AR040251A1 - Compuestos de ariloximas como inhibidores de la fosfodiesterasa iv. su uso para el tratamiento del asma, alergia, inflamacion, enfermedades autoinmunes o enfermedades miocardicas - Google Patents

Compuestos de ariloximas como inhibidores de la fosfodiesterasa iv. su uso para el tratamiento del asma, alergia, inflamacion, enfermedades autoinmunes o enfermedades miocardicas

Info

Publication number
AR040251A1
AR040251A1 ARP030102023A ARP030102023A AR040251A1 AR 040251 A1 AR040251 A1 AR 040251A1 AR P030102023 A ARP030102023 A AR P030102023A AR P030102023 A ARP030102023 A AR P030102023A AR 040251 A1 AR040251 A1 AR 040251A1
Authority
AR
Argentina
Prior art keywords
inhibitors
group
replaced
antagonists
hydrochloride
Prior art date
Application number
ARP030102023A
Other languages
English (en)
Inventor
Eggenweiler Hans-Michael Dr
Beier Norbert Dr
Schelling Pierre Dr
Wolf Michael Dr
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR040251A1 publication Critical patent/AR040251A1/es

Links

Classifications

    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/06—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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/06—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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biotechnology (AREA)
  • Ophthalmology & Optometry (AREA)
  • AIDS & HIV (AREA)

Abstract

Reivindicación 1: Compuestos de la fórmula (1) donde R1, R2 son en cada caso, independientemente entre sí: H, OH, OR8, -SR8, -SOR8, -SO2R8 o Hal; R1 y R2 también son juntos -OCH2O-, u -OCH2CH2O-; R3 es H, A''R7, COA''R7, COOA''R7, CONH2, CONHA''R7, CON(A''R7)(A'''R7), CONR10Het, NH2, NHA''R7, N(A''R7)(A'''R7), NCOA''R7 o NCOOA''R7; B es un radical isocíclico o heterocíclico aromático, que puede estar insustituido o mono, di o tri sustituido por R4, R5 y/o R6; X es alquileno C1-10 o alquenileno C2-8, donde 1, 2, o 3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NA''R7, 1-7 átomos de H pueden estar reemplazados por F y/o Cl; R4, R5, R6 son en cada caso, independientemente entre sí, H, A''R7, OH, OA''R7, NO2, NH2, NHA''R7, N(A''R7)(A'''R7), NHCOA''R7, NHCOOA''R7, NHCONH2, NHCONHA''R7, NHCON(A''R7)(A'''R7), Hal, COOH, COOA''R7, CONH2, CONHA''R7, CON(A''R7)(A'''R7), o como se muestra en el grupo de fórmulas (2); R7 es H, COOH, COOA, CONH2, CONHA, CONAA', NH2, NHA, NAA', NCOA, NCOOA, OH u OA; R8 es A, cicloalquilo C3-7, alquilen-cicloalquilo(C4-8) o alquenilo C2-8; R9 es alquilo C1-10, cicloalquilo C3-7, alquilencicloalquilo C4-8 o alquenilo C2-8, donde 1, 2, o 3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe, NEt y/o por grupos -CH=CH, 1-7 átomos de H pueden estar reemplazados por F y/o Cl y/o 1 átomo de H puede estar reemplazado por R7; Y es alquileno C1-10 o alquenileno C2-8, donde 1, 2 o 3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; A, A' son en cada caso, independientemente entre sí, alquilo C1-10 o alquenilo C2-8, donde 1, 2 o 3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl, o arilo o Het, A y A' también son juntos una cadena de alquileno C2-7, donde 1, 2, o 3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR9, NCOR9 o NCOOR9; A'', A''' en cada caso, independientemente entre sí, están ausentes, son alquileno C1-10, alquenileno C2-8 o cicloalquileno C3-7, donde 1, 2, o 3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; A'' y A''' también son juntos una cadena de alquileno C2-7, donde 1, 2 o 3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR9, NCOR9 o NCOOR9; arilo es fenilo, naftilo, fluorenilo o bifenilo insustituido o mono, di o trisustituido por Hal, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2A, COR10, SO2N(R10)2, S(O)mR11; R10 es H o alquilo C1-6; R11 es alquilo C1-6; Het es un heterociclo mono o bicíclico saturado, no saturado o aromático con 1 a 2 átomos de N, O y/o S, que puede estar insustituido o mono o disustituido por el O del carbonilo, Hal, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2R11, COR10, SO2NR10 y/o S(O)mR11; Hal es F, Cl, Br, o I; m es 0, 1 ó 2, así como los derivados, solvatos, estereoisómeros e isómeros E/Z de los mismos de uso farmacéutico, incluyendo las mezclas de los mismos en todas las proporciones. Reivindicación 16: Medicamento que comprende al menos un compuesto de la fórmula (1) de acuerdo con una o varias de las reivindicaciones 1 a 13 y/o los derivados, solvatos, estereoisómeros e isómeros E/Z de los mismos de uso farmacéutico, incluyendo las mezclas de los mismos en todas las proporciones y, opcionalmente, excipientes y/o auxiliares. Reivindicación 17: Uso de compuestos de la fórmula (1) de acuerdo con una o varias de la reivindicaciones 1 a 13 y/o las sales o solvatos fisiológicamente aceptables de los mismos para preparar un medicamento para tratar a un paciente que padece de una enfermedad o condición mediada por la isoenzima PDE IV en su papel de regular la activación y desgranulación de los eosinófilos humanos. Reivindicación 24: Combinación de un compuesto de acuerdo con las reivindicaciones 1 a 13 junto con uno o más miembros del siguiente grupo: (a) inhibidores de la biosíntesis de leucotrieno: inhibidores de 5-lipoxigenasa (5-LO) y antagonistas de la proteína activadora de 5-lipoxigenasa (FLAP) seleccionados del grupo formado por zileuton, ABT-761, fenleuton, tepoxalina, Abbott-79175, Abbott-85761, tiofen-2-alquilsulfonamidas N-(5-sustituidas), 2,6-di-ter-butilfenolhidrazonas, Zeneca ZD-2138, SB-210661, compuesto 2-cianonaftaleno sustituido con piridinilo L-739.010, compuesto 2-cianoquinolina L-746.530, compuestos indol y quinolina MK-591, MK-886 y BAY x 1005; (b) antagonistas del receptor de los leucotrienos LTB4, LTC4, LTD4, y LTE4 seleccionados del grupo formado por la clase de compuestos fenotiazin-3-ona L-651.392, compuesto amidino CGS-25019c, compuesto benzoxaolamina ontazolast, compuesto bencencarboximidamida BILL 284/260, compuestos zafirlukast, ablukast, montelukast, pranlukast, verlukast (MK-679), RG-12525, Ro-245913, iralukast (CGP 45715A) y BAY x 7195; (c) inhibidores de PDE IV; (d) inhibidores de 5-lipoxigenasa (5-LO); antagonistas de la proteína activadora de 5-lipoxigenasa (FLAP); (e) inhibidores dobles de 5-lipoxigenasa (5-LO) y antagonistas del factor activador de plaquetas (PAF); (f) antagonistas de leucotrieno (LTRAs) incluyendo antagonistas de LTB4, LTC4, LTD4 y LTE4; (g) antagonistas del receptor H1 antihistamínico incluyendo cetirizina, loratadina, desloratadina, fexofenadina, astemizol, azelastina y clorfeniramina; (h) antagonistas del receptor H2 gastroprotector; (i) agentes simpaticomimeticos vasoconstrictores agonistas de los adrenoceptores a1 y a2 administrados por vía oral o tópica como descongestivos del grupo que consiste en propilhexedrina, fenilefrina, fenilpropanolamina, pseudoefedrina, clorhidrato de nafazolina, clorhidrato de oximetazolina, clorhidrato de tetrahidrozolina, clorhidrato de xilometazolina y clorhidrato de etilnorepinefrina; (j) uno o más agonistas de los adrenoceptores a1 y a2 tal como se mencionó anteriormente en el punto (i) en combinación con uno o más inhibidores de 5-lipoxigenasa (5-LO) tal como se enumeró con anterioridad en el punto (a); (k) agentes anticolinérgicos incluyendo bromuro de ipratropio, bromuro de tiotropio, bromuro de oxitropio, pirenzepina y telenzepina; (l) agonistas de los adrenoceptores b1 a b4 seleccionados del grupo que consiste en etaproterenol, isoproterenol, isoprenalina, albuterol, salbutamol, formoterol, salmeterol, terbutalina, orciprenalina, bitolterol y pirbuterol; (m) teofilina y aminofilina; (n) cromoglicato de sodio; (o) antagonistas de los receptores muscarínicos (M1, M2 y M3); (p) inhibidores de COX-1 (NSAIDs) y NSAIDs de óxido nítrico; (q) inhibidores selectivos de COX-2; (r) miméticos del factor de crecimiento de tipo insulina tipo 1 (IGF-1); (s) ciclesonida; (t) glucocorticoides inhalados con efectos colaterales sistémicos reducidos del grupo prednisona, prednisolona, flunisolida, triamcinolonacetonida, dipropionato de beclometasona, budesonida, propionato de fluticasona y furoato de mometasona; (u) inhibidores de triptasa; (v) antagonistas del factor activador de plaquetas (PAF); (w) anticuerpos monoclonales activos contra agentes inflamatorios endógenos; (x) IPL 576; (y) agentes del factor de necrosis antitumoral (TNFa) del grupo etanercept, infliximab y D2E7; (z) DMARDs seleccionados del grupo que consiste en leflunomida; (aa) péptidos TCR, (bb) inhibidores de la enzima convertidora de interleuquinas (ICE); (cc) inhibidores de IMPDH; (dd) inhibidores de moléculas de adhesión incluyendo antagonistas de VLA-4; (ee) catepsinas; (ff) inhibidores de MAP quinasa; (gg) inhibidores de la glucosa-6-fosfato deshidrogenasa; (hh) antagonistas de los receptores de quinina B1 y B2; (ii) oro en la forma de un grupo aurotio junto con numerosos grupos hidrofílicos; (jj) agentes inmunosupresores del grupo ciclosporina, azatioprina y metotrexato; (kk) agentes anti-gota del grupo colchicinas; (ll) inhibidores de xantina oxidasa del grupo alopurinol; (mm) agentes uricosúricos del grupo probenecida, sulfinpirazona y benzbromarona; (nn) agentes antineoplásicos que son drogas antimitóticas del grupo vinblastina y vincristina; (oo) secretagogos de la hormona de crecimiento; (pp) inhibidores de las metaloproteasas de matriz (MMPs) del grupo estromelisinas, colagenasas, gelatinasas, agrecanasa, colagenasa-1 (MMP-1), colagenasa-2 (MMP-8), colagenasa-3 (MMP-13), estromelisina-1 (MMP-3), estromelisina-2 (MMP-10) y estromelisina-3 (MMP-11); (qq) factor de crecimiento y transformación (TGFb); (rr) factor de crecimiento derivado de plaquetas (PDGF); (ss) factor de crecimiento de fibroblastos del grupo factor de crecimiento de fibroblastos básico (bFGF); (tt) factor estimulante de colonias de macrófagos-granulocitos (GM-CSF); (uu) capsaicina; (vv) antagonistas del receptor de taquiquinina NK1 y NK3 del grupo NKP-608C, SB233412 (talnetant) y D-4418; (ww) inhibidores de elastasa del grupo UT-77 y ZD-0892; y (xx) agonistas del receptor de adenosina A2a.
ARP030102023A 2002-06-10 2003-06-06 Compuestos de ariloximas como inhibidores de la fosfodiesterasa iv. su uso para el tratamiento del asma, alergia, inflamacion, enfermedades autoinmunes o enfermedades miocardicas AR040251A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10225574A DE10225574A1 (de) 2002-06-10 2002-06-10 Aryloxime

Publications (1)

Publication Number Publication Date
AR040251A1 true AR040251A1 (es) 2005-03-23

Family

ID=29557700

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030102023A AR040251A1 (es) 2002-06-10 2003-06-06 Compuestos de ariloximas como inhibidores de la fosfodiesterasa iv. su uso para el tratamiento del asma, alergia, inflamacion, enfermedades autoinmunes o enfermedades miocardicas

Country Status (17)

Country Link
US (2) US7135471B2 (es)
EP (1) EP1511737B1 (es)
JP (1) JP4607582B2 (es)
KR (1) KR20050008817A (es)
CN (1) CN1659148A (es)
AR (1) AR040251A1 (es)
AT (1) ATE457980T1 (es)
AU (1) AU2003240259B2 (es)
BR (1) BR0311311A (es)
CA (1) CA2488934C (es)
DE (2) DE10225574A1 (es)
ES (1) ES2339646T3 (es)
MX (1) MXPA04012211A (es)
PL (1) PL371920A1 (es)
RU (1) RU2004139233A (es)
WO (1) WO2003104205A1 (es)
ZA (1) ZA200500134B (es)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
GB0401334D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
GB0411056D0 (en) 2004-05-18 2004-06-23 Novartis Ag Organic compounds
GT200500281A (es) 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
GB0424284D0 (en) 2004-11-02 2004-12-01 Novartis Ag Organic compounds
GB0426164D0 (en) 2004-11-29 2004-12-29 Novartis Ag Organic compounds
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
US7910708B2 (en) 2005-10-21 2011-03-22 Novartis Ag Anti-IL13 human antibodies
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
GB0601951D0 (en) 2006-01-31 2006-03-15 Novartis Ag Organic compounds
KR20080110925A (ko) 2006-04-21 2008-12-19 노파르티스 아게 아데노신 ａ２ａ 수용체 효능제로서 사용하기 위한 퓨린 유도체
DE602007013441D1 (de) 2006-09-29 2011-05-05 Novartis Ag Pyrazolopyrimidine als pi3k-lipidkinasehemmer
CA2667962A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
US7978848B2 (en) * 2007-01-09 2011-07-12 Microsoft Corporation Content encryption schema for integrating digital rights management with encrypted multicast
DE602007011670D1 (de) 2007-01-10 2011-02-10 Irm Llc Verbindungen und zusammensetzungen als kanal-aktivierende proteasehemmer
BRPI0811562A2 (pt) 2007-05-07 2014-12-09 Novartis Ag Compostos orgânicos
WO2009061516A1 (en) * 2007-11-08 2009-05-14 New York University School Of Medicine Medical implants containing adenosine receptor agonists and methods for inhibiting medical implant loosening
EP2231280B1 (en) 2007-12-10 2016-08-10 Novartis AG Amiloride-like Pyrazine-carboxamides as ENaC blockers
PL2231642T3 (pl) 2008-01-11 2014-04-30 Novartis Ag Pirymidyny jako inhibitory kinazy
US8236808B2 (en) 2008-06-10 2012-08-07 Novartis Ag Pyrazine derivatives as ENAC blockers
PT2391366E (pt) 2009-01-29 2013-02-05 Novartis Ag Benzimidazoles substituídos para o tratamento de astrocitomas
AR077215A1 (es) * 2009-06-24 2011-08-10 Boehringer Ingelheim Int Derivados de piperidina, composiciones farmaceuticas y metodos relacionados con ellos
WO2010149685A1 (en) * 2009-06-24 2010-12-29 Boehringer Ingelheim International Gmbh New compounds, pharmaceutical composition and methods relating thereto
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
EP2464649A1 (en) 2009-08-12 2012-06-20 Novartis AG Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation
NZ598220A (en) 2009-08-17 2014-02-28 Intellikine Llc Heterocyclic compounds and uses thereof
CA2771432A1 (en) 2009-08-20 2011-02-24 Novartis Ag Heterocyclic oxime compounds
CA2777245A1 (en) 2009-10-22 2011-04-28 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
US10309974B2 (en) 2010-11-12 2019-06-04 Cedars-Sinai Medical Center Citrullinated proteins: a post-translated modification of myocardial proteins as marker of physiological and pathological disease
JP5701994B2 (ja) * 2010-11-12 2015-04-15 ザ・ジョンズ・ホプキンス・ユニバーシティー シトルリン化タンパク質：生理学的および病理学的疾患のマーカーとしての心筋タンパク質の翻訳後修飾
JP2014505088A (ja) 2011-02-10 2014-02-27 ノバルティス アーゲー Ｃ−ＭＥＴチロシンキナーゼ阻害剤としての［１，２，４］トリアゾロ［４，３−ｂ］ピリダジン化合物
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン， エルエルシー 複素環化合物およびその使用
US9102671B2 (en) 2011-02-25 2015-08-11 Novartis Ag Compounds and compositions as TRK inhibitors
UY34305A (es) 2011-09-01 2013-04-30 Novartis Ag Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar
UY34329A (es) 2011-09-15 2013-04-30 Novartis Ag Compuestos de triazolopiridina
EP2755652B1 (en) 2011-09-16 2021-06-02 Novartis AG N-substituted heterocyclyl carboxamides
WO2013038373A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
ES2558457T3 (es) 2011-09-16 2016-02-04 Novartis Ag Compuestos heterocíclicos para el tratamiento de fibrosis quística
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
WO2013038378A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
US9174994B2 (en) 2011-11-23 2015-11-03 Intellikine, Llc Enhanced treatment regimens using mTor inhibitors
US8809340B2 (en) 2012-03-19 2014-08-19 Novartis Ag Crystalline form
CN104245701A (zh) 2012-04-03 2014-12-24 诺华有限公司 有酪氨酸激酶抑制剂的组合产品和其应用
US9433680B2 (en) 2013-01-31 2016-09-06 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US8778365B1 (en) 2013-01-31 2014-07-15 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US9446131B2 (en) 2013-01-31 2016-09-20 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US9452173B2 (en) 2013-01-31 2016-09-27 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
EP2968340A4 (en) 2013-03-15 2016-08-10 Intellikine Llc COMBINING KINASE INHIBITORS AND USES THEREOF
TW201605450A (zh) 2013-12-03 2016-02-16 諾華公司 Ｍｄｍ２抑制劑與ＢＲＡＦ抑制劑之組合及其用途
WO2015162456A1 (en) 2014-04-24 2015-10-29 Novartis Ag Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors
JP6433509B2 (ja) 2014-04-24 2018-12-05 ノバルティス アーゲー ホスファチジルイノシトール３−キナーゼ阻害薬としてのアミノピラジン誘導体
BR112016023967A2 (pt) 2014-04-24 2017-08-15 Novartis Ag derivados de pirazina como inibidores de fosfatidilinositol 3-cinase
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
KR20170036037A (ko) 2014-07-31 2017-03-31 노파르티스 아게 조합 요법
EP3268085A4 (en) 2015-03-13 2018-10-31 The Board of Trustees of The Leland Stanford Junior University Ltb4 inhibition to prevent and treat human lymphedema
EP3311176A4 (en) 2015-06-18 2019-03-13 Cedars-Sinai Medical Center ROLE OF CITRULLINATION IN THE DIAGNOSIS OF ILLNESSES
CN107286101B (zh) * 2017-07-27 2020-04-21 云南大学 1-芳醛肟尿嘧啶及其制备方法
US20200383960A1 (en) 2019-06-10 2020-12-10 Novartis Ag Pyridine and Pyrazine derivative for the Treatment of CF, COPD, and Bronchiectasis
JP2022547427A (ja) 2019-08-28 2022-11-14 ノバルティス アーゲー 置換１，３－フェニルヘテロアリール誘導体及び疾患の治療におけるその使用
TW202140550A (zh) 2020-01-29 2021-11-01 瑞士商諾華公司 使用抗ｔｓｌｐ抗體治療炎性或阻塞性氣道疾病之方法
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
CN117558997B (zh) * 2024-01-11 2024-04-02 河南鑫泉能源科技有限公司 一种锂离子电池电解液及其制备方法与电池

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19632549A1 (de) 1996-08-13 1998-02-19 Merck Patent Gmbh Arylalkanoylpyridazine
DE19826841A1 (de) * 1998-06-16 1999-12-23 Merck Patent Gmbh Arylalkanoylpyridazine
DE19915364A1 (de) * 1999-04-06 2000-10-12 Merck Patent Gmbh Verwendung von Arylalkanoylpyridazinen

Also Published As

Publication number Publication date
RU2004139233A (ru) 2005-09-10
CA2488934C (en) 2011-10-11
KR20050008817A (ko) 2005-01-21
MXPA04012211A (es) 2005-02-25
JP2005533050A (ja) 2005-11-04
ATE457980T1 (de) 2010-03-15
ZA200500134B (en) 2005-07-06
AU2003240259B2 (en) 2009-02-19
DE50312422D1 (en) 2010-04-01
WO2003104205A1 (de) 2003-12-18
CN1659148A (zh) 2005-08-24
EP1511737A1 (de) 2005-03-09
AU2003240259A1 (en) 2003-12-22
US7135471B2 (en) 2006-11-14
CA2488934A1 (en) 2003-12-18
JP4607582B2 (ja) 2011-01-05
ES2339646T3 (es) 2010-05-24
US20060205708A1 (en) 2006-09-14
DE10225574A1 (de) 2003-12-18
US20050209240A1 (en) 2005-09-22
PL371920A1 (en) 2005-07-11
BR0311311A (pt) 2005-02-15
EP1511737B1 (de) 2010-02-17
US7470687B2 (en) 2008-12-30

Similar Documents

Publication Publication Date Title
AR040251A1 (es) Compuestos de ariloximas como inhibidores de la fosfodiesterasa iv. su uso para el tratamiento del asma, alergia, inflamacion, enfermedades autoinmunes o enfermedades miocardicas
ES2322650T3 (es) Indol 1,2,3,4-tetrasustituido para el tratamiento de enfermedades respiratorias.
RU2004139032A (ru) Производные пиридазина
CA2489902C (en) Thiazole derivatives as phosphodiesterase iv inhibitors
CN101541789B (zh) 用作基质金属蛋白酶抑制剂的乙内酰脲衍生物
RU2460727C2 (ru) Хинолиновые производные для лечения воспалительных заболеваний
RU2302412C2 (ru) Гидразоно-малонитрилы
CA2471538A1 (en) Pyrrolopyrimidines
CA2462525A1 (en) Type 4 phosphodiesterase inhibitors and uses thereof
WO2010142985A1 (en) Substituted n-[1-cyano-2-(phenyl)ethyl]piperidin-2-ylcarboxmide compounds 761
CN101300240A (zh) 作为β2肾上腺素受体激动剂的7-（2-氨基-1-羟基-乙基）-4-羟基苯并噻唑-2(3H)-酮衍生物
CN101006058A (zh) 化合物ⅰ
ES2349622T3 (es) Benzoilpiridazinas.
CN101282950A (zh) 新颖的苯并噻唑酮衍生物

Legal Events

Date Code Title Description
FA Abandonment or withdrawal