| Arylpiperazines having activity at the serotonin 1a receptor -> Monitor Keywords |
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Arylpiperazines having activity at the serotonin 1a receptorRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Six-membered Consisting Of Two Nitrogens And Four Carbon Atoms (e.g., Pyridazines, Etc.), 1,4-diazine As One Of The Cyclos, Piperazines (i.e., Fully Hydrogenated 1,4-diazines), Additional Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic BondingArylpiperazines having activity at the serotonin 1a receptor description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20050282817, Arylpiperazines having activity at the serotonin 1a receptor. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS REFERENCE [0001] This application is a continuation of U.S. application Ser. No. 10/613,798 filed Jul. 2, 2003, which is a division of U.S. application Ser. No. 10/022,045 filed Dec. 18, 2001, now U.S. Pat. No. 6,645,967, which is a division of U.S. application Ser. No. 09/753,645 filed Jan. 3, 2001, now U.S. Pat. No. 6,358,958, which is a division of U.S. application Ser. No. 09/208,553 filed Dec. 9, 1998, now U.S. Pat. No. 6,239,135, which claims the benefit of U.S. Provisional Application Nos. 60/069,722 filed Dec. 16, 1997, 60/069,791 filed Dec. 16, 1997 and 60/089,589 filed Jun. 17, 1998. FIELD OF THE INVENTION [0002] The present invention belongs to the fields of pharmacology and medicinal chemistry, and provides new pharmaceuticals which are useful for the treatment of diseases which are caused or affected by disorders of the serotonin-affected neurological systems, particularly those relating to the 1.sub.A receptor. BACKGROUND OF THE INVENTION [0003] Pharmaceutical researchers have discovered in recent years that the neurons of the brain which contain monoamines are of extreme importance in a great many physiological processes which very strongly affect many psychological and personality-affecting processes as well. In particular, serotonin (5-hydroxytryptamine; 5-HT) has been found to be a key to a very large number of processes which affect both physiological and psychological functions. Drugs which influence the function of serotonin in the brain are accordingly of great importance and are now used for a surprisingly large number of different therapies. [0004] The early generations of serotonin-affecting drugs tended to have a variety of different physiological functions, considered from both the mechanistic and therapeutic points of view. More recently, it has become possible to study the function of drugs at individual receptors in vitro or ex vivo, and it has also been realized that therapeutic agents with a single mechanism of action are often advantageous to the patient. Accordingly, the objective of research now is to discover not only agents which affect only functions of serotonin, but agents which affect only a single function of serotonin, at a single identifiable receptor. [0005] The present invention provides compounds which have highly selective activity as antagonists of the serotonin 1.sub.A receptor. SUMMARY OF THE INVENTION [0006] The present invention provides a series-of new aryl piperazine compounds, methods of using them for pharmaceutical purposes, and pharmaceutical compositions whereby the compounds may be conveniently administered. [0007] The invention also provides methods of antagonizing, the 5HT-1.sub.A receptor, and therapeutic methods which are related to their effect on the 5HT-1.sub.A receptor. Such methods of treatment include, particularly, methods of alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine, comprising the administration to a patient in need of such treatment of a compound of Formula I 1 [0008] wherein [0009] Ar' is a mono- or bi-cyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy, (C.sub.1-C.sub.6)alkylthio, (C.sub.2-C.sub.6)alkenyl, (C.sub.2-C.sub.6)alkynyl, (C.sub.1-C.sub.6)alkylhalo, (C.sub.3-C.sub.8)cycloalkyl, (C.sub.3-C.sub.8)cycloalkenyl or halo; [0010] R.sup.1 is hydrogen, (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy, (C.sub.1-C.sub.6)alkylthio; [0011] R.sup.2 is phenyl, naphthyl or (C.sub.3-C.sub.12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen, (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy, (C.sub.1-C.sub.6)alkylthio, (C.sub.2-C.sub.6)alkenyl, (C.sub.2-C.sub.6)alkynyl, (C.sub.1-C.sub.6)alkylhalo, (C.sub.3-C.sub.8)cycloalkyl, (C.sub.3-C.sub.8)cycloalkenyl or halo; [0012] R.sup.3 is selected from the group consisting of hydrogen, (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy, (C.sub.1-C.sub.6)alkylth- io, (C.sub.2-C.sub.6)alkenyl, (C.sub.2-C.sub.6)alkynyl, (C.sub.1-C.sub.6)alkylhalo, (C.sub.3-C.sub.8)cycloalkyl, (C.sub.3-C.sub.8)cycloalkenyl or halo; [0013] X is --C(.dbd.O)--, --CHOH-- or --CH.sub.2--; [0014] or a pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof. [0015] Further, such therapeutic methods include methods of treatment of anxiety, depression, hypertension, cognitive disorders, psychosis, sleep disorders, gastric motility disorders, sexual dysfunction, brain trauma, memory loss, eating disorders and obesity, substance abuse, obsessive-compulsive disease, panic disorder and migraine. [0016] A further treatment method provided by the present invention is a method for potentiating the action of a serotonin reuptake inhibitor, comprising administering to a patient an effective amount of a compound of Formula I in combination with the serotonin reuptake inhibitor. [0017] More specifically, the present invention provides compounds of formula Ia; 2 [0018] or the pharmaceutically acceptable salts thereof. [0019] The compounds of formula Ia are enclosed within the scope of the compounds of Formula I and are therefore useful for the methods described herein for Formula I. For example, the present invention provides methods of antagonizing, the 5HT-1.sub.A receptor, and therapeutic methods which are related to their effect on the 5HT-1.sub.A receptor. Such methods of treatment include, particularly, methods of alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine, comprising the administration to a patient in need of such treatment, an effective amount of a compound of formula Ia. Further, such therapeutic methods include methods of treatment of anxiety, depression, hypertension, cognitive disorders, psychosis, sleep disorders, gastric motility disorders, sexual dysfunction, brain trauma, memory loss, eating disorders and obesity, substance abuse, obsessive-compulsive disease, panic disorder and migraine. [0020] In addition, the present invention provides a method for potentiating the action of a serotonin reuptake inhibitor, comprising administering to a patient an effective amount of a compound of formula Ia in combination with the serotonin reuptake inhibitor. Continue reading about Arylpiperazines having activity at the serotonin 1a receptor... Full patent description for Arylpiperazines having activity at the serotonin 1a receptor Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Arylpiperazines having activity at the serotonin 1a receptor patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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