C=x Bonded Directly Or Indirectly By An Acyclic Carbon Or Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring (e.g., Tryptophan, Etc.) (x Is Chalcogen) Patents (Class 514/419)
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Publication number: 20110086803Abstract: The present invention relates to a process to produce a composition comprising water-soluble peptides and having a Trp/LNAA ratio of more than 0.15, which comprises hydrolyzing lysozyme, preferably hen eggs lysozyme, to prepare a hydrolysate having a DH of between 5 and 45.Type: ApplicationFiled: October 30, 2007Publication date: April 14, 2011Inventors: Andre Leonardus De Roos, Luppo Edens, Rudolf Franciscus Van Beckhoven, Alexander Lucia Leonardus Duchateau, Joris Kloek
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Publication number: 20110086885Abstract: Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.Type: ApplicationFiled: November 25, 2005Publication date: April 14, 2011Inventors: Stuart Edward Bradley, Thomas Martin Krulle, Gerard Hugh Thomas
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Publication number: 20110082119Abstract: A highly safe and effective prophylactic/ameliorating or therapeutic agent for NACH and the method for using the same are provided. A prophylactic/ameliorating or therapeutic agent for NASH containing a combination of at least one first ingredient selected from the group consisting of an ?3PUFA and pharmaceutically acceptable salts and esters thereof and at least one second ingredient selected from the group consisting of (a) a biguanide hypoglycemic agent, (b) a nonsteroidal anti-inflammatory drug, (c) a 3-hydroxy-3-methyl glutaryl coenzyme A reductase inhibitor, and (d) an angiotensin II receptor blocker as the active ingredients; and its method of use.Type: ApplicationFiled: June 12, 2009Publication date: April 7, 2011Inventor: Takashi YANO
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Patent number: 7919519Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: GrantFiled: March 21, 2007Date of Patent: April 5, 2011Assignee: Epix Pharmaceuticals Inc.Inventors: Roland Burli, Victor J. Cee, Jennifer Golden, Brian Alan Lanman, Susana Neira, Ashis Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert C. Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker, Zhaoda Zhang
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Publication number: 20110077269Abstract: Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions.Type: ApplicationFiled: September 10, 2010Publication date: March 31, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Corey Anderson
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Publication number: 20110071175Abstract: Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.Type: ApplicationFiled: December 12, 2008Publication date: March 24, 2011Inventors: George Hynd, John Gary Montana, Harry Finch, Rosa Arienzo, Barbara A. Vitabile-Woo, Mathias Domostoj
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Publication number: 20110071176Abstract: In various embodiments, the present invention provides compositions and methods for treating and/or preventing a cardiovascular-related disease in subject in need thereof.Type: ApplicationFiled: September 23, 2010Publication date: March 24, 2011Applicant: AMARIN PHARMA, INC.Inventor: Jonathan Rowe
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Publication number: 20110070272Abstract: The subject invention provides materials and methods for modulating a variety of biological factors to treat biological conditions associated with the factors. In one embodiment of the invention, a cysteamine compound is administered to a patient to treat hypercholesterolemia and/or complications associated with hypercholesterolemia. In another embodiment, a cysteamine compound is administered to a patient to prevent the onset of diabetes in an at-risk patient and/or treat or prevent the onset of diabetes-associated complications.Type: ApplicationFiled: November 30, 2010Publication date: March 24, 2011Inventors: Bill Piu Chan, Gary Kwan Po Wong, Jinxian Xu, Francis Chi
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Publication number: 20110065757Abstract: We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma.Type: ApplicationFiled: January 30, 2009Publication date: March 17, 2011Applicants: JOSKIN DIABETES CENTER, ACTIVESITE PHARMACEUTICALS, INC.Inventors: Lloyd P. Aiello, Tamie Jo Chilcote, Sukanto Sinha, Edward P. Feener
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Publication number: 20110065685Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.Type: ApplicationFiled: June 14, 2010Publication date: March 17, 2011Applicant: Abbott LaboratoriesInventors: Jennifer M. Frost, Karin Tietje, Michael J. Dart, Michael D. Meyer
