипроизводного, активного ингибитора hcv
AR044152A1 (es) Derivados de alquilarilo, metodo de preparacion y uso para el tratamiento de la obesidad
CL2012000999A1 (es) Compuestos derivados de pirazoloespirocetona sustituida, inhibidores de acetil-coa carboxilasa; composicion farmaceutica que los comprende; uso para tratar o retrasar la progresion o el inicio de diabetes tipo 2, higado graso no alcoholico (hgna) o la resistencia hepatica a la insulina.
EA201071370A1 (ru) Серосодержащее гетероциклическое производное, обладающее активностью ингибитора бета-секретазы
AR081426A1 (es) Derivados de pirazol inhibidores del receptor sigma
CO6362007A2 (es) Derivados de azaspiranil-alquilcarbamatos de heterociclos de 5 eslabones, su preparación y su aplicación en terapeútica
EA201071019A1 (ru) Кристаллические формы производных фениламинопиримидина
AR044715A1 (es) Compuestos tipo amidas que inhiben la reabsorcion de las monoaminas
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
CR11208A (es) Derivados de pirimidina utiles para el tratamiento de condiciones inflamatorias o alergicas
CU20210006A7 (es) Derivados de fenil-n-quinolina y proceso para su preparación
UY29393A1 (es) Nuevos derivados de amidas, sales farmacéuticas aceptables, composiciones que los contienen, procedimientos de preparación y aplicaciones.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal