Abstract: Base compounds including 1,3-oxazinan-6-one derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde, and their application as corrosion inhibitors with multifunctional properties serving as inhibitory/dispersant of asphaltene in production processes, transportation, refining and storage of crude oil and derivatives. The corrosion inhibitor with inhibitory/dispersant of asphaltenes properties comprises an active substance base of 1,3-oxaninan-6-ones and hydrocarbon solvents such as benzene, toluene, mixed xylenes, o-xylene, m-xylene and p -xylene, diesel, kerosene, jet fuel, alcohols, aliphatic branched and unbranched alcohols containing from 3 to 10 carbon atoms, such as isopropanol, butanol and pentanol, and mixtures of hydrocarbon solvents with aliphatic branched or unbranched liquid fuels. In addition, a process for obtaining 1,3-oxazinan-6-ones derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde is described.

Abstract: Base compounds including 1,3-oxazinan-6-one derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde, and their application as corrosion inhibitors with multifunctional properties serving as inhibitory/dispersant of asphaltene in production processes, transportation, refining and storage of crude oil and derivatives. The corrosion inhibitor with inhibitory/dispersant of asphaltenes properties comprises an active substance base of 1,3-oxaninan-6-ones and hydrocarbon solvents such as benzene, toluene, mixed xylenes, o-xylene, m-xylene and p-xylene, diesel, kerosene, jet fuel, alcohols, aliphatic branched and unbranched alcohols containing from 3 to 10 carbon atoms, such as isopropanol, butanol and pentanol, and mixtures of hydrocarbon solvents with aliphatic branched or unbranched liquid fuels. In addition, a process for obtaining 1,3-oxazinan-6-ones derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde is described.

Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.

Abstract: Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.

Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.

Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.

Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.

Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.

Abstract: Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors.

Abstract: This invention relates to novel compounds of the Formula (I), dependent compounds of Formula (II), (II-A), (II-B), (II-C), (II-D), (II-E), (II-F), (II-G), (II-H), (III), (III-A), (III-B), (III-C), (IV), (IV-A), (IV-B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ic), (Ie), (If), (Ig), (Ih), (Ii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: The present invention is directed to a process for the production of high density polyethylene by polymerisation of ethylene in the presence of a supported chromium oxide based catalyst which is modified with an organic compound comprising oxygen and a nitrogen atom which is selected from the group consisting of saturated heterocyclic organic compounds with a five or six membered ring, amino esters and amino alcohols. Such organic compounds allow manufacturing of HDPE with increases molecular weight distribution and increased molecular weight.

Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof. Values for the variables in Formula (I) are defined herein.

Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.

Abstract: Provided herein are processes for the production of methionine or selenomethionine from homoserine. In particular, the processes proceed via the production of carbamate intermediates.

Abstract: Disclosed are syntheses of 11?-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).

Abstract: Provided herein are processes for the production of methionine or selenomethionine from homoserine. In particular, the processes proceed via the production of carbamate intermediates.

Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.

Abstract: A one pot method of preparing cyclic carbonyl compounds comprising an active pendant pentafluorophenyl ester group is disclosed. The cyclic carbonyl compounds can be polymerized by ring opening methods to form ROP polymers comprising repeat units comprising a side chain pentafluorophenyl ester group. Using a suitable nucleophile, the pendant pentafluorophenyl ester group can be selectively transformed into a variety of other functional groups before or after the ring opening polymerization.

Abstract: Disclosed is a compound represented by Formula (I): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (I) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (I) are defined herein.

Abstract: Disclosed are syntheses of 11?-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).

Abstract: This invention relates to novel compounds of the Formula (I), (II), (II-A), (II-B), (II-C), (II-D), (III). (III-A). (IIII-B). (III-C). (III-D), (III-E) (IV), (IV-A), (IV-B). (IV-C), (IV-D). (V), (V-A), (V-B), (V-C), (V-D), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: This invention relates to substituted 1,3-oxazin-2-one compounds of the Formula (I), (II), (IIA), (IIB), (IIC), (II D), (IIE), (III), (III A), (III B), (IV), (IV A), (IV B), (IV C), (IV D), (V), (V A), (V B), (VI), (VI A), (VI B), (VII), (VII A), (VII B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.

