Abstract: Provided herein are novel amide prodrug forms of pharmaceutically active agents useful for central nervous system disorders.

Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.

Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention relates to beta-O/S/N fatty acids and derivatives thereof, in particular the compounds of formula (I) as described and defined herein, and their pharmaceutical use, including their use in the treatment or prevention of bacterial as well as protozoan infections, in particular the treatment or prevention of infections with Gram-positive and/or Gram-negative bacteria and infectious diseases caused by and/or related to Gram-positive and/or Gram-negative bacteria. The invention further relates to the use of these compounds for preventing or eliminating biofilms.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.

Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention relates to a process for the purification of crude bimatoprost to obtain pure bimatoprost comprising a chromatography, preferably a chromatography using an achiral stationary phase and an eluent comprising an alcohol and an apolar solvent; and crystallization of the product obtained the chromatography to obtain pure bimatoprost.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: The present invention provides a new crystalline form of bimatoprost, designated as crystalline form II. This new crystalline form is the most stable form known to date of bimatoprost. Moreover, it has been found that bimatoprost crystalline form II is readily prepared from crystalline form I.

Abstract: Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.

Abstract: The crystalline form A of Bimatoprost of formula I, its preparation method and use are provided. There are characteristic peaks where diffraction angles 2? are 3.2±0.2°, 5.5±0.2°, 11.4±0.2°, 16.7±0.2°, 17.6±0.2°, 19.9±0.2°, 20.8±02° and 22.8±0.2° in the X-ray powder diffraction pattern of the crystalline form A.

Abstract: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

Abstract: The present invention provides a new crystalline form of bimatoprost, designated as crystalline form II. This new crystalline form is the most stable form known to date of bimatoprost. Moreover, it has been found that bimatoprost crystalline form II is readily prepared from crystalline form I.

Abstract: The present invention relates to a process for preparing a prostaglandin derivative and an intermediate therefor. In accordance with the present invention, the prostaglandin F (PGF) derivative can be efficiently prepared with high purity by removing the protecting group of a protected prostaglandin E (PGE) derivative obtained from conjugate addition and then stereoselectively reducing the ketone group on the cyclopentanone ring of the PGE derivative.

Abstract: A method for a prevention and/or treatment of irritable bowel syndrome or amelioration of a symptom thereof in a subject, comprises administering to said subject an effective amount of a compound of formula I:

Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.

Abstract: A process for preparing a prostaglandin analogue comprising a step of converting a compound of formula (8?): to the prostaglandin analogue, wherein R3 represents hydrogen or a hydroxyl protecting group.

Abstract: Microwave irradiation is used to synthesize graphene and metallic nanocatalysts supported on graphene either by solid or solution phase. In solid phase methods, no solvents or additional reducing agents are required so the methods are “environmentally friendly” and economical, and the graphene and nanocatalysts are substantially free of residual contaminants. Recyclable, high efficiency Pd nanocatylysts are prepared by these methods.

Abstract: The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.

Abstract: The present invention is directed to compositions and methods for enhancing the health of nails and cuticles in a mammal, including humans. The compositions may be administered topically to the nail bed, nail matrix and cuticle in an amount effective to enhance nail health. The composition is also effective in strengthening and growing nails.

Abstract: Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.

Abstract: The crystalline form A of Bimatoprost of formula I, its preparation method and use are provided. There are characteristic peaks where diffraction angles 2? are 3.2+0.2°, 5.5+0.2°, 11.4+0.2°, 16.7+0.2°, 17.6+0.2°, 19.9+0.2°, 20.8±02° and 22.8+0.2° in the X-ray powder diffraction pattern of the crystalline form A.

Abstract: The invention relates to a novel hydroxyphenyl compound, to the preparation of the compound and intermediates used therein, to the use of the compound as an antibacterial medicament and pharmaceutical compositions containing the compound.

Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.

Abstract: The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions.

Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.

Abstract: The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: The present invention relates to a process for preparing a prostaglandin derivative and an intermediate therefor. In accordance with the present invention, the prostaglandin F (PGF) derivative can be efficiently prepared with high purity by removing the protecting group of a protected prostaglandin E (PGE) derivative obtained from conjugate addition and then stereoselectively reducing the ketone group on the cyclopentanone ring of the PGE derivative.

Abstract: The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3? each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.

Abstract: The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.

Abstract: The invention concerns a new process for the preparation of prostaglandin derivatives, in particular prostaglandin F2? derivatives, for example bimatoprost, latanoprost and travoprost, the new intermediates of said process and their use in the preparation of prostagblandin derivatives.

Abstract: The invention provides a novel polymorphic form I of crystalline bimatoprost, method for preparation thereof and new crystalline intermediates in the preparation. This form I of crystalline bimatoprost is used in purification of crude bimatoprost and in storage of bimatoprost as active pharmaceutical intermediate. Use of the physical form of bimatoprost in the manufacture of a medicament is also disclosed.

Abstract: The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract: PROBLEM Provided is a seed treatment agent having excellent control effect on plant diseases and a method for protecting a plant from plant diseases. SOLUTION A seed treatment agent comprising, as an active ingredient, an ?-methoxyphenylacetic acid compound represented by formula (1).

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: The present invention provides a new crystalline form of bimatoprost, designated as crystalline form II. This new crystalline form is the most stable form known to date of bimatoprost. Moreover, it has been found that bimatoprost crystalline form II is readily prepared from crystalline form I.

Abstract: The invention provides a novel polymorphic form I of crystalline bimatoprost, method for preparation thereof and new crystalline intermediates in the preparation. This form I of crystalline bimatoprost is used in purification of crude bimatoprost and in storage of bimatoprost as active pharmaceutical intermediate. Use of the physical form of bimatoprost in the manufacture of a medicament is also disclosed.

Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein emulsions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal.

Abstract: Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.

Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.

Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.

Abstract: The present invention provides a method of forming an ion of formula (I) comprising the steps of: (i) reacting a compound of the formula (IIa); with a biopolymer, BP, having at least one group capable of reacting with M to form a covalent linkage, to provide a biopolymer derivative of the formula (IIIa); and (ii) cleaving the C—X bond between X and the ?-carbon atom of the derivative of formula (IIIa) to form the ion of formula (I); where: (IV) is a carbon atom bearing a single positive charge or a single negative charge; and X is a group comprising a thioether sulphur atom bound directly to the ?-carbon which is capable of being cleaved from the ?-carbon atom to form an ion of formula (I). The biopolymer derivatives of the invention have enhanced ionisability with respect to free biopolymer (BP) enabling improved analysis of the biopolymer using mass spectrometry.

Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.

Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

Abstract: The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.