Polycyclo Ring System Patents (Class 514/569)
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Publication number: 20140163107Abstract: A pharmaceutical composition for treating viral infections by an influenza type A virus, includes a compound capable of acting as an inhibitor of the binding of the viral RNA to the nucleoprotein of influenza type A viruses, and capable of binding to the viral-RNA-binding domain on the nucleoprotein. A pharmaceutical composition for treating viral infections by an orthomyxovirus, includes a compound capable of acting as an inhibitor of the binding of the viral RNA to the nucleoprotein of orthomyxoviruses, and capable of binding to the viral-RNA-binding domain on the nucleoprotein of the viruses. A compound acting as an inhibitor of the binding of the viral RNA to the nucleoprotein of influenza type A viruses, and binding to the viral-RNA-binding domain on the nucleoprotein of influenza type A viruses and a method for identifying such a compound having these properties are also described.Type: ApplicationFiled: April 20, 2012Publication date: June 12, 2014Applicant: Institut National de la Recherche AgronimiqueInventors: Anny Slama Schwok, Bernard Delmas, Stephane Quideau, Helene Bertrand, Bogdan Tarus
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Publication number: 20140162988Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.Type: ApplicationFiled: January 14, 2014Publication date: June 12, 2014Applicant: BIOCOPEA LIMITEDInventors: Robin M. Bannister, John Brew, Richard R. Reiley, III, Wilson Caparros Wanderley
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Publication number: 20140162987Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a severe pain in an individual using such pharmaceutical compositions.Type: ApplicationFiled: January 14, 2014Publication date: June 12, 2014Applicant: BIOCOPEA LIMITEDInventors: Robin M. Bannister, John Brew, Richard R. Reiley, III, Wilson Caparros Wanderley
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Patent number: 8748416Abstract: A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.Type: GrantFiled: December 20, 2011Date of Patent: June 10, 2014Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol, Michael L. English
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Patent number: 8748462Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I?A or I?B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: GrantFiled: October 13, 2009Date of Patent: June 10, 2014Assignee: Amgen Inc.Inventors: Sean P. Brown, Paul Dransfield, Xiaohui Du, Zice Fu, Jonathan Houze, XianYun Jiao, Sujen Lai, An-Rong Li, Jiwen Liu, Zhihua Ma, Julio C. Medina, Vatee Pattaropong, Wang Shen, Marc Vimolratana, Yingcai Wang, Zhongyu Wang, Ming Yu, Liusheng Zhu
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Patent number: 8748491Abstract: The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5-acyloxy or C1-6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are —CH2—O— or —O—CH2—; or R5 and R10 taken together are —CO—O—, —O—CO—, —CH2—O— or —O—CH2—; R6 is hydrogen, or R5 and R6 together to form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for thType: GrantFiled: September 3, 2013Date of Patent: June 10, 2014Assignee: DSM IP Assets B.V.Inventors: Antione De Saizieu, Ann Fowler, Regina Goralczyk, Claus Kilpert, Goede Schueler, Christof Wehrli
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Publication number: 20140154320Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: ApplicationFiled: February 4, 2014Publication date: June 5, 2014Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: David A. DILL
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Publication number: 20140154266Abstract: The invention provides methods of treatment of metabolic syndrome with HSP90 inhibitors, particularly HSP90? inhibitors. The invention provides methods of diagnosis and monitoring of metabolic syndrome using HSP90, particularly HSP90?, expression and activity level.Type: ApplicationFiled: May 24, 2013Publication date: June 5, 2014Applicant: BERG PHARMA LLCInventors: Niven Rajin Narain, Rangaprasad Sarangarajan, Vivek K. Vishnudas, Enxuan Jing
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Publication number: 20140142184Abstract: Dapsone and dapsone/adapalene compositions can be useful for treating a variety of dermatological conditions. The compositions of this disclosure include dapsone and/or adapalene in a polymeric viscosity builder. Subject compositions can be adjusted to optimize the dermal delivery profile of dapsone to effectively treat dermatological conditions and improve the efficiency of pharmaceutical products applied to the skin. Use of the polymeric viscosity builder provides compositions with increased concentrations of diethylene glycol monoethyl ether relative to compositions without the polymeric viscosity builder.Type: ApplicationFiled: November 18, 2013Publication date: May 22, 2014Applicant: ALLERGAN, INC.Inventors: Kevin S. Warner, Ajay P. Parashar, Vijaya Swaminathan, Varsha Bhatt
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Patent number: 8729127Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.Type: GrantFiled: February 10, 2011Date of Patent: May 20, 2014Assignee: Galderma Research & DevelopmentInventors: Michael Graeber, Janusz Czernielewski
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Publication number: 20140128353Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.Type: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Applicant: Biocopea LimitedInventors: Robin M. Bannister, John Brew, Richard R. Reiley, III, Wilson Caparros Wanderley
