Abstract: The invention relates to substituted 9-alkyladenines of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined as set forth in the specification. The invention is also directed to the use of such compounds to inhibit adenosine A1 receptor activation in a mammal. The compounds of the present invention are useful as diuretics, renal protectives against acute or chronic renal failure, as well as agents to improve the therapeutic outcome resulting from defibrillation or cardiopulmonary resuscitation by preventing post-resuscitation bradycardia, bradyarrythmia and cardioplegia, to restore cardiac function following a cardioplegic procedure, and to treat or prevent intermittent claudication.
Abstract: A transdermal therapeutic system, comprising a backing layer inert to the components of the matrix, a self-adhesive matrix layer containing (?)-5,6,7,8-tetrahydro-6-[propyl-[2-(2-thienyl)ethyl]amino]-1-naphthalenol in an effective amount and a protective foil or sheet to be removed prior to use, is characterised by a matrix that is based on a non-aqueous, acrylate-based or silicone-based polymer adhesive system having a solubility of ?5% (w/w) for (?)-5,6,7,8-tetrahydro-6-[propyl-[2-(2-thienyl)ethyl]-amino]-1-naphthalenol, and said matrix is substantially free of inorganic silicate particulates.
Type:
Grant
Filed:
March 18, 1999
Date of Patent:
April 26, 2005
Assignees:
LTS Lohmann Therapie-Systeme AG, Aderis Pharmaceuticals, Inc.
Abstract: A substantially solvent-free matrix layer containing (?)-5,6,7,8-tetrahydro-6-[propyl-[2-(2-thienyl)ethyl]amino]-1-naphthalenol is produced by adding an active substance to an adhesive solution, coating the resultant active substance-containing adhesive solution onto a suitable sheet, and removing the solvents in a drying process to give said substantially solvent-free matrix layer.
Type:
Application
Filed:
September 7, 2004
Publication date:
February 10, 2005
Applicants:
LTS Lohmann Therapie-Systeme AG, Aderis Pharmaceuticals, Inc.
Abstract: The present invention relates to the use of N6-cyclopentyl-5?-(N-ethyl)carboxamidoadenosine (DTI-0009) or a pharmaceutically acceptable salt or ester thereof in the treatment of atrial fibrillation or atrial flutter in a human. Especially an acute attack of atrial fibrillation or atrial flutter is treated by the method of this invention.
Type:
Application
Filed:
April 26, 2004
Publication date:
January 13, 2005
Applicants:
Aderis Pharmaceuticals, Inc., Fujisawa Healthcare, Inc.
Inventors:
Shrikant Gadgil, William Wheeler, Shawn McDonald, Stephen O'Dell
Abstract: The present invention discloses a method for treating heart rhythm disturbances in a mammal in need thereof by the administration of N6-substituted-5′-(N-substituted)carboxamidoadenosines.
Abstract: The present invention discloses a method for treating heart rhythm disturbances in a mammal in need thereof by the administration of N6-substituted-5′-(N-substituted)carboxamidoadenosines.
Abstract: The present invention discloses a method for treating heart rhythm disturbances in a mammal in need thereof by the administration of N6-substituted-5′(N-substituted)carboxamidoadenosines. More particularly, the invention is directed to a method for treatment of heart rhythm disturbances in a mammal that would benefit from the induction of negative dromotropic and/or negative chronotropic actions, comprising the administration to said mammal an effective amount of a compound of the Formula:
or a pharmaceutically acceptable salt or ester thereof; wherein
R1 is C3-7 secondary alkyl, or C3-8 cycloalkyl; and
R2 is C1-4 alkyl or C3-5 cycloalkyl
The invention is also directed to novel dosage forms comprising said compounds.
Abstract: The present invention relates to a process for preparing optically active and racemic nitrogen-substituted 2-aminotetralins of the following Formula (I):
wherein R1, R2, R3, R4, and n are set in the specification, wherein the process comprises alkylating the corresponding unsubstituted 2-aminotetralin of Formula (II):
with a reactant of the Formula (III):
Z—(CH2)n—R3 (III)
wherein Z is a leaving group, in the presence of a base, wherein the base is selected from the group consisting of alkali metal carbonate and alkali metal bicarbonate, and wherein the amount of the base is less than about a 1.9-fold molar excess with respect to the amount of the 2-aminotetralin.