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Publication number: 20110060026Abstract: Indole derivatives having therapeutic utility are of formula (I): X is —SO2— or *—SO2NR3— wherein the bond marked with an asterisk is attached to Ar1; R1 and R2 are, independently, hydrogen, fluoro, chloro, CN or CF3; R3 is hydrogen, C1-C8alkyl or C3-C7cycloalkyl; and Ar1 and Ar2 are, independently, phenyl or a 5- or 6-membered heteroaryl group, wherein the phenyl or heteroaryl group is optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C7cycloalkyl, —O(C1-C4alkyl) or C1-C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.Type: ApplicationFiled: January 16, 2009Publication date: March 10, 2011Inventors: George Hynd, JOhn Gary Montana, Harry Finch
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Patent number: 7902251Abstract: The present invention provides pharmaceutical compositions useful in a method for treating neuropathic pain, said method comprising administration of a pain-ameliorating effective amount of the compound according to formula I wherein R is an alk(en)yl group, R1 is an alkylen(yl) group, n is 0 or 1 and Ar is a carbocyclic aryl group.Type: GrantFiled: October 13, 2006Date of Patent: March 8, 2011Assignee: Allergan, Inc.Inventors: Vincenzo Di Marzo, Luciano De Petrocellis, Sabatino Malone, Vito De Novellis
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Patent number: 7902250Abstract: Compositions based on amino acids are described, in particular for oral or parenteral use, suitable for treating heart insufficiency. The compositions according to the invention comprise up to 75% of the branched chain amino acids leucine, isoleucine and valine, as active ingredients. Preferably, the compositions also comprise, as further active ingredients, up to 50% of threonine and lysine. Other essential amino acids are preferably also provided (in particular methionine, phenylalanine, histidine, triphtophan) as well as non essential amino acids (in particular tyrosine and/or cyst(e)ine—i.e. cystine and cyst(e)ine). Other amino acids can be added, provided that their sum is in a percentage being lower than 20% with respect to the other active ingredients, and less than 10% for each single amino acid.Type: GrantFiled: June 28, 2001Date of Patent: March 8, 2011Assignee: Professional Dietetics S.R.L.Inventor: Francesco Saverio Dioguardi
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Publication number: 20110052688Abstract: A solid dispersion extended release tablet composition is provided. The composition comprises fluvastatin sodium and a polymer, wherein molecules of the fluvastatin sodium are separate from one another and dispersed in the polymer, and wherein the composition displays two distinct peaks at about 3.5 and 20.4.degrees 2? of X-ray diffraction.Type: ApplicationFiled: October 19, 2010Publication date: March 3, 2011Inventors: San-Laung Chow, David Wong, Edward Lin
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Publication number: 20110052704Abstract: Compositions containing tocotrienol, non-tocotrienol lipids and surface active agents; compositions containing particles having a statin and a tocotrienol wherein the particle size is less than 1000 nm; and microemulsions containing a statin and a tocotrienol are disclosed. Methods relating to the creation of such compositions and the use of such compositions are further disclosed.Type: ApplicationFiled: September 1, 2010Publication date: March 3, 2011Applicant: First Tech International LimitedInventors: Sami Mahmoud Nazzal, Paul W. Sylvester
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Publication number: 20110052683Abstract: The present invention provides a pharmaceutical preparation comprising a prior-release compartment containing a hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor as a pharmacologically active ingredient, and a delayed-release compartment containing a non-dihydropyridine calcium channel blocker as a pharmacologically active ingredient. The preparation of the present invention provides synergistic effects through combined administration of the non-dihydropyridine calcium channel blocker and the HMG-CoA reductase inhibitor, and induces the time-dependent absorption, metabolism and action mechanism of individual drugs through the controlled release thereof to avoid competitive antagonism between drugs, thus maximizing the effects of each pharmacologically active ingredient while minimizing side effects, for example, the risk of myopathy, and substantially increasing the compliance of patients by taking one tablet once a day.Type: ApplicationFiled: February 21, 2009Publication date: March 3, 2011Applicant: HANALL BIOPHARMA CO., LTD.Inventors: Sung Wuk Kim, Sung Soo Jun, Ja Seong Koo, Young Joo Lee, Seok Young Jang, Young Gwan Jo
