Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/411)
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Publication number: 20120132204Abstract: An inhaler includes a first body member and a second body member fit closely together to form an inhaler body, and an outlet. The first body member has a medicament chamber containing a unit dose of powdered medicament. A seal such as a foil strip seals the medicament chamber and extends outwardly of the inhaler body. In use, one end of the seal can be grasped by a user and withdrawn, fully or partially, from the inhaler body, to release the powdered medicament from the medicament chamber. The second body member includes a medicament collection well in which the medicament is collected upon its release from the medicament chamber. The medicament collection well forms part of an airway connecting into the outlet. In use, air can be drawn by inhalation at the outlet to entrain the powder medicament in the collection well for inhalation by a user.Type: ApplicationFiled: February 9, 2012Publication date: May 31, 2012Applicant: INNOVATA BIOMED LIMITEDInventors: Samuel W. Lucking, Glen P. Martyn
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Patent number: 8188116Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.Type: GrantFiled: July 13, 2007Date of Patent: May 29, 2012Assignee: Vanderbilt UniversityInventors: Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby K. Wyatt
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Patent number: 8183388Abstract: The present invention relates to the compound of the formula: to pharmaceutical compositions comprising the compound of Formula (I); and to methods for treating or preventing hypogonadism, osteoporosis, osteopenia, sarcopenia, cachexia, muscle atrophy, sexual dysfunction or erectile dysfunction, comprising administering to a patient in need thereof an effective amount of the compound of Formula (I).Type: GrantFiled: November 10, 2010Date of Patent: May 22, 2012Assignee: Eli Lilly and CompanyInventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan
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Patent number: 8182464Abstract: Implant devices for intravesical administration and local drug delivery. The device has a body which includes a hollow tube formed of a biocompatible material; at least one reservoir in the tube which contains a drug; and one or more apertures through which the drug can be released. The device is configured for minimally invasive insertion into a body cavity, such as the bladder. The hollow tube may be elastomeric to permit the device to be elastically deformed from its initial shape into an elongated shape for passage through a catheter, where following such passage the device can return to or toward its initial shape to facilitate retention of the device in the body cavity. The body may have a narrow, elongated shape effective to permit insertion of the drug delivery device through a catheter without necessarily deforming the body, yet include flexible projections which effect retention within the body cavity.Type: GrantFiled: February 22, 2010Date of Patent: May 22, 2012Assignees: Massachusetts Institute of Technology, Children's Medical Center CorporationInventors: Heejin Lee, Karen Danielle Daniel, Hong Linh Ho Duc, Michael J. Cima, Mario Castillo, Steven Froelich, Jordan Dimitrakov, Grace Y. Kim
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Publication number: 20120122870Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.Type: ApplicationFiled: May 10, 2010Publication date: May 17, 2012Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
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Publication number: 20120121720Abstract: This present invention relates to methods, compositions, and kits useful for treating a patient having or at risk for developing a disorder associated with decreased expression of ?2 adrenergic receptors or need for increased 132 adrenergic receptor activity.Type: ApplicationFiled: March 31, 2010Publication date: May 17, 2012Inventors: Jonathan S. Stamler, Liang Xie
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Publication number: 20120114751Abstract: The present invention relates to a granular pharmaceutical composition comprising an HCV protease inhibitor and at least one poloxamer.Type: ApplicationFiled: November 8, 2011Publication date: May 10, 2012Inventors: Andreas Leiminer, Kai Lindenstruth, Dave Alan Miller, Emmanuel Scheubel, Navnit Hargovindas Shah
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Publication number: 20120114740Abstract: Disclosed are formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs which minimize the side effects of unencapsulated non-steroidal anti-inflammatory drugs while maintaining or improving efficacy. Methods of making and administering the formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs and their use as medicaments are also provided.Type: ApplicationFiled: October 27, 2011Publication date: May 10, 2012Applicant: PACIRA PHARMACEUTICALS, INCInventors: Louie Daniel Garcia, Liangjin Zhu, William Joseph Lambert, Gary Patou
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Publication number: 20120115897Abstract: The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children.Type: ApplicationFiled: December 24, 2009Publication date: May 10, 2012Applicants: WUXI HONGRUI BIO-PHARMA-TECH CO., LTD .Inventors: Luhong Tang, Ajuan Dai, Ze Wang, Yang Sun, Xinning Liu, Lingyan Xu, Xin Fang, Shuang Qiu, Yaqing Cao, Xiaomin Xu, Ruixia Jiang, Chao Wu
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Publication number: 20120115921Abstract: Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.Type: ApplicationFiled: January 19, 2012Publication date: May 10, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Carl Berthelette, Nicolas Lachance, Lianhai Li, Claudio Sturino, Zhaoyin Wang
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Patent number: 8173678Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: GrantFiled: October 25, 2010Date of Patent: May 8, 2012Assignee: Research Triangle InstituteInventors: Frank Ivy Carroll, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
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Publication number: 20120101067Abstract: Described herein are methods for improving engraftment of hematopoietic cells in an individual following hematopoietic progenitor cell transplantation (e.g., via bone marrow or cord blood transplantation). Methods for increasing hematopoietic progenitor cell proliferation in individuals with bone marrow aplasia are also described. The methods involve administering an agent that inhibits adipogenesis, adipocyte growth, adipocyte differentiation and/or adipocyte proliferation.Type: ApplicationFiled: April 15, 2010Publication date: April 26, 2012Applicant: CHILDREN'S MEDICAL CENTER CORPORATIONInventors: Olaia Naveiras, George Daley, Pamela L. Wenzel
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Publication number: 20120093938Abstract: The compositions of the present invention comprise a therapeutically effective amount of particles consisting of diphenhydramine or pharmaceutically acceptable salts thereof, optionally in combination with another drug such as pseudoephedrine, or phenylephrine and hydrocodone, in combination with rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol and/or a saccharide. These compositions are useful in treating the symptoms of one or more diseases or conditions in which diphenhydramine (alone or in combination with one or two other drugs) is a therapeutically effective, e.g. allergic rhinitis, sinusitis, upper respiratory tract infections, motion sickness, Parkinson's disease, insomnia, the common cold, and nighttime pain management, particularly for subjects or patients with dysphagia, and people ‘on the move’.Type: ApplicationFiled: July 14, 2011Publication date: April 19, 2012Applicant: EURAND INC.Inventors: Gopi M. VENKATESH, Jin-Wang LAI, Phillip PERCEL, Craig KRAMER
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Publication number: 20120095004Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: ApplicationFiled: October 19, 2011Publication date: April 19, 2012Applicant: APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Kevin J. French, Yan Zhuang
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Patent number: 8158670Abstract: Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell, coupled to a therapeutic agent dosage form that inhibits a cellular activity of the muscle cell. Methods are also provided for the direct and/or targeted delivery of therapeutic agents to vascular smooth muscle cells that cause a dilation and fixation of the vascular lumen by inhibiting smooth muscle cell contraction, thereby constituting a biological stent.Type: GrantFiled: January 4, 2007Date of Patent: April 17, 2012Assignee: Boston Scientific Scimed, Inc.Inventors: Lawrence L. Kunz, Peter G. Anderson
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Patent number: 8148546Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.Type: GrantFiled: April 25, 2008Date of Patent: April 3, 2012Assignee: AEterna Zentaris GmbHInventors: Tilmann Schuster, Klaus Paulini, Peter Schmidt, Silke Baasner, Emmanuel Polymeropoulos, Eckhard Guenther, Michael Teifel
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Publication number: 20120077869Abstract: Phosphotyrosine phosphatase (PTP) encoded by PF13_0027 is a desirable drug target for the human malaria parasite Plasmodium falciparum. This PTP is critical for intraerythrocytic parasite development and invasion of erythrocytes by malaria merozoites. Mutation of the PF13_0027 gene or blocking expression of PTP function to create a PTP-null parasite severely attenuates the malaria parasite's ability to survive, making the PTP-null parasite suitable as an attenuated blood-stage parasite vaccine.Type: ApplicationFiled: September 20, 2011Publication date: March 29, 2012Applicant: UNIVERSITY OF SOUTH FLORIDAInventors: John H. Adams, Bharath Balu, Steven P. Maher, Christopher O. Campbell, Roman Manetsch
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Patent number: 8143303Abstract: Carbazole derivatives of formula (I), useful in treatment of a CNS disorders related to or affected by the 5-HT6 receptor are described. The pharmacological profile of these compounds includes high affinity binding with 5-HT6 receptor along with good selectivity towards the receptor. Stereoisomers, the salts, methods of preparation and medicines containing the carbazole derivatives are also described.Type: GrantFiled: June 9, 2006Date of Patent: March 27, 2012Assignee: Suven Life Sciences LimitedInventors: Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Vikas Shreekrishna Shirsath, Jagadish Babu Konda, Santosh Vishwakarma, Venkateswarlu Jasti
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Patent number: 8143304Abstract: The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.Type: GrantFiled: August 2, 2007Date of Patent: March 27, 2012Assignee: Actelion Pharmaceutical Ltd.Inventors: Heinz Fretz, Julien Pothier, Philippe Risch
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Publication number: 20120071423Abstract: Disclosed are heterotricyclic compounds, pharmaceutical compositions, methods of treatment, and methods for selectively antagonizing a glutamate receptor. The pharmaceutical compositions may include and the methods may utilize heterotricyclic compounds that are glutamate analogues which have specificity for AMPA receptors. The pharmaceutical compositions may be utilized to treat or prevent neurological diseases or disorders.Type: ApplicationFiled: March 21, 2011Publication date: March 22, 2012Applicant: NORTHWESTERN UNIVERSITYInventors: Geoffrey T. Swanson, Martin B. Gill, Ryuichi Sakai, Masato Oikawa
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Publication number: 20120071510Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.Type: ApplicationFiled: November 9, 2011Publication date: March 22, 2012Applicant: MANNKIND CORPORATIONInventors: Andrea Leone-Bay, Grayson W. Stowell, Joseph J. Guarneri, Dawn M. Carlson, Marshall Grant, Chad C. Smutney
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Patent number: 8138170Abstract: The present invention provides compositions and methods comprising ningalins for use in modulating immune responses to infection, injury, allergy and/or transplantation.Type: GrantFiled: August 29, 2005Date of Patent: March 20, 2012Assignee: Memorial Sloan-Kettering Cancer CenterInventor: Ting-Chao Chou
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Publication number: 20120058996Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: November 9, 2011Publication date: March 8, 2012Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Publication number: 20120052118Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.Type: ApplicationFiled: July 18, 2011Publication date: March 1, 2012Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
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Patent number: 8124644Abstract: The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof.Type: GrantFiled: May 8, 2009Date of Patent: February 28, 2012Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Sigalit Levi
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Publication number: 20120046237Abstract: Compositions for protection against SVFS induced by niacin, a carcinoid, mesenteric traction, serotonin, post-menopause, alcohol, monosodium glutamate, mastocytosis, atopic dermatitis, food-allergy or food intolerance, and mast cell activation syndrome, or against individual symptoms of SVFS, superficial vasodilation, feeling of warmth, itching (pruritus) and hives, comprising a flavonoid compound of the structure 2-phenyl-4H-1-benzopyran or 2-phenyl-4-keto-1-benzopyran or glycosides thereof, or chalconoid compounds, with appropriate substitutions of their hydroxyl groups to render them water soluble or in combination with a pshospholipid or cyclodextrin to render them to have higher oral absorption, administered alone or together with an anti-superficial vasodilation dose of one or more of, olive kernel oil, a serotonin inhibitor, a prostaglandin inhibitor, willow bark extract.Type: ApplicationFiled: May 20, 2011Publication date: February 23, 2012Inventor: Theoharis C. THEOHARIDES
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Publication number: 20120046251Abstract: The invention discloses methods of using cis-epoxyeicosantrienoic acids (“EETs”), inhibitors of soluble epoxide hydrolase (“sEH”), or a combination of an EET and an inhibitor of sEH, to reduce or prevent niacin-induced cutaneous vasodilation (“flushing”) in subjects suffering from this undesirable side effect of receiving therapeutic amounts of niacin.Type: ApplicationFiled: April 5, 2010Publication date: February 23, 2012Applicant: The Regents of the University of CaliforniaInventors: Saul Schaefer, Bruce D. Hammock, Ahmet Bora Inceoglu
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Publication number: 20120041044Abstract: The present invention relates to a process for the preparation of carvedilol as well as of the optically active R and S enantiomers thereof and of mixtures of these enantiomers and, more particularly, relates to an improved process for the preparation of carvedilol and its enantiomers characterized by the use of ethyl acetate as reaction solvent.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Applicant: ZACH SYSTEM S.P.A.Inventors: Elisenda Trepat Guixer, Anna Munoz Alvarez, Marta Pomares Marco, Francisco Marquillas Olondriz
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Publication number: 20120039804Abstract: The compounds of the invention are modulators of cannabinoid receptors CB1 or CB2. The compounds can be used for the prevention or treatment of, e.g., pain, cancer, skin diseases, weight-associated disorders, chemical addictions, psychiatric disorders, neurodegenerative disorders, bone diseases, and inflammatory diseases. The compounds of the invention can further be used to study these diseases and disorders, as well as cannabinoid receptor biology, by coupling the compounds to, e.g., imaging agents.Type: ApplicationFiled: June 6, 2011Publication date: February 16, 2012Inventors: Philippe Diaz, Fanny Diaz, Ravil Rashitovich Petrov
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Patent number: 8114900Abstract: The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof.Type: GrantFiled: May 8, 2009Date of Patent: February 14, 2012Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Santiago Ini, Sigalit Levi, Mili Abramov, Eran Turgeman
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Patent number: 8110596Abstract: The present invention provides a triprenyl phenol compound represented by the following formula (II) and (III) and having a thrombolysis-enhancing activity, and an efficient method for producing the triprenyl phenol compound. In formula (II) and (III), R1 represents an aromatic group having as a substituent or as a part of a substituent at least one member selected from the group consisting of a carboxyl group, a hydroxyl group, a sulfonic acid group and a secondary amino group, or an aromatic group which comprises a secondary amino group and may comprise nitrogen; R4 in the general formula (III) represents an aromatic amino acid residue represented by the general formula (III-1) below; X represents —CHY—(CH3)2Z; and Y and Z are respectively —H or —OH or together form a single bond: (III-1) wherein R5 represents a hydroxyl group which may be present or absent; and n represents an integer of 0 or 1.Type: GrantFiled: March 20, 2007Date of Patent: February 7, 2012Assignee: Tokyo University of Agriculture and Technology TLO Co., Ltd.Inventors: Keiji Hasumi, Yoshikazu Kitano, Hideo Ohishi, Haruki Koide, Keiko Hasegawa, Ritsuko Narasaki
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Publication number: 20120028944Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.Type: ApplicationFiled: January 27, 2011Publication date: February 2, 2012Applicant: OCULIS EHFInventors: Thorsteinn Loftsson, Einar Stefansson
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Publication number: 20120027721Abstract: The present invention is directed to a combination product for treating or ameliorating hepatitis C virus (HCV) infection or disorders or symptoms associated therewith in a subject in need thereof comprising, a HCV inhibitor and one or more therapeutic agents selected from either or both a HCV protease inhibitor and one or more different therapeutic agents administered in combination in an effective amount to the subject.Type: ApplicationFiled: April 6, 2010Publication date: February 2, 2012Applicant: PTC THERAPEUTICS, INC.Inventor: Zhengxian Gu
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Publication number: 20120022096Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: July 7, 2011Publication date: January 26, 2012Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Publication number: 20120021989Abstract: The invention relates to procedures and methods of determining a susceptibility to cardiac arrhythmia, including Atrial Fibrillation, Atrial Flutter and Stroke, by assessing the presence or absence of alleles at polymorphic markers found to be associated with risk of these conditions. The invention further relates to kits encompassing reagents for assessing such markers, and diagnostic 5 methods, uses and procedures for utilizing such susceptibility markers.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: deCODE Genetics ehf.Inventors: Hilma Holm, Daniel Gudbjartsson
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Patent number: 8101781Abstract: The present invention relates to a process for the efficient preparation of highly optical pure chiral carvedilol. According to the present invention, a chiral oxazolidin-2-one or oxazolidin-2-thione having formula 2, produced from the reaction of N-protected 2-(2-methoxyphenoxy)ethylamine with a chiral glycidol derivative is used as a key intermediate for the preparation of the chiral carvedilol. Specifically, the process for the preparation of the chiral carvedilol comprises a) reacting a compound of formula 2 with a halogenation agent, a sulfonation agent or a mitsunobu reagent to activate a hydroxyl group of the compound of formula 2, followed by nucleophilic substitution reaction with 9H-4-hydroxy carbazole to produce a compound of formula 7, and b) subjecting the obtained compound of formula 7 to a deprotection reaction in a presence of an inorganic base to produce the targeted chiral carvedilol. The process of the present invention can be accomplished in a mild condition.Type: GrantFiled: August 31, 2006Date of Patent: January 24, 2012Assignees: AHN-Gook Pharmaceutical Co., Ltd., RSTech CorporationInventors: Seong-Jin Kim, Chang Woo Jong, Hyun Bin Kang, Byung Hyun Moon, Long Guo Quan, Duk Kwon Won, Kyung Yong Jin
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Publication number: 20120015943Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmacuticals, Inc.Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
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Patent number: 8097642Abstract: Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell, coupled to a therapeutic agent dosage form that inhibits a cellular activity of the muscle cell. Methods are also provided for the direct and/or targeted delivery of therapeutic agents to vascular smooth muscle cells that cause a dilation and fixation of the vascular lumen by inhibiting smooth muscle cell contraction, thereby constituting a biological stent.Type: GrantFiled: February 27, 2007Date of Patent: January 17, 2012Inventors: Lawrence L. Kunz, Peter G. Anderson
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Publication number: 20120010125Abstract: Compounds and pharmaceutical compositions containing such compounds having formula I are provided: where R1, R2a, R2b, R3, R4, and R5 are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including anxiety and mood disorders such as depression.Type: ApplicationFiled: April 19, 2011Publication date: January 12, 2012Inventors: Eric A. Stone, Yan Lin, David Quartermain, Yasmeen Sarfraz
