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:
March 19, 2003
Date of Patent:
March 16, 2004
Assignee:
Allergan, Inc.
Inventors:
Stephen A. Munk, James A. Burke, Michael E. Garst
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: Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.
Abstract: A gene encoding the human EP3 prostaglandin receptor has been cloned and sequenced. The protein encoded by this gene has seven transmembrane domains and is 81% homologous to the murine EP3 receptor. Two variants that differ in their carboxy terminal coding sequence, and one variant that differs in its 3′ untranslated sequence only, have also been cloned. The proteins, when expressed in eukaryotic cells, are capable of binding prostaglandins and their agonists and regulating adenylate cyclase activity in response to prostaglandins.
Type:
Grant
Filed:
September 14, 2000
Date of Patent:
December 30, 2003
Assignees:
Allergan, Inc., Arizona Board of Regents
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: A method for treating hypoparathyroidism and/or hypocalcemia by local administration of a neurotoxin, such as a botulinum toxin, to a parathyroid gland, thereby reducing an inhibitory effect upon parathyroid hormone secretion. A method for treating hyperparathyroidism and/or hypercalcemia by local administration of a neurotoxin, such as a botulinum toxin, to a sympathetic ganglion which innervates a parathyroid hormone secreting parathyroid cell, thereby reducing a stimulatory effect upon parathyroid hormone secretion.
Abstract: Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.
Abstract: A method for treating hypoparathyroidism and/or hypocalcemia by local administration of a neurotoxin, such as a botulinum toxin, to a parathyroid gland, thereby reducing an inhibitory effect upon parathyroid hormone secretion. A method for treating hyperparathyroidism and/or hypercalcemia by local administration of a neurotoxin, such as a botulinum toxin, to a sympathetic ganglion which innervates a parathyroid hormone secreting parathyroid cell, thereby reducing a stimulatory effect upon parathyroid hormone secretion.
Abstract: Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.
Abstract: Methods for treating fibromyalgia may include administering a therapeutically effective amount of a Clostridial toxin to a peripheral location on the body of a patient. This peripheral location is other than the site on the body where the pain emanates.
Abstract: Methods for treating a movement disorder by intracranial administration to a human patient of a therapeutically effective amount of a neurotoxin, such as a botulinum toxin type A.
Abstract: Compounds of the formula
where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR&agr; retinoid receptors.
Type:
Grant
Filed:
September 19, 2002
Date of Patent:
September 16, 2003
Assignee:
Allergan, Inc.
Inventors:
Tien T. Duong, Richard Beard, Roshantha A. Chandraratna
Abstract: Compounds having Formula 4 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:
February 21, 2002
Date of Patent:
August 5, 2003
Assignee:
Allergan, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I:
wherein wavy line attachments indicate either the alpha (&agr;) or beta (&bgr;) configuration; dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of —OR1, —N(R1)2, R1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of —OR1, —N(R1)2 and —N(R5)SO2R6, wherein R5 represents hydrogen or CH2OR6 and R6 represents hydrogen or a lower alkyl radical having up to six carbon atoms and halogen substituted derivatives of said lower alkyl radical, e.g. a fluoro substituted lower alkyl radical; Y is ═O or represents 2 hydrogen radicals.
Abstract: A recombinant plasmid for expression of Moloney Murine Leukemia Virus (MMLV)-derived reverse transcriptase in E. coli cells deficient in the expression of RNAse activity, a method for purification of the recombinant enzyme, and a purified recombinant reverse transcriptase for suitable use in cDNA and nucleic acid amplification procedures are disclosed.
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 relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I:
wherein the hatched segment represents an &agr; bonds, the solid triangle represents a &bgr; bond, the wavy segments represent &agr; or &bgr; bond, dashed lines represent a double bond or a single bond R, , R1, R2 and R3 are as defined in the specification.
Type:
Grant
Filed:
May 24, 2002
Date of Patent:
July 1, 2003
Assignee:
Allergan, Inc.
Inventors:
Robert M. Burk, Mark Holoboski, Mari F. Posner
Abstract: A biocompatible implant for continuous in vivo release of a neurotoxin over a treatment period extending from one month to five years. The implant can be made of casting a solution of a polymer, such as an ethyl vinyl acetate copolymer and the neurotoxin. The neurotoxin can be a botulinum toxin.
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.