Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/443)
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Publication number: 20110237525Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.Type: ApplicationFiled: June 18, 2010Publication date: September 29, 2011Inventors: Boyd E. Haley, Niladri Narayan Gupta
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Publication number: 20110230488Abstract: The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.Type: ApplicationFiled: November 25, 2009Publication date: September 22, 2011Applicant: TRT PHARMA INC.Inventors: Jian Hui Wu, Gerald Batist, Jinming Zhou, Guoyan Geng, Rongtuan Lin
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Patent number: 8022102Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substitutents are defined as in Claim 1.Type: GrantFiled: June 21, 2005Date of Patent: September 20, 2011Assignee: Janssen Pharmaceutica, NVInventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20110212969Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G 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: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Publication number: 20110212970Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: March 17, 2011Publication date: September 1, 2011Applicant: CALCIMEDICA, INC.Inventors: GONUL VELICELEBI, KENNETH A. STAUDERMAN, JEFFREY P. WHITTEN, YAZHONG PEI, JIANGUO CAO, ZHIJUN WANG, EVAN ROGERS, BRIAN DYCK, JONATHAN GREY
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Publication number: 20110213003Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G 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: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8003692Abstract: Fluorene-based molecules and their derivatives are described in compositions for the treatment of intestinal fluid loss.Type: GrantFiled: June 13, 2008Date of Patent: August 23, 2011Assignees: Board of Regents, The University of Texas System, Mission Pharmacal Co.Inventors: Catherine H. Schein, Johnny W. Peterson, Scott R. Gilbertson, Deliang Chen, Maria Estrella-Jimenez, Mary A. Walter, Jian Gao
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Patent number: 8003684Abstract: Crystalline forms of (+)-R-zileuton, which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of (+)-R-zileuton are characterized by a variety of properties and physical measurements. As well, methods of producing crystalline (+)-R-zileuton, and using it to inhibit 5-lipoxygenase activity in subjects to treat a number of diseases, are also discussed.Type: GrantFiled: February 21, 2007Date of Patent: August 23, 2011Assignee: Cornerstone Therapeutics, Inc.Inventor: Jason A. Hanko
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Patent number: 7999001Abstract: Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections.Type: GrantFiled: January 14, 2008Date of Patent: August 16, 2011Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Mohammad Javad Aman, Sina Bavari, James C. Burnett, Kelly Lyn Warfield
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Patent number: 7985768Abstract: The present invention relates to thiophene containing compounds of formula (I) wherein R1, R2, R3, and n are as defined in the specification, pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions.Type: GrantFiled: August 31, 2007Date of Patent: July 26, 2011Assignee: Abbott LaboratoriesInventors: Derek W. Nelson, Steven P. Latshaw
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Patent number: 7981924Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.Type: GrantFiled: November 22, 2006Date of Patent: July 19, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
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Patent number: 7977380Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: November 20, 2009Date of Patent: July 12, 2011Assignee: Activesite Pharmaceticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20110165188Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Way Tsun Yue
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Patent number: 7973074Abstract: Monomeric, oligomeric or polymeric compound corresponding to the following formula (I): in which: A represents an optionally substituted polycyclic group, the said polycyclic group comprising at least one group capable of making possible the attachment of a chromophoric group, X1 and X2, which are identical or different, each independently represent a group of formula (II): in which: B and D, which are identical or different, each independently represent an aromatic carbon ring or an aromatic heterocycle which is optionally substituted. Use of the said compound in an optoelectronic device, such as a photovoltaic cell, a field-effect transistor or an electrochemical sensor. Photovoltaic cell comprising an active layer comprising an electron donor composed of the said compound.Type: GrantFiled: April 20, 2005Date of Patent: July 5, 2011Assignee: Commissariat a l'Energie AtomiqueInventors: Renaud Demadrille, Adam Pron, Muriel Firon, Jocelyne Leroy
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Patent number: 7973181Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi— or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein RType: GrantFiled: May 4, 2006Date of Patent: July 5, 2011Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, David Festus Charles Moffat
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Publication number: 20110145970Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Patent number: 7964598Abstract: The present invention provides compounds that inhibit apoE4 domain interaction; and compositions, including pharmaceutical compositions, comprising the compounds. The present invention provides methods of treating apoE4-related disorders. The methods generally involve administering to an individual in need thereof a therapeutically effective amount of an apoE4 domain interaction inhibitor.Type: GrantFiled: October 4, 2005Date of Patent: June 21, 2011Assignee: The J. David Gladstone InstitutesInventors: Robert W. Mahley, Karl H. Weisgraber, Yadong Huang
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Patent number: 7964632Abstract: This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.Type: GrantFiled: January 15, 2010Date of Patent: June 21, 2011Assignee: Eli Lilly and CompanyInventors: Eric David Moher, James Allen Monn, Concepcion Pedregal-Tercero, Ivan Collado Caño, Jaime Gonzalo Blanco-Urgoiti
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Publication number: 20110144170Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: ApplicationFiled: February 18, 2011Publication date: June 16, 2011Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Publication number: 20110144094Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: ApplicationFiled: February 16, 2011Publication date: June 16, 2011Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20110136816Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 14, 2011Publication date: June 9, 2011Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110130363Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 31, 2011Publication date: June 2, 2011Applicant: Genentech, Inc.Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
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Publication number: 20110124681Abstract: Methods of treating, preventing, reducing the occurrence of, or slowing progression of folliculitis, partial or full hair loss, thinning of the hair, changes in the texture of hair, graying or whitening (loss of pigmentation) of the hair, dermatological conditions, and other hair-related conditions, comprising administering topical and injectable formulations containing one or more leukotriene receptor antagonists.Type: ApplicationFiled: May 6, 2009Publication date: May 26, 2011Inventor: Larry S. Schlesinger
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Publication number: 20110111031Abstract: The present specification provides drug delivery platforms useful for the controlled release of a compound over time in an individual.Type: ApplicationFiled: October 22, 2010Publication date: May 12, 2011Inventors: GUANG-LIANG JIANG, ADAM L. COLLETTE, REBECCA L. HORAN, JINGSONG CHEN, GREGORY H. ALTMAN, WHA BIN IM
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Publication number: 20110112180Abstract: The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: September 10, 2008Publication date: May 12, 2011Applicant: Boston Biomedical, Inc.Inventors: Zhiwei Jiang, Chiang Jia Li, Wei Li, David Leggett
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Publication number: 20110112142Abstract: The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R3 is selected from the group consisting of ORA; —CHO; —C(O)C1-4alkyl; —C(O)phenyl; —O—C(O)RA; and N(RB)2; R6 is selected from certain cyclic groups defined in the specification; and the remaining groups are defined in the specification; together with a pharmaceutically acceptable carrier. Most of the compounds are novel. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: April 8, 2009Publication date: May 12, 2011Inventors: Daniel Nöteberg, Elisabet Kallin, Mattias Wennerstål
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Patent number: 7939528Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: GrantFiled: October 12, 2006Date of Patent: May 10, 2011Assignee: GlaxoSmithKline LLCInventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
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Patent number: 7935724Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having a benzothiophene or thiophene backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit historic deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells.Type: GrantFiled: October 8, 2004Date of Patent: May 3, 2011Assignee: Merck HDAC Research, LLCInventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
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Patent number: 7935725Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: GrantFiled: October 30, 2008Date of Patent: May 3, 2011Assignee: Janssen Pharmaceutica NVInventors: Scott D. Bembenek, Wendy Eccles, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Taraneh Mirzadegan, Alejandro Santillán, Jr.
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Publication number: 20110098333Abstract: The invention is directed to methods of treating organ specific infections in a host organism by administering compounds that target host receptors and/or host cellular signaling molecules to prevent a pathogen from infecting the organ. For example, the administration of a compound to prevent a pathogen from crossing the blood-brain barrier to prevent a brain infection.Type: ApplicationFiled: June 12, 2009Publication date: April 28, 2011Applicant: The Johns Hopkins UniversityInventor: Kwang Sik Kim
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METHODS OF INHIBITING THE FORMATION OF AMYLOID-BETA DIFFUSABLE LIGANDS USING ACYLHYDRAZIDE COMPOUNDS
Publication number: 20110098309Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers using acylhydrazide compounds. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers using acylhydrazide compounds.Type: ApplicationFiled: July 11, 2008Publication date: April 28, 2011Applicant: ACUMEN PHARMACEUTICALS, INC.Inventors: Gary Charles Look, Lauri Schultz, Alexandre Mikhaylovich Polozov, Nikhil Bhagat, Jian Wang, David E. Zembower, William F. Goure, Todd Pray, Grant A. Krafft -
Patent number: 7932283Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions:Type: GrantFiled: April 5, 2007Date of Patent: April 26, 2011Assignee: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stéphane Carbonne, Stéphanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
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Publication number: 20110092578Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present.Type: ApplicationFiled: December 20, 2010Publication date: April 21, 2011Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski
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Publication number: 20110092517Abstract: Provided herein are methods for treatment, prevention, or amelioration of one or more symptoms of a disease or condition related to disorders of insulin and/or glucose metabolism, inflammatory conditions, mitochondrial disease, muscle disorders, or pulmonary disorders, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist. In one embodiment, the disease or condition is selected from myopathy, inflammatory vascular diseases, Parkinson's and Alzheimer's diseases, systemic inflammatory disorders, renal ischemia, inflammatory rheumatic disorders, and inflammatory diseases of the lung. In another embodiment, methods for increasing oxidative muscle fibers, reducing mitochondria disease, decreasing insulin resistance, decreasing plasma glucose, or decreasing weight, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist, are provided.Type: ApplicationFiled: August 13, 2010Publication date: April 21, 2011Inventors: Ronald Barbaras, Daniela Carmen Oniciu, Jean-Louis H. Dasseux, Robert A. Scott, John R. Wetterau
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Publication number: 20110086877Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.Type: ApplicationFiled: October 1, 2010Publication date: April 14, 2011Inventors: SINA BAVARI, RICK GUSSIO, JAMES C. BURNETT
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Publication number: 20110086907Abstract: The invention relates to the use of lipooxigenase inhibitors for treating acne, particularly inflammatory acne. The inventive lipooxigenase inhibitor can be used alone or in combination with other lipooxigenase inhibitors or anti-acne active agents in a pharmaceutically suitable composition, particularly through oral and/or local-topic application.Type: ApplicationFiled: July 9, 2009Publication date: April 14, 2011Inventor: Christos C. Zouboulis
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Publication number: 20110086023Abstract: The invention provides a topical pharmaceutical composition for application to the nasal or ocular mucosa which comprises (1) a pharmaceutical excipient suitable for topical administration, (2) a mucosal adjuvant, (3) an antihistamine drug and (4) a mast cell stabilizer, a non-steroidal anti-inflammatory drug, a phosphodiesterase inhibitor, an anti-IgE agent, heparin, a topical steroid or a leukotriene blocker.Type: ApplicationFiled: December 20, 2010Publication date: April 14, 2011Applicant: Fairfield Clinical Trials LLCInventor: Edward M. Lane
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Publication number: 20110086838Abstract: The present invention relates to thiophene containing compounds of formula (I) wherein m, n, p, q, r, s, R1, R2, and R3 are as defined in the description. Included also are pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions.Type: ApplicationFiled: December 14, 2010Publication date: April 14, 2011Applicant: ABBOTT LABORATORIESInventors: Derek W Nelson, Jennifer M. Frost
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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: 20110076291Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 27, 2010Publication date: March 31, 2011Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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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: 20110065724Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: September 15, 2010Publication date: March 17, 2011Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers
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Publication number: 20110052643Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 7, 2009Publication date: March 3, 2011Applicant: Synta Pharmaceuticals Corp.Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen, Lijun Sun
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Publication number: 20110052695Abstract: The present specification provides drug delivery platforms useful for the controlled release of a compound over time in an individual.Type: ApplicationFiled: September 1, 2010Publication date: March 3, 2011Applicant: ALLERGAN, INC.Inventors: Guang-Liang Jiang, Adam L. Collette, Rebecca L. Horan, Jing Song Chen, Gregory H. Altman, Wha Bin Im
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Publication number: 20110053941Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprisType: ApplicationFiled: December 1, 2008Publication date: March 3, 2011Applicant: NEWLINK GENETICSInventors: Mario Mautino, Firoz Jaipuri, Agnieszka Marcinowicz-Flick, Tanay Kesharwani, Jesse Waldo, Steven James Collier
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Patent number: 7897789Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzothiophene compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.Type: GrantFiled: July 6, 2009Date of Patent: March 1, 2011Assignee: Eli Lilly and CompanyInventors: Jianliang Lu, Tainwei Ma, Sunil Nagpal, Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee, Michael John Rupp
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Publication number: 20110044938Abstract: Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.Type: ApplicationFiled: August 15, 2007Publication date: February 24, 2011Applicant: NYCOMED GMBHInventors: Bjorn Bartels, Mathias Schmidt, Klaus Pekari, Thomas Beckers, Astrid Zimmermann, Volker Gekeler
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Patent number: 7893084Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all of whichType: GrantFiled: November 26, 2008Date of Patent: February 22, 2011Assignee: Boehringer Ingelheim Canada Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-André Poupart, Jean Rancourt
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Patent number: 7893107Abstract: Methods are provided directed to administering a therapeutically effective amount of a prostaglandin EP4 agonist component to a mammal afflicted with or prone to afflicted with a disease or condition selected from an esophageal ulcer, alcohol gastropathy, a duodenal ulcer, non-steroidal anti-inflammatory drug-induced gastropathy, non-steroidal anti-inflammatory drug-induced enteropathy and intestinal ischemia. Such administration results in treating the disease or condition.Type: GrantFiled: November 30, 2005Date of Patent: February 22, 2011Assignee: Allergan, Inc.Inventors: Guang-Liang Jiang, Wha Bin Im, Larry A. Wheeler
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Patent number: RE42327Abstract: An alkyl ether derivative represented by the formula: wherein R1, R2, R3, R4, m and n are as defined in the specification, or salts thereof exhibits synergistically improved anti-hypoxic activity when combined with a compound having an acetylcholine esterase inhibitory activity. Therefore, the combination according to the present invention is useful as a method for improving cerebral function. Further, a pharmaceutical composition containing the compound relating to the combination according to the present invention is useful for treatment and prevention of dysfunction of cerebral acetylcholine neurons in the sequelae of cerebrovascular dementia, senile dementia, Alzheimer's disease and ischemic cerebral lesion and in the cerebral apoplexy or the memory impairment caused by selective neuronal death.Type: GrantFiled: April 3, 2003Date of Patent: May 3, 2011Assignee: Toyama Chemical Co., Ltd.Inventors: Yasushi Nakada, Masaya Nakagawa, Satoshi Ono