Only Two Ring Oxygens In The Hetero Ring Which Is Not A Polycyclo Ring System (e.g., Dioxolane, Etc.) Patents (Class 514/467)
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Publication number: 20130150416Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.Type: ApplicationFiled: June 2, 2012Publication date: June 13, 2013Inventors: Richard D. Wood, William Welsh
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Patent number: 8436042Abstract: The present disclosure relates to methods of preparation of compounds resulting from the reaction of levulinic esters and epoxidized unsaturated fatty acid esters. The compounds are useful as renewable biomass-based plasticizers for a variety of polymers. Mono-, di- and tri-ketal adducts formed in a reaction between alkyl esters of levulinate and epoxidized unsaturated fatty acid esters derived from vegetable oils are also disclosed.Type: GrantFiled: November 22, 2006Date of Patent: May 7, 2013Assignee: Segetis, Inc.Inventor: Sergey Selifonov
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Publication number: 20130109639Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: November 1, 2012Publication date: May 2, 2013Inventors: Adam D. HUGHES, Erik FENSTER, Melissa FLEURY, Roland GENDRON
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Publication number: 20130102641Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.Type: ApplicationFiled: December 13, 2012Publication date: April 25, 2013Applicant: XENOPORT, INC.Inventor: XENOPORT, INC.
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Publication number: 20130040954Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:Type: ApplicationFiled: April 3, 2012Publication date: February 14, 2013Inventors: Rosemarie MANG, Werner HEILMAYER, Rudolf BADEGRUBER, Dirk B. STRICKMANN, Rodger NOVAK, Mathias FERENCIC, Atchyuta Rama Chandra Murty BULUSU
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Publication number: 20120329866Abstract: The invention provides compounds of Formula (I): R1?R2??(I) wherein R1 and R2 have any of the values or specific values defined herein, as well as compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.Type: ApplicationFiled: May 23, 2012Publication date: December 27, 2012Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATIONInventors: Gerald B. Hammond, Bo Xu, Paula J. Bates
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Publication number: 20120309819Abstract: The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.Type: ApplicationFiled: June 5, 2012Publication date: December 6, 2012Inventors: James D. McChesney, John T. Henri, Sylesh Kumar Venkataraman, Mahesh Kumar Gundluru
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Patent number: 8318800Abstract: The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.Type: GrantFiled: December 13, 2007Date of Patent: November 27, 2012Assignee: SanofiInventors: Bernard Abramovici, Jean-Claude Gautier, Jean-Claude Gromenil, Jean-Marie Marrier
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Publication number: 20120270934Abstract: This invention relates to novel prostacyclin derivatives and acceptable salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.Type: ApplicationFiled: July 2, 2010Publication date: October 25, 2012Inventors: Craig E. Masse, Scott L. Harbeson, Roger D. Tung
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Publication number: 20120225917Abstract: The present invention provides a pest control composition having an excellent controlling effect on pests, which comprises a combination of an ester compound represented by the formula (1): and a cyclic compound represented by the formula (2a) and/or a cyclic compound represented by the formula (2b).Type: ApplicationFiled: November 19, 2010Publication date: September 6, 2012Inventors: Masahiro Yamada, Yoshito Tanaka
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Patent number: 8258177Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: August 11, 2011Date of Patent: September 4, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Publication number: 20120208807Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.Type: ApplicationFiled: July 1, 2010Publication date: August 16, 2012Applicant: VALOCOR THERAPEUTICS, INC.Inventors: Timothy Scott Daynard, Geoffrey C. Winters, David W.C. Hunt
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Patent number: 8188089Abstract: Compounds of Formula I are described: preferably subject to the proviso that either (a) R2 and R3 together form —O—CH(R10)—O—, or (b) R5 and R6 together form —O—CH(R10)—O—, wherein R10 is H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described.Type: GrantFiled: December 20, 2006Date of Patent: May 29, 2012Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Linyi Wei, Kenneth F. Bastow, Arnold Brossi, Tian-Shung Wu
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Publication number: 20120122844Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Publication number: 20120115862Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1? and/or TNF-?. They can therefore be used for treatment of diseases connected with a disturbance in the immune system.Type: ApplicationFiled: October 9, 2009Publication date: May 10, 2012Inventors: Stefan Laufer, Wolfgang Albrecht
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Publication number: 20120088823Abstract: Provided is a composition for scalp and hair treatment, comprising a menthol derivative and a prostaglandin compound having two hetero atoms at the 15 position. The composition of the present invention is effective not only for preventing dandruff and itchy scalp but also for preventing or treating hair loss, baldness, or hair thinness.Type: ApplicationFiled: December 19, 2011Publication date: April 12, 2012Applicant: R-TECH UENO, LTD.Inventors: Masato IINO, Satoshi YAMAKI, Satoshi NAKANISHI, Masahiro TAJIMA, Ryuji UENO
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Publication number: 20120076744Abstract: The present invention relates to a compound with the following general formula (I): in which: R1 is a hydrocarbon chain of an unsaturated fatty acid from C12 to C24 including at least one unsaturation; and R2 and R3 are, independently or simultaneously: a hydrogen or a C1-C3 alkyl or a phenyl; and R4: a hydrogen atom or COR1?, where R1? is a hydrocarbon chain of an unsaturated fatty acid from C12 to C24 including at least one unsaturation, advantageously 1 to 6 and preferably 1 to 4.Type: ApplicationFiled: June 8, 2010Publication date: March 29, 2012Applicant: PIERRE FABRE DERMO-COSMETIQUEInventors: Stéphane Poigny, Sylvie Daunes-Marion, Nathalie Castex Rizzi, Patrick Bogdanowicz
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Publication number: 20120035196Abstract: [Problem] The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes. [Means for Solution] The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the present invention or a pharmaceutically acceptable salt thereof, in which a carboxylic acid is bonded to a bicyclic or tricyclic moiety through methylene, and further, a benzene ring substituted with a monocyclic 6-membered aromatic ring is bonded to a bicyclic or tricyclic moiety through —O-methylene or —NH-methylene, has an excellent GPR40 agonistic activity. They have also found that the compound has an excellent insulin secretion promoting action and strongly inhibits increase in the blood glucose after glucose loading, thereby completing the present invention.Type: ApplicationFiled: April 21, 2010Publication date: February 9, 2012Inventors: Kenji Negoro, Kei Ohnuki, Yasuhiro Yonetoku, Kazuyuki Kuramoto, Yasuharu Urano, Hideyuki Watanabe
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Publication number: 20120022100Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventors: Juergen Klaus Maibaum, Daniel K. Baeschlin, Holger Sellner
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Publication number: 20110312904Abstract: The present invention provides compounds of Formula (I), compositions comprising an effective amount of a compound of Formula (I), optionally with chemotherapeutic drugs such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, treating or preventing cancer or a neuropathic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making compounds of Formula (I).Type: ApplicationFiled: August 27, 2009Publication date: December 22, 2011Applicants: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH, TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Samuel J. Danishefsky, Ting-Chao Chou, Xiaoguang Lei, Heedong Yun, Fay Ng, John Hartung, Dalibor Sames
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Publication number: 20110294875Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: ApplicationFiled: August 11, 2011Publication date: December 1, 2011Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Publication number: 20110294830Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Jyun Iwata, Masahiro Kawaguchi, Akiko Mizui
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Publication number: 20110275709Abstract: Use of tellurium-containing compounds for maintaining and/or augmenting fertility in a male subject following chemotherapy and/or radiotherapy is disclosed. The tellurium-containing compound is utilized in combination with a chemotherapeutic agent and/or radiation, such that the male subject treated by the chemotherapeutic agent and/or radiation and by the tellurium-containing compound is instructed to refrain from conceptive sex for a pre-determined time period, following the chemotherapy and/or radiotherapy, during which conception is undesired.Type: ApplicationFiled: January 7, 2010Publication date: November 10, 2011Applicant: BIOMAS LTD.Inventors: Benjamin Sredni, Michael Albeck, Benjamin Ron
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Patent number: 8053468Abstract: The present disclosure relates to the preparation of ketal compounds from glycerol and levulinic acid and esters, and uses thereof.Type: GrantFiled: November 22, 2006Date of Patent: November 8, 2011Assignee: Segetis, Inc.Inventor: Sergey Selifonov
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Publication number: 20110245206Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: February 23, 2011Publication date: October 6, 2011Inventors: XIN JIANG, XIAOFENG LIU, JACK GREINER, STEPHEN S. SZUCS, MELEAN VISNICK
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Publication number: 20110223105Abstract: There is provided a compound of Formula and salts thereof wherein R1 is an imine or an alkylated imine, said imine or alkylated imine comprising a linear or branched alkyl group of length C1 to C5; R2 are each independently (a) an unsubstituted or substituted linear or branched alkyl group of chain length C1-7; (b) an aryl substituted alkyl group, wherein said aryl group is substituted, (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group; or (d) an H atom; wherein said substituents in (a) and (b) are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo and fluoro groups. R3 and R4 are linear or branched alkyl groups of length C1 to C6 constituting a ketal or a cyclic ketal. The compounds claimed may be used for the manufacture of a medicament.Type: ApplicationFiled: September 1, 2009Publication date: September 15, 2011Inventors: Leif A. Eriksson, Lennart Löfgren
