Nitrogen Containing Hetero Ring Patents (Class 514/176)
  • Publication number: 20140079636
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Publication number: 20140080769
    Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Applicants: The Chancellor, Masters and Scholars of the University of Oxford, The Government of the United States of America, as represented by the Secretary, Department of Healt
    Inventors: Frances Mary Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
  • Publication number: 20140069419
    Abstract: Glucocorticosteroids that are derivatives of isoxazolidine are useful as anti-inflammatory and antiallergic compounds of the glucocorticosteroid series.
    Type: Application
    Filed: August 12, 2013
    Publication date: March 13, 2014
    Applicant: Chiesi farmaceutici S.p.A.
    Inventor: Eleonora GHIDINI
  • Patent number: 8664210
    Abstract: New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
    Type: Grant
    Filed: September 18, 2008
    Date of Patent: March 4, 2014
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Giuseppe Bianchi, Giorgio Fedrizzi, Patrizia Ferrari, Mauro Gobbini, Marco Torri, Giuseppe Marazzi, Walter Cabri
  • Patent number: 8653054
    Abstract: Novel chemical agents are described herein. More specifically, 2-(N-substituted piperazinyl) pregnane and 2-(N-substituted piperazinyl) androstane derivatives exhibiting cytotoxicity on a variety of cancer cell lines are disclosed herein.
    Type: Grant
    Filed: November 25, 2009
    Date of Patent: February 18, 2014
    Assignee: Universite Laval
    Inventors: Donald Poirier, Jenny Roy, Rene Maltais
  • Publication number: 20140045804
    Abstract: A topical cream to be applied to the clitoris and hood of the vaginal area to create an intense libido and drive for orgasm. The cream comprises a base cream having from about 9.5% to about 10%, by volume, of a steroid, based upon the total volume of the cream. Preferably, at least about 1% to about 10% by volume, of the steroid, based on the total volume of the cream. The topical cream may, also, include from about 0.1% to about 2.0%, by volume, of oxytocin. The addition of the small amount thereof enhances the efficacy of the cream.
    Type: Application
    Filed: January 21, 2013
    Publication date: February 13, 2014
    Inventor: Edward M. Lichten
  • Publication number: 20140030340
    Abstract: A method for preparing poorly water soluble drug particles is disclosed. The method comprises dissolving a drug in at least one organic solvent to form a drug/organic mixture, spraying the drug/organic mixture into an aqueous solution and concurrently evaporating the organic solvent in the presence of the aqueous solution to form an aqueous dispersion of the drug particles. The resulting drug particles are in the nanometer to micrometer size range and show enhanced dissolution rates and reduced crystallinity when compared to the unprocessed drug. The present invention additionally contemplates products and processes for new drug formulations of insoluble drug particles having high dissolution rates and extremely high drug-to-excipient ratios.
    Type: Application
    Filed: October 3, 2013
    Publication date: January 30, 2014
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Keith P. Johnston, Robert O. Williams, III, Xiaoxia Chen
  • Publication number: 20140031326
    Abstract: The invention relates to methods for the treatment of fibromyalgia and chronic fatigue syndrome by administration of a transdermally applied androgen composition. The treatment is both safe and effective for treating fibromyalgia-related pain and fatigue, as well as chronic fatigue syndrome.
    Type: Application
    Filed: November 17, 2011
    Publication date: January 30, 2014
    Applicant: WHITE MOUNTAIN PHARMA. INC.
    Inventors: Hillary D. White, Robert Gyurik
  • Patent number: 8637662
    Abstract: Novel glucocorticosteroids that are derivatives of isoxazolidine are useful as anti-inflammatory and antiallergic compounds.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: January 28, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta Armani, Eleonora Ghidini, Ilaria Peretto, Andrea Virdis
  • Publication number: 20140018337
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Application
    Filed: September 16, 2013
    Publication date: January 16, 2014
    Applicant: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20140018336
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Application
    Filed: September 16, 2013
    Publication date: January 16, 2014
    Applicant: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20140011786
    Abstract: Disclosed are the general structural formula of LQC-Y as well as the synthesis and use thereof. Pharmacological experiments demonstrated the marked antitumor effect of such compounds. Single day administration of LQC-Y3 to mice at a maximum dose of 6000 mg/kg showed no toxicity response during the 14-day continuous observation period, indicating the high safety of the compounds, and the compounds can be used to prepare medicaments for preventing and treating carcinomas such as liver cancer, lung cancer.
    Type: Application
    Filed: September 4, 2013
    Publication date: January 9, 2014
    Inventor: Haimin Lei
  • Publication number: 20140005156
    Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.
    Type: Application
    Filed: August 28, 2013
    Publication date: January 2, 2014
    Applicant: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)
    Inventors: MARC POIROT, PHILIPPE DE MEDINA, SANDRINE POIROT
  • Publication number: 20140005132
    Abstract: The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase ?4 and are useful as contraceptive agents.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 2, 2014
    Applicants: REGENTS OF THE UNIVERSITY OF MINNESOTA, THE UNIVERSITY OF KANSAS
    Inventors: Gustavo Blanco, Gunda I. Georg, Shameem Sultana Syeda
  • Publication number: 20130336996
    Abstract: A conjugated compound of formula Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a lipid covalently linked to an amino acid or peptide coupled to a polyamine group, and a process for the manufacture of the conjugated compound, as well as a complex formed between the conjugated compound and a polyanionic molecule and a pharmaceutical composition containing the conjugated compound or complex. Also described is the use of the conjugated compound or complex in the treatment of infection, cancer or immune disorders or for use in vaccines.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 19, 2013
    Applicant: CAYLA
    Inventors: Fabienne VERNEJOUL, Arnaud DEBIN, Daniel DROCOURT, Eric PEROUZEL, Gerard TIRABY, Thierry LIOUX
  • Publication number: 20130316995
    Abstract: The invention relates to fatty acid statin conjugates and fatty acid FXR agonist conjugates; compositions comprising an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate; and methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate.
    Type: Application
    Filed: May 1, 2013
    Publication date: November 28, 2013
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventor: Catabasis Pharmaceuticals, Inc.
  • Patent number: 8586568
    Abstract: The present invention relates to the treatment of diseases and conditions with an effective amount of a steroid having those formulas given in the specification, or a pharmacologically-acceptable salt or ester thereof. The disease or conditions treatable according to the invention include angiogenic diseases and conditions of the eye, angiogenic diseases and conditions of the brain, inflammatory diseases and conditions of the eye, inflammatory diseases and conditions of the brain and neurodegenerative diseases.
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: November 19, 2013
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Patent number: 8586569
    Abstract: The present invention relates to betulonic and betulinic acid derivatives and, in particular, to C-28 and C-3 derivatives. The present invention relates to betulonic acid esters, dihydro-betulonic acid esters, PAG-modified betulinic acid derivatives, and PAG-modified dihydro-betulinic acid derivatives. Betulinic acid and derivatives thereof may be bound to a poly(alkylene glycol) (PAG) such as poly(ethylene glycol). Binding may be via a linker, such as a diamine, an amino acid, a peptide, an ester or a carbonate. The compounds of the present invention may be used for the treatment of cancer or a viral infection. The present invention also provides pharmaceutical compositions comprising the compounds of the present invention. The present invention further provides processes for the preparation of the compounds of the present invention, for example, from betulin.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: November 19, 2013
    Inventors: Jean-Claude Leunis, Emmanuel Couche
  • Publication number: 20130303500
    Abstract: The invention features compounds, pharmaceutical compositions and methods useful for the treatment of neoplasia. In particular embodiments, the compounds of the invention are useful for the treatment of multidrug resistant neoplasia.
    Type: Application
    Filed: July 29, 2011
    Publication date: November 14, 2013
    Applicant: Medexis S.A.
    Inventors: Konstantinos Alevizopoulos, Theodora Calogeropoulou
  • Publication number: 20130280391
    Abstract: Disclosed herein are anti-microbial wash compositions and methods for using such compositions in controlling microbe growth on a non-meat food product (e.g., fruits, vegetables, grains, eggs, etc.) by applying or contacting the anti-microbial wash composition with a surface of the food product to kill microbes (e.g., bacteria) on a surface of the food product. The anti-microbial wash compositions include a ceragenin compound dispersed in a fluid carrier. The ceragenin compound includes a sterol backbone and a number of cationic groups attached to the sterol backbone. The cationic groups may be attached to the sterol backbone by a hydrolysable linkage so that the ceragenin compound has a relatively short half life (e.g., less than about 40 days), and the wash composition may be applied prior to shipping and washed off after shipping to minimize any ceragenin compound residue.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 24, 2013
    Applicant: BRIGHAM YOUNG UNIVERSITY
    Inventor: Paul B. Savage
  • Publication number: 20130252930
    Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: December 16, 2011
    Publication date: September 26, 2013
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Publication number: 20130251804
    Abstract: A method to improve the safety of handling of drug substances that are dispensed as solid oral dosage forms is described that does not alter the drug-release profile and the therapeutic efficacy of the pharmaceutical product.
    Type: Application
    Filed: March 21, 2013
    Publication date: September 26, 2013
    Applicant: Emphascience, Inc.
    Inventors: Rebanta Bandyopadhyay, Susen Werle
  • Publication number: 20130243840
    Abstract: A composite that includes a polymeric material having a void structure and particulate ceragenin material (i.e., ceragenin particles) associated with the void structure. The average particle size of the ceragenin particles in the composite is in a range from 5 nm to 20 ?m, 50 nm to 10 ?m, 100 nm to 5 ?m, or 1 ?m to 10 ?m. The composite has a high loading of ceragenin particles (e.g., about 10% to about 25%, by weight). The composite has good polymer stability, the ability to release ceragenins from the ceragenin particles disposed in the composite over a sustained period of time at a characteristic elution rate, and the ability to kill large numbers of bacteria and other susceptible microbes over the sustained period of time.
    Type: Application
    Filed: August 24, 2012
    Publication date: September 19, 2013
    Inventors: Paul B. Savage, Carl Genberg
  • Patent number: 8536160
    Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: September 17, 2013
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Giorgio Fedrizzi, Alessandra Benicchio, Giuseppe Bianchi, Patrizia Ferrari, Mauro Gobbini, Rosamaria Micheletti, Marco Pozzi, Piero Enrico Scotti
  • Publication number: 20130237507
    Abstract: The present invention provides compounds of formula (1) wherein n, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: April 17, 2013
    Publication date: September 12, 2013
    Inventors: Frank Burkamp, Balint Gabos, Svetlana Ivanova, Alice Ingrid Annea Lisius
  • Patent number: 8524654
    Abstract: Provided herein are methods for reducing or preventing neutrophilic inflammation in a subject comprising selecting a subject with or at risk for neutrophilic inflammation and administering to the subject an agent that inhibits the expression or activity of prolyl endopeptidase. Provided herein are also methods for treatment or prevention of diseases associated with neutrophilic inflammation.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: September 3, 2013
    Assignee: The UAB Research Foundation
    Inventors: J. Edwin Blalock, Uros V. Djekic, Patricia L. Jackson, Amit Gaggar, Brett Noerager, Philip J. O'Reilly
  • Patent number: 8524694
    Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: September 3, 2013
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Marc Poirot, Philippe De Medina, Sandrine Poirot
  • Patent number: 8518934
    Abstract: The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: June 11, 2009
    Date of Patent: August 27, 2013
    Assignee: Shonogi & Co., Ltd.
    Inventor: Hidenori Mikamiyama
  • Publication number: 20130210785
    Abstract: This disclosure relates to progesterone derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation resulting from traumatic brain injury or stroke.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 15, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: Emory University
  • Publication number: 20130210787
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: February 6, 2013
    Publication date: August 15, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130184245
    Abstract: A pharmaceutical composition comprises at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprises danazol in an amount of about 3% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days. The composition is useful for intravaginal administration to treat a condition such as endometriosis for which danazol is indicated.
    Type: Application
    Filed: January 3, 2013
    Publication date: July 18, 2013
    Applicant: DRUGTECH CORPORATION
    Inventor: DRUGTECH CORPORATION
  • Patent number: 8481517
    Abstract: The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of pyrrolidine.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: July 9, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Eleonora Ghidini, Andrea Rizzi, Andrea Virdis, Fabio Rancati, Anna Rencurosi
  • Publication number: 20130156705
    Abstract: Bivalent multifunctional A? oligomerization inhibitors (BMAOIs) that target multiple risk factors involved in Alzheimer's disease are provided. The BMAOIs are useful for the treatment and/or prevention of Alzheimer's disease, as well as for diagnostic imaging of A? plaques in brain tissue. The BMAOIs comprise i) an A? oligomer (ApO)-inhibitor moiety which may have antioxidant activity (e.g. curcumin, curcumin derivatives, curcumin hybrids, resveratrol, etc.); ii) a cell membrane/lipid raft (CM/LR) anchoring moiety (e.g. cholesterol, cholesterylamine, a steroid, etc.
    Type: Application
    Filed: July 14, 2011
    Publication date: June 20, 2013
    Applicant: Virginia Commonwealth University
    Inventors: Shujin Zhang, Tai Liang Guo
  • Publication number: 20130150336
    Abstract: Provided are methods and compositions for reducing superoxide anions such that a prophylactic or therapeutic effect against conditions associated with excess oxidative stress achieved. The compositions and methods provide for reducing inflammation and for enhancing lifespan of eukaryotic organisms. A screen for identifying compounds that can be used in these methods is also provided.
    Type: Application
    Filed: March 24, 2011
    Publication date: June 13, 2013
    Applicants: STC.UNM, HEALTH RESEARCH, INC.
    Inventors: WIlliam C. Burhans, Catherine E. Prudom, Christopher P. Allen, Oleg Ursu, Anna Waller, Larry A. Sklar
  • Publication number: 20130137648
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: January 23, 2013
    Publication date: May 30, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130123225
    Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
    Type: Application
    Filed: January 4, 2013
    Publication date: May 16, 2013
    Inventor: North Carolina State University
  • Patent number: 8435973
    Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: May 7, 2013
    Assignee: Abbott Products GmbH
    Inventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
  • Publication number: 20130101657
    Abstract: Described herein are methods of inhibiting angiogenesis, and treating or preventing a disease or disorder (or symptoms thereof) associated with angiogenesis, wherein an anti-angiogenesis compound is administered to a subject.
