Abstract: Novel tris-substituted biguanide compounds are made by reaction of sodium dicyanamide with a trifunctional primary amine followed by reaction with anilines. The tris-substituted biguanide compounds are potent biocide and useful as a disinfectant. The novel compounds have biocidal activity comparable to those of widely used chlorhexidine with respect to width of antibacterial spectrum and in immediate effectiveness. The novel tris-substituted biguanide compounds can also be used for cleaning wounds, preventing dental plaque, treating yeast infections of the mouth, and to keep urinary catheters from blocking, These novel compounds have superior aqueous solubility and bioavailability and have potent antibacterial activity especially against A. baumanni and K. pneumonia.

Abstract: Novel tris-substituted biguanide compounds are made by reaction of sodium dicyanamide with a trifunctional primary amine followed by reaction with anilines. The tris-substituted biguanide compounds are potent biocide and useful as a disinfectant. The novel compounds have biocidal activity comparable to those of widely used chlorhexidine with respect to width of antibacterial spectrum and in immediate effectiveness. The novel tris-substituted biguanide compounds can also be used for cleaning wounds, preventing dental plaque, treating yeast infections of the mouth, and to keep urinary catheters from blocking, These novel compounds have superior aqueous solubility and bioavailability and have potent antibacterial activity especially against A. baumanni and K. pneumonia.

Abstract: Biocidal branched polymeric biguanide compounds are made by polycondensation of sodium dicyanamide and a Afunctional primary amine and/or a tetrafunctional primary amine and optionally with a difunctional primary amine. The branched polymeric biguanide compounds have 2-dimensional conformation that provides better coverage over the surfaces of microorganisms and enhances efficacy as biocides as compared to most commercially available linear (one-dimensional) polymeric biguanide compounds. The bulkier 2-dimensional conformation of this invention limits the uptake, accumulation and release of these branched polymers to and from contact lenses. Therefore, these branched biguanide polymers can reduce the cytotoxicity, enhance compatibility and suitable for ophthalmic use. The highly branched polymers can be prepared with minimum or no difunctional primary amines.

Abstract: Biocidal branched polymeric biguanide compounds are made by polycondensation of sodium dicyanamide and a Afunctional primary amine and/or a tetrafunctional primary amine and optionally with a difunctional primary amine. The branched polymeric biguanide compounds have 2-dimensional conformation that provides better coverage over the surfaces of microorganisms and enhances efficacy as biocides as compared to most commercially available linear (one-dimensional) polymeric biguanide compounds. The bulkier 2-dimensional conformation of this invention limits the uptake, accumulation and release of these branched polymers to and from contact lenses. Therefore, these branched biguanide polymers can reduce the cytotoxicity, enhance compatibility and suitable for ophthalmic use. The highly branched polymers can be prepared with minimum or no difunctional primary amines.

Abstract: Biocidal branched quaternary ammonium polymers are made by condensing a difunctional halide with a trifunctional tertiary amine and optionally with a difunctional amine. The branched quaternary ammonium polymers have 2-dimensional conformation that provides better coverage over the surfaces of microorganisms and enhances efficacy as biocides as compared to most commercially available linear (one-dimensional) quaternary ammonium polymers. The bulkier 2-dimensional conformation of this invention limits the uptake, accumulation and release of these branched polymers to and from contact lenses. Therefore, these branched quaternary ammonium polymers can reduce the cytotoxicity, enhance compatibility and suitable for ophthalmic use. The highly branched polymers can be prepared with minimum or no difunctional tertiary amines. The lightly branched polymers can be prepared with of a minimum ratio of trifunctional tertiary amines/difunctional tertiary amines.

Abstract: Biocidal branched quaternary ammonium polymers are made by condensing a difunctional halide with a trifunctional tertiary amine and optionally with a difunctional amine. The branched quaternary ammonium polymers have 2-dimensional conformation that provides better coverage over the surfaces of microorganisms and enhances efficacy as biocides as compared to most commercially available linear (one-dimensional) quaternary ammonium polymers. The bulkier 2-dimensional conformation of this invention limits the uptake, accumulation and release of these branched polymers to and from contact lenses. Therefore, these branched quaternary ammonium polymers can reduce the cytotoxicity, enhance compatibility and suitable for ophthalmic use. The highly branched polymers can be prepared with minimum or no difunctional tertiary amines. The lightly branched polymers can be prepared with of a minimum ratio of trifunctional tertiary amines/difunctional tertiary amines.

Abstract: New polymeric quaternary ammonium compounds with vicinal hydroxyl groups are disclosed. These compounds are useful as disinfectants in contact lens care compositions and/or as preservatives in ophthalmic compositions. Compositions containing these compounds are also disclosed. These compositions are especially useful for disinfecting/cleaning contact lenses.

Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.

Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.

Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.

Abstract: Methods for using hydroxyamino- and amino-substituted pyridine analogs are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of hydroxyamino- and amino-substituted pyridine analogs, are disclosed herein.

Abstract: Methods for using 6-aminoimidazo[1,2-b]pyridazine analogs are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of 6-aminoimidazo[1,2-b]pyridazine analogs, are disclosed herein.

Abstract: Methods for using (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines, are disclosed herein.

Abstract: Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention.

Abstract: Methods for using 6-aminoimidazo[1,2-b]pyridazine analogs are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of 6-aminoimidazo[1,2-b]pyridazine analogs, are disclosed herein.

Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.

Abstract: Methods for using (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines, are disclosed herein.

Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.

Abstract: Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention.

Abstract: Substituted pyranoindoles useful for lowering and controlling IOP and glaucoma are disclosed.