AR085398A1 - Ureas asimetricas y usos medicos de las mismas - Google Patents

Ureas asimetricas y usos medicos de las mismas

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Publication number
AR085398A1
AR085398A1 ARP120100611A ARP120100611A AR085398A1 AR 085398 A1 AR085398 A1 AR 085398A1 AR P120100611 A ARP120100611 A AR P120100611A AR P120100611 A ARP120100611 A AR P120100611A AR 085398 A1 AR085398 A1 AR 085398A1
Authority
AR
Argentina
Prior art keywords
substituents
group
heteroarylalkyl
heterocycloalkyl
arylalkyl
Prior art date
Application number
ARP120100611A
Other languages
English (en)
Inventor
Claudio Giuliano
Zhigang Li
Rubio Silvino Garcia
Claudio Pietra
Original Assignee
Helsinn Healthcare Sa
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 Helsinn Healthcare Sa filed Critical Helsinn Healthcare Sa
Publication of AR085398A1 publication Critical patent/AR085398A1/es

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    • 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
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    • 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
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94—Oxygen atom, e.g. piperidine N-oxide
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    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
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    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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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    • 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
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    • 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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  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Compuestos, composiciones y métodos para la prevención y/o tratamiento de enfermedades cuya fisiopatología está mediada por el receptor de ghrelina.Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1), o una sal aceptable farmacéuticamente o aducto del mismo, donde: R se selecciona entre el grupo que consiste en arilo, arilalquilo, anillo carbocíclico, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo y heteroarilalquilo, opcionalmente sustituido con uno o más sustituyentes R103 independientes; R1 se selecciona entre el grupo que consiste en hidrógeno, hidroxi, hidroxialquilo, amino, alquilo, alquenilo, cicloalquilo, halógeno, alcoxi, alcoxialquilo, -C(O)R101, -C(O)OR101, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo y heteroarilalquilo, cada uno opcionalmente sustituido en forma independiente con uno o más sustituyentes R103 independientes; R2 es hidrógeno; R3 se selecciona entre el grupo que consiste en hidrógeno, alquilo, alquenilo, cicloalquilo, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, -C(O)R101, -C(O)OR101, -C(O)NR101R102, -S(O)2R102, -SR101 y -S(O)2NR101R102, opcionalmente sustituido con uno o más sustituyentes R103 independientes; R4 se selecciona entre el grupo que consiste en alquilo, alquenilo, cicloalquilo, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, -OR103, NR101R102, -C(O)R101, -C(O)OR101, -C(O)NR101R102, -alquilNR101R102, -S(O)2R102, -SR101 y -S(O)2NR101R102, opcionalmente sustituido con uno o más sustituyentes R103 independientes; o R3 y R4, junto con los átomos que conectan R3 y R4, forman un anillo mono, bicíclico o tricíclico, heterocíclico o carbocíclico, fusionado o no fusionado que está opcionalmente sustituido en forma independiente con uno o más sustituyentes R103; R5 se selecciona entre el grupo que consiste en alquilo, alquenilo, cicloalquilo, arilo, arilalquilo, heterocicloalquilo, heteroarilo, heteroarilalquilo, óxido (=O), -C(O)R101, -C(O)OR101, -C(O)NR101R102, -S(O)2R102, -SR101 y -S(O)2NR101R102; R6, R7, R8, R9, R10, R11, R12, R13 y R14 se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, ciano, -NO2, -OR101, hidroxi, amino, alquilo, alquenilo, cicloalquilo, halógeno, alcoxi, alcoxialquilo, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, -C(O)R101, -C(O)OR101, -C(O)NR101R102, -NR101R102, -NR101S(O)R102, -NR101C(O)R102, -S(O)2R102, -SR101 y -S(O)2NR101R102, cada uno opcionalmente sustituido en forma independiente con uno o más sustituyentes R103 independientes; o cualesquier dos o más sustituyentes seleccionados entre el grupo que consiste en R6, R7, R8, R9, R10, R11, R12, R13 y R14 junto con los átomos que los conectan, forman un anillo mono, bicíclico o tricíclico, heterocíclico o carbocíclico, fusionado o no fusionado que está opcionalmente sustituido en forma independiente con uno o más sustituyentes R103; y R101, R102 y R103 se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, ciano, -NO2, -OR104, hidroxi, amino, alquilo, alquenilo, cicloalquilo, halógeno, alcoxi, alcoxialquilo, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, -C(O)R104, -C(O)OR104, -C(O)NR104R105, -NR104R105, -NR104S(O)2R105, -NR104C(O)R105, -S(O)2R104, -SR104 y -S(O)2NR104R105, cada uno opcionalmente sustituido en forma independiente con uno o más sustituyentes R103 independientes; o R101, R102, junto con los átomos que los conectan, forman un anillo mono, bicíclico o tricíclico, heterocíclico o carbocíclico, fusionado o no fusionado que está opcionalmente sustituido en forma independiente con uno o más sustituyentes R103; y R104 y R105 se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, ciano, -NO2, hidroxi, hidroxialquilo, amino, alquilo, alquenilo, cicloalquilo, halógeno, alcoxi, alcoxialquilo, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo y heteroarilalquilo.
ARP120100611A 2011-02-25 2012-02-24 Ureas asimetricas y usos medicos de las mismas AR085398A1 (es)

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Application Number Priority Date Filing Date Title
PCT/CN2011/000298 WO2012113103A1 (en) 2011-02-25 2011-02-25 Asymmetric ureas and medical uses thereof
US201161466070P 2011-03-22 2011-03-22

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AR085398A1 true AR085398A1 (es) 2013-09-25

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