Abstract: The present invention provides novel compounds represented by the general formula I.
wherein m, n, X, Y, Z, R, R1 and R2 are as defined in the specification or a pharmaceutically acceptable salt thereof. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.
Abstract: The present invention provides novel compounds represented by the general formula I.
and pharmaceutically acceptable salts thereof wherein m, n, X, R, R1 and R2 are as defined in the specification. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.
Type:
Grant
Filed:
February 28, 2002
Date of Patent:
January 21, 2003
Assignee:
Allergan, Inc.
Inventors:
Robert M. Burk, Yariv Donde, Michael E. Garst
Abstract: A controlled release system for multiphasic, in vivo release of therapeutic amounts of botulinum toxin in a human patient over a prolonged period of time. The controlled release system can comprise a plurality of botulinum toxin incorporating polymeric microspheres.
Abstract: Agents for treating pain, methods for producing the agents and methods for treating pain by administration to a patient of a therapeutically effective amount of the agent. The agent can include a clostridial neurotoxin, or a component or fragment or derivative thereof, attached to a targeting moiety, wherein the targeting moiety is selected from a group consisting of transmission compounds which can be released from neurons upon the transmission of pain signals by the neurons, and compounds substantially similar to the transmission compounds.
Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
Type:
Grant
Filed:
June 7, 2001
Date of Patent:
December 17, 2002
Assignee:
Allergan, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
Abstract: Methods and compositions for the treatment of lung disease such as emphysema and/or bronchopulmonary dysplasia in a mammal. Also disclosed are methods and compositions promoting the formation of alveolar septa and increasing the gas-exchange surface area of a mammalian lung, and for the prevention and/or treatment of alveolar destruction.
Type:
Grant
Filed:
April 13, 2000
Date of Patent:
December 10, 2002
Assignee:
Allergan, Inc.
Inventors:
Roshantha A. Chandraratna, Donald Massaro, Gloria DeCarlo Massaro
Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g.
Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.
Type:
Grant
Filed:
March 28, 2001
Date of Patent:
October 22, 2002
Assignee:
Allergan, Inc.
Inventors:
Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
Abstract: Compounds of the formula
where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
Type:
Grant
Filed:
July 6, 2001
Date of Patent:
October 15, 2002
Assignee:
Allergan, Inc.
Inventors:
Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
Abstract: The present invention provides a method of providing neuroprotection to a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on its nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death
wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof. Such noxious action may result from ischemia, e.g. spinal ischemia.
Type:
Grant
Filed:
February 22, 2002
Date of Patent:
October 15, 2002
Assignee:
Allergan, Inc.
Inventors:
Larry A. Wheeler, Elizabeth Woldemussie, Ronald K. Lai
Abstract: Compounds of Formula 1 and of Formula 2
where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.
Type:
Grant
Filed:
August 4, 2000
Date of Patent:
October 15, 2002
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
Abstract: Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.
Type:
Grant
Filed:
August 4, 2000
Date of Patent:
October 15, 2002
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
Abstract: A method of treating ocular hypotension, hypertension, hemorrhage, myocardial ischemia, angina pectoris, coronary contraction, cerebrovascular contraction after subarachnoidal hemorrhage, cerebral hemorrhage and asthma which comprises administering to a mammal suffering therefrom a therapeutically effective amount of a thromboxane ligand which is a compound formula I,
wherein Y is (CH2)x; Z is selected from the group consisting of O, OCH2,
and (CR2)x, x is an integer of 1 or 2; n is 0 or 1; R2 is hydrogen or an alkyl radical of from 1 to 4 carbons; A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups or said alkylene or alkenylene may have one or more enchained oxa or imino radicals; B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroar
Type:
Grant
Filed:
July 5, 2001
Date of Patent:
October 8, 2002
Assignee:
Allergan, Inc.
Inventors:
Robert M. Burk, Achim H-P Krauss, David F. Woodward
Abstract: Compounds of the formula
Y3(R4)—X—Y1(R1R2)—Z—Y2(R2)—A—B
where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.
Type:
Grant
Filed:
November 8, 2000
Date of Patent:
September 24, 2002
Assignee:
Allergan, Inc.
Inventors:
Tae K. Song, Min Teng, Roshantha A. Chandraratna
Abstract: Silicone-containing organic compounds useful as modulators of mammalian nuclear hormone receptors, particularly the retinoid receptors and the farnesoid receptors.
Type:
Grant
Filed:
June 9, 2000
Date of Patent:
September 17, 2002
Assignee:
Allergan Sales, LLC
Inventors:
Richard L. Beard, Michael E. Garst, Roshantha A. Chandraratna
Abstract: A method for treating hypothyroidism by local administration of a neurotoxin, such as a botulinum toxin, to a thyroid, thereby reducing an inhibitory effect upon thyroid hormone secretion. A method for treating hyperthyroidism by local administration of a neurotoxin, such as a botulinum toxin, to a sympathetic ganglion which innervates the thyroid, thereby reducing a stimulatory effect upon thyroid hormone secretion. Methods for treating calcium metabolism disorders by local administration of a neurotoxin to modulate calcitonin secretion are also disclosed.
Abstract: The invention provides for the use of a presynaptic neurotoxin (for example a bacterial neurotoxin such as botulinum toxin B) for the manufacture of a medicament for the treatment of cerebral palsy in juvenile patients. The juvenile patients are preferably juveniles of up to 6 years in age.
Abstract: A pharmaceutical composition for the controlled release of therapeutic agents from carboxylic acid ortho ester polymers contains a pharmaceutically acceptable salt of an acid, which together with the acid R1-COOH liberated from the decomposition of the ortho ester polymer forms a buffer system in a physiologically acceptable pH range.
Type:
Grant
Filed:
July 27, 1998
Date of Patent:
August 27, 2002
Assignee:
Allergan Sales, Inc.
Inventors:
Robert Gurny, Monia Zignani, Cyrus Tabatabay
Abstract: The invention encompasses a method for treating hyperinsulinemic type 2 diabetes by local administration of a neurotoxin, such as a botulinum toxin, into the pancreas, thereby reducing insulin secretion from a B cell, and a method for treating hypoinsulinemic type 2 diabetes by local administration of a neurotoxin, such as a botulinum toxin, into a sympathetic ganglion, thereby reducing an inhibitory effect upon insulin secretion.