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Monocyclic

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514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514002000 - Peptide containing (e.g., protein, peptones, fibrinogen, etc.) DOAI

514009000 - Cyclopeptides

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DocumentTitleDate
20090298752APLIDINE TREATMENT OF CANCERS - Aplidine demonstrates considerable promise in phase (I) clinical trials for treatment of tumors, and various dosing regimes are given. Tumor reduction has been observed in several tumor types including renal carcinoma, colorectal cancer, lung carcinoid, medullary thyroid carcinomas and melanoma. It has also been found that aplidine has a role in inhibiting angiogenesis, complementing the anti-tumor activity.12-03-2009
20090075870DEUTERIUM-ENRICHED CASPOFUNGIN - The present application describes deuterium-enriched caspofungin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20100041593NON-IMMUNOSUPPRESSIVE CYCLOSPORIN FOR TREATMENT OF ULLRICH CONGENITAL MUSCULAR DYSTROPHY - The present invention relates to the use of a nonimmunosuppressive cyclosporin A derivative for reducing mitochondrial dysfunction and the rate of apoptosis of muscle cells of patients diagnosed with Ullrich congenital muscular dystrophy or Bethlem myopathy.02-18-2010
20080318847Use of Antagonist of Oxytocin and/or Vasopressin in Assisted Reproduction - The present invention relates to the use of antagonists of oxytocin, antagonists of oxytocin and vasopressin, or antagonists of vasopressin, or their pharmaceutically accepted salts, or their combinations with other drugs for the manufacture of a medicament which main profile of action is inhibition of oxytocin and/or vasopressin receptors in non-pregnant uterus of mammals, that results in improvement of uterine receptivity in embryo transfer. It further relates to the application of these substances for the manufacture of a medicament for regulating the uterine contractile activity in cases of artificial insemination.12-25-2008
20100144607ANTI-INFLAMMATORY AND ANTIALLERGIC CYCLIC PEPTIDES - The present invention refers to synthetic, cyclic peptides containing a sequence of 13 L-amino acids in their primary structure which present anti-inflammatory and antiallergic activities, useful for the treatment of acute or chronic inflammation and/or allergies, being particularly useful for the treatment of acute or chronic allergic asthma. The invention also describes a pharmaceutical composition containing said peptides, its use and a method to treat or prevent acute and/or chronic inflammatory and/or allergic disorders.06-10-2010
20090170755Cyclic Peptide Compounds - The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, to a process for preparation thereof comprising a rearrangement reaction under a mild acidic condition and the following amino acid changing reactions etc., to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.07-02-2009
20090318336Deuterated Cyclosporine Analogs and Methods of Making the Same - Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.12-24-2009
20100099605CHAPERONIN 10 IMMUNOSUPPRESSION - The invention is directed to the use of cpn10 in transplantation and particularly to treatment and/or prevention of graft versus host disease. The invention provides a method of administration of cpn10 to a donor and/or recipient animal or cells, tissues or organs derived from the donor, although in a particularly advantageous form treatment of both the donor and recipient animal. The method may further include the administration to the donor and/or recipient animal at least one other immunosuppressive agent to prevent or alleviate graft versus host disease.04-22-2010
20100041594Use of Aplidine for the Treatment of Pancreatic Cancer - Aplidine is active against cancer of the pancreas, including metastatic pancreatic cancer.02-18-2010
20090156473PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF VIRAL INFECTIONS AND/OR TUMOR DISEASES BY INHIBITING PROTEIN FOLDING AND PROTEIN BREAKDOWN - The invention relates to the treatment of viral diseases with at least one proteasome inhibitor and one inhibitor of protein-folding enzymes.06-18-2009
20090124539Methods of treating infection - The present invention relates to methods of inhibiting the proliferation of bacteria for either ex vivo or in vivo use. The invention also relates to methods of treating a patient infected with an antibiotic resistant bacteria by administering a pharmaceutical composition comprising an Empedopeptin; methods of sanitizing surfaces and instruments; and methods of assaying bacteria for Empedopeptin resistance.05-14-2009
20090170757METHODS OF USING MACROCYCLIC MODULATORS OF THE GHRELIN RECEPTOR - The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.07-02-2009
20090042774Parathyroid hormone analogues and methods of use - The present invention is directed to novel methods of treating a subject with a bone deficit disorder. The methods generally include administering to a subject in need thereof a pharmaceutically acceptable formulation comprising a parathyroid hormone (PTH) peptide analogue in a daily dose sufficient to result in an effective pharmacokinetic profile and maintained adenylate cyclase activity, while simultaneously reducing undesirable side effects.02-12-2009
20100130409CYCLIC PEPTIDE CXCR4 ANTAGONISTS - Provided are lactam-cyclized peptide CXCR4 antagonists useful in the treatment of cancers, rheumatoid arthritis, pulmonary fibrosis, and HIV infection.05-27-2010
20100130408USE OF MODIFIED CYCLOSPORINS - Disclosed are non-immunosuppressive cyclophilin-binding cyclosporine having useful properties in the prevention or treatment of liver diseases.05-27-2010
20090305960Melanocortin Receptor-Specific Peptides for Treatment of Obesity / 669 - Melanocortin receptor-specific cyclic peptides of the formula12-10-2009
20090305959Use of Peptidic Vasopressin Receptor Agonists - The present invention relates to the use of novel compounds for the manufacture of a medicament for treatment of, inter alia, conditions associated with critical care as well as to a method for treatment of said conditions, wherein said compounds are administered. The compounds utilised are represented by the general formula (I), as further defined in the specification.12-10-2009
20090286718Stable Aqueous Cyclosporin Compositions - An aqueous ophthalmic composition is disclosed. The composition may comprise a cyclosporin in an amount from about 0.001 to about 1%, glycerin, and purified water, wherein the composition is substantially free of NaCl and sodium bisulfite or sodium metabisulfite. The composition is useful for the treatment of ocular conditions.11-19-2009
20090270311TREATMENT OF INSULIN RESISTANCE BY MODULATING SOMATOSTATIN USING SOMATOSTATIN RECEPTOR ANTAGONISTS - The present invention provides the use of somatostatin antagonists for treating and preventing HISS-dependent insulin resistance and hemorrhage induced insulin resistance. The present further provides pharmaceutical compositions comprising a somatostatin antagonist and a pharmaceutically acceptable liver targeting compound.10-29-2009
20080242599Compositions and Methods for Increasing Osteoblast Cell Differentiation and Bone Generation - The present invention relates to the discovery of a novel pathway for the induction of osteoblast cellular differentiation and bone generation. Specifically, the present invention envisions a novel screening tool for the determination of compounds capable of promoting osteoblast cellular differentiation that could be used in the treatment of various bone-loss or bone density decreasing disorders. The method of screening of the present invention enables one to determine whether a compound affects certain pathways that promote via direct induction, or the downregulation of inhibiting activity, the differentiation of progenitor cells into osteoblasts. This promotion of osteoblasts could provide for treatments for bone-loss or bone density disorders. The invention further encompasses methods of increasing bone density using the compounds, the compounds, and pharmaceutical compositions comprising the compounds.10-02-2008
20090029910COMBINATIONS OF SOMATOSTATIN-ANALOGS WITH DIFFERENT SELECTIVITY FOR HUMAN SOMATOSTATIN RECEPTOR SUBTYPES - The present invention relates to a combination of two or more Somatostatin (SRIF) peptidomimetics (also referred to as Somatostatin- or SRIF-analogs) which have different selectivity for the five human somatostatin receptor subtypes, the use of such combination in the treatment of a disease mediated by activation of somatostatin receptors, and to pharmaceutical compositions comprising such a combination.01-29-2009
20090264344RETROCYCLINS: ANTIVIRAL AND ANTIMICROBIAL PEPTIDES - Retrocyclin peptides are small antimicrobial agents with potent activity against bacteria and viruses. The peptides are nonhemolytic, and exhibit minimal in vitro cytotoxicity. A pharmaceutical composition comprising retrocyclin as an active agent is administered therapeutically to a patient suffering from a bacterial and/or viral infection, or to an individual facing exposure to a bacterial and/or viral infection, especially one caused by the HIV-1 retrovirus or other sexually-transmitted pathogens.10-22-2009
20090018057OIL IN WATER EMULSION COMPRISING NSAIDs AND QUATERNARY AMMONIUM HALIDES - Oil-in-water emulsion comprising a non-steroidal anti-inflammatory drug and a quaternary ammonium halide useful for the prevention and treatment of inflammation in the eye, and process for manufacturing thereof.01-15-2009
20080318845Selective Vpac2 Receptor Peptide Agonists - The present invention relates to peptides that selectively activate the VPAC2 receptor and are useful in the treatment of diabetes.12-25-2008
20100035801METHOD FOR ACCELERATING CUTANEOUS BARRIER RECOVERY - A method for accelerating cutaneous barrier recovery by inducing efflux of potassium ion from an epidermal cell as well as a method for preventing epidermal hyperplasia induced by inducing efflux of potassium ion from an epidermal cell are provided.02-11-2010
20090298750DAPTOMYCIN FOR THE TREATMENT OF BIOFILM AND CATHETER SALVAGE - Daptomycin can be used for biofilm treatment (particularly central venous catheter salvage for 12-03-2009
20100144610PHARMACEUTICAL FORMULATIONS - An aspect of the present invention provides for a medicament including a solution containing pleconaril or a pharmaceutically acceptable salt thereof, wherein at least one solvent including the solution is a pleconaril-dissolving hydrofluorocarbon.06-10-2010
20100056434Depsipeptides and Their Therapeutic Use - Compounds which are Spiruchostatin analogues of the general formula (I) or (I′), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R03-04-2010
20100173835Peptides for Treatment of Obesity - The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.07-08-2010
20090124538Selective R-cadherin antagonists and methods - An isolated peptide useful as a selective antagonist of mammalian R-cadherin comprises 3 to 30 amino acid residues, three contiguous residues of the peptide having the amino acid sequence Ile-Xaa-Ser; wherein Xaa is an amino acid residue selected from the group consisting of Asp, Asn, Glu, and Gln. Preferably Xaa is Asp or Asn. In one preferred embodiment the peptide is a cyclic peptide having 3 to 10 amino acid residues arranged in a ring. The selective R-cadherin antagonist peptides of the invention are useful for inhibiting the targeting of stem cells, such as endothelial precursor cells, to developing vasculature, for inhibiting R-cadherin mediated cellular adhesion, and for inhibiting retinal angiogenesis.05-14-2009
20100197571EXTRUDATES WITH IMPROVED TASTE MASKING - The invention relates to extrudates comprising one or more pharmaceutically active substances, where the extrudates have a strand diameter of 0.5 mm or less, and to the use of these extrudates for the manufacture of medicaments.08-05-2010
20100144612PHOSPHORYLATED PYRONE ANALOGS AND METHODS - The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.06-10-2010
20100069295NOVEL POLY(ETHYLENE OXIDE)-BLOCK-POLY(ESTER) BLOCK COPOLYMERS - The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer.03-18-2010
20090088373USE OF COMPOSITIONS TO ENHANCE INNATE IMMUNE RESPONSE - The present invention discloses methods of using of compounds for the enhancement of the innate immune system of a patient. In particular, the active compounds of the present invention include at least one calcineurin inhibitor, mTOR inhibitor or non-immunosuppresive derivative, or a derivative, isomer, or pharmaceutically acceptable salt thereof; and optionally, at least one calciferol or LMW inhibitor, or a derivative, isomer, or pharmaceutically acceptable salt thereof. Pharmaceutical formulations comprising same are also disclosed.04-02-2009
20100035800NOVEL FORMULATIONS OF PHARMACOLOGICAL AGENTS, METHODS FOR THE PREPARATION THEREOF AND METHODS FOR THE USE THEREOF - In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.02-11-2010
20100099606EFFECTIVE USE METHOD OF MEDICAMENTS AND METHOD OF PREVENTING EXPRESSION OF SIDE EFFECT - To provide a medicament which efficiently expresses an immunosuppressive agent or an anti-inflammatory agent and reduces expression of side effect.04-22-2010
20100120672 CYCLIC PEPTIDE COMPOUNDS - The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.05-13-2010
20100081610MATRIX METALLOPROTEINASE INHIBITORS - The present invention relates to β-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.04-01-2010
20100081611STABILIZED MAML PEPTIDES AND USES THEREOF - Stably cross-linked a polypeptides related to human MAML are described. These cross-linked polypeptides contain at least two modified amino acids that together form an internal cross-link or tether that can help to stabilize the alpha-helical secondary structure that is thought to be important for binding of MAML peptides to the Notch transcription complex, a complex that includes ICN and CSL.04-01-2010
20090221474HISTONE DEACETYLASES, AND USES RELATED THERETO - The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.09-03-2009
20100125050Process for the Manufacture of Eptifibatide - Process for manufacturing eptifibatide which comprises subjecting a solution of eptifibatide derivative in a solvent to a concentration step, wherein the pH of said solution is less than or equal to 7.05-20-2010
20100125051Parenteral Formulations Comprising Sugar-Based Esters and Ethers - The present invention relates to formulations for the parenteral administration of therapeutic agents, which contain sugar-based esters and ethers of fatty acids and fatty alcohols as surfactants. The formulations are advantageous for therapeutic agents which are insoluble or poorly soluble in water, and for reducing toxicity associated with common surfactants used in pharmaceutical formulations.05-20-2010
20090286719MODIFICATION OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF - The present invention provides modified cupredoxin derived peptides with pharmacologic activity that have improved pharmacokinetic properties, and methods to use them to treat mammals suffering from various conditions related to the pharmacologic activities. Modifications of the cupredoxin derived peptides include amino acid sequence variants and structural derivations that increase the plasma half-life of the peptide, increase the specific activity of the pharmacologic activity, decrease immunogenicity, and decrease the biotransformation of the peptides. The modified cupredoxin derived peptides can be used in methods to treat mammals for cancer, conditions related to inappropriate angiogenesis, viral and bacterial infections, and specifically HIV and malaria, conditions related to ephrin signaling, and to deliver cargo compounds, including diagnostic compounds, to cancer cell11-19-2009
20100137199Dab9 DERIVATIVES OF LIPOPEPTIDE ANTIBIOTICS AND METHODS OF MAKING AND USING THE SAME - The present invention provides Dab06-03-2010
20100056435Depsipeptides and Their Therapeutic Use - A compound of the general Structure (VII) or (VIII) including isoteres and pharmaceutically acceptable salts thereof, wherein R03-04-2010
20080274951PHARMACEUTICAL COMPOSITIONS INCLUDING LOW DOSAGES OF DESMOPRESSIN - The present invention is directed to a pharmaceutical composition comprising 0.5 ng to 20 μg desmopressin and a pharmaceutically acceptable carrier. The present invention is also directed to a pharmaceutical composition comprising desmopressin and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition is effective to establish a steady plasma/serum desmopressin concentration in the range of from about 0.1 picograms desmopressin per mL plasma/serum to about 10.0 picogram desmopressin per mL plasma/serum. Articles of manufacture and methods of using the above invention are also disclosed.11-06-2008
20090286720PHARMACEUTICAL COMPOSITION FOR THE DIAGNOSIS, PREVENTION OR TREATMENT OF A TUMORAL PATHOLOGY COMPRISING AN AGENT MODULATING THE POLYMERIZATION STATE OF ACTIN - A pharmaceutical composition for the treatment, prevention or diagnosis of a tumoral pathology comprising an active agent which stabilizes an actin network of a cellular cytoskeleton.11-19-2009
20090170754TREATING LIVER DISEASES - This document provides methods and materials related to treating liver conditions. For example, the methods and materials relating to the use of cAMP inhibitors to treat liver conditions are provided.07-02-2009
20090170756CHIMERIC NATRIURETIC PEPTIDES - Peptides of 07-02-2009
20080280820Novel Peptides for Use in the Treatment of Obesity - The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.11-13-2008
20080287347Novel Lipopeptides as Antibacterial Agents - The present invention relates to novel lipopeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The invention also relates to methods of producing these novel lipopeptide compounds and intermediates used in producing these compounds.11-20-2008
20080305994Pharmaceutical Compositions and Method for Treating, Reducing, Ameliorating, Alleviating, or Preventing Dry Eye - A composition for treating, reducing, ameliorating, alleviating, or preventing a dry eye condition or an opthalmologic disorder that has an etiology in inflammation comprises an inhibitor of activity of poly(ADP-ribose) polymerase (“PARP”). The composition can also include a modulator of pro-inflammatory gene expression.12-11-2008
20080312141PEPTIDE LIGANDS FOR PROSTATE SPECIFIC ANTIGEN - The present invention relates to novel peptide ligands for prostate specific antigen (PSA) binding specifically with it and enhancing its enzyme activity, to a process for preparation of these peptides, to diagnostic and pharmaceutical compositions comprising these peptides, to the use of these peptides for pharmaceutical and research preparations, to methods using these peptides in diagnostic assays for determination of the concentrations of various molecular forms of PSA, to methods for modulating the PSA enzyme activity and PSA activity dependent conditions by using these peptides either in vivo or in vitro and to the use of these peptides in procedures for biochemical isolation and purification of PSA.12-18-2008
20080214447Cyclic Peptide Compound - A cyclic peptide compound of the following general formula (I): Wherein R09-04-2008
20080207496ORGANIC COMPOUND - A combination which comprises (a) a staurosporine derivative and (b) an agent effective in preventing, delaying or treating transplant rejection in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier; for simultaneous, separate or sequential use.08-28-2008
20100144609METHODS USING CYCLOSPORIN IN TREATING PATIENTS WITH INTRAOCULAR LENSES - Methods of treating a patient are disclosed in which a cyclosporine component is administered to the patient and an intraocular lens is inserted into an eye of the patient. One or more benefits to the patient may be obtained by practicing the present methods.06-10-2010
20090264348TREATMENT WITH CYCLOSPORIN A - Disclosed herein is a method comprising administering cyclosporin A topically to an eye of a person for the purpose of treating or preventing loss of vision from keratoconus.10-22-2009
20090264347Use of Blood Coagulation Factor XIII for Treating Hemophilia A - A patient having hemophilia A is treated by administering factor XIII generally in conjunction with factor VIII or desmopressin.10-22-2009
20090264346MACROCYCLIC PEPTIDES ACTIVE AGAINST THE HEPATITIS C VIRUS - Compounds of formula (I):10-22-2009
20090264345MACROCYCLIC PEPTIDES AND METHODS FOR MAKING AND USING THEM - The invention provides novel macrocyclic peptides and methods for their preparation. The invention also provides pharmaceutical compositions and methods to treat, prevent or ameliorate a cell proliferative disease or conditions. e.g., a cancer. in a subject in need thereof, including but not limited to a colon cancer, such as MSS or MSI colon cancer, and pancreatic cancer. This invention provides for the synthesis and development of novel anticancer agents that are based on the core structure Sansalvamide A (San A).10-22-2009
20090069221Somatostatin Analogue Formulations - The present invention relates to pre-formulations of a low viscosity mixture containing: a) at least one diacyl glycerol; b) at least one phosphatidyl choline; c) at least one oxygen containing organic solvent; d) at least one somatostatin analogue; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The formulations are useful for generating depot composition for the controlled release of somatostatin analogues such as octreotide. Methods of treatment comprising the administration of such formulations are also provided, as are pre-filled administration devices and kits containing the formulations.03-12-2009
20090298751Arylalkyl and Heteroarylalkyl Derivaties of Cyclosporine a for the Treatment and Prevention of Viral Infection - This invention provides compounds of general formula (T): (I) wherein A, B, R12-03-2009
20090253616COMBINATION THERAPY FOR THE TREATMENT OF CANCER - A combination comprising an aurora kinase inhibitor and an efflux transporter inhibitor wherein the aurora kinase inhibitor is a compound of formula (I) or pharmaceutically acceptable salt thereof for use in the treatment of hyperproliferative diseases such as cancer.10-08-2009
20090186810POTASSIUM CHANNEL MODULATORS AND PLATELET PROCOAGULANT ACTIVITY - Methods of modulating platelet procoagulant response are taught herein. Inhibition of platelet procoagulant response with agents that inhibit the Ca07-23-2009
20090054310Method for Maximizing Efficacy and Predicting and Minimizing Toxicity of Calcineurin Inhibitor Compounds - The invention provides methods for predicting toxicity related to calcineurin inhibition therapy by measuring the peak concentration of drug and the trough concentration of the drug, calculating a peak-trough fluctuation, and comparing this peak-trough fluctuation to known values to predict if the patient will exhibit calcineurin-inhibition therapy-related toxicity. The invention also provides methods for monitoring drug levels to ensure that a patient receiving calcineurin inhibition therapy remains within a therapeutic window which maximizes the efficacy and minimizes the toxicity of the calcineurin inhibitor. The invention also provides dosage methods which maximize the peak concentration, minimize the trough concentration, and maximize the fluctuation between peak and trough concentration of calcineurin inhibitors, to maximize the efficacy of the calcineurin inhibition therapy, and minimize the risk of developing calcineurin-inhibition therapy-related toxicity. This dose regimen, which may be a once-daily dose regimen, maximizes efficacy associated with peak concentrations of drug and minimizes toxicity by maximizing the peak-trough fluctuation, a measurement determined to be associated with toxicity. Calcineurin inhibitors useful for these methods include members of the cyclosporin family of compounds, including cyclosporin A and ISA247, FK506, pimecrolimus and ascomycin.02-26-2009
20080318846SENSITIZATION OF TUMOR CELLS TO RADIATION THERAPY THROUGH THE ADMINISTRATION OF ENDOTHELIN AGONISTS - Methods to sensitize tumor cells to radiation therapy through the administration of an endothelin agonist such as the ET12-25-2008
20090247453Kallikrein Inhibitors and Anti-thrombolytic Agents and Uses Thereof - Methods, kits and compositions are described that include a non-naturally occurring kallikrein inhibitor and an anti-thrombolytic agent, e.g., an anti-fibrinolytic agent, for preventing or reducing blood loss and/or ischemia, e.g., ischemia associated with perioperative blood loss and cerebral ischemia, the onset of systemic inflammatory response, and/or reperfusion injury, e.g., reperfusion injury associated with cerebral ischemia or a focal brain ischemia, e.g., in patients subjected to invasive surgical procedures, especially procedures requiring cardiopulmonary bypass.10-01-2009
20090082260COMBINATION OF AN IMMUNOSUPPRESSANT AND A PPAR GAMMA AGONIST FOR THE TREATMENT OF AN UNDESIRABLE IMMUNE RESPONSE - A method for the treatment or prevention of an undesirable immune response, comprising the simultaneous administration of an immunosuppressant such as cyclosporine and a PPAR-gamma agonist, such as pioglitazone or rosiglitazone. Undesirable immune responses include, for example, rheumatoid arthritis, psoriasis, systemic lupus erythematosus, or transplant rejection.03-26-2009
20090054309Peptidic vasopressin receptor agonists - The present invention relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of inter alia shock conditions as well as to a method for treatment of said conditions, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.02-26-2009
20090054311Novel Cyclosporin Analog Formulations - The present invention relates to formulations containing cyclosporin analogs that are structurally similar to cyclosporin A, in particular isomeric mixtures of cyclosporin analogs that are structurally similar to cyclosporin A. The formulations form stable microemulsion preconcentrates and may provide superior drug bioavailability and/or may reduce one or more adverse effects associated with the administration of cyclosporin. Also disclosed are methods for using and preparing the formulations.02-26-2009
20090105131USE OF POLY-ALPHA2,8-SIALIC ACID MIMETIC PEPTIDES TO MODULATE NCAM FUNCTIONS - The invention relates to the use of a peptide consisting of 5 to 30 amino acid residues, preferably 9 to 15, most preferably about 12 amino acid residues, said peptide comprising a B epitope of a poly-α2,8 sialic acid attached to NCAM, which is recognized by an anti-poly-α2,8 sialic acid (PSA) antibody, for the preparation of a medicament for modulating NCAM functions, to be administered for the prevention and/or the treatment of neurodegenerative diseases, brain and spine lesions, age-related learning and memory problems, and cancer.04-23-2009
20090082261UREA-CONTAINING PEPTIDES AS INHIBITORS OF VIRAL REPLICATION - The invention provides compounds urea-containing peptide compounds of Formula I03-26-2009
20090203585CAPREOMYCIN DERIVATIVES AND THEIR USE AS ANTIBACTERIALS - The present invention relates to phenylurea derivatives of capreomycin I, IIB, IIA, or IB, and metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present invention are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial infections by administering such compounds. The present invention also relates to methods of preparing such compounds.08-13-2009
20090105132Method for Enchancing Cyclodextrin Complexation - The present invention is directed to a method for complexing a cyclodextrin with a cyclosporin, according to which method the complexation is carried out at a temperature of the most 15° C.04-23-2009
20090170758COMPOSITIONS COMPRISING PULMONARY SURFACTANTS AND A POLYMYXIN HAVING IMPROVED SURFACE PROPERTIES - Pulmonary surfactants comprising additives, such as polymyxins, that improve their surface tension lowering properties. A method for improving the resistance to inactivation of a modified natural surfactant, such as one containing a lipid extract of minced mammalian lung comprising administering a surfactant in combination with a polymyxin.07-02-2009
20090215678Preventing Vertical Endoparasite Infections - The present invention relates to the use of endoparasiticidal depsipeptides for producing pharmaceuticals for preventing vertical infection with endoparasites.08-27-2009
20090221473ANTITUMOR AGENTS - Compounds and methods useful for the treatment of cancer in subjects in need of such treatment. The compounds are metabolites of the compound FK228 which have been identified as possessing HDAC inhibitory activity and anticancer properties. Further provided are compounds and methods for inducing apoptosis in cancer cells. Further provided are compounds and methods for inhibiting HDAC in cancer cells.09-03-2009
20090239792SHORT FATTY ACID TAIL POLYMYXIN DERIVATIVES AND USES THEREOF - The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms; and to a combination product comprising at least two such derivatives. The invention further relates to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; and for sensitizing clinically important bacteria to a host defense mechanism complement present in serum. The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent. Finally, the invention relates to a process for preparing such polymyxin derivatives.09-24-2009
20100152102USE OF SOMATOSTATIN OR ONE OF ITS ANALOGUES FOR PREPARING A MEDICAMENT INTENDED TO REGULATE THE OVARIAN FOLLICULAR RESERVE IN NON-MENOPAUSAL WOMEN - The invention primarily relates to the use of somatostatin or one of the agonistic analogs thereof for producing a medicament serving to regulate the ovarian follicular reserve and, in particular, to reduce the depletion of the ovarian follicular reserve over time in non-menopausal women or to the use of an antagonistic analog of somatostatin for producing a medicament serving to accelerate the start of growing of quiescent follicles in non-menopausal women. The invention also relates to in vitro applications of somatostatin and of agonistic and antagonistic analogs thereof.06-17-2010
20100152104Methods for Inhibiting Growth of Prolactin-Responsive Cancer Cells with Cyclosporine A or Other Cyclophilin Inhibitors - Methods are provided for inhibiting growth of prolactin-responsive cancer cells and treating prolactin-responsive malignancies via administration an agent such as cyclosporine A which directly inhibits an enzymatic activity of a cyclophilin.06-17-2010
20100152105USE OF RAPAMYCIN DERIVATIVES IN CHRONIC REJECTION - The present invention is directed to the use of a rapamycin derivative of formula I in combination with cyclosporin for preventing or treating manifestations of chronic rejection in a recipient of an organ or tissue transplant.06-17-2010
20100190695LIQUID CRYSTAL EMULSION TYPE PHARMACEUTICAL COMPOSITION CONTAINING CYCLOSPORINE, AND THEREPEUTIC METHOD OF TREATING CUTANEOUS DISEASE THEREWITH - A dermal external pharmaceutical composition that excels in feeling at application or after application and that by enhancing of the transdermal absorption of cyclosporine, exerts medicinal benefits at low concentration. There is provided a liquid crystal emulsion-type pharmaceutical composition comprising cyclosporine, a hydrophilic nonionic surfactant, a lipophilic nonionic surfactant, an oil, a fatty acid that is insoluble in the oil at room temperature, a solid fatty alcohol that is insoluble in the oil at room temperature and a water-soluble polyhydric alcohol that is immiscible with the oil at room temperature, and a method of treating cutaneous diseases with the use of the pharmaceutical composition.07-29-2010
20100184649NOVEL ANTIBACTERIAL AGENTS FOR THE TREATMENT OF GRAM POSITIVE INFECTIONS - The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against 07-22-2010
20100227800TRIAZOLE DERIVATIVES AS KINASE INHIBITORS - The invention relates to compounds of formula (I); wherein X and R09-09-2010
20100160214DESMOPRESSIN COMPOSITION - Disclosed is a pharmaceutical formulation that may be used in the treatment of nocturia, primary nocturnal enuresis, incontinence, urinary frequency, diabetes insipidus, or any disease or syndrome where desmopressin therapy is useful or where safe temporary suppression of urine production may lead to beneficial health effects or increased convenience in voiding control.06-24-2010
20100144611TREATMENT OF T-CELL MEDIATED DISEASES - The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.06-10-2010
20090075869HCV NS3 protease inhibitors - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.03-19-2009
20100210518Peg-lipid conjugates for increasing the solubility of drug compounds - Diacyl lipid-polymer conjugates are used to enhance the solubility of lipophilic drugs in aqueous solution. The conjugates comprise a backbone, two lipophilic acyl groups and a hydrophilic polymer.08-19-2010
20100222256Novel polypeptide anti-HIV agent containing the same - The present invention provides novel polypeptides of A1-Arg-A2-Cys-Tyr-A3-A4-X-A5-A6-Cit Cys-A7 (I) or their salts (wherein A1 is hydrogen or a residue of arginine, lysine, ornithine, citrulline, alanine, or the like; A2 is an aromatic amino acid residue; A3, A4 and A6 are each a residue of arginine, lysine, ornithine, citrulline, or alanine; A5 is a residue of tyrosine, phenylalanine, alanine, naphthylalanine, or citrulline; A7 is a lysine or arginine residue whose carboxyl group may be converted into amido; and X is a residue of D-ornithyl-proline, prolyl-D-ornithine, D-lysylproline, or the like, with the proviso that any one of A1, A3, A4, A5, A6 and A7 is a residue of alanine or the like or that X is citrulline or the like), and methods of using same in the treatment of HIV.09-02-2010
20100197570Cyclodepsipeptides with Antineoplastic Activity and Methods of Using to Inhibit Cancer and Microbial Growth - The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.08-05-2010
20100216700METHODS OF TREATING OCULAR DISORDERS - This invention is directed to treatments of ocular disorders using emulsions and molecular dispersions in the form of a gel comprising a hydrophobic ocular agent.08-26-2010
20100234285Benzofuranyl Derivatives - The present invention provides compounds of Formula (I)09-16-2010
20090069225SOMATOSTATIN ANALOGUES - The invention provides cyclo[{4-(NH03-12-2009
20090069224Linear and Cyclic Melanocortin Receptor-Specific Peptidomimetics - Linear and cyclic peptidomimetics which bind to one or more melanocortin receptors are provided, which peptidomimetics include at least one ring-constrained amino acid surrogate of formula I:03-12-2009
20090069223Method for treatment of vascular hyperpermeability - A method for the treatment of apoptotic-induced vascular hyperpermeability is disclosed herein. Administration of various compounds including intrinsic mitochondrial regulatory proteins, certain pharmaceuticals, antioxidants and endothelial growth factors alone or in combination results in elevating the threshold for apoptosis in patients with hemorrhagic shock. Elevating the threshold for apoptosis in patients with hemorrhagic shock decreases the amount of vascular hyperpermeability exhibited by the injured patient. Decreasing the amount of vascular hyperpermeability in a traumatized patient facilitates resuscitation and recovery from trauma and decreases the mortality and morbidity rate in injured patients.03-12-2009
20090069222Compounds Useful as Modulators of the Proteasome Activity - The present invention relates to the use of compounds of the following general formula (I): wherein n03-12-2009
20100210519PEPTIDE SLOW-RELEASE FORMULATIONS - A composition for the delayed delivery of a peptide active agent comprising; i) a salt of said peptide active agent comprising at least one positively charged peptide ion and at least one negatively charged counter-ion ii) a sustained-release delivery vehicle. Wherein said at least one negatively charged counter-ion is a halide ion, preferably a chloride or bromide ion.08-19-2010
20100210517CYCLIC RECEPTOR-ASSOCIATED PROTEIN (RAP) PEPTIDES - The present invention relates generally to receptor-selective variants of the low-density lipoprotein receptor-associated protein (RAP) and compositions thereof, methods of generating such variants and methods of using such receptor-selective RAP variant compositions for therapeutic purposes.08-19-2010
20090312242FLIBANSERIN FOR THE TREATMENT OF URINARY INCONTINENCE AND RELATED DISEASES - The invention relates to the use of Flibanserin for the treatment or prevention of urinary incontinence and related diseases. In a further embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment or prevention of urinary incontinence and related diseases.12-17-2009
20090312241Macrocyclic Compounds as Antiviral Agents - The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R12-17-2009
20100056436Pharmaceutical Compositions Including Low Dosages of Desmopressin - The present invention is directed to a pharmaceutical composition comprising 0.5 ng to 20 μg desmopressin and a pharmaceutically acceptable carrier. The present invention is also directed to a pharmaceutical composition comprising desmopressin and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition is effective to establish a steady plasma/serum desmopressin concentration in the range of from about 0.1 picograms desmopressin per mL plasma/serum to about 10.0 picogram desmopressin per mL plasma/serum. Articles of manufacture and methods of using the above invention are also disclosed.03-04-2010
20100069296USE OF SOMATOSTATIN ANALOGS IN CLUSTER HEADACHE - The present invention relates to the use of a Somatostatin (SRIF) analog which has a high binding affinity to human SSTR1,2,3,5, or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical composition for the treatment of cluster headache.03-18-2010
20090291883COMBINATION OF AN IMMUNOSUPPRESSIVE AGENT AND NONSTEROIDAL ANTI -INFLAMMATORY DRUGS TO TREAT DISEASE - The present invention provides methods and compositions for the treatment and prevention of neoplasia by administering an effective amount of a NSAID in combination with an effective amount of an immunosuppressant agent. In particular, the present invention provides methods and compositions for the treatment and prevention of neoplasia by administering an effective amount of COX-2 inhibitor in combination with an effective amount of an immunosuppressant agent.11-26-2009
20090298753METHODS FOR THE THERAPEUTIC USE OF CYCLOSPORINE COMPONENTS - Methods of treating humans or animals having various conditions are disclosed which include administering a therapeutically effective amount of a cyclosporine component to the human or animal, thereby treating the condition. Among the conditions treated are systemic lupus eryhematosis, multiple sclerosis, maloplabia of the skin, oral frictional hyperkeratosis, oral manifestations of autoimmune blistering disease, oral lichen planus, aphthous ulcers, nasal polyps, rhinosporiodosis, sinusitis, iritis, carcinoid lung, laryngitis and atrophic gastritis.12-03-2009
20090118170BUCCAL, POLAR AND NON-POLAR SPRAY OR CAPSULE - Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: polar solvent 37-98.58%, active compound 0.005-55%, optionally containing flavoring agent 0.1-10%.05-07-2009
20090062186Compounds Binding To P-Selectin - The present invention relates to derivatives of compounds which bind selectively to the adhesion molecule human P-selectin, and particularly to such derivatives which comprise a peptide moiety or a functional equivalent of said peptide moiety and are represented by X(A03-05-2009
20080242600Backbone Cyclized Melanocortin Stimulating Hormone (Alpha Msh) Analogs - Backbone cyclized peptides which are α-melanocortin stimulating hormone (αMSH) analogs, having improved Melanocortin-4 receptor agonist activity are disclosed. The backbone cyclized peptide analogs disclosed possess unique and superior properties over other analogs, such as metabolic stability, increased oral bioavailability, improved intestinal permeability and pharmacological activity in-vivo. Pharmaceutical compositions that include the backbone cyclized αMSH analogs, and methods of using such compositions for the treatment of metabolic disorders including obesity are also disclosed.10-02-2008
20100144608Macrocyclic hepatitis C serine protease inhibitors - The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.06-10-2010
20080214446Gene Introduction Efficiency Enhancer - A gene transfer efficiency enhancer of the present invention which contains a histone deacetylase inhibitor (especially compound (A)) as an active ingredient is capable of enhancing gene transfer efficiency in a gene transfer mediated by an adeno-associated virus vector while retaining the advantages of the adeno-associated virus vector.09-04-2008
201001679963-Ether and 3-Thioether Substituted Cyclosporin Derivatives For the Treatment and Prevention of Hepatitis C Infection - This invention relates to cyclosporin derivatives of general formula (I):07-01-2010
20100197572USE OF SOMATOSTATIN-14 AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Ala-Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Ala-Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.08-05-2010
20100184648Therapeutic agent for non-alcoholic fatty liver disease, and screening method for drug candidate compound for treatment or prevention of non-alcoholic fatty liver disease - A therapeutic agent for a non-alcoholic fatty liver disease comprising a melanin-concentrating hormone receptor antagonist as an active ingredient, which is developed based on a novel mechanism of action that a melanin-concentrating hormone receptor is involved in non-alcoholic fatty liver diseases. A method for screening a drug candidate compound for the treatment or prevention of a non-alcoholic fatty liver disease by utilizing the mechanism.07-22-2010
201001521034-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION - The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I06-17-2010
20090176698Benzimidazolone Derivatives for the Treatment of Urinary Incontinence - The invention relates to compositions comprising benzimidazolone derivatives of formula (I), optionally in form of the free base or in form of the pharmacologically acceptable acid addition salts thereof and methods of treating or preventing urinary incontinence, comprising the administration of a therapeutically effective amount of compound of formula (I), wherein R07-09-2009
20100190696TREATMENT OF T-CELL MEDIATED DISEASES - The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.07-29-2010
20100190693METHOD FOR SCREENING COMPOUNDS & USES THEREFOR - In accordance with the present invention, it has been discovered that glucose and incretin hormones promote pancreatic islet cell survival via the calcium and cAMP dependent induction, respectively, of the transcription factor CREB. Specifically, a signaling module has been identified which mediates cooperative effects of calcium and cAMP on islet cell gene expression by stimulating the dephosphorylation and nuclear entry of TORC2, a cytoplasmic CREB coactivator. The module comprises a cAMP regulated snfl-like kinase called SIK2 and the calcium regulated phosphatase calcineurin, both of which associate with TORC2 in the cytoplasm. TORC2 is repressed under basal conditions through a phosphorylation dependent interaction with 14-3-3 proteins. cAMP and calcium signals stimulate CREB target gene expression via complementary effects on TORC2 dephosphorylation; cAMP disrupts TORC2-associated activity of SIK2 or related family members, whereas calcium induces TORC2 dephosphorylation via calcineurin. These findings provide a novel mechanism by which CREB activates cellular gene expression, depending on nutrient and energy status, and facilitate development of assays to identify compounds which modulate the role of TORCs. In accordance with the present invention, it has been discovered that fasting and energy-sensing pathways regulate the gluconeogenic program in liver by modulating the nuclear entry of a transcriptional coactivator called Transducer of Regulated CREB Activity 2 (TORC2). Hepatic TORC2 over-expression induces fasting hyperglycemia, whereas knockdown of TORC2 leads to fasting hypoglycemia and silencing of the gluconeogenic program. Since a majority of individuals with Type II diabetes exhibit fasting hyperglycemia due to elevated hepatic gluconeogenesis, compounds that enhance TORC2 phosphorylation will find use as therapeutic agents in this setting.07-29-2010
20100029551Treatment Of Inflammatory Lung Conditions With Aerosolized Macrolide Antibiotics - Provided herein are pharmaceutical compositions comprising an anti-inflammatory macrolide compound suitable for aerosolized administration to the lungs by inhalation, and methods of treating inflammatory lung conditions, particularly those characterized by chronic inflammation, by administering an aerosolized anti-inflammatory macrolide compound to the lungs by inhalation. Also provided are unit dose formulations of an anti-inflammatory macrolide for aerosolized administration to the lungs by inhalation. Advantageously, the described methods and compositions allow for the targeted, localized delivery of anti-inflammatory macrolide compounds throughout the lungs without significant systemic absorption or deposition.02-04-2010
20100029550ORGANIC COMPOUNDS - A pharmaceutical composition for parenteral administration of a somatostatin analogue salt of aspartate, e.g. mono- or diaspartate, lactate, succinate, e.g. mono- or disuccinate, acetate, glutamate, e.g. mono- or diglutamate or citrate and water forming a gelling depot system after injection in contact with the body fluid.02-04-2010
20100022449RECEPTOR-AVID EXOGENOUS OPTICAL CONTRAST AND THERAPEUTIC AGENTS - Cyanine and indocyanine dye compounds and bioconjugates are disclosed. The present invention includes several cyanine and indocyanine dyes, including bioconjugates of the same, with a variety of bis- and tetrakis (carboxylic acid) homologues. The compounds of the invention may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of compounds of the invention allows favorable delivery to tumor cells as compared to larger molecular weight imaging agents. Further, use of a biocompatible organic solvent such as dimethylsulfoxide may be said to assist in maintaining the fluorescence of compounds of the invention. The compounds and bioconjugates herein disclosed are useful in a variety of medical applications including, but not limited to, diagnostic imaging and therapy, endoscopic applications for the detection of tumors and other abnormalities, localized therapy, photoacoustic tumor imaging, detection and therapy, and sonofluorescence tumor imaging, detection and therapy.01-28-2010
20100022450OCTREOTIDE IMPLANT HAVING A RELEASE AGENT - Methods, formulations and kits are described that allow for the controlled release of octreotide, e.g., octreotide acetate, in a subject.01-28-2010
20100022448PEPTIDES - An internally-constrained cyclic oligopeptide comprising a ring of at least six amino acids for specifically binding to a target ligand, wherein the ring comprises a plurality of amino acid domains, each domain comprising at least two epitope-forming amino acids, and two or more associating functional groups positioned so that they form one or more intra-cyclic associations; whereby the cyclic oligopeptide is constrained in a single conformation so that the epitope-forming amino acids form an epitope in each domain, each epitope being capable of specifically binding to a target ligand.01-28-2010
20080300178Method For Treating Huntington's Disease by Inhibiting Dephosphorylation of Huntingtin at S421 - The present invention relates to a method for treating patients having Huntington's disease by a drug increasing the phosphorylation of huntingtin at position S421, thereby decreasing the polyQ-huntingtin-induced toxicity.12-04-2008
20090209457TREATMENT OF ANTI-ERYTHROPOIETIN ANTIBODY-MEDIATED DISORDERS WITH SYNTHETIC PEPTIDE-BASED EPO RECEPTOR AGONISTS - The present invention relates to peptide compounds that are agonists of the erythropoietin receptor (EPO-R). The invention also relates to therapeutic methods using such peptide compounds to treat or to prevent anti-erythropoietin (EPO) antibody-mediated disorders such as pure red cell aplasia (PRCA) that are characterized by anti-EPO antibodies. Pharmaceutical compositions, which comprise the peptide compounds of the invention, are also provided.08-20-2009
20090054312SMIPs: Small molecule inhibitors of p27 depletion in cancers and other proliferative diseases - Methods are provided for screening for SMIPs (small molecule inhibitors of p27 depletion). The SMIPs thus identified are useful for treating cancers and other proliferative diseases.02-26-2009
20090239791PHARMACEUTICAL COMPOSITION CONTAINING LIPOPHILIC SUBSTANCE WHICH INHIBITS IL-2 PRODUCTION - A pharmaceutical composition comprising a lipophilic substance which inhibits IL-2 production, and a base capable of inhibiting blood exposure of the substance and delivering the substance to lymph following oral administration, is disclosed. The pharmaceutical composition can inhibit blood exposure of the substance to reduce its adverse effects, and can develop desired pharmacological effects.09-24-2009
20100190694Methods for identifying patients who will respond well to cancer treatment - The invention provides methods for identifying patients who will respond well to cancer treatment with a therapeutic regimen that comprises the use of a histone deacetylase inhibitor (HDACi) and one or more further chemotherapeutic agents. The invention also relates to methods of treating such patients with a therapeutic regimen comprising the use of a histone deacetylase inhibitor (HDACi) and one or more further chemotherapeutic agents.07-29-2010
20100062976Synthesis of Cyclosporin Analogs - The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISA03-11-2010
20100120671NOVEL ANTIMICROBIAL AGENTS - New antimicrobial polymeric agents which are designed to exert antimicrobial activity while being stable, non-toxic and avoiding development of resistance thereto and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and a method of treating medical conditions associated with pathological microorganisms, a medical device, an imaging probe and a food preservative utilizing same.05-13-2010
20100227801PHARMACEUTICAL COMPOSITIONS - This invention relates to combinations comprising 3-[(R)-2-(N,N-dimethylamino)ethylthio-Sar]-4-(gammahydroxymethylleucine)cyclosporine, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and certain nucleoside analogues, and their use in the treatment of hepatitis C virus.09-09-2010
20100062975METHOD FOR THE TREATMENT AND PREVENTION OF OCULAR DISORDERS - Provided herein are methods for treatment of ocular diseases. The methods comprise administering a compound of general Formula (I): wherein R03-11-2010
20100120670CYCLISED ALPHA-CONOTOXIN PEPTIDES - This invention relates to an oral or enteral pharmaceutical preparation comprising at least one synthetically cyclised alpha-conotoxin peptide having an amide cyclised backbone such that the peptide has no free N- or C-terminus, said peptide having the ability to inhibit a nicotinic acetylcholine receptor and comprising four cysteine residues bonded in pairs to form two disulfide bonds, wherein the N-terminus of the corresponding linear/non-cyclised conotoxin peptide is linked to the C-terminus by a peptide linker, in a vehicle which is pharmaceutically suitable for oral or enteral administration.05-13-2010
20080207495CYCLOSPORIN COMPOSITIONS FOR OCULAR ROSACEA TREATMENT - Disclosed herein are methods of treating ocular rosacea with cyclosporin A. Compositions and medicaments related thereto are also disclosed.08-28-2008
20100152101TRIAZOL COMPOUNDS FOR TREATING BIOFILM FORMATION - The present invention relates to the use of a Compound of formula I06-17-2010
20080318849Kahalalide F and Related Compounds - A process is provided for preparing kahalalide F and which leads to other kahalalide mimic compounds having useful biological activity.12-25-2008
20100160215ANTIBIOTIC COMPOSITIONS FOR THE TREATMENT OF GRAM NEGATIVE INFECTIONS - Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin B06-24-2010
20090143282ENHANCED RECOVERY FOLLOWING OCULAR SURGERY - An ocular method comprising localized ocular administration of a pharmaceutically acceptable formulation and effective concentration of at least one neuro-stimulatory agent, which may include a macrolide, for a duration sufficient to at least partially restore corneal sensation, or at least one macrolide to reduce scarring after ocular surgery. The neuro-stimulatory agent may be one or more of a macrolide, macrolide analog, neurotrophin, or neuropoietic factor. The method is used in a patent following ocular surgery, such as vision-correction surgery, glaucoma surgery, or retinal detachment repair surgery.06-04-2009
20090118169NOVEL COMPOUNDS AND PHARMACEUTICAL USE THEREOF - A compound comprising the atom corresponding to N05-07-2009
20100167995PEPTOID COMPOUNDS - The invention relates to new peptoid compounds of formula (I), as well as their use in the treatment of bacterial infections, such as those caused by vancomycin resistant microorganisms, and to compositions thereof.07-01-2010
20100041592Use of Amphiphilic Biocompatible Polymers for Solubilization of Hydrophobic Drugs - The present invention provides polymer aggregates as delivery vehicles for therapeutics and diagnostics. The present invention additionally provides methods of synthesis and uses for such aggregates.02-18-2010
20100173837DOSING FORMS AND REGIMENS COMPRISING 3-[(R)-2-(N,N-DIMETHYLAMINO)ETHYLTHIO-SAR]-4-(GAMMAHYDROXYMETHYLLEUCINE)C- YCLOSPORINE - Provided herein are specific doses of, and dosing regimens for, using SCY-635 in treating or preventing diseases, in particular hepatitis C virus (HCV) infection.07-08-2010
20090105130DEPSIPEPTIDE-CONTAINING INJECTION SOLUTION - [Problems] An injection preparation containing a depsipeptide having a disulfide bond in its molecule, which can be easily prepared, and which is stable, is provided.04-23-2009
20100093614Novel Composition for Tumor Growth Control - The invention describes a pharmaceutical composition comprising at least compound selected from the group of demethylating agents and HDAC inhibitors and at least one somatostatin analog or dopamine agonist for the treatment of a tumor which expresses a somatostatin and/or dopamine receptor.04-15-2010
20100093615ANTIBACTERIAL COMPOUNDS AND PROCESSES FOR ITS PRODUCTION - This invention relates to a novel antibiotic compounds, pharmaceutically acceptable salts and derivatives thereof, and to methods for obtaining such compounds.04-15-2010
20090131307PHARMACEUTICAL COMPOSITIONS COMPRISING CYCLOSPORINS - A composition is described herein comprising cyclosporin A, polysorbate 80, a polyoxyethylene stearate, and an oil; wherein the composition is an emulsion which is ophthalmically acceptable. Methods of treating diseases or conditions using said compositions, and medicaments related thereto, are also disclosed herein.05-21-2009
20100173838NOVEL PROCESS FOR THE PREPARATION OF CYCLOSPORIN DERIVATIVES - The invention concerns a novel method for preparing an intermediate polyanion for preparing cyclosporin derivatives by treating a cyclosporin with a hexamethyldisilazane metal salt, optionally in the presence of a metal halide. The treated cyclosporin has one or several free hydroxy groups and/or non-methylated nitrogen atoms in position α and/or any other acid group capable of deprotonation which are optionally deprotonated or in protected form.07-08-2010
20100173836NOVEL MACROCYCLES - Disclosed herein are compounds of general formula (I):07-08-2010
20100048463TEMPLATE-FIXED PEPTIDOMIMETICS - The template-fixed B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-02-25-2010
20090275501Somatostatin-dopamine chimeric analogs - Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 11-05-2009
20090275500PEPTIDE-CONTAINING FOOD INTAKE REGULATOR - A safe and widely-applicable food intake regulator can be provided by using at least one peptide selected from the group consisting of a fish or mammalian melanin-concentrating hormone (MCH) and enzymatic digests thereof, which have the activity to suppress food intake.11-05-2009
20080300177CYCLIC PEPTIDE CXCR4 ANTAGONISTS - Provided are lactam-cyclized peptide CXCR4 antagonists useful in the treatment of cancers, rheumatoid arthritis, pulmonary fibrosis, and HIV infection.12-04-2008
20100204090USE OF A PEPTIDE AS A THERAPEUTIC AGENT - The present invention is directed to the use of the peptide compound Cyclo(-Gly-Ile-Cys-Arg-Cys-Ile-Cys-Gly-Arg-Gly-Ile-Cys-Arg-Cys-Ile-Cys-Gly-Arg) as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Cyclo(-Gly-Ile-Cys-Arg-Cys-Ile-Cys-Gly-Arg-Gly-Ile-Cys-Arg-Cys-Ile-Cys-Gly-Arg) optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.08-12-2010
20100222257SUBSTITUTED PHENETHYLAMINES - Disclosed herein are substituted phenethylamine alpha adrenergic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.09-02-2010
20100184650Treating post-seizure patients - Patients are subject to a post-seizure treatment regime to separately inhibitor consecutive targets of an epileptogenic cascade comprising neurotransmitter receptor signaling, kinase/phosphatase activity, protein translation, and apoptosis or inflammation.07-22-2010
20080255038PHARMACEUTICAL COMPOSITIONS - This invention relates to a compound of general formula (I):10-16-2008
20080255037Endoparasiticidal Compositions - The present invention relates to compositions for external application which comprise emodepside and praziquantel or epsiprantel and 1,2-isopropylideneglycerol, to their preparation and to their use for controlling endoparasites.10-16-2008
20080249002CYCLOSPORIN ALKYNE ANALOGUES AND THEIR PHARMACEUTICAL USES - The compounds of the present invention are represented by the chemical structure found in Formula I:10-09-2008
20090156472Cyclic Depsipeptides - The present application relates to cyclic depsipeptides, or derivatives thereof, having the structure of formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7 and human neutrophil elastase.06-18-2009
20090131306CHEMICALLY MODIFIED CYCLIC PEPTIDES CONTAINING CELL ADHESION RECOGNITION (CAR) SEQUENCES AND USES THEREFOR - Chemically modified cyclic peptides comprising cell adhesion recognition (CAR) sequences are provided having improved properties, such as improved stability. Also provided are methods of making and using same.05-21-2009

Patent applications in class Monocyclic