Piperazine derivatives
First Claim
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1. A compound of formula ##STR11## and the pharmaceutically acceptable acid addition salts thereof, wherein R represents hydrogen or one or two same or different C1 -C6 alkyl groups,R1 is a mono- or bicyclic aryl radical selected from phenyl, naphthyl;
- a monocyclic heteroaryl group of 5 or 6 ring atoms one or two of which are nitrogen;
or a bicyclic heteroaryl radical of 9 or 10 ring atoms, one or two of which are nitrogen atoms wherein the nitrogen atoms are not common to the two flags, wherein the aryl or heteroaryl group may be optionally substituted by one or more substituents selected from C1 -C6 alkyl, hydroxy, C1 -C6 -alkoxy, halogen, hydroxy-C1 -C6 -alkyl, C1 -C6 -alkoxy-C1 -C6 -alkyl, C1 -C6 -alkoyloxy-C1 -C6 -alkyl, C1 -C6 -alkylcarbonyl, C1 -C6 -alkylcarbonyl-C1 -C6 -alkyl, halo-C1 -C6 -alkyl, nitro, nitrilo, aminocarbonyl, C1 -C6 -alkoxycarbonyl, amino, C1 -C6 -alkylamino, di-C1 -C6 -alkylamino, C1 -C6 -alkoxycarbonyloxy-C1 -C6 -alkyl, aminocarbonyloxy-C1 -C6 -alkyl, C1 -C6 -alkylaminocarbonyloxy-C1 -C6 -alkyl, di-C1 -C6 -alkylaminocarbonyloxy-C1 -C6 -alkyl, C1 -C6 -alkoxycarbonyl-C1 -C.sub. 6 -alkyl, aminocarbonyl-C1 -C6 -alkyl, C1 -C6 -alkylaminocarbonyl-C1 -C6 -alkyl, di-C1 -C6 -alkylaminocarbonyl-C1 -C6 -alkyl, C1 -C6 -acylamino, phenyl- or naphthylcaxbonyl, phenyl- or naphthylcarbonyl-C1 -C6 -alkyl and formyl- or R1 is an aryl group of the formula ##STR12## wherein the heterocyclic ting containing the oxygen atom is non-aromatic, contains a total of 5 to 7 ring members, and optionally contains one or two further heteroatom ring members selected from oxygen and sulfur in addition to the oxygen atom, and said non-aromatic heterocyelic ring may be optionally substituted by one or more substituents as enumerated above as optional substituents for the aryl or heretoaryl group;
R2 is phenyl or naphthyl optionally substituted as above for an aryl or heteroaryl radical, andA is an alkylene chain of 2 to 5 carbon atoms optionally substituted by one or more C1 -C6 -alkyl groups.
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Abstract
Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT1A binding agents, particularly 5-HT1A antagonists and may be used, for example, as anxiolytics. In the formula R is hydrogen or one or two lower alkyl groups, R1 is a mono of bicyclic aryl or heteroaryl radical, R2 is aryl and A is a C2-5 alkylene chain optionally substituted by lower alkyl.
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Citations
7 Claims
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1. A compound of formula ##STR11## and the pharmaceutically acceptable acid addition salts thereof, wherein R represents hydrogen or one or two same or different C1 -C6 alkyl groups,
R1 is a mono- or bicyclic aryl radical selected from phenyl, naphthyl; - a monocyclic heteroaryl group of 5 or 6 ring atoms one or two of which are nitrogen;
or a bicyclic heteroaryl radical of 9 or 10 ring atoms, one or two of which are nitrogen atoms wherein the nitrogen atoms are not common to the two flags, wherein the aryl or heteroaryl group may be optionally substituted by one or more substituents selected from C1 -C6 alkyl, hydroxy, C1 -C6 -alkoxy, halogen, hydroxy-C1 -C6 -alkyl, C1 -C6 -alkoxy-C1 -C6 -alkyl, C1 -C6 -alkoyloxy-C1 -C6 -alkyl, C1 -C6 -alkylcarbonyl, C1 -C6 -alkylcarbonyl-C1 -C6 -alkyl, halo-C1 -C6 -alkyl, nitro, nitrilo, aminocarbonyl, C1 -C6 -alkoxycarbonyl, amino, C1 -C6 -alkylamino, di-C1 -C6 -alkylamino, C1 -C6 -alkoxycarbonyloxy-C1 -C6 -alkyl, aminocarbonyloxy-C1 -C6 -alkyl, C1 -C6 -alkylaminocarbonyloxy-C1 -C6 -alkyl, di-C1 -C6 -alkylaminocarbonyloxy-C1 -C6 -alkyl, C1 -C6 -alkoxycarbonyl-C1 -C.sub. 6 -alkyl, aminocarbonyl-C1 -C6 -alkyl, C1 -C6 -alkylaminocarbonyl-C1 -C6 -alkyl, di-C1 -C6 -alkylaminocarbonyl-C1 -C6 -alkyl, C1 -C6 -acylamino, phenyl- or naphthylcaxbonyl, phenyl- or naphthylcarbonyl-C1 -C6 -alkyl and formyl- or R1 is an aryl group of the formula ##STR12## wherein the heterocyclic ting containing the oxygen atom is non-aromatic, contains a total of 5 to 7 ring members, and optionally contains one or two further heteroatom ring members selected from oxygen and sulfur in addition to the oxygen atom, and said non-aromatic heterocyelic ring may be optionally substituted by one or more substituents as enumerated above as optional substituents for the aryl or heretoaryl group;
R2 is phenyl or naphthyl optionally substituted as above for an aryl or heteroaryl radical, andA is an alkylene chain of 2 to 5 carbon atoms optionally substituted by one or more C1 -C6 -alkyl groups. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- a monocyclic heteroaryl group of 5 or 6 ring atoms one or two of which are nitrogen;
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Current AssigneeJohn Wyeth & Brother Limited (Pfizer Inc.)
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Original AssigneeJohn Wyeth & Brother Limited (Pfizer Inc.)
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InventorsIfill, Anderson D., Mansell, Howard L., White, Alan C., Cliffe, Ian A., Ward, Terence J.
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Primary Examiner(s)TSANG, CECILIA J
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Application NumberUS08/234,036Time in Patent Office438 DaysField of Search544/392, 544/295, 544/372, 544/363, 544/373, 544/364, 544/295, 544/, 544/376, 544/377, 544/392, 514/252, 514/254US Class Current514/254.11CPC Class CodesC07D 295/096 with the ring nitrogen atom...
