Serotonergic 5HT7receptor compounds for treating ocular and CNS disorders

• US 7,060,704 B2
• Filed: 04/07/2005
• Issued: 06/13/2006
• Est. Priority Date: 05/19/1998
• Status: Expired due to Fees

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Alcon Manufacturing Limited (Alcon Incorporated)
• Inventors: Sharif, Najam A., Chen, Hwang-Hsing, May, Jesse A., Dean, Thomas R.
• Primary Examiner(s): Kifle, Bruck
• Application Number:
  US11/100,918
• Publication Number:
  US 20050187214A1
• Time in Patent Office: 432 Days
• Field of Search: 544/373, 514/254.09
• US Class Current: 514/254.09
• CPC Class Codes: C07D 209/08 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
• CPC Class Codes: C07D 217/04 with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
• CPC Class Codes: C07D 235/26 Oxygen atoms
• CPC Class Codes: C07D 295/088 to an acyclic saturated chain
• CPC Class Codes: C07D 295/13 to an acyclic saturated chain
• CPC Class Codes: C07D 401/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 513/04 Ortho-condensed systems

Abstract

Compounds with 5HT₇ receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.

Claims

1. A compound of the formula:

7. The Compound of claim 1 selected from the group consisting of:

3-[4-(3-Chlorophenyl)piperazin-1-yl]propylsulfonyl-2,3-dihydro-1H-indole;

3-[4-(3-Trifluoromethylphenyl)piperazin-1-yl]propylsulfonyl-2,3-dihydro-1H-indole;

3-[4-(2-Methoxyphenyl)piperazin-1-yl]propylsulfonyl-2,3-dihydro-1H-indole.

2. A method for lowering IOP which comprises administering to a person in need thereof, a composition comprising an effective amount of a compound of the formula:

3. A method for improving blood flow to the optic nerve head and the retina which comprises administering to a person in need thereof, a composition comprising an effective amount of a compound of the formula:

4. A method for treating retinal diseases which comprises administering to a person in need thereof, a composition comprising an effective amount of a compound of the formula:

5. A method for treating persons suffering from a sleeping disorder, depression, schizophrenia, anxiety, obsessive compulsive disorders, circadian rhythm disorders, and centrally and peripherally mediated hypertension which comprises, administering a composition comprising a pharmaceutically effective amount of a compound of the formula:

6. A composition comprising a pharmaceutically effective amount of a compound of the formula: