ES2104259T3 - Fenilsulfonamidas sustituidas como agonistas beta3 selectivos para el tratamiento de la diabetes y la obesidad. - Google Patents

Fenilsulfonamidas sustituidas como agonistas beta3 selectivos para el tratamiento de la diabetes y la obesidad.

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Publication number
ES2104259T3
ES2104259T3 ES94200303T ES94200303T ES2104259T3 ES 2104259 T3 ES2104259 T3 ES 2104259T3 ES 94200303 T ES94200303 T ES 94200303T ES 94200303 T ES94200303 T ES 94200303T ES 2104259 T3 ES2104259 T3 ES 2104259T3
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Spain
Prior art keywords
compounds
obesity
diabetes
treatment
levels
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Expired - Lifetime
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ES94200303T
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English (en)
Inventor
Michael H Fisher
Emma R Parmee
Robert J Mathvink
Ann E Weber
Hyun O Ok
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Merck and Co Inc
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Merck and Co Inc
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
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    • C07C311/14—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/44—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

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Abstract

SE PRESENTAN FENILSULFONAMIDOS SUSTITUIDOS QUE TIENEN LA FORMULA (I) EN LAS QUE LAS VARIABLES SE HAN DEFINIDO EN LA DEMANDA 1; Y SON COMPETIDORES SELECTIVOS DEL RECEPTOR ADRENERGICO BETA-3 CON MUY PEQUEÑA ACTIVIDAD COMO RECEPTORES ADRENERGICOS BETA-1 Y BETA-2 Y COMO TALES, LOS COMPUESTOS SON CAPACES DE INCREMENTAR LA LIPOLISIS Y EL GASTO DE ENERGIA EN LAS CELULAS, LOS COMPUESTOS TIENEN, DE ESTA FORMA, UNA ACTIVIDAD MUY POTENTE EN EL TRATAMIENTO DE LA DIABETES DE TIPO II Y DE LA OBESIDAD. LOS COMPUESTOS PUEDEN USARSE TAMBIEN PARA REDUCIR LOS NIVELES DE TRIGLICERIDOS Y LOS NIVELES DE COLESTEROL O PARA ELEVAR LOS NIVELES DE LIPOPROTEINAS DE ALTA DENSIDAD O PARA REDUCIR LA MOTILIDAD DEL INTESTINO. ADEMAS, LOS COMPUESTOS PUEDEN UTILIZARSE PARA REDUCIR LAS INFLAMACIONES NEUROGENICAS O COMO AGENTES ANTIDEPRESIVOS. LOS COMPUESTOS SE PREPARAN MEDIANTE EL ACOPLAMIENTO DE UN AMINOALQUILFENILSULFONAMIDO CON UN EPOXIDO DE ALQUIL APROPIADAMENTE SUSTITUIDO. TAMBIEN SE PRESENTAN LAS COMPOSICIONES Y METODOSPARA EL USO DE LOS COMPUESTOS EN EL TRATAMIENTO DE LA DIABETES Y DE LA OBESIDAD Y PARA LA REDUCCION DE LOS NIVELES DE TRIGLICERIDOS Y DE LOS NIVELES DE COLESTEROL O PARA ELEVAR LOS NIVELES DE LIPOPROTEINAS DE ALTA DENSIDAD Y PARA INCREMENTAR LA MOTILIDAD DEL INTESTINO.
ES94200303T 1993-02-09 1994-02-03 Fenilsulfonamidas sustituidas como agonistas beta3 selectivos para el tratamiento de la diabetes y la obesidad. Expired - Lifetime ES2104259T3 (es)

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US1568993A 1993-02-09 1993-02-09
US08/168,105 US5451677A (en) 1993-02-09 1993-12-15 Substituted phenyl sulfonamides as selective β 3 agonists for the treatment of diabetes and obesity

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AT (1) ATE154594T1 (es)
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DE69403823D1 (de) 1997-07-24
IL108507A0 (en) 1994-05-30
JPH0710827A (ja) 1995-01-13
AU5498694A (en) 1995-06-29
DE69403823T2 (de) 1998-01-29
AU670477B2 (en) 1996-07-18
EP0611003A1 (en) 1994-08-17
DK0611003T3 (da) 1997-08-25
JP2690006B2 (ja) 1997-12-10
GR3024672T3 (en) 1997-12-31
EP0611003B1 (en) 1997-06-18
IL108507A (en) 1998-09-24
ZA94846B (en) 1994-09-05
ATE154594T1 (de) 1997-07-15
WO1994018161A1 (en) 1994-08-18
US5451677A (en) 1995-09-19
CA2114712A1 (en) 1994-08-10

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