Phosphorus Acid Ester Of Polyhydric Alcohol Or Thioalcohol (e.g., P-x-r-x-p Group, Etc., Wherein X Is Chalcogen And R Is The Residue Of The Polyhydric Alcohol Or Thioalcohol) Patents (Class 514/103)
  • Patent number: 9974770
    Abstract: The invention provides a pharmaceutical composition for intranasal administration comprising a salt of sumatriptan or a physiologically acceptable solvate thereof, an alkyl glycoside or saccharide alkyl ester and optionally at least one pharmaceutically acceptable excipient, wherein the said composition provides Tmax value of less than 30 minutes upon said administration. Other aspects and embodiments are contemplated and described. The invention also provides a pharmaceutical composition for intranasal administration comprising a triptan, a pharmaceutically acceptable vehicle and a mucosal permeation enhancer, wherein upon said administration said composition provides a Tmax substantially equivalent to subcutaneous administration of said triptan. Other aspects and embodiments are contemplated and described.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: May 22, 2018
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Rajesh Gandhi, Sreekanth Manikonda, Arun Jana, Sameer Shrinivas Kunte
  • Patent number: 9839695
    Abstract: The invention provides for preparing a polymer-active agent conjugate, the method comprising the steps of reacting an amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: December 12, 2017
    Assignee: Nektar Therapeutics
    Inventor: Antoni Kozlowski
  • Patent number: 9211282
    Abstract: The invention provides a pharmaceutical composition for intranasal administration comprising a salt of sumatriptan or a physiologically acceptable solvate thereof, an alkyl glycoside or saccharide alkyl ester and optionally at least one pharmaceutically acceptable excipient, wherein the said composition provides Tmax value of less than 30 minutes upon said administration. Other aspects and embodiments are contemplated and described. The invention also provides a pharmaceutical composition for intranasal administration comprising a triptan, a pharmaceutically acceptable vehicle and a mucosal permeation enhancer, wherein upon said administration said composition provides a Tmax substantially equivalent to subcutaneous administration of said triptan. Other aspects and embodiments are contemplated and described.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: December 15, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Rajesh Gandhi, Sreekanth Manikonda, Arun Jana, Sameer Shrinivas Kunte
  • Patent number: 9006279
    Abstract: The present disclosure relates to therapeutic compositions comprising substituted imidazoliums having multiple acidic groups. The compounds may be used to treat diseases or conditions such as those associated with bone, cancer, or pain. Compositions, dosage forms, methods of treating diseases or conditions, methods of preparation, and other related embodiments related to the substituted imidazoliums are also described herein.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: April 14, 2015
    Assignee: Antecip Bioventures II LLC
    Inventor: Herriot Tabuteau
  • Publication number: 20150080346
    Abstract: The present invention relates to a composition, in particular a cosmetic composition, comprising, in a physiologically acceptable medium, at least glyceryl caprylate, 1,3-propanediol and phytic acid or any of the salts thereof, said composition being free from perlite. The present invention further relates to a composition, in particular a cosmetic composition, comprising, in a physiologically acceptable medium, at least glyceryl caprylate, 1,3-propanediol and phytic acid or any of the salts thereof.
    Type: Application
    Filed: December 21, 2012
    Publication date: March 19, 2015
    Applicant: L'OREAL
    Inventors: Géraldine Lerebour, Catherine Marion
  • Publication number: 20140356423
    Abstract: The present invention provides a pharmaceutical formulation suitable for filling softgel capsules comprising: (a) from about 1% to about 90% by weight of a bisphosphonic acid or a pharmaceutically acceptable salt; (b) from 1% to about 99% by weight of lycopene and (c) from about 40% to about 80% by weight of a liquid carrier comprising 50% to 80% by weight polyethylene glycol; 5% to 15% by weight of glycerin; and 5% to 20% by weight water. The invention also describes a method for preparing alendronate or its pharmaceutical acceptable salts in encapsulated therapeutic dosage form in combination with lycopene.
    Type: Application
    Filed: May 28, 2013
    Publication date: December 4, 2014
    Inventor: Isaac A. Angres
  • Patent number: 8883201
    Abstract: The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: November 11, 2014
    Assignee: Merrion Research III Limited
    Inventor: Thomas W. I. Leonard
  • Patent number: 8835650
    Abstract: The present disclosure relates to therapeutic compositions comprising substituted imidazoliums having multiple acidic groups. The compounds may be used to treat diseases or conditions such as those associated with bone, cancer, or pain. Compositions, dosage forms, methods of treating diseases or conditions, methods of preparation, and other related embodiments related to the substituted imidazoliums are also described herein.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: September 16, 2014
    Assignee: Antecip Bioventures II LLC
    Inventor: Herriot Tabuteau
  • Publication number: 20140199261
    Abstract: Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.
    Type: Application
    Filed: July 25, 2013
    Publication date: July 17, 2014
    Applicants: Universite de Strasbourg, NormOxys, Inc.
    Inventors: Yves Claude Nicolau, Jean-Marie Lehn, Claudine Kieda
  • Publication number: 20140072571
    Abstract: Disclosed are methods of identifying subjects with osteoporosis or osteopenia, subjects at risk for developing osteoporosis, osteopenia, and bone fractures, methods of evaluating the effectiveness of osteoporosis treatments in subjects with osteoporosis or osteopenia, and methods of selecting therapies for treating osteoporosis or osteopenia, using biomarkers.
    Type: Application
    Filed: March 11, 2013
    Publication date: March 13, 2014
    Applicant: TETHYS BIOSCIENCE, INC.
    Inventors: Mickey S. Urdea, Michael P. McKenna, Patrick A. Arensdorf
  • Publication number: 20140038921
    Abstract: A pharmaceutical composition for treating tuberculotic diseases with no side effect/low side effect is provided by the present invention, which pharmaceutically effective amount of one or more compounds chosen from isoniazid, rifampin, pyrazinamide and ethambutol, and pharmaceutically effective amount of substances which can reduce the side effect of the antituberculosis agents.
    Type: Application
    Filed: April 20, 2011
    Publication date: February 6, 2014
    Applicant: NATIONAL DEFENSE EDUCATION AND RESEARCH FOUNDATION
    Inventors: Oliver Yaopu Hu, Tonho Young, Chenghuei Hsiong, Wenliang Chang, Tungyuan Shih, Hsintien Ho
  • Patent number: 8569269
    Abstract: The present invention discloses a method of treating, reducing the occurrence of, or improving the symptoms associated with a skin condition by topical application of a compound of formula (I) or a salt thereof, wherein said skin condition is selected from the group consisting of melanogenesis, oxidative damage, inflammation, skin irritation from inflammation, loss of cell adhesion, loss of desquamation, extra-cellular including connective tissue matrix breakdown and skin tone loss thereof, loss of keratinization, cellular senescence, skin aging from cellular senescence, loss of skin whiteness, loss of skin barrier function, loss of skin firmness, rosacea, skin wrinkles and fine lines from cellular senescence, cellular oxidation, loss of skin collagen, topical wounds, and combinations thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: October 29, 2013
    Assignee: Island Kinetics, Inc.
    Inventors: David Wayne Peter, John Dillon Stanek, Shyam K Gupta
  • Patent number: 8481692
    Abstract: In one aspect, the invention relates to an immunogenic composition that includes a mutant Clostridium difficile toxin A and/or a mutant Clostridium difficile toxin B. Each mutant toxin includes a glucosyltransferase domain having at least one mutation and a cysteine protease domain having at least one mutation, relative to the corresponding wild-type C. difficile toxin. The mutant toxins may further include at least one amino acid that is chemically crosslinked. In another aspect, the invention relates to antibodies or binding fragments thereof that binds to said immunogenic compositions. In further aspects, the invention relates to isolated nucleotide sequences that encode any of the foregoing, and methods of use of any of the foregoing compositions.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: July 9, 2013
    Assignee: Wyeth LLC
    Inventors: Maninder K. Sidhu, Annaliesa Sybil Anderson, Robert G. K. Donald, Kathrin Ute Jansen, Narender K. Kalyan, Justin Keith Moran, Mark E. Ruppen, Michael James Flint
  • Publication number: 20130090371
    Abstract: The present invention generally relates to compositions and kits comprising a ?2-AR agonist and a modulator of a ?2-AR regulator gene, where the modulator of the ?2-AR regulator gene inhibits the internalization and/or degradation of the ?2-ad-renergic receptor (?2-AR). More specifically, the present invention relates to the use of an agonist of ?2-adrenergic receptor (?2-AR) and an agent which inhibits agonist induced ?2-adrenergic receptor (?2-AR) internalization and/or degradation in method for the treatment of a respiratory disorder in a subject.
    Type: Application
    Filed: April 20, 2011
    Publication date: April 11, 2013
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventor: Quan Lu
  • Publication number: 20130005690
    Abstract: Provided herein are methods for ameliorating the pathophysiology cysteine protease exotoxin comprising the step of administering to said individual an effective dose of an S-nitrosylating agent and an inositol phosphate or analog thereof.
    Type: Application
    Filed: May 31, 2012
    Publication date: January 3, 2013
    Applicant: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Tor C. Savidge, Jonathan Stamler
  • Patent number: 8236292
    Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Grant
    Filed: June 6, 2005
    Date of Patent: August 7, 2012
    Assignee: Camurus AB
    Inventors: Krister Thuresson, Fredrik Tiberg, Markus Johansson, Ian Harwigsson, Fredrik Joabsson, Markus Johnsson
  • Patent number: 8236784
    Abstract: This application discloses compositions containing synthetic threitol phosphates, in particular threitol monophosphate, threitol-bis-phosphate, threitol diphosphate, and/or threitol triphosphate. The threitol phosphates are useful in treating wounds, for cosmetic applications, and for bone and periodontal regeneration.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: August 7, 2012
    Assignee: Sunny Biodiscovery, Inc.
    Inventors: Hui Zhao, Krzysztof Bojanowski, Fariba Aria, Reza Mortezaei
  • Patent number: 8236755
    Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one opioid bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: August 7, 2012
    Assignee: Camurus AB
    Inventors: Krister Thuresson, Fredrik Tiberg, Markus Johansson, Ian Harwigsson, Fredrik Joabsson, Markus Johnsson
  • Publication number: 20120189566
    Abstract: A pantethine phosphate ester represented by the following formula (1) or formula (2) exhibits superior tyrosinase inhibitory effect and melanin production inhibitory effect.
    Type: Application
    Filed: September 6, 2010
    Publication date: July 26, 2012
    Applicant: DAIICHI FINE CHEMICAL CO., LTD.
    Inventors: Koichi Wada, Koichi Sumi, Shihoko Shimomura
  • Publication number: 20120172337
    Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.
    Type: Application
    Filed: March 8, 2012
    Publication date: July 5, 2012
    Applicant: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20120148604
    Abstract: The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.
    Type: Application
    Filed: August 20, 2010
    Publication date: June 14, 2012
    Applicant: TRANSPOSAGEN BIOPHARMACEUTICALS, INC.
    Inventors: Eric M. Ostertag, John Stuart Crawford
  • Publication number: 20120128762
    Abstract: The present invention provides pharmaceutical compositions and methods for the instillation of lipid vehicles comprised of liposomes containing sphingomyelin or sphingomyelin metabolites to prevent, manage, ameliorate and/or treat disorders involving neuropathic pain and aberrant muscle contractions, such as what occurs in bladder hyperactivity disorders such as interstitial cystitis (IC) in animals or humans in need thereof. Also provided is a liposome-based delivery of drugs, e.g., antibiotics, pain treatments and anticancer agents, to the bladder, genitourinary tract, gastrointestinal system, pulmonary system and other organs or body systems. In particular, liposome-based delivery of vanilloid compounds, such as resiniferatoxin, capsaicin, or tinyatoxin and toxins, such as botulinum toxin is provided for the treatment of bladder conditions, including pain, inflammation, incontinence and voiding dysfunction.
    Type: Application
    Filed: January 13, 2012
    Publication date: May 24, 2012
    Inventors: Michael B. Chancellor, Pradeep Tyagi, Matthew O. Fraser, Yao-Chi Chuang, William C. de Groat, Leaf Huang, Naoki Yoshimura
  • Patent number: 8178514
    Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphosphate (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: May 15, 2012
    Assignee: Normoxys, Inc.
    Inventors: Yves Claude Nicolau, Jean-Marie Lehn, Konstantina C. Fylaktakidou, Ruth Greferath
  • Publication number: 20120021901
    Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from the class of the organophosphates or carbamates, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids.
    Type: Application
    Filed: March 25, 2009
    Publication date: January 26, 2012
    Applicant: BAYER CROPsCIENCE AG
    Inventors: Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
  • Publication number: 20120003327
    Abstract: Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.
