C=x Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding (x Is Chalcogen) Patents (Class 514/423)
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Patent number: 8283363Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: November 5, 2010Date of Patent: October 9, 2012Assignees: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20120252830Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 7, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20120252865Abstract: The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.Type: ApplicationFiled: March 8, 2010Publication date: October 4, 2012Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Walter Cabri, Patrizia Minetti, Giuseppe Campiani, Stefania Butini
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Publication number: 20120251464Abstract: Compounds are described that are effective in enhancing the efficacy of antimicrobial agents. Also described are methods of using such compounds and compositions that include such compounds. The composition includes a chalcone compound and, optionally, an antimicrobial agent.Type: ApplicationFiled: December 18, 2009Publication date: October 4, 2012Applicants: Indian Institute of Integrative Medicine, Colgate-Palmolive ComplanyInventors: Ravi Subramanyam, Laurence Du-Thumm, Ghulam Nabi Qazi, Inshad Ali Khan, Krishan Avtar Suri, Naresh Kumar Satti, Furqan Ali, Nitin Pal Kalia
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Publication number: 20120252866Abstract: The invention relates to a compound having general formula I, wherein: X represents CH2, C?O, C?S or CHOH, R1 represents an amino acid optionally substituted by one or more halogen atoms, or by one or more CF3 groups and n=0.1 or 2, or R1 represents a peptide containing two amino acids, each amino acid being optionally substituted by one or more halogen atoms, or by one or more CF3 groups and n=0 or 1, or XR1 represent PO3H or SO3H and n=0.1 or 2; R2 represents H, XR1, an alkyl group at C1-C6, an aralkyl group at C1-C6 or an aryl group, whereby the alkyl, aralkyl and aryl groups can be substituted by an amine NH2, a carboxylic group COOH, one or more halogen atoms.Type: ApplicationFiled: April 2, 2012Publication date: October 4, 2012Applicants: Centre National De La Recherche Scientifique (CNRS), PHARMAMENSInventors: Pierre Potier, Guy Jean Marie Potier, Marie Claude Denise Michele Zelveyan, Catherine Marie Germaine Magnan, Odette Drion, Nobumichi André Sasaki, Maria Concepcion Achab Garcia Alvarez, Qian Wang-Zhu, Lioudmila Ermolenko, Joanna Bakala, Gisèle Franck, Naïma Bakrim Nhiri
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Patent number: 8278343Abstract: This invention relates to a class of pyrrolidine compounds of formula (I), and pharmaceutically acceptable derivatives thereof, to their use in medicine, to compositions containing them, and to processes for their preparation. It also relates to intermediates used in the preparation of such compounds and derivatives. In particular the compounds of formula (I) are useful for the treatment of EP2-mediated conditions, such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), chronic pelvic pain syndrome.Type: GrantFiled: November 6, 2009Date of Patent: October 2, 2012Assignee: Pfizer Inc.Inventors: Kevin N. Dack, James E. Mills, Sarah E. Skerratt
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Patent number: 8278344Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: GrantFiled: August 20, 2010Date of Patent: October 2, 2012Assignees: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard College, Tufts UniversityInventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev
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Publication number: 20120244220Abstract: The present invention provides an atorvastatin-containing coated preparation comprising a solid formulation containing atorvastatin, a pharmacologically acceptable atorvastatin salt, or a solvate thereof coated with a coating agent comprising a polyvinyl alcohol copolymer, a method for inhibiting generation of related substances of atorvastatin, a pharmacologically acceptable atorvastatin salt, or a solvate thereof, comprising coating the solid formulation with a coating agent comprising a polyvinyl alcohol copolymer, and a method for stabilizing atorvastatin, a pharmacologically acceptable atorvastatin salt, or a solvate thereof.Type: ApplicationFiled: November 8, 2010Publication date: September 27, 2012Applicant: SAWAI PHARMACEUTICAL CO., LTD.Inventors: Toshihiro Yanagi, Kenji Nozawa, Kazuaki Maeda, Shinya Takada, Yasufumi Okamura
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Publication number: 20120237449Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Inventors: J. Marc Simard, Mingkui Chen
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Patent number: 8268880Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.Type: GrantFiled: December 15, 2006Date of Patent: September 18, 2012Assignee: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
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Patent number: 8263640Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.Type: GrantFiled: June 1, 2010Date of Patent: September 11, 2012Assignee: NUtech VenturesInventors: Concetta Dirusso, Paul Black
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Patent number: 8263637Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of a selective cytokine inhibitory drug alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of a selective cytokine inhibitory drug. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: May 16, 2003Date of Patent: September 11, 2012Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Publication number: 20120225881Abstract: The compounds shown by the structural formulas below have analgesic effect and are used in compositions and methods for treating mammal in need of such treatment.Type: ApplicationFiled: April 19, 2012Publication date: September 6, 2012Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Fabien (Jacques) Schweighoffer
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Patent number: 8258159Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.Type: GrantFiled: June 7, 2006Date of Patent: September 4, 2012Assignee: The Trustees Of The University Of PennsylvaniaInventors: William F. DeGrado, Joel S. Bennett, Seth Elliott Snyder, Sungwook Choi
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Patent number: 8258315Abstract: 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 solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.Type: GrantFiled: April 4, 2011Date of Patent: September 4, 2012Assignee: Pfizer Inc.Inventors: Antone J deBettencourt, III, Peter R. Rose, Evgenyi Shalaev, George J. Quallich, Carl B. Ziegler, Jr.
