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23rd week of 2012 patent applcation highlights part 53
Patent application numberTitlePublished
20120142599EXTRACT OF R. MIEHEI - Topical compositions comprising extracts of 2012-06-07
20120142600Analogs of ShK Toxin and their Uses in Selective Inhibition of Kv1.3 Potassium Channels - Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore and such fluorophore-tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.2012-06-07
20120142601Modified Peptides and Uses Thereof - The invention includes compounds that are useful in treating perioperative shivering or temperature spiking, lowering body temperature, treating psychosis or treating pain. The invention also includes methods for treating perioperative shivering or temperature spiking, lowering body temperature, treating psychosis or treating pain in a subject in need thereof.2012-06-07
20120142602Composition and Method for Preventing or Treating a Tauopathy - The present invention is a composition and method for the prevention and treatment of a tauopathy. The composition of the invention includes N-terminal amino acid residues of the tau protein, which have been identified as being involved in toxic activation of a PP1/GSK3 signaling cascade and inhibition of fast axonal transport in human tauopathies.2012-06-07
20120142603BIOADHESIVE PATCH FOR SUTURELESS CLOSURE OF SOFT TISSUE - Provided herein are compositions and methods for treating soft tissue injuries using a patch having a polymer on its surface linked to polypeptides having a disintegrin domain. The polypeptides having a disintegrin domain can include contortrostatin, vicrostatin, and ADAM derived polypeptides. Compositions of the invention can be used for the treatment of injuries to soft tissues that include the eye, liver and brain.2012-06-07
20120142604NOVEL APPLICATIONS OF HIP/PAP OR DERIVATIVES THEREOF - The use of the HIP/PAP protein or a protein derivative thereof for manufacturing a medicament for preventing or treating: 2012-06-07
20120142605METHODS OF TREATING PSORIASIS - The invention includes methods for treating patients having psoriasis and methods for testing the efficacy of such treatments. The methods include treating the patients with a TNF inhibitor plus a topical preparation containing a glucocorticoid.2012-06-07
20120142606TUMOR TARGETING PEPTIDES, THERAPEUTIC AND DIAGNOSTIC COMPOSITIONS COMPRESSING THE PEPTIDES - The present invention is directed to peptides having affinity for tumor cells. The peptides are useful in pharmaceutical compositions in particular for the treatment of cancer. Further, the peptides are useful in diagnostic compositions, in particular for the diagnosis and imaging of cancer. The peptides according to the present invention are peptides selected from the group consisting of: Z2012-06-07
20120142607Antibodies and molecules derived therefrom that bind to STEAP-1 proteins - Antibodies and molecules derived therefrom that bind to novel STEAP-1 protein, and variants thereof, are described wherein STEAP-1 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table I. Consequently, STEAP-1 provides a diagnostic, prognostic, prophylactic and/or therapeutic target for cancer. The STEAP-1 gene or fragment thereof, or its encoded protein, or variants thereof, or a fragment thereof, can be used to elicit a humoral or cellular immune response; antibodies or T cells reactive with STEAP-1 can be used in active or passive immunization.2012-06-07
20120142608RCA LOCUS ANALYSIS TO ASSESS SUSCEPTIBILITY TO AMD AND MPGNII - The invention relates to gene polymorphisms and genetic profiles associated with an elevated or a reduced risk of alternative complement cascade deregulation disease such as AMD and/or MPGNII. The invention provides methods and reagents for determination of risk, diagnosis and treatment of such diseases. In an embodiment, the present invention provides methods and reagents for determining sequence variants in the genome of a individual which facilitate assessment of risk for developing such diseases.2012-06-07
20120142609NON HUMAN ANIMAL MODELS FOR INCREASED RETINAL VASCULAR PERMEABILITY - The present invention relates to a non human animal model for increased retinal vascular permeability wherein said increased retinal vascular permeability is induced by inhibiting in Müller cells of said animal the expression of a gene encoding for Dp71 or a dystrophin associated protein (DAP). Furthermore, the present invention relates to methods and compositions for the treatment of a disease associated with an increased retinal vascular permeability in a subject in need thereof.2012-06-07
20120142610TREATMENT OF 'IQ MOTIF CONTAINING GTPASE ACTIVATING PROTEIN' (IQGAP) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO IQGAP - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of ‘IQ motif containing GTPase activating protein’ (IQGAP), in particular, by targeting natural antisense polynucleotides of ‘IQ motif containing GTPase activating protein’ (IQGAP). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of IQGAP.2012-06-07
20120142611REPEAT PROTEIN FROM COLLECTION OF REPEAT PROTEINS COMPRISING REPEAT MODULES - A repeat protein from a collection of repeat proteins, wherein each repeat protein of said collection comprises a repeat domain, which comprises a set of consecutive repeat modules, wherein the repeat modules have the same fold and stack tightly to create a superhelical structure having a joint hydrophobic core, wherein each of the repeat modules is derived from one or more repeat units and wherein the repeat units comprise framework residues, which contribute to the folding topology of the repeat unit or contribute to an interaction with a neighboring repeat unit, and target interaction residues, which contribute to an interaction with a target substance, wherein the repeat proteins of the collection differ from other repeat proteins in the collection in at least one amino acid position of the repeat modules is described as are related pharmaceuticals and nucleic acid molecules.2012-06-07
20120142612CYTOKINE PROTEIN FAMILY - The present invention relates to polynucleotide and polypeptide molecules for zcyto20, zcyto21, zcyto22, zycto24, and zcyto25 proteins which are most closely related to interferon-α at the amino acid sequence level. The receptor for this protein family is a class II cytokine receptor. The present invention includes methods of reducing viral infections and increasing monocyte counts. The present invention also includes antibodies to the zcyto20 polypeptides, and methods of producing the polynucleotides and polypeptides.2012-06-07
20120142613Cell-Permeable Peptide Inhibitors of the JNK Signal Transduction Pathway - The invention provides cell-permeable peptides that bind to JNK proteins and inhibit JNK-mediated effects in JNK-expressed cells.2012-06-07
20120142614Guanylate Cyclase Receptor Agonists For The Treatment Of Tissue Inflammation And Carcinogenesis - A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis. Thus, the method may be used to treat, inter alia, inflammation, including gastrointestinal inflammatory disorders, general organ inflammation and asthma, and carcinogenesis of the lung, gastrointestinal tract, bladder, testis, prostate and pancreas, or polyps.2012-06-07
20120142615METHODS RELATED TO THE TREATMENT OF NEURODEGENERATIVE AND INFLAMMATORY CONDITIONS - The invention includes methods of neuroprotection, inducing release of neurotrophic factors, inhibiting the over-activation of innate immune cells, attenuating the toxin-induced death and/or damage of tissues, reducing inflammation, treating an inflammation-related condition, and inhibiting NADPH oxidase, that includes contacting or administering an effective amount of at least one compound of the invention that include: valproic acid, sodium butyrate, and salts thereof; opioid peptides; a peptide comprising the tripeptide GGF; and morphinans, such as naloxone, naltrexone, 3-hydroxy-morphinan and dextromethorphan.2012-06-07
20120142616Antineoplastic Hydrogels, and Enzyme-Instructed Preparations Thereof - Disclosed is a general methodology to create nano fibers of therapeutic molecules that have a dual role, as both the delivery vehicle and the drug itself. It is shown that with proper molecular design, the integration of enzymatic reaction and self-assembly provides a powerful method to create molecular hydrogels of clinically-used therapeutics without compromising their bioactivities. In addition, the results disclosed herein demonstrate enzyme-instructed self-assembly as a facile strategy for generating the supramolecular hydrogels of molecules that inherently have poor solubility in water. For example, by covalently connecting paclitaxel with a motif that is prone to self-assemble, a hydrogel of paclitaxel can be formed without compromising the activity of the paclitaxel.2012-06-07
20120142617ANTIVIRAL THERAPEUTIC AGENTS - The invention provides compounds of Formula I:2012-06-07
20120142618KETOGENIC SACCHARIDES - A novel ketogenic compound is provided having general formula (R(OCH(CH2012-06-07
20120142619MEDICINAL CARBOHYDRATES FOR TREATMENT OF RESPIRATORY CONDITIONS - The present invention relates to a method and compounds of Formula (1) and/or (2) or their pharmaceutically acceptable inorganic or organic salt thereof, and their compositions for treating respiratory conditions including post viral/bacterial infections, acute/chronic bronchitis, COPD, cystic fibrosis, and inflammatory conditions. It has been found by the applicants that the compounds of Formula (1) and/or (2) or their pharmaceutically acceptable inorganic or organic salt thereof could speed up the recovery of the viability of damaged respiratory tract cells by restoring sialylglyco-conjugates on their surface.2012-06-07
20120142620CORE 2 GLCNAC-T INHIBITORS - A method of treating a subject in need of therapy for a condition involving detrimental activity of the enzyme core 2 GlcNAc-T is provided, comprising administration of a therapeutically effective amount of an inhibitor of core 2 GlcNAc-T of formula I to a patient in need thereof2012-06-07
20120142621Purified Ethyl Ester Sophorolipid for the Treatment of Sepsis - A microbial ethyl esther sophorolipid derivative with no acetylated groups produced by 2012-06-07
20120142622STAMBOMYCIN AND DERIVATIVES, THEIR PRODUCTION AND THEIR USE AS DRUGS - The present invention relates to Stambomycin compounds, their derivatives and their pharmaceutically acceptable salt thereof.2012-06-07
20120142623Compositions And Methods For Predicting Inhibitors Of Protein Targets - Compositions and methods are provided for predicting inhibitors of protein targets related to treatment of infectious disease, for example, bacterial, viral, or parasitic diseases. Methods are provided for predicting inhibitors of protein targets related to treatment infectious disease, for example, microbial disease, utilizing a docking with dynamics protocol to identify inhibitors, or utilizing a protein structure energy function to identify peptide or peptidomimetic inhibitors.2012-06-07
20120142624AKT PHOSPHORYLATION AT SER473 AS AN INDICATOR FOR TAXANE-BASED CHEMOTHERAPY - Methods for determining whether a cancer patient is likely to benefit from treatment with a taxane compound based on Akt-Ser473 phosphorylation status are provided, together with kits for determining Akt-Ser473 phosphorylation status and methods for improving treatment of a cancer patient that include obtaining a determination of the Akt-Ser473 phosphorylation status of the cancer. 2012-06-07
20120142625Substituted Purine And 7-Deazapurine Compounds - The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.2012-06-07
20120142626COMPOUNDS - Disclosed herein are 2′-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.2012-06-07
20120142627MONOPHOSPHATE PRODRUGS OF DAPD AND ANALOGS THEREOF - The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV and HBV, in human patients or other animal hosts. The compounds are certain 6-substituted-2-amino-purine dioxolane monophosphates or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof.2012-06-07
20120142628METHODS FOR TREATING CREPITUS - Methods for treating and/or preventing crepitus and other joint problems using hyaluronic acid based formulations are provided.2012-06-07
20120142629PHARMACEUTICAL COMPOSITION FOR RELIEVING PAIN - The present invention relates to a pharmaceutical composition for relieving pain in a joint disease, including a hyaluronic acid and a pharmaceutically acceptable carrier, in which the hyaluronic acid is cross-linked by cyclizing a double bond in the moiety of a cinnamic acid in a partially amidated hyaluronic acid represented by Formula (1): [Ar—CH═CH—COO—(CH2012-06-07
20120142630PROCESS FOR PURIFYING GUAR - The present invention relates to processes for purifying guar comprising combining borate and guar in an aqueous solution and treating the aqueous solution with an organic solvent to induce precipitation of purified guar. Another embodiment of the present invention is directed to ophthalmic formulations comprising purified guar produced by the processes described.2012-06-07
20120142631MEDICINAL ANTIDIAPER RASH CREAM INCORPORATING A BIOPOLYMER AND A PROCESS TO MAKE IT - The present invention is directed to a composition for treating diaper rashes, along with skin rejuvenation containing a) a biopolymer in the form of Chitosan, b) a combination of active pharmaceutical ingredients (APIs), Benzalkonium Chloride & Cetrimide used in treating diaper rashes, c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants, and d) water.2012-06-07
20120142632DIAGNOSTIC AND PROGNOSTIC ASSAY - The present disclosure relates generally to the field of diagnostic and prognostic assays for diseases and conditions of the systemic vasculature. The present disclosure teaches an assay for identifying such a disease or condition of the systemic vasculature as well as classifying and determining the state or stage of the disease or condition or the risk of developing the disease or condition. The assay enabled herein is also useful in the stratification of a subject with respect to a risk of developing various diseases and conditions of systemic vasculature. The assay taught herein is also capable of integration into pathology architecture to provide a diagnostic and reporting system.2012-06-07
20120142633METHYLPYRROLOPYRIDINECARBOXAMIDES - The compounds of Formula (I),2012-06-07
20120142634Method of Treating Cancer with a Combination of a Proteasome Inhibitor and Salubrinal - The disclosure provides methods for treating or preventing a cancerous condition, such as multiple myeloma, by administering a therapeutically effective combination of a proteasome inhibitor and salubrinal.2012-06-07
20120142635OXAZOLIDINONE-QUINOLONE HYBRID ANTIBIOTICS - The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:2012-06-07
20120142636NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME - Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure2012-06-07
20120142637PRODRUGS OF 6-CYCLOHEXYL-1-HYDROXY-4-METHYLPYRIDIN-2-(1H)- ONE AND DERIVATIVES THEREOF - A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, 2012-06-07
20120142638COMBINATION OF ORGANIC COMPOUNDS - The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising a therapeutic agent acting on the renin-angiotensin system (RAS) or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof.2012-06-07
20120142639OXADIAZOLE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.2012-06-07
20120142640ALKYNE AND ALKENE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE-1 RECEPTOR MODULATORS - The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.2012-06-07
20120142641TARGETTED DRUG DELIVERY TO THE BONE - The present invention relates to a complex of a bisphosphonate compound, methods of preparing such complex and uses thereof.2012-06-07
20120142642NOVEL OXIME DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel oxime derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.2012-06-07
20120142643CLONIDINE AND GABA COMPOUNDS IN A BIODEGRADABLE POLYMER CARRIER - Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine and a gamma-aminobutyric acid compound at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.2012-06-07
20120142644METHOD FOR PRODUCING PHYTOSTEROL/PHYTOSTANOL PHOSPHOLIPID ESTERS - The present invention relates to a method of producing a phytosterol ester and/or a phytostanol ester comprising: a) admixing a phospholipid composition comprising at least between about 10% to about 70% plant phospholipid and at least about 5% water; a lipid acyltransferase; and a phytosterol and/or a phytostanol; and b) separating or isolating or purifying at least one phytosterol ester and/or phytostanol ester from said admixture. The present invention also relates to compositions comprising the phytosterol ester and/or phytostanol ester produced by this method, including foodstuffs and personal care product (cosmetic) compositions.2012-06-07
20120142645NEUROACTIVE STEROID COMPOSITIONS AND METHODS OF USE FOR LOWERING CHOLESTEROL - Methods for ameliorating a symptom associated with hypercholesterolemia, hyperlipidemia, or both in a subject. In some embodiments, the methods include administering to a subject in need thereof an effective amount of a composition comprising pregnenolone (PG), allopregnanolone (ALLO), dehydroepiandrosterone (DHEA), progesterone (PROG), precursors thereof, metabolites thereof, pharmaceutically acceptable salts thereof, derivatives thereof, or combinations thereof. Also provided are methods for ameliorating at least one symptom resulting from undesirable cholesterol biosynthesis in a subject and methods for lowering cholesterol, low density lipoprotein, or both in the serum of a subject.2012-06-07
20120142646Novel Compounds 621 - The present invention provides compounds of formula (I)2012-06-07
20120142647Novel Compounds as Respiratory Stimulants for Treatment of Breathing Control Disorders or Diseases - The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.2012-06-07
20120142648METHODS FOR DELIVERING CLONIDINE COMPOSITIONS IN BIODEGRADABLE POLYMER CARRIER AND LOCAL STERIODS TO A TARGET TISSUE SITE - Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine and a steroid at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.2012-06-07
20120142649COMPOSITIONS AND METHODS FOR DELIVERING CLONIDINE AND BUPIVACAINE TO A TARGET TISSUE SITE - Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of immediate release bupivacaine or lidocaine and a sustained release clonidine at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days or longer.2012-06-07
20120142650METHOD FOR TREATING LUNG DISEASE - Methods of treating lung diseases comprising administering inducers of NAD(P)H:quinone oxidoreductase 1 (NQO1) are disclosed. Inducers of NQO1 include naphthoquinones such as β-lapachone. Methods of predicting whether a subject with a lung disease will respond to treatment with a naphthoquinone are also described herein.2012-06-07
20120142651METHOD OF TREATMENT OF ALLERGIC RHINITIS - There is provided a method of treatment of allergic rhinitis which comprises administering to a patient a pharmaceutically acceptable amount of a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I)2012-06-07
20120142652COMPOSITIONS AND METHODS FOR LOCALIZED THERAPY OF THE EYE - Compositions, and methods of using such compositions, useful for injection into the posterior segments of human or animal eyes are provided. Such compositions include small particles of a poorly soluble therapeutic agent that facilitates formation of concentrated regions of the therapeutic agent in the retinal pigmented epithelium of an eye. The particles are formed by combining a therapeutic agent with an ophthalmically acceptable polymer component. The particles have sizes less than about 3000 nanometers, and in some cases, less than about 200 nanometers. One example of composition includes particles of triamcinolone acetonide and hyaluronic acid have a size less than about 3000 nanometers.2012-06-07
20120142653C-28 AMIDES OF MODIFIED C-3 BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 and C-28 betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.2012-06-07
20120142654PROGNOSTIC MARKER FOR MAMMA CARCINOMA - The invention provides an analytical method for the determination of the susceptibility of a human patient suffering from breast cancer to anti-cancer treatment by providing an analytical method for determining the genetic predisposition of a patient in respect of susceptibility, e.g. responsiveness, to anti-cancer treatment, especially treatment using at least one chemotherapeutical agent and/or at least one anti-hormonal agent on the basis of analysis of a genetic marker.2012-06-07
20120142655NOVEL CRYSTAL FORM OF AN ORGANIC COMPOUND AND PROCESS FOR THE PREPARATION THEREOF - The present invention relates to novel crystalline Form II of 17α-acetoxy-21-methoxy-11β-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124), processes for the preparation thereof and pharmaceutical compositions comprising it. Form II can be crystallized from different medium such as esters of C1-C4 alcohols and carboxylic acids, ketones, cyclohexane, acetonitrile, dimethylformamide, dimethyl sulfoxide, water and any mixture thereof.2012-06-07
20120142656BUCCAL APPLICATION SYSTEM COMPRISING 17A-ESTRADIOL - The invention relates to application systems for buccal application, comprising 17α-estradiol in a dosage of 50 to 400 μg, preferably 200 to 400 μg, particularly preferably 300 μg, together with one or more pharmaceutically acceptable additives or media for implementing the treatment or minimization of hot flashes in women having estrogen deficiencies.2012-06-07
20120142657GABA-STEROID ANTAGONISTS AND THEIR USE FOR THE TREATMENT OF CNS DISORDERS - Compounds exhibiting 3alpha-hydroxy-5alpha/beta-steroid blocking action with no or only low antagonism against the gamma-aminobutyric acid (A) receptor (GABA-A), and compounds exhibiting partial antagonism against said receptor are presented. Methods for the prevention, treatment and/or alleviation of various CNS-disorders are suggested, as well as pharmaceutical compositions for such use.2012-06-07
20120142658THERAPEUTICAL USE OF TERNARY COMPLEXES OF VALPROIC ACID - A method of treating a human subject having a condition responsive to valproic acid therapy, includes administering to the subject an effective amount of a metal-based ternary complex of valproic acid with nitrogen donor ligands, in particular with diimines or diamines.2012-06-07
20120142659COMPOUNDS AND THEIR USE AS IKACH BLOCKERS - The invention relates to compounds according to Formula I:2012-06-07
20120142660AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.2012-06-07
20120142661NOVEL OXIME AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel oxime azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.2012-06-07
20120142662NOVEL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.2012-06-07
20120142663NOVEL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.2012-06-07
20120142664NOVEL BENZYL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.2012-06-07
20120142665TRIAZOLOPYRIDINE COMPOUNDS - The invention is concerned with triazolopyridine compounds of formula (I)2012-06-07
20120142666Azetidine 2-Carboxamide Derivatives Which Modulate The CB2 Receptor - Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.2012-06-07
20120142667PYRIMIDINE DERIVATIVES AS ZAP-70 INHIBITORS - The invention relates to compounds of formula (I)2012-06-07
20120142668CATHEPSIN C INHIBITORS - Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.2012-06-07
20120142669N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I):2012-06-07
20120142670N-(amino-heteroaryl)-1H-pyrrolopyridine-2-carboxamides derivatives preparation thereof and their use in therapy - The invention relates to compounds of the general formula (I):2012-06-07
20120142671BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.2012-06-07
20120142672HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and use thereof.2012-06-07
20120142673Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors - There is provided a compound of formula I:2012-06-07
20120142674N-PHENYL-(HOMO)PIPERAZINYL-BENZENESULFONYL OR BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I2012-06-07
20120142675Methods for Treating Diseases of the Retina - Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a compound selected from the group consisting of olanzapine, certain of its metabolites, clozapine, and n-desmethyl clozapine.2012-06-07
20120142676Oxathiazine and dithiine oxides as inhibitors of sulfhydryl-dependent biomolecules - Novel derivatives of dihydro-1,4,2-oxathiazine and dihydro-1,4-dithiine oxides, more particularly, novel derivatives of dihydro-1,4,2-oxathiazine and dihydro-1,4-dithiine oxides that target cysteine residues of biomolecules of pharmacological importance are provided as pharmaceutically useful compounds, for example, as anticancer, antiinfectious, antigastric acid secretion, antiosteoporosic, and antiinflammatory agents.2012-06-07
20120142677Pyrrolidine Compounds Which Modulate The CB2 Receptor - Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. (I)2012-06-07
20120142678NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.2012-06-07
20120142679NOVEL 2,3-DIHYDRO-1H-IMIDAZO(1,2-A)PYRIMIDIN-5-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF - The invention relates to the novel materials of formula (I), where R2012-06-07
20120142680HETEROALKYL LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases.2012-06-07
20120142681HETEROCYCLIC HYDRAZONE COMPOUNDS - The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).2012-06-07
20120142682ANTIVIRULENCE COMPOUNDS INHIBITING BACTERIAL MONO-ADP-RIBOSYLTRANSFERASE TOXINS - Compounds that inhibit bacterial virulence factors from the mono-ADP-ribosyltransferase (mART) family of toxins have been identified that are not toxic to cells or the producing bacterial pathogen. These compounds have great potential as antivirulence agents for treating many bacterial infections and disease states.2012-06-07
20120142683PYRIMIDINE SUBSTITUTED PURINE COMPOUNDS AS KINASE (S) INHIBITORS - The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure (I) or a pharmaceutically acceptable salt thereof2012-06-07
20120142684COMPOUNDS AND METHODS FOR SKIN REPAIR - The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.2012-06-07
20120142685ORGANIC COMPOUNDS - The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.2012-06-07
20120142686VIRAL POLYMERASE INHIBITORS - The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:2012-06-07
20120142687INDOLECARBOXYLIC ACID DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY - The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. 2012-06-07
20120142688PREPARATION OF 1-(SUBSTITUTED ARYL)-5-TRIFLUOROMETHYL-2-(1H)PYRIDONE COMPOUNDS AND SALTS THEREOF AND THEIR APPLICATIONS - A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.2012-06-07
20120142689SEROTONIN REUPTAKE INHIBITORS - In one aspect, the invention relates to compounds of formula I:2012-06-07
20120142690Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.2012-06-07
20120142691PICOLINAMIDE DERIVATIVES AS TTX-S BLOCKERS - The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.2012-06-07
20120142692ANTIFOLATE COMBINATIONS - The present invention provides combinations of active agents, such combinations comprising one or more antifolate compounds. The particularly can include methotrexate and one or more further antifolate compounds. In specific embodiments, the combinations are useful for treating certain conditions, such as rheumatoid arthritis. The invention also provides articles useful to provide the combinations in desirable dosage forms and combinations. The combinations further may be useful in the treatment of further conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.2012-06-07
20120142693CRYSTALLINE COMPOUND OF 7-[(3R)-3-AMINO-1-OXO-4-(2, 4, 5-TRIFLUORPHENYL)BUTYL]-5, 6, 7, 8-TETRAHYDRO-3-(TRI FLUORMETHYL)-1, 2, 4 -TRIAZOLO[4,3-A]PYRAZIN - A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 12012-06-07
20120142694SUBSTITUTED 4-HYDROXYPYRIMIDINE-5-CARBOXAMIDES - The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.2012-06-07
20120142695COMPOUNDS AS BRADYKININ B1 ANTAGONISTS - Compounds of the formula I2012-06-07
20120142696SUBSTITUTED INDOLE/INDAZOLE-PYRIMIDINYL COMPOUNDS - The present disclosure provides indole/indazole-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I):2012-06-07
20120142697Salt forms of 4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl) pyrimidin-2-ylamino)phenyl]-benzamide - The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.2012-06-07
20120142698MICROBIOCIDAL HETEROCYCLES - The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R2012-06-07