C=x Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding (x Is Chalcogen) Patents (Class 514/423)
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Publication number: 20110265786Abstract: The present invention is directed to an inhalable formulation for the treatment of pulmonary hypertension in a mammal (e.g., humans), wherein the formulation comprises at least one hypertension reducing agent, including but not limited to an angiotensin converting enzyme inhibitor, angiotensin receptor blocker, beta-blocker, calcium-channel blocker or vasodilator, or any combination thereof. The formulations of the present invention may be a solution or suspension, and preferably are suitable for administration via nebulization. The present invention is also directed to a method and kit for treating a mammal suffering from pulmonary hypertension.Type: ApplicationFiled: February 3, 2011Publication date: November 3, 2011Inventor: Imtiaz Chaudry
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Publication number: 20110269723Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.Type: ApplicationFiled: July 12, 2011Publication date: November 3, 2011Applicant: Taro Pharmaceuticals U.S.A., Inc.Inventors: Satish ASOTRA, Xiaoli Wang, Zoltan Bodor
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Patent number: 8048909Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug theType: GrantFiled: September 30, 2005Date of Patent: November 1, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Terufumi Takagi
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Patent number: 8048910Abstract: Novel combinations based on anticholinergics, ?2-adrenoceptor agonists, PDE 4 Inhibitors, glucocorticoids, and leukotriene-receptor antagonists, process for their production and their use for the treatment of inflammatory diseases, preferably respiratory diseases as bronchial asthma and chronic obstructive pulmonary diseases (COPD) or rheumatic or autoimmune diseases. A particular combination comprises R,R-glycopyrrolate, rolipram, and budesonide, or physiologically acceptable salts thereof, wherein dosage amounts are such that a synergistic therapeutic effect is achieved.Type: GrantFiled: December 21, 2006Date of Patent: November 1, 2011Assignee: Meda Pharma GmbH & Co. KGInventors: Joachim Maus, Horst Kastrup, Istvan Szelenyi, Peter Jürgen Cnota, Artur Bauhofer
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Patent number: 8048907Abstract: The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.Type: GrantFiled: February 18, 2010Date of Patent: November 1, 2011Assignee: Glaxo Group LimitedInventors: Laura J Chambers, Robert Gleave, Stefan Senger, Daryl Simon Walter
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Patent number: 8048880Abstract: Administration of sPLA2 inhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLA2 inhibitors was found to decrease cholesterol levels even when the inhibitors were administered only once per day. Therefore, provided herein are methods of treating dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome, by administering one or more sPLA2 inhibitors. Significantly, administration of sPLA2 inhibitors and various compounds used in the treatment of CVD, such as for example statins, resulted in greater decreases in LDL and LDL particle levels in a synergistic manner. In addition, administration of sPLA2 inhibitors and statins resulted in a synergistic decrease in plaque content.Type: GrantFiled: May 2, 2008Date of Patent: November 1, 2011Assignee: Anthera Pharmaceuticals, Inc.Inventors: Joaquim Trias, Colin Hislop, Paul Truex, Bernadine Fraser, Debra Odink, Scott Chadwick, Kenneth Gould, Marian Mosior, Patrick Eacho
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Publication number: 20110263540Abstract: Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin.Type: ApplicationFiled: July 24, 2009Publication date: October 27, 2011Inventors: Yuan-Ping Pang, Nilgun Ereken Tumer, Charles B. Millard
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Publication number: 20110263478Abstract: Methods and compositions are provided that are utilized for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN). In particular, the methods and compositions are inhibitors of a particular NCca-ATP channel and include, for example, inhibitors of SUR1 and/or inhibitors of TRPM4. Kits for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury, are also provided. The present invention also concerns treatment and/or prevention of intraventricular hemorrhage in infants, including premature infants utilizing one or more inhibitors of the channel is provided to the infant, for example to brain cells of the infant.Type: ApplicationFiled: September 16, 2009Publication date: October 27, 2011Inventor: J. Marc Simard
