18th week of 2011 patent applcation highlights part 59 |
Patent application number | Title | Published |
20110105484 | FILAMIN A-BINDING ANTI-INFLAMMATORY ANALGESIC - A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within. | 2011-05-05 |
20110105485 | Alpha-(N-Sulfonamido)Acetamide Derivatives as Beta-Amyloid Inhibitors - There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) | 2011-05-05 |
20110105486 | THIAZOLE DERIVATIVES - Wherein n is an integer of from 0 to 3; R | 2011-05-05 |
20110105487 | FILAMIN A BINDING ANTI-INFLAMMATORY AND ANALGESIC - A compound or its pharmaceutically acceptable salt, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within. | 2011-05-05 |
20110105488 | SUBSTITUTED PYRROLIDINE AND PIPERIDINE COMPOUNDS, DERIVATIVES THEREOF, AND METHODS FOR TREATING PAIN - The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia. | 2011-05-05 |
20110105489 | PLANT DISEASE CONTROLLING COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASE - A plant disease controlling composition comprising, as active ingredients, a compound represented by the formula (I), as well as at least one compound A selected from the group consisting of dimoxystrobin, trifloxystrobin, azoxystrobin, pyraclostrobin, a compound represented by the formula (II) and an agrochemically acceptable salt of the compound represented by the formula (II) : wherein, R1, Q, X, Y, Z, M and n are as defined in the description. | 2011-05-05 |
20110105490 | 2,3-DIHYDRO-1H-ISOINDOL-1-IMINE DERIVATIVES USEFUL AS THROMBIN PAR-1 RECEPTOR ANTAGONIST - The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists. | 2011-05-05 |
20110105491 | THIAZOLIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R | 2011-05-05 |
20110105492 | ARYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease | 2011-05-05 |
20110105493 | HETEROCYCLYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. | 2011-05-05 |
20110105494 | HETEROARYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2A RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. | 2011-05-05 |
20110105495 | CYCLOPENTATHIOPHENE MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF - A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R | 2011-05-05 |
20110105496 | Methods For The Treatment Of Myosin Heavy Chain-Mediated Conditions Using 4,7-Dihydrothieno[2,3-B]Pyridine Compounds - This invention relates generally to methods for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions. | 2011-05-05 |
20110105497 | COMPOUNDS AND METHODS FOR TREATMENT OF CANCER - Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using the compounds together with another chemotherapy, radiation therapy, hormonal therapy, biological therapy, or immunotherapy. Pharmaceutical compositions suitable for use in the methods are also disclosed. | 2011-05-05 |
20110105498 | Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators and methods of use thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 2011-05-05 |
20110105499 | Pyrazolo-Pyrazinone Compounds and Methods of Use Thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 2011-05-05 |
20110105500 | PYRAZINE SUBSTITUTED PURINES - The present invention relates to purine compounds of formula (I) that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumours and cancers as well as other disorders or conditions related to or associated with PI3K and/or mTOR kinases. | 2011-05-05 |
20110105501 | PHARMACEUTICAL COMBINATIONS - The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): | 2011-05-05 |
20110105502 | TETRAHYDROISOQUINOLINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to tetrahydroisoquinoline of the formula (I) | 2011-05-05 |
20110105503 | ARALKYL PIPERIDINE DERIVATIVES AND THEIR USES AS ANTALGIC OR ATARACTIC AGENT - The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects. | 2011-05-05 |
20110105504 | Inhibitors Of 11beta-Hydroxysteroid Dehydrogenase Type 1 - This invention relates to novel compounds of the Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. | 2011-05-05 |
20110105505 | THIAZOLYL PIPERIDINE DERIVATIVES - Compounds of the formula (I), in which R | 2011-05-05 |
20110105506 | Diaminoalkane aspartic protease inhibitors - Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I. | 2011-05-05 |
20110105507 | VINYL ETHER COMPOUNDS AND METHODS OF THEIR PREPARATION AND USE - Provided are new functionalized surfactants and methods of their preparation and use. The surfactants are compounds of formula I: | 2011-05-05 |
20110105508 | QUINOXALINE AND QUINOLINE DERIVATIVES AS KINASE INHIBITORS - A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. | 2011-05-05 |
20110105509 | INDOLE BASED RECEPTOR CRTH2 ANTAGONISTS - Disclosed are compounds of Formula (I): | 2011-05-05 |
20110105510 | PROPHYLACTIC/AMELIORATING OR THERAPEUTIC AGENT FOR NON-ALCOHOLIC STEATOHEPATITIS - Disclosed are: a safe and highly effective prophylactic/ameliorating or therapeutic agent for NASH; and a method for using the agent. The prophylactic/ameliorating or therapeutic agent for NASH comprises a combination of at least one component selected from the group consisting of ω3PUFAs, a pharmaceutically acceptable salt thereof and an ester thereof and a PDE4 inhibitor as active ingredients. | 2011-05-05 |
20110105511 | POLYCYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 2011-05-05 |
20110105512 | BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using the compounds in treating diseases or conditions associated with AxI activity are also disclosed. | 2011-05-05 |
20110105513 | AMINO-QUINOXALINE AND AMINO-QUINOLINE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(═NOH)NH | 2011-05-05 |
20110105514 | 5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE COMPOUNDS - The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I) wherein R | 2011-05-05 |
20110105515 | TARGETING THE ONCOPROTEIN NUCLEOPHOSMIN - (+)-Avrainvillamide, a naturally occurring alkaloid with antiproliferative activity, is shown to bind to the oncoprotein nucleophosmin. Nucleophosmin is known to regulate the tumor suppressor protein p53 and is overexpressed in many different human tumors. The invention provides methods of modulating nucleophosmin and p53 using (+)-avrainvillamide and analogues thereof. These compounds may provide leads for the development of novel anti-cancer therapies that target nucleophosmin. | 2011-05-05 |
20110105516 | POLYMERIZED MICELLES - Polymerised micelles comprising polymerised amphiphilic molecules obtained starting from amphiphilic molecules having one or two lipid chains each comprising one or two polymerisable moieties and linked to a polar head. | 2011-05-05 |
20110105517 | THERAPEUTIC AGENT FOR AMYOTROPHIC LATERAL SCLEROSIS - Disclosed is a safe and effective therapeutic agent that can alleviate the symptoms of the intractable disease ALS and slow the progress thereof. The therapeutic agent for amyotrophic lateral sclerosis contains bromocriptine or a pharmaceutically acceptable salt thereof as the active ingredient. | 2011-05-05 |
20110105518 | THERAPEUTIC AGENT FOR SPINAL CANAL STENOSIS - The main object of the present invention is to provide a novel agent for the treatment of spinal canal stenosis. | 2011-05-05 |
20110105521 | COMBINATION OF (A) A PHOSPHOINOSITIDE 3-KINASE INHIBITOR AND (B) A MODULATOR OF RAS/RAF/MEK PATHWAY - The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human. | 2011-05-05 |
20110105522 | KETOCONAZOLE-DERIVATIVE ANTAGONIST OF HUMAN PREGNANE X RECEPTOR AND USES THEREOF - The application discloses ketoconazole derivatives that are antagonists of the human pregnane X receptor (PXR), methods of preparing the derivatives, uses of the derivatives with drug therapy, and methods of inhibiting tumor cell proliferation and multidrug resistance using inhibitors of PXR. | 2011-05-05 |
20110105523 | BIFEPRUNOX DERIVATIVES - The present invention relates to bifeprunox derivatives of formula (I) wherein R1 is one substituent chosen from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, or a solvate or hydrate of any of the foregoing. The compounds of the invention may be used in the treatment or alleviation of dopamine D | 2011-05-05 |
20110105524 | CYSTEINE PROTEASE INHIBITORS - Compounds of the formula II: | 2011-05-05 |