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Publication number: 20140128466Abstract: Described are compounds of the structural formula (I): Also provided are pharmacologically acceptable isomers and salts of the compound of (I). The compounds are useful in the treatment of inflammatory bowel disease.Type: ApplicationFiled: July 20, 2012Publication date: May 8, 2014Applicant: VENANTIUS LIMITEDInventors: Neil Frankish, Helen Sheridan
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Patent number: 8716343Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.Type: GrantFiled: April 24, 2012Date of Patent: May 6, 2014Assignee: Regents of the University of MinnesotaInventors: Kevin H. Mayo, Thomas R. Hoye, Xuemei Chen
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Patent number: 8716342Abstract: A method for preparing molecular complexes between Adapalene and cyclodextrins using the technology of dense fluids under pressure, especially that of CO2 is described.Type: GrantFiled: April 9, 2010Date of Patent: May 6, 2014Assignee: Galderma Research & DevelopmentInventors: Hubert Lochard, Bernard Freiss
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Patent number: 8716341Abstract: Topical compositions containing from 0.01% to 0.09% by weight of adapalene or salts thereof are useful for the treatment or prevention of keratinization disorders, particularly acne, and additionally contain at least one gelling agent selected from among carbomers, polysaccharides, cellulose and its derivatives, copolymers of acrylate and of alkyl acrylate, copolymers of acrylamide and of sodium acrylamido-2-methylpropanesulfonate, and xanthan gum.Type: GrantFiled: January 5, 2010Date of Patent: May 6, 2014Assignee: Galderma Research & DevelopmentInventor: Jean-Daniel Doutremepuich
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Patent number: 8703820Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthanoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.Type: GrantFiled: October 12, 2010Date of Patent: April 22, 2014Assignee: Galderma Research & DevelopmentInventors: Michael Graeber, Janusz Czernielewski
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Patent number: 8703184Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent.Type: GrantFiled: March 20, 2013Date of Patent: April 22, 2014Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Publication number: 20140107194Abstract: Compounds particularly for use in an autoimmune inflammatory disease and especially the treatment of inflammatory bowel disease have the formula: wherein R is selected from one or more of the same or different of hydrogen, hydroxyl, optionally substituted alkyl, optionally substituted aryl, alkoxy, aryloxy, thiol, and optionally substituted amino, and wherein R1 is selected from one or more of the same or different of hydrogen, acetyl, optionally substituted alkyl, optionally substituted aryl, and an amino acid selected from leucine, valine, isoleucine, and glycine.Type: ApplicationFiled: July 20, 2012Publication date: April 17, 2014Applicant: Venantius LimitedInventors: Neil Frankish, Helen Sheridan
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Publication number: 20140094465Abstract: The present invention is directed to compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: June 5, 2012Publication date: April 3, 2014Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20140094439Abstract: Novel drug carriers capable of targeted and/or pH dependent release of biologically active agents into selected pH environments including the gastrointestinal (GI), ophthalmic, urinary, or reproductive tracts. Unexpectedly, carriers including free fatty acids (FFA) are able to deliver biologically active agents to various pH environments. Such targeted delivery is tailorable and useful for active agents that are: (a) injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) acid labile, (c) impermeable/insoluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.Type: ApplicationFiled: June 3, 2013Publication date: April 3, 2014Inventors: Upendra K. Marathi, Susann Edler Childress, Shaun L. Gammill, Robert W. Strozier
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Publication number: 20140093562Abstract: The invention provides a composition consisting essentially of a solid naproxen concentrate, wherein the solid naproxen concentrate comprises (a) a solid naproxen free acid and (b) a solid naproxen alkali salt, and wherein at least 90% of the weight of the solid naproxen concentrate is naproxen free acid and naproxen alkali salt, as well methods of producing such a solid naproxen concentrate.Type: ApplicationFiled: December 3, 2013Publication date: April 3, 2014Applicant: Pharmaceutics International, Inc.Inventors: EmadEldin M. Hassan, Sridhar Gumudavelli
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Patent number: 8685453Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: GrantFiled: March 20, 2013Date of Patent: April 1, 2014Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Patent number: 8680251Abstract: The invention describes novel triterpenoid 2-deoxy glycosides of general formula I, wherein at least one of the substituents X1 and R2 contains a 2-deoxy glycosidic group, method of preparation thereof, their cytotoxic activity and a pharmaceutical formulation containing these compounds.Type: GrantFiled: November 6, 2009Date of Patent: March 25, 2014Assignee: Univerzita Palackeho V OlomouciInventors: Jan {hacek over (S)}arek, Pavla Spá{hacek over (c)}ilová, Marian Hajduch
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Patent number: 8680147Abstract: The present invention relates to novel composition for the treatment, co-treatment or prevention of inflammatory disorders comprising an effective amount of carnosic acid 12-methylether.Type: GrantFiled: November 21, 2007Date of Patent: March 25, 2014Assignee: DSM IP Assets B.V.Inventors: Daniel Raederstorff, Goede Schueler, Joseph Schwager, Christof Wehrli
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Publication number: 20140080842Abstract: The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.Type: ApplicationFiled: May 11, 2012Publication date: March 20, 2014Applicant: B.R.A.I.N. Biotechnology Research and Information Network AGInventors: Michael Krohn, Dirk Sombroek
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Patent number: 8673910Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in formula I: or a pharmaceutically acceptable salt or hydrate thereof. In another embodiment, a compound of the invention has the chemical structure shown in formula II: or a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: June 30, 2009Date of Patent: March 18, 2014Assignees: H. Lee Moffitt Cancer Center and Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Patent number: 8658694Abstract: Buffer solutions for pharmaceutical preparations that have bactericidal activity preferentially against gram negative bacteria are provided. The buffers have a pH of greater than about 10 or less than about 4.5 with low buffer capacity. Methods of their use in reducing the occurrence of blood stream infections in a mammal is also provided.Type: GrantFiled: February 7, 2011Date of Patent: February 25, 2014Assignee: United Therapeutics CorporationInventors: Roger Andrew Jeffs, David Zaccardelli
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Patent number: 8653140Abstract: Dermatological disorders having an inflammatory or proliferative component are treated with pharmaceutical compositions containing on the order of 0.3% by weight of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid (adapalene) or salt thereof, formulated into pharmaceutically acceptable media therefor, advantageously topically applicable gels, creams or lotions.Type: GrantFiled: May 18, 2012Date of Patent: February 18, 2014Assignee: Galderma Research & DevelopmentInventors: Michael Graeber, Janusz Czernielewski
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Patent number: 8652525Abstract: This invention provides biodegradable, sustained-release pharmaceutical compositions of non-steroidal, anti-inflammatory drugs (NSAIDs) formulated with biocompatible, biodegradable tyrosine-derived polyarylates. The compositions are particularly suitable for localized delivery of NSAIDs for various disease states. For example, implantation of the compositions at the site of surgery leads to relatively high local concentrations of the NSAID to reduce or alleviate post-surgical pain. Long term zero order release of certain NSAIDs can also be provided by with certain polymer formulations.Type: GrantFiled: July 8, 2009Date of Patent: February 18, 2014Assignee: TYRX, Inc.Inventors: Arikha Moses, Fatima Buevich, Satish Pulapura, Arvind Viswanathan
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Publication number: 20140044813Abstract: Extracts of plants of the Lamiaceae family are shown to improve cognitive health and function.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Inventors: Michael Ceddia, Kelli Herrlinger, Brandon Lewis, Harry Feng
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Publication number: 20140037727Abstract: A medicament tablet containing paracetamol (acetaminophen) as the (or an) active ingredient, and an encapsulated flavorant. The tablet may be swallowed in tablet form or may be dissolved or dispersed in water to form a palatable drink.Type: ApplicationFiled: October 8, 2013Publication date: February 6, 2014Applicant: Reckitt Benckiser Healthcare (UK) LimitedInventor: Paul Frederick Field
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Publication number: 20140037725Abstract: The present invention is related to a bilayer pharmaceutical composition comprising naproxen or a pharmaceutically acceptable salt thereof. The present invention is particularly related to a bilayer pharmaceutical composition comprising an immediate release component and a controlled release component of naproxen or a pharmaceutically acceptable salt thereof and the process for preparation thereof. Moreover, the present invention is related to the treatment of rheumatoid arthritis, oesteoarthritis, ankylosing spondylitis, pain, primary dysmenorrhoea, acute tendinitis, bursitis and acute gout.Type: ApplicationFiled: July 29, 2013Publication date: February 6, 2014Applicant: CADILA HEALTHCARE LIMITEDInventors: Muthaiyyan Esakkimuthu KANNAN, Gaurav Navinbhai MISTRY, Priteshkumar Chadrakant MISTRY
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Patent number: 8642656Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.Type: GrantFiled: September 28, 2012Date of Patent: February 4, 2014Assignee: Regents of the University of MinnesotaInventors: Kevin H. Mayo, Thomas R. Hoye, Xuemei Chen
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Publication number: 20140031427Abstract: Adapalene or a pharmaceutically acceptable salt thereof formulated into a pharmaceutical composition is useful for reducing the number of acne lesions, via daily topical application, in combination or in association with benzoyl peroxide (BPO); such treatment may be via administration of a pharmaceutical composition combining adapalene and BPO or by a concomitant application of two pharmaceutical compositions, one containing adapalene and the other containing BPO.Type: ApplicationFiled: September 26, 2013Publication date: January 30, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Marie-Line ABOU-CHACRA VERNET, Denis GROSS, Christian LOESCHE, Michel PONCET
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Publication number: 20140030313Abstract: A method for relieving menstrual pain and reducing menstrual blood loss in a female is provided. The method comprises administering intravaginally to the female a first therapeutically effective amount of a non-steroidal anti-inflammatory drug (NSAID) that relieves menstrual pain and a second therapeutically effective amount of an active agent that reduces menstrual blood loss, wherein the NSAID and the active agent are simultaneously administered by the same drug delivery device, wherein the active agent is any one of an antifibrinolytic agent and a hemostatic agent.Type: ApplicationFiled: September 30, 2013Publication date: January 30, 2014Applicant: ARSTAT Inc.Inventor: Arkady RUBIN
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Publication number: 20140031338Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.Type: ApplicationFiled: April 13, 2012Publication date: January 30, 2014Applicant: LABORATOIRE BIODIMInventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
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Publication number: 20140018429Abstract: The invention provides compositions comprising sulindac, R-epimer sulindac, S-epimer sulindac, derivatives, metabolites, and structural analogs thereof which protect normal cells against damage caused by solar rays, oxidative damage, environmental factors, diseases and organisms.Type: ApplicationFiled: July 16, 2013Publication date: January 16, 2014Inventors: Herbert Weissbach, Nathan Brot
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Publication number: 20140018430Abstract: The present invention provides a composition comprising at least one prostacyclin or prostacyclin analogue or a pharmaceutically acceptable salt thereof and at least one phosphodiesterase (PDE) 4 inhibitor and optionally a further PDE inhibitor for use in preventing or treating cystic fibrosis by selectively increasing the cAMP levels in bronchoepithelial cells.Type: ApplicationFiled: February 3, 2012Publication date: January 16, 2014Applicant: SciPharm SaRLInventors: Michael Freissmuth, Christina Gloeckel, Xaver Koenig, Simon Keuerleber
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Publication number: 20140018431Abstract: The present invention describes methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of interstitial lung disease or asthma, or a condition, such as pulmonary fibrosis, associated with interstitial lung disease or a condition associated with asthma. The invention also relates to kits for treatment and/or prevention of such condition that include an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 18, 2013Publication date: January 16, 2014Applicant: United Therapeutics CorporationInventors: Michael Wade, Stuart Rich, Eugene Sullivan, Robert Roscigno, Roger Jeffs
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Publication number: 20140010884Abstract: Dermatological compositions containing, in a physiologically acceptable medium, at least one retinoid, dispersed benzoyl peroxide and at least one gelling agent of the family of the carrageenans, are useful for treating dermatological conditions and afflictions linked to disorders of cell differentiation and/or proliferation and/or keratinization, notably for treating acne vulgaris.Type: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Fabienne LOUIS, Sandrine SEGURA, Nathalie WILLCOX
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Publication number: 20140005270Abstract: The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5-acyloxy or C1-6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are —CH2—O— or —O—CH2—; or R5 and R10 taken together are —CO—O—, —O—CO—, —CH2—O— or —O—CH2—; R6 is hydrogen, or R5 and R6 together to form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for thType: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: DSM IP ASSETS B.V.Inventors: Antoine DE SAIZIEU, Ann Fowler, Regina Goralczyk, Claus Kilpert, Goede Schueler, Christof Wehrli
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Patent number: 8617607Abstract: This invention provides biodegradable, sustained-release pharmaceutical compositions of a psychoactive drug formulated with biocompatible, biodegradable tyrosine-derived polyarylates.Type: GrantFiled: July 10, 2009Date of Patent: December 31, 2013Assignee: TYRX, Inc.Inventors: Arikha Moses, Fatima Buevich, Satish Pulapura
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Publication number: 20130345249Abstract: The invention encompasses pharmaceutical formulations for the prevention and treatment of Wolbachia-related disease wherein the formulations comprise a compound previously unknown and unused for such a purpose, the compound being one or more of: Pararosaniline Pamoate, Pyrvinium Pamoate, Clofoctol, and Isoreserpine, derivatives, metabolites, precursors, pro-drugs and variants thereof.Type: ApplicationFiled: January 13, 2012Publication date: December 26, 2013Applicant: The Regents of the University of CaliforniaInventors: Alain Debec, Laura Serbus, Frederic Landmann, William Sullivan
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Publication number: 20130337031Abstract: The present disclosure is drawn to topical formulations, transdermal systems, and related methods. In one embodiment, a topical formulation is provided that includes a local anesthetic, a first compound, and a second compound. The first compound and second compound are different and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate.Type: ApplicationFiled: March 8, 2013Publication date: December 19, 2013Applicant: Nuvo Research Inc.Inventor: Nuvo Research Inc.
