Abstract: The present disclosure provides adamantyl compounds having one or more amine groups and one or more nitrate groups. The aminoadamantyl nitrate compounds can be used to treat disorders of the central nervous system, including neurodegenerative and non-neurodegenerative diseases.

Abstract: The present invention relates to amantadine nitrate compounds having neural protective effect, and preparation method and medical use thereof. The compounds have the structure of the general formula (II). The compounds have multifunctional mechanisms, including inhibiting NMDA receptors, releasing NO, inhibiting calcium influxes, and having protective effects on cells particularly neurocytes. The compounds can be used in the preparation of medicaments having a cellular protective effect, for prevention or treatment of the diseases related to such as NMDA receptors and elevation of calcium anions in cells, including the diseases related to neurodegeneration such as Alzheimer's disease, Parkinson's disease, cerebral paralysis and glaucoma, and the diseases related to cardio-cerebral-vascular system such as Parkinson's syndrome combined with cerebral arteriosclerosis, as well as respiratory tract infections caused by influenza virus.

Abstract: The present invention relates to amantadine nitrate compounds having neural protective effect, and preparation method and medical use thereof. The compounds have the structure of the general formula (I). The compounds have multifunctional mechanisms, including inhibiting NMDA receptors, releasing NO, inhibiting calcium influxes, and having protective effects on cells particularly neurocytes. The compounds can be used in the preparation of medicaments having a cellular protective effect, for prevention or treatment of the diseases related to such as NMDA receptors and elevation of calcium anions in cells, including the diseases related to neurodegeneration such as Alzheimer's disease, Parkinson's disease, cerebral paralysis and glaucoma, and the diseases related to cardio-cerebral-vascular system such as Parkinson's syndrome combined with cerebral arteriosclerosis, as well as respiratory tract infections caused by influenza virus.

Abstract: The present invention relates generally to the cosmetic treatment of aged skin. More specifically, the invention relates to the use of ingenol compounds, particularly ingenol angelates, in treating photo-aged and/or chronologically-aged skin.

Abstract: A compound of Formula I or pharmaceutically acceptable salt thereof and its preparation method and applications, the new structure of the compound of formula I has not been reported in literature. It is isolated from Isodon forrestii var. forrestii and can be a compound served as Trx1 selective inhibitor. The present invention further discloses a pharmaceutical composition, preparation of the compound of Formula I and its applications in preparing medicines for preventing or treating cancer. Iso A of the present invention has the advantages of low toxicity, high safety and strong pharmacological effect, which suggests a potential prospect in pharmaceutical applications.

Abstract: The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.

Abstract: The invention provides ingenol compounds for treating seborrheic keratosis.

Abstract: A substantially anhydrous pharmaceutical gel composition for cutaneous application comprising an ingenol derivative in dissolved or solubilized form, a solvent mixture of (a) a hydrophilic non-ionic surfactant; (b) a lipophilic non-ionic co-surfactant; (c) an oil; the composition further comprising an acidic compound, a co-solvent, a viscosity-increasing agent and a pharmaceutically acceptable, substantially anhydrous, non-solvent lipid carrier.

Abstract: The present invention relates to cyclic or repeated use of the ingenol mebutate for topical treatment of actinic keratosis lesions. Generally speaking, the present invention comprises a first ingenol mebutate treatment cycle and a second ingenol mebutate treatment cycle, wherein the first treatment cycle topically treats a treatment area with a topical gel formulated with ingenol mebutate at a selected dosage strength for a specified treatment regimen, and the second ingenol mebutate treatment cycle comprises topically re-treating the treatment area with the same topical ingenol mebutate gel for the same specified treatment regimen, if following the first treatment cycle, the treatment area failed to clear or failed to remain clear of AK lesions. The present invention further relates to spot or individual lesion therapy in the treatment area following the topical bi-cyclic therapy with ingenol mebutate.

Abstract: The present invention broadly relates to the use of certain ingenol derivatives as HIV reactivators of latent HIV virus in viral reservoirs. In another aspect, the present invention relates to an association comprising such ingenol derivatives and antiretroviral agents substantially active against actively replicating virus.

Abstract: The invention relates to the treatment of actinic keratosis (AK) lesions using sequential cryotherapy and field treatment with ingenol mebutate (e.g., PEP005 Gel).

