Abstract: The present invention relates to the use of creatine compounds including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds can be used as therapeutically effective agents against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer's disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases.

Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.

Abstract: The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4?-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3?-position of their B aryl ring. Similarly, 3?-amino combretastatin is 4?-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.

Abstract: The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to an anti-inflammatory composition containing docosahexaenoyl lysophosphatidylamine as an active ingredient. Particularly, one of polyunsaturated lysophosphatidylcholines, docosahexaenoyl lysophosphatidylcholine inhibits intracellular NO generation mediated by lipopolysaccharide and suppresses zymosan A induced peritonitis in vivo, suggesting that it has excellent anti-inflammatory effect but has no cytotoxicity, so that it can be effectively used for prevention and treatment of inflammatory disease.

Abstract: Low levels of antibodies reactive with a PAF-conjugate are related to an increased risk of developing cardiovascular diseases. Thus, compositions and methods of diagnosis and therapy for cardiovascular diseases are provided.

Abstract: Provided are compounds, methods and pharmaceutical compositions for treating a host, especially a human, infected with a togavirus, herpes virus and/or coronavirus, and in particular SARS-CoV, cytomegalovirus or varicella-zoster virus. The method in one embodiment comprises administering to that host an effective amount of an anti-togavirus, anti-herpes virus and/or anti-coronavirus phospholipid or a pharmaceutically acceptable salt or prodrug thereof. The phospholipid compound is, e.g., a 3-alkylamido-2-alkoxypropylphosphocholine compound or salt thereof. The compound may be administered alone or in combination and/or alternation with one or more other anti-viral agents.

Abstract: The invention relates to metabolic disease, including non alcoholic fatty liver disease, to risk factors associated with same and to phospholipid-containing compositions.

Abstract: Treatment and/or prevention of sepsis using an enteral composition containing phospholipids, triglycerides and cholesterol or precursors thereof. With the composition of the invention the natural level of chylomicrons is maintained, in particular in gut associated lymphoid tissue (GALT), which ensures that most of LPS and/or LTA which are released in the body can be neutralized, substantially decreasing the risk of locally occurring high levels of LPS and/or LTA and thus sepsis.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)phosphinic acid; and ii) (2R/S, 3R)-(3-amino-2-hydroxybutyl)phosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as processes for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

Abstract: Disclosed is the use of compounds of formula (I) wherein X, Y and Z are as defined in the description of the invention, for the preparation of an antitumor medicament, optionally in combination with different biologically active substances.

Abstract: A pharmaceutical association or combination comprising a therapeutic effective amount of insulin or insulin analogue, and a therapeutic effective amount of a pharmaceutically acceptable betaine, in which the insulin and the betaine possibly form a chemical entity or complex, and in which the amount of betaine is adapted for controlling the degradation and/or for increasing the duration of action and/or for enhancing the therapeutically effect of the insulin or insulin analogue.

Abstract: The present invention relates to methods for treating an infected tissue comprising treating the infected tissue with a formulation comprising a N-halogenated amino acid and a phosphine oxide or amine oxide. This specification also discloses methods for improving the antimicrobial activity of a formulation comprising a N-halogenated amino acid, the method comprising adding a phosphine oxide or amine oxide to said formulation.

Abstract: A method of administering an antifolate to a mammal in need thereof, comprising administering an effective amount of said antifolate in combination with a methylmalonic acid lowering agent.

Abstract: The present invention provides various biomarkers of depression. The present invention also provides various methods of using the biomarkers, including methods for diagnosis of depression, methods of determining predisposition to depression, methods of monitoring progression/regression of depression, methods of assessing efficacy of compositions for treating depression, methods of screening compositions for activity in modulating biomarkers of depression, methods of treating depression, as well as other methods based on biomarkers of depression.

Abstract: Neuro-metabolic and endocrine-function regulating/modulating compositions, are disclosed. The compositions of the present invention comprise Selegiline Hydrochloride, Procaine Hydrochloride, Vinpocetine, trimethylglycine, and an ingredient selected from a group consisting of N-nicotinoyl-gamma-aminobutyric acid (N-GABA), niacin, niacinamide, gamma-aminobutyric acid (GABA), and combinations thereof. Methods of using the compositions, compositions, and compositions of the present invention are also disclosed.

Abstract: The invention relates to the use of alkylphosphocholines in combination with antimetabolite antitumor substances for the treatment of benign and malignant oncoses in humans and animals. It is possible in this connection for the alkylphosphocholines to be employed in a combination according to the invention with one or more antimetabolite antitumor substances. Preferred alkylphosphocholines are described by the Formula II. One such preferred alkylphosphocholine is perifosine.

Abstract: The invention relates to pharmaceutical compositions comprising alkylphosphocholines and antimetabolite antitumor substances. The pharmaceutical compositions of the invention are useful for the treatment of benign and malignant oncoses in humans and animals. Preferred alkylphosphocholines are described by the Formula II. One such preferred alkylphosphocholine is perifosine.

Abstract: The present invention features methods for treating, stabilizing, preventing, and/or delaying cancer by administering nanoparticles that comprise rapamycin or a derivative thereof. The invention also provides compositions (e.g., unit dosage forms) comprising nanoparticles that comprise a carrier protein and rapamycin or a derivative thereof. The invention further provides combination therapy methods of treating cancer comprising administering to an individual an effective amount of nanoparticles that comprise rapamycin or a derivative thereof and a second therapy.

Abstract: Phospholipid-analogous compounds of the general formula (I) in which A where R1 and R2 are, independently of one another, hydrogen, a saturated or unsaturated acyl or alkyl radical which can optionally be branched or/and substituted, where the total of the carbon atoms in the acyl and alkyl is 16 to 44 C atoms, s is an integer from 0 to 8, c is a radical of a primary or secondary alcohol of the formula RO—, where R is a saturated or unsaturated alkyl radical, mainly with cis double bond, of from 12 to 30 carbon atoms, n is an integer from 2 to 8, R3 a can be 1,2-dihydroxypropyl or b can be alkyl with 1 to 3 C atoms when z is >0 or c can be alkyl with 1 to 3 carbon atoms when n?2 and z=0, m is 1 or 2, x is an integer from 0 to 8, y is 1 for z=1 to S? or is 1 to 4 for z=1 z is an integer from 0 to 5, are novel and are suitable as liposome constituents, solubilizers and pharmaceuticals.

Abstract: Compositions and methods for treating mitochondrial disorders are provided. The compositions include compounds having a mitochondrial targeting moiety, for example a lipophilic cation. Certain compounds are effective for increasing the ratio of phosphocreatine/creatine in a host, for example a mammal. Other compounds decrease the ratio of phophocreatine/creating in a host. An exemplary compound is defined by the following structure (Formula Ia): wherein R1 is H or phosphate and the double bond is between N1 and C1 or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N1 C1, and N together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: The invention relates to a process for controlling plant pathogens comprising the application of alkylphospholipids as active substances. Further, the invention relates to the use of alkylphospholipids for controlling plant pathogens, and to an agent for controlling plant pathogens containing an effective amount of at least one alkylphospholipid.

Abstract: Chronic obstructive airway diseases are treated by administering an osmotically active compound such as a salt, sugar, sugar alcohol, or organic osmolyte to the afflicted airway surface. The compound may be administered as a liquid or dry powder aerosol formulation. Diseases that can be treated by the method include cystic fibrosis, chronic bronchitis, and ciliary dyskinesia. The formulations of the invention can also be used in conjunction with other active agents such as bronchodilators, sodium channel blockers, antibiotics, enzymes, or purinoceptor agonists on airway surfaces.

Abstract: The invention relates to the use of oleyl phosphocholine and oleyl-phospho-(N.N.-dimethyl-N-ethyl)-ethyl-ammonium for the long-term and continuous treatment of serious illnesses, such as cancer, leishmaniasis, ehrlichiosis, multiple sclerosis and psoriasis, in addition to other indications mentioned in the application.

Abstract: We disclose a method of activating soluble guanylyl cyclase (sGC) in a patient, comprising administering to the patient a composition comprising a corrin and a pharmaceutically-acceptable carrier. We also disclose a composition, comprising a corrin, an NO-independent sGC activator selected from the group consisting of BAY 41-2272, BAY 58-2667, HMR1766, YC-I, and S3448, and a pharmaceutically-acceptable carrier.

