The Additional Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/319)
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Publication number: 20140243278Abstract: Disclosed is an acid addition salt of donepezil, wherein acid counterion is selected from the group consisting of pamoic acid, cypionic acid, camphor sulfonic acid, enanthic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, valeric acid, Dibenzoyl-D-Tartaric acid and terephthalic acid. Disclosed is a process for the preparation and pharmaceutical composition comprising the same. More specifically, disclosed is concerned with the pamoate acid addition salts of donepezil. Disclosed also is long acting formulation comprising the acid addition salt of donepezil and process for the preparation thereof.Type: ApplicationFiled: July 3, 2012Publication date: August 28, 2014Inventors: Sunil Sadanand Nadkarni, Arunkumar Gupta, Jaya Abraham, Manish Parikh, Mahesh Suthar, Bipin Manavadariya, Vivek Mishra
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Publication number: 20140243334Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20140243335Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
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Publication number: 20140235628Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: September 10, 2012Publication date: August 21, 2014Inventors: Shawn Walsh, Alexander Pasternak, Brian Cato, Paul E. Finke, Jessica Frie, Qinghong Fu, Dooseop Kim, Barbara Pio, Aurash Shahripour, Zhi-Cai Shi, Haifeng Tang
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Publication number: 20140235641Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 21, 2014Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
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Patent number: 8809381Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: GrantFiled: August 18, 2008Date of Patent: August 19, 2014Assignees: The University of Mississippi, L'Universite Catholique de LouvainInventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
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Publication number: 20140228375Abstract: The present invention involves new and original sigma receptors ligands: (Mono-or dialkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.Type: ApplicationFiled: March 12, 2014Publication date: August 14, 2014Applicant: Anavex Life Sciences Corp.Inventor: Alexandre Vamvakides
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Patent number: 8802659Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: GrantFiled: August 5, 2010Date of Patent: August 12, 2014Assignee: Biogen Idec MA Inc.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20140142140Abstract: An anti-epileptic agent for use in the treatment of a neurological disorder other than epilepsy characterised in that the anti-epileptic agent is the sole active agent and that the daily dose of the anti-epileptic is less than 20% of the minimum daily dose which is effective for mood stabilisation or treatment of epileptic symptoms.Type: ApplicationFiled: July 9, 2012Publication date: May 22, 2014Applicant: GOSFORTH CENTRE (HOLDINGS) PTY LTDInventor: Philip Bird
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Publication number: 20140141059Abstract: Provided is a patch that ensures high storage stability of donepezil or a salt thereof and allows stable transdermal administration of the donepezil or salt thereof in an amount that provides a pharmaceutical effect. The patch includes a substrate 1 and an adhesive layer 2 stacked on and integrated with one surface of the substrate 1 and containing donepezil or a salt thereof and an acrylic adhesive containing a copolymer obtained by copolymerizing monomers that each contain a (meth)acrylic acid ester of a saturated aliphatic alcohol and do not contain vinylpyrrolidone.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: SEKISUI MEDICAL CO., LTD.Inventors: Toshikazu KOMODA, Yukihiko NODA
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Patent number: 8729092Abstract: The invention discloses a method for the treatment of diseases, particularly those diseases characterized by diminished or aberrant cellular function, including AIDS, cancer, and Alzheimer's Disease. The method comprises administering a therapeutically effective amount of rosuvastatin enantiomer compounds in their (3R,5R), (3S,5R), or (3S,5S) configurations, or pharmaceutically acceptable salts thereof. Biologically-active rosuvastatin enantiomer compounds with (3R,5R), (3S,5R), and (3S,5S) stereochemistry are also disclosed.Type: GrantFiled: September 24, 2012Date of Patent: May 20, 2014Inventor: Terence J. Scallen
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Publication number: 20140134243Abstract: The invention provides methods for treating CNS-related conditions with amantadine and donepezil, in which the amantadine is in an extended release form, wherein the extended release amantadine formulation provides a change in plasma concentration as a function of time (dC/dT) that is less than 40% of the dC/dT of the same quantity of an immediate release form of amantadine.Type: ApplicationFiled: April 15, 2013Publication date: May 15, 2014Inventors: Gregory T. Went, Timothy J. Fultz, Laurence R. Meyerson
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Patent number: 8722722Abstract: The present invention includes new salts of Raltegravir and crystalline forms thereof, pharmaceutical compositions containing the salts or crystalline forms, methods of using the salts or crystalline forms or the compositions to treat HIV infection or to prepare medicament for treating HIV infection, and a process for preparing Raltegravir potassium.Type: GrantFiled: December 7, 2012Date of Patent: May 13, 2014Assignee: Teva Pharmaceutical Industries LtdInventors: Ana Kwokal, Lilach Hedvati, Revital Burstein, Adi Yeori, Rinat Moshkovits-Kaptsan
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Publication number: 20140121193Abstract: The invention provides methods for treating or ameliorating cognitive dysfunction, fatigue, energy, concentration, mood, and pain associated with fibromyalgia using compositions containing methylphenidate or pharmaceutically equivalents thereof.Type: ApplicationFiled: November 1, 2013Publication date: May 1, 2014Inventors: Robert S. KATZ, Frank LEAVITT
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Publication number: 20140121210Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.Type: ApplicationFiled: January 8, 2014Publication date: May 1, 2014Applicant: HELSINN HEALTHCARE SAInventors: Silvina GARCIA RUBIO, Claudio PIETRA, Claudio GIULIANO, Zhigang LI
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Patent number: 8703957Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.Type: GrantFiled: June 19, 2013Date of Patent: April 22, 2014Assignee: Janssen Pharmaceutica NVInventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
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Patent number: 8703721Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 12, 2011Date of Patent: April 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20140099366Abstract: An object of the present invention is to provide, for the case of implementing a therapeutic method in which at least two kinds of anti-dementia drugs are used together, a composition that has a good therapeutic effect on dementia, and also gives excellent compliance. Another object of the present invention is to provide a composition containing at least two kinds of anti-dementia drugs, in which release of the anti-dementia drugs from the composition is controlled, whereby a combined effect of the anti-dementia drugs can be achieved well. Still another object of the present invention is to provide a composition for which the frequency of administration and the amount taken are reduced and hence compliance can be improved, and a method of manufacturing such a composition.Type: ApplicationFiled: December 13, 2013Publication date: April 10, 2014Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Susumu Kimura, Yosuke Ueki, Masami Nohara, Yukifumi Dota
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Publication number: 20140100218Abstract: The present invention relates to methods of treatment using [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl amine (“COMPOUND I”) or a pharmaceutically acceptable salt thereof. In various embodiments, the methods of treatment include treatment of mild-to-moderate dementia of Alzheimer's type, diabetes, insomnia, and other indications. The present invention also relates to pharmaceutical compositions comprising COMPOUND I or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 22, 2013Publication date: April 10, 2014Applicant: TransTech Pharma, LLCInventors: Cesare Orlandi, David J. Clark, Imogene M. Grimes, Maria Carmen Valcarce Lopez, Matthew J. Kostura
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Patent number: 8691993Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: December 6, 2012Date of Patent: April 8, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Fariborz Firooznia, Tai-An Lin, Eric Mertz, Achyutharao Sidduri, Sung-Sau So, Jefferson Wright Tilley
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Publication number: 20140094492Abstract: Derivatives of sulindac that lack cyclooxygenase inhibitory activity are provided along with pharmaceutical compositions containing them and use for treatment or prevention of cancer. The derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: ApplicationFiled: March 30, 2012Publication date: April 3, 2014Applicant: Southern Research InstituteInventors: Robert Reynolds, Bini Mathew, Gary A. Piazza
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Publication number: 20140094464Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.Type: ApplicationFiled: May 25, 2012Publication date: April 3, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Mark R. Kelley, James H. Wikel
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Publication number: 20140086910Abstract: The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of Alzheimer's diseases.Type: ApplicationFiled: August 29, 2013Publication date: March 27, 2014Applicant: DARA BIOSCIENCES, INC.Inventor: Mary Katherine Delmedico
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Publication number: 20140080811Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.Type: ApplicationFiled: February 27, 2013Publication date: March 20, 2014Applicant: Remedy Pharmaceuticals, Inc.Inventor: Remedy Pharmaceuticals, Inc.
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Patent number: 8669275Abstract: The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: October 3, 2012Date of Patent: March 11, 2014Assignee: DeuteRx, LLCInventor: Anthony W. Czarnik
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Publication number: 20140051702Abstract: The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient.Type: ApplicationFiled: August 15, 2013Publication date: February 20, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Sandeep Gupta, Tony Priestley, Nicholas James Laping
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Publication number: 20140052081Abstract: The present invention relates to a donepezil transdermal patch comprising a backing layer and a pressure sensitive adhesive matrix layer, wherein the pressure sensitive adhesive matrix layer comprises donepezil free base and an acrylic pressure sensitive adhesive agent selected from the group consisting of a copolymer of 2-ethylhexyl acrylate and vinyl acetate and a copolymer of 2-ethylhexyl acrylate, vinyl acetate, and hydroxyl-containing monomers, and wherein 2-ethylhexyl acrylate is present in an amount of about 65% to about 75%, vinyl acetate is present in an amount of about 25% to about 35%, and the hydroxyl-containing monomers are in an amount of about 0% to about 10%, based on the total weight of the copolymer.Type: ApplicationFiled: January 12, 2012Publication date: February 20, 2014Applicant: TAIWAN BIOTECH CO. LTD.Inventors: Kuo-Hua Yang, Chih-Sheng Yang, Hsuen-Yau Lin
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Publication number: 20140031341Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.Type: ApplicationFiled: December 19, 2011Publication date: January 30, 2014Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENTInventors: Jerome Aubert, Martin Steinhoff
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Patent number: 8623875Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.Type: GrantFiled: June 10, 2008Date of Patent: January 7, 2014Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Ty Wagerle, Ming Xu
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Patent number: 8618136Abstract: Methods of treating, preventing and/or managing a myeloproliferative disease are disclosed. Specific methods encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent, and/or the transplantation of blood or cells. Particular second active agents are capable of suppressing the overproduction of hematopoietic stem cells or ameliorating one or more of the symptoms of a myeloproliferative disease. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: March 8, 2006Date of Patent: December 31, 2013Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 8618133Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereof. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.Type: GrantFiled: June 8, 2009Date of Patent: December 31, 2013Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.Inventors: Jianqi Li, Kai Gao, Wangping Cai, Yongyong Zheng
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Publication number: 20130337021Abstract: The present invention relates to a percutaneous absorption preparation that is lower skin irritation and enables efficient transdermal administration of an anti-dementia drug. More specifically, the present invention relates to a percutaneous absorption preparation comprising an anti-dementia drug, a polymer compound having an amino group, a polyvalent carboxylate ester, a fatty acid alkyl ester, a styrenic polymer compound, and a tackifier resin.Type: ApplicationFiled: August 22, 2013Publication date: December 19, 2013Inventor: Takeshi Goto
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Publication number: 20130324576Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which m, n, W, X, Y, Z, R, R1, R2, R3 and R4 are as defined in the specification, for use in therapy.Type: ApplicationFiled: May 29, 2013Publication date: December 5, 2013Inventors: Colm Carroll, Anne Goldby, Martin Teall
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Patent number: 8598217Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: GrantFiled: April 30, 2010Date of Patent: December 3, 2013Assignees: Astex Therapeutics Ltd., Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
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Patent number: 8597666Abstract: A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about 25 weight percent. A manufacturing method may include blending the active compound and starch, compressing the blend into a solid, comminuting the solid into granules, wetting the granules, drying the granules, and tabletting the dried granules to make a solid pharmaceutical formulation.Type: GrantFiled: October 28, 2011Date of Patent: December 3, 2013Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Ilan Zalit, Fanny Leska, Mali Kadosh, Dorit Marco, Yonit Messer-Triger
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Publication number: 20130309297Abstract: A liposome composition, which is obtained by mixing a water-miscible organic solution in which a phospholipid and cholesterol are contained in a total concentration of 100 to 200 w/v % in a water-miscible organic solvent with a first aqueous phase solution in an amount of 3/1 to 12/1 in terms of volume ratio to the water-miscible organic solution, thereby obtaining an emulsion in which the total concentration of the phospholipid and cholesterol in the resulting mixed phase is 15 to 50 w/v %, followed by subjecting the emulsion to external solution exchange with a second aqueous phase solution, wherein an ion gradient is formed between an aqueous phase in an internal region of a liposome membrane, including the first aqueous phase solution, and an aqueous phase in an external region of the liposome membrane, including the second aqueous phase solution, and a drug can be introduced in a high encapsulation amount.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: TERUMO KABUSHIKI KAISHAInventors: Keiko YAMASHITA, Shigenori Nozawa, Naoki Otomo
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Patent number: 8580822Abstract: The present invention provides novel indanone derivatives which can be advantageously used for treating and/or preventing of a medical condition for which inhibition of a cholinesterase is desired.Type: GrantFiled: June 8, 2012Date of Patent: November 12, 2013Assignee: Reviva Pharmaceuticals, Inc.Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra
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Publication number: 20130296324Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.Type: ApplicationFiled: February 25, 2013Publication date: November 7, 2013Applicant: VIVUS, Inc.Inventor: Jerry M. Held
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Publication number: 20130296283Abstract: Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid.Type: ApplicationFiled: July 5, 2013Publication date: November 7, 2013Inventor: Hesheng Zhang
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Publication number: 20130289019Abstract: One embodiment of an aspect of the present invention is a method for lessening the symptoms of depression, anxiety, and post-traumatic stress disorder comprising the step of administering a therapeutically effective quantity of a cholinergic M1 receptor antagonist and a therapeutically effective quantity of one or more cholinomimetic agents to lessen the symptoms of depression, anxiety, and post-traumatic stress disorder. Typically, the cholinergic M1 receptor antagonist is selected from the group consisting of telenzepine, amytriptyline, biperiden, trihexyphenidyl, darifenacin, dicyclomine, and tiotropium. Another aspect of the present invention is directed to methods and compositions employing other therapeutic agents and combinations of therapeutic agents for emulating the theoretical pharmacological effects of the non-selective mAChR antagonist scopolamine. The invention also encompasses pharmaceutical compositions incorporating one or more therapeutic agents and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 25, 2013Publication date: October 31, 2013Applicant: Amazing Grace, Inc.Inventor: David T. Chau
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Publication number: 20130280330Abstract: A nanosphere or microsphere drug carrier, formulations comprising the drug carrier and the preparation method of the formulations and the use of the carrier are disclosed. The carrier comprises a biodegradable methoxy end-capped polyethylene glycol-polylactide block copolymersor a derivative thereof represented by formula (I) as the main carrier material: CH3O—[CH2—CH2—O]m—[C(O)—CH(CH3)—O]n—R (I).Type: ApplicationFiled: July 30, 2010Publication date: October 24, 2013Applicant: XI'AN LIBANG MEDICAL TECHNOLOGY CO., LTD.Inventors: Renle Hu, Jiucheng Wang, Tao Chen, Hua Liang, Duohao Ding, Yaqi Jiao
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Patent number: 8557800Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: GrantFiled: October 19, 2011Date of Patent: October 15, 2013Assignee: Apogee Biotechnology CorporationInventors: Charles D. Smith, Kevin J. French, Yan Zhuang
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Publication number: 20130267560Abstract: The present invention relates to sustained release pharmaceutical compositions of donepezil or pharmaceutically acceptable salts thereof. The compositions of the invention are stable and provide sustained therapeutically effective plasma levels over a twenty four hour period with reduced incidences of cholinergic side effects. The invention also relates to process of making such compositions.Type: ApplicationFiled: October 24, 2011Publication date: October 10, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Sunilendu Roy, Sushrut Krishnaji Kulkarni, Ajaykumar Handa
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Patent number: 8541450Abstract: The invention relates to enantiomerically pure 3-(phthalimido)piperidines and processes for preparing enantiomerically pure 3-(phthalimido)piperidines.Type: GrantFiled: March 30, 2009Date of Patent: September 24, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Thorsten Pachur
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Patent number: 8541592Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: November 13, 2006Date of Patent: September 24, 2013Assignees: Amgen Inc., Biovitrum ABInventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle, Teresa L. Marshall
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Patent number: 8541452Abstract: A method for treating anxiety disorders and other disorders using cholinesterase inhibitors including donepezil and its pharmaceutically acceptable salts.Type: GrantFiled: October 6, 2005Date of Patent: September 24, 2013Inventors: Guy Chouinard, Charles-Siegfried Peretti
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Patent number: 8530434Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: GrantFiled: January 17, 2011Date of Patent: September 10, 2013Assignee: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Publication number: 20130231319Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.Type: ApplicationFiled: November 16, 2011Publication date: September 5, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
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Publication number: 20130225588Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: February 14, 2013Publication date: August 29, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130225605Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 22, 2013Publication date: August 29, 2013Applicant: SANOFIInventor: SANOFI