AR047448A1 - Compuestos derivados de acidos fosfinicos y fosfonicos que poseen actividad inhibitoria de serina proteasa y su uso en la preparacion de un medicamento para el tratamiento de trastornos mediados por la quimasa. - Google Patents

Compuestos derivados de acidos fosfinicos y fosfonicos que poseen actividad inhibitoria de serina proteasa y su uso en la preparacion de un medicamento para el tratamiento de trastornos mediados por la quimasa.

Info

Publication number
AR047448A1
AR047448A1 ARP050100230A ARP050100230A AR047448A1 AR 047448 A1 AR047448 A1 AR 047448A1 AR P050100230 A ARP050100230 A AR P050100230A AR P050100230 A ARP050100230 A AR P050100230A AR 047448 A1 AR047448 A1 AR 047448A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
group
optionally substituted
heteroaryl
Prior art date
Application number
ARP050100230A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR047448A1 publication Critical patent/AR047448A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32—Esters thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C07F9/5728—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/60—Quinoline or hydrogenated quinoline ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/62—Isoquinoline or hydrogenated isoquinoline ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
    • C07F9/65517—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring
    • C07F9/655354—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657181—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative

Landscapes

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

Abstract

Uso de estos compuestos en la preparacion de medicamentos para tratar trastornos mediados por al serina protreasa. Reivindicacion 1: Un compuesto de formula (1), en la cual: R1 se selecciona del grupo integrado por hidrogeno y alquilo C1-4; El circulo A se selecciona en forma independiente del grupo integrado por arilo, heteroarilo, heterociclilo fusionado con benzo, y cicloalquilo fusionado con benzo, opcionalmente sustituido con R2 y R3; R2 es uno a tres sustituyentes seleccionados en forma independiente del grupo integrado por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, metoxi, alcoxi C2-6, alquiltio C1-6, -OCF3, -NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), arilo, heteroarilo, ariloxi, heteroariloxi, halogeno, hidroxi y nitro; además, R2 es opcionalmente oxo cuando A es heteroarilo o heterociclilo; donde el arilo y ariloxi están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente del grupo integrado por alquilo C1-6, alcoxi C1-6, alquenilo C2- 6, alquiltio C1-6, -NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), arilo, heteroarilo, ariloxi, heteroariloxi, halogeno, hidroxi y nitro; donde los sustituyentes alquilo C1-6, alcoxi C2-6 y alquiltio C1-6 de R2 están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente del grupo integrado por -NR11R12, arilo, heteroarilo, uno a tres halogenos e hidroxi; donde R11 y R12 son sustituyentes seleccionados en forma independiente del grupo integrado por hidrogeno; alquilo C1-6 y arilo; donde el sustituyente alquilo C1-6 de R11 o R12 están sustituido opcionalmente con un sustituyente seleccionado de hidroxi, arilo, C(=O)alcoxi(C1-4) y -NR15R16; donde R15 y R16 son sustituyentes seleccionados en forma independiente del grupo integrado por hidrogeno, alquilo C1-6, y arilo, y dichos R15 y R16 se toman opcionalmente junto con los átomos a los cuales están unidos para formar un anillo de cinco a siete miembros; R3 es uno a tres sustituyentes seleccionados en forma independiente del grupo integrado por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alquiltio C1-6, -OCF3, -OCH2alquenilo(C2-6), -NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), -NHC(=O)Cy, -N(alquil C1-6)C(=O)Cy, -C(=O)alcoxi(C1-4), - C(=O)NR17R18, -C(=O)Nhcicloalquilo, -C(=O)N(alquil C1-6)cicloalquil-C(=O)NHCy, -C(=O)N(alquil C1-6)Cy, -C(=O)Cy, -OC(=O)NR19R20, -C(=O)Oarilo, -C(=O)Oheteroarilo, -CO2H, halogeno, hidroxi, nitro, ciano, arilo, heteroarilo, heteroariloxi y ariloxi; donde los sustituyentes alquilo C1-6, alcoxi C1-6 y alquiltio C1-6 de R3 están opcionalmente sustituidos con uno a tres sustituyentes seleccionados del grupo integrado por -NR21R22, -NH(cicloalquilo), -Nalquil(C1-6)cicloalquilo, -NHCy, -N(alquil C1- 6)Cy, arilo, heteroarilo, hidroxi, halogeno, -C(=O)NR23R24, -OC(=O)NR25R26, -C(=O)alcoxi(C1-4) y -C(=O)Cy; donde dichos R17, R18, R19, R20, R21, R22, R23, R24, R25, R26 son sustituyentes seleccionados en forma independiente del grupo integrado por hidrogeno, alquilo C1-6 y arilo, donde alquilo C1-6 está opcionalmente sustituidos con hidroxi, arilo, -C(=O)C1-4alcoxi, NH2, NH(alquilo C1-6) o -Ndialquilo(C1-6); y R17 y R18, R19 y R20, R21 y R22, R23 y R24 y R25 y R26 se toman opcionalmente junto con los átomos a los cuales están unidos para formar un anillo de cinco a siete miembros; Cy es un heterociclilo opcionalmente sustituido con un sustituyente seleccionado del grupo integrado por alquilo C1-6, alquil(C1-6)C(=O)alquilo(C1-6), alquil(C1-6)C(=O)alcoxi(C1-6), alquil(C1-6)C(=O)arilo, -C(=O)alquilo(C1-6), -C(=O)alcoxi(C1-6), -C(=O)arilo, -SO2arilo, arilo, heteroarilo y heterociclilo; donde arilo y la porcion arilo del alquil(C1-6)C(=O)arilo, C(=O)arilo y -SO2arilo está opcionalmente sustituido con uno a tres sustituyentes seleccionados en forma independiente del grupo integrado por alquilo C1-6, alcoxi C1-6, alquiltio C1-6, halogeno, hidroxi, NH2, NH(alquilo C1-6) y -Ndialquilo(C1-6); y donde heterociclilo está opcionalmente sustituido con arilo, uno a tres átomos de halogeno, o uno a tres sustituyentes oxo; y donde heterociclilo está opcionalmente espiro-fusionado a dicho Cy; y donde los sustituyentes alquenilo C1-6 y alquinilo C1-6 de R3 están opcionalmente sustituidos con arilo o -C(=O)NR27R28; donde dichos R27 y R28 son sustituyentes seleccionados en forma independiente del grupo integrado por hidrogeno, alquilo C1-6 y arilo, donde alquilo está sustituido opcionalmente con hidroxi, arilo, -C(=O)alcoxi C1-4, NH2, NH(alquilo C1-6) o -Ndialquilo(C1-6); y R27 y R28 se toman opcionalmente junto con los átomos a los cuales están unidos para formar un anillo de cinco a siete miembros; y donde los sustituyentes arilo, heteroarilo y cicloalquilo de R3 están opcionalmente sustituidos con uno a tres sustituyentes seleccionados en forma independiente de R14; donde R14 es uno a tres sustituyentes seleccionados en forma independiente del grupo integrado por hidrogeno, alquilo C1-6, alcoxi C1-6, alquenilo C2-6, alquiltio C1-6, -NH2, -NH(alquilo C1-6), -Ndialquilo(C1-6), arilo, heteroarilo, ariloxi, heteroariloxi, halogeno, hidroxi y nitro; donde los sustituyentes alquilo C1-6, alcoxi C1-6 y alquiltio C1-6 de R14 están opcionalmente sustituidos sobre un átomo de carbono terminal con un sustituyente seleccionado de -NR29R30, arilo, heteroarilo, uno a tres átomos de halogeno o hidroxi; donde dichos R29 y R30 son sustituyentes seleccionados en forma independiente del grupo integrado por hidrogeno; alquilo C1-6 y arilo; donde el alquilo C1-6 está opcionalmente sustituido con hidroxi, arilo, -C(=O)alcoxi C1-4, NH2, NH(alquilo C1-6) o -Ndialquilo(C1-6); y R29 y R30 se toman opcionalmente junto con los átomos a los cuales están unidos para formar un anillo de cinco a siete miembros; n es 0 o 1; W es O o S; X es hidrogeno o alquilo C1-3; Y se selecciona en forma independiente del grupo integrado por alquilo C1-6; SO3H, CO2H, heteroarilo, -OC(=O)NH2 y P(=O)OR5R6; donde alquilo está sustituido con un sustituyente seleccionado del -OSO2NH2 o hidroxi; y siempre que cuando Y es CO2H, A y Z deben ser ambos sistemas anulares bicíclicos; R5 se selecciona en forma independiente de hidrogeno; alquilo C1-6 o arilo; donde alquilo está opcionalmente sustituido con un sustituyente seleccionado del grupo integrado por NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), uno a tres átomos de halogenos e hidroxi; y donde el arilo está opcionalmente sustituido con un sustituyente seleccionado en forma independiente de hidrogeno, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquenilo, -NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), arilo, heteroarilo, ariloxi, heteroariloxi, halogeno, hidroxi, o nitro; R6 se selecciona en forma independiente del grupo integrado por alquilo C1-8, alquenilo C2-8, heteroarilo, arilo e hidroxi; donde alquilo C1-8 y alquenilo C2-8 están opcionalmente sustituidos con un sustituyentes seleccionados del grupo integrado por alcoxi C1-6, arilo, heterociclilo, heteroarilo, NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), uno a tres átomos de halogeno e hidroxi; con la condicion de que cuando R6 es alquilo C1-8, el alquilo C1-8 está opcionalmente sustituido con uno a cuatro átomos de halogeno adicionales, donde uno a tres de los átomos de halogeno son opcionalmente cloro y uno a siete de los átomos de halogeno son opcionalmente fluor; donde los sustituyentes heteroarilo y arilo de R6 están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente del grupo integrado por alquilo C1-6, alcoxi C1-6, alquenilo C2-6, alquiltio C1-6, -NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), arilo, heteroarilo, ariloxi, heteroariloxi, halogeno, hidroxi y nitro; Z es un sistema anular monocíclico o policíclico de siete a quince miembros seleccionado del grupo integrado por arilo, heteroarilo, heterociclilo fusionado con benzo o cicloalquilo fusionado con benzo, opcionalmente sustituido con R4; es uno a tres sustituyentes seleccionados del grupo integrado por alquilo C1-6, alquenilo C1-6, alcoxi C1-6, alquiltio C1-6, arilalquilo C1-6, arilalquenilo C2-6, halogeno, -C(=O)Cy, -C(=O)NR31R32, arilo, -CO2H, oxo y ciano; donde el alquilo C1-6, alquenilo C1-6 y alcoxi C1-6 están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente de -NR33R34, arilo, heteroarilo, cicloalquilo, uno a tres átomos de halogeno o hidroxi; donde el arilo y heteroarilo están opcionalmente sustituidos con un sustituyente seleccionado en forma independiente del grupo integrado por alquilo C1-6, alcoxi C1-6, alquenilo C2-6, alquiltio C1-6, -NH2, -NHalquilo(C1-6), -Ndialquilo(C1-6), arilo, heteroarilo, ariloxi, heteroariloxi, uno a tres átomos de halogeno, hidroxi y nitro; donde dichos R31, R32, R33 y R34 son sustituyentes seleccionado en forma independiente del grupo integrado por hidrogeno, alquilo C1-6 y arilo, donde alquilo está opcionalmente sustituido con hidroxi, arilo, - C(=O)C1-4alcoxi, NH2, NH(alquilo C1-6) o -Ndialquilo(C1-6); y R31 con R32, y R33 con R34 se toman opcionalmente junto con los átomos a los cuales están unidos para formar un anillo de cinco a siete miembros; y sus sales aceptables para uso farmacéutico.
ARP050100230A 2004-01-23 2005-01-21 Compuestos derivados de acidos fosfinicos y fosfonicos que poseen actividad inhibitoria de serina proteasa y su uso en la preparacion de un medicamento para el tratamiento de trastornos mediados por la quimasa. AR047448A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US53866304P 2004-01-23 2004-01-23

