Patent
Pyridyl-and pyrimidylpiperazine derivatives
| العنوان: | Pyridyl-and pyrimidylpiperazine derivatives |
|---|---|
| Patent Number: | 5,652,240 |
| تاريخ النشر: | July 29, 1997 |
| Appl. No: | 08/374,776 |
| Application Filed: | January 31, 1995 |
| مستخلص: | The present invention concerns compounds of the formula (I) ##STR1## wherein Ar are the same or different and are a phenyl group, optionally substituted with fluorine, or a pyrid-4-yl group, R.sub.1 and R.sub.2 are the same or different and are selected from hydrogen or lower alkyl, n is 2 or 3, X is nitrogen or methine and A is pyrimid-2-yl or a substituted or unsubstituted pyridyl group. The compounds are useful for treating mental disorders. |
| Inventors: | Abramo, Lisbeth (Bjarred, SEX); Lundstedt, Torbjorn (Loddekopinge, SEX); Nordvi, Curt (Malmo, SEX); Olsson, Knut Gunnar (Malmo, SEX); Brodszki, Martin (Malmo, SEX) |
| Assignees: | Pharmacia Aktiebolag (Stockholm, SEX) |
| Claim: | We claim |
| Claim: | 1. A compound having the formula (I) ##STR15## wherein each Ar is the same or different and is selected from ##STR16## wherein R.sub.3 is a fluoro or hydrogen |
| Claim: | R.sub.1 and R.sub.2 are each hydrogen |
| Claim: | n is 2 or 3 |
| Claim: | X is nitrogen |
| Claim: | Y is methylene |
| Claim: | A is ##STR17## wherein R.sub.4 and R.sub.5 are each the same or different and are selected from hydrogen, halogen, lower alkyl, an electron donor group and an electron acceptor group |
| Claim: | or a pharmaceutically acceptable salt thereof. |
| Claim: | 2. The compound of claim 1, wherein R.sub.4 is hydrogen, alkyl, trifluoromethyl, alkoxy, amide, nitro, alkylcarboxylate or cyano and R.sub.5 is hydrogen, alkyl, alkoxy, nitro, halogen, cyano, alkylcarboxylate or an amide group. |
| Claim: | 3. The compound of claim 2, wherein R.sub.4 is hydrogen and R.sub.5 is hydrogen, alkyl, alkoxy, nitro, halogen, cyano, alkylcarboxylate or an amide group. |
| Claim: | 4. The compound of claim 1, which is 1-{3-[bis-(4-fluorophenyl)amino]propyl}-4-(2-pyridyl)-piperazine or a pharmacologically acceptable salt thereof. |
| Claim: | 5. The compound of claim 4, which is the dihydrochloride salt of said compound. |
| Claim: | 6. A method for treating a patient suffering from a mental disorder, which comprises the step of |
| Claim: | administering to said living animal body an effective 5-HT.sub.1A agonistic and 5-HT.sub.2 antagonistic amount of a compound, which is 1-{3-[bis-(4-fluorophenyl)amino]propyl}-4-(2-pyridyl)-piperazine or a pharmaceutically acceptable salt thereof. |
| Current U.S. Class: | 514/252; 544/295; 544/360; 544/364; 544/365 |
| Current International Class: | A61K 31495; A61K 31505; C07D40306 |
| Patent References Cited: | 4292321 September 1981 Pattison 4766215 August 1988 Abou-Gharbia et al. 4908365 March 1990 Buzas et al. 4937245 June 1990 Fex et al. 4994459 February 1991 Butera et al. 4994460 February 1991 Dextraze et al. 5418236 May 1995 Carmosin et al. |
| Other References: | Vadodaria et al, J. Med. Chem., vol. 12, pp. 860-865 (1969). Burger, Medical Chemistry, Third Edition, Part I, pp. 74-77 (1970). |
| Primary Examiner: | Grumbling, Matthew V. |
| Attorney, Agent or Firm: | Birch, Stewart, Kolasch & Birch, LLP |
| رقم الانضمام: | edspgr.05652240 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |