Use of tetrahydrocarbazone derivatives as 5HT.sub.1 receptor agonists

• US 5,464,864 A
• Filed: 12/23/1993
• Issued: 11/07/1995
• Est. Priority Date: 06/26/1991
• Status: Expired due to Term

• Current Assignee: Endo Pharmaceuticals Incorporated (Endo International PLC)
• Original Assignee: Smithkline Beecham PLC
• Inventors: King, Francis D., Gaster, Laramie M., Young, Rodney C., Kaumann, Alberto J.
• Primary Examiner(s): Springer, David B.
• Application Number:
  US08/167,846
• Time in Patent Office: 684 Days
• Field of Search: 548/439, 514/468
• US Class Current: 514/468
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 209/88 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system

Abstract

##STR1## Use of a compound of general formula (I), wherein R¹ represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C_1-6 alkyl, C_1-6 alkoxy, arylC_1-6 alkoxy, --CO₂ R⁴, --(CH₂)_n CN, --(CH₂)_n CONR⁵ R⁶, --(CH₂)_n SO₂ NR⁵ R⁶, C_1-6 alkanoylamino(CH₂)_n, or C_1-6 alkylsulphonylamino(CH₂)_n ; R⁴ represents hydrogen, C_1-6 alkyl or arylC_1-6 alkyl; R⁵ and R⁶ each independently represent hydrogen or C_1-6 alkyl, or R⁵ and R⁶ together with the nitrogen atom to which they are attached form a ring; n represents 0, 1 or 2; and R² and R³ each independently represent hydrogen, C_1-6 alkyl; or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring; or a physiologically acceptable salt thereof, in the manufacture of a medicament for the treatment of a condition where a 5-HT₁ -like agonist is indicated, for example migraine. Novel compounds of formula (I), processes for preparing them and pharmaceutical compositions containing them are also described.

Claims

1. A compound of formula (I) which is 3-methylamino-6-carboxamido-1,2,3,4-tetrahydrocarbazole, or a salt, solvate or hydrate thereof.

2. A method of treatment of a condition wherein a 5-HT₁ -like agonist is indicated, which comprises administering to a subject in need thereof an effective amount of a compound of claim 1.

3. The method according to claim 1 wherein the condition is migraine.

4. The method according to claim 1 wherein the condition is cluster headache.

5. The method according to claim 1 wherein the condition is headache associated with vascular disorders.

6. A pharmaceutical composition comprising the compound according to claim 1, or a physiologically acceptable salt thereof and a physiologically acceptable carrier.