Z Forms A Phenoxy Alkyl Or Phenoxy Alkenyl Radical Patents (Class 514/543)
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Publication number: 20100216879Abstract: Resveratrol ferulate compounds and compositions.Type: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Inventors: Daniel H. Maes, Fatemeh Mohammadi, Lisa Qu, Anna Czarnota, Thomas Mammone, Lieve Declercq, Julius R. Zecchino
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Publication number: 20100212036Abstract: The present invention provides for methods of treating and preventing cardiac hypertrophy. Class I HDACs, which are known to participate in regulation of chromatin structure and gene expression, have generally been considered as pro-hypertrophic in their action. However, the present invention demonstrates that inhibition of certain Class I HDACs should be avoided in the treatment of cardiac hypertrophy, thereby pointing toward selective, and not global, inhibition of Class I HDACs. In particular, the present invention provides for selective inhibition of HDACs 1 and/or 2, and the avoidance of inhibition of HDAC3.Type: ApplicationFiled: September 29, 2009Publication date: August 19, 2010Inventors: Eric N. Olson, Lawrence Melvin, Rusty L. Montgomery
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Publication number: 20100204195Abstract: Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described.Type: ApplicationFiled: July 28, 2008Publication date: August 12, 2010Applicant: CIPLA LIMITEDInventors: Amar Lulla, Geena Malhotra
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Publication number: 20100197784Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.Type: ApplicationFiled: April 12, 2010Publication date: August 5, 2010Applicants: The University of North Carlina at Chapel Hill, The University of Rochester Medical Center, Androscience CorporationInventors: Kuo-Hsiung Lee, Li Lin, Charles C-Y Shih, Ching-Yuan Su, Junko Ishida, Hironori Ohtsu, Hui-Kang Wang, Hideji Itokawa, Chawnshang Chang
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Patent number: 7767711Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: GrantFiled: June 20, 2007Date of Patent: August 3, 2010Assignees: University of South Florida, McGill University, The Hong Kong Polytechnic UniversityInventors: Q. Ping Dou, Tak-Hang Chan, David M. Smith
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Publication number: 20100190855Abstract: A compound of formula (I) wherein Y is oxygen or sulfur, and X1, X2 and X3 are independently of each other hydrogen, halogen, hydroxy or linear or branched (C1-6)-alkoxy, or hydroxy-(C1-6)alkyl or (C1-6)alkoxy-(C1-6)alkyl, mono- or dihalogenated (C1-6)-alkyl, amino(C1-6)-alkyl, hydroxy(C1-6)-alkyl, with one of the two provisos that: (1) at least of X1, X2 and X3 is other than hydrogen, and (2) X2 is other than hydroxy, when X1 and X3 are hydrogen.Type: ApplicationFiled: July 11, 2008Publication date: July 29, 2010Applicant: NABRIVA THERAPEUTICS AGInventors: Klaus Thirring, Werner Heilmayer
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Publication number: 20100184856Abstract: The present invention provides compounds, and compositions comprising these compounds, which have immunomodulatory activity and/or anti-inflammatory activity.Type: ApplicationFiled: December 28, 2009Publication date: July 22, 2010Inventors: Allan Sy Lau, Lai Hung Cindy Yang, Chi Chung Stanley Chik, Chun Bong James Li
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Publication number: 20100179182Abstract: The present invention provides processes for making and forms of solid dispersions of pharmaceutical active ingredients.Type: ApplicationFiled: March 24, 2010Publication date: July 15, 2010Inventors: Rama Ali Abu Shmeis, James Kowalski, Steven L. Krill, Lakshman Jayanth Parthiban, Zeren Wang
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Publication number: 20100173852Abstract: The present invention provides compositions and methods for treating glaucoma, ocular hypertension, and age-related macular degeneration. More specifically, the present invention describes the use of agents that down-regulate expression of tanis and/or p21Waf1/Cip1/Sd1 genes to treat such disorders of the eye.Type: ApplicationFiled: March 8, 2010Publication date: July 8, 2010Applicant: ALCON, INC.Inventors: Colene D. Drace, Gary W. Williams, Curtis R. Kelly, Najam A. Sharif