Abstract: A targeted osmotic lysis (TOL) of tumor cells that over-express voltage-gated sodium channels (VGSCs) has been developed that uses a combined therapy of a drug that blocks sodium, potassium-adenosine triphosphatase (Na+, K+-ATPase) that is then followed by an activation of VGSCs, for example, by electrical or pharmacological stimulation. Activation of VGSCs conducts sodium into the cancer cells in much greater amounts than non-cancer cells. Water follows this sodium gradient into the cancer cells, causing swelling and lysis. Because non-cancerous cells do not over-express VGSCs, less sodium and less water will enter the cells, and the non-cancerous cells will not lyse. This method is applicable to all cells that over-express VGSCs, including, but not limited to, highly invasive breast cancer, prostate cancer, small cell lung cancer, non-small cell lung carcinoma, lymphoma, mesothelioma, neuroblastoma, and cervical cancer.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Substantially anhydrous topical gel compositions comprising a homogeneous mixture of: (a) ingenol-3-angelate in dissolved form; and (b) anon-aqueous carrier.

Abstract: The present invention relates to a topical gel composition comprising ingenol-3-angelate, wherein the composition provides greater flux, according to the in vitro diffusion test, of ingenol-3-angelate into the stratum corneum, epidermis and dermis after application of the gel composition to skin than does a reference gel of ingenol-3-angelate, namely the PICATO® product.

Abstract: A topical composition for cutaneous application which is a water-in-oil emulsion comprises an oily phase comprising (a) an ingenol derivative in dissolved form; (b) at least one non-ionic surfactant selected from the group consisting of polyoxyl glycerides, polyoxyethylene castor oil derivatives, polyoxyethylene alkyl ethers, polysorbates, or a mixture of acrylamide acryloyldimethyl taurate copolymer, isohexadecane and polysorbate 80, sterols, fatty alcohols, fatty acid phosphonates, mono- or diglycol esters, mono- di- or polyglyceryl esters, mono-, di- or plyglucose esters, sucrose esters or sorbitan esters, the non-ionic surfactant being present in an amount of from about 0.5% by weight to about 10% by weight of the composition; (c) a solvent for the ingenol derivative; and an aqueous phase buffered to a pH of 2.6-3.7.

Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.

Abstract: Analgesic compounds for treatment of pain or fever, comprising a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering the compounds.

Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: The present invention relates to novel crystalline forms of ingenol ingenol-3-angelate and methods of preparation and use thereof. More specifically, the invention relates to a novel crystalline form and purified forms of the compound of Formula 1 (ingenol-3-mebutate; ingenol-3-angelate; isoform ‘b’; PEP005), which is characterized by, for example, attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy, single crystal X-Ray crystallography (XRC), X-ray powder diffraction, and, Differential Scanning Calorimetry (DSC), and methods of preparation and use thereof.

Abstract: The present invention is directed to the prophylatic field treatment of photodamaged skin with topical ingenol mebutate. More specifically, the present invention concerns field-directed treatment of UV-damaged skin with topical ingenol mebutate for reducing the number of skin lesions that emerge from the UV-damaged skin over time. In addition, the present invention concerns field-directed treatment for removing photodamaged skin, mutated keratinocytes, cutaneous immunosuppressive environments and/or p53+ patches caused by UV with topical ingenol mebutate. By way of example, the present invention is directed to treating photodamaged skin with topical ingenol mebutate at about 0.05% concentration. The present invention is also concerned with the treatment of SCC tumors with topical ingenol mebutate for reducing the number of SCC tumors. By example, the present invention is directed to treating and curing SCC xenografts with topical ingenol mebutate at about 0.25% concentration.

Abstract: Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.

Abstract: A composition is provided that, when utilized in combination with warfarin, greatly improves the anticoagulant effects of warfarin in mammalian subjects. The composition is a compound having a naphthohydroquinone ring system substantially similar to the ring system of the reduced form of vitamin K1 and has the general formula: where R1 and R4 are hydrogen or acyl, R2 is a saturated or unsaturated alkyl group with up to 6 carbons, and R3 is a saturated or unsaturated alkyl group with up to 20 carbons, or R2 and R3 are part of a cyclic or polycyclic ring system.

Abstract: The present invention relates to a novel crystalline form of ingenol mebutate, methods of preparation thereof, and to its use. More specifically, the invention relates to the conversion of amorphous ingenol mebutate (ingenol-3-angelate, PEP005) to a crystalline form, which was characterized by single crystal X-Ray crystallography (XRC), attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy and Differential Scanning calorimetry (DSC).

Abstract: An improved drug delivery composition and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative. The composition can be administered as is or after being be dissolved or rapidly reconstituted in an aqueous vehicle to afford a homogeneous solution or uniform colloidal systems.

Abstract: The invention relates to compounds of general formula I, (I), wherein R is wherein R is aryl substituted by R3; or R is (C3-Ci3)-cycloalkyl, (C3-Ci3)-cycloalkenyl or (C7-Ci3)-cycloalkynyl optionally substituted by R4; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

Abstract: The invention relates to compounds of general formula (I) wherein R is (C1-C7)alkyl, (C2-C7)alkenyl or (C2-C7)alkynyl; wherein R is substituted with R1; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

Abstract: Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.

Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.

Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.

Abstract: Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: A targeted osmotic lysis (TOL) of tumor cells that over-express voltage-gated sodium channels (VGSCs) has been developed that uses a combined therapy of a drug that blocks sodium, potassium-adenosine triphosphatase (Na+, K+-ATPase) that is then followed by an activation of VGSCs, for example, by electrical or pharmacological stimulation. Activation of VGSCs conducts sodium into the cancer cells in much greater amounts than non-cancer cells. Water follows this sodium gradient into the cancer cells, causing swelling and lysis. Because non-cancerous cells do not over-express VGSCs, less sodium and less water will enter the cells, and the non-cancerous cells will not lyse. This method is applicable to all cells that over-express VGSCs, including, but not limited to, highly invasive breast cancer, prostate cancer, small cell lung cancer, non-small cell lung carcinoma, lymphoma, mesothelioma, neuroblastoma, and cervical cancer.

Abstract: The invention provides for the use of protein kinase activators or boosters of nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF) or other neurotrophic factors to treat stroke. Specifically, the present invention provides methods of treating stroke comprising the steps of identifying a subject having suffered a stroke and administering to said subject an amount of a pharmaceutical composition comprising a protein kinase C (PKC) activator or 4-methylcatechol acetic acid (MCBA) and a pharmaceutically acceptable carrier effective to treat at least one symptom of stroke.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Abstract: The present invention concerns methods for treating and preventing renal/kidney disease, insulin resistance/diabetes, fatty liver disease, and/or endothelial dysfunction/cardiovascular disease using synthetic triterpenoids, optionally in combination with a second treatment or prophylaxis.

Abstract: Process for the preparation of a compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a compound of formula IIa or in a mixture of a compound of formula IIa with a compound of formula IIb and isolating a compound of formula I from the reaction mixture; compounds and salts of compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a compound of formula I.

Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: A coating on a balloon of a medical device is provided. The coating comprises a drug and a polymer. Also provided are methods of forming and using the coating.

Abstract: Improved antibiotic analogs, and synergistic combinations of antibiotics designed based on structural crystallographic analysis, are provided as well as pharmaceutical compositions that include these improved analogs and synergistic combinations, along with methods for their production and use. The synergistic combinations target neighboring sites in the ribosome demonstrating the importance of the corresponding ribosomal sites for development of clinically-relevant synergistic antibiotics.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: This invention refers to pharmaceutical use of multicyclic compounds chosen from ingenols, lanosta-8,24-dien-3-ols and their mixtures, as anti-AIDS agents.

Abstract: The present invention relates generally to the field of cancer including tumor therapy. More particularly, the present invention relates to the treatment of solid cancers, including solid tumors, and the prevention or reduction of cancer metastasis, by chemoablation of cancer cells by an agent which also stimulates the generation of cancer-specific T-cells, a process referred to herein as immunostimulatory chemoablation. The present invention further contemplates combination therapy comprising immunostimulatory chemoablation and one or more other therapeutic regimens, which enhance, co-operate and/or synergize with the cancer-specific T-cells induced by the chemoablation. The present invention also relates to pharmaceutical compositions for use in treating cancers.

Abstract: The present invention provides methods of manufacturing a sterile ciclesonide-containing aqueous suspension comprising the step of sterilization by autoclaving a ciclesonide-containing aqueous suspension.

Abstract: The provision of animal feed pellets is described, which pellets comprise, as antibiotic, a pleuromutilin derivative is stabilized form, namely in the form of microspherules. The pleuromutilin derivatives in question have the general formula (I) wherein R1 is ethyl or vinyl, there is either a double bond or a single bond between carbon atoms 1 and 2, Ra and Rb are each independently of the other hydrogen or halogen, and T is a short or long-chain organic radical.