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Patent number: 8093283Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.Type: GrantFiled: November 12, 2010Date of Patent: January 10, 2012Assignee: Celgene CorporationInventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge, Jean Xu
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Publication number: 20120003316Abstract: This invention relates to a multi-configured, transmucosal pharmaceutical dosage form and, more particularly, to a pharmaceutical dosage form which has a single monolithic/heterogeneous layer or a plurality of such layers. The dosage form is suitable for the delivery of one or more pharmaceutical compositions via the buccal, sublingual, rectal, vaginal or transmucosal delivery route in a human or animal body. It provides for selected delivery profiles resulting from, but not limited to, a porosity-enabled composite matrix of one or more layers/components of the pharmaceutical composition/s. The invention also provides for a method of manufacturing said transmucosal pharmaceutical dosage form in a plurality of configurations.Type: ApplicationFiled: June 3, 2009Publication date: January 5, 2012Inventors: Deshika Reddy, Oluwatoyin Ayotomilola Adeleke, Viness Pillay, Yahya Choonara
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Publication number: 20120004224Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.Type: ApplicationFiled: June 29, 2011Publication date: January 5, 2012Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elisc Rioux, Sasmita Tripathy, Terrance W. Deyle
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Publication number: 20110319462Abstract: The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides.Type: ApplicationFiled: October 6, 2009Publication date: December 29, 2011Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Jürgen Benting, Peter Dahmen, Arnd Voerste, Ralf Dunkel, Stefan Hillebrand, Klaus-Günther Tietjen, Stephane Brunet
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Publication number: 20110319399Abstract: An external preparation containing the following components (A) and (B): (A) a non-steroidal analgesic/anti-inflammatory agent, and (B) an organic amine. The external preparation of the present invention has improved skin permeation and excellent stability of a non-steroidal analgesic/anti-inflammatory agent in the external preparation. The external preparation of the present invention also has excellent appearance.Type: ApplicationFiled: March 11, 2010Publication date: December 29, 2011Applicant: KOWA CO., LTD.Inventors: Seiji Miura, Tsutomu Awamura, Yuhiro Yamazaki, Hironari Fujii
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Publication number: 20110318351Abstract: Improved methods for treatment of cancer which involve the targeting of slow-growing, relatively mutationally-spared cancer stem line are provided. These methods are an improvement over previous cancer therapeutic methods because they provide for very early cancer treatment and reduce the likelihood of clinical relapse after treatment.Type: ApplicationFiled: September 12, 2011Publication date: December 29, 2011Inventor: Ivan Bergstein
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Patent number: 8084620Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: GrantFiled: December 17, 2009Date of Patent: December 27, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Publication number: 20110312918Abstract: The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein.Type: ApplicationFiled: December 8, 2009Publication date: December 22, 2011Applicant: Children's Hospital Medical CenterInventor: Rashmi Hegde
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Publication number: 20110311455Abstract: A nano-capsule construct for imaging and therapeutic uses and method for production are provided. One nano-probe embodiment based on genome-depleted plant brome mosaic virus (BMV) whose interior is doped with indocyanine green (ICG), an FDA-approved near infrared fluorescent dye, is used to illustrate the invention. The material encapsulated in viral shell components may be coated with functionalized coatings such as branched, dendritic polymer coatings to improve longevity and distribution in the body as well as antibody conjugation for increased target specificity. The constructs can also be coated with ferromagnetic iron oxide nanoparticles, enabling the ICG-containing capsules to be used as nano-probes with the capability of being detected in both optical and magnetic resonance imaging. The capsules may be produced by purifying a plant or animal viruses and disassembling the viruses to provide virus shell components.Type: ApplicationFiled: June 8, 2011Publication date: December 22, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: Bahman Anvari
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Publication number: 20110305661Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.Type: ApplicationFiled: October 5, 2009Publication date: December 15, 2011Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
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Patent number: 8076348Abstract: [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.Type: GrantFiled: August 7, 2006Date of Patent: December 13, 2011Assignee: Astellas Pharma Inc.Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada