Abstract: In the course of developing 2-[[[2-[(hydroxyacetyl) amino]-4-pyridinyl] methyl] thio]-N-[4-(trifluoromethoxy) phenyl]-3-pyridinecarboxamide (compound A), there are the multiple problems: 1) compound A or its salt is difficult to be recrystallized, the storage stability largely differs depending on the kind of the salt, and it is very difficult to obtain a salt of compound A having excellent storage stability; 2) in a crystallization process of compound A, it is very difficult to control a crystal polymorph, and 3) compound A (free body) causes mineral deposition in the stomach when it is orally administered repeatedly.
Abstract: Provided is a pharmaceutical preparation for treatment or prevention of glaucoma or ocular hypertension, comprising 0.0003 to 0.01% (w/v) of isopropyl(6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate, or a salt thereof.
Abstract: A composition for preventing or treating glaucoma or ocular hypertension including a combination of isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl} pyridin-2-ylamino) acetate and at least one other drug for preventing or treating glaucoma or ocular hypertension, with the proviso that tafluprost is excluded.
Abstract: The present invention relates to a pharmaceutical composition comprising a compound represented by the formula (1) or a salt thereof and polyethylene glycol.
Abstract: An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method.
Abstract: Described herein are liquid rapamycin formulations. Described herein are methods of treating or preventing diseases or conditions, such as choroidal neovascularization, wet AMD and dry AMD, and preventing transition of dry AMD to wet AMD, using the liquid rapamycin formulations described herein.
Type:
Grant
Filed:
January 9, 2014
Date of Patent:
July 12, 2016
Assignee:
SANTEN PHARMACEUTICAL CO., LTD.
Inventors:
Sreenivasu Mudumba, Philippe J M Dor, Thierry Nivaggioli, David A. Weber, Sidiq Farooq
Abstract: Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; liquid formulations comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration in a subject.
Type:
Grant
Filed:
November 25, 2014
Date of Patent:
July 5, 2016
Assignee:
SANTEN PHARMACEUTICAL CO., LTD.
Inventors:
Sreenivasu Mudumba, Philippe J M Dor, Thierry Nivaggioli, David A. Weber, Sidiq Farooq
Abstract: In the course of developing 2-[[[2-[(hydroxyacetyl) amino]-4-pyridinyl]methyl]thio]-N-[4-(trifluoromethoxy) phenyl]-3-pyridinecarboxamide(compound A), there are the multiple problems: 1) compound A or its salt is difficult to be recrystallized, the storage stability largely differs depending on the kind of the salt, and it is very difficult to obtain a salt of compound A having excellent storage stability; 2) in a crystallization process of compound A, it is very difficult to control a crystal polymorph, and 3) compound A (free body) causes mineral deposition in the stomach when it is orally administered repeatedly.
Abstract: A composition for treating or preventing glaucoma or ocular hypertension including a isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate and a beta-receptor antagonist, in a combined pharmaceutically acceptable amount. As for the administration form, these drugs may be administered concomitantly or may be administered as a combination drug.
Abstract: An ophthalmic formulation which is an aqueous solution of a prostaglandin derivative, the prostaglandin derivative being 16-phenoxy-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F2 ? or an isopropyl ester thereof, said prostaglandin derivative being contained in the aqueous solution as an active ingredient in a concentration of 0.00005 to 0.05 weight %, a nonionic surfactant which is polysorbate 80 in a concentration in the solution of 10 times or more to 100 times or less of the prostaglandin derivative and an antioxidant in an amount sufficient to inhibit decomposition of the prostaglandin derivative.
Abstract: A compound represented by the formula (1): wherein R1 represents a hydroxyl group, a dimethylphosphynoyloxy group, etc.; and R2 and R3 represent a methoxy group, etc., or a pharmaceutically acceptable salt thereof can reduce a score of telangiectasia around the meibomian gland orifices and a number of obstruction at the orifices, so that it is useful as a prophylactic and/or therapeutic agent for meibomian gland dysfunction.
Abstract: The present invention relates to a prophylactic or therapeutic agent for a posterior ocular disease containing the compound represented by a formula (1), its enantiomer or diastereomer, or their pharmaceutically acceptable salt thereof as an active ingredient.
Abstract: In the course of developing 2-[[[2-[(hydroxyacetyl) amino]-4-pyridinyl]methyl]thio]-N-[4-(trifluoromethoxy) phenyl]-3-pyridinecarboxamide(compound A), there are the multiple problems: 1) compound A or its salt is difficult to be recrystallized, the storage stability largely differs depending on the kind of the salt, and it is very difficult to obtain a salt of compound A having excellent storage stability; 2) in a crystallization process of compound A, it is very difficult to control a crystal polymorph, and 3) compound A (free body) causes mineral deposition in the stomach when it is orally administered repeatedly.
Abstract: A method of protecting a retinal neuronal cell by administering an effective amount of a prostaglandin F2? derivative to a patient. A method of preventing or treating an eye disease associated with retinal neuronal cell damage by administering a therapeutically effective amount of a prostaglandin F2? derivative to a patient.