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Plural hetero atoms in the tricyclo ring system

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514277000 - Hetero ring is six-membered consisting of one nitrogen and five carbon atoms

514279000 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos

514290000 - Tricyclo ring system having the six-membered hetero ring as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514292000 Plural ring nitrogens in the tricyclo ring system 225
Entries
DocumentTitleDate
20120172389TREATMENT OF FIBROSING DISORDERS - A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula07-05-2012
20090192185MEDICAL PRODUCT - The invention discloses a medical product for use in a treatment of respiratory disorders, and comprises a metered dose of a tiotropium dry powder formulation, directly loaded and sealed into a container made to act as a dry high barrier seal to prevent the capture and ingress of moisture into the tiotropium powder. The dose of tiotropium is further adapted for inhalation and the container is so tight that the efficacy of the dose when delivered is unaffected by moisture. In a further aspect of the invention a type of inhaler is illustrated, which may accept at least one sealed, moisture-tight container of a dose of tiotropium, to deliver the dose with a consistent fine particle dose, over the expected shelf life of the product.07-30-2009
20100069425GLUCOCORTICOID RECEPTOR MODULATOR AND METHODS OF USE - The present invention provides Compound (I): Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof.03-18-2010
20120178775METHODS FOR TREATING FRONTOTEMPORAL LOBAR DEGENERATION WITH UBIQUITINATED INCLUSIONS (FTLD-U) - Methods for rescuing learning, memory and/or motor function deficits associated with frontotemporal lobar degeneration with ubiquitinated inclusions (FTLD-U) are disclosed. The method comprises: a) administering to an animal having FTLD-U a therapeutically effective amount of an autophagy inducer; b) causing a decrease in the amount of ubiquitinated TDP-43 aggregation forms in the brain of the animal; and c) causing an improvement of the learning, memory capacities and/or motor function of the animal.07-12-2012
20090069366DEUTERIUM-ENRICHED TACROLIMUS - The present application describes deuterium-enriched tacrolimus, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20130040980CCI-779 CONCENTRATE FORMULATIONS - This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.02-14-2013
20130040979CCR1 INHIBITORS USEFUL FOR THE TREAMENT OF MULTIPLE MYELOMA AND OTHER DISORDERS - The invention relates to the use of inhibitors of CCR1 for the treatment of cancers and osteolytic bone disorders. In some embodiments, the invention relates to methods for the treatment of multiple myeloma, smoldering multiple myeloma and secondary bone cancers.02-14-2013
20100105717TACROLIMUS FOR IMPROVED TREATMENT OF TRANSPLANT PATIENTS - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.04-29-2010
20100069426Therapeutic polymeric nanoparticles with mTor inhibitors and methods of making and using same - The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a mTOR inhibitor; and about 70 to about 99 weight percent biocompatible polymer.03-18-2010
20080249123WORTMANNIN-RAPAMYCIN CONJUGATE AND USES THEREOF - A rapamycin—wortmannin conjugate is described, in which the conjugate is formed by linking the rapamycin and wortmannin together in such a manner that the rapamycin and the wortmannin are separated following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.10-09-2008
20100130526Methods for Disease Therapy - The present invention discloses disease-linked SNPs, microRNAs, and microRNA-targeted mRNAs relevant to the pathogenesis of several major human disorders including, but not limited to, multiple types of cancers, type 2 diabetes, type 1 diabetes, Crohn's disease, coronary artery disease, hypertension, rheumatoid arthritis, bipolar disorder. Also provided are methods for the identification of disease phenotype-defining sets of SNPs, microRNAs, and mRNAs that are defined here as a “consensus disease phenocode” as well as methods of using the information provided by these consensus disease phenocodes for various diagnostic, prognostic, and/or therapeutic applications.05-27-2010
20090306120TERPOLYMERS CONTAINING LACTIDE AND GLYCOLIDE - The present invention provides an amorphous terpolymer for a coating on an implantable device for controlling release of drug and methods of making and using the same.12-10-2009
20090093510Use of Nitrooxyderivatives of Drug for the Treatment of Muscular Dystrophies - The present invention relates to the use of nitric oxide releasing compounds for retarding or reversing muscular dystrophies such as Duchenne and Becker dystrophies.04-09-2009
20130059878TREATMENT OF DISEASES MODULATED BY A H4 RECEPTOR AGONIST - The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.03-07-2013
20130059877TREATMENT OF SOLID TUMORS WITH RAPAMYCIN DERIVATIVES - Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent.03-07-2013
20090270441MACROLIDES - The invention relates to the stabilization of poly-ene macrolides and to a particular macrolide obtained in crystalline form.10-29-2009
20110021553IMMUNOSUPPRESSIVE MACROLIDE POWDER FOR ORAL SUSPENSION - The present invention describes pharmaceutical compositions that comprise a tacrolimus powder for oral suspension that exhibits great stability as a powder for suspension and also, once prepared, as the extemporaneous suspension, without the formation of cake-like clusters, same having a satisfactory flavour and a pleasant aroma. The invention also describes the method for preparing the pharmaceutical compositions, same being a dry method that comprises mixing tacrolimus and pre-sieved pharmaceutically acceptable carriers for a suitable length of time, and the use of the pharmaceutical compositions for treating and preventing rejection of transplanted organs and atopic dermatitis.01-27-2011
20120115897Aryl (Ethanoic) Propanoic Acid Ascorbyl Ester, Preparation Method Thereof And Medicament Containing The Same - The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers.05-10-2012
20120115896ISOGENIC HUMAN CELL LINES COMPRISING MUTATED CANCER ALLELES AND PROCESS USING THE CELL LINES - Isogenic human cell lines comprising at least one mutated cancer allele under the control of the cell line endogenous promoter, which corresponds to the wild-type cancer allele promoter are disclosed, as well as an in vitro process for determining sensitivity/resistance of a patient suffering from a tumor to a pharmacological agent comprising the following steps: a) identifying at least one mutated cancer allele in a tissue affected by a tumor of said patient; b) providing an isogenic human cell line representative of the tissue, wherein the cell line comprises at least the identified mutated cancer allele, which is under the control of the cell line endogenous promoter corresponding to the wild-type cancer allele promoter; c) putting in contact said cell line with the pharmacological agent; d) determining a variation of proliferation, apoptosis or cytotoxicity of the cell line in presence of the pharmacological agent; wherein the variation of proliferation, apoptosis car cytotoxicity indicative of the sensitivity/resistance of the patient tumor to the pharmacological agent.05-10-2012