    Type: Application
    Filed: September 26, 2012
    Publication date: April 25, 2013
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventor: The Johns Hopkins University
  • Patent number: 8410081
    Abstract: The present invention discloses a therapeutic target for the treatment of cystic fibrosis. It was found that inhibition of non-lysosomal glucosylceramidase (GBA2) sufficiently restores chloride current in cells from CF patients carrying the common delF508-CFTR mutation. With the catalytic center (4) of the enzyme positioned on top of the membrane bilayer face particularly potent inhibitors are found in deoxynojirimycin derivatives having a group that is capable of inserting in the membrane bilayer.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: April 2, 2013
    Assignee: Academisch Medisch Centrum
    Inventors: Johannes Maria Franciscus Gerardus Aerts, Rolf Gabriel Boot
  • Publication number: 20130072465
    Abstract: Compounds of Formula I: that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: September 20, 2012
    Publication date: March 21, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130071321
    Abstract: The invention described herein pertains to folate-receptor targeted agents comprising therapeutic agents useful for the treatment of inflammatory disease, including folate-receptor targeted liposomes (folate-targeted liposomes) containing entrapped therapeutic agents and folate-receptor targeted dendrimers conjugated to therapeutic agents (folate-targeted dendrimer conjugates), useful for the treatment of inflammatory disease, including auto-immune disease, as well as to folate-targeted liposomes containing entrapped imaging agents and dendrimer conjugates conjugated to imaging agents, for use in the diagnosis and monitoring of treatment in such disease.
    Type: Application
    Filed: May 27, 2011
    Publication date: March 21, 2013
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Philip Stewart Low, Scott Poh
  • Publication number: 20130072464
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.
    Type: Application
    Filed: February 8, 2011
    Publication date: March 21, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
  • Publication number: 20130035318
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: January 27, 2012
    Publication date: February 7, 2013
    Inventors: ALICIA REGUEIRO-REN, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Publication number: 20130035320
    Abstract: Novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series according to formulae (I) and (I?) are effective for the prevention and/or treatment of diseases in which the number, activity, and movement of inflammatory cells is implicated.
    Type: Application
    Filed: July 30, 2012
    Publication date: February 7, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Eleonora Ghidini, Anna Maria Capelli
  • Publication number: 20130035304
    Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: January 31, 2011
    Publication date: February 7, 2013
    Inventors: Loren D. Walensky, Michelle L. Stewart, Nicole Cohen
  • Publication number: 20130029953
    Abstract: Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.
    Type: Application
    Filed: July 28, 2011
    Publication date: January 31, 2013
    Inventors: Klaus Nickisch, Kesavaram Narkunan, Baishakhi Debnath, Bindu Santhamma
  • Publication number: 20130029954
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 31, 2013
    Inventors: Alicia Regueiro-Ren, Jacob Swidorski, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell, Zheng Liu
  • Patent number: 8362069
    Abstract: Pharmaceutical/dermatological emulsions containing at least one avermectin compound, notably ivermectin, include at least one fatty phase and at least one aqueous phase, the at least one avermectin compound being solubilized in the fatty phase, which emulsions are useful for the treatment of a variety of dermatological conditions/afflictions, in particular rosacea.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: January 29, 2013
    Assignee: Galderma S.A.
    Inventors: Fanny Diaz-Astruc, Nathalie Barthez, Sandrine Segura-Orsoni
  • Patent number: 8361996
    Abstract: The present invention provides a novel series of imidazolyl substituted steroidal and indan-1-one derivatives and salts thereof having the following general structural formulae (A and B)
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: January 29, 2013
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ranju Bansal, Sheetal Guleria, Gaurav Narang, Rolf Wolfgang Hartmann
  • Publication number: 20130022593
    Abstract: The present invention provides biomarkers for the diagnosis and prognosis of endometriosis. Generally, the methods of this invention find use in diagnosing or for providing a prognosis for endometriosis by detecting the expression levels of biomarkers, which are differentially expressed (up- or down-regulated) in endometrial cells from a patient with endometriosis. Similarly, these markers can be used to diagnose reduced fertility in a patient with endometriosis or to provide a prognosis for a fertility trial in a patient suffering from endometriosis. The present invention also provides methods of identifying a compound for treating or preventing endometriosis. Finally, the present invention provides kits for the diagnosis or prognosis of endometriosis.
    Type: Application
    Filed: July 20, 2012
    Publication date: January 24, 2013
    Applicant: The Regents of the University of California
    Inventor: Linda C. Giudice