Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
Type:
Grant
Filed:
September 27, 2000
Date of Patent:
May 14, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
Abstract: Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
Abstract: The invention concerns the use of a substance P antagonist in a cosmetic composition used to treat sensitive skin. More specifically, the invention relates to a substance P antagonist used to prevent and/or combat skin irritations, desquamation, erythemas, sensations of dysesthesia/overheating, or pruritus of the skin.
Abstract: The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise spirobicyclic ammonium moieties and optionally, further comprise a hydrophobic substituent, a quaternary ammonium-containing substituent or a combination thereof.
Type:
Grant
Filed:
December 1, 1998
Date of Patent:
August 7, 2001
Assignee:
GelTex Pharmaceuticals, Inc.
Inventors:
Pradeep K. Dhal, Steven C. Polomoscanik
Abstract: The present invention relates to novel substituted pyridines/pyrimidines of the formula I
where A is CH or N; X is NH, oxygen or S(O)q where q is 0, 1 or 2; Y is a direct bond or CH2; Z is oxygen, NR7 or S(O)m is 0, 1 or 2, and the radicals R1, R2, R3, R4, R5, R6 and R7 are as defined in the description, to processes for their preparation, and to their use as pesticides, fungicides, ovicides or as veterinary medicaments.
Type:
Grant
Filed:
April 1, 1997
Date of Patent:
March 27, 2001
Assignee:
Hoechst Schering
Inventors:
Ralf Braun, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and methods of using them as analgesics and anti-pruritic agents are provided.
The compounds of formula IV have the structure:
wherein
X9;
R1, R2, R3, R4; and
n are as described in the specification.
Type:
Grant
Filed:
November 8, 1999
Date of Patent:
January 30, 2001
Assignee:
Adolor Corporation
Inventors:
Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang