AR032331A1 - Derivados heterociclicos, procesos para su preparacion, composiciones farmaceuticas, y usos de dichos derivados en la fabricacion de medicamentos - Google Patents

Derivados heterociclicos, procesos para su preparacion, composiciones farmaceuticas, y usos de dichos derivados en la fabricacion de medicamentos

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Publication number
AR032331A1
AR032331A1 ARP010102321A ARP010102321A AR032331A1 AR 032331 A1 AR032331 A1 AR 032331A1 AR P010102321 A ARP010102321 A AR P010102321A AR P010102321 A ARP010102321 A AR P010102321A AR 032331 A1 AR032331 A1 AR 032331A1
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Argentina
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alkyl
optionally substituted
heterocyclyl
hydroxy
halo
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ARP010102321A
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Astrazeneca Ab
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
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    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/08—Antibacterial agents for leprosy
    • A—HUMAN NECESSITIES
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    • A61P33/00—Antiparasitic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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

Abstract

Derivados heterocíclicos que tienen la formula (1), R1 es alquilo C1-6, cicloalquilo C3-7, alquenilo C3-8 o alquinilo C3-8, cada uno opcionalmente sustituido con uno o más de los siguientes: halo, hidroxi, ciano, nitro, cicloalquilo C3-7, NR8R9, C(O)R10, NR13C(O)R14, C(O)NR17R18, NR19C(O)NR20R21, S(O)nR22, alcoxi C1-6 (opcionalmente sustituido con heterociclilo o C(O)NR23R24), heterociclilo, heterocicliloxi, arilo, ariloxi, heteroarilo o heteroariloxi; R2 es hidrogeno, alquilo C1-8 alquenilo C3-8, alquinilo C3-8, cicloalquilo C3-7, arilo, heteroarilo, heterociclilo, arilalquilo (C1-4), heteroarilalquilo (C1-4) o heterociclilalquilo (C1-4); R3 es alquilo C1-8 alquenilo C2-8, NR45R46, alquinilo C2-8, cicloalquilo C3-7, cicloalquenilo C3-7, arilo, heteroarilo, heterociclilo, arilalquilo (C1-4), heteroarilalquilo (C1-4) o heterociclilalquilo (C1-4); R46 es alquilo C1-8, alquenilo C3-8, alquinilo C3-8, cicloalquilo C3-7, arilo, heteroarilo, heterociclilo, arilalquilo (C1-4), heteroarilalquilo (C1-4) o heterociclilalquilo (C1-4); donde los grupos R2, R3 y R46 y las porciones heterociclilo, arilo y heteroarilo de R1 están independiente y opcionalmente sustituidas con uno o más de los siguientes: halo, ciano, nitro, hidroxi, S(O)qR25, OC(O)NR26R27, NR28R29, NR30C(O)R31, NR32C(O)NR33R34, S(O)2NR35R36, NR37S(O)2R38, C(O)NR39R40, C(O)R41, CO2R42, NR43CO2R44, alquilo C1-6, cicloalquilo C3-10, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, fenilo, fenilalquilo (C1-4), fenoxi, feniltio, fenilalcoxi(C1-4), heteroarilo, heteroarilalquilo (C1-4), heteroariloxi o heteroarilalcoxi (C1-4); donde cualquiera de las porciones fenilo y heteroarilo inmediatamente anteriores están opcionalmente sustituidas con halo, hidroxi, nitro, S(O)kalquilo C1-4, S(O)2NH2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NH(alquilo C1-4), CO2H, CO2(alquilo C1-4), NHC(O)(alquilo C1-4), NHS(O)2(alquilo C1-4), C(O)(alquilo C1-4), CF3 o OCF3; las porciones cicloalquilo C3-7, arilo, heteroarilo y heterociclilo de R1, R2 y R3 están, adicional y opcionalmente sustituidos con alquilo C1-6, alquenilo C2-6, alquinilo C2-6 o alcoxiC1-6alquilo(C1-6); R4, R5, R6 y R7 son independientemente, hidrogeno, alquilo C1-6 {opcionalmente sustituido con halo, ciano, hidroxi, alcoxi C1-4 OCF3, NH2, NH(alquilo C1-4), N(alquilo C1-4)2, NHC(O)(alquilo C1-4), N(alquilo C1-4), C(O) (alquilo C1-4), NHS(O)2(alquilo C1-4), N(alquilo C1-4)S(O)2(alquilo C1-4), CO2(alquilo C1-4), C(O)NH(alquilo C1-4), C(O)N(alquilo C1-4)2, C(O)NH2, CO2H, S(O2)(alquilo C1-4), S(O)2NH(alquilo C1-4), S(O)2N(alquilo C1-4)2, heterociclilo o C(O)(heterociclilo)}, S(O)2NH2, S(O)2NH(alquilo C1-4), C(O)N(alquilo C1-4)2, C(O)(alquilo C1-4), CO2H, CO2(alquilo C1-4) o C(O)(heterociclilo); o dos de R4, R5, R6 y