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Publication number: 20110263674Abstract: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.Type: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Inventor: S. Bruce King
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Publication number: 20110263673Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy-C4-C6 alkyl group; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like; R5 represents a C1-C3 alkyl group; and R6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.Type: ApplicationFiled: October 7, 2009Publication date: October 27, 2011Applicants: DAIICHI SANKYO COMPANY, LIMITED, EXELIXIS, INC.Inventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Kazumasa Aoki, Hiroyuki Tsuruoka, Noriyuki Hayashi, Tsuyoshi Homma
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Publication number: 20110263544Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a hydroxy-C1-C4 alkyl group and the like; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like, —R5 represents a sulfamoyl group or a C1-C3 alkylsulfonyl group; R6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.Type: ApplicationFiled: October 7, 2009Publication date: October 27, 2011Applicants: DAIICHI SANKYO COMPANY, LIMITED, EXELIXIS, INC.Inventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Hiroyuki Tsuruoka, Kazumasa Aoki, Masatoshi Honzumi, Yusuke Asoh, Keiji Saito, Tsuyoshi Homma
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Publication number: 20110263526Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.Type: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventor: Apparao SATYAM
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Publication number: 20110263604Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.Type: ApplicationFiled: April 18, 2011Publication date: October 27, 2011Applicant: Oryzon Genomics, S.A.Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
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Patent number: 8044086Abstract: The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.Type: GrantFiled: July 15, 2005Date of Patent: October 25, 2011Assignee: Lek Pharmaceuticals D.D.Inventors: Rok Grahek, Darko Kocjan, Andrej Bastarda, Andrej Kocijan, Matjaz Kracun
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Patent number: 8043422Abstract: The present invention relates to combinations of a phenylpyrrole, or a salt thereof, and a pyrion compound which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of a phenylpyrrole selected from fludioxonil, fenpiclonil or pyrrolnitrin, or a salt thereof, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox, pyrion disulfide, sodium pyrithione and zinc pyrithione; in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like.Type: GrantFiled: February 5, 2009Date of Patent: October 25, 2011Assignee: Janssen Pharmaceutica, NVInventors: Jan Pieter Hendrik Bosselaers, Dany Leopold Jozefien Bylemans, Tony Mathilde Jozef Kempen, Hans Bernhard Leithoff, Amber Paula Marcella Thys, Mark Arthur Josepha Van Der Flaas
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Publication number: 20110257149Abstract: The invention relates to a formulation for delivering by oral transmucosal administration at least one lipid-lowering active principle, preferably from the statin family, said formulation including said active principle in the base or salt form, an aqueous alcohol solution titrating at least 30° alcohol, and optionally a pH correcting agent and/or an antioxidant, said active principle being in a stable and completely dissolved state in the aqueous alcohol solution. The invention also relates to a method of preparing said formulation and to the use thereof, preferably in single-dose packaging, for treating and preventing hyperlipemia and/or cardiovascular conditions.Type: ApplicationFiled: December 17, 2009Publication date: October 20, 2011Inventors: Philippe Perovitch, Marc Maury
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Publication number: 20110257240Abstract: The present invention is directed to statin formulations having improved solubility and/or stability and methods for the same.Type: ApplicationFiled: April 16, 2010Publication date: October 20, 2011Applicant: Cumberland Pharmaceuticals Inc.Inventors: Leo Pavliv, Andrew Vila
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Publication number: 20110257182Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: June 25, 2011Publication date: October 20, 2011Inventor: Christelle Bolea
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Publication number: 20110257130Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.Type: ApplicationFiled: October 16, 2009Publication date: October 20, 2011Inventor: Desikan Rajagopal
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Publication number: 20110257164Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.Type: ApplicationFiled: January 7, 2010Publication date: October 20, 2011Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