Publications (1)

Publication Number Publication Date
AR047448A1 true AR047448A1 (es) 2006-01-18

Family

ID=34826001

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050100230A AR047448A1 (es) 2004-01-23 2005-01-21 Compuestos derivados de acidos fosfinicos y fosfonicos que poseen actividad inhibitoria de serina proteasa y su uso en la preparacion de un medicamento para el tratamiento de trastornos mediados por la quimasa.

Country Status (24)

Country Link
US (2) US7459444B2 (es)
EP (1) EP1716160B1 (es)
JP (1) JP5022711B2 (es)
KR (1) KR101182143B1 (es)
CN (2) CN101863923B (es)
AR (1) AR047448A1 (es)
AT (1) ATE493421T1 (es)
AU (1) AU2005207856B2 (es)
BR (1) BRPI0507052A (es)
CA (1) CA2554205C (es)
CR (1) CR8563A (es)
DE (1) DE602005025600D1 (es)
EA (1) EA011745B1 (es)
EC (1) ECSP066721A (es)
ES (1) ES2357013T3 (es)
HK (1) HK1148753A1 (es)
IL (1) IL177037A (es)
MX (1) MXPA06008375A (es)
NO (1) NO20063647L (es)
NZ (1) NZ548684A (es)
SG (1) SG149880A1 (es)
TW (1) TW200539881A (es)
WO (1) WO2005073214A2 (es)
ZA (1) ZA200607024B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100048513A1 (en) 2008-08-20 2010-02-25 Hawkins Michael J Novel inhibitors of chymase
KR101278522B1 (ko) 2004-12-02 2013-06-25 다이이찌 산쿄 가부시키가이샤 7원환 화합물 및 그 제조법 및 의약 용도
AU2007207749A1 (en) * 2006-01-12 2007-07-26 Janssen Pharmaceutica N.V. Processing of SLPI by chymase
WO2007134107A2 (en) 2006-05-10 2007-11-22 Janssen Pharmaceutica N.V. Cold menthol receptor-1 antagonists
US8629281B2 (en) 2011-01-14 2014-01-14 Janssen Pharmaceutica, Nv Cold menthol receptor-1 antagonists
CN101495463B (zh) 2006-05-31 2012-08-15 第一三共株式会社 7-元环化合物、其制备方法和药物用途
CA2666658C (en) * 2006-10-06 2015-01-20 Boehringer Ingelheim International Gmbh Chymase inhibitors
CA2666780A1 (en) * 2006-10-18 2008-04-24 Janssen Pharmaceutica, N.V. Novel inhibitors of chymase
UY30648A1 (es) * 2006-10-20 2008-05-02 Janssen Pharmaceutica Nv Formas salinas de compuestos de benzotienilo sustituido
US20080287398A1 (en) * 2007-05-02 2008-11-20 Colburn Raymond W Cold menthol receptor-1 antagonists
TW200932752A (en) * 2007-10-16 2009-08-01 Janssen Pharmaceutica Nv Process for synthesizing phosphonic and phosphinic acid compounds
WO2009102384A2 (en) * 2007-12-21 2009-08-20 Molecular Insight Pharmaceuticals, Inc. Radiolabeled derivatives of potent chymase inhibitors
FR2934267B1 (fr) * 2008-07-23 2010-08-13 Pharmaleads Derives aminophosphiniques utiles dans le traitement de la douleur
WO2010051372A1 (en) * 2008-10-29 2010-05-06 Janssen Pharmaceutica Nv Process for the preparation of chymase modulators
JP5587914B2 (ja) 2009-01-30 2014-09-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング キマーゼ阻害剤として有用なアザキナゾリンジオン
WO2010101967A2 (en) * 2009-03-04 2010-09-10 Idenix Pharmaceuticals, Inc. Phosphothiophene and phosphothiazole hcv polymerase inhibitors
JP5676480B2 (ja) 2009-12-25 2015-02-25 第一三共株式会社 ７員環化合物並びにその医薬用途
US8558011B2 (en) 2010-08-31 2013-10-15 Janssen Pharmaceutica, Nv Cold menthol receptor-1 antagonists
CN106467515B (zh) * 2015-08-18 2019-09-24 宁波洞密生物科技有限公司 一类6-吡啶苯并咪唑吲哚衍生物及其制备方法与医药领域的应用
CN107573263B (zh) * 2017-08-14 2020-04-07 大连理工大学 一种ω-取代缩二脲类化合物的合成方法
CN108383875B (zh) * 2018-03-22 2020-04-28 昆明学院 一种银催化的3-膦酰甲基吲哚啉及制备方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1399089A (en) 1971-05-14 1975-06-25 Glaxo Lab Ltd Carboxylic acids and derivatives thereof
FR2713637B1 (fr) * 1993-12-15 1996-01-05 Cird Galderma Nouveaux composés bi-aromatiques dérivés d'amide, compositions pharmaceutiques et cosmétiques les contenant et utilisations.
US5508273A (en) * 1993-12-30 1996-04-16 Ortho Pharmaceutical Corporation Substituted phosphonic acids and derivatives useful in treating bone wasting diseases
JP4009460B2 (ja) * 2000-03-14 2007-11-14 アクテリオン ファマシューティカルズ リミテッド １，２，３，４−テトラヒドロイソキノリン誘導体
US6852734B2 (en) * 2000-05-02 2005-02-08 Meiji Seika Kaisha, Ltd. Indole derivatives exhibiting chymase-inhibitory activities and process for preparation thereof

