| 36th week of 2008 patent applcation highlights part 50 |
| Patent application number | Title | Published |
|---|
| 20080214521 | Sensitization of Drug-Resistant Lung Caners to Protein Kinase Inhibitors - The present invention relates to a method of treating non-small cell lung cancer with FLT-3 kinase inhibitor such as PKC412. The invention also relates to a pharmaceutical combination of a FLT-3 kinase inhibitor and an activator of permeabilization of the mitochondrial outer membrane, such as an activator of BAK. It also relates to the use of a pharmaceutical combination of an activator of permeabilization of the mitochondrial outer membrane and a FLT-3 kinase inhibitor for the treatment of non-small cell lung cancer and the use of such a pharmaceutical composition for the manufacture of a medicament for the treatment of same. | 2008-09-04 |
| 20080214522 | Antiviral indoles - Compounds of the formula (I): | 2008-09-04 |
| 20080214523 | Method for treating severe heart failure and medicament therefor - A method for treating severe heart failure, comprising administering to a patient an effective amount of a benzazepine compound (1): wherein R | 2008-09-04 |
| 20080214524 | FUSED AZABICYCLIC COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1 (VR1) RECEPTOR - Compounds of formula (I) | 2008-09-04 |
| 20080214525 | Alkyl 4- [4- (5-Oxo-2,3,5, 11A-Tetrahydo-5H-Pyrrolo [2, 1-C] [1,4] Benzodiazepine-8-Yloxy) -Butyrylamino]-1H-Pyrrole-2-Carboxylate Derivatives and Related Compounds For the Treatment of a Proliferative Disease - A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R | 2008-09-04 |
| 20080214526 | Macrocyclic Compounds and Compositions Useful as Bace Inhibitors - The invention relates to novel macrocyclic compounds of the formula in which R | 2008-09-04 |
| 20080214527 | Hiv Integrase Inhibitors - The present invention features compounds that are HIV integrase inhibitors useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 2008-09-04 |
| 20080214528 | ANTI-INFECTIVE AGENTS - The present invention provides HCV polymerase inhibiting compounds having the formula (I): | 2008-09-04 |
| 20080214529 | SATURATED FUSED [1,2-b]PYRIDAZINONE COMPOUNDS - The invention is directed to saturated fused [1,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus. | 2008-09-04 |
| 20080214530 | Photo-Activated Disinfection - The present invention relates to photo-activated disinfection. In particular, the present invention relates to photo-activated disinfection in the oral cavity. We describe a dental apparatus comprising a light source producing light at a predetermined wavelength and power, and optical transmission means to train the light from the light source onto at least one external side of a tooth. Preferably, the optical transmission means comprises at least one optical guide. In a preferred embodiment, the optical transmission means comprises a pair of substantially parallel elongate light guides each light guide having a distal end provided with a reflective surface inclined at 45° to the direction of light transmission along the light guides, the reflective surfaces of the light guides being opposed such that light emitted from each light guide is parallel but opposite in direction. Preferably, the light source is a light emitting diode or array of light emitting diodes and the has a wavelength of from 550 to 690 nm, more preferably from 600 nm to 680 nm, even more preferably from 625 to 660 nm. | 2008-09-04 |
| 20080214531 | Methods and compositions for the treatment of insulin resistance, diabetes, and diabetes-associated dyslipdemia - Methods for the treatment of insulin resistance, diabetes, and/or diabetes associated dyslipidemia by administering niacin and meloxicam are disclosed. | 2008-09-04 |
| 20080214532 | Carboxanilides as Microbiocides -
Compounds of the formula (I) in which the substituents are as defined in claim | 2008-09-04 |
| 20080214533 | Cyclic Iminocarbamates And Their Use - The invention relates to novel cyclic iminocarbamates of formula (I), | 2008-09-04 |
| 20080214534 | (1,10B-Dihydro-2-(Aminoalkyl-Phenyl)-5H-Pyrazolo[1,5-C][1,3]Benzoxazin-5-Yl)Phenyl Methanone Derivatives as Hiv Viral Replication Inhibitors - The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS. | 2008-09-04 |
| 20080214535 | Amorphous Aprepitant Coprecipitates - A coprecipitate comprising amorphous aprepitant and a pharmaceutically acceptable carrier is prepared by rapidly removing solvent from a solution containing aprepitant and the carrier. | 2008-09-04 |
| 20080214536 | Amido-Substituted 6-Phenylphenanthridines - Compounds of a certain formula (I) | 2008-09-04 |
| 20080214537 | BRIDGED PHENANTHRIDINES - Bridged phenanthridine compounds having the structure of formula I or of formula II are provided: | 2008-09-04 |
| 20080214538 | Pyridoindolone Derivatives Substituted in the 3-Position by a Phenyl, Their Preparation and Their Application in Therapeutics - The present disclosure relates to pyridoindolone derivatives of general formula (I): | 2008-09-04 |
| 20080214539 | Benzisoxazole Piperidine Compounds and Methods of Use Thereof - The invention includes benzisoxazole piperidine compositions and methods of using them for modulating sleep. | 2008-09-04 |
| 20080214540 | Substituted indolealkanoic acids - Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis. | 2008-09-04 |
| 20080214541 | COMPOSITIONS AND METHODS FOR INDUCING OSTEOGENESIS - The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage. | 2008-09-04 |
| 20080214542 | Arylpiperazine Derivatives and their Use as Selective Dopamine D3 Receptor Ligands - The invention concerns compounds of general formula (I), a method for preparing same, as well as their use as therapeutic agent. | 2008-09-04 |
| 20080214543 | N-Phenyl-(2R,5S)Dimethylpiperazine Derivative - The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention. | 2008-09-04 |
| 20080214544 | Substituted heterocycles and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as c-met mediated diseases and/or HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 2008-09-04 |
| 20080214545 | Substituted Pyrazolyl Urea Derivatives Useful in the Treatment of Cancer - The present invention relates to compounds of formula (I), pharmaceutical compositions which contain them and methods for treating cancer using compounds of formula (I). | 2008-09-04 |
| 20080214546 | N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE - The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. | 2008-09-04 |
| 20080214547 | METHODS AND COMPOSITIONS OF TRAIL-DEATH RECEPTOR AGONISTS/ACTIVATORS - This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies. | 2008-09-04 |
| 20080214548 | 2-Cyano-Pyrimidines and-Triazines as Cysteine Protease Inhibitors - The invention relates to compounds of the formula I | 2008-09-04 |
| 20080214549 | N-Substituted Glycine Derivatives: Hydroxylase Inhibitors - The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) | 2008-09-04 |
| 20080214550 | Novel inhibitors of folic acid-dependent enzymes - The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof: | 2008-09-04 |
| 20080214551 | Treatment of Burns - The present invention provides methods of treatment of burns, which comprise the step of applying to the burns of a subject a therapeutically effective amount of a metal ion chelating agent. | 2008-09-04 |
| 20080214552 | Substituted Pyridazinecarboxamides and Derivatives Thereof - The present invention relates to compounds of the formula (I) | 2008-09-04 |
| 20080214553 | 2-(4-Oxo-4H-Quinazolin-3-Yl) Acetamides and Their Use as Vasopressin V3 Antagonists - The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression. | 2008-09-04 |
| 20080214554 | Methods for preventing or treating cardiac arrhythmia - Disclosed are methods of preventing or treating cardiac arrhythmia comprising administering to a mammal in need thereof, such as a human, an effective amount of vanoxerine (GBR 12909) or a pharmaceutically acceptable salt, derivative or metabolite thereof. | 2008-09-04 |
| 20080214555 | USE OF RANOLAZINE FOR THE TREATMENT OF CARDIOVASCULAR DISEASES - Disclosed are methods for treating patients suffering from cardiovascular diseases comprising administering an intravenous (IV) infusion of ranolazine. In one embodiment, the IV infusion of ranolazine is followed by an orally administered sustained release ranolazine dosage formulation to maintain human ranolazine plasma levels at therapeutic levels in patients. | 2008-09-04 |
| 20080214556 | USE OF RANOLAZINE FOR THE TREATMENT OF CARDIOVASCULAR DISEASES - Disclosed are methods for treating patients suffering from cardiovascular diseases comprising administering an intravenous (IV) infusion of ranolazine. In one embodiment, the IV infusion of ranolazine is followed by an orally administered sustained release ranolazine dosage formulation to maintain human ranolazine plasma levels at therapeutic levels in patients. | 2008-09-04 |
| 20080214557 | METHOD FOR PREPARATION OF PHARMACEUTICAL COMPOSITION HAVING IMPROVED DISINTEGRATABILITY AND PHARMACEUTICAL COMPOSITION MANUFACTURED BY SAME METHOD - There exists a strong desire both for pharmaceutical compositions which rapidly exhibit pharmacological effects without an increase in the size of the dosage form or a decline in quality due to interactions between a pharmaceutically active ingredient and the disintegrant, and also for a method of preparing such pharmaceutical compositions. Such a desire is especially acute with regard to, for example, preparations which contain a drug such as an analgesic or a quick-acting hypoglycemic drug that requires the rapid appearance of pharmacological effects following administration, preparations which have a high content of the pharmaceutically active ingredient, and preparations which contain two or more different pharmaceutically active ingredients. Thus, the object of the present invention is to improve the disintegratability of the pharmaceutical compositions without increasing the size of the dosage form and without a decline in quality due to interactions between the pharmaceutically active ingredient and the disintegrant. The present invention provides a method for preparing a pharmaceutical composition having a rapid disintegration time, comprising: blending, in the pharmaceutical composition containing a pharmaceutically active ingredient, at least one disintegrant and at least one water-soluble salt having a pH being from 3 to 9 in an aqueous solution of 2.5% concentration. The invention also provides a premix composition obtained by the preliminary mixture of a disintegrant with a water-soluble inorganic salt having a pH of from 3 to 9 in an aqueous solution of 2.5% concentration. | 2008-09-04 |
| 20080214558 | PYRIMIDINE-2,4-DIAMINE DERIVATIVES AND THEIR USE AS JAK2 KINASE INHIBITORS - Pyrimidine-2,4-diamines derivatives having activity as JAK2 kinase inhibitors are disclosed, as well as pharmaceutical compositions and methods for using the same in the treatment of cancer and other JAK2 kinase-associated conditions. | 2008-09-04 |
| 20080214559 | COMPOUNDS WITH A COMBINATION OF CANNABINOID CB1 ANTAGONISM AND SEROTONIN REUPTAKE INHIBITION - Compounds with a combination of cannabinoid CB | 2008-09-04 |
| 20080214560 | Use of Pyrimidine Derivatives in the Manufacture of a Medicament for Prevention and/or Treatment of Alzheimer's Disease - Pyrimidine derivatives of formula I, | 2008-09-04 |
| 20080214561 | SOLID FORMS OF [4-(3-FLUORO-5-TRIFLUOROMETHYL-PYRIDIN-2-YL)-PIPERAZIN-1-YL-[5-METHANESULFONYL-2-((S)-2,2,2-TRIFLUORO-1-METHYL-ETHOXY)-PHENYL]-METHANONE - The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparation of pharmaceutical compositions. The compounds of present invention are suitable for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease. | 2008-09-04 |
| 20080214562 | Chemical Compounds - The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to a chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell. | 2008-09-04 |
| 20080214563 | Benzimidazole Thiophene Compounds As Plk Modulators - The present invention provides 5-heteroaryl substituted benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. | 2008-09-04 |
| 20080214564 | MACROLIDE COMPOUND IN SOLID FORM, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed. | 2008-09-04 |
| 20080214565 | Oxazolidinone Derivatives as Antimicrobials - The present invention relates to certain substituted phenyl oxazolidinones of formula I and H and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms as | 2008-09-04 |
| 20080214566 | Amorphous ziprasidone mesylate - Provided is amorphous form of ziprasidone mesylate and process for its preparation. Also provided is a process for preparing ziprasidone mesylate dihydrate needle crystals. | 2008-09-04 |
| 20080214567 | Benzimidazole Thiophene Compounds - The present invention provides benzimidazole thiophene compounds, pharmaceutical compositions containing the same, and their use as pharmaceutical agents. | 2008-09-04 |
| 20080214568 | Pharmaceutical Combination Comprising an Antifungal Agent and an Active Substance Selected From Carveol, Eugenol, Thymol, Borneol, Carvacrol, and Alpha- and Beta-Ionones - The present invention relates to a pharmaceutical composition. The inventive pharmaceutical composition comprises: at least a first therapeutically-active substance which is selected from carveol, thymol, eugenol, borneol, carvacrol, alpha-ionone, beta-ionone and the isomers, derivatives and mixtures thereof; and at least a second therapeutically-active substance which is an antifungal agent. | 2008-09-04 |
| 20080214569 | Use of phosphatases to treat tumors overexpressing N-CoR - This invention provides a method of treating a patient suffering from a tumor overexpressing N—CoR comprising administering to the patient a phosphatase ligand, alone or in combination with a retinoid receptor ligand, a histone deacetylase ligand, or both, in amounts effective to treat the patient. This invention also provides a method of inhibiting tumor growth in a patient suffering from a tumor overexpressing N—CoR. This invention further provides a method of identifying a compound or a mixture of compounds capable of inducing differentiation of cells of a tumor overexpressing N—CoR. This invention still further provides a method of determining the likelihood of successfully treating a subject suffering from a tumor overexpressing N—CoR. This invention also provides a method of assessing the likelihood that a patient is suffering from a tumor overexpressing N—CoR. This invention yet also provides a method of assessing the likelihood that a patient previously suffering from and treated for a tumor overexpressing N—CoR has suffered a recurrence of a tumor overexpressing N—CoR. Finally, this invention provides analogous methods for use on glioblastoma multiforme. | 2008-09-04 |
| 20080214570 | Therapeutic Agents - The present invention relates to compounds of formula I and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 2008-09-04 |
| 20080214571 | NOVEL COMPOUNDS - Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of anxiety. | 2008-09-04 |
| 20080214572 | Selected Tetracyclic Tetrahydrofuran Derivatives Containing a Cyclic Amine Side Chain - This invention concerns novel tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain with binding affinities towards serotonin receptors, in particular 5-HT | 2008-09-04 |
| 20080214573 | Compounds Useful for Inhibiting Chk1 - Substituted urea compounds useful in the treatment of diseases and C | 2008-09-04 |
| 20080214574 | Inhibition of the Activity of the Capsaicin Receptor in the Treatment of Obesity or Obesity-Related Diseases and Disorders - The present invention provides a method of treating diseases or disorders benefiting from inactivating or down regulating the activity of the capsaicin receptor in a mammal by inhibiting the activity of the capasaicin receptor. | 2008-09-04 |
| 20080214575 | PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS - The present invention provides a compound of the formula | 2008-09-04 |
| 20080214576 | Topoisomerase Inhibitors and Prodrugs - Compositions and methods for treating cancer and other hyperproliferatice disease conditions with topoisomerase inhibitors and their prodrugs are disclosed. | 2008-09-04 |
| 20080214577 | New Compounds 320 - This invention relates to novel compounds having the structural formula I below: | 2008-09-04 |
| 20080214578 | Novel 5-Substituted 7-Amino-[1,3]Thiazolo[4,5-D]Pyrimidine Derivatives 793 - There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R | 2008-09-04 |
| 20080214579 | THIENOPYRIMIDINEDIONES AND THEIR USE IN THE MODULATION OF AUTOIMMUNE DISEASE - The invention relates to thienopyrimidinediones of formula (1): | 2008-09-04 |
| 20080214580 | 6-SUBSTITUTED 2-(BENZIMIDAZOLYL)PURINE AND PURINONE DERIVATIVES FOR IMMUNOSUPPRESSION - The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II: | 2008-09-04 |
| 20080214581 | Purine Derivatives as Agonists of the Adenosine A2a Receptor - A compound of formula (I): | 2008-09-04 |
| 20080214582 | Purine Derivatives as Inhibitors of Receptor Tyrosine Kinase Activity - Compounds of the formula (I), in which R | 2008-09-04 |
| 20080214583 | 7H-Pyrrolo[2,3-D]Pyrimidine Derivatives, As Well As Their Therapeutically Acceptable Salts, Pharmaceutical Preparations Containing Them And Process For Production The Active Agent - The invention relates to new 7H-pyrrolo[2,3-d]pyrimidine derivatives, as well as their therapeutically acceptable salts, pharmaceutical preparations containing them and process for producing the active agent. The pharmaceutical preparation is adventageously antiphlogistic and analgetic one, a preparation reducing neuropathic hyperalgesia and rheumatic arthritis, a preparation for hindering destruction of bones chondrus, being applicable for treatment of other diseases, which may be connected with other inflammatory processes e.g. asthma, eczema or psoriasis. | 2008-09-04 |
| 20080214584 | Method for treating cancer - The present invention provides a method for treating cancer, which includes selecting a patient coexpressing HER2 and HER3, and administering an effective amount of a HER2 inhibitor to the patient. | 2008-09-04 |
| 20080214585 | NEW CLASSICAL ANTIFOLATES - The present invention is directed to antifolate compounds having the structure | 2008-09-04 |
| 20080214586 | 2-Amino-4-Phenylquinazoline Derivatives and the Use Thereof as Hsp90 Modulators - Novel phenylquinazoline derivatives of the formula (I), in which R | 2008-09-04 |
| 20080214587 | Processes For the Preparation of Azoxystrobin Using Dabco as a Catalyst and Novel Intermediates Used in the Processes - The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO | 2008-09-04 |
| 20080214588 | Hiv Inhibiting 2-(4-Cyanophenyl)-6-Hydroxylaminopyrimidines - HIV replication inhibitors of formula (I) pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R | 2008-09-04 |
| 20080214589 | Thrombin Inhibiting 2,4-Dioxo-3,4-Dihydropyrimidine Derivatives - There is provided a compound of formula I wherein R | 2008-09-04 |
| 20080214590 | Zalcitabine (Ddc) Boosted Lamivudine (3Tc) Compositions for Antiretroviral Therapy - Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound is a new therapeutic anti HIV option, in combination with another drug such as a NRTI or a protease inhibitor. It's heightened and sustained antiretroviral potency is due to the increased intracellular level of 3TC triphosphate, the active form of 3TC. This effect is obtained by combining 3TC, in usual doses, with a reduced dose of ddC, in the same pharmaceutical formulation. The product could be administered twice or even once daily, which is convenient, and does not increase the pill burden for the patient. The reduced ddC dosage prevents the occurrence of ddC related side effects. Other cytidine derivatives (racemic or negative enantiomers) could have the same effects as ddC and could probably be combined with 3TC, and have the same effect. On the other hand, low dose ddC may also increase the intracellular levels of other cytidine derivatives as it does for 3TC. Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound could also be formulated in combination with another drug such as another NRTI (e.g. abacavir) or any protease inhibitor in the same capsule or tablet. This approach offers a dual anti-HIV therapy that is as efficacious as the routine triple therapy. In this way the HIV treatment cost could be significantly reduced which is imperative for resource-poor settings. This new formulation is convenient and well tolerated with no additional toxicity than that of the combining drug (NRTI or protease inhibitor) and 3TC. Moreover, this will enable a larger number of patients to benefit from the already known 3TC effects. It will also increase the 3TC effects in those organs or HIV sanctuaries with usually reduced 3TC concentrations or activity. It could be indicated in both the initial as well as in salvage HIV therapy. It could also be used for therapy optimization or simplification. Moreover, in combination with another NRTI such as abacavir, or even alone, it could be beneficial for reducing the HIV harm in resource-poor settings. | 2008-09-04 |
| 20080214591 | N-Aryl Diazaspirocyclic Compounds and Methods of Preparation and Use Thereof - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle). | 2008-09-04 |
| 20080214592 | METHODS OF TREATING ANXIETY DISORDERS - Disclosed are methods of treating an anxiety disorder, e.g., obsessive compulsive disorder, in an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to restore normal monoaminergic tone within the synapse. | 2008-09-04 |
| 20080214593 | TETRACYCLIC AMINO AND CARBOXAMIDO COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to Tetracyclic Amino Compounds and Tetracyclic Carboxamido Compounds, compositions comprising an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, Parkinson's disease, renal failure, a vascular disease, a cardiovascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound. | 2008-09-04 |
| 20080214594 | Inhibitors Of Checkpoint Kinases - The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 2008-09-04 |
| 20080214595 | Use 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. | 2008-09-04 |
| 20080214596 | BIOMARKERS 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. | 2008-09-04 |
| 20080214597 | Tricyclic Lactam Derivatives as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors - the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein
| 2008-09-04 |
| 20080214598 | Novel Piperidine Carboxylic Acid Amide Derivatives - The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin. | 2008-09-04 |
| 20080214599 | Use of Par-1/Par-4 Inhibitors for Treating or Preventing Vascular Diseases - Use of a compound of formula (I) or a compound selected from the group consisting of a prasugrel metabolite, clopidogrel, a clopidogrel metabolite, ticlopidine, a ticlopidine metabolite, cangrelor, a cangrelor metabolite, AZD-6140, and an AZD-6140 metabolite for the treatment of and/or prevention of coagulation induced vascular diseases and recurrence thereof in a patient in need thereof. | 2008-09-04 |
| 20080214600 | Quaternized Quinuclidine Esters - Compounds of formula (I) | 2008-09-04 |
| 20080214601 | 2-ALKYLBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS - Compounds of formulae I and II: | 2008-09-04 |
| 20080214602 | N-Biarylamides - The invention relates to N-biarylamides useful for the prophylaxis and/or treatment of impairments of perception, concentration, learning and/or memory, and to processes for preparing them, and pharmaceutical compositions containing them. | 2008-09-04 |
| 20080214603 | 5-Ht7 Receptor Antagonists - The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders. | 2008-09-04 |
| 20080214604 | Medicinal Composition - A pharmaceutical composition comprising: an active ingredient consisting of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, salt thereof, or solvate of the foregoing; and (i) a compound, a 5% (w/w) aqueous solution or suspension of which has a pH of 8 or more, and/or (ii) silicic acid, salt thereof, or solvate of the foregoing is a highly stable pharmaceutical composition, wherein under humidified and heated storage conditions, the decomposition of said compound is sufficiently reduced, or the gelation on the surface of the pharmaceutical composition is sufficiently inhibited. | 2008-09-04 |
| 20080214605 | Alkyl Sulfoxide Quinolines as Nk-3 Receptor Ligands - Compounds of Formula I | 2008-09-04 |
| 20080214606 | Methods for the Identification and Use of Compounds Suitable for the Treatment of Drug Resistant Cancer Cells - The present invention relates to novel methods for the identification of compounds useful for the treatment of drug resistance, and to novel treatment methods using the identified compounds. | 2008-09-04 |
| 20080214607 | HETEROAROMATIC QUINOLINE COMPOUNDS - The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders. | 2008-09-04 |
| 20080214608 | New generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments - This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use. | 2008-09-04 |
| 20080214609 | Development of new selective estrogen receptor modulators - The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs are disclosed, including pharmaceutical formulations of the disclosed novel compounds in useful compositions. | 2008-09-04 |
| 20080214610 | Thiazolylimidazole Derivatives and Their Use as Inhibitors of Microsmal Triglyceride Transfer Protein - The present invention relates to thiazolylimidazole derivatives of the general formula (I) in which: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3; and R | 2008-09-04 |
| 20080214611 | Pharmaceutical Compositions - 659 - The invention relates to a process for the preparation of a stable dispersion of amorphous particles of a CB1 modulator of sub-micron size in an aqueous medium. | 2008-09-04 |
| 20080214612 | SELECTIVE ESTROGEN RECEPTOR MODULATORS CONTAINING A PHENYLSULFONYL GROUP - The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata. | 2008-09-04 |
| 20080214614 | CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE - The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions. | 2008-09-04 |
| 20080214615 | N-methylaminomethyl isoindole compounds and compositions comprising and methods of using the same - This invention relates to N-methylaminomethyl-isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 2008-09-04 |
| 20080214616 | Pyridine Derivatives as Dipeptedyl Peptidase Inhibitors - The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C | 2008-09-04 |
| 20080214617 | Carbamate compounds - Carbamate compounds having a structure represented by formula I (where R | 2008-09-04 |
| 20080214618 | Gastric Therapies Amd Compositions Therefor - 1. A composition, in one or more parts, for the treatment of gastric and/or duodenal | 2008-09-04 |
| 20080214619 | Business method to treat and/or prevent a gastric acid disorder with a proton pump inhibitor (PPI) and a cholinergic agonist to induce rapid onset of PPI action with or without food - Pharmaceutical proton pump inhibitor (PPI) medications and methods are disclosed for preventing and/or treating gastrointestinal disorders characterized by abnormalities in gastric acid secretion at anytime of the day or night without the need for food effect or to be taken with food. The medications comprise a PPI and a cholinergic agonist for inducing rapid onset of PPI action, for increasing the duration of PPI efficacy and for optimizing clinical PPI effectiveness that may be administered at any time of the day or night without food or on an empty stomach, and possibly on an as-needed or on demand basis. In carrying out the methods, a PPI and cholinergic agonist may be administered together as a single unitary dose in the form of a liquid or solid, or administered together, but separately as either liquids or solids or a combination thereof. Preferably, an oral solid dosage form of the present invention allows for release of a proton pump inhibitor at a pH of about 5 or higher, e.g., pH about 5.5, 6, 6.5 or 7, followed by release of a cholinergic agonist within between about 10 minutes and about 60 minutes, preferably within about 15 minutes and about 30 minutes, after release of the proton pump inhibitor from the dosage form, so that it can be administered at any time of the day or night independent of food or food effect. It is believed that the methods and compositions of the present invention will increase the duration of PPI efficacy by between at least about 5 fold and about 10 fold or even about 20 fold, as compared to the duration of PPI efficacy derived from current PPI dosage forms administered alone and without food or a food effect. Kits comprising a PPI, a cholinergic agonist and optionally an antacid are disclosed, such as kits containing each drug in conventional and commercially available dry or liquid dosage forms for simultaneous or concomitant administration or in dry dosage forms to provide for the easy preparation of a liquid composition from the dry dosage forms. These new medications and methods will simplify the traditional continuous PPI regimen and improve patient compliance. | 2008-09-04 |
| 20080214620 | NOVEL INHIBITORS OF GLUTAMINYL CYCLASE - The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, | 2008-09-04 |
| 20080214621 | Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 - The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention compositions containing these compounds for the treatment of metabolic syndrome, diabetes, hyperglycemia obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula I wherein G | 2008-09-04 |
