PE20040682A1 - Derivados de ciclobutano como antagonistas de nk1 - Google Patents

Derivados de ciclobutano como antagonistas de nk1

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Publication number
PE20040682A1
PE20040682A1 PE2003000252A PE2003000252A PE20040682A1 PE 20040682 A1 PE20040682 A1 PE 20040682A1 PE 2003000252 A PE2003000252 A PE 2003000252A PE 2003000252 A PE2003000252 A PE 2003000252A PE 20040682 A1 PE20040682 A1 PE 20040682A1
Authority
PE
Peru
Prior art keywords
alkyl
antagonists
cycloalkyl
halogen
refers
Prior art date
Application number
PE2003000252A
Other languages
English (en)
Inventor
Neng-Yang Shih
Gregory A Reichard
Dong Xiao
Michelle Laci Wrobleski
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of PE20040682A1 publication Critical patent/PE20040682A1/es

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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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Abstract

SE REFIERE A DERIVADOS DE CICLOBUTANO DE FORMULA I DONDE Ar1 Y Ar2 SON HETEROARILO SUSTITUIDO O NO CON (R21)r, ENTRE OTROS; X1 ES O, S, SO, SO2, NR20, CON LA CONDICION DE QUE CUANDO X1 ES SO, SO2, N(COR20) o N(SO2R17), ENTONCES R1 Y R2 SON H, ALQUILO C1-C6, HIDROXI-ALQUILO C1-C3, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, HIDROXI-ALQUILO C1-C3, ENTRE OTROS; R4 Y R5 SON H, ALQUILO C1-C6, HALOGENO, OR20, ENTRE OTRAS; R6 ES (CH2)n1-G, DONDE n1 ES 0 A 5, G ES H, OH, O-ALQUILO C1-C6, ENTRE OTROS; R7 ES (CR40R41)n6-J, DONDE R40 Y R41 SON H o ALQUILO C1-C12; n6 ES 0 A 5; J ES H, CF3, CHF2, ENTRE OTROS; CON LA CONDICION DE CUANDO R6 ES (CH2)n1-G Y n1 ES 0, ENTONCES G ES OH, O-(ALQUILO C1-C6), O-CICLOALQUILO C3-C8, ENTRE OTROS; R8 Y R9 SON H, ALQUILO C1-C6, HALOGENO, OR20; R20 ES H, ALQUILO C1-C6, ENTRE OTROS; R21 ES ALQUILO C1-C6, CICLOALQUILO C3-C8, OH, ENTRE OTROS; r ES DE 1 A 3. SON COMPUESTOS PREFERIDOS 2,2-DICLORO-3-{[1-(3,5-DIFLUOROMETILFENIL)ETOXI]METIL}-3-FENILCICLOBUTANONA ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE LO CONTIENE QUE COMPRENDE ESTOS COMPUESTOS QUE SON ANTAGONISTAS DEL RECEPTOR NEUROPEPTIDO NEUROQUININA-1 (NK1) Y ADEMAS PUEDE CONTENER UN ANTAGONISTA DEL RECEPTOR DE NEUROQUININA NK1, UN INHIBIDOR DE REABSORCION DE SEROTONINA, UN AGONISTA DE RECEPTORES DE DOPAMINA, ENTRE OTROS UTILES PARA EL TRATAMIENTO DE DEPRESION, ANSIEDAD, EMESIS
PE2003000252A 2002-03-13 2003-03-12 Derivados de ciclobutano como antagonistas de nk1 PE20040682A1 (es)

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