Abstract: Glutamate causes migration and proliferation of retinal pigment epithelium and/or glial cells, and glutamate antagonists can prevent, treat or reduce retinal pigment epithelium and/or glial migration and the subsequent development of proliferative vitreoretinopathy. Avoidance or management of proliferative vitreoretinopathy can be achieved by administering to the patient a compound capable of reducing glutamate-induced retinal cell migration in a concentration effective to reduce such migration.
Abstract: A compound of formula I
in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.
These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.
Type:
Grant
Filed:
May 1, 2001
Date of Patent:
May 27, 2003
Assignee:
Allergan
Inventors:
Stephen A. Munk, James A. Burke, Michael E. Garst
Abstract: Methods for treating benign bone tumors by local administration to a patient of a therapeutically effective amount of a neurotoxin, such as a botulinum toxin, to alleviate pain associated with the bone tumor and/or to cause necrosis of the tumor.
Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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:
May 8, 2002
Date of Patent:
April 29, 2003
Assignee:
Allergan, Inc.
Inventors:
Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
Abstract: Methods and compositions for the treatment of pain using thiourea derivatives. Particularly disclosed are new compositions for the treatment of chronic pain, and methods for their use.
Type:
Grant
Filed:
February 5, 2001
Date of Patent:
April 8, 2003
Assignee:
Allergan Sales, Inc.
Inventors:
Ken Chow, Daniel W. Gil, Wenkui Fang, Michael E. Garst, Wheeler A. Larry
Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
Type:
Grant
Filed:
April 3, 2002
Date of Patent:
April 1, 2003
Assignee:
Allergan Sales, LLC
Inventors:
Steven W. Andrews, Julie A. Wurster, Clarence E. Hull, III, Edward H. Wang, Thomas Malone, Xialing Guo, Zhen Zhu
Abstract: Compounds of the formula
where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist and/or retinoid inverse-agonist-like biological activity.
Type:
Grant
Filed:
January 13, 2000
Date of Patent:
March 25, 2003
Assignee:
Allergan
Inventors:
Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
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;
where in A, B, D, X, Y, Z, R1, R3 and R4 are as defined in the specification.
Type:
Grant
Filed:
March 20, 2002
Date of Patent:
March 25, 2003
Assignee:
Allergan, Inc.
Inventors:
Robert M. Burk, Mark Holoboski, Mari F. Posner
Abstract: Retinoid compounds which act specifically or selectively on RAR&agr; receptor subtypes in preference over RAR&bgr; and RAR&Ggr; receptor subtypes, possess desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.
Type:
Grant
Filed:
July 9, 1999
Date of Patent:
March 18, 2003
Assignee:
Allergan Sales, Inc.
Inventors:
Min Teng, Tien T. Duong, Roshantha A. Chandraratna
Abstract: Compounds of formula (i) and of formula (ii)
wherein the symbols have the meaning disclosed in the specification, specifically or selectively modulate &agr;2B and/or &agr;2C adrenergic receptors in preference over &agr;2A adrenergic receptors, and as such are useful for alleviating chronic pain and allodynia and have no or only minimal cardivascular and/or sedatory activity.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
March 18, 2003
Assignee:
Allergen Sales, Inc.
Inventors:
Ken Chow, Daniel W. Gil, Wenkui Ken Fang, Michael E. Garst
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 hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration and a dotted line represents the presence or absence of a double bond;
A and B are CH2;
D represents a covalent bond or CH2, O, S or NH;
X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or
Y is O, OH, OCOR2, halogen or cyano;
Z is CH2 or a covalent bond;
R is H or R2;
R1 is H, R2, phenyl, or COR2;
R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR2, CO2R and OR.
Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Grant
Filed:
December 5, 2001
Date of Patent:
March 11, 2003
Assignee:
Allergan Sales, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, 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: 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 23, 2000
Date of Patent:
February 18, 2003
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: Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.
Type:
Grant
Filed:
June 9, 2000
Date of Patent:
February 18, 2003
Assignee:
Allergan, Inc.
Inventors:
Elliott S. Klein, Yang-Dar Yuan, Roshantha A. Chandraratna
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.