Abstract: The present invention relates to new quinazoline inhibitors of EGFR tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new steroid modulators of progesterone receptor activity and/or glucocorticoid receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: It is an object of the present invention to provide a means for promoting amyloid protein degradation and a means for inhibiting amyloid protein aggregation. The present invention relates to a composition for promoting amyloid protein degradation, a composition for inhibiting amyloid protein aggregation, and a composition for preventing or treating diseases associated with amyloidosis, each of which comprises a plasmalogen as an active ingredient.

Abstract: In one embodiment, the invention provides a method of suppressing, inhibiting, preventing, or treating conjunctivitis in a subject, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound via an ester or amide bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof to a subject with conjunctivitis.

Abstract: A lipid preparation including a glycerophospholipid or salt, conjugate and derivatives thereof, particularly phosphatidylserine (PS), phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidyl-inositol (PI), phosphatidylglycerol (PG) and phosphatidic acid (PA), and poly-unsaturated fatty acid (PUFA) acyl groups, particularly long-chain poly-unsaturated fatty acid (LC-PUFA) acyl groups such as omega-3 and/or omega-6 acyl groups, wherein said PUFA is covalently bound to said glycerophospholipid. The preparation possesses an improved bioactivity, and is useful in the treatment of various cognitive and mental conditions and disorders and for maintenance of normal functions of brain-related systems and processes.

Abstract: Liquid formulations of bone morphogenetic proteins are provided for prolonged use at elevated temperatures. More specifically, the invention relates to liquid formulations comprising rhGDF-5, trehalose, and one or more biocompatible excipients that provide stability to the protein for at least 30 days at temperatures up to body temperature.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell.

Abstract: The invention provides a new class of compounds capable of inhibiting carnitine palmitoyl transferase (CPT) having formula (I) The invention also relates to pharmaceutical compositions, which comprise at least one new compound according to the invention, and their therapeutic use in the treatment of hyperglycaemic conditions such as diabetes and the pathologies associated with it, such as for example congestive heart failure and obesity.

Abstract: The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.

Abstract: The expression of a steroid receptor from circulating carcinoma cells in a blood sample is detected by isolating the carcinoma cells from the blood sample, making an extract from the isolated carcinoma cells and then performing on the extract a sensitive immunoassay capable of detecting the carcinoma cell-associated steroid receptor. A positive result indicates the presence of the steroid receptor in the carcinoma cells. This method can be used to identify cancer patients who are likely to benefit from treatment with an endocrine therapeutic agent.

Abstract: The present invention provides animal models and methods for the evaluation of maternal treatments that could improve or compromise the epigenetic state, the imprinting, or the DNA methylation and thus the health or disease propensity, of human or other mammalian offspring. In particular, the present invention provides animal models with naturally occurring epigenetic variation for the evaluation of treatments through effects on the epigenetically determined and imprinted characteristics of coat color, coat color pattern, DNA methylation, long terminal repeat (LTR) expression and LTR activity of offspring.

Abstract: Disclosed are systems and methods as may be used for development of compounds that can be utilized for prevention of pathological calcification. Disclosed are functional models can represent in great detail the first steps in protein-membrane interaction leading to calcification. Disclosed compounds include those that interfere with pathologic calcification processes and thus may be used as part of a formulation or composition for preventing pathological calcifications. Modeling methods and systems can include in vitro and/or in silico dynamic molecular modeling of biological materials including representative mineralization models in conjunction with substances that can affect normal or pathogenic calcification processes. Disclosed models can examine interactions of biological components involved in calcification including calcium, inorganic phosphate, phosphatidylserine, and annexin-5 protein.

Abstract: A method for the treatment or prevention of tissue damage in a subject having an inflammatory and/or tissue damaging condition, which comprises administering to the subject an effective amount of a compound capable of inhibiting the binding of C-reactive protein (CRP) to an autologous or extrinsic ligand.

Abstract: A liposome formulation for stably incorporating high content of hydrophobic substance is disclosed. The liposome includes two phospholipids with different phase transition temperatures such as saturated and unsaturated phosphatidyl cholines, hydrophobic substances, cholesterol, cholesterol derivatives, antioxidant and hydrophilic polymer-modified lipids such as MPEG-DSPE.

Abstract: The present invention relates of the use of certain inner ionic (zwitter ionic) phospholipids, phosphonolipids and phosphate derivatives for the preparation of a pharmaceutical composition for the treatment, prevention and/or amelioration of an immunological disorder related to mast cell sensitization. Preferred in this context are edelfosine and miltefosine. In a particularly preferred embodiment, the present invention relates to the use of miltefosine for the preparation of a pharmaceutical composition for the treatment, prevention and/or amelioration of allergic diseases, in particular acute hyperallergic diseases, like asthma.

Abstract: The present invention relates to methods of treating Alzheimer's Disease which utilize agents that increase neuronal phosphotidylinositol 4,5-biphosphate (PIP2), and to differentiated stem cell-based assay systems that may be used to identify agents that modulate phosphoinositide levels and thereby treat a variety of diseases. It is based, at least in part, on the discovery that edelfosine, an agent that increases PIP2 levels by inhibiting an enzyme that catalyzes PIP2 breakdown, decreases levels of neurotoxic A&bgr;42 peptide, particularly in cells expressing a mutant presenilin gene associated with Familial Alzheimer's Disease.

Abstract: The present invention relates to ophthalmic compositions such as contact lens care solutions, containing miltefosine. The present invention further relates to ophthalmic compositions or contact lens care systems containing miltefosine in combination with additional other active microbiocidal substances or proteases. Furthermore, the invention relates to the use of the compositions for the removal and eradication of protozoan parasites such as Acanthamoeba from contact lenses.

Abstract: The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the activity of the viral infection.

Abstract: The use of certain synthetic phospholipids to preserve pharmaceutical compositions from microbial contamination is described. The synthetic phospholipids have unique molecular arrangements wherein a phosphate group is linked to a quaternary ammonium functionality via a substituted-propenyl group, and the quaternary ammonium functionality is further linked to at least one long hydrocarbon chain. Such molecular arrangements are what make the phospholipids of formula (I) highly water soluble, e.g., the length of the hydrocarbon chain assists to maintain solubility and efficacy of the molecules for the uses described herein. The synthetic phospholipids described herein have been found to be particularly useful as antimicrobial preservatives for ophthalmic, otic and nasal pharmaceutical compositions, especially ophthalmic compositions. These compounds may also be utilized to disinfect contact lenses.

Abstract: Novel synthetic oxidized lipids and methods utilizing oxidized lipids for treating and preventing an inflammation associated with an endogenous oxidized lipid are provided.

Abstract: The invention as disclosed herein provides pharmaneutical compositions and methods for treating, ameliorating, or preventing the symptoms of fatty acids imbalance and cell membrane dysfunction. The pharmaneutical compositions of the invention contain in an effective amount a first and a second composition, the first composition comprises an effective amount of one or more phosphatidylcholine formulations and the second composition comprises an effective amount of one or more constituents comprising essential fatty acid supplements, trace minerals, phenylbutyrate, electrolytes, methylating agents, reduced glutathione, or a combination thereof, in a suitable carrier.

Abstract: Pharmaceutical composition for regulation of pancreatic juice secretion characterized by comprising a lisophosphatidic acid (LPA) receptor modulator. Since an LPA receptor modulator has an effect of regulating the secretion of pancreatic juice, a compound acting on this receptor is useful in treating diseases in association with disorders in pancreatic juice secretion. For example, an LPA receptor agonist is useful in treating and/or preventing pancreatic diseases and obesity, while an LPA receptor antagonist is useful in treating and/or preventing maldigestion, constipation, diarrhea and cibophobia.

Abstract: The present invention aims at providing a phospholipid membrane preparation wherein an antigen or an allergen is bound onto the surface of a phospholipid membrane comprising a phospholipid containing an acyl group or a hydrocarbon group having 10 to 12 carbon atoms, and a stabilizer of a phospholipid membrane. The present invention provides a phospholipid membrane preparation having an immune response controlling function that suppresses production of IgE antibody to increases production of practically sufficient IgG antibody and usable as a vaccine that does not easily cause an allergic response.

Abstract: The invention concerns biphosphonic compounds of formula (I); microbiological anti-contamination compositions containing same, and their use for preventing or limiting fixing of macromolecules, micro-organisms and biofilm on solid surfaces, such as metal or mineral surfaces.