20110105525 | PHARMACEUTICAL COMPOSITIONS CONTAINING A CRYSTALLINE FORM OF POSACONAZOLE - The present invention relates to a pharmaceutical composition comprising crystalline form Y of posaconazole. The pharmaceutical composition can be used to treat or prevent fungal infections. | 2011-05-05 |
20110105526 | SELECTIVE SUBTYPE ALPHA 2 ADRENERGIC AGENTS AND METHODS FOR USE THEREOF - The invention provides oxazolidine and thiazolidine derivatives that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors. | 2011-05-05 |
20110105528 | 1-(7-(HEXAHYDROPYRROLO [3, 4-C] PYRROL-2 (1H)-YL) QUINOLIN-4-YL) -3- (PYRAZIN-2-YL) UREA DERIVATIVES AND RELATED COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 (GSK-3) - The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. | 2011-05-05 |
20110105529 | ERCC-1 Gene Expression Predicts Chemotherapy Outcome - The invention provides compositions and methods for determining the likelihood of successful treatment with a first line FOLFOX chemotherapy regimen or in further combination with PTK/ZK. The methods comprise determining the gene expression levels of a gene of interest and correlating the high or low expression to the predictive response. Patients identified as responsive are then treated with the appropriate therapy. | 2011-05-05 |
20110105530 | ORGANIC COMPOUNDS - The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed. | 2011-05-05 |
20110105531 | COMPOSITIONS AND METHODS FOR IDENTIFICATION OF SUBSPECIES CHARACTERISTICS OF MYCOBACTERIUM TUBERCULOSIS - The present invention provides compositions, kits and methods for rapid genotyping of strains of | 2011-05-05 |
20110105532 | Haloalkyl-substituted amides as insecticides and acaricides - The present invention relates to halogen-substituted amide derivatives of the general formula (I) | 2011-05-05 |
20110105533 | Heterocyclic Sulfonamides, Uses and Pharmaceutical Compositions Thereof - The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: | 2011-05-05 |
20110105534 | MOLLUSCICIDE - The present invention relates to the use of compounds for the control of gastropods. In particular, it relates to a method of controlling gastropods using strobilurin compounds. | 2011-05-05 |
20110105535 | INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE - Compounds of formula I | 2011-05-05 |
20110105536 | DOSING REGIMEN ASSOCIATED WITH LONG-ACTING INJECTABLE PALIPERIDONE ESTERS - The present application provides a method for treating patients in need of psychiatric treatment, wherein said patient misses a stabilized dose of a monthly maintenance regimen of paliperidone palmitate. The present application also provides a method for treating psychiatric patients in need of a switching treatment to paliperidone palmitate in a sustained release formulation. | 2011-05-05 |
20110105537 | 5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES FOR THE SELECTIVE INHIBITION OF CHEMOKINE RECEPTORS - There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) | 2011-05-05 |
20110105538 | DRUG RESPONSE MARKERS - The present invention relates to a method for predicting the response of a disease in a subject, preferably a human, to a drug providing 6-mercaptopurine, the method comprising the step of: (i) determining the presence or absence of a variant allele at a polymorphic site in a human leucocyte antigen (HLA)-G gene wherein the presence of said variant allele at said polymorphic site is indicative of clinical response or tolerance to said drug. The invention also provides a method of treating a subject suffering from a condition that would benefit from a drug providing 6-mercaptopurine. | 2011-05-05 |
20110105539 | 2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS - A process for obtaining 2′-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2′-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1′-methylbenzimidazole-2-il)benzimidazole to afford 3′-(2′-halo-biphenyl-4-ylmethyl)-1,7′-dimethyl-2′-propyl-1H,3′H-[2,5′]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described. Further described is use of in line analytics for monitoring the aforementioned reactions, process for preparing a pharmaceutical composition and/or dosage for, or use in preparing a medicament. | 2011-05-05 |
20110105540 | 2-AMINO-9-[4-(4-METHOXY-PHENOXY)-PIPERIDIN-1-YL]-4-PHENYL-INDENO[1,2-D]PYR- IMIDIN-5-ONE AND ITS USE AS A HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONIST - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. | 2011-05-05 |
20110105541 | ALKYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. | 2011-05-05 |
20110105542 | PYRAZOLO--QUINAZOLINES - The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C | 2011-05-05 |
20110105543 | NOVEL TRIARYL DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R | 2011-05-05 |
20110105544 | CARBOXYLIC DERIVATIVES FOR USE IN THE TREATMENT OF CANCER - The invention provides novel compounds of formula (I), wherein: R | 2011-05-05 |
20110105545 | GPBP inhibition using Q2 peptidomimetics - Disclosed are compounds of formula: | 2011-05-05 |
20110105546 | SPIROTROPANE COMPOUNDS - Compounds according to formula (I): | 2011-05-05 |
20110105547 | FILAMIN A-BINDING ANTI-INFLAMMATORY ANALGESIC - A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within. | 2011-05-05 |
20110105548 | 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). | 2011-05-05 |
20110105549 | BRANCHED 3- AND 6-SUBSTITUTED QUINOLINES AS CGRP RECEPTORS ANTAGONISTS - The present invention is directed to novel branched 3- and 6-substituted quinoline derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 2011-05-05 |
20110105550 | FORMS OF RIFAXIMIN AND USES THEREOF - The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them. | 2011-05-05 |
20110105551 | Analgesics for nasal administration - An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, C | 2011-05-05 |
20110105552 | BELOXEPIN AND ANALOGS FOR THE TREATMENT OF PAIN - This present disclosure provides methods of treating pain with beloxepin and/or beloxepin analogs. | 2011-05-05 |
20110105553 | NEW CLASSES OF GABAA/BZR LIGANDS - The present invention relates to novel GABA | 2011-05-05 |
20110105554 | MEANS FOR TREATING MYOSIN-RELATED DISEASES - The present invention provides a method of designing a modulator of a myosin, the method comprising molecular modeling of a compound such that the modeled compound interacts with at least three amino acid residues of said myosin, said residues being selected from (a) ranges K265-V268, V411-L441, N588-Q593, D614-T629, and V630-E646 of SEQ ID NO: 2, said myosin comprising or consisting of (i) the sequence of SEQ ID NO: 2; (ii) the sequence encoded by the sequence of SEQ ID NO: 1; (iii) a sequence being at least 40% identical to the sequence of SEQ ID NO: 2 or to the sequence encoded by the sequence of SEQ ID NO: 1; or (iv) a sequence encoded by a sequence being at least 40% identical to the sequence of SEQ ID NO: 1; wherein said sequence of (iii) or (iv) comprises said three amino acid residues, and wherein said residues comprise K265; or (b) ranges of any one of SEQ ID NOs: 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102, 104, 106 or 108, respectively, said ranges aligning with the ranges of SEQ ID NO: 2 as defined in (a), said myosin comprising or consisting of (i) the sequence of any one of SEQ ID NO: 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102, 104, 106 or 108, respectively; (ii) the sequence encoded by the sequence of any one of SEQ ID NO: 3, 5, 7, 9, 11, 13, 15, 17, 19, 21, 23, 25, 27, 29, 31, 33, 35, 37, 39, 41, 43, 45, 47, 49, 51, 53, 55, 57, 59, 61, 63, 65, 67, 69, 71, 73, 75, 77, 79, 81, 83, 85, 87, 89, 91, 93, 95, 97, 99, 101, 103, 105, 107 or 109; respectively; (iii) a sequence being at least 40% identical to the sequence of any one of SEQ ID NO: 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102, 104, 106 or 108, respectively, or to the sequence encoded by the sequence of any one of SEQ ID NO: 3, 5, 7, 9, 11, 13, 15, 17, 19, 21, 23, 25, 27, 29, 31, 33, 35, 37, 39, 41, 43, 45, 47, 49, 51, 53, 55, 57, 59, 61, 63, 65, 67, 69, 71, 73, 75, 77, 79, 81, 83, 85, 87, 89, 91, 93, 95, 97, 99, 101, 103, 105, 107 or 