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Publication number: 20130338230Abstract: Intermediate compositions and in particular gels and suspensions for a foam composition comprising adapalene are described. Also described, is the dermatological use of such compositions.Type: ApplicationFiled: December 22, 2011Publication date: December 19, 2013Inventor: Emmanuelle At
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Publication number: 20130338229Abstract: Provided is a drug substance and a method of treating an ailment comprising administering an oral dose of a drug product comprising the drug substance wherein the drug substance comprises an organic acid addition salt of methadone. The organic acid addition salt is selected from the group consisting of pamoate and xinafoate wherein the drug substance is bioavailable under gastrointestinal administration but is not bioavailable under administration at a mucosal membrane other than gastrointestinal or release from a depot injectable product.Type: ApplicationFiled: July 29, 2013Publication date: December 19, 2013Applicant: Pisgah National Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David William Bristol, Michael L. English
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Publication number: 20130337016Abstract: The present invention relates to a method for treating, reducing or preventing acne. In particular, the present invention relates to methods for reducing the total number, incidence and severity of acne lesions on the skin which includes both inflammatory and non-inflammatory lesions. Further, the invention relates to reducing the incidence and severity of adverse events resulting from topical application of anti-acne agents resulting in improvement of skin tone. The method includes administering a novel and stable topical anti-acne pharmaceutical composition.Type: ApplicationFiled: October 19, 2011Publication date: December 19, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Ravindra Mittal, Sunilendu Bhushan Roy, Jay Shantilal Kothari, Shafiq Sheikh, Jitendra Dasharathlal Patel, Jinesh Suresh Pancholi
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Patent number: 8609087Abstract: Compounds and methods for designing and identifying compounds which inhibit TFPP-like aspartyl protease enzymes by targeting the aspartic acid residues of the active site or mimicking peptides corresponding to the region surrounding the substrate's cleavage site are provided. Agents identified as inhibitors of TFPP-like aspartyl proteases such as type 4 prepilin peptidases are expected to be useful as anti-bacterial agents and in inhibiting development of drug resistant strains of bacteria.Type: GrantFiled: March 4, 2005Date of Patent: December 17, 2013Assignee: Trustees of Dartmouth CollegeInventors: Ronald K. Taylor, Christian F. LaPointe
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Patent number: 8609728Abstract: One embodiment relates to a method of treating pulmonary hypertension based upon co-administering to a subject in need thereof a pharmaceutically effective amount of an oral therapeutic agent for treating pulmonary hypertension and a pharmaceutically effective amount of an inhaled therapeutic agent for treating pulmonary hypertension. The benefit of the co-administration of these agents is to eliminate or reduce one or more side effects associated with mono-therapy of either agent, as well as one or more side effects associated with other administration routes such as subcutaneous or intravenous administration.Type: GrantFiled: March 14, 2011Date of Patent: December 17, 2013Assignee: United Therapeutics CorporationInventors: Martine A. Rothblatt, Lewis J. Rubin
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Patent number: 8604082Abstract: The present invention belongs to the fields of pharmacology, medicine and medicinal chemistry, and provides methods and compositions for treating sexual dysfunction; more particularly, the invention relates to treatment of premature ejaculation in humans.Type: GrantFiled: December 11, 2006Date of Patent: December 10, 2013Assignee: Trinity Laboratories, Inc.Inventor: Chandra U. Singh