Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/154)
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Patent number: 11938228Abstract: A device for delivery of a first therapeutic agent and a second therapeutic agent to a site in epithelial tissue includes a first layer having a first, freeze-dried polymeric matrix having first and second opposed surfaces, formed by a composition including chitosan, a hydration promoter, a particle adhesion inhibitor, and a particle aggregation inhibitor, and a plurality of first particles embedded within the first matrix so as to be directly surrounded by, and in contact with, the first matrix, the first particles containing the first therapeutic agent and having a coating around the first therapeutic agent, the coating including chitosan. The device further includes a second layer, adjacent to the first layer, having a second, freeze-dried polymeric matrix containing the second therapeutic agent, the first layer and/or the second layer is configured to be attached to the site in the epithelial tissue.Type: GrantFiled: January 7, 2019Date of Patent: March 26, 2024Assignee: PRIVO TECHNOLOGIES, INC.Inventors: Manijeh Nazari Goldberg, Brandon LaPorte, Aaron Manzi, Amritpreet Birdi
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Patent number: 9346738Abstract: A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.Type: GrantFiled: May 22, 2013Date of Patent: May 24, 2016Assignee: SciPharm SaRLInventors: Nareshkumar Jain, Michael Kirkup, Michael Marella, Sanjeevani Ghone
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Patent number: 9125866Abstract: The antidepressant compounds are compounds of the formula: wherein R1 and R2 are either both hydrogen or both halogen (particularly chlorine), and if R1 and R2 are both hydrogen, R3 and R4 are both halogen (particularly chlorine), otherwise both R3 and R4 are hydrogen; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 28, 2015Date of Patent: September 8, 2015Assignee: KING SAUD UNIVERSITYInventors: Usama Sayed Karama, Mujeeb Abdullah Saeed Sultan, Kamal Eldin Hussein El Tahir, Abdulrahman Ibrahim Almansour
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Patent number: 9040567Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.Type: GrantFiled: August 17, 2012Date of Patent: May 26, 2015Assignees: Emory University, Board of Regents of the University of Texas SystemInventors: Xingming Deng, Jia Zhou, Chunyong Ding
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Publication number: 20150119373Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.Type: ApplicationFiled: April 19, 2013Publication date: April 30, 2015Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Mamnoor Prem Kumar, Kasireddy Bhaskar Reddy, Mogili Narsingam, Mukkera Venkati, Lanka VL Subrahmanyam, Ravi Mallikarjun Reddy
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Patent number: 9012433Abstract: The present invention pertains to tetracycline compounds of formula (VIIa): R5*, R5*?, R7r*, and R9m* are defined herein. These tetracycline compounds can be used to treat tetracycline compound-responsive states, such as multiple sclerosis and rheumatoid arthritis.Type: GrantFiled: November 27, 2012Date of Patent: April 21, 2015Assignee: Paratek Pharmaceuticals, Inc.Inventors: Paul Abato, Todd Bowser
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Publication number: 20150034887Abstract: A novel photochromic compound which develops a color of a neutral tint (double peak characteristic) and has high color optical density, high fading speed and excellent durability. Like a compound represented by the following formula (20), the photochromic compound having a group (methylthio group in the following formula 20) which has a sulfur atom bonded to the 7-position carbon atom is a photochromic compound having high color optical density, high fading speed and excellent durability.Type: ApplicationFiled: March 11, 2013Publication date: February 5, 2015Applicant: TOKUYAMA CORPORATIONInventors: Shinobu Izumi, Yasutomo Shimizu, Junji Momoda
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Patent number: 8916071Abstract: A chromene compound which has a sulfur-containing substituent represented by the following formula (2) at the 6-position and/or 7-position carbon atom of an indeno(2,1-f)naphtho(1,2-b)pyran structure and is excellent in photochromic properties and stability at a high temperature. In the formula (2), ring X is an aromatic hydrocarbon ring or aromatic heterocyclic ring, R3 and R4 are each independently an alkyl group, haloalkyl group, cycloalkyl group, alkoxy group, amino group, heterocyclic group containing a ring member nitrogen atom and bonded to the ring X bonded thereto via the nitrogen atom, halogen atom, aryloxy group or aryl group, and “a” is an integer of 0 to 4.Type: GrantFiled: September 21, 2012Date of Patent: December 23, 2014Assignee: Tokuyama CorporationInventors: Yasutomo Shimizu, Shinobu Izumi, Junji Takenaka, Junji Momoda
