ECSP961783A - DERIVATIVES OF PIRIMIDINDIONA PIRIMIDINTRIONA TRIACINDIONA TETRAHIDRO- QUINAZOLINDION AS ANTAGONISTS ADRENOCEPTORES CASE RAN 4013/26 - Google Patents

DERIVATIVES OF PIRIMIDINDIONA PIRIMIDINTRIONA TRIACINDIONA TETRAHIDRO- QUINAZOLINDION AS ANTAGONISTS ADRENOCEPTORES CASE RAN 4013/26

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Publication number
ECSP961783A
ECSP961783A ECSP961783A ECSP961783A EC SP961783 A ECSP961783 A EC SP961783A EC SP961783 A ECSP961783 A EC SP961783A EC SP961783 A ECSP961783 A EC SP961783A
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EC
Ecuador
Prior art keywords
alkyl
aryl
heteroaryl
alkyloxy
halo
Prior art date
Application number
Other languages
Spanish (es)
Inventor
David Morgans
Todd Richard Elworthy
Jurg Roland Pfister
Eric Brian Sjogren
Francisco Xavier Talamas
Gary W Bantle
Angel Guzman
Tapia Francisco Javier Lopez
Medrano Arturo Perez
Saul Jaime-Figueroa
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.)
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Publication date
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Priority to ECSP961783 priority Critical patent/ECSP961783A/en
Publication of ECSP961783A publication Critical patent/ECSP961783A/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

El invento se refiere a nuevos antagonistas 1-adrenoceptores de la fórmula I (gráfico), en donde: R1 es acetilamino, amino, ciano, trifluoroacetilamino, halo, hidro, hidroxilo, nitro, metilsulfonilamino, 2-propiniloxilo, un grupo elegido entre (C1-6) alquilo, (C3-6) cicloalquilo, (C3-6)-cicloalquil (C1-4) alquilo, (C1-6) alquiloxilo, (C3-6) cicloalquil-oxilo, (C3-6) cicloalquil (C1-4) alquiloxilo y (C1-4) alquiltio (cuyo grupo está opcionalmente sustituido adicionalmente por uno a tres tomos de halo) o un grupo elegido entre arilo, aril-(C1-4) alquilo, heteroarilo, heteroaril(C1-4)= alquilo, ariloxi, aril (C1-4)-alquiloxilo, heteroariloxilo y heteroaril (C1-4)-alquiloxilo (cuyo arilo y heteroarilo están opcionalmente sustituidos adicionalmente por uno a dos radicales elegidos independientemente entre halo y ciano); R2 es ciano, halo, hidro, hidroxilo, o un grupo elegido entre (C1-6) alquilo y (C1-6) alquiloxilo (cuyo grupo está opcionalmente sustituido adicionalmente por uno a tres tomos de halógeno); R3 y R4 son ambos hidro o metilo o juntos son etileno y R5 es un grupo elegido de las fórmulas (a), (b), (c) y (d) (gráfico), en donde X es C(O), CH2 o CH(Oh); Y es CH2 O CH(OH); Z es N o C(R), en donde R9 es hidro, (C1-6) alquilo o hidroxilo R6 es hidro, un grupo elegido entre (C1-6) alquilo, (C3-6) cicloalquilo, (C3-6) cicloalquil (C1-4) alquilo (cuyo grupo está opcionalmente sustituido adicionalmente por uno o tres tomos de halo) o un grupo elegido entre arrilo, heteroarilo, aril (C1-4) alquilo y heteroaril (C1-4) alquilo (cuyo arilo y heteroarilo están opcionalmente sustituidos adicionalmente por uno o tres radicales elegidos entre halo, ciano, (C1-6) alquiloxilo, (C1-6)-alquilo y arilo; R7 es (C1-6) alcanoilo, carbamoilo, ciano, di(C1-6)alquilamino, halo, hidro, hidroxilo, hidroximinometilo, (C1-6) alquil-sulfonilo (C1-4) alquiltio, un grupo elegido entre (C1-6) alquilo (C3-6) cicloalquilo, (C1-6) alquiloxilo y (C1-6) alquil-oxi (C1-4) alquilo (cuyo grupo está opcionalmente sustituido adicionlmente por uno a tres radicales elegidos entre halo, hidroxilo o (C1-6) alquiloxilo o un grupo elegido entre arilo, heteroarilo, aril(C1-4) alquilo y heteroaril (C1-4) alquilo cuyo arilo y heteroarilo están opcionalmente sustituidos adicionalmente por uno a tres radicales elegidos entre halo, ciano (C1-6) alquiloxilo, (C1-6)alquilo y arilo o R7 y R9 juntos son tetrametileno; y cada R8 es independientemente hidro, hidroxilo, metilo, etilo; y sus sales farmacéuticamente aceptables y N-óxidos.The invention relates to novel 1-adrenoceptor antagonists of formula I (graph), wherein: R1 is acetylamino, amino, cyano, trifluoroacetylamino, halo, hydro, hydroxyl, nitro, methylsulfonylamino, 2-propynyloxy, a group chosen from ( C1-6) alkyl, (C3-6) cycloalkyl, (C3-6) -cycloalkyl (C1-4) alkyl, (C1-6) alkyloxy, (C3-6) cycloalkyl-oxyl, (C3-6) cycloalkyl ( C1-4) alkyloxy and (C1-4) alkylthio (the group of which is optionally further substituted by one to three halo atoms) or a group chosen from aryl, aryl- (C1-4) alkyl, heteroaryl, heteroaryl (C1-4 ) = alkyl, aryloxy, (C1-4) aryl-alkyloxy, heteroaryloxy and heteroaryl (C1-4) -alkyloxy (which aryl and heteroaryl are optionally further substituted by one to two radicals independently chosen from halo and cyano); R2 is cyano, halo, hydro, hydroxyl, or a group chosen from (C1-6) alkyl and (C1-6) alkyloxy (the group of which is optionally further substituted by one to three halogen atoms); R3 and R4 are both hydro or methyl or together are ethylene and R5 is a group chosen from the formulas (a), (b), (c) and (d) (graph), where X is C (O), CH2 or CH (Oh); Y is CH2 O CH (OH); Z is N or C (R), where R9 is hydro, (C1-6) alkyl or hydroxyl R6 is hydro, a group chosen from (C1-6) alkyl, (C3-6) cycloalkyl, (C3-6) cycloalkyl (C1-4) alkyl (the group of which is optionally further substituted by one or three halo atoms) or a group chosen from aryl, heteroaryl, aryl (C1-4) alkyl and heteroaryl (C1-4) alkyl (whose aryl and Heteroaryl are optionally further substituted by one or three radicals chosen from halo, cyano, (C1-6) alkyloxy, (C1-6) -alkyl and aryl; R7 is (C1-6) alkanoyl, carbamoyl, cyano, di (C1- 6) alkylamino, halo, hydro, hydroxyl, hydroxyminomethyl, (C1-6) alkyl-sulfonyl (C1-4) alkylthio, a group chosen from (C1-6) alkyl (C3-6) cycloalkyl, (C1-6) alkyloxy and (C1-6) alkyl-oxy (C1-4) alkyl (the group of which is optionally further substituted by one to three radicals chosen from halo, hydroxyl or (C1-6) alkyloxy or a group chosen from aryl, heteroaryl, aryl ( C1-4) alkyl and heteroaryl (C1 -4) alkyl whose aryl and heteroaryl are optionally further substituted by one to three radicals chosen from halo, cyano (C1-6) alkyloxy, (C1-6) alkyl and aryl or R7 and R9 together are tetramethylene; and each R8 is independently hydro, hydroxyl, methyl, ethyl; and its pharmaceutically acceptable salts and N-oxides.

ECSP961783 1996-06-06 1996-06-06 DERIVATIVES OF PIRIMIDINDIONA PIRIMIDINTRIONA TRIACINDIONA TETRAHIDRO- QUINAZOLINDION AS ANTAGONISTS ADRENOCEPTORES CASE RAN 4013/26 ECSP961783A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
ECSP961783 ECSP961783A (en) 1996-06-06 1996-06-06 DERIVATIVES OF PIRIMIDINDIONA PIRIMIDINTRIONA TRIACINDIONA TETRAHIDRO- QUINAZOLINDION AS ANTAGONISTS ADRENOCEPTORES CASE RAN 4013/26

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ECSP961783 ECSP961783A (en) 1996-06-06 1996-06-06 DERIVATIVES OF PIRIMIDINDIONA PIRIMIDINTRIONA TRIACINDIONA TETRAHIDRO- QUINAZOLINDION AS ANTAGONISTS ADRENOCEPTORES CASE RAN 4013/26

Publications (1)

Publication Number Publication Date
ECSP961783A true ECSP961783A (en) 1997-11-20

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Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP961783 ECSP961783A (en) 1996-06-06 1996-06-06 DERIVATIVES OF PIRIMIDINDIONA PIRIMIDINTRIONA TRIACINDIONA TETRAHIDRO- QUINAZOLINDION AS ANTAGONISTS ADRENOCEPTORES CASE RAN 4013/26

Country Status (1)

Country Link
EC (1) ECSP961783A (en)

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