    Type: Application
    Filed: February 23, 2011
    Publication date: January 5, 2012
    Inventors: Yves Claude NICOLAU, Jean-Marie LEHN, Claudine KIEDA
  • Publication number: 20110293595
    Abstract: A composition and method for the treatment of Alzheimer's Disease, and/or related protein aggregation diseases and/or amyloidoses and/or a neuro-degenerative disease, and/or Parkinson's Disease and/or Parkinsonism including an effective amount of a compound selected from the group consisting of phytic acid (inositol hexakisphosphate), a phytate salt, an isomer or hydrolysate of phytic acid or a phytate salt, or a mixture of any combination thereof, being administered to a person in an amount from about 0.5 grams to about 18.75 grams at least once a week up to once per day, with or without a dephosphorylating enzyme. The dosage may be proportionately or disproportionately divided so that the dosage is administered in proportionally or disproportionately reduced amounts which cumulatively add up to a predetermined dosage, in a time period where the proportionately or disproportionately divided dosages are cumulatively equivalent in quantity to the dosage.
    Type: Application
    Filed: August 9, 2011
    Publication date: December 1, 2011
    Inventor: Robert Sabin
  • Publication number: 20110281825
    Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphosphate (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.
    Type: Application
    Filed: February 10, 2011
    Publication date: November 17, 2011
    Applicant: Normoxys
    Inventors: Yves Claude NICOLAU, Jean-Marie LEHN, Konstantina FYLAKTAKIDOU, Ruth GREFERATH
  • Publication number: 20110165239
    Abstract: The present invention provides stable pharmaceutical compositions comprised of atorvastatin and sodium bicarbonate or L-arginine. The compositions are prepared as bulk drug compositions and also as oral dosage units, such as tablets or capsules. The compositions are useful for preparation of monolithic and bi-layer tablets containing atorvastatin as the only active agent or combined with one or more additional active agents. The compositions are useful for treating hypercholesterolemia and related conditions.
    Type: Application
    Filed: September 21, 2009
    Publication date: July 7, 2011
    Inventors: Laman Alani, Soumojeet Ghosh
  • Publication number: 20110091440
    Abstract: A composition and method for the treatment of Alzheimer's disease and related amyloid plaque development and reduction of amyloid plaque, amyloidosis and amyotrophic lateral sclerosis, as well as neuro-degenerative diseases and protein aggregation diseases, includes an effective amount of a compound selected from the group consisting of phytic acid (inositol hexakisphosphate), a phytate salt, an isomer or hydrolysate of phytic acid or a phytate salt, or a mixture of any combination thereof, being administered to a person in an amount from about 0.5 grams to about 18.75 grams per day, with or without a dephosphorylating enzyme.
    Type: Application
    Filed: September 27, 2010
    Publication date: April 21, 2011
    Inventor: Robert Sabin
  • Patent number: 7915238
    Abstract: The present invention is directed to methods of treating diseases and disorders related to immune responses by administering one or more immunomodulatory compounds. In particular, the invention is directed to methods of stimulating and reducing immune responses, therapeutic and prophylactic treatment of cancer, treating autoimmune conditions, treating allergic reactions and asthma, and preventing ischemic damage and asthma by administering one or more immunomodulatory compounds.
    Type: Grant
    Filed: April 26, 2006
    Date of Patent: March 29, 2011
    Assignee: Eisai R & D Management Co., Ltd.
    Inventors: Lynn D. Hawkins, Sally T. Ishizaka
  • Publication number: 20110003748
    Abstract: The present invention relates to the use of D-chiroinositol or a phosphate thereof in combination with folate for the reduction or prevention of congenital deformations such as anorectal malformations, neural tube defects, cleft-lip, cleft palate, and other birth defects. The invention further relates to the use of D-chiroinositol or a phosphate thereof in quieting or preventing the sensitivity of breast tissue to estrogenic, progestogenic, and or anti-androgenic insult, whether from environmental, dietary, or medicinal sources. Co-therapies as well as combination products of D-chiro-inositol (or a phosphate thereof) with at least one of (a) a folate source and (b) one or more of an estrogenic substance, a progestogenic substance, and/or an antiandrogenic substance are also claimed.
    Type: Application
    Filed: September 8, 2010
    Publication date: January 6, 2011
    Inventor: Barbara L. Jennings-Spring
  • Publication number: 20100323000
    Abstract: The invention provides novel methods for preparing cardiolipin and cardiolipin analogs having varying fatty acid chain lengths, particularly 1,1?,2,2?-tetramyristoyl cardiolipin. The methods comprise reacting a starting compound, such as a 1,2-O-sn-diacylglycerol and a 2-protected glycerol, with a phosphoramidite reagent to produce a protected cardiolipin, which is deprotected to prepare cardiolipin. The cardiolipin and cardiolipin analogs may be prepared in the presence of an activator, such as pyridinium trifluororacetate. The methods of the present invention are used to prepare cardiolipin and cardiolipin analogs in large quantities. The cardiolipin prepared by the present methods can be incorporated into liposomes which can also include active agents such as hydrophobic or hydrophilic drugs. Such liposomes can be used to treat diseases or in diagnostic and/or analytical assays.
    Type: Application
    Filed: February 22, 2007
    Publication date: December 23, 2010
    Applicant: NEOPHARM, INC.
    Inventors: Shoukath M. Ali, Moghis U. Ahmad, Imran Ahmad
  • Patent number: 7833993
    Abstract: The present invention is directed to methods of treating diseases and disorders related to immune responses by administering one or more immunomodulatory compounds. In particular, the invention is directed to methods of stimulating and reducing immune responses, treating autoimmune conditions, treating allergic reactions and asthma, and preventing ischemic damage and asthma by administering one or more immunomodulatory compounds.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: November 16, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Lynn D. Hawkins, Sally T. Ishizaka
  • Patent number: 7833992
    Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.
    Type: Grant
    Filed: April 30, 2003
    Date of Patent: November 16, 2010
    Assignee: Merck Sharpe & Dohme
    Inventors: Chandra Vargeese, Peter Haeberli, Weimin Wang, Tongqian Chen
  • Publication number: 20100286073
    Abstract: The present invention relates to compounds, as well as to compositions, methods and kits comprising such compounds, for use in the treatment or prophylaxis of fibromyalgia, chronic fatigue syndrome, myofascial pain syndrome, Gulf War syndrome and related conditions, wherein the compound is a fatty acid oxidation inhibitor and/or a carbohydrate oxidation activator.
    Type: Application
    Filed: October 3, 2008
    Publication date: November 11, 2010
    Inventor: Paul JENKINS
  • Publication number: 20100256209
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Application
    Filed: October 15, 2009
    Publication date: October 7, 2010
    Inventor: Jean-Louis Henri Dasseux
  • Publication number: 20100120720
    Abstract: The invention relates to the use of a hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor and of a farnesyl-pyrophosphate synthase inhibitor, or of one of their associated physiologically acceptable salts, in the preparation of a composition, particularly a pharmaceutical composition, for use in the treatment of human or animal, pathological or nonpathological situations related to the accumulation and/or the persistence of prenylated proteins in cells, such as during progeria (Hutchinson-Gilford syndrome), restrictive dermopathy or physiological aging.
    Type: Application
    Filed: July 5, 2007
    Publication date: May 13, 2010
    Applicant: UNIVERSITE DE LA MEDITERRANEE AIX-MAR SEILLE II
    Inventors: Nicolas Levy, Pierre Cau, Carlos Lopez-Otin
  • Publication number: 20100105637
    Abstract: The invention involves sustained-release pharmaceutical compositions containing a water-soluble ionic small molecule pharmaceutical agent complexed with an oppositely charged surfactant, particularly a natural bile surfactant. The complexes are sustained-release ionic complexes. The complexes release the ionic pharmaceutical agents into aqueous solution slowly and with zero-order kinetics. Thus, they can be formulated into sustained-release pharmaceutical compositions.
    Type: Application
    Filed: October 22, 2009
    Publication date: April 29, 2010
    Inventor: Cherng-ju Kim
  • Publication number: 20100092479
    Abstract: The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E).
    Type: Application
    Filed: August 17, 2009
    Publication date: April 15, 2010
    Applicant: CombinatoRx (Singapore) Pte. Ltd.
    Inventors: Lisa M. Johansen, Christopher M. Owens
  • Publication number: 20100069334
    Abstract: A method for prognosing osteoporosis phenotypes or estimating osteoporosis quantitative traits comprising determining outcomes for selected SNP variables and clinical variables. Products and methods for genotyping multiple osteoporosis associated genetic variations.
    Type: Application
    Filed: July 12, 2007
    Publication date: March 18, 2010
    Inventors: Ainara Cadaval, Diego Tejedor Hernández, Antonio Martínez Martínez, Laureano Simón Buela
  • Publication number: 20100062037
    Abstract: Subcutaneous implants obtained by extrusion containing an active ingredient dispersed in a PLGA matrix obtained by grinding an extruded product consisting of a blend of: at least two PLGA having different lactic acid/glycolic acid molar ratios and different weight average molecular weights, or a PLGA and PLA having different weight average molecular weight.
    Type: Application
    Filed: August 1, 2007
    Publication date: March 11, 2010
    Inventors: Patrice Mauriac, Pierre Marion
  • Publication number: 20100048511
    Abstract: Provided is a solid dispersion comprising vitamin D or a derivative thereof and a cyclodextrin; a complex formulation for the prevention or treatment of osteophorosis, which includes the solid dispersion and a bisphosphonate; and a method for preparing said complex formulation. The complex formulation can maintain a constant therapeutic level of vitamin D or a derivative thereof through its improved drug stability, while enhancing the patient compliance by minimizing inconvenience and adverse effects when administered to patients.
    Type: Application
    Filed: November 6, 2007
    Publication date: February 25, 2010
    Applicant: HANMI PHARM CO., LTD.
    Inventors: Jong Soo Woo, Hong Gi Yi, Ju Nam Jin
  • Publication number: 20100034752
    Abstract: The present invention provides for methods of administering by a pulmonary route a bisphosphonate active agent in combination with a pyrazolone derivative to a subject. Also provided are pharmaceutical compositions for use in practicing methods according to embodiments of the invention. The methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone absorption disease conditions.
    Type: Application
    Filed: December 9, 2008
    Publication date: February 11, 2010
    Inventors: Toru Hibi, Akira Yamamoto, Hidemasa Katsumi
  • Publication number: 20100028421
    Abstract: The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.
    Type: Application
    Filed: September 3, 2009
    Publication date: February 4, 2010
    Inventors: Kenneth I. Cumming, Zebunnissa Ramtoola
  • Publication number: 20100022480
    Abstract: The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.
    Type: Application
    Filed: June 10, 2009
    Publication date: January 28, 2010
    Inventor: Thomas W. I. Leonard
  • Publication number: 20090238876
    Abstract: A novel method of treating endometriosis is disclosed. The method comprises administering to a female subject in need thereof a therapeutically effective amount of particles comprising an agent capable of inhibiting phagocytic cells of the female subject.
    Type: Application
    Filed: February 16, 2006
    Publication date: September 24, 2009
    Inventors: Haim Danenberg, Morey Schachter, Gershon Golomb
  • Publication number: 20090197837
    Abstract: Disclosed is a liquid, oral dosage form comprising alendronic acid or pharmaceutically acceptable salts thereof, a process for the preparation of such liquid dosage forms, and use thereof.
    Type: Application
    Filed: February 4, 2009
    Publication date: August 6, 2009
    Inventors: Vivek S. Desai, Yogeeta Suresh Narkar
  • Publication number: 20090170815
    Abstract: The invention features an oral pharmaceutical solution comprising a therapeutically effective amount of alendronate or a salt thereof and a pharmaceutically acceptable liquid carrier. The solution is substantially free from degradation products, with the proviso that the solution has no buffer and no complexing agent. The oral solution avoids the difficulties in swallowing tablets of the prior art. Moreover, the oral solution is surprisingly stable without the use of buffering systems and complexing agents of the prior art.
    Type: Application
    Filed: December 23, 2008
    Publication date: July 2, 2009
    Applicant: ROXANE LABORATORIES INCORPORATED.
    Inventors: Veronica Anne SHANLINE, Eric Martin SPILLER
  • Publication number: 20090163447
    Abstract: The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject. The compositions include at least one alkyl glycoside and at least one therapeutic agent, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms.
    Type: Application
    Filed: December 22, 2008
    Publication date: June 25, 2009
    Inventor: Edward T. Maggio
  • Patent number: 7517858
    Abstract: Lipid prodrugs of pharmaceutical agents and their analogs that have increased anticancer, anti-viral, anti-inflammatory, anti-proliferative activity over the parent drug, and methods for making lipid prodrugs. Compositions comprising lipid prodrugs for treating disease and methods for treating disease which involve using the compositions.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 14, 2009
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, Ganesh D. Kini, James R. Beadle