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Publication number: 20140343064Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.Type: ApplicationFiled: November 30, 2012Publication date: November 20, 2014Applicant: Hanghzhou Bensheng Pharmaceutical Co., LtdInventors: Rongzhen Xu, Frank Rong, Hongxi Lai, Fuwen Xie
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Publication number: 20140303150Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.Type: ApplicationFiled: December 22, 2011Publication date: October 9, 2014Applicant: LEO Laboratories LimitedInventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
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Publication number: 20140256731Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:Type: ApplicationFiled: May 21, 2014Publication date: September 11, 2014Applicant: NABRIVA THERAPEUTICS AGInventors: Rosemarie MANG, Werner HEILMAYER, Rudolf BADEGRUBER, Dirk B. STRICKMANN, Rodger NOVAK, Mathias FERENCIC, Atchyuta Rama Chandra Murty BULUSU
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Publication number: 20140256730Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.Type: ApplicationFiled: January 13, 2014Publication date: September 11, 2014Applicant: Corsair Pharma, Inc.Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
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Publication number: 20140221361Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
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Patent number: 8778236Abstract: A novel photochromic compound which develops a color of a neutral tint and has high color optical density, high fading speed and excellent durability. The present invention is a chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as the basic skeleton in which a hetero ring having two hetero atoms including at least one sulfur atom is directly bonded to the 6-position and the 7-position of the indeno(2,1-f)naphtho(1,2-b)pyran structure via the hetero atom like the compound represented by the following formula (18).Type: GrantFiled: March 7, 2012Date of Patent: July 15, 2014Assignee: Tokuyama CorporationInventors: Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Toshiaki Takahashi, Mitsuyoshi Sando, Shinobu Izumi
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Publication number: 20140178374Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.Type: ApplicationFiled: August 17, 2012Publication date: June 26, 2014Applicants: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, EMORY UNIVERSITYInventors: Xingming Deng, Jia Zhou, Chunyong Ding
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Patent number: 8709308Abstract: The chromene compound is represented by the following formula (I), wherein R3 at the 11-position is a sulfur-containing substituent selected from the group consisting of thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group, heteroarylthio group, sulfonyl group and sulfinyl group, R1 and R2 at the 6-position and the 7-position are a combination of an aryl group or a heteroaryl group and an electron donating group having a Hammett constant ?p of ?0.1 or less, or R1 and/or R2 is sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group.Type: GrantFiled: January 26, 2012Date of Patent: April 29, 2014Assignee: Tokuyama CorporationInventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Mitsuyoshi Sando, Shinobu Izumi
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Patent number: 8691977Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: GrantFiled: August 22, 2011Date of Patent: April 8, 2014Assignee: Neupharma, Inc.Inventors: Xiangping Qian, Yong-Liang Zhu
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Patent number: 8691120Abstract: A photochromic chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as its basic skeleton, an aryl group or a heteroaryl group at the 6-position carbon atom of the structure and an electron donor group having a Hammett constant ?p of not more than ?0.1 at the 7-position carbon atom.Type: GrantFiled: September 15, 2010Date of Patent: April 8, 2014Assignee: Tokuyama CorporationInventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Mitsuyoshi Sando, Kazuhiro Teranishi
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Publication number: 20130310558Abstract: Methods for the synthesis and use of functionalized, substituted naphthalenes are described. The functionalized, substituted naphthalenes display useful properties including liquid crystals and fluorescence properties, such as solvatochromatic fluorescence, with high quantum yields, Stoke's shift, and show emission maxima that are significantly red-shifted.Type: ApplicationFiled: March 15, 2013Publication date: November 21, 2013Inventor: Key M. Brummond
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Publication number: 20130274240Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.Type: ApplicationFiled: November 5, 2012Publication date: October 17, 2013Inventor: JAPAN TOBACCO INC.