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Publication number: 20120220643Abstract: A method for increasing the vasodilative characteristics of amino acids in a human or animal is disclosed. The method includes administering to the human or animal a pharmaceutically effective amount of an amino acid compound consisting essentially of a nitrate or nitrite of an amino acid selected from the group consisting of Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, Phenylalanine, Carnitine, Taurine, and Betaine.Type: ApplicationFiled: May 10, 2012Publication date: August 30, 2012Applicant: THERMOLIFE INTERNATIONAL, LLCInventors: Ronald Kramer, Alexander Nikolaidis
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Publication number: 20120219514Abstract: In one aspect, the present invention relates to use of an ACE inhibitor and/or angiotensin II receptor antagonist for the preparation of a medicament for the treatment of a dermatological disorder, particularly by topical application of said ACE inhibitor and/or angiotensin II receptor antagonist. The present invention also provides cosmetic methods for improving and/or maintaining the skin tone of an individual suffering from, or at risk of suffering from, a dermatological disorder, said method comprising contacting the skin of said individual with an ACE inhibitor and/or angiotensin II receptor antagonist.Type: ApplicationFiled: November 18, 2011Publication date: August 30, 2012Inventor: Richard Bonnichsen
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Publication number: 20120220642Abstract: Methods for increasing the bioabsorption of amino acids and for preventing the development of nitrate tolerances in a human or animal are disclosed. The methods include administering to the human or animal a pharmaceutically effective amount of an amino acid compound consisting essentially of a nitrate or nitrite of an amino acid selected from the group consisting of Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, Phenylalanine, Carnitine, Taurine, and Betaine.Type: ApplicationFiled: May 7, 2012Publication date: August 30, 2012Applicant: THERMOLIFE INTERNATIONAL, LLCInventors: Ronald Kramer, Alexander Nikolaidis
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Publication number: 20120220577Abstract: The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.Type: ApplicationFiled: June 4, 2010Publication date: August 30, 2012Inventors: Markus Henrich, Angela Hansen, Jens Nagel, Valerjans Kauss, Jevgenijs Rozhkovs, Ginta Grunsteine, Dina Trifanova
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Publication number: 20120220564Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
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Publication number: 20120213702Abstract: The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3? and R3? is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention.Type: ApplicationFiled: August 31, 2010Publication date: August 23, 2012Inventors: Christoph Bremer, Carsten Höltke
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Publication number: 20120213758Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: DeCODE Genetics enfInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO, Timothy HAGEN
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Publication number: 20120214734Abstract: The present invention provides methods for treating, preventing, and/or delaying the onset of metabolic disorders including multi-factorial syndromes such as insulin-insensitivity and metabolic syndrome by administering an effective amount of an ACE inhibitor.Type: ApplicationFiled: May 12, 2011Publication date: August 23, 2012Inventor: Paul Anthony TALBOT
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Publication number: 20120213845Abstract: There is disclosed a composition that provides improved anti-aging benefits and creates a healthier skin using the combination of skin exfoliation, brightening, and collagen synthesis. In one embodiment, the composition comprises, a skin exfoliation ingredient such as citric acid and gluconolactone, at least one skin brightening ingredient, such licorice extract, and at least one collagen enhancing ingredient, such as hydroxyproline, bioactive polypeptides or combinations thereof. Depending on the end-use, various optional ingredients, such as moisturizers, anti-inflammatory agents, UVA/UVB protectants, and cleansers, may be added to the composition, which may take various forms, such as a cream, mousse, serum, or gel.Type: ApplicationFiled: October 19, 2011Publication date: August 23, 2012Inventor: Eric F. Bernstein
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Publication number: 20120214858Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.Type: ApplicationFiled: August 16, 2010Publication date: August 23, 2012Applicant: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
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Publication number: 20120214802Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: ApplicationFiled: October 9, 2009Publication date: August 23, 2012Inventors: Geoffrey M. Bilcer, Thippeswamy Devasamudram, Sudha V. Ankala, John C. Lilly, Chunfeng Liu, Hui Lei, Arun K. Ghosh, Makoto Inoue
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Publication number: 20120207769Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: April 26, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Patent number: 8242286Abstract: The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.Type: GrantFiled: July 28, 2008Date of Patent: August 14, 2012Assignee: Medicis Pharmaceutical CorporationInventors: Jin Li, Nicole Lee Kolosko
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Patent number: 8241674Abstract: Compositions and methods for enhancing heavy metal detoxification are described. The compositions and methods described provide enhanced activity of key detoxification systems including that the induction of phase II detoxification enzymes, such as glutathione S-transferases (GSTs), and NADPH quinone reductase (NQO1) activity.Type: GrantFiled: February 13, 2008Date of Patent: August 14, 2012Assignee: Metaproteomics, LLCInventors: Matthew L. Tripp, Veera Konda, Amy Hall, Anu Desai, Jeffrey S. Bland
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Publication number: 20120202820Abstract: The present invention relates to a pharmaceutical composition that comprises the active substance metformin in combination with one of the active substances sitagliptin or vildagliptin. The present invention further relates to a method of production of said pharmaceutical composition.Type: ApplicationFiled: September 13, 2010Publication date: August 9, 2012Applicant: Ratiopharm GMBHInventors: Katrin Rimkus, Ralph Stefan
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Publication number: 20120202848Abstract: This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases.Type: ApplicationFiled: December 2, 2011Publication date: August 9, 2012Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: MARK I. GREENE, WAYNE W. HANCOCK, MAKOTO KATSUMATO, YAN XIAO
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Patent number: 8236798Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: April 27, 2010Date of Patent: August 7, 2012Assignees: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20120196885Abstract: The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): wherein: R1 and R2 represent, independently, an optionally substituted C6-C10 aryl radical or an optionally substituted heteroaryl radical; A and M represent, independently, a methylene group or a single bond, in which case the adjacent aromatic ring would be attached directly to the amide group; the Y?Z group represents together and indistinctly an oxygen atom, a sulfur atom, a cis-vinylidene group, an imino group, or a methine group with a sp2-hybridized carbon atom; X represents indistinctly a methine group, a cis-vinylidene group or a nitrogen atom; and W represents a hydroxyl group, an optionally substituted C1-C6 alkyl group, an optionally substituted heteroaryl group or an optionally substituted C6-C10 aryl group; or a salt, solvate or prodrug thereof, as well as to the process for their preparation and the use thereof for the treatment of cancer.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Applicant: IKERCHEM, S.L.Inventors: Fernando Pedro Cossío Mora, Aizpea Zubia Olascoaga, Yosu Vara Salazar, Eider Ion San Sebastián Larzabal, Dorleta Otaegui Ansa, María del Carmen Masdeu Margalef, Eneko Aldaba Arévalo
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Patent number: 8232295Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.Type: GrantFiled: November 29, 2010Date of Patent: July 31, 2012Assignee: Heartdrug Research, L.L.C.Inventor: Victor L. Serebruany
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Publication number: 20120189684Abstract: This invention relates to skincare compositions, in particular compositions effective in the treatment of acne vulgaris, and to methods of treatment of the skin that involve the application of such compositions, wherein the compositions comprise salicylic acid or a salt thereof in combination with at 2 actives selected from the group consisting of lactic acid or a salt thereof; glycyrrhizinic acid or a salt or derivative thereof; bisabolol; cetylhydroxyproline palmitamide; allantoin; niacinamide; and epilobium angustifolium extract.Type: ApplicationFiled: July 19, 2010Publication date: July 26, 2012Applicant: Reckitt Benckiser Healthcare International LimitedInventors: Carolyn Buckley, Stuart Jackson, Neil Kilcullen, Diane Marie Pavis
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Publication number: 20120190649Abstract: 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: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: 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: 20120190618Abstract: The invention provides a method and a pharmaceutical composition in the form of a hydroalcoholic solution in which at least one hypoglycemia-inducing/insulinotropic active principle is dissolved in a stable and complete manner at a dosage that is reduced by 30% to 50% compared with the usual oral unit dosage, for its trans-buccal mucosal application in the spot treatment of postprandial hyperglycemia in type II diabetes in man or animals. The invention also pertains to a method of preparing said formulation and to its specific use in the spot treatment of postprandial hyperglycemia (PPHG) in the context of type II diabetes.Type: ApplicationFiled: July 7, 2010Publication date: July 26, 2012Inventors: Philippe Perovitch, Marc Maury, Jean-Pierre Dumonteix
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Publication number: 20120184593Abstract: Disclosed is a novel composition which has a function of stimulating production of laminin-332. The composition is stable and safe, and can be used routinely. Specifically disclosed is a laminin-332 production stimulating composition which contains one or more compounds selected from the group consisting of D-alanine, D-hydroxyproline, derivatives and/or salts thereof. The composition may be used for the purpose of suppressing and/or improving a skin condition. The skin condition may include, but is not limited to a photoaging, wrinkles, a rough skin, fine wrinkles and a dry skin. The composition may be used for an external preparation for the skin or a food.Type: ApplicationFiled: May 14, 2010Publication date: July 19, 2012Applicant: SHISEIDO COMPANY, LTDInventors: Yosuke Tojo, Jun-ichi Hosoi, Kayo Matsumoto
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Patent number: 8222228Abstract: A2A agonists of formula (I) is provided, wherein R1, R2, R4, R5, X, Y, Z, n, p, and q are as described herein. Also provided are compositions comprising and methods of using compounds of formula (I).Type: GrantFiled: December 29, 2010Date of Patent: July 17, 2012Assignee: Forest Laboratories Holdings LimitedInventors: Jayson M. Rieger, Robert D. Thompson
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Patent number: 8222274Abstract: [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).Type: GrantFiled: February 19, 2007Date of Patent: July 17, 2012Assignee: Astellas Pharma Inc.Inventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
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Publication number: 20120178761Abstract: The invention provides compounds of formula wherein R1, R2, R3, R4, R5, and R6 are as defined herein or a pharmaceutically suitable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: January 2, 2012Publication date: July 12, 2012Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian
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Publication number: 20120178780Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20120178666Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.Type: ApplicationFiled: September 15, 2010Publication date: July 12, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
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Publication number: 20120178724Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.Type: ApplicationFiled: March 22, 2012Publication date: July 12, 2012Applicant: WARNER CHILCOTT COMPANY, LLCInventors: Joseph Michael Sprafka, II, Jose Mauro Goulart-Brum
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Publication number: 20120178789Abstract: The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: September 16, 2010Publication date: July 12, 2012Inventors: Eric J. Gilbert, Michael W. Miller, Duane Eugene DeMong, Andrew W. Stamford, William J. Greenlee
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Publication number: 20120178732Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 6, 2011Publication date: July 12, 2012Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20120171262Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.Type: ApplicationFiled: March 15, 2012Publication date: July 5, 2012Inventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
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Publication number: 20120171158Abstract: The present invention relates to methods for the treatment of infection, a disease, or a condition using CD26 (DPIV) inhibitors. The present invention also relates to an antibody that binds to the IP-10 protein and a method of monitoring the necessity for administering a CD26 inhibitor to a patient, comprising evaluating a level of sIP-10, a activity of CD26, and/or a level of CXCR3 cells in a sample.Type: ApplicationFiled: January 20, 2012Publication date: July 5, 2012Applicant: INSTITUT PASTEURInventors: Matthew Albert, Armanda Casrouge, Jeremie Decalf, Stanislas Pol, Arnaud Fontanet, Mostafa Mohamed
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Patent number: 8211926Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: June 16, 2010Date of Patent: July 3, 2012Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Patent number: 8211931Abstract: The novel active compound combinations consisting, firstly, of cyclic ketoenols and, secondly, of beneficial species (natural enemies) have very good insecticidal and/or acaricidal properties.Type: GrantFiled: June 5, 2007Date of Patent: July 3, 2012Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Heike Hungenberg, Ralf Nauen, Hans-Jürgen Schnorbach, Wolfgang Thielert