Abstract: A one pot method of preparing cyclic carbonyl compounds comprising an active pendant pentafluorophenyl ester group is disclosed. The cyclic carbonyl compounds can be polymerized by ring opening methods to form ROP polymers comprising repeat units comprising a side chain pentafluorophenyl ester group. Using a suitable nucleophile, the pendant pentafluorophenyl ester group can be selectively transformed into a variety of other functional groups before or after the ring opening polymerization.

Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: This invention relates to novel compounds of the Formula (I), dependent compounds of Formula (II), (II-A), (II-B), (II-C), (II-D), (II-E), (II-F), (II-G), (II-H), (III), (III-A), (III-B), (III-C), (IV), (IV-A), (IV-B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.

Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.

Abstract: Novel herbicides are provided. A haloalkylsulfonanilide derivative represented by the formula (1) or an agrochemically acceptable salt thereof: the formula (1): wherein Z is —C(R9)(R10)— or —N(R11)—, A is an oxygen atom, a sulfur atom or —N(R12)—, W is an oxygen atom or a sulfur atom, m is an integer of from 0 to 3, n is an integer of from 0 to 3, m+n is from 1 to 3, R1 is halo C1-C6 alkyl, R2 is a hydrogen atom, C1-C6 alkyl or the like, each of R3 and R4 is independently a hydrogen atom, C1-C6 alkyl or the like, each of R5, R6, R7, R8, R9 and R10 is independently a hydrogen atom, a halogen, C1-C6 alkyl or the like, each of R11 and R12 is a hydrogen atom, C1-C6 alkyl, halo C1-C6 alkyl or the like, and X is independently a hydrogen atom, a halogen, C1-C6 alkyl, or the like.

Abstract: This invention relates to novel compounds of the Formula Formulas (I), (Ia1-20), (Ib1-20), (Ic1-20), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: Base compounds including 1,3-oxazinan-6-one derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde, and their application as corrosion inhibitors with multifunctional properties serving as inhibitory/dispersant of asphaltene in production processes, transportation, refining and storage of crude oil and derivatives. The corrosion inhibitor with inhibitory/dispersant of asphaltenes properties comprises an active substance base of 1,3-oxaninan-6-ones and hydrocarbon solvents such as benzene, toluene, mixed xylenes, o-xylene, m-xylene and p -xylene, diesel, kerosene, jet fuel, alcohols, aliphatic branched and unbranched alcohols containing from 3 to 10 carbon atoms, such as isopropanol, butanol and pentanol, and mixtures of hydrocarbon solvents with aliphatic branched or unbranched liquid fuels. In addition, a process for obtaining 1,3-oxazinan-6-ones derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde is described.

Abstract: Disclosed are syntheses of 11?-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).

Abstract: A haloalkylsulfonanilide derivative represented by general formula (I) or a salt thereof wherein R1 represents a halo(C1-C8)alkyl group, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent hydrogen atoms, etc., n represents 1 or 2, A represents an oxygen atom, W represents an oxygen atom, X represents a halogen atom and m represents an integer of 0 to 4, are compounds useful as herbicides having both of remarkable herbicidal effect and characteristics such as excellent crop-weed selectivity.

Abstract: This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell.

Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.

Abstract: Provided herein are processes for the production of methionine or selenomethionine from homoserine. In particular, the processes proceed via the production of carbamate intermediates.

Abstract: The invention is directed to a process for the preparation of cyclic carbamates of formula and/or a salt thereof, from the corresponding o-aminobenzyl alcohol and/or a salt thereof.

Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie),(If), (Ig), (Ih), (Ii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

Abstract: This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 Ia1-3-Ij1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih); (Ii); (Ij), (Ik), (II) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: A PEPCK inhibitor can include identifying a molecule that has a size capable of fitting into and interacting with the PEPCK binding site and at least one of the following: (a) a first terminal substituent having co-planar atoms acting as metal ligands to the active site metal ion PEPCK; (b) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent includes a neutral carbon center or include an oxygen, sulfur, selenium, or other atom with similar physiochemical properties; (c) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent is devoid of an electropositive atom or substituents; or (d) a second terminal substituent opposite of the first terminal substituent, said second terminal substituent having an atom that is a hydrogen boding acceptor and/or is negatively charged.

Abstract: The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.

Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.

Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:

Abstract: Disclosed are syntheses of 11 ?-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).

Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.