AR057977A1 - Derivados de benzooxazol, oxazolopiridina, benzotiazol y tiazolopiridina. composiciones farmaceuticas. - Google Patents

Derivados de benzooxazol, oxazolopiridina, benzotiazol y tiazolopiridina. composiciones farmaceuticas.

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Publication number
AR057977A1
AR057977A1 ARP060103784A ARP060103784A AR057977A1 AR 057977 A1 AR057977 A1 AR 057977A1 AR P060103784 A ARP060103784 A AR P060103784A AR P060103784 A ARP060103784 A AR P060103784A AR 057977 A1 AR057977 A1 AR 057977A1
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alkyl
alkoxy
halogen
group
hydrogen
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ARP060103784A
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Hoffmann La Roche
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Composiciones farmacéuticas que contienen dichos compuestos, y uso de los mismos para el tratamiento y/o prevencion de enfermedades asociadas con la modulacion de los receptores de SST del subtipo 5. Reivindicacion 1: Compuestos de la formula general (1), en la que X es S u O; A es CR3 y B es CR4, o A es N o N+-O- y B es CR4 o B es N o N+-O- y A es CR3; R1 y R2 con independencia entre sí se eligen entre el grupo formado por hidrogeno, halogeno, ciano, nitro, alquilo C1-7, hidroxi-alquilo C1-7, alcoxi C1-7-alquilo C1-7-alcoxi C1-7, hidroxi-alcoxi C2-7, dihidroxi-alcoxi C3-7, carboxi-alcoxi C1-7, (alcoxi C1-7)-carbonil-alcoxi C1-7, carboxi-alquilo C1-7, (alcoxi C1-7)-carbonil-alquilo C1-7, 1H-tetrazol-5-il-alcoxi C1-7, piridinil- alcoxi C1-7, -NR5R6, -NHCOR7, -NHSO2R8, -SO2NR9R10, 1H-tetrazoI-5-ilo, fenilo sin sustituir y fenilo sustituido de una a tres veces por sustituyentes elegidos entre alquilo C1-7, cicloalquilo C3-7, halogeno, halogeno-alquilo C1-7 y alcoxi C1-7 y R2 puede elegirse además entre el grupo formado por carboxi, alcoxi C1-7-carbonilo y -CONR11R12; R5 y R6 con independencia entre sí se eligen entre el grupo formado por hidrogeno, alquilo C1-7, hidroxi-alquilo C1-7 y cicloalquilo C3-7; R7 se elige entre el grupo formado por alquilo C1-7, cicloalquilo C3-7, halogeno-alquilo C1-7, hidroxi-alquilo C1-7, alcoxi C1-7-alquilo C1-7, carboxi-alquilo C1-7, (alcoxi C1-7)-carbonil-alquilo C1-7, 1H-tetrazol-5-il-alquilo C1-7, fenilo sin sustituir, fenilo sustituido de una a tres veces por restos elegidos entre el grupo formado por alquilo C1-7, cicloalquilo C3-7, alcoxi C1-7, halogeno-alquilo C1-7 y halogeno; heteroarilo sin sustituir, heteroarilo sustituido por uno o dos restos elegidos entre alquilo C1-7, cicloalquilo C3-7, alcoxi C1-7, halogeno-alquilo C1-7 o halogeno; heteroaril-alquilo C1-7 sin sustituir y heteroaril-alquilo C1-7, en el que el heteroarilo está sustituido por uno o dos grupos elegidos entre alquilo C1-7, cicloalquilo C3-7, alcoxi C1-7, halogeno-alquilo C1-7 y halogeno; R8 se elige entre el grupo formado por alquilo C1-7, cicloalquilo C3-7, heteroarilo sin sustituir y heteroarilo sustituido por uno o dos restos elegidos entre alquilo C1-7, cicloalquilo C3-7, alcoxi C1-7, halogeno-alquilo C1-7 y halogeno; R9 y R10 con independencia entre sí se eligen entre el grupo formado por hidrogeno, alquilo C1-7, cicloalquilo C3-7, heteroarilo sin sustituir y heteroarilo sustituido por uno o dos restos elegidos entre alquilo C1-7, cicloalquilo C3-7, alcoxi C1-7, halogeno-alquilo C1-7 y halogeno; o R9 y R10 junto con el átomo de nitrogeno al que están unidos forman un anillo de pirrolidina o de piperidina; R11 se elige entre el grupo formado por hidrogeno, alquilo C1-7 y cicloalquilo C3-7; R12 se elige entre el grupo