AR035497A1 - Compuestos no-imidazol, composicion farmaceutica que los comprenden y el uso de los mismos para la preparacion de medicamentos - Google Patents

Compuestos no-imidazol, composicion farmaceutica que los comprenden y el uso de los mismos para la preparacion de medicamentos

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Publication number
AR035497A1
AR035497A1 ARP010104831A ARP010104831A AR035497A1 AR 035497 A1 AR035497 A1 AR 035497A1 AR P010104831 A ARP010104831 A AR P010104831A AR P010104831 A ARP010104831 A AR P010104831A AR 035497 A1 AR035497 A1 AR 035497A1
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AR
Argentina
Prior art keywords
alkyl
aryl
formula
halogen
alkylaryl
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ARP010104831A
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English (en)
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Schering Corp
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Publication of AR035497A1 publication Critical patent/AR035497A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
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    • 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
    • A61P25/06—Antimigraine agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
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    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
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    • 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
    • A61P9/10—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
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Otolaryngology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto que tiene la fórmula (1) o una sal o solvato farmacéuticamente aceptable de la misma, en la cual: (1) R1 está seleccionado de: arilo, heteroarilo, heterocicloalquilo, alquilo, cicloalquilo, o alquilarilo, donde dichos grupos R1 están opcionalmente sustituidos con 1 a 4 sustituyentes independientemente seleccionados de: halógeno, hidroxilo, alcoxi inferior, -CF3, CF3O, -NR4R5, fenilo, -NO2, -CO2R4, -CON(R4)2 donde cada R4 es igual o diferente, -S(O)mN(R20)2 donde cada R20 es igual o diferente H o un grupo alquilo preferiblemente alquilo C1-4, más preferiblemente alquilo C1-2 y más preferiblemente metilo, -CN, o alquilo, o (2) R1 y X tomados conjuntamente forman un grupo seleccionado de fórmula (2) o (3); (3) X está seleccionado de: =C(O), =C(NOR3), =C(NNR4R5), fórmula (4) o (5), (4) M1 es carbono, (5)M2 está seleccionado de C o N, (6) M3 y M4 están independientemente seleccionados de C o N, (7) Y está seleccionado de: -CH2-, =C(O), =C(NOR20)(donde R20 es tal como se ha definido anteriormente), o =C(S), (8) Z es un grupo alquilo C1-6, (9) R2 es un anillo heteroarilo de 5 o 6 miembros, comprendiendo dicho anillo heteroarilo de 6 miembros 1 o 2 átomos de nitrógeno, siendo los átomos remanentes carbono, y conteniendo dicho anillo heteroarilo de 5 miembros 1 o 2 heteroátomos seleccionados de: nitrógeno, oxígeno o azufre, siendo el resto de los átomos del anillo carbono; estando opcionalmente dicho anillo heteroarilo de 5 o 6 miembros opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados de: halógeno, hidroxilo, alquilo inferior, alcoxi inferior, -CF3, CF3O-, -NR4R5, fenilo, -NO2, -CO2R4, -CON(R4)2, donde cada R4 es igual o diferente, -CH2NR4R5, -(N)C(NR4R5)2, -CN; (10) R3 está seleccionados de hidrógeno, alquilo C1-6, arilo, heteroarilo, heterocicloalquilo, arilalquilo, -(CH2)e-C(O)N(R4)2 donde cada R4 es igual o diferente, -(CH2)e-C(O)OR4, -(CH2)e-C(O)R30 donde R30 es un grupo heterocicloalquilo, tal como por ejemplo, morfolinilo, piperidinilo, piperazinilo o pirrolidinilo, que incluye fórmula (6), -CF3, o -CH2CF3, donde dicho arilo, heteroarilo, heterocicloalquilo y la porción arilo de dicho arilalquilo, están opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados de: halógeno, -OH, -OCF3, -CF3, -CN, -N(R45)2, -CO2R45, o -C(O)N(R45)2, donde cada R45 está independientemente seleccionado de: H, alquilo, alquilarilo o alquilarilo donde dicha porción arilo está sustituida con 1 a 3 sustituyentes independientemente seleccionados de -CF3, -OH, halógeno, alquilo, -NO2, o -CN; (11) R4 está seleccionado de: hidrógeno, alquilo C1-6, arilo, alquilarilo, estando dichos grupos arilo y alquilarilo opcionalmente sustituidos con 1 a 3 sustituyentes seleccionados de: halógeno, -CF3, -OCF3, -OH, -N(R45)2, -CO2R45, -C(O)N(R45)2, o -CN, donde R45 es tal como se ha definido anteriormente; (12) R5 está seleccionado de hidrógeno, alquilo C1-6, -C(O)R4, -C(O)2R4, o -C(O)N(R4)2, donde cada R4 está independientemente seleccionado, y R4 es tal como se ha definido anteriormente; (13) o R4 y R5 tomados conjuntamente con el átomo de nitrógeno al cual están unidos forman un anillo heterocicloalquilo de 5 o 6 miembros; (14) R6 está seleccionado de: alquilo, arilo, alquilarilo, halógeno, hidroxilo, alcoxi inferior, -CF3, CF3O-, -NR4R5, fenilo, -NO2, -CO2R4, -CON(R4)2, donde cada R4 es igual o diferente, o -CN; (15) R12 está seleccionado de: alquilo, hidroxilo, alcoxi o flúor; (16) R3 está seleccionado de: alquilo, hidroxilo, alcoxi o flúor; (17) a es 0 a 2; (18) b es 0 a 2; (19) c es 0 a 2; (20) e es 0 a 5; (21) m es 1 o 2; (22) n es 1, 2 o 3; y (23) p es 1, 2 o 3, con la condición de que cuando M3 y M4 son ambos nitrógeno, entonces p es 2 o 3. También se describen composiciones farmacéuticas que comprenden los compuestos de la fórmula (1). Se describen también composiciones farmacéuticas que comprende los compuestos de la fórmula (1) para tratar varias enfermedades o condiciones, tales como por ejemplo alergia, respuestas de las vías respiratorias inducidas por alergia, y congestión (congestión nasal) usando los compuestos de la fórmula (1) en combinación con un antagonista receptor H1. Asimismo se describen el uso de dichos compuestos para la manufactura de medicamentos métodos para tratar varias enfermedades o condiciones, tales como, por ejemplos, alergia, respuestas de las vías respiratorias inducidas por alergia, y congestión (por ejemplo, congestión nasal), usando los compuestos de la fórmula (1).
ARP010104831A 2000-10-17 2001-10-15 Compuestos no-imidazol, composicion farmaceutica que los comprenden y el uso de los mismos para la preparacion de medicamentos AR035497A1 (es)

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US (3) US6720328B2 (es)
EP (2) EP1326858B1 (es)
JP (2) JP4093859B2 (es)
KR (1) KR100567266B1 (es)
CN (2) CN1243751C (es)
AR (1) AR035497A1 (es)
AT (2) ATE420863T1 (es)
AU (2) AU1535502A (es)
BR (1) BR0114754A (es)
CA (1) CA2424664C (es)
CY (2) CY1105227T1 (es)
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EC (1) ECSP034559A (es)
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HU (1) HUP0303835A3 (es)
IL (1) IL155031A0 (es)
MX (1) MXPA03003529A (es)
NO (1) NO325997B1 (es)
NZ (1) NZ524857A (es)
PE (1) PE20020507A1 (es)
PL (1) PL361978A1 (es)
PT (1) PT1571145E (es)
RU (2) RU2301231C2 (es)
SI (1) SI1326858T1 (es)
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TW (2) TWI258474B (es)
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