AR076984A1 - Derivados de pirazol oxadiazol - Google Patents

Derivados de pirazol oxadiazol

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Publication number
AR076984A1
AR076984A1 ARP100101985A ARP100101985A AR076984A1 AR 076984 A1 AR076984 A1 AR 076984A1 AR P100101985 A ARP100101985 A AR P100101985A AR P100101985 A ARP100101985 A AR P100101985A AR 076984 A1 AR076984 A1 AR 076984A1
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AR
Argentina
Prior art keywords
alkyl
indicates
het1
cor4
carbon atoms
Prior art date
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ARP100101985A
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English (en)
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Merck Serono Sa
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Publication of AR076984A1 publication Critical patent/AR076984A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P31/12—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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • 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
    • C07D413/02—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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
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  • Communicable Diseases (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente se refiere a derivados de pirazol oxadiazolos de la Formula (1), y al uso de los mismos para tratar esclerosis multiple y otras enfermedades. Reivindicacion 1: Compuestos de la formula (1): en donde R1 indica Ar1, Het1, Cyc, A, (C1-6)alquilo, (C2-6)alquilo, -(CH2)nAr1, (CH2)nHet1, (CH2)nHet2; R2 es Ar2, Het1; R3 indica Ar1, Ar2, Het1, Het2, Cyc o A, o si R1 es Het1, Cyc, A, -(CH2)nAr1, (CH2)nHet1, (CH2)nHet2, (C2-6)alquilo, o si R1 indica Ar1 o R2 es Ar2, Het1 o Het2 en donde Ar1 y Ar2 son mono, di o trisustituidos por los sustituyentes mencionados en la presente, R3 también indica CH3 o si R1 indica Het1, Cyc, A, (C1-6)alquilo, (C2-6)alquilo, -(CH2)nAr1, (CH2)nHet1, (CH2)nHet1, R3 también indica S-(C1-6-alquil), A es un alquilo ramificado o lineal que posee 2 a 12 átomos de carbono, en donde uno o más, preferentemente 1 a 7 átomos H pueden reemplazarse por Hal, OR4, CN, CO2R4, CF3, cicloalquilo con 3 a 7 átomos de carbono de anillo, Ar1, Ar2, o N(R4)2 y en donde uno o más, preferentemente 1 a 7 grupos CH2- no adyacentes pueden reemplazarse por O, NR4, -CO-, NR4CO2-, -CO2-, -NR4CONR4-, -CH=CH-, -C:::C-, o indica cicloalquilo o cicloalquilalquileno con 3-7 átomos de carbono de anillo, o indica Het1 o Het2; Z es un alquilo ramificado o lineal que posee 2 a 12 átomos de carbono, en donde uno o más, preferentemente 1 a 7 átomos H son reemplazados por Hal, OR4, CN, CO2R4, CF3, cicloalquilo con 3 a 7 átomos de carbono de anillo, Ar1, Ar2, N(R4)2 y/o en donde uno o más, preferentemente 1 a 7 grupos CH2- son reemplazados por O, NR4, S, -CO-, NR4CO2-, -NR4CONR4-, -CH=CH-, -C:::C-, o indica cicloalquilo o cicloalquilalquileno con 3-7 átomos de carbono de anillo; Hal es F, Cl, Br o I; Ar1 indica un anillo carbocíclico monocíclico o bicíclico, insaturado o aromático con 6 a 14 átomos de carbono que puede ser insustituido, monosustituido, disustituido o trisustituido por sustituyentes seleccionados entre A, Hal, -OR4, -SO2R4, -CN, -NO2, -N(R3)2, -CO(NR4)2, -OR4, (NR4)COR4, -CO2R4, -COR4, -SO2N(R4)2, -SO2alquilo, NR4SO2alquilo, NR4SO2alquilo, o C1-6 alquilo; Ar2 indica un anillo carbocíclico monocíclico o bicíclico, insaturado o aromático con 6 a 14 átomos de carbono que puede ser insustituido, monosustituido, disustituido o trisustituido por sustituyentes seleccionados entre Z, F, Br, I, -OR4, -(CH2)OR4, -(CH2)N(R4)2, Perfluoro-alcoxi, -SO2R4, -CN, -NO2, - N(R4)2, -CO(NR4)2, (NR4)COR4, -CO2R4, -COR4, -SO2N(R4)2, -SO2 (C1-6)alquilo, NR4SO2(C1-6)alquilo, -(CH2)nHet1, -OHet1, -(CH2)nHet2, -OHet2, o si R3 es Het1, Het2, Ar1, Ar2 o Cyc, o si R1 es Het1, Cyc, A, (C1-6)alquilo, (C2-6)alquilo, -(CH2)nAr1, (CH2)nHet1, (CH2)nHet1, Ar2 también indica un anillo carbocíclico monocíclico o bicíclico, insaturado o aromático con 6 a 14 átomos de carbono que puede ser insustituido, monosustituido, disustituido o trisustituido por CF3. Het1 indica un anillo monocíclico saturado, insaturado o heterocíclico aromático o un anillo bicíclico, saturado o heterocíclico insaturado que posee 1 a 4 átomos N y/o O que puede ser insustituido, monosustituido, disustituido o trisustituido por sustituyentes seleccionados entre A, Hal, -OR4, -(CH2)OR4, Perfluoro-alquilo, Perfluoro-alcoxi, -SO2(R4)2, CN, NO2, -N(R4)2, -CO(NR4)2, (NR4)COR4, -CO2R4, -COR4, -SO2N(R4)2, -SO2alquilo, NR4SO2alquilo, NR4SO2alquilo, o C1-6 alquilo. Het2 indica un anillo monocíclico o bicíclico saturado, insaturado o heterocíclico aromático con 1 a 4 átomos N, O y/o S que puede ser insustituido, moriosustituido, disustituido o trisustituido por sustituyentes seleccionados entre A, F, Br, I, -OR4, -(CH2)OR4, Perfluoro-alquilo, Perfluoro-alcoxi, -SO2(R4)2, CN, NO2, -N(R4)2, -CO(NR4)2, (NR4)COR4, -CO2R4, -COR4, -SO2N(R4)2, -SO2alquilo, NR4SO2alquilo, NR4SO2alquilo, o C1-6 alquilo; Cyc indica un anillo carbocíclico saturado o insaturado que contiene 3 a 7 átomos de carbono que puede ser sustituido por Hal, A, (C1-6)alquilo, -[C(R4)2]n-Ar, -[C(R4)2]n-cicloalquilo, OR4, CF3, OCF3, N(R4)2, NR4CON(R4)2, NO2, CN, -[C(R4)2]n-COOR4, -[C(R4)2]n-CON(R4)2, NR4COA, NR4SO2A, COR4, CO2R4, SO2N(R4)2, SOA, y/o SO2A. R4 es H, A, Cyc o (C1-6)alquilo, preferentemente H o (C1-6)alquilo; n es 1, 2, 3 o 4 y derivados farmacéuticamente aceptables, solvatos, tautomeros, sales y estereo-isomeros de los mismos, incluyendo mezclas de los mismos en todas las proporciones como un medicamento, especialmente para tratar esclerosis multiple y otras enfermedades.
ARP100101985A 2009-06-08 2010-06-04 Derivados de pirazol oxadiazol AR076984A1 (es)

