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Substituted piperazines and diazepanesSubstituted piperazines and diazepanes description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20080113968, Substituted piperazines and diazepanes. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001]This application is a continuation of application Ser. No. 10/185,861 filed on Jun. 27, 2002 and claims priority under 35 U.S.C. 119 of Danish application no. 2001 01046 filed Jul. 2, 2001 and PA 2001 01878 filed Dec. 14, 2001 and Priority of U.S. provisional application Nos. 60/304,371 filed Jul. 10, 2001 and 60/342,871 filed Dec. 17, 2001, the contents of which are fully incorporated herein by reference. FIELD OF THE INVENTION [0002]The present invention relates to novel substituted piperazines and diazapanes, to the use of these compounds as pharmaceutical compositions, to pharmaceutical compositions comprising the compounds, and to a method of treatment employing these compounds and compositions. The present compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor. BACKGROUND OF THE INVENTION [0003]The existence of the histamine H3 receptor has been known for several years and the receptor is of current interest for the development of new medicaments (see eg Stark, H.; Schlicker, E.; Schunack, W., Drugs Fut. 1996, 21, 507-520; Leurs, R.; Timmerman, H.; Volling a, R. C., Progress in Drug Research 1995, 45, 107-165). Recently, the human histamine H3 receptor has been cloned, cf Lovenberg, T. W. et al, Molecular Pharmacology, June 1999, 55, 1101-1107. The histamine H3 receptor is a presynaptic autoreceptor located both in the central and the peripheral nervous system, the skin and in organs such as the lung, the intestine, probably the spleen and the gastrointestinal tract. Recent evidence suggests that the H3 receptor show intrinsic, constitutive activity, in vitro as well as in vivo (ie it is active in the absence of an agonist; see eg Morisset et al., Nature 2000, 408, 860-864). Compounds acting as inverse agonists can inhibit this activity. The histamine H3 receptor has been demonstrated to regulate the release of histamine and also of other neurotransmitters such as serotonin and acetylcholine. A histamine H3 receptor antagonist or inverse agonist would therefore be expected to increase the release of these neurotransmitters in the brain. A histamine H3 receptor agonist, on the contrary, leads to an inhibition of the biosynthesis of histamine and an inhibition of the release of histamine and also of other neurotransmitters such as serotonin and acetylcholine. These findings suggest that histamine H3 receptor agonists, inverse agonists and antagonists could be important mediators of neuronal activity. Accordingly, the histamine H3 receptor is an important target for new therapeutics. [0004]Piperazines similar to the compounds of the present invention have previously been prepared, and their biological properties have been investigated. [0005]JP 57175168, JP 01035827 and WO 81/02421 disclose the compound: [0006]JP 63026754 discloses the compound: [0007]Nishi et al. (Chem. Pharm. Bull.; 31; 3; 1983; 852-860) disclose the compound: [0008]Tiwari et al. (Drug Des. Discovery 1995; 12(3); 249-58) and Meanwell et al. (J. Med. Chem. 1992; 35(14); 2688-96 disclose the compound: [0009]WO 95/00512 discloses the compound: [0010]WO 00/51984 discloses indole-containing piperazine derivatives. [0011]DE 19621221 discloses the compound: [0012]U.S. Pat. No. 2,724,713 discloses the following compound: [0013]Dauzonne et al. (J. Med. Chem. Chim. Ther.; 30; 1; 1995; 53-60) disclose the compound: [0014]Vejdelek et al. (Res. Inst. Pharm. Biochem. Commun.; 48; 10; 1983; 2977-88) disclose the following compound as a potential antitussive: [0015]Brown et al. (J. Am. Chem. Soc.; 119; 14; 1997; 3288-3295) disclose the following compound: [0016]Gayral et al. (Arzneim.-Forsch.; 45; 10; 1995; 1122-1127) disclose the following compound: [0017]WO 00/76970 discloses the compound: [0018]EP 0 203 743 discloses the compound: [0019]WO 92/02498 and Valenta et al. (Collect. Czech. Chem. Commun. 1990; 55(6); 1613-29) disclose the compound: [0020]DE 2360362 discloses the compound: [0021]CA59:13982a discloses the compound: Continue reading about Substituted piperazines and diazepanes... Full patent description for Substituted piperazines and diazepanes Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Substituted piperazines and diazepanes patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. 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