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Publication number: 20110053955Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: February 7, 2008Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Patent number: 7897160Abstract: Stable emulsions comprising as a base one or more diene conjugated fatty acids. Amino acids and other macromolecules can be used to stabilize the emulsion. The emulsion is also useful as a carrier and delivery vehicle of the macromolecules to humans or animals in need of the macromolecules. Plant oil extracts, such as conjugated linoleic acid and its acylated derivatives, are useful as the diene conjugated fatty acids that form the base of the stable emulsion. The emulsions formed are useful as nutritional or cosmetic adjuvant for oral based nutrition, skin diseases, cosmetic utility, enhancing oral nutrition, or pharmacological benefit. Methods of producing and using the emulsions are also provided.Type: GrantFiled: June 2, 2006Date of Patent: March 1, 2011Inventor: David G. Changaris
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Patent number: 7897788Abstract: The invention relates to indol-1-yl-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds.Type: GrantFiled: March 8, 2005Date of Patent: March 1, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Anja Fecher, Heinz Fretz, Kurt Hilpert, Markus Riederer
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Publication number: 20110046090Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a GABA agent or GABA analog, in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Applicant: BrainCells Inc.Inventors: Carrolee BARLOW, Todd Carter, Andrew Morse, Kai Treuner, Kym Lorrain, Jammieson Pires
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Patent number: 7888383Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.Type: GrantFiled: December 7, 2006Date of Patent: February 15, 2011Assignee: Novartis AGInventor: David Andrew Sandham
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Patent number: 7888384Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: GrantFiled: April 16, 2009Date of Patent: February 15, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
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Publication number: 20110034531Abstract: The invention relates to the use of an HDAC inhibitor, more specifically or a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for the treatment of melanoma; the use of an HDAC inhibitor or a pharmaceutically acceptable salt thereof in the treatment of melanoma; a method of treating warm-blooded animals including mammals, especially humans, suffering from melanoma by administering to a said animal in need of such treatment a dose effective against said disease of an HDAC inhibitor or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 9, 2008Publication date: February 10, 2011Applicant: NOVARTIS AGInventor: Peter Wisdom Atadja
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Publication number: 20110033393Abstract: The present invention relates to hydrazone compounds of Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.Type: ApplicationFiled: May 12, 2010Publication date: February 10, 2011Inventors: Philip STEIN, Robert DAINES, Dennis SPROUS, Harold O'GRADY
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20110021540Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: January 27, 2011Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria Ek, Jorg Holenz, Martin H. Johansson, Annika Kers, Katja Narhi, Gunnar Nordvall, Liselotte Ohberg, Daniel Sohn, Jenny Viklund, Stefan Von Berg
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Publication number: 20110020436Abstract: The invention is a topical therapeutically effective amount of melatonin encapsulated in a liposome applied topically to an area of skin affected by immunologic response, radiation treatment induced dermatitis, acne, insect bite or other irritant stimulus such as sunburn in order to reduce itching. The invention also proposes a topical therapeutically effective amount of melatonin and reduced glutathione encapsulated in a liposome applied topically to an area of skin for relief of those afflictions.Type: ApplicationFiled: October 6, 2010Publication date: January 27, 2011Inventor: F. Timothy Guilford
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Publication number: 20110014277Abstract: Disclosed is a compound and methods for use by an individual attempting to reduce or cease tobacco smoking or one exposed to environmental tobacco smoke. The compound includes a first component blocking nicotine receptor sites to reduce nicotine cravings or withdrawal symptoms, a second component increasing serotonin levels and acting synergistically with the first component to reduce nicotine cravings or withdrawal symptoms, assisting in maintaining body weight and reducing increased stress and anxiety, and a third component acting synergistically with the first and/or second component to reduce nicotine cravings or withdrawal symptoms, maintain body weight, and/or reduce increased stress and anxiety. The third component comprises a supplement that replenishes depleted body substance(s), repairs damaged body substance(s), and/or ameliorates the impaired function of body substance(s). Some combination of the first, second, and third component alters the perceived taste of tobacco smoke.Type: ApplicationFiled: September 29, 2010Publication date: January 20, 2011Inventor: Harlan Clayton Bieley
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Patent number: 7872040Abstract: It is intended to find a compound that is structurally simpler than yohimbine, a pentacyclic condensed heterocyclic compound, and has an effect similar to that of yohimbine. The present invention relates to a pharmaceutical or food composition for ?2 receptor blockage comprising a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (wherein R1 represents a hydrogen, alkyl group, alkenyl group, alkynyl group, aromatic group, aralkyl group, acyl group, arylsulfonyl group, alkylsulfonyl group, or hydroxyl group; R2 represents a hydrocarbon group; R3, R4, R5, R6, and R7 are the same or different and represent a hydrogen, halogen, alkyl group, or alkoxy group; R8 represents a hydrogen or acyl group; n represents an integer of 1 to 6; and a and b are the same or different and represent 1 or 0).Type: GrantFiled: September 16, 2005Date of Patent: January 18, 2011Inventors: Masanori Somei, Koki Shigenobu, Yoshio Tanaka
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Publication number: 20110009448Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.Type: ApplicationFiled: July 23, 2010Publication date: January 13, 2011Inventors: Nigel Vicker, Su Xiangdong, Dharshini Ganeshapillai, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
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Publication number: 20110009453Abstract: Disclosed herein are compositions and methods for treating inflammation using S1 P3 receptor inhibitors.Type: ApplicationFiled: March 16, 2009Publication date: January 13, 2011Inventors: John E. Donello, Mohammed I. Dibas
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Publication number: 20110003851Abstract: The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Ligand Pharmaceuticals, Inc.Inventors: Lin Zhi, Andrew R. Hudson, Cornelis A. Van Oeveren, Steven L. Roach, Jason C. Pickens, Yixing Shen, Catalina Cuervo, Lino J. Valdez, Jillian Basinger, Virgina H. Grant
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Patent number: 7863335Abstract: Methods for treating or reducing the risk of transmission of chlamydia to a recipient by topically applying a metalloprotease inhibitor to a site on the recipient which is likely to be exposed to Chlamydia. Topical compositions containing metalloprotease inhibitors are also disclosed for treating or reducing the risk of transmission of Chlamydia, as well as barrier contraceptive devices coated therewith.Type: GrantFiled: July 25, 2005Date of Patent: January 4, 2011Assignee: The University of Medicine and Dentistry of New JerseyInventor: Huizhou Fan
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Patent number: 7863315Abstract: Provided herein are isolated compounds of formula I: processes for their preparation and isolation, as well as pharmaceutical compositions which comprise these therapeutic agents, and methods of use therefore the treatment and/or control of conditions associated with or mediated by effects of histone deacetylase.Type: GrantFiled: January 14, 2009Date of Patent: January 4, 2011Assignee: Shenzhen Chipscreen Biosciences, Ltd.Inventors: Xian-Ping Lu, Zhi-bin Li, Zhi-Qiang Ning
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Publication number: 20100331383Abstract: The present invention provides methods for treating Acquired Immunodeficiency Syndrome (AIDS) and other viral diseases and Human Immunodeficiency Virus (HIV) related infections by administering one or more compounds of formula I: wherein: the dotted line represents a single or a double bond; and R1 and R2 are the same or different and independently of each other represent —CH2OH, —CH2OR4, —CH(OH)CH3, —CH(OR4)CH3 or a group represented by the formula: or salts or hydrates thereof in a carrier which minimizes micellar formation or van der Waals attraction of molecules of said compound. The invention also provides S enantiomeric forms of such compounds which possess the ability to inhibit cell growth whilst being of low toxicity to such cells and methods of making such compounds.Type: ApplicationFiled: July 12, 2010Publication date: December 30, 2010Applicant: Novaremed LimitedInventor: Eliahu Kaplan
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Publication number: 20100324009Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 23, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100324075Abstract: Compounds, pharmaceutical compositions, and their methods of use in raising serum HDL levels in subjects in need thereof are provided. Also provided are compounds, pharmaceutical compositions, and their methods of use in increasing reverse cholesterol transport in subjects in need thereof. Finally, methods for treating disease by raising serum HDL levels and increasing reverse cholesterol transport are provided.Type: ApplicationFiled: December 19, 2008Publication date: December 23, 2010Applicant: UNIVERSITY OF CINCINNATIInventors: David Y. Hui, Philip N. Howles
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Publication number: 20100324109Abstract: The use, as a dermatological or cosmetic medicament, of compounds capable of transiently interacting with the AhR receptor (aryl hydrocarbon receptor) as agents for modulating skin functions such as sebaceous function, skin healing, skin atrophy termed “dermatoporosis”, estrogen deprivation and defense against infection, without inducing other toxic effects of the TCDD type. The compounds that interact with the AhR receptor are chosen in that they have a metabolism favorable to the dissociation of these effects, in particular by virtue of in situ production from a precursor and/or metabolization modulated in situ.Type: ApplicationFiled: January 23, 2009Publication date: December 23, 2010Inventor: Jean Hilaire Saurat
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Patent number: 7855225Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: GrantFiled: March 1, 2007Date of Patent: December 21, 2010Assignee: Astellas Pharma Inc.Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
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Publication number: 20100317710Abstract: Substantially pure 3-(3-indolyl)propionic acid free acid is synthesized by converting the free acid to 3-(3-indolyl)propionic acid calcium salt (3-IPA calcium), precipitating and washing, and then reconverting the 3-IPA calcium to the free acid. 3-IPA calcium is suitable for use in pharmaceutical compositions in tablet and sustained-release dosage forms. 3-IPA calcium can be used to inhibit the cytotoxic effects of amyloid beta protein on cells, to treat fibrillogenic diseases in a mammal, and to treat diseases or conditions in which free radicals or oxidative stress plays a role.Type: ApplicationFiled: January 21, 2010Publication date: December 16, 2010Applicant: INTELLECT NEUROSCIENCES INC.Inventor: Norman H. Rogers
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Publication number: 20100317644Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 16, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100311803Abstract: The present invention relates a method of preventing and/or reducing an inflammatory response and/or inflammation in one or more tissues. The method includes delivering to the one or more tissues an effective amount of a substance P receptor antagonist.Type: ApplicationFiled: December 7, 2007Publication date: December 9, 2010Inventors: Alan John Nimmo, Karen Margaret Whitfield, Konrad Reardon, Robert Vink
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Publication number: 20100311805Abstract: This invention relates to organic compounds of formula (I): in particular, to pharmaceutical compositions for use in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease.Type: ApplicationFiled: August 9, 2010Publication date: December 9, 2010Applicant: NOVARTIS AGInventor: Richard William Versace
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Publication number: 20100311804Abstract: The present invention provides improved treatment methods by the administration of both an inhibitor of indoleamine-2,3-dioxygenase in addition to the administration of an additional therapeutic agent.Type: ApplicationFiled: August 27, 2009Publication date: December 9, 2010Applicant: Medical College of Georgia Research Institute, Inc.Inventors: David MUNN, Andrew Mellor
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Publication number: 20100311710Abstract: The present invention relates to new cyclobutanemethanamine inhibitors of monoamine reuptake, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 4, 2009Publication date: December 9, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar, Manouchehr M. Shahbaz
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Publication number: 20100303919Abstract: Pharmaceutical compositions comprising fluvastatin, HPMC and optionally other pharmaceutical excipients which are colour-stable upon prolonged periods of storage.Type: ApplicationFiled: July 13, 2010Publication date: December 2, 2010Inventors: OSKAR Kalb, Stephen Valazza
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Publication number: 20100305183Abstract: The present invention relates to a method of preventing and/or reducing reperfusion injury to a tissue, organ, or organ system in a subject. The method includes administering to the subject an effective amount of a substance P receptor antagonist.Type: ApplicationFiled: December 7, 2007Publication date: December 2, 2010Inventors: Alan John Nimmo, Karen Margaret Whitfield, Renée Jade Turner, Robert Vink
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Publication number: 20100305184Abstract: The present invention includes inhibitors of the amino acid transporter ATB0,+ and methods of uses thereof.Type: ApplicationFiled: October 8, 2009Publication date: December 2, 2010Inventors: Vadivel Ganapathy, Muthusamy Thangaraju, Puttur Prasad