Also Published As

Publication number Publication date
WO2005073214A3 (en) 2005-10-20
CA2554205C (en) 2013-08-27
JP5022711B2 (ja) 2012-09-12
NO20063647L (no) 2006-10-19
ES2357013T3 (es) 2011-04-15
IL177037A0 (en) 2006-12-10
CN1934120A (zh) 2007-03-21
IL177037A (en) 2013-05-30
CN1934120B (zh) 2010-05-26
EP1716160A2 (en) 2006-11-02
SG149880A1 (en) 2009-02-27
US20090036409A1 (en) 2009-02-05
ZA200607024B (en) 2010-02-24
EP1716160B1 (en) 2010-12-29
EA200601358A1 (ru) 2007-02-27
AU2005207856B2 (en) 2011-07-14
NZ548684A (en) 2009-04-30
CN101863923B (zh) 2013-04-24
US20050176769A1 (en) 2005-08-11
ATE493421T1 (de) 2011-01-15
US7459444B2 (en) 2008-12-02
DE602005025600D1 (de) 2011-02-10
JP2007518807A (ja) 2007-07-12
BRPI0507052A (pt) 2007-06-12
AU2005207856A1 (en) 2005-08-11
CR8563A (es) 2009-01-14
TW200539881A (en) 2005-12-16
CN101863923A (zh) 2010-10-20
WO2005073214A2 (en) 2005-08-11
KR101182143B1 (ko) 2012-09-13
ECSP066721A (es) 2006-10-31
HK1148753A1 (en) 2011-09-16
CA2554205A1 (en) 2005-08-11
MXPA06008375A (es) 2007-03-21
EA011745B1 (ru) 2009-06-30
KR20060129401A (ko) 2006-12-15

Similar Documents

Publication Publication Date Title
AR047448A1 (es) Compuestos derivados de acidos fosfinicos y fosfonicos que poseen actividad inhibitoria de serina proteasa y su uso en la preparacion de un medicamento para el tratamiento de trastornos mediados por la quimasa.
AR049126A1 (es) Derivados de 5, 6, 7, 8 - tetrahidroimidazo[1,5a]piridina con actividad inhibitoria de la aldosterona sintasa, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento del hiperaldosterismo y del sindrome de cushing.
PE20090042A1 (es) Analogos de ciclopamina
JP2016505012A5 (es)
AR032467A1 (es) Derivados de piridina, procedimiento para prepararlos, el uso de dichos derivados para la preparacion de medicamentos y los medicamentos que contienen dichos derivados
AR038240A1 (es) Compuesto de piperidina, uso del mismo para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para su preparacion
AR032353A1 (es) Compuestos derivados biciclicos sustituidos para el tratamiento del crecimiento celular anormal y su uso en la fabricacion de medicamentos y composicion farmaceutica que los contiene
AR058287A1 (es) Derivados de isoquinolina y composicion farmaceutica
ES2722048T3 (es) Compuestos de triazolopirimidina y usos de los mismos
PE20080769A1 (es) Derivados de biaril-sulfonamida
AR061737A1 (es) Compuestos derivados de pirimidina, un peoceso para su preparacion y composiciones farmaceuticas que los contienen
AR079689A1 (es) Derivados de imidazo[1,2a]piridina, composiciones farmaceuticas que los comprenden y uso de los mismos en trastornos mieloproliferativos, leucemia y enfermedades inmunologicas e inflamatorias.
AR046600A1 (es) Diazaespiroalcanos y su uso como tratamiento para enfermedades mediadas por ccr8
AR074226A1 (es) Octahidrociclopenta[c]pirrol-4-aminas sustituidas como bloqueantes de los canales de calcio, composiciones farmaceuticas que las comprenden y el uso de las mismas para el tratamiento del dolor.
AR067443A1 (es) Derivados heterociclicos de n-benziloxazolidinonas potenciadores de receptores de glutamato mglur2, composiciones farmaceuticas que los contienen y usos de los mismos en el tratamiento de trastornos del sistema nervioso central
AR062224A1 (es) Tetrazolilos macrociclicos como inhibidores de serina proteasa ns3 del virus de hepatitis c y composiciones farmaceuticas que los comprenden.
AR064304A1 (es) Formulaciones de ansamicina y sus metodos de uso
AR036032A1 (es) Compuesto derivado de quinolina, composicion que lo comprende; uso del mismo en la fabricacion de medicamentos, proceso para prepararlo, y metodo para detectar y seleccionar un agente que module la actividad del mif
AR035260A1 (es) Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer
AR083849A1 (es) Antagonistas de mdm2 de espiro-oxindol
AR057716A1 (es) Inhibidores de las serina proteasas y composiciones farmaceuticas
AR057959A1 (es) 5-pirazolpiperidinas-(sustituidas)
PE20100737A1 (es) Nuevos compuestos
PE20080182A1 (es) Derivados pirrolo-quinoxalinona como antibacterianos
AR056470A1 (es) Sulfonamidos n- ciclicos puenteados inhibidores de gamma secretasa

Legal Events

Date Code Title Description
FA Abandonment or withdrawal