109, respectively; or (iv) a sequence encoded by a sequence being at least 40% identical to the sequence of any one of SEQ ID NO: 3, 5, 7, 9, 11, 13, 15, 17, 19, 21, 23, 25, 27, 29, 31, 33, 35, 37, 39, 41, 43, 45, 47, 49, 51, 53, 55, 57, 59, 61, 63, 65, 67, 69, 71, 73, 75, 77, 79, 81, 83, 85, 87, 89, 91, 93, 95, 97, 99, 101, 103, 105, 107 or 109, respectively; wherein said sequence of (iii) or (iv) comprises said three amino acid residues, and wherein said residues comprise the residue aligning with K265 of SEQ ID NO: 2; thereby obtaining said modulator of a myosin. Furthermore provided are a method of identifying a modulator of a myosin, pharmaceutical compositions and methods of treating cardiovascular diseases, cancer, diseases of the central nervous system, viral infections, and infections by parasites of the Apicomplexa family. | 2011-05-05 |
20110105555 | SUBSTITUTED N-IMIDAZO[2,1-B]THIAZOLE-5-SULFONAMIDE DERIVATIVES AS 5-HT6 LIGANDS - The invention relates to compounds having pharmacological activity towards the 5-HT | 2011-05-05 |
20110105556 | TRIS-QUARTERNARY AMMONIUM SALTS AND METHODS FOR MODULATING NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS - Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders. | 2011-05-05 |
20110105557 | FARNESYL PROTEIN TRANSFERASE INHIBITOR COMBINATIONS WITH ANTIESTROGEN AGENTS - The present invention is concerned with combinations of a farnesyl transferase inhibitor and an antiestrogen agent for inhibiting the growth of tumor cells, useful in the treatment of cancer. | 2011-05-05 |
20110105558 | EYE-DROP PREPARATION AND USE THEREOF - Disclosed is a technique for preventing the decomposition of latanoprost (a thermally unstable substance) contained in an eye-drop solution to stabilize the eye-drop solution. Specifically disclosed is an eye-drop preparation comprising latanoprost and carteolol hydrochloride. By adding carteolol hydrochloride to an eye-drop solution containing latanoprost which is a thermally unstable substance and is likely to be adhered on the surface of a container, it becomes possible to prevent the decomposition of latanoprost in the eye-drop solution and also prevent the loss of latanoprost caused by the adsorption of latanoprost on the surface of a container. | 2011-05-05 |
20110105559 | Compositions and Methods for Treating, Controlling, Reducing, Ameliorating, or Preventing Allergy - A composition for treating, controlling, reducing, ameliorating, or preventing allergy comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an anti-allergic medicament and/or an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. The anti-allergic medicament can comprise an antihistamine, a mast-cell stabilizer, a leukotriene inhibitor, an immunomodulator, an anti-IgE agent, or a combination thereof. | 2011-05-05 |
20110105560 | TREATMENT OF CNS DISORDERS ASSOCIATED WITH MUTATIONS IN GENES ENCODING LYSOSOMAL ENZYMES - Described is a method for treating an individual having a neurological disorder with an associated mutation or mutations in a gene encoding a lysosomal enzyme. Specifically, the individual is administered a specific pharmacological chaperone for the lysosomal enzyme which increases trafficking of the protein from the ER to the lysosome in neural cells, with or without concomitantly increasing enzyme activity in neural cells. Restoration of trafficking relieves cell stress and other toxicities associated with accumulation of mutant proteins. Restoration of enzyme activity relieves substrate accumulation and pathologies associated with lipid accumulation. In a specific embodiment, the neurological disorder is Parkinson's disease or parkinsonism which is associated with mutations in glucocerebrosidase. | 2011-05-05 |
20110105561 | SEROTONIN TRANSPORTER (SERT) INHIBITORS FOR THE TREATMENT OF DEPRESSION AND ANXIETY - The present invention relates to trans-derivatives of formula | 2011-05-05 |
20110105562 | ALKYNYL DERIVATIVES USEFUL AS DPP-1 INHIBITORS - The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1. | 2011-05-05 |