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Patent number: 8039507Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: June 6, 2006Date of Patent: October 18, 2011Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 8039495Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: October 15, 2010Date of Patent: October 18, 2011Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110251162Abstract: The present subject matter relates to pathogenesis of MRSA. Specifically, the present disclosures identifies the pro-inflammatory properties of PVL as the cause of MRSA. Viewed from this new perspective, the present subject matter achieves novel methods and apparatus for treating MRSA infection in a subject involving the administration of an anti-inflammatory drug to the subject. Furthermore the present subject matter teaches methods and apparatus for treating a Panton-Valetine leukocidin associated infection in a subject involving the administration of an anti-inflammatory drug to the subject.Type: ApplicationFiled: September 25, 2009Publication date: October 13, 2011Applicant: CEDARS-SINAI MEDICAL CENTERInventors: George Y. Liu, Ching Wen Tseng
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Publication number: 20110250197Abstract: This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof.Type: ApplicationFiled: June 1, 2011Publication date: October 13, 2011Applicant: RANBAXY LABORATORIESInventors: Jitendra A. SATTIGERI, Vinay S. BANSAL
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Publication number: 20110245250Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar1 and Ar2 are aryl or heteroaryl; a is 0 to 5; R1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R1 may be the same or different; b is 0 to 5; R2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R2 may be the same or different; V is selected from the group consisting of (CR3aR3b)pCON(R3b)X and (CR3aR3b)pN(R3b)CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X is hydrogeType: ApplicationFiled: July 20, 2009Publication date: October 6, 2011Applicant: Ramot at tel-Aviv University Ltd.Inventors: Simon David Edwards, Meriel Ruth Kimberley, Richard Edward Armer, Nawaz Mohammed Khan
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Publication number: 20110245283Abstract: The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.Type: ApplicationFiled: December 21, 2010Publication date: October 6, 2011Inventor: Glen H. Murata
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Publication number: 20110240504Abstract: A method of packaging one or more pharmaceuticals comprising separating a plurality of unit doses into a plurality of unit dose compartments, wherein each unit dose compartment of the plurality of unit dose compartments holds only one unit dose of the plurality of unit doses, each unit dose having the same strength, wherein the plurality of unit doses is precisely a quantity equal to a most commonly prescribed number of unit doses in individual prescriptions for the unit dose, or a multiple thereof is provided. Also provided are kits prepared by the method. Methods for designing such kits and packaging are also provided.Type: ApplicationFiled: December 3, 2009Publication date: October 6, 2011Applicant: APOTEX TECHNOLOGIES INC.Inventors: Arturo Tramonte, Maria L. Tagliabracci, Ryan W. Unwin
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Publication number: 20110245188Abstract: The present invention relates to methods and compositions of treating or preventing inflammatory diseases or conditions in a patient comprising administering to the patient a therapeutically effective amount of a composition comprising a glutathione donor, 5-amino 4-imidazolecarboxamide ribotide (AICAR), a 3-hydroxy-3-methylgluatryl-coenzymeA (HMG-CoA) reductase inhibitor, D-threo-1-Phenyl-2-decanoylamino-3-morpholino-1-propanol HCl (D-PDMP), and/or 1,5-(butylimino)-1,5-dideoxy-D-glucitol (Miglustat), or derivatives thereof.Type: ApplicationFiled: March 25, 2011Publication date: October 6, 2011Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventor: Inderjit Singh
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Publication number: 20110245317Abstract: This application is directed to methods for improving glucose control by administering metformin in combination with a DPP-IV inhibitor to a patient in need thereof, in an amount sufficient to control the glucose level over an extended period of time.Type: ApplicationFiled: April 11, 2011Publication date: October 6, 2011Inventor: Thomas Edward HUGHES
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Publication number: 20110244045Abstract: The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.Type: ApplicationFiled: May 11, 2009Publication date: October 6, 2011Applicant: TIARA PHARMACEUTICALS ,INC.Inventors: Yadon Arad, Liang C. Dong
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Publication number: 20110244016Abstract: One embodiment of the invention relates to a medical implant whose surface is completely or partially covered by a coating composed of at least one active substance or containing at least one active substance.Type: ApplicationFiled: March 24, 2011Publication date: October 6, 2011Inventors: Matthias Gratz, Alexander Borck, Kathleen Koeck
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Patent number: 8030489Abstract: Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.Type: GrantFiled: March 25, 2008Date of Patent: October 4, 2011Assignee: Astellas Pharma Inc.Inventors: Tatsuya Zenkoh, Eisuke Nozawa, Keisuke Matsuura, Ryushi Seo
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Patent number: 8030341Abstract: The present invention relates to symmetric and asymmetric dimeric Dmt (2?,6?-ditnethyl) compounds and Dmt derivative compounds with dual ? and ? opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.Type: GrantFiled: August 30, 2006Date of Patent: October 4, 2011Assignees: The United States of America as represented by the Secretary of the Department of Health and Human Services, Kobe Gakuin UniversityInventors: Lawrence H. Lazarus, Yoshio Okada, Tingyou Li
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Publication number: 20110236479Abstract: Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.Type: ApplicationFiled: June 6, 2011Publication date: September 29, 2011Inventors: James Kowalski, Jay Parthiban Lakshman, Arun P. Patel
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Publication number: 20110237537Abstract: Described herein are assays, kits and methods for treating mood disorders by testing for one or more polymorphisms in a specific group of genes and for analyzing the results of polymorphism testing; the genes included may converge in one or more signaling pathways, and may be epigenetic. The genes are included based on the relationships of the proteins encoded by the genes in the context of particular signaling pathways and provide a diagnostically relevant nexus. Also described herein are methods of presenting the data collected by the screen, including methods of delivering interpretive comments and/or treatment guidance based on the results of the genetic screening either individually or based on the genetic composition of particular clusters of genes which may be related to each other. Importantly, drugs which modulate these genetic disturbances are described for targeted therapeutic use based upon companion diagnostic method.Type: ApplicationFiled: March 29, 2011Publication date: September 29, 2011Inventor: Jay L. Lombard
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Publication number: 20110237525Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.Type: ApplicationFiled: June 18, 2010Publication date: September 29, 2011Inventors: Boyd E. Haley, Niladri Narayan Gupta
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Publication number: 20110237642Abstract: A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solutilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.Type: ApplicationFiled: April 4, 2011Publication date: September 29, 2011Inventors: Antone J. deBettencourt, III, Peter R. Rose, Evgenyi Shalaev, George J. Quallich, Carl B. Ziegler, JR.
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Publication number: 20110236461Abstract: The invention is directed to a method for stimulating chondrogenesis comprising administering to a subject in need thereof a composition comprising a therapeutically effective amount of a potassium channel inhibitor.Type: ApplicationFiled: August 12, 2009Publication date: September 29, 2011Inventor: T. Michael Underhill
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Publication number: 20110237592Abstract: The present invention relates to substituted amido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: October 29, 2009Publication date: September 29, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ingo Hartung, Marion Hitchcock, Knut Eis, Florian Puhler
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Patent number: 8026237Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.Type: GrantFiled: July 30, 2005Date of Patent: September 27, 2011Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B Mac, Larry W Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C Stevens, Tie-Lin Wang, Yong Wang, Jason H Wu
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Patent number: 8026258Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.Type: GrantFiled: January 21, 2010Date of Patent: September 27, 2011Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Jacques Froissant, Christian Hoornaert
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Patent number: 8026272Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.Type: GrantFiled: October 30, 2009Date of Patent: September 27, 2011Assignee: Zealand Pharma A/SInventors: Bjarne Due Larsen, Jørgen Søberg Petersen, Ketil Jørgen Haugan, John A. Butera, James K. Hennan, Edward H. Kerns, Evgueni Lvovich Piatnitski
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Publication number: 20110230437Abstract: A composition comprising a compound of formula I CH3CH(OH)CC?O)NR1R2 (I) where R1 and R2 are each independently hydrogen; or C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl, each of which is optionally substituted by up to three substituents independently selected from phenyl, hydroxy, C1-5 alkoxy, morpholinyl and NR3R4 where R3 and R4 are each independently C1-3 alkyl; or phenyl optionally substituted by up to three substituents independently selected from C1-3 alkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl, pyrrolidinyl, piperidinyl or azepanyl ring, each of which is optionally substituted by up to three substituents independently selected from C1-3 alkyl; and at least one agrochemical selected from Othe group consisting of Tri nexepac ethyl, Mandipropamid, Abamcctin and Emamectin, with the proviso that the agrochemical is not abamectin or emamectin when the solvent is N-(B-hydroxyethyl)-lactamide.Type: ApplicationFiled: August 12, 2008Publication date: September 22, 2011Applicant: SYNGENTA LIMITEDInventors: Gordon Alastair Bell, Clair Louise Harris, Ian David Tovey
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Publication number: 20110230539Abstract: Compounds having a structure of Formula (A) are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are provided. Uses of compounds having a structure of Formula (F) for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.Type: ApplicationFiled: August 24, 2009Publication date: September 22, 2011Inventors: Marianne D. Sadar, Nasrin R. Mawji, Jun Wang, Raymond J. Andersen, David E. Williams, Mike Leblanc, Lu-Ping Yan
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Patent number: 8022032Abstract: The method set out herein involves identifying the concentration of each of two or more active therapeutics tailored to treat a particular patient's unique metabolism and one or more diseases, communicating that information to a producer who has multiple fixed or variable concentrations of each active available, where the producer then combines the individual concentrations of each active into single units such as a tablets or pills, and distributes those indirectly or directly to the patient.Type: GrantFiled: November 18, 2005Date of Patent: September 20, 2011Assignee: SmithKline Beecham CorporationInventors: Richard L. Kirsh, Steven D. Finkelmeier, Robert Glinecke, Luigi Martini
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Patent number: 8017647Abstract: Crystalline sodium atorvastatin, compositions containing the same and methods for the production thereof.Type: GrantFiled: August 15, 2006Date of Patent: September 13, 2011Assignees: Arrow International Limited, Zhejiang Neo-Dankong Pharmaceutical Co. Ltd.Inventors: Kailan Zhou, Hong Liu, Zhirong Chen, Huabin Hong, Yang Sun, Yunde Wang, Jiangchun Pan
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Patent number: 8017607Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: GrantFiled: October 6, 2010Date of Patent: September 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Patent number: 8017633Abstract: The invention relates to the use of Roflumilast and/or Roflumilast N-Oxide for the treatment of diabetes mellitus and accompanying disorders thereof. The invention additionally relates to combinations of Roflumilast and/or Roflumilast N-Oxide with other active agents for the treatment of diabetes mellitus.Type: GrantFiled: March 3, 2006Date of Patent: September 13, 2011Assignee: Nycomed GmbHInventors: Hans-Peter Kley, Guido Hanauer, Daniela Hauser, Beate Schmidt, Dirk Bredenbroeker, Wilhelm Wurst, Joerg Kemkowski
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Publication number: 20110217374Abstract: Disclosed is a pharmaceutical composition simultaneously having a rapid acting property and a long-acting property, comprising a sustained-release part coated with a water-insoluble polymer on the surface, comprising a first active pharmaceutical ingredient, at least one release control base selected from the group consisting of water-insoluble polymer, and water-soluble viscous polymer, and a pharmaceutically acceptable carrier; and, an immediate release part comprising a second active pharmaceutical ingredient and a pharmaceutically acceptable carrier.Type: ApplicationFiled: May 16, 2011Publication date: September 8, 2011Applicant: YUNGJIN PHARM. CO., LTD.Inventors: Dong-Joon OH, Byoung-Ki Kim, Byung-Kwan Moon, Ji-Seok Yoo, Dae-Hee Shin, Byung-Hwan Ryoo