20100087474MATERIALS AND METHODS FOR ENHANCED DEGRADATION OF MUTANT PROTEINS ASSOCIATED WITH HUMAN DISEASE - The invention features compositions and methods that are useful for treating or preventing a protein conformation disease in a subject by enhancing the degradation of misfolded proteins in vivo.04-08-2010
20080293759Method for Treating Cancer Based on the Modulation of Calcineurin - The present invention relates to methods for treating a haematopoietic tumor by administering a drug inhibiting calcineurin and/or the calcineurin/NFAT pathway, alone or in combination with other cancer therapy, pharmaceutical compositions useful in such methods, and screening methods for identifying a compound useful for treating a haematopoietic tumor.11-27-2008
20080293758Combination of a Steroid Sulfatase Inhibitor and an Ascomycin - A combination of a steroid sulfatase inhibitor and an ascomycin, which combination is useful as a pharmaceutical.11-27-2008
201301654712-SUBSTITUTED-THIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS - Disclosed herein are 2-substituted-thienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula06-27-2013
20100227878NOSCAPINE ANALOGS AND THEIR USE IN TREATING CANCERS, INCLUDING DRUG-RESISTANT CANCERS - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes. Representative analogs include the 9-nitro, 9-bromo-, 9-iodo-, and 9-fluoro-noscapines, which bind tubulin and induce apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. Surprisingly, treatment with one of the analogs, 9-nitro-nos, at doses as high as 100 μM, did not affect the cell cycle profile of normal human fibroblasts. This selectivity for cancer cells represents a unique edge over the other available antimitotics. The compounds can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, the compounds are novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.09-09-2010
20120190705METHODS OF INHIBITING CHOROIDAL NEOVASCULARIZATION - The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular tissues. The treatment, inhibition, and/or prevention of choroidal neovasculature (CNV) is provided, along with an animal model for CNV and imaging techniques that permit the screening of potential agents as anti-angiogenesis and anti-CNV agents.07-26-2012
20100331356SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS - Self-microemulsifying drug delivery systems and microemulsions used to enhance the solubility of pharmaceutical ingredients comprising a polyoxyethylene sorbitan fatty acid ester emulsifier; a fatty acid ester co-emulsifier and an oil.12-30-2010
20110281906SUSTAINED RELEASE FORMULATION FOR TACROLIMUS - A sustained release pharmaceutical composition for tacrolimus, comprising a solid dispersion containing tacrolimus or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a dissolution rate of tacrolimus after 4 hours from the beginning of a dissolution test is less than 35%, is disclosed.11-17-2011
200900884494-ACYLAMINOPYRIDINE DERIVATIVE MEDIATED NEUROGENESIS - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes methods based on use of a 4-acylaminopyridine derivative to stimulate or activate the formation of new nerve cells.04-02-2009
20090062326M3 MUSCARINIC RECEPTOR ANTAGONISTS FOR TREATMENT OF M3 MUSCARINIC RECEPTOR-EXPRESSING TUMORS - The present disclosure provides methods of treating a tumor using M3 muscarininc receptor antagonists, such as darifenacin. In some examples, the tumor expresses M3 muscarinic receptors, such as tumors associated with smoking. Also provided are compositions that can be used to practice such methods.03-05-2009
20090253732Production Of Polyketides And Other Natural Products - The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. Therefore in aspect the present invention provides 17-desmethylrapamycin and analogues thereof, methods for their production, including recombinant strains, and isolation and uses of the compounds of the invention. In a further aspect the present invention provides for the use of 17-desmethylrapamycin and analogues thereof in the induction or maintenance of immunosuppression, the stimulation of neuronal regeneration or the treatment of cancer, B-cell malignancies, fungal infections, transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation vascular disease and fibrotic diseases, and in the regulation of wound healing.10-08-2009
20110118298COMPOSITIONS, KITS, AND METHODS FOR IDENTIFICATION, ASSESSMENT, PREVENTION, AND THERAPY OF CANCER - Described herein are compositions, kits, and methods for determining whether subjects having cancer(s) are likely to respond to treatment with an HSP90 inhibitor, as a single agent or in combination therapy. Further described are methods for prognosing a time course of disease in a subject having such cancer.05-19-2011
20110301189STABLE PHARMACEUTICAL COMPOSITIONS OF RAPAMYCIN ESTERS - A stable pharmaceutical compositions of Rapamycin Esters, in particular Rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid that is free of antioxidants and a process of preparing the same.12-08-2011
20110294845PARENTERAL FORMULATIONS - This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.12-01-2011
20090286824Pyridine Classical Cannabinoid Compounds and Related Methods of Use - Disclosed are compounds of the formula I:11-19-2009
20090099225Method for the production of propellant gas-free aerosols from aqueous medicament preparations - The present invention relates to pharmaceutical preparations in the form of aqueous solutions for the production of propellant-free aerosols.04-16-2009
20100113501Ophthalmic Composition Comprising Ascomycin - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis.05-06-2010
20110201640TRICYCLIC COMPOUND - Provided is a tricyclic compound having a PPAR γ agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R08-18-2011
20100267760Methods of and Combination Therapies for Treating or Delaying the Onset of Dyskinesia - Methods of treating or delaying onset of levodopa-induced dyskinesia in an individual comprise administering to the individual an effective amount of mammalian target of rapamycin (mTOR) inhibitor. Methods of treating or delaying onset of dyskinesia in an individual, wherein the dyskinesia is induced by administration of a drug causing abnormal protein expression in striatal medium-size spiny neurons (MSNs), comprise administering to the individual an effective amount of mTOR inhibitor. Further, a combination therapy for an individual having Parkinson's Disease comprises levodopa or a precursor or functional analogue thereof and mTOR inhibitor.10-21-2010
20100280061NOVEL ANALGESIC THAT BINDS FILAMIN A - A compound, composition and method are disclosed that can bind to FLNA and provide analgesia. A contemplated compound has a structure that corresponds to Formula I, wherein R11-04-2010