20110105563 | IL-8 RECEPTOR ANTAGONISTS - This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). | 2011-05-05 |
20110105564 | THIENYLPYRIDYLCARBOXAMIDES - Novel thienylpyridylcarboxamides of the formula (I) | 2011-05-05 |
20110105565 | WATER SOLUBLE SMALL MOLECULE INHIBITORS OF THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - Provided herein are highly water soluble, thiazolidinone derivative compounds and glycine hydrazide derivative compounds that inhibit the ion transport activity of the cystic fibrosis transmembrane conductance regulator (CFTR). The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea. The compounds may also be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease. | 2011-05-05 |
20110105566 | FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES - The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 2011-05-05 |
20110105567 | Pyrrole Compounds Having Sphingosine-1-Phosphate Receptor Agonist Or Antagonist Biological Activity - Disclosed herein are compounds represented by: therapeutic methods, compositions, and medicaments related thereto are also disclosed. | 2011-05-05 |
20110105568 | NOVEL METHOD FOR THE PRODUCTION OF SULPHONYLPYRROLES AS HDAC INHIBITORS - Process for the preparation of a compound of formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, comprising the step of reacting an acrylic acid chloride compound of formula (II′): wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, with aqueous hydroxylamine and optionally converting the resulting compound into an acid addition salt thereof. | 2011-05-05 |
20110105569 | PHOSPHODIESESTERASE 4 INHIBITORS FOR THE TREATMENT OF A COGNITIVE DEFICIT - The present invention provides methods of treating cognitive deficits associated with mental retardation. The methods comprise combining cognitive training protocols and a general administration of phosphodiesterase 4 inhibitors. | 2011-05-05 |
20110105570 | PHOSPHODIESESTERASE 4 INHIBITORS FOR THE TREATMENT OF A COGNITIVE DEFICIT - The present invention provides methods of treating cognitive deficits associated with mental retardation. The methods comprise combining cognitive training protocols and a general administration of phosphodiesterase 4 inhibitors. | 2011-05-05 |
20110105572 | CARBAMIC ACID COMPOUNDS COMPRISING AN AMIDE LINKAGE AS HDAC INHIBITORS - This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: | 2011-05-05 |
20110105573 | BENZIMIDAZOLE ACETIC ACIDS EXHIBITING CRTH2 RECEPTOR ANTAGONISM AND USES THEREOF - The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D | 2011-05-05 |
20110105574 | PAI-1 EXPRESSION AND ACTIVITY INHIBITORS FOR THE TREATMENT OF OCULAR DISORDERS - The invention concerns in one embodiment a method for treating glaucoma or elevated IOP in a patient comprising administering to the patient an effective amount of a composition comprising an agent that inhibits PAI-1 expression or PAI-1 activity. Another embodiment of the present invention is a method of treating a PAI-1-associated ocular disorder in a subject in need, comprising administering to the patient an effective amount of a composition comprising an agent that inhibits PAI-1 activity or expression. | 2011-05-05 |
20110105575 | METHOD OF TREATMENT OF HEREDITARY HEMOCHROMATOSIS - The present invention relates to the use of Compound I of the following formula | 2011-05-05 |
20110105576 | PESTICIDAL COMBINATIONS - A method of controlling or preventing pathogenic damage and/or pest damage in a plant propagation material, a plant, part of a plant and/or plant organ that grow at a later point in time, which comprises applying on the plant, part of the plant, plant organ, plant propagation material or a surrounding area thereof a combination comprising (I) prochloraz, (II) metconazole, and optionally (III) metalaxyl or mefenoxam. | 2011-05-05 |
20110105577 | Method For Reducing Mycotoxin Contamination In Maize - The present application relates to a method for the reduction of mycotoxin contamination of maize or corn plants and/or plant material from maize or corn before and/or after harvest and/or during storage, in particular genetically modified maize or corn by the use of one or a combination of two or more fungicidally active compounds. | 2011-05-05 |
20110105578 | Substituted Imidazole Derivatives And Methods Of Use Thereof - The present invention provides imidazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof. | 2011-05-05 |
20110105579 | Plant Health Composition - The present invention relates to a method for improving the plant health of at least one plant variety, which method comprises treating the plant propagules with an amide compound having the formula I (compound I). The present invention also N relates to a method for improving the plant health of at least one plant variety, which method comprises treating the plant propagules with a mixture comprising an amide compound having the formula I (compound I) and at least one compound selected from the group consisting of a further fungicide Il (compound II), a further fungicide III (compound lib) and an insecticide III (compound III). | 2011-05-05 |
20110105580 | NOVEL POLYMORPHIC FORMS OF SUNITINIB BASE - The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals. | 2011-05-05 |
20110105581 | OPHTHALMIC FORMULATIONS CONTAINING SUBSTITUTED GAMMA LACTAMS AND METHODS FOR USE THEREOF - The invention provides ophthalmic formulations containing well-defined substituted gamma lactams. The formulations described herein are useful in treating a variety of ocular diseases related to ocular hypertension, such as for example, glaucoma. | 2011-05-05 |
20110105582 | Composition for inhibiting function of human flt3 - To provide a means of controlling the function of Flt3. A composition for inhibiting the function of human Flt3, a method of inducing apoptosis by using the composition, and a kit for the method. | 2011-05-05 |
20110105583 | METHODS OF USING MIR34 AS A BIOMARKER FOR TP53 FUNCTIONAL STATUS - In one aspect, the invention generally relates to use of miR-34 as a biomarker to estimate TP53 function in a cell. In another aspect, the invention generally relates to multiple uses of miR-34 and siRNAs functionally and structurally related to miR-34 for the treatment of cancer. | 2011-05-05 |
20110105584 | RTP80IL SIRNA COMPOUNDS AND METHODS OF USE THEREOF - The invention provides chemically modified siRNA oligonucleotides that target RTP801L, compositions comprising same and to the use of such molecules to treat, inter alia, respiratory diseases including acute and chronic pulmonary disorders, eye diseases including glaucoma and ION, microvascular disorders, angiogenesis- and apoptosis-related conditions, and hearing impairments. | 2011-05-05 |
20110105585 | METHODS FOR DIAGNOSING AND TREATING SQUAMOUS CELL CARCINOMA UTILIZING miRNA-205 AND INHIBITORS THEREOF - Disclosed are diagnostic and therapeutic methods related to squamous cell carcinoma. In particular, the diagnostic methods relate to detecting miRNA-205, thereby diagnosing an aggressive form of squamous cell carcinoma. The therapeutic methods relate to inhibiting the function of miRNA-205, thereby treating an aggressive form of squamous cell carcinoma. | 2011-05-05 |
20110105586 | COMPOSITIONS AND THEIR USES DIRECTED TO GEMIN GENES - Disclosed herein are compounds, compositions and methods for modulating the expression of a Gemin Gene. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders. | 2011-05-05 |
20110105587 | TARGET SEQUENCES AND METHODS TO IDENTIFY THE SAME, USEFUL IN TREATMENT OF NEURODEGENERATIVE DISEASES - The present invention relates to methods and assays for identifying agents capable of inhibiting the mutant huntingtin protein, inhibiting or reducing cell death, in particular cell death associated with polyglutamine-induced protein aggregation, which inhibition is useful in the prevention, amelioration and/or treatment of neurodegenerative diseases, and Huntington's disease more generally. In particular, the present invention provides methods and assays for identifying agents for use in the prevention and/or treatment of Huntingtons disease. The invention provides polypeptide and nucleic acid TARGETs and siRNA sequences based on these TARGETS. | 2011-05-05 |