formado por hidrogeno, alquilo C1-7, cicloalquilo C3-7, halogeno-alquilo C1-7, hidroxi-alquilo C1-7, alcoxi C1-7-alquilo C1-7, carboxialquilo C1-7, (alcoxi C1-7)-carbonil-alquilo C1-7, fenilo sin sustituir, fenilo sustituido de una a tres veces por restos elegidos entre el grupo formado por alquilo C1-7, cicloalquilo C3-7, alcoxi C1-7, halogeno-alquilo C1-7 y halogeno; heteroarilo sin sustituir, heteroarilo sustituido por uno o dos restos elegidos entre alquilo C1-7, cicloalquilo C3-7, alcoxi C1-7, halogeno-alquilo y halogeno; uno de R3 y R4 se elige entre el grupo formado por hidrogeno, alquilo C1-7, nitro y alcoxi C1-7 o está ausente en el caso de que uno de A o B sea N o N+-O-, y el otro de R3 y R4 se elige entre el grupo formado por hidrogeno, alquilo C1-7, alcoxi C1-7, hidroxi, hidroxi-alquilo C1-7, ciano-alcoxi C1-7, cicloalquiloxi C3-7, donde el grupo cicloalquilo está sustituido por carboxi o alcoxi C1-7- carbonilo; carboxi, alcoxi C1-7-carbonilo, carboxi-alcoxi C1-7, (alcoxi C1-7)-carbonil-alquilo C1-7, carboxi-alquilo C1-7, (alcoxi C1-7)-carbonil-alcoxi C1-7, 1H-tetrazol-5-il-alcoxi C1-7, triazolil-alcoxi C1-7, alquilsulfoniloxi C1-7, alquilsulfoniloxi C1-7-alcoxi C1-7, hidroxi-alcoxi C2-7, dihidroxi-alcoxi C3-7, alcoxi C1-7-alcoxi C1-7, -(CH2)n-N R13R14, -(CH2)n-NHCOR15, amino-alcoxi C1-7, aminocarbonil-alcoxi C1-7, alquil C1-7-aminocarbonil-alcoxi C1-7 y 1H-tetrazol-5-ilo; R13 y R14 con independencia entre sí se eligen entre el grupo formado por hidrogeno, alquilo C1-7 y cicloalquilo C3-7; R15 se elige entre el grupo formado por alquilo C1-7, cicloalquilo C3-7, halogeno-alquilo C1-7, hidroxi-alquilo C1-7, alcoxi C1-7- alquilo C1-7, carboxi-alquilo C1-7 y (alcoxi C1-7)-carbonil-alquilo C1-7; n es un numero entero elegido entre 1, 2 y 3; con la condicion de que se excluyan los benzooxazoles y benzotiazoles en los que R1, R2, R3 y R4 son hidrogeno; G se elige entre los restos G1 a G5, en los que R16 es hidrogeno o halogeno; R17 se elige entre el grupo formado por alcoxi C1-7, alqueniloxi C2-7, cicloalquiloxi C3-7, -NR29R30, halogeno-alcoxi C1-7, alcoxi C1-7-alcoxi C1-7 y alcoxi C1-7-alquilo C1-7; R29 y R30 con independencia entre sí son hidrogeno o alquilo C1-7; R18 se elige entre el grupo formado por hidrogeno, alquilo C1-7, halogeno-alquilo C1-7, hidroxi, alcoxi C1-7, halogeno-alcoxi C1-7, cicloalquiloxi C3-7, halogeno, pirrolilo, imidazolilo, triazolilo, -CO2R31, -NR32R33, -SOR34; fenilo sin sustituir y fenilo sustituido por uno o dos restos elegidos entre el grupo formado por alquilo C1-7, halogeno-alquilo C1-7, halogeno-alcoxi C1-7, alcoxi C1-7 y halogeno; R31 es hidrogeno o alquilo C1- 7; R32 y R33 con independencia entre sí son hidrogeno o alquilo C1-7; R34 es alquilo C1-7; R19 se elige entre el grupo formado por hidrogeno, alquilo C1-7, halogeno, alcoxi C1-7, alqueniloxi C2-7, -O-tetrahidropiranilo, cicloalquiloxi C3-7, halogenoalcoxi C1-7, alcoxi C1-7-alcoxi C1-7 y alcoxi C1-7-alquilo C1-7; R20 es hidrogeno o halogeno; R21 es hidrogeno o alquilo C1-7; R22 y R23 con independencia entre sí se eligen entre el grupo formado por hidrogeno, alquilo C1-7, alcoxi C1-7 y nitro; R24 es fenilo sin sustituir o fenilo sustituido por uno o dos restos elegidos entre el grupo formado por alquilo C1-7, alcoxi C1-7 y halogeno; R25 es alcoxi C1-7; R26 y R27 con independencia entre sí son alquilo C1-7; R28 es alcoxi C1-7; y las sales farmacéuticamente aceptables de los mismos.
ARP060103784A 2005-09-02 2006-08-30 Derivados de benzooxazol, oxazolopiridina, benzotiazol y tiazolopiridina. composiciones farmaceuticas. AR057977A1 (es)

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US (2) US20070093521A1 (es)
EP (1) EP1924579B1 (es)
JP (1) JP4855468B2 (es)
KR (1) KR101047221B1 (es)
CN (1) CN101253171B (es)
AR (1) AR057977A1 (es)
AT (1) ATE497959T1 (es)
AU (1) AU2006286573B2 (es)
BR (1) BRPI0615449A2 (es)
CA (1) CA2620127A1 (es)
DE (1) DE602006020049D1 (es)
ES (1) ES2359431T3 (es)
IL (1) IL189664A (es)
TW (1) TW200740827A (es)
WO (1) WO2007025897A2 (es)

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US20060168066A1 (en) * 2004-11-10 2006-07-27 David Helsper Email anti-phishing inspector
AU2006222243B2 (en) * 2005-03-09 2012-04-05 F. Hoffmann La-Roche Ag Benzothiazole, thiazolopyridine, benzooxazole and oxazolopyridine derivatives as antidiabetic compounds
EP1900729A1 (en) * 2006-09-15 2008-03-19 Novartis AG Benzoxazoles and oxazolopyridines being useful as Janus kinases inhibitors
US7799806B2 (en) 2007-04-04 2010-09-21 Hoffmann-La Roche Inc. Substituted n-benzyl piperidines as somatostatin receptor modulators
US20080306116A1 (en) * 2007-06-08 2008-12-11 Christ Andreas D Aryloxazole, aryloxadiazole and benzimidazole derivatives
CA2743489A1 (en) * 2008-11-17 2010-05-20 Merck Sharp & Dohme Corp. Substituted bicyclic amines for the treatment of diabetes
WO2011031628A1 (en) * 2009-09-14 2011-03-17 Schering Corporation Inhibitors of diacylglycerol acyltransferase
TW201114762A (en) * 2009-09-30 2011-05-01 Sumitomo Chemical Co Composition and method for controlling arthropod pests
US8481547B2 (en) 2009-12-18 2013-07-09 Janssen Pharmaceutica Nv Substituted benzothiazole and benzoxazole derivatives useful as inhibitors of DPP-1
US20130040978A1 (en) * 2010-05-18 2013-02-14 Joseph L. Duffy Spiro isoxazoline compounds as sstr5 antagonists
EP2605658B1 (en) 2010-08-18 2016-03-23 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
CA2989098A1 (en) 2015-06-22 2016-12-29 Actelion Pharmaceuticals Ltd Nadph oxidase 4 inhibitors
AR114136A1 (es) 2017-10-10 2020-07-29 Hoffmann La Roche Compuestos heterocíclicos

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US2469697A (en) * 1946-12-05 1949-05-10 Eastman Kodak Co Preparation of 2-chlorobenzothiazole
US4861785A (en) * 1984-12-03 1989-08-29 Janssen Pharmaceutica N.V. Benzoxazol-and benzothiazolamine derivatives, useful as anti-anoxic agents
CA1260474A (en) * 1984-12-03 1989-09-26 Raymond A. Stokbroekx Benzoxazol- and benzothiazolamine derivatives
FR2766822B1 (fr) * 1997-07-30 2001-02-23 Adir Nouveaux derives de benzimidazole, de benzoxazole et de benzothiazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
ATE375333T1 (de) * 2002-08-07 2007-10-15 Neuraxon Inc Aminobenzothiazolverbindungen mit nos-hemmender wirkung
GB0315203D0 (en) * 2003-06-28 2003-08-06 Celltech R&D Ltd Chemical compounds
UA82888C2 (en) * 2003-07-28 2008-05-26 Janssen Pharmaceutica Nv Benzimidazole, benzthiazole and benzoxazole derivatives and their use as lta4h modulators
AU2006222243B2 (en) * 2005-03-09 2012-04-05 F. Hoffmann La-Roche Ag Benzothiazole, thiazolopyridine, benzooxazole and oxazolopyridine derivatives as antidiabetic compounds

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JP2009506996A (ja) 2009-02-19
WO2007025897A3 (en) 2007-05-10
US20070093521A1 (en) 2007-04-26
AU2006286573B2 (en) 2012-05-31
CN101253171B (zh) 2011-06-15
DE602006020049D1 (de) 2011-03-24
KR101047221B1 (ko) 2011-07-06
ES2359431T3 (es) 2011-05-23
TW200740827A (en) 2007-11-01
IL189664A (en) 2011-12-29
EP1924579A2 (en) 2008-05-28
KR20080043380A (ko) 2008-05-16
CN101253171A (zh) 2008-08-27
EP1924579B1 (en) 2011-02-09
ATE497959T1 (de) 2011-02-15
BRPI0615449A2 (pt) 2011-05-17
US20090163517A1 (en) 2009-06-25
IL189664A0 (en) 2008-06-05
CA2620127A1 (en) 2007-03-08
WO2007025897A2 (en) 2007-03-08
AU2006286573A1 (en) 2007-03-08
JP4855468B2 (ja) 2012-01-18

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