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Patent number: 7956087Abstract: The present invention is to provide skin cosmetics and anti-wrinkle agents which are excellent in reducing effect on wrinkle caused by photoaging. Skin cosmetics and anti-wrinkle agents which comprise a sugar alcohol derivative represented by the following formula (1): (wherein n is 1 to 5, preferably n=2.).Type: GrantFiled: April 12, 2006Date of Patent: June 7, 2011Assignee: Kao CorporationInventors: Kyoko Miura, Akinori Haratake
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Publication number: 20110124690Abstract: The present invention relates to compositions comprising an effective amount of a Panaxytriol Compound and a tubulin-binding drug, methods for treating or preventing cancer or a neurotrophic disorder comprising administering to a subject in need thereof an effective amount of a Panaxytriol Compound and a tubulin-binding drug, and methods for making a Panaxytriol Compound.Type: ApplicationFiled: February 22, 2008Publication date: May 26, 2011Inventors: Samuel J. Danishefsky, Heedong Yun, Ting-Chao Chou, Xiaoguang Lei, Dalibor Sames
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Publication number: 20110117147Abstract: The invention relates to a cooling sensation agent composition with a prolonged cool sensation effect comprising at least one compound selected from Formula (1) wherein each of A and B is a hydrogen atom or a hydrocarbon group which may have one or more substituents, in which A and B are not hydrogen atoms simultaneously, and the total number of carbon atoms in A and B is in the range of 6 to 18; and Formulae (2) to (4) wherein R1, R2, and R3 each represent a residue of an alcohol selected from 1-menthol, 1-isopulegol, 3-(1-menthoxy)propan-1,2-diol, 2-(1-menthoxy)ethan-1-ol, 3-(1-menthoxy)propan-1-ol, 2-methyl-3-(1-menthoxy)propan-1,2-diol and para-menthan-3,8-diol), and R4 represents a residue of a branched or straight-chain, cyclic or linear, or saturated or unsaturated alcohol having 6 to 18 carbon atoms that may have one or more aromatic rings that may have a condensed ring and substituent groups such as hydroxyl and ether groups; and R6 represents a hydrocarbon group having 11 to 19 carbon atoms that mayType: ApplicationFiled: April 1, 2009Publication date: May 19, 2011Inventors: Kenya Ishida, Takashi Aida, Tetsuya Yamamoto
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Publication number: 20110098350Abstract: Novel substituted cyclohexylidene-ethylidene-octahydro-indene compounds and compositions comprising the same are described. The compounds exhibit profound anti-proliferative effects, in comparison to other compounds known for their anti-cancer and anti-hyperproliferative ability. Methods of use of such compounds and compositions are described for treating a variety of cancers, inflammatory and other hyperproliferative diseases and disorders.Type: ApplicationFiled: June 16, 2009Publication date: April 28, 2011Inventors: Shimon Ben Shabat, Amnou Sintov
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Patent number: 7932252Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: GrantFiled: May 12, 2005Date of Patent: April 26, 2011Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Publication number: 20110044918Abstract: The present invention relates to the cosmetic use of a compound of formula (I) and also the cosmetically acceptable salts thereof, solvates thereof and isomers thereof, for non-therapeutic skincare.Type: ApplicationFiled: October 29, 2010Publication date: February 24, 2011Applicant: L'OREALInventors: Xavier Marat, Benoit Muller
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Patent number: 7879906Abstract: The invention provides compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.Type: GrantFiled: November 21, 2007Date of Patent: February 1, 2011Assignee: Anchen Laboratories, Inc.Inventors: Jenn-Tsang Hwang, Chrong-Shiong Hwang, Yow-Lone Chang, Chung-Niang Yao
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Publication number: 20100324001Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.Type: ApplicationFiled: June 30, 2010Publication date: December 23, 2010Applicant: Cortical Pty LTDInventors: Eric Francis Morand, Magdy Naguib Iskander, Colin Edward Skene
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Publication number: 20100305131Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 27, 2010Publication date: December 2, 2010Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20100297256Abstract: Compositions and methods for inhibiting integrin and treating integrin-related conditions, utilizing tellurium-containing compounds, are disclosed. The tellurium-containing compounds comprise at least one tellurium dioxo moiety and may have any one of Formulae I to IV as defined in the specification. Further disclosed are compositions and methods for treating a neoplastic condition characterized by a resistance to an anti-neoplastic agent and by a high level of expression of an integrin by neoplastic cells.Type: ApplicationFiled: November 23, 2008Publication date: November 25, 2010Inventors: Benjamin Sredni, Michael Albeck
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Patent number: 7815942Abstract: Disclosed are pharmaceutical preparations of R(+)-N-propargyl-1-aminoindan salts having enhanced content uniformity, processes for preparation of the compositions, and their uses.Type: GrantFiled: February 22, 2006Date of Patent: October 19, 2010Assignee: Teva Pharmaceutical Industries, Ltd.Inventor: Tirtza Berger Peskin
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Patent number: 7816401Abstract: A process for producing a compound represented by Formula (11): wherein P1, P7, P8, P9 and R1 are the same as defined herein, characterized by including reacting a compound represented by Formula (12): with a compound represented by Formula (13): in the presence of a catalyst.Type: GrantFiled: October 13, 2006Date of Patent: October 19, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Regina Mikie Kanada, Daisuke Ito, Takashi Sakai, Naoki Asai, Yoshihiko Kotake, Jun Niijima
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Patent number: 7776863Abstract: The invention encompasses pharmaceutical compositions and methods for using Compound 1 in combination with other agents for treating patients with AIDS or HIV infection.Type: GrantFiled: February 24, 2005Date of Patent: August 17, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Pin-Fang Lin, Beata Nowicka-Sans, Gregory Yamanaka
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Patent number: 7750049Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.Type: GrantFiled: December 6, 2007Date of Patent: July 6, 2010Assignee: Pharmeste S.R.L.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
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Patent number: 7749541Abstract: Disclosed are pharmaceutical preparations of R(+)-N-propargyl-1-aminoindan salts having enhanced content uniformity, processes for preparation of the compositions, and their uses.Type: GrantFiled: February 22, 2006Date of Patent: July 6, 2010Assignee: Teva Pharmaceutical Industries, Ltd.Inventor: Tirtza Berger Peskin
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Publication number: 20100111888Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A13 and CYP2B6.Type: ApplicationFiled: March 20, 2008Publication date: May 6, 2010Applicant: GIVAUDAN SAInventors: Boris Schilling, Thierry Granier, Georg Frater, Andreas Hanhart
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Publication number: 20100113460Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.Type: ApplicationFiled: March 20, 2008Publication date: May 6, 2010Applicant: Givaudan SAInventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
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Patent number: 7666903Abstract: The invention relates to reaction products of 2-propylheptanol with 1-halo-2,3-epoxypropanes and 1-hydroxy-2,3-epoxypropane (glycidol), to methods for their production, and to their use as cosurfactants, cleaning surfactants or thickeners.Type: GrantFiled: October 1, 2003Date of Patent: February 23, 2010Assignee: BASF AktiengesellschaftInventors: Christian Wulff, Ralf Noerenberg, Michael Kluge, Norbert Wagner
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Patent number: 7629382Abstract: A novel neuroprotective agent is disclosed for the treatment and prevention of neurodegenerative disorders which is based on the administration of an effective amount of a tellurium compound which has a specific ability to induce the differentiation and interfere with apoptotic cell death pathways of neuronal PC-12 cells.Type: GrantFiled: September 15, 2005Date of Patent: December 8, 2009Assignee: BioMAS Ltd.Inventors: Benjamin Sredni, Michael Albeck
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Publication number: 20090291102Abstract: There are provided various compounds and compositions comprising polyunsaturated fatty acid monoglycerides and derivatives thereof. These compounds and compositions can be useful as cancer chemopreventive agents. They can also be useful for enhancing solubility of various active agents and enhancing their bioavailability.Type: ApplicationFiled: August 5, 2009Publication date: November 26, 2009Inventor: Samuel FORTIN
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Publication number: 20090208427Abstract: The invention relates to a sensory stimulant composition containing one or more of vanillin acetals represented by the general formula (1), and a flavor and fragrance composition, a beverage or food product, a fragrance or cosmetic product, a daily utensil product, an oral composition, or a pharmaceutical product containing the sensory stimulant composition with a warming sensation agent or cooling sensation substance, if necessary. Vanillin acetals represented by the general formula (1) show an excellent pungent and/or warming sensation effect and a cooling sensation-emphasizing effect.Type: ApplicationFiled: July 5, 2006Publication date: August 20, 2009Inventors: Kenya Ishida, Takashi Aida
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Publication number: 20090197924Abstract: 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alkType: ApplicationFiled: January 27, 2009Publication date: August 6, 2009Applicants: Oroxcell, Alexis DenisInventors: Jean Pachot, Christophe Dini, Alexis Denis
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Publication number: 20090182031Abstract: Mammalian hair growth is reduced by topically applying a composition including a heat shock protein inhibitor.Type: ApplicationFiled: March 11, 2009Publication date: July 16, 2009Inventors: Natalia Botchkareva, Gurpreet S. Ahluwalia, Douglas Shander