20120149725ANHYDRATE OT TIOTROPIUM BROMIDE - Novel Anhydrate The present invention relates to a novel form of anhydrous tiotropium bromide, processes for the preparation of anhydrous tiotropium bromide, pharmaceutical compositions comprising anhydrous tiotropium bromide and uses of the compositions.06-14-2012
20100249174CCR1 ANTAGONISTS AND METHODS OF USE THEREFOR - The invention provides compounds having the formula:09-30-2010
20100249173DIHYDROQUINOLINONES AS ECTOPARASITICIDES - Disclosed are uses of dihydroquinolinone derivatives for combating ectoparasites on non-human animals. Example ectoparasites include, for example, representatives of the order acarina, including ticks and mites. Also disclosed are compositions containing dihydroquinolinone derivatives.09-30-2010
201002491729-CHLORO NOSCAPINE AND ITS USE IN TREATING CANCERS, INCLUDING DRUG-RESISTANT CANCERS - 9-Chloro-nos, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-chloro-nos, and methods of preparation and use thereof are disclosed. 9-Chloro-nos is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-Chloro-nos can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-chloro-nos is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.09-30-2010
20110028507PYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - Disclosed herein are pyridine derivatives, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylation of HIF α in a subject, modulating expression of HIF-regulated genes in a subject, treating an HIF-related disorder in a subject, increasing levels of endogenous EPO in a subject, or treating a disorder in a subject, using the disclosed compounds.02-03-2011
20120108625NOVEL FORMS OF TIOTROPIUM BROMIDE AND PROCESSES FOR PREPARATION THEREOF - This invention relates to novel crystalline forms of tiotropium bromide, processes for preparing them, and their use in pharmaceutical formulations.05-03-2012
2010008168239-Desmethoxy Derivatives of Rapamycin - The present invention relates to 39-desmethoxyrapamycin derivatives and their uses thereof. The present invention provides for the use of these compounds in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.04-01-2010
20090062325DEUTERIUM-ENRICHED TIOTROPIUM - The present application describes deuterium-enriched tiotropium, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-05-2009
20090221625COSMECEUTICAL COMPOSITION - Topical compositions comprising: —a physiologically acceptable alkanediol, ether diol or diether alcohol containing up to (8) carbon atoms; —water; and—optionally an unsaturated fatty alcohol; and optionally further conventional excipients, for use as a cosmeceutical, in particular for use in the repair or maintenance of skin barrier function. They are indicated for use in e.g. moisturizing skin, nail and mucosa and, when an optional pharmaceutically active agent is present, additionally in the treatment of various skin, nail and mucosal diseases. Also disclosed are compositions suitable for topical application to infants and babies for treating dry skin, and soothing skin irritated from diaper rash and scrapes.09-03-2009
20090093511Mast cell stabilizers in the treatment of obesity - The present invention is directed to methods of treating or preventing the development of obesity by administering compounds that stabilize mast cells. In addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing obesity.04-09-2009
20090286823CCR1 Inhibitors useful for the treatment of multiple myeloma and other disorders - The invention relates to the use of inhibitors of CCR1 for the treatment of cancers and osteolytic bone disorders. In some embodiments, the invention relates to methods for the treatment of multiple myeloma, smoldering multiple myeloma and secondary bone cancers.11-19-2009
20080207670Dermally Applicable Formulations For Treating Skin Diseases in Animals - The invention relates to pharmaceutical formulations comprising a tricyclic compound for the dermal treatment of skin diseases in animals.08-28-2008
20090137621Capsules Containing Inhalable Tiotropium - The invention relates to capsules for inhalation (inhalettes) made from specific capsule materials with a reduced moisture content, which contain the active substance tiotropium in the form of powdered preparations and are characterised by increased stability.05-28-2009
20080287482Production of Polyketides and Other Natural Products - The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these compounds. The invention is particularly concerned with methods for the efficient transformation of strains that produce FKBP analogues and recombinant cells in which cloned genes or gene cassettes are expressed to generate novel compounds such as polyketide (especially rapamycin) FKBP-ligand analogues, and to processes for their preparation, and to means employed therein (e.g. nucleic acids, vectors, gene cassettes and genetically modified strains).11-20-2008
20080207671Diagnosis and treatment of diseases arising from defects in the tuberous sclerosis pathway - The present invention relates to compositions, methods for identifying, and methods for treating abnormalities in TSC signaling pathways. In particular, the present invention relates to methods of diagnosing, treating and preventing disorders caused by defects in the TSC signaling pathway (e.g., TSC-1, TSC-2, TSC-1/TSC-2, Rheb, mTOR, S6K, and 4EBP-1) such as tuberous sclerosis, diabetes, and complications related to diabetes (e.g., insulin resistance, obesity, nephropathy). The present invention further relates to compositions for treating and preventing disorders such as tuberous sclerosis, diabetes, and complications related to diabetes (e.g., insulin resistance, obesity, nephropathy).08-28-2008
20090030028Tetrahydroquinolines - Disclosed are compounds of formula (I), wherein W, R, R01-29-2009
20090163531Use of Tiotropium Salts in the Treatment of Severe Persistent Asthma - The instant invention relates to the use of tiotropium salts for the manufacture of a medicament for the treatment of patients suffering from severe persistent asthma.06-25-2009
20120071500MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE - The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula:03-22-2012
20110224245Treatment Of Neurological Disorders Using Huperzine - Methods and compositions containing huperzine for direct delivery to central nervous system (CNS) tissue are used to alleviate pain and for the prevention and/or treatment of seizures and epilepsy. The invention is also directed to methods and compositions for using huperzine for the prevention and/or treatment of neuropathic pain and orthostatic hypotension.09-15-2011
20080234309MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE - The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula:09-25-2008
20090325998SOIL TREATING AGENT OR SEED TREATING AGENT COMPRISING QUINOLINE COMPOUNDS OR SALTS THEREOF AS ACTIVE INGREDIENT,OR METHOD FOR PREVENTING PLANT DISEASES BY USING THE SAME - A soil treating agent or a seed treating agent having excellent prevention effects against various plant pathogens (particularly against rice blast) is provided. A soil treating agent or seed treating agent, comprising one or more compounds of the general formula (Ia), (Ib) or (Ic):12-31-2009
20110230515COMPOUNDS AND METHODS FOR TREATMENT AND PREVENTION OF DISEASES - A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases.09-22-2011
20110230516CCR1 Antagonists and Methods of Use Therefor - The invention provides compounds having the formula:09-22-2011
20090023768RAPAMYCIN DERIVATIVES FOR TREATING NEUROBLASTOMA - A rapamycin derivative for use in the treatment of neuroblastome, optionally in combination with a second drug substance.01-22-2009
20110224246PHARMACEUTICAL COMPOSITIONS COMPRISING ASCOMYCIN - The invention relates to pharmaceutical compositions comprising an ascomycin in dissolved form and a pharmaceutically acceptable cellulose derivative for prevention or reduction of crystal growth.09-15-2011
20090105294Biosynthetic Gene Cluster for the Production of a Complex Polyketide - A polyketide synthase complex composed of polyketide synthase with 15 total modules, a non-ribosomal peptide synthetase with 1 module, and a cytochrome P450 hydroxylase is described. Also provided are novel 04-23-2009
20120077838Beta-2-Adrenoreceptor Agonists - Compounds of formula03-29-2012
20090221626AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 411 and 460.32 mg per 100 ml of medicament preparation.09-03-2009
20090239895Novel 3-thia-10-aza-phenanthrene derivatives - The compounds of formula I09-24-2009
20090247567BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.10-01-2009
20100152224SCOPINE MODULATORS OF MUSCARINIC ACETYLCHOLINE RECEPTOR - The present invention relates to new scopine modulators of muscarinic acetylcholine receptors, pharmaceutical compositions thereof, and methods of use thereof.06-17-2010
20100197719MEDICAMENT COMPOSITIONS CONTAINING ANTICHOLINERGICALLY-EFFECTIVE COMPOUNDS AND BETAMIMETICS - A pharmaceutical composition comprising: 08-05-2010
20100184798Methods to Predict Cholesterol Elevations during Immunosuppressant Therapy - This invention provides methods to predict the degree of elevation of serum cholesterol levels in patients treated with immunosuppressive medication. This invention also provides treatment strategies based on these predictions and kits to carry out these methods.07-22-2010
20100227879LIQUID FORMULATIONS FOR TREATMENT OF DISEASES OR CONDITIONS - Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age-related macular degeneration in a subject. The liquid formulations may comprise rapamycin or other therapeutic agents.09-09-2010
20090076060DEUTERIUM-ENRICHED TEMSIROLIMUS - The present application describes deuterium-enriched temsirolimus, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20130217717COMPOUND USEFUL FOR THE TREATMENT OF NONSENSE-MUTATION-MEDIATED DISEASES AND PHARMACEUTICAL COMPOSITION COMPRISING SAID COMPOUND - The present invention relates to the compound of formula (I)08-22-2013
20100210680TRICYCLIC HETEROCYCLIC DERIVATIVES - The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.08-19-2010
20110028506Pharmaceutical Composition For Preventintion And Treatment Of Restenosis Comprising Isoxazole Derivatives - There is provided a pharmaceutical composition for prevention and treatment of restenosis comprising isoxazole derivatives. The pharmaceutical composition includes a therapeutic effective amount of isoxazole derivatives represented by Formula 1 or pharmaceutically available salts thereof. The pharmaceutical composition may be useful to prevent and treat vascular restenosis since the pharmaceutical composition shows an anti-restenosis activity and accelerates the re-endothelization.02-03-2011
20110028508NOVEL PROCESS FOR THE PREPARATION OF SCOPINE ESTERS - The present invention relates to novel processes for the preparation of scopine esters and their quaternary salts. In particular, the present invention relates to a process for the preparation of tiotropium bromide, pharmaceutical compositions comprising tiotropium bromide and the use of such compositions in the treatment of respiratory disorders.02-03-2011
20100081681METHODS AND COMPOSITIONS FOR PREVENTING OR TREATING AGE-RELATED DISEASES - The invention provides methods for treating or preventing an age-related disease, condition, or disorder comprising administering a therapeutically effective amount of an inhibitor of TOR to a patient in need thereof. The invention also provides pharmaceutical compositions and topical formulations for treating or preventing an age-related disease, condition, or disorder comprising an inhibitor of TOR and a pharmaceutically acceptable carrier. In particular, the invention provides methods, pharmaceutical compositions, and topical formulations comprising rapamycin or an analog of rapamycin.04-01-2010
20080280940Rapamycin Derivative or an Impdh Inhibitor For Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative.11-13-2008
20090036479METHOD OF INHIBITING CHOROIDAL NEOVASCUARIZATION - The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular tissues. The treatment, inhibition, and/or prevention of choroidal neovasculature (CNV) is provided, along with an animal model for CNV and imaging techniques that permit the screening of potential agents as anti-angiogenesis and anti-CNV agents.02-05-2009
20110034503RAPAMYCIN AND ITS DERIVATIVES FOR THE TREATMENT OF LIVER-ASSOCIATED FIBROSING DISORDERS - A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula optionally in conjunction with a co-agent.02-10-2011
20110039876SOLUTION FORMULATIONS OF SIROLIMUS AND ITS ANALOGS FOR CAD TREATMENT - Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. Therapeutic agents may also be delivered to the region of a disease site. In regional delivery, liquid formulations may be desirable to increase the efficacy and deliverability of the particular drug. Also, the devices may be modified to promote endothelialization. Various materials and coating methodologies may be utilized to maintain the drugs, agents or compounds on the medical device until delivered and positioned. In addition, the devices utilized to deliver the implantable medical devices may be modified to reduce the potential for damaging the implantable medical device during deployment. Medical devices include stents, grafts, anastomotic devices, perivascular wraps, sutures and staples. In addition, various polymer combinations may be utilized to control the elution rates of the therapeutic drugs, agents and/or compounds from the implantable medical devices.02-17-2011
20090253733RAPAMYCIN CARBONATE ESTERS - Certain embodiments include carbonate esters of rapamycin at position 42 that are synthesized by a lipase catalyzed regio-specific process. These compounds or a pharmaceutically acceptable salt thereof are useful in the treatment of organ and tissue transplant rejection, autoimmune disease, proliferative disorder, restenosis, cancer, or microbial infection.10-08-2009
20090215813HISTONE DEACETYLASE INHIBITORS AS IMMUNOSUPPRESSANTS - A method of preventing or suppressing an immune response or immune mediated response comprising administering an effective amount of an histone deacetylase inhibitor compound alone or in combination with a second pharmacologically active agent.08-27-2009
20090215812BIOMARKERS FOR EVALUATING LIKELIHOOD OF TUMOR SENSITIVITY TO AN MTOR INHIBITOR - The present invention provides compositions and methods for evaluating the likelihood that a tumor is sensitive to an mTOR inhibitor, e.g., rapamycin or a rapamycin analog. The invention provides FKBP proteins as biomarkers for predicting the likelihood that a tumor is sensitive to an mTOR inhibitor. The methods include assessing the expression or activity of an FKBP protein, e.g., FKBP 12, in a subject with a tumor or in a sample derived from a tumor. Additional biomarkers and biomarker combinations are also provided. The invention also provides kits containing, e.g., a validated antibody or ligand for assessing the expression or activity of an FKBP protein.08-27-2009
20100063084MULTI-PHASE RELEASE METHSCOPOLAMINE COMPOSITIONS - Formulations have been developed administering methscopolamine in multi-phases. In a preferred embodiment, the formulation contains methscopolamine in an immediate release. (“IR”) form and a sustained or delayed release (“DR”) form and/or poised release (“PR”) form. In another embodiment, the methscopolamine is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. This kit can be a blister pack or equivalent, wherein the drug is packaged so that a first dosage is taken, then sequentially larger dosages. The dosages can be the same in each unit, and instructions provided so that the correct dosage is obtained through the number of units and the time of administration or the dosages may be different, and the units ordered so dial the desired dosage administration profile is obtained when the patient takes the units in order as instructed.03-11-2010
20110098317USE OF UNSATURATED SPHINGOSINE COMPOUNDS AS CHEMOTHERAPEUTIC AGENTS FOR THE TREATMENT OF CANCER - The present invention is directed to unsaturated sphingosine compounds which are useful as therapeutic agents for the treatment of cancer and for the treatment of other diseases including diabetes and infection with intracellular bacteria. This invention is also directed to methods of using the compounds and pharmaceutical compositions comprising the compounds in treating these diseases.04-28-2011
20110251232Modified release compositions comprising tacrolimus - A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.10-13-2011
20110251231Modified release compositions comprising tacrolimus - A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.10-13-2011
20100130527INDIVIDUALIZED CANCER TREATMENT - Methods to formulate treatments for individual cancer patients by assessing genomic and/or phenotypic differences between cancer and normal tissues and integrating the results to identify dysfunctional pathways are described.05-27-2010
20110152307OPHTHALMIC COMPOSITION COMPRISING ASCOMYCIN - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis.06-23-2011
201202028422-HETEROARYLCARBOXYLIC ACID AMIDES - The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.08-09-2012
20100280060Methods of screening and compositions for life span modulators - Identification of nucleic acids involved in life span diseases and disorders or related diseases and disorders, and the use of such methods for identifying candidate agents which modulate life span diseases and disorders or related diseases and disorders are provided. Compositions and methods for treating life span diseases and disorders or related diseases and disorders are provided. Pharmaceutical compositions for treating life span diseases and disorders or related diseases and disorders are also provided11-04-2010
20120065222DEVICES AND METHODS FOR REDUCING SCAR TISSUE FORMATION - Disclosed is a cytostatic drug attached to a sterile sheet that is designed to be placed between internal body tissues to prevent the formation of post-operative adhesions, which adhesions are really scar tissue formation. This sheet onto or into which the drug is placed may be either a permanent implant or it may be biodegradable. By impregnating an existing product such as the Johnson & Johnson SURGICEL™ absorbable hemostat gauze-like sheet with an anti-proliferative drug such as sirolimus, the biodegradable, drug impregnated mesh would act as a barrier to cell proliferation and hence be a deterrent to the formation of adhesions or scar tissue. Another embodiment of this invention is a cytostatic drug attached to a sheet that is placed at the site of an anastomosis to decrease scar tissue formation from within the vessel at the site of the anastomosis.03-15-2012
20120122913COMBINATION OF CURCUMINOIDS AND MTOR INHIBITORS FOR THE TREATMENT OF TAUOPATHIES - Methods, uses, compositions, combinations and kits relating to the decrease of Tau protein levels, and prevention and/or treatment of diseases or disorders associated with Tau protein (Tauophathies), such as Alzheimer's disease, using a curcuminoid and a mammalian target rapamycin (mTOR) inhibitor, are described.05-17-2012
20120202841Topical Compositions Comprising Ascomycins - The present invention relates to a composition for topical administration comprising an ascomycin and a carrier vehicle comprising means to retain water in the outer skin layer and means to hinder water evaporating from the skin.08-09-2012
20090247565Tyrosine Kinase Inhibitors - The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.10-01-2009
20080312267Diagnosis and Treatment of Diseases Arising from Defects in the Tuberous Sclerosis Pathway - The present invention relates to compositions and methods for identifying abnormalities in TSC signaling pathways. In particular, the present invention relates to methods of diagnosing and treating disorders such as tuberous sclerosis, which are caused by mutations in the TSC genes. The present invention further relates to methods and compositions for treating cancers mediated by TSC signaling disorders.12-18-2008
20100280062(E)-N--METHANESULFONAMIDE AS GLUCOCORTICOID RECEPTOR MODULATOR FOR THE TREATMENT OF RHEUMATOID ARTHRITIS - The present invention provides Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and discloses methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof.11-04-2010
20080214595Use Of Rapamycin Derivatives For The Treatment And/Or Prevention Of Cardiovas Cular Disorders - The present invention provides methods of treating and/or preventing cardiovascular disorders comprising administering rapamycin derivative compounds.09-04-2008
20080255177ANTI-TUMOR ACTIVITY OF CCI-779 IN PAPILLARY RENAL CELL CANCER - This invention provides the method or use of CCI-779 in the treatment of papillary renal cell carcinoma.10-16-2008
20120302595FKBP52-TAU INTERACTION AS A NOVEL THERAPEUTICAL TARGET FOR TREATING THE NEUROLOGICAL DISORDERS INVOLVING TAU DYSFUNCTION - The invention relates generally to neuro-protection and repair in neurological disorders involving Tau dysfunction (including Alzheimer's disease). The invention describes AND INCLUDES a direct interaction between proteins FKBP52 and Tau. More particularly, the invention relates to a method for screening a drug for the prevention and treatment of neurological disorders involving Tau dysfunction comprising the following steps: a) determining the ability of a candidate compound, to modulate the interaction between a Tau polypeptide and a FKBP52 polypeptide and b) selecting positively the candidate compound that modulates said interaction. The present invention finally relates to diagnostic, prognostic, and monitoring assays of neurological disorders involving Tau dysfunction.11-29-2012
20100305151O-Methylated Rapamycin Derivatives For Alleviation And Inhibition Of Lymphoproliferative Disorders - The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal.12-02-2010
2009017681939-Desmethoxy-39-Methyl Derivatives of Rapamycin - The present invention relates to novel 39-desmethoxy-39-methylrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxy-39-methylrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.07-09-2009
20120077837ANTI-TUMOR AGENT - A combination therapy for tumor is provided. Disclosed is a method of treating tumor, the method comprises administering to a patient, a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and everolimus represented by Formula (II):03-29-2012
20110136852Rapamycin Derivative or an Impdh Inhibitor for Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative.06-09-2011
20110263632Solid dispersions comprising tacrolimus - A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.10-27-2011
20100029705BETA-2-ADRENORECEPTOR AGONISTS - Compounds of formula02-04-2010
20100022578MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I)01-28-2010
20100022579SUBSTITUTED TETRAHYDROQUINOLINES - Compounds of the formula (I), in which R01-28-2010
20080214596BIOMARKERS FOR SENSITIVITY OF PROLIFERATIVE DISEASES TO MTOR INHIBITORS - Disclosed is a method for determining the sensitivity of a proliferate disease in a subject to treatment with an mTOR inhibitor, comprising determining the level of expression and/or phosphorylation state of S6 in a sample derived from the subject, as well as related methods of treatment and uses.09-04-2008
20110118297Tivozanib and Temsirolimus in Combination - A method of treating a tumor in a human patient is disclosed. The method comprises co-administering to the patient: (a) a dose of 1.5 mg tivozanib per day; and (b) a dose of 25 mg temsirolimus per week. In some embodiments of the invention, the tivozanib is administered on a repeating schedule of one dose per day for three weeks, followed by one week without tivozanib administration. The disclosed method is particularly suitable for treatment of renal cell carcinoma.05-19-2011
20080207672Methods of treating keratin hyperproliferation disorders using mTOR inhibitors - A method of treating or preventing keratin hyperproliferation skin disorders is set forth. The method includes the administration of an mTOR inhibitor to a subject afflicted with the hyperproliferation disorder. The mTOR inhibitor can be administered to the subject via any means known in the art including oral, topical, and transdermal administration.08-28-2008
20110306630PHARMACEUTICAL COMPOSITIONS COMPRISING COLLOIDAL SILICON DIOXIDE - A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight.12-15-2011
20080275076Pharmaceutical Compositions Comprising Sirolimus and/or an Analogue Thereof - The present invention relates to pharmaceutical compositions in particulate form or in solid dosage forms comprising sirolimus (rapamycin) and/or derivatives and/or analogues thereof. Compositions of the invention exhibit an acceptable bioavailability of sirolimus and/or a derivative and/or an analogue thereof. The pharmaceutical compositions of the invention are designed to release sirolimus in a controlled manner so that the plasma levels stays within the narrow therapeutic window that exist for this class of substances. An extended release profile, where the peak concentration has been reduced without loosing significant bioavailability, together with less variable absorption, is expected to improve the safety/efficacy ratio of the drug. Furthermore, compositions according to the invention provide for a significant reduced food effect and a delayed release of sirolimus is expected to reduce the number of gastro-intestinal related side effects.11-06-2008
20090082386Ascomycin and pimecrolimus having reduced levels of desmethylascomycin and 32-deoxy-32-epichloro-desmethylascomycin respectively, and methods for preparation thereof - Provided is ascomycin that has a low level of an FK523 impurity, and pimecrolimus that has a low level of a 32-deoxy-32-epichloro-FK523 impurity, methods of preparing them, and the use of such pimecrolimus for preparing a pharmaceutical composition.03-26-2009
20120041019PROTEASE INHIBITORS - Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.02-16-2012
20120046311CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF - Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by:02-23-2012
20120010234USE OF VEGF-D IN THE DIAGNOSIS OF LYMPHANGIOLEIOMYOMATOSIS (LAM) DISEASE - Described herein are methods of diagnosing lymphangioleiomyomatosis (LAM) that permits differentiating LAM from another lung disorder. Methods of treatment are also provided.01-12-2012
20120252835STABLE TEMSIROLIMUS COMPOSITION AND PROCESS OF PREPARING SAME - The present disclosure describes a stable composition of Temsirolimus for parenteral administration. The composition includes BHA or BHT as anti-oxidants and alcoholic solvent. The pH of the composition is below 5.0. The composition also can include a chelating agent and/or a surfactant. A method of producing the composition is also described.10-04-2012
20110166172Rapamycin Carbonic Ester Analogues, Pharmaceutical Compositions, Preparations and Uses Thereof - Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.07-07-2011
20120015971OPHTHALMIC COMPOSITION COMPRISING ASCOMYCIN - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis.01-19-2012
20120022095TOPICAL RAPAMYCIN FOR TREATMENT OF FACIAL ANGIOFIBROMAS IN TUBEROUS SCLEROSIS - The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about 0.25% to about 2% rapamycin to a small body surface area.01-26-2012
20120059027TACROLIMUS INJECTION PREPARATION - A tacrolimus injection preparation comprising tacrolimus, polyoxyethylene castor oil (35), and non-aqueous solvent is disclosed. Preferably the weight ratio of polyoxyethylene castor oil (35) to tacrolimus in the injection preparation is 0-20:1. The injection preparation significantly decreased the clinical risk.03-08-2012
20120059028THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS - The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.03-08-2012
20100168151NOVEL PROCESSES FOR PREPARING 6-(DIFLUOROMETHOXY)[1]BENZOFURO[3,2-C]PYRIDINE-9-CARBALDEHYDE, A NOVEL INTERMEDIATE FOR THE SYNTHESIS OF PDE IV INHIBITORS - The present invention relates to novel processes for preparing 6-(difluoromethoxy)[1] benzofuro[3,2-c]pyridine-9-carbaldehyde, which is a novel and useful intermediate for preparing compounds with PDE4 inhibitory activity, such as 3,5-dichloro-4-(6-difluoromethoxybenzo[4,5]furo[3,2-c]pyridin-9-ylcarboxamido)-1-pyridiniumolate.07-01-2010
20090247566Pyrano [3,2-C] Pyridones and Related Heterocyclic Compounds as Pharmaceutical Agents for Treating Disorders Responsive to Apoptosis, Antiproliferation or Vascular Disruption, and the Use Thereof - A pharmaceutical composition comprising a pharmaceutically acceptable excipient or carrier and a compound Formula I:10-01-2009
20110071186ORGANIC COMPOUNDS - This invention is directed to ophthalmic compositions comprising an ascomycin for once-a-day administration.03-24-2011
20120208836COMPOSITIONS AND METHODS FOR THE TREATMENT OF OBESITY AND RELATED DISORDERS - Provided herein are compositions and methods for the treatment of obesity and related disorders, including, but not limited to insulin resistance, diabetes, and hepatic steatosis. For example, in some embodiments, pharmaceutically acceptable compositions and methods are provided employing amlexanox, a derivative thereof, or a pharmaceutically acceptable salt thereof, alone or in combination with other agents and/or medical interventions, for the treatment, prevention, and management of such diseases and conditions.08-16-2012
20080287483Polyketides and Their Synthesis and Use - The rapamycin gene cluster is an example of a gene cluster which includes a gene (rapL) leading to the formation of a precursor compound (pipecolic acid, in this case) which is required for inclusion in the larger product (rapamycin) produced by the enzymes encoded by the cluster. We have produced a mutant strain containing a rapamycin gene cluster in which the rapL gene is disabled. The strain does not naturally produce rapamycin but does so if fed with pipecolic acid. By feeding with alternative carboxylic acids we have produced variants of rapamycins. Tests have shown biological activity.11-20-2008
20120309780MICELLE COMPOSITION OF POLYMER AND PASSENGER DRUG - Hydrophobic drugs become more practical for treatments by being encapsulated in micelle compositions for increasing solubility. Micelle compositions may include an excipient tocopherol and/or prodrug formulations of the drug. Micelles extend the time period the drug remains in the micelles to improve drug circulation time and thereby drug delivery. Hydrophobic drugs for micelle encapsulation may include rapamycin, geldanamycin, and paclitaxel. Administration of these micelle compositions does not require Cremophor EL or Tween 80, avoiding serious side effects associated with these products which would previously accompany such drug administration.12-06-2012
20110184010METHOD OF TREATING MANTLE CELL LYMPHOMA - This invention provides the use of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) in the treatment or inhibition of mantle cell lymphoma.07-28-2011
20120165364NOVEL FORMS OF TIOTROPIUM BROMIDE AND PROCESSES FOR PREPARATION THEREOF - This invention relates to novel crystalline forms of tiotropium bromide, processes for preparing them, and their use in pharmaceutical formulations.06-28-2012
20100210679PREVENTIVE AND THERAPEUTIC MEDICAMENT FOR GASTROESOPHAGEAL REFLUX DISEASE - The compound of the following formula:08-19-2010
20120214836SENSITIZER, PHARMACEUTICAL COMPOSITION, KIT AND USE FOR TARGET THERAPY - A target therapy sensitizer including rapamycin and substituted quinoline is disclosed. In addition, a pharmaceutical composition containing the sensitizer, a target therapy sensitization kit containing the two aforementioned compounds, and a use of a combination of the two aforementioned compounds as a target therapy sensitizer are also disclosed. The application of the target therapy sensitizer, pharmaceutical composition, kit and use is advantageous for improving the treatment effect of target therapies.08-23-2012
20120214837SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE10A) - The invention relates to compounds of the formula08-23-2012
20120214834IMMUNE ENHANCEMENT COMPOSITION AND KIT AND USE THEREOF - An immune enhancement composition is disclosed. The immune enhancement composition includes rapamycin, substituted quinoline and a pharmaceutically acceptable carrier, diluent, excipient or a combination thereof. An immune enhancement kit containing the two aforementioned compounds and a use of a combination containing the two aforementioned compounds as an immune enhancement composition are also disclosed. The application of the composition, kit and use is advantageous for promoting the activity of the immune system.08-23-2012
20120214835SENSITIZER, KIT AND USE FOR CANCER THERAPY - A cancer therapy sensitizer is disclosed. The cancer therapy sensitizer includes rapamycin and substituted quinoline. The present invention discloses a cancer therapy sensitization kit containing the two aforementioned compounds and a use of a combination of the two aforementioned compounds as a cancer therapy sensitizer as well. The application of the cancer therapy sensitizer, the kit and the use of the present invention is advantageous for improving the treatment effect of cancer therapies.08-23-2012
20100179182PHARMACEUTICAL FORMULATION - The present invention provides processes for making and forms of solid dispersions of pharmaceutical active ingredients.07-15-2010
20120136023Inhibitors of HIV Replication - The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.05-31-2012
20100173928Phosphorylation and regulation of AKT/PKB by the rictor-mTOR complex - In certain aspects, the invention relates to methods for identifying compounds which modulate Akt activity mediated by the rictor-mTOR complex and methods for treating or preventing a disorder that is associated with aberrant Akt activity.07-08-2010
20110201639STABILIZED TACROLIMUS COMPOSITION - The invention relates to a stable pharmaceutical composition comprising comprising a solid dispersion of tacrolimus in a vehicle further comprising a stabilizing agent capable of providing a pH below 7 in the composition, as measured after re-dispersion in water, and preventing or reducing the formation upon storage of major degradation products of tacrolimus, in particular the 8-epitacrolimus.08-18-2011
20090042923Method of Treating Tumors with Azaxanthones - The use of azaxanthones for treating diseases associated with tumor cells which express one or more protein of S100 family, and in treating patients that have malignancies consisting of tumors of an epithelial or mesenchymal nature, where these compounds are effective in retarding the progression and/or metastasis of these tumors.02-12-2009
20100292266Oxazolyl Piperidine Modulators of Fatty Acid Amide Hydrolase - Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).11-18-2010
20120220619Rapamycin Derivative or an Impdh Inhibitor for Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative.08-30-2012
20110212988TACROLIMUS PREPARATION FOR EXTERNAL APPLICATIONS - The present invention provides tacrolimus containing ointment having low dermal irritation and excellent stability. It was found that an ointment comprising triacetin as a solubilizer for tacrolimus may sufficiently solubilize tacrolimus, has low dermal irritation and excellent stability. Preferably, the ointment of the present invention is an o/o type (oil-in-oil type) ointment in which tacrolimus-solubilized triacetin droplets are dispersed in an ointment base, preferably a mixture of beeswax and petrolatum.09-01-2011
20120101120PURE ISOMERS OF TRITOQUALINE - The invention provides an isolated stereoisomer of tritoqualine having the structure of FIG. 04-26-2012
20120289536Pharmaceutical Compositions Comprising Colloidal Silicon Dioxide - A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight.11-15-2012
20130018069SUSTAINED RELEASE DELIVERY SYSTEMS FOR THE PREVENTION AND TREATMENT OF HEAD AND NECK CANCERS - The present invention discloses a method of treating a head and neck cancer or preventing the development of pre-malignant lesions to this cancer, by administering locally to the oral cavity, a sustained release drug delivery system comprising a drug for the treatment of this cancer or for the prevention of said lesions, and at least one polymer, such that said system is attached to a surface in the oral cavity and remains attached thereto for at least 1 hour, accompanied by release of the drug and maintaining an effective therapeutic concentration thereof in the cavity, for at least 1 hour. Further are disclosed a sustained release drug delivery system and a liquid precursor varnish composition to this system.01-17-2013
20080249124WORTMANNIN-RAPALOG CONJUGATE AND USES THEREOF - An anti-neoplastic wortmannin conjugate is described formed by a linking a rapalog and wortmannin. Such a linkage is removable following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.10-09-2008
20130184305PROCESS FOR PREPARATION OF NOVEL 42-O-(HETEROALKOXYALKYL) RAPAMICIN COMPOUNDS WITH ANTI-PROLIFERATIVE PROPERTIES - The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol, Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2-methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2-dimethyl-6-phenyl 2H-Pyran-3-ol.07-18-2013
20130178494PHENYL N-MUSTARD LINKED TO DNA-AFFINIC MOLECULES OR WATER-SOLUBLE ARYL RINGS, METHOD AND THEIR USE AS CANCER THERAPEUTIC AGENTS - The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.07-11-2013
20090105293USE OF THIENOPYRIDONE DERIVATIVES AS AMPK ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Use of thienopyridone derivatives of formula (I), in which B, R, R04-23-2009
20120252834NOVEL USE AND METHOD OF RAPAMYCIN TO TREAT TOXIC SHOCK - Rapamycin is used for prevention and treatment of toxic shock. The toxic shock is induced, for example, by a toxin, such as 10-04-2012
20130172383TREATMENT OF FIBROSING DISORDERS - A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula07-04-2013
20130116271TACROLIMUS-CONTAINING OIL-IN-WATER TYPE CREAMY COMPOSITION - The purpose is to provide a tacrolimus-containing pharmaceutical composition which is a creamy preparation for external application having good feeling upon use and has high stability of a main ingredient contained therein (high main ingredient residual ratio), and allows easy control of skin concentration of the main ingredient.05-09-2013
20130096150Substituted Azoanthracene Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof - The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.04-18-2013
20110275659Tacrolimus For Improved Treatment Of Transplant Patients - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.11-10-2011
20110237617THIENO[2,3-C] ISOQUINOLINES FOR USE AS INHIBITORS OF PARP - The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula:09-29-2011
20110257215NOVEL CO-CRYSTAL OF TIOTROPIUM BROMIDE - The invention relates to a new crystalline form of tiotropium bromide, processes for preparing it and its use for preparing a pharmaceutical composition for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.10-20-2011
20130150397RAPAMYCIN COMPOSITION - In one aspect, the present invention is directed to a dry, flowable and compressible rapamycin composition comprising a specific mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers. In other aspects, the present invention is directed to a method of making the composition.06-13-2013
20100305150TUBEROUS SCLEROSIS TREATMENT - Rapamycin derivatives for use in the treatment of neurocutaneous disorders.12-02-2010
20120283285TREATMENT OF SOLID TUMORS WITH RAPAMYCIN DERIVATIVES - Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent.11-08-2012
20110288114COMPOSITIONS FOR THE TREATMENT OF FIBROTIC DISEASES OR CONDITIONS - A method of treating a fibrotic disease or condition in a patient comprising administering noscapine and a pharmaceutical carrier to said patient.11-24-2011
201102948449-AMINONOSCAPINE AND ITS USE IN TREATING CANCERS, INCLUDING DRUG-RESISTANT CANCERS - 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.12-01-2011
20090176820POLYMORPHIC FORMS AND PROCESS - The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula I07-09-2009
2009020957236-Des(3-Methoxy-4-Hydroxycyclohexyl) 36-(3-Hydroxycycloheptyl) Derivatives of Rapamycin for the Treatment of Cancer and Other Disorders - The present invention relates to novel 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.08-20-2009
20120029009Tacrolimus For Improved Treatment Of Transplant Patients - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.02-02-2012
20130197024LIQUID FORMULATIONS FOR TREATMENT OF DISEASES OR CONDITIONS - Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age-related macular degeneration in a subject. The liquid formulations may comprise rapamycin or other therapeutic agents.08-01-2013
20080280939Combination of Organic Compounds - The invention relates to a pharmaceutical combinations comprising an AT1 receptor blocker or pharmaceutically acceptable salts thereof and a mTOR inhibiting agent, e.g. rapamycin or a rapamycin derivative, optionally in the presence of a pharmaceutically acceptable carrier.11-13-2008
20120295933TREATMENT OF COPD, GASTRO-ESOPHAGEAL REFLUX DISEASE (GERD), FOOD ALLERGIES AND OTHER GASTROINTESTINAL CONDITIONS AND DISORDERS AMELIORATED BY PROPER HISTAMINE MANAGEMENT USING A COMBINATION OF HISTIDINE DECARBOXYLASE INHIBATORS, LRA DRUGS, ANTI-H1 AND/OR ANTI-H2 DRUGS - The invention provides a method for the treatment of COPD and/or gastrointestinal disease conditions ameliorated by histamine management in a subject, comprising administering to the subject an effective amount of a histidine decarboxylase inhibitor.11-22-2012
20120065223SOLID FORMS OF A CHEMOKINE RECEPTOR ANTAGONIST AND METHODS OF USE THEREOF - The citrate salt of (S)-4-(4-Chloro-phenyl)-1-{3-[7-(1-hydroxy-1-methyl-ethyl)-11H-10-oxa-1-aza-dibenzo[a,d]cyclohepten-5-ylidene]-propyl}-3,3-dimethyl-piperidin-4-ol, which may be used in pharmaceutical applications, is disclosed. The crystalline Citrate Salt, including particular single crystal forms and combinations of the single crystalline forms, are also discussed. Mixtures for forming the crystalline salts are discussed. As well, methods of producing the Citrate Salt, and crystalline forms thereof, and using such Citrate Salt, and crystalline forms thereof, in treating diseases associated with aberrant leukocyte recruitment, activation, or recruitment and activation are also discussed.03-15-2012

Patent applications in class Plural hetero atoms in the tricyclo ring system

Patent applications in all subclasses Plural hetero atoms in the tricyclo ring system