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 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: 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:
August 5, 2002
Date of Patent:
December 9, 2003
Assignee:
Allergan, Inc.
Inventors:
Tae K. Song, Min Teng, Roshantha A. Chandraratna
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: 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: The present invention is directed to an ophthalmic formulation which comprises a therapeutically effective amount of ethyl 4-(8-chloro-5,6-dihydro-11-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate, known as loratadine, a fatty acid ester, and a surfactant, which has been found to be useful in treating ocular allergies, especially allergic conjunctivitis, and related conditions.
Type:
Grant
Filed:
January 9, 2003
Date of Patent:
October 21, 2003
Assignee:
Allergan, Inc.
Inventors:
Chin-Ming Chang, Eldon Q. Farnes, Orest Olejnik, James N. Chang
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: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.
Abstract: A process and pharmaceutical compositions for treating several diseases and conditions which are normally treatable with retinoid like compounds are disclosed where the compound used for the treatment are substantially non-teratogenic and not irritant to the skin. The process is useful for treating female mammals, including humans, who are pregnant or in the child bearing age. An important partial structural feature of the compounds which provides the non-teratogenic effect and lack of irritation of skin is shown by the formula where the partially drawn ring signifies an aromatic ring which may be carbocyclic or heteroaromatic, 6-membered or 5-membered, and may be condensed with another ring. R1 is lower alkyl, Cl, Br, or I, R2 is H, lower alkyl, Cl, Br, or I, and R3 is lower alkyl, Cl, Br, I, or is an ether, thioether, ester, thioester, amine or substituted amine group.
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 of the formula
where the symbols are as defined in the specification, have retinoid agonist, antagonist or negative hormone-like biological activity.
Type:
Grant
Filed:
March 23, 2000
Date of Patent:
September 2, 2003
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
Abstract: Retinoid compounds which act specifically or selectively on RAR&agr; receptor subtypes in preference over RAR&bgr; and RAR&Ggr; receptor subtypes, posses 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:
November 29, 2001
Date of Patent:
August 26, 2003
Assignee:
Allergan, Inc.
Inventors:
Min Teng, Tien T. Duong, 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: 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 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: 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: The present invention provides cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-[5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl]heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma.
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 X, Y, Z, D and R3 are as defined in the specification.
Type:
Grant
Filed:
May 14, 2002
Date of Patent:
June 3, 2003
Assignee:
Allergan, Inc.
Inventors:
David W. Old, Danny Thang Dinh, Robert M. Burk