R7, pueden unirse para formar, junto con el anillo al que están unidos, un sistema de anillo bicíclico; o dos de R4, R5, R6 y R7 pueden formar un enlace endocíclico (resultando así en un sistema de anillo no saturado); X es C(O), S(O)2, C(O)C(O), un enlace directo o C(O)C(O)NR47; k, m, n, p y q son independientemente 0, 1 o 2; R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43 y R44, son independientemente, alquilo C1-8, alquenilo C3-8, alquinilo C3-8, cicloalquilo C3-7, arilo, heteroarilo, o heterociclilo donde cada uno de los cuales está opcionalmente sustituido con halo, ciano, nitro, hidroxi, alquilo C1-4, alcoxi C1-4, SCH3, S(O)CH3, S(O)2CH3, NH2, NHCH3, N(CH3)2, NHC(O)NH2, C(O)NH2, NHC(O)CH3, S(O)2N(CH3)2, S(O)2NHCH3, CF3, CHF2, CH2F, CH2CF3 o OCF3; y R26, R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43 y R44 pueden adicionalmente ser hidrogeno; R8, R9, R10, R13, R14, R17, R18, R19, R20, R21, R23, R24, R45 y R47 son, independientemente, hidrogeno, alquilo {opcionalmente sustituido con halo, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heterociclilo o fenilo (opcionalmente sustituido con halo, hidroxi, ciano, alquilo C1-4 o alcoxi C1-4)}, fenilo (opcionalmente sustituido con halo, hidroxi, nitro, S(O)kalquilo C1-4, S(O)2NH2, ciano, alquilo C1-4, alcoxi C1-4 C(O)NH2, C(O)NH(alquilo C1-4), CO2(alquilo C1-4), NHC(O)(alquilo C1-4), NHS(O)2(alquilo C1-4), C(O)(alquilo C1-4) CF3 o OCF3) o heteroarilo (opcionalmente sustituido con halo, hidroxi, nitro S(O)k alquilo C1-4, S(O)2NH2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NH(alquilo C1-4), CO2H, CO2(alquilo C1-4), NHC(O)(alquilo C1-4), NHS(O)2(alquilo C1-4), C(O)(alquilo C1-4), CF3 o OCF3); R22 es alquilo {opcionalmente sustituido con halo, hidroxi, alcoxi C1-6, haloalcoxi C1-6, heterociclilo o fenilo (opcionalmente sustituido con halo, hidroxi, ciano, alquilo C1-4 o alcoxi C1-4)}, fenilo (opcionalmente sustituido con halo, hidroxi, ciano, alquilo C1-4 o alcoxi) o heteroarilo (opcionalmente sustituido con halo, hidroxi, ciano, alquilo C1-4 o alcoxi C1-4); los pares de sustituyentes R8, R9, R13, y R14, R17 y R18, R20 y R21, R23 y R24, R26 y R27, R28 y R29, R30 y R31, R32 con tanto R33 o R34, R33 y R34, R35 y R36, R37 y R38, R39 y R40 y R43 y R44, pueden, independientemente unirse para formar un anillo y, este anillo puede además comprender un átomos de oxígeno azufre o nitrogeno; donde para cualquiera de los grupos heterocíclicos anteriores que tienen una porcion -N(H)- del anillo, esa porcion ûN(H)- puede estar opcionalmente sustituida con alquilo C1-4 (opcionalmente sustituida con hidroxi). C(O)(alquilo C1-4), C(O)NH(alquilo C1-4), C(O)N(alquilo C1-4)2 o S(O)2(alquilo C1-4); un átomo de nitrogeno y/o azufre del anillo está opcionalmente oxidado para formar un N-oxido y/o un S-oxido; los anillos heteroarilo y heterociclilo anteriores están C-, o donde es posible, N-unidos; o su sal o solvato farmacéuticamente aceptable; procesos para su preparacion, composiciones farmacéuticas, y usos de dichos derivados en la fabricacion de medicamentos. Los compuestos modulan la actividad del receptor CCR5 y se utilizan para tratar enfermedades autoinmunes, inflamatorias, proliferativas o hiperproliferativas o enfermedades mediadas por el sistema inmunologico (transplante y sida).
ARP010102321A 2000-05-17 2001-05-16 Derivados heterociclicos, procesos para su preparacion, composiciones farmaceuticas, y usos de dichos derivados en la fabricacion de medicamentos AR032331A1 (es)

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GBGB0011838.0A GB0011838D0 (en) 2000-05-17 2000-05-17 Chemical compounds

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US (1) US20040006081A1 (es)
EP (1) EP1289957A1 (es)
JP (1) JP2003533510A (es)
KR (1) KR20030001511A (es)
CN (1) CN1441781A (es)
AR (1) AR032331A1 (es)
AU (1) AU2001258981A1 (es)
BR (1) BR0110767A (es)
CA (1) CA2407258A1 (es)
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HK (1) HK1052507A1 (es)
HU (1) HUP0302153A2 (es)
IL (1) IL152418A0 (es)
IS (1) IS6608A (es)
MX (1) MXPA02011304A (es)
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