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EP09162206 2009-06-08
US21847709P 2009-06-19 2009-06-19

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AR (1) AR076984A1 (es)
AU (1) AU2010257564B2 (es)
CA (1) CA2763683C (es)
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WO2012040532A1 (en) 2010-09-24 2012-03-29 Bristol-Myers Squibb Company Substituted oxadiazole compounds and their use as s1p1 agonists
JP2014062047A (ja) * 2011-01-21 2014-04-10 Taisho Pharmaceutical Co Ltd ピラゾール誘導体
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CN106573893B (zh) 2014-07-31 2020-06-09 巴斯夫欧洲公司 制备吡唑的方法
EP3294725B1 (en) 2015-05-11 2021-05-05 Basf Se Process for preparing 4-amino-pyridazines
PE20181539A1 (es) 2016-02-02 2018-09-26 Basf Se Proceso de hidrogenacion catalitico para preparar pirazoles
CN112552288A (zh) * 2021-02-19 2021-03-26 南京桦冠生物技术有限公司 一种4-肟-5`-（2-甲基丙酰基）尿苷的制备方法
WO2024049829A2 (en) * 2022-08-29 2024-03-07 Case Western Reserve University Compositions and methods for treating and detecting cancer

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US8802663B2 (en) 2014-08-12
IL216692A (en) 2017-09-28
CA2763683C (en) 2018-05-15
JP2012529459A (ja) 2012-11-22
JP5837482B2 (ja) 2015-12-24
EP2440554B1 (en) 2016-10-05
ES2638398T3 (es) 2017-10-20
US20120071460A1 (en) 2012-03-22
AU2010257564B2 (en) 2016-09-29
IL216692A0 (en) 2012-02-29
AU2010257564A1 (en) 2011-12-08
EP2440554A1 (en) 2012-04-18
WO2010142628A1 (en) 2010-12-16
CA2763683A1 (en) 2010-12-16

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