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Publication number: 20100166857Abstract: The invention provides solid dispersions of at least one insoluble active pharmaceutical ingredient, pharmaceutical dosage forms comprising the solid dispersions, and methods of manufacturing same. In an embodiment, a solid dispersion of the present invention includes a plurality of coated particles comprising inert particles with a coating, wherein the coating comprises an insoluble active pharmaceutical ingredient dispersed in a hydrophilic polymer, and wherein the inert particles comprise nonpareils; and a plurality of granules comprising an insoluble active pharmaceutical ingredient with at least one pharmaceutically acceptable excipient. In an embodiment, the insoluble active pharmaceutical ingredient in the coating and the insoluble active pharmaceutical ingredient of the granules are the same type. A solid dispersion of the present invention may optionally be encapsulated in capsules or compressed into a tablet.Type: ApplicationFiled: December 30, 2009Publication date: July 1, 2010Inventors: Dong Yan, Lee Foong Siew, Richard Ting, Tzu-Yuan Chen, Mahendra Sudhakar Pawar
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Publication number: 20100168045Abstract: The invention concerns novel polyunsaturated compounds of formula (I) wherein: R1 represents a R?1, -A-R?1 group, R?1 being selected from —COOH, —COOR3, —CONH2, —CONHR3, —CONR3, R4, —CHO, —CH2OH, —CH2OR5, and A represents a C2-C16 alkylene, alkenylene or alkynylene; R2 represents: an optionally substituted aryl group or an optionally substituted heteroaryl group; a sugar residue or, a fatty acid residue optionally branched and/or substituted preferably at the chain terminus and particularly by hydroxy, acetoxy radical or by an optionally protected amino radical; a —OC—(CH2)n CO-tocopheryl (alpha, beta or gamma or delta) group, with 2 $m(F) n $m(F) 10; a —R?2—O—R6 group, wherein R?2 is an optionally substituted arylene group or an optionally substituted heteroarylene group, and R6 represents a hydrogen atom, a straight or branched optionally substituted C1-C16 alkyl, a straight or branched optionally substituted C2-C16 alkenyl, or a straight or branched C2-C16 alkynyl group, an optionally substituted tocopheryType: ApplicationFiled: December 14, 2006Publication date: July 1, 2010Applicant: Pierre Fabre Dermo-CosmetiqueInventors: Pascal Bordat, Roger Tarroux, Jean-Hilaire Saurat, Olivier Sorg, Jean-Louis Brayer, Natacha Frison
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Publication number: 20100151035Abstract: The present invention relates to a stable pharmaceutical composition of a poorly water-soluble drug with a view to increasing its solubility and bioavailability. The present invention relates to a solid dispersion of a poorly water-soluble drug.Type: ApplicationFiled: March 10, 2008Publication date: June 17, 2010Applicant: Sandoz AGInventors: Bharatrajan Ramaswami, Manisha Rajesh Patil, Aditi Das
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Publication number: 20100152143Abstract: Embodiments of the invention generally relate to pharmaceutical compositions containing at least one caffeic acid compound and methods for the topical treatment of proliferative and inflammatory skin disorders such as plaque psoriasis, atopic dermatitis, and other disorders. In some embodiments, the topical treatment includes applications of the pharmaceutical composition containing at least one caffeic acid compound or a mixture of caffeic acid compounds such as caffeic acid ester compounds, caffeic acid amide compounds, analogues thereof, derivatives thereof, salts thereof, or mixtures thereof. The pharmaceutical composition or topical dosage may contain the caffeic acid compound at a concentration by weight within a range from about 0.01% to about 20%, preferably, from about 0.1% to about 15%, preferably, from about 1% to about 10%, more preferably, from about 3% to about 7%, and more preferably, from about 4% to about 6%.Type: ApplicationFiled: September 30, 2009Publication date: June 17, 2010Applicant: MOLECULIN, LLCInventors: Waldemar Priebe, Charles Conrad, Timothy Madden
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Publication number: 20100143420Abstract: Pharmaceutical formulations are disclosed comprising a multi-phasic pharmaceutical composition comprising an active pharmaceutical ingredient, wherein the active pharmaceutical ingredient is in a particulate state, a solubilized state, or in both a particulate state and in a solubilized state; a solvent; a non-miscible liquid; a stabilizer, and water; wherein the pharmaceutical formulation is an oral dosage form. Such pharmaceutical formulations are capable of reducing the fed/fast variability and improving oral bioavailability to which a number of active pharmaceutical ingredients are susceptible. The pharmaceutical formulations of the invention, therefore are bioequivalent in fed and fasted states and improved oral bioavailability.Type: ApplicationFiled: January 22, 2008Publication date: June 10, 2010Inventors: Dinesh Shenoy, Robert Lee
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Publication number: 20100130605Abstract: The present invention relates to substances which can be used as cosmetic ingredients, especially for skin whitening and as cosmetic agents against signs of ageing skin. The present invention also relates to the use of such substances for the manufacture of a medicament for the treatment of disorders related to the pigmentation of the skin. The invention furthermore relates to specific substances.Type: ApplicationFiled: February 26, 2008Publication date: May 27, 2010Applicant: Cognis IP Management GmbHInventors: Thomas Markert, Philippe Moussou, Louis Danoux, Andreas Rathjens
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Publication number: 20100119482Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.Type: ApplicationFiled: December 24, 2009Publication date: May 13, 2010Inventors: Anthony Joonkyoo Yun, Partic Yuarn-Bor Lee
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Publication number: 20100120909Abstract: The invention concerns compositions comprising substituted 1,3-diphenylprop-2-en-1-one derivatives designed for therapeutic use. The inventive compositions are useful in particular for preventing or treating cardiovascular diseases, syndrome X, Ia restenosis, diabetes, obesity, hypertension, inflammatory diseases, cancers or neoplasms (benign or malignant tumors), neurodegenerative, dermatological diseases and disorders related to oxidative stress, for preventing or treating the effects of ageing in general and for example skin ageing, in particular in the field of cosmetics (occurrence of wrinkles and the like).Type: ApplicationFiled: October 30, 2009Publication date: May 13, 2010Applicant: GENFITInventors: Jamila Najib, Karine Caumont-Bertrand
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Publication number: 20100113592Abstract: The present invention relates to compounds and compositions of formula I, which are unsymmetrical aromatic ether diacids, and polymers formed from the same. [R?—(Y)p—O]q—Ar—[O—(X)r—R?]s??I The compounds are expected to be useful in a variety of medical and/or cosmetics applications. Polymers formed from the functionalized unsymmetrical aromatic ether diacids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range.Type: ApplicationFiled: January 8, 2010Publication date: May 6, 2010Applicant: Bezwada Biomedical, LLCInventor: Rao S. Bezwada
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Publication number: 20100111921Abstract: Methods of treating, inhibiting, or ameliorating gout, including chronic acute (refractory) gout, pseudogout, or drug-induced gout, in a human subject in need thereof, comprising administering to a subject in need a therapeutic amount of an interleukin 1 (IL-1) antagonist, wherein the incidence of a gout flare is reduced or inhibited.Type: ApplicationFiled: September 28, 2009Publication date: May 6, 2010Applicant: Regeneron Pharmaceuticals, Inc.Inventors: Catherine Vicary, Scott Mellis
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Publication number: 20100105772Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed lipoxins, generated from the interaction between a dietary omega-6 polyunsaturated fatty acid (PUFA) such as arachidonic acid (AA), oxygenases and the analgesic aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy containing derivatives of AA containing compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- and tri-hydroxy derivatives of AA (lipoxins, aspirin-triggered epi-lipoxins) that diminish, prevent, or eliminate NV, hemangiogenesis and/or angiogenic condition(s) of corneal tissue. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.Type: ApplicationFiled: April 27, 2009Publication date: April 29, 2010Inventors: Charles N. Serhan, Reza Dana, Yiping Jin
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Publication number: 20100098690Abstract: The present invention provides a pharmaceutical composition comprising a combination of an Hsp 90 family protein inhibitor and at least one compound, the said pharmaceutical composition wherein the Hsp 90 family protein inhibitor is a benozoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl, or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like], or a prodrug thereof; or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: March 5, 2008Publication date: April 22, 2010Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Shiro Soga, Toshihiko Ishii, Takayuki Nakashima, Yukimasa Shiotsu, Shiro Akinaga
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Patent number: 7683193Abstract: Benzolipoxin analogs, methods of their preparation and pharmaceutical compositions containing the compounds are provided. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease and abnormal cell proliferation.Type: GrantFiled: April 4, 2006Date of Patent: March 23, 2010Assignee: University of Southern CaliforniaInventor: Nicos A. Petasis
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Publication number: 20100063011Abstract: The invention relates to organic compounds having the ability to reduce or suppress the onset of skin irritation induced by extraneous cause selected from the group of 2-heptylcyclopentanone, 2-ethoxynaphthalene; 2-methoxynaphthalene; 1-methoxy-4-(prop-1-enyl)benzene; 1-(cyclopropylmethyl)-4-methoxybenzene; wherein X, Y, and R1 to R11 have the same meaning as given in the description. Furthermore the invention refers to compositions for topical application to the skin comprising them. It further relates to a method of reducing or suppressing the formation of skin irritation.Type: ApplicationFiled: September 8, 2006Publication date: March 11, 2010Applicant: GIVAUDAN SAInventors: Andreas Natsch, Michael Wasescha
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Publication number: 20100056627Abstract: It is intended to reinforce the anti-fungal, anti-viral and anti-bacterial activities of alkyl gallates, and to provide a new technology and means which allow the solubilization of the alkyl gallates in water. A pharmaceutical composition of alkyl gallates of the present invention is characterized by containing (A) an alkyl gallate in which the carbon number of the alkyl group is in the range of 5 to 16 and (B) another alkyl gallate in which the carbon number of the alkyl group is smaller than that of (A). Preferably, the carbon number of the alkyl group of the alkyl gallate (B) is in the range of 2 to 7, and the composition further contains (C) at least one member selected from an alkali metal salt, boric acid, sodium borate and an organic salt.Type: ApplicationFiled: December 27, 2007Publication date: March 4, 2010Inventors: Tomihiko Higuchi, Hirofumi Shibata, Masanori Higuchi
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Publication number: 20100048701Abstract: Disclosed is an amide compound represented by the formula (1) below, which has excellent plant disease controlling activity. In the formula, X1 represents a fluorine atom or a methoxy group; X2 represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group or the like; X3 represents a halogen atom, a C1-C4 alkyl group or the like; Z represents an oxygen atom or a sulfur atom; and A represents an A1-CR11R12R13 group, an A2-Cy1 group or an A3-Cy2 group, wherein A1 represents a CH2 group or the like, A2 represents a single bond, a CH2 group or the like, A3 represents a C1-C3 haloalkyl group, a C2-C4 alkenyl group or the like, Cy1 represents a C3-C6 cycloalkyl group substituted with a C1-C6 alkoxy group or the like, Cy2 represents a C3-C6 cycloalkyl group which may be substituted with a halogen atom or the like, R11 and R12 independently represent a C1-C4 alkyl group, and R13 represents a halogen atom, a hydroxyl group or the like.Type: ApplicationFiled: April 25, 2008Publication date: February 25, 2010Inventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
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Publication number: 20100048702Abstract: Aspirin (ASA) triggers a switch in the biosynthesis of lipid mediators, inhibiting prostanoid production and initiating 15-epi-lipoxin generation, through the acetylation of cyclooxygenase II.Type: ApplicationFiled: August 24, 2009Publication date: February 25, 2010Inventor: Charles N. Serhan
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Publication number: 20100003332Abstract: A powder comprising nanoparticles of a sparingly water-soluble drug prepared in accordance with the present invention exhibits enhanced bioavailability without generating adverse side effects caused by impurities, while the nano-particle size of the drug remains unchanged when administered. Accordingly, the powder can be useful for the development of a formulation of a sparingly water-soluble drug for oral and parenteral administration.Type: ApplicationFiled: July 26, 2007Publication date: January 7, 2010Applicant: Amorepacific CorporationInventors: Joon Ho Bae, Jong Hwi Lee, Hyeok Lee, Jung Ju Kim
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Publication number: 20090306111Abstract: An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye. There are provided an agent for promoting proliferation of a meibomian gland epithelial cell or a corneal epithelial cell, containing a PPAR? or ? agonist as an active ingredient, as well as an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye, containing a PPAR? or ? agonist as an active ingredient.Type: ApplicationFiled: November 27, 2006Publication date: December 10, 2009Inventors: Yoshikuni Nakamura, Ikuko Hanano, Jun Inoue
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Publication number: 20090257968Abstract: The present invention provides an enhanced gelling agent composition comprising a mixture of an anionic surfactant and a coupling agent. The invention also describes compositions in gel form comprising: (a) a solvent selected from the group consisting of polar solvents, non-polar solvents and combinations thereof; and (b) a gelling agent in an amount sufficient to impart gelation to the composition, the gelling agent being a mixture comprising an anionic surfactant and a coupling agent. The gels of the invention may be substantially anhydrous or may optionally contain water as part of the formulation.Type: ApplicationFiled: May 6, 2009Publication date: October 15, 2009Inventors: Richard Walton, Edward T. Borish
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Patent number: 7601756Abstract: A method for treating irritable bowel syndrome (IBS) is included. The method includes the step of administering a fibric acid derivative to a patient diagnosed with IBS in order to alleviate the symptoms associated with IBS.Type: GrantFiled: June 4, 2004Date of Patent: October 13, 2009Assignee: Snowden Pharmaceuticals, LLCInventor: Peter Sterling Mueller
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Publication number: 20090247522Abstract: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.Type: ApplicationFiled: April 22, 2009Publication date: October 1, 2009Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Shinji Nara, Hiroshi Nakagawa, Yutaka Kanda, Takayuki Nakashima, Shiro Soga, Jiro Kajita, Jun-ichi Saito, Yukimasa Shiotsu, Shiro Akinaga
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Publication number: 20090227673Abstract: It has been discovered that polyphenols are effective as a co-pharmaceutical in combination with traditional dual drug therapies of catecholamines and decarboxylase inhibitors for the treatment of Parkinson's disease. Accordingly, a method of treating Parkinson's disease comprising administering to a subject suffering from Parkinson's disease a pharmaceutical composition comprising at least one catecholamine, at least one decarboxylase inhibitor, and at least one polyphenol is provided.Type: ApplicationFiled: January 12, 2007Publication date: September 10, 2009Inventor: Bao Ting Zhu
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Publication number: 20090137561Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: 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: ApplicationFiled: October 3, 2008Publication date: May 28, 2009Applicant: Amgen Inc.Inventors: Sean P. Brown, Qiong Cao, Paul John Dransfield, Xiaohui Du, Jonathan Houze, Xian Yun Jiao, Yong-Jae Kim, Todd J. Kohn, SuJen Lai, An-Rong Li, Daniel Lin, Jian Luo, Julio C. Medina, Jeffrey D. Reagan, Vatee Pattaropong, Margrit Schwarz, Wang Shen, Yongli Su, Gayathri Swaminath, Marc Vimolratana, Xiang Wang, Yumei Xiong, Li Yang, Ming Yu, Jie Zhang, Liusheng Zhu
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Patent number: 7534815Abstract: Provided is a method of treating hypertension, which comprises administering an effective amount of a compound represented by the following formula (1) or (2): wherein, R1 and R2 are the same or different and each independently represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxyalkyl, aryl, alkylaryl, aralkyl, or acyl, R3 represents hydroxyl, ester bond residue, or amide bond residue, R4 represents ester bond residue or amide bond residue, or a pharmaceutically acceptable salt thereof (except ferulic acid).Type: GrantFiled: March 29, 2004Date of Patent: May 19, 2009Assignee: Kao CorporationInventors: Atsushi Suzuki, Ryuji Ochiai, Ichiro Tokimitsu
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Publication number: 20090123446Abstract: Methods of treating, inhibiting, or ameliorating gout, including chronic acute (refractory) gout, pseudogout, or drug-induced gout, in a human subject in need thereof, comprising administering to a subject in need a therapeutic amount of an interleukin 1 (IL-1) antagonist, wherein the incidence of a gout flare is reduced or inhibited.Type: ApplicationFiled: August 28, 2008Publication date: May 14, 2009Applicant: Regeneron Pharmaceuticals, Inc.Inventors: Catherine Vicary, Scott Mellis
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Publication number: 20090098200Abstract: Compositions are provided comprising a lipophilic active compound, e.g., a human or veterinary drug or a nutraceutical, interwoven with a polymeric matrix formed by two or more polymers, wherein one of the polymers is an amphiphilic polymer and the other polymer is either an amphiphilic polymer with a different hydrophobic-hydrophilic balance or a hydrophilic polymer, and the active lipophilic compound has modified physicochemical properties. The composition forms colloidal nanodispersion upon contact with aqueous media.Type: ApplicationFiled: September 25, 2008Publication date: April 16, 2009Applicant: SOLUBEST LTD.Inventors: Galia Temtsin Krayz, Maryana Averbuch, Ilya Zelkind, Larisa Gitis
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Patent number: 7504091Abstract: antiperspirant compositions comprise an antiperspirant active and a carrier oil in which the carrier oil comprises an aromatic ester oil obeying the general formula: R1—CO2—X—Y—R2 in which R1 and R2 each represent a phenyl group, X represents an alkylene group containing from 2 to 4 carbons including at least one pendant alkyl group and Y represents a bond, or an ether or ester linkage.Type: GrantFiled: April 13, 2005Date of Patent: March 17, 2009Assignee: Unilever Home & Personal Care USA, division of Conopco, Inc.Inventor: Kevin Ronald Franklin
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Publication number: 20090036389Abstract: Provided are cosolvent evaporation methods and compositions for improving the solubility of hydrophobic compounds, including therapeutic agents such as anticancer drugs, polyene antibiotics, antilipidemic agents, and hydrophobic compounds used in various industries, and/or for reducing the toxicity of certain hydrophobic therapeutic agents, especially polyene antibiotics, in particular, Amphotericin B (AmB), and therapeutics such as paclitaxel, tamoxifen, an acylated prodrug or an acylated cis-platin, by incorporating these agents within micelles comprising an amphiphilic block-forming copolymer.Type: ApplicationFiled: September 29, 2008Publication date: February 5, 2009Applicants: Abbott Laboratories, Wisconsin Alumni Research FoundationInventors: Glen S. Kwon, Devalina Law, Monica Adams, Karen Kostick, Eric A. Schmitt
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Publication number: 20090030077Abstract: The invention provides novel omega-3 oil liquid formulations of fenofibrate. These formulations can be substantially free of any food effect, effective in small volumes, and readily bioavailable. Notably, because the formulations of the invention contain an omega-3 oil as the major ingredient, they not only provide anithypercholesterolemic and antihypertriglyceridemic effects due to the fenofibrate active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof.Type: ApplicationFiled: August 1, 2008Publication date: January 29, 2009Applicant: Transform Pharmaceuticals Inc.Inventors: Orn Almarsson, Pasut Ratanabanangkoon, Julius Remenar, Hector Guzman
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Publication number: 20090011059Abstract: The present invention relates to the use of a ginger extract on its own or in combination with pharmaceutical compositions for inhibiting human drug transporters for positively influencing the oral bioavailability and pharmacokinetics of active substances.Type: ApplicationFiled: December 20, 2006Publication date: January 8, 2009Inventors: Naoki Ishiguro, Wataru Kishimoto, Thomas Ebner, Willy Roth
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Patent number: 7465752Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes, to pharmaceutical compositions comprising them and to the processes for the preparation of these compounds.Type: GrantFiled: April 6, 2005Date of Patent: December 16, 2008Assignee: Merck Patent GmbHInventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
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Patent number: 7446124Abstract: Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.Type: GrantFiled: July 11, 2005Date of Patent: November 4, 2008Assignees: Prolx Pharmaceuticals Corp., The University of Pittsburgh, Arizona Board of Regents, Acting on Behalf of the University of ArizonaInventors: Lynn Kirkpatrick, Garth Powis, Peter Wipf
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Publication number: 20080221018Abstract: The present invention provides crystalline solid and amorphous forms of (?)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (?)-halofenate.Type: ApplicationFiled: April 20, 2006Publication date: September 11, 2008Applicant: METABOLEX, INC.Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
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Patent number: 7410983Abstract: The present invention relates to a combination of a peroxisome proliferator activated receptor (PPAR) activator and a benzoquinone and their use in treating and/or preventing disorders characterized by endothelial dysfunction, such as cardiovascular disease, strokes and myocardial infarction. According to a preferred embodiment of the invention the benzoquinone or precursor thereof is a ubiquinone or precursor thereof, more preferably, coenzyme Q10 or a precursor thereof, and the PPAR activator is a fibrate or a thiazolidinedione, more preferably fenofibrate.Type: GrantFiled: October 23, 2001Date of Patent: August 12, 2008Assignee: Fournier Laboratories Ireland LimitedInventors: Gerald Francis Watts, David Alan Playford
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Publication number: 20080161276Abstract: The present invention relates to compositions containing a) at least one monoacyl lipid; b) at least one diacyl glycerol and/or tochopherol; and c) at least one fragmentation agent; and optionally an active agent. The compositions are capable of self-dispersing to provide colloidal non-lamellar particles upon contact with an aqueous fluid. The invention additionally provides a method for forming non-lamellar particles from such compositions, and pharmaceutical formulations containing the compositions, plus non-lamellar particles formable from the compositions.Type: ApplicationFiled: August 4, 2005Publication date: July 3, 2008Inventors: Markus Johnsson, Fredrik Joabsson, Fredrik Tiberg
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Publication number: 20080138424Abstract: The present invention is directed to fibrate compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The fibrate particles of the composition have an effective average particle size of less than about 2000 nm.Type: ApplicationFiled: October 31, 2007Publication date: June 12, 2008Inventors: Tuula Ryde, Evan E. Gustow, Stephen B. Ruddy, Rajeev Jain, Rakesh Patel, Michael John Wilkins
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Publication number: 20080131420Abstract: Disclosed herein are methods for treating mucositis (e.g., Alternaria-activated mucositis) that involves the direct mucoadministration of an active agent that is antifungal and antibacterial in an amount and for a duration effective to treat mucositis.Type: ApplicationFiled: July 13, 2007Publication date: June 5, 2008Applicant: Accentia, Inc.Inventor: Francis E. O'Donnell
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Patent number: 7355063Abstract: The compound represented by the following formula (1): wherein A, B, R1, R2, R3 and Z are as defined in the specification is analogous to shogaol and gingerol useful in the fields of foods, medicines, quasi-drugs, cosmetics, etc., and more highly active in tyrosinase activity inhibition, etc. than shogaol and gingerol.Type: GrantFiled: March 26, 2004Date of Patent: April 8, 2008Assignee: Toagosei Co., Ltd.Inventors: Shuhei Yamaguchi, Hisatoyo Kato
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Patent number: 7345191Abstract: A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z? are defined herein.Type: GrantFiled: February 26, 2005Date of Patent: March 18, 2008Assignee: Cambrex Charles City, Inc.Inventors: Paul Alan Jass, Jason Scott Douglas
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Patent number: 7329771Abstract: The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has ?3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.Type: GrantFiled: September 5, 2002Date of Patent: February 12, 2008Assignee: Kissei Pharmaceuticals Co., Ltd.Inventors: Nobuyuki Tanaka, Tetsuro Tamai, Harunobu Mukaiyama, Takehiro Ishikawa, Junichi Kobayashi, Satoshi Akahane, Hiromu Harada