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Publication number: 20130210785Abstract: This disclosure relates to progesterone derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation resulting from traumatic brain injury or stroke.Type: ApplicationFiled: February 14, 2013Publication date: August 15, 2013Applicant: EMORY UNIVERSITYInventor: Emory University
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Publication number: 20130203712Abstract: In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: May 19, 2011Publication date: August 8, 2013Applicant: University of Iowa Research FoundationInventors: Christopher M. Adams, Steven D. Kunkel
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Patent number: 8492365Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: GrantFiled: June 9, 2009Date of Patent: July 23, 2013Assignees: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
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Publication number: 20130184263Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.Type: ApplicationFiled: December 14, 2012Publication date: July 18, 2013Applicant: GlaxoSmithKline LLCInventor: GlaxoSmithKline LLC
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Publication number: 20130102779Abstract: The present invention pertains to tetracycline compounds of formula (VIIa): R5*, R5*?, R7r*, and R9m* are defined herein. These tetracycline compounds can be used to treat tetracycline compound-responsive states, such as multiple sclerosis and rheumatoid arthritis.Type: ApplicationFiled: November 27, 2012Publication date: April 25, 2013Applicant: PARATEK PHARMACEUTICALS, INC.Inventor: Paratek Pharmaceuticals, 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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Patent number: 8343972Abstract: The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.Type: GrantFiled: July 26, 2006Date of Patent: January 1, 2013Assignee: Nabriva Therapeutics AGInventors: Rosemarie Mang, Heinz Berner
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Patent number: 8318706Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.Type: GrantFiled: December 21, 2007Date of Patent: November 27, 2012Assignee: Paratek Pharmaceuticals, Inc.Inventors: Oak Kim, Haregewein Assefa, Laura Honeyman
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Publication number: 20120251492Abstract: Provided are a triterpene derivative represented by a general formula (I), a pharmaceutically acceptable salt thereof, and an agent for preventing or treating chronic hepatitis C comprising the triterpene derivative or the salt as an active ingredient: [in the formula (I), R1 represents a carboxyl group, a hydroxymethyl group, —CH2OSO3H, or and R2 represents —OR3 or —O— (CH2) m-OR4, where R3 represents a benzyl group which may be substituted with a hydroxymethyl group, a dimethylaminomethyl group, a phenylaminomethyl group, a morpholinomethyl group, a carboxyl group, or a formyl group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or a hydroxy C1-6 alkyl group, R4 represents a phenyl group which may be substituted with a carboxyl group, and m represents an integer of 1 to 3, with the proviso that a case where R1 is —CH2OH, and R3 is a C1-6 alkyl group, a C2-6 alkenyl group, or a benzyl group is excluded].Type: ApplicationFiled: December 15, 2010Publication date: October 4, 2012Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Makoto Ishikawa, Shigeki Suzuki, Makoto Aoki, Nobuto Minowa, Kokichi Suzuki
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Publication number: 20120252776Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of 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, for example as antioxidant inflammation modulators, and compositions thereof are also provided.Type: ApplicationFiled: March 12, 2012Publication date: October 4, 2012Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
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Publication number: 20120170098Abstract: A photochromic chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as its basic skeleton, an aryl group or a heteroaryl group at the 6-position carbon atom of the structure and an electron donor group having a Hammett constant ?p of not more than ?0.1 at the 7-position carbon atom.Type: ApplicationFiled: September 15, 2010Publication date: July 5, 2012Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Mitsuyoshi Sando, Kazuhiro Teranishi
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Publication number: 20120135968Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.Type: ApplicationFiled: May 7, 2010Publication date: May 31, 2012Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
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Publication number: 20120115818Abstract: Efficient method for preparing the enone intermediate (VII) used in the synthesis of tetracyclines derivatives. In particular, the invention provides a synthesis which allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.Type: ApplicationFiled: April 30, 2010Publication date: May 10, 2012Applicant: President and Felows of Harvard CollegeInventors: Andrew G. Myers, David A. Kummer, Derun Li, Evan Hecker, Amelie Dion, Peter M. Wright
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Publication number: 20120115819Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.Type: ApplicationFiled: May 13, 2010Publication date: May 10, 2012Inventors: Roger B. Clark, Diana Katharine Hunt, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus P. Rönn
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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: 20120052019Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: ApplicationFiled: August 22, 2011Publication date: March 1, 2012Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20120046291Abstract: The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).Type: ApplicationFiled: November 2, 2007Publication date: February 23, 2012Inventors: Theodore J. Nitz, Christian Montalbetti, Richard Mears, Xinjie Gai, Edward Glenn
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Publication number: 20110182828Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.Type: ApplicationFiled: December 18, 2008Publication date: July 28, 2011Applicant: Schering CorporationInventors: John C. Anthes, Kevin D. Mccormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Daniel M. Solomon, Phillippa H. Solomon, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar
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Publication number: 20110086822Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: ApplicationFiled: October 8, 2010Publication date: April 14, 2011Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Upul Bandarage, Joel Berniac, Beena Bhatia, Jackson Chen, Mohamed Y. Ismail, Oak Kim, Laura Honeyman, Rachid Mechiche, Andre Pearson, Laxma Reddy Nagavelli, Paul Sheahan, Atul K. Verma, Peter Viski, Tadeusz Warchol
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Publication number: 20110077251Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2010Publication date: March 31, 2011Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
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Publication number: 20110021480Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.Type: ApplicationFiled: September 28, 2010Publication date: January 27, 2011Applicant: Solvay Pharmaceuticals GmbHInventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
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Publication number: 20100327735Abstract: Optoelectronic devices include triplet blocking compounds of formula I wherein R1 is, independently at each occurrence, C1-20 hydrocarbyl and at least one of R1 is R3; R2 is independently at each occurrence C1-20 hydrocarbyl, C1-20 hydrocarbyloxy, C1-20 thioether, C1-20 hydrocarbylcarbonyloxy or cyano; R3 is —R4XR5; R4 is a direct bond, C1-20 aryl, C1-20 arylalkyl, C1-20 alkylaryl, C1-20 substituted aryl, C1-20 substituted arylalkyl, or C1-20 substituted alkylaryl; R5 is C1-20 hydrocarbyl or C1-20 hydrocarbyl containing at least one S, N, O or P atom between carbon atoms; R6 is C1-20 alkyl or C1-20 substituted alkyl; X is —O—, —S—, —COO—, —OOC—, —CSS—, —SSC—, NR6 or PR6; a is independently at each occurrence 0, 1 or 2; and n is 0 or 1.Type: ApplicationFiled: June 29, 2009Publication date: December 30, 2010Applicant: GENERAL ELECTRIC COMPANYInventors: James Anthony Cella, Joseph John Shiang
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Publication number: 20100305129Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.Type: ApplicationFiled: August 11, 2010Publication date: December 2, 2010Applicant: Burnham Institute for Medical ResearchInventors: Zéev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
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Publication number: 20100305072Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.Type: ApplicationFiled: December 21, 2007Publication date: December 2, 2010Inventors: Oak K. Kim, Mark L. Nelson, Paul Abato, Haregewein Assefa, Joel Bernaiac, Mohamed Y. Ismail, Todd Bowser, Mark Grier, Beena Bhatia, Atul K. Verma, Laura Honeyman, Jingwen Pan
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Publication number: 20100105671Abstract: The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.Type: ApplicationFiled: August 7, 2009Publication date: April 29, 2010Inventors: Jingye Zhou, Xiao-Yi Xiao, Louis Plamondon, Diana Katharine Hunt, Roger B. Clark, Robert B. Zahler
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Publication number: 20100048892Abstract: 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: April 20, 2009Publication date: February 25, 2010Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
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Patent number: 7655653Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.Type: GrantFiled: October 25, 2007Date of Patent: February 2, 2010Assignee: N.V. OrganonInventor: Hubert Jan Jozef Loozens
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Patent number: 7557208Abstract: Described are naphthols useful in the manufacture of novel indeno-fused photochromic naphthopyran materials.Type: GrantFiled: November 11, 2008Date of Patent: July 7, 2009Assignee: Transitions Optical, Inc.Inventors: Robert W. Walters, Anil Kumar, Clara E. Nelson, Anu Chopra
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Publication number: 20090118267Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: February 13, 2006Publication date: May 7, 2009Inventors: Dirk Finsinger, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Kai Schiemann, Wolfgang Staehle, Christiane Amendt, Nina Heiss, Frank Zenke
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Patent number: RE42700Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.Type: GrantFiled: July 25, 2008Date of Patent: September 13, 2011Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State UniversityInventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs