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AR052446A1 - Piperidinas 3,4-sustituidas - Google Patents

Piperidinas 3,4-sustituidas

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Publication number
AR052446A1
AR052446A1 ARP050105578A ARP050105578A AR052446A1 AR 052446 A1 AR052446 A1 AR 052446A1 AR P050105578 A ARP050105578 A AR P050105578A AR P050105578 A ARP050105578 A AR P050105578A AR 052446 A1 AR052446 A1 AR 052446A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
alkyl
formula
hydroxyl
Prior art date
Application number
ARP050105578A
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English (en)
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Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR052446A1 publication Critical patent/AR052446A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/104Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/108Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
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    • 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
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    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 aromatic rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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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    • C07D401/00Heterocyclic 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
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • 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
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    • 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
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    • C07DHETEROCYCLIC COMPOUNDS
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    • 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

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  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
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  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) en donde: R1 es H, alquilo insustituido o sustituido, alquenilo insustituido o sustituido, alquinilo insustituido o sustituido, arilo insustituido o sustituido, heterociclilo insustituido o sustituido, o cicloalquilo insustituido o sustituido; R2 es alquilo insustituido o sustituido, alquenilo insustituido o sustituido, alquinilo insustituido o sustituido, arilo insustituido o sustituido, heterociclilo insustituido o sustituido, cicloalquilo insustituido o sustituido, o acilo; W es una fraccion seleccionada a partir de aquellas de las formulas (1A), (1B), y (1C) en donde el asterisco (*) denota la posicion en donde se enlaza la fraccion W con el átomo de C-4 en el anillo d3 piperidina de la formula (1), y en donde: X1, X2, X3, X4, y X5 se seleccionan independientemente a partir de C y N, en donde X4 en la formula 1B, y X1 en la formula 1C pueden tener uno de estos significados, o se pueden seleccionar adicionalmente a partir de S y O, en donde los átomos de C y N del anillo pueden llevar el numero requerido de H o sustituyentes R3 o - si está presente dentro de las limitaciones dadas más adelante- R4 para completar el numero de enlaces que surjan desde un C del anillo hasta 4, desde un N del anillo hasta 3; con la condicion de que, en la formula 1A, cuando menos 2, y de preferencia cuando menos 3 de X1 a X5 son C, y en las formulas 1B y 1C cuando menos uno de X1 a X4 es C, de preferencia dos de X1 a X4 son C; y es 0, 1, 2, o 3; z es 0, 1, 2, 3 o 4; R3, que solamente se puede enlazar a cualquiera de X1, X2, X4, y X4 es H, o de preferencia alquilo C1-7 insustituido o sustituido, alquenilo C2-7 insustituido o sustituido, alquinilo C2-7 insustituido o sustituido, arilo insustituido o sustituido,, heterociclilo insustituido o sustituido,, cicloalquilo insustituido o sustituido, halogeno, hidroxilo, hidroxilo eterificado o esterificado, mercapto insustituido o sustituido, sulfinilo insustituido o sustituido,, sulfonilo insustituido o sustituido, amino, amino mono- o di- sustituido, carboxilo, carboxilo esterificado o amidado, sulfamoilo insustituido o sustituido,, nitro o ciano, con la condicion de que si R3 es H, y y z son 0; R4 -si y o z es 2 o más, independientemente - se selecciona a partir de un grupo de sustituyentes que consisten en alquilo C1-7 insustituido o sustituido, alquenilo C2-7 insustituido o sustituido, alquinilo C2-7 insustituido o sustituido, halogeno, hidroxilo, hidroxilo eterificado o esterificado, mercapto insustituido o sustituido, sulfinilo insustituido o sustituido, sulfonilo insustituido o sustituido, amino, amino mono- o di-sustituido, carboxilo, carboxilo esterificado o amidado, sulfamoilo insustituido o sustituido, nitro, y ciano; T es metileno (-CH2-) o carbonilo (-C(=O)-), y R11 es H, hidroxilo, halogeno, alquilo C1-7, halo-alquilo C1-7, cicloalquilo, cicloalquilo sustituido por halogeno, alcoxilo C1-7, halo-alcoxilo C1-7, o ciano, o una sal del mismo.
ARP050105578A 2004-12-30 2005-12-28 Piperidinas 3,4-sustituidas AR052446A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0428526.8A GB0428526D0 (en) 2004-12-30 2004-12-30 Organic compounds

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AR052446A1 true AR052446A1 (es) 2007-03-21

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ARP050105578A AR052446A1 (es) 2004-12-30 2005-12-28 Piperidinas 3,4-sustituidas

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US (2) US8084450B2 (es)
EP (2) EP1833816B1 (es)
JP (1) JP5188814B2 (es)
KR (1) KR20070091174A (es)
CN (1) CN101094848B (es)
AR (1) AR052446A1 (es)
AT (1) ATE448217T1 (es)
AU (1) AU2005321475B2 (es)
BR (1) BRPI0519769A2 (es)
CA (1) CA2587348A1 (es)
DE (1) DE602005017665D1 (es)
ES (1) ES2336470T3 (es)
GB (1) GB0428526D0 (es)
GT (1) GT200500359A (es)
MX (1) MX2007008078A (es)
PE (1) PE20061332A1 (es)
PL (1) PL1833816T3 (es)
PT (1) PT1833816E (es)
RU (1) RU2411239C2 (es)
TW (1) TW200635915A (es)
WO (1) WO2006069788A1 (es)

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BRPI0912388A2 (pt) 2008-05-05 2017-09-26 Merck Frosst Canada Ltd composto, forma cristalina, processo para preparar compostos, composição farmacêutica, e, uso de um composto, e, método para o tratamento ou profilaxia de doenças
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