Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/154)
  • Patent number: 9346738
    Abstract: 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: Grant
    Filed: May 22, 2013
    Date of Patent: May 24, 2016
    Assignee: SciPharm SaRL
    Inventors: Nareshkumar Jain, Michael Kirkup, Michael Marella, Sanjeevani Ghone
  • Patent number: 9125866
    Abstract: 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: Grant
    Filed: January 28, 2015
    Date of Patent: September 8, 2015
    Assignee: KING SAUD UNIVERSITY
    Inventors: Usama Sayed Karama, Mujeeb Abdullah Saeed Sultan, Kamal Eldin Hussein El Tahir, Abdulrahman Ibrahim Almansour
  • Patent number: 9040567
    Abstract: 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: Grant
    Filed: August 17, 2012
    Date of Patent: May 26, 2015
    Assignees: Emory University, Board of Regents of the University of Texas System
    Inventors: Xingming Deng, Jia Zhou, Chunyong Ding
  • Publication number: 20150119373
    Abstract: 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: Application
    Filed: April 19, 2013
    Publication date: April 30, 2015
    Inventors: 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
  • Patent number: 9012433
    Abstract: 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: Grant
    Filed: November 27, 2012
    Date of Patent: April 21, 2015
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Paul Abato, Todd Bowser
  • Publication number: 20150034887
    Abstract: 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: Application
    Filed: March 11, 2013
    Publication date: February 5, 2015
    Applicant: TOKUYAMA CORPORATION
    Inventors: Shinobu Izumi, Yasutomo Shimizu, Junji Momoda
  • Patent number: 8916071
    Abstract: 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: Grant
    Filed: September 21, 2012
    Date of Patent: December 23, 2014
    Assignee: Tokuyama Corporation
    Inventors: Yasutomo Shimizu, Shinobu Izumi, Junji Takenaka, Junji Momoda
  • Publication number: 20140343064
    Abstract: 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: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Applicant: Hanghzhou Bensheng Pharmaceutical Co., Ltd
    Inventors: Rongzhen Xu, Frank Rong, Hongxi Lai, Fuwen Xie
  • Publication number: 20140303150
    Abstract: 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: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Publication number: 20140256730
    Abstract: 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: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140256731
    Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Applicant: NABRIVA THERAPEUTICS AG
    Inventors: Rosemarie MANG, Werner HEILMAYER, Rudolf BADEGRUBER, Dirk B. STRICKMANN, Rodger NOVAK, Mathias FERENCIC, Atchyuta Rama Chandra Murty BULUSU
  • Publication number: 20140221361
    Abstract: 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: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Patent number: 8778236
    Abstract: 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: Grant
    Filed: March 7, 2012
    Date of Patent: July 15, 2014
    Assignee: Tokuyama Corporation
    Inventors: Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Toshiaki Takahashi, Mitsuyoshi Sando, Shinobu Izumi
  • Publication number: 20140178374
    Abstract: 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: Application
    Filed: August 17, 2012
    Publication date: June 26, 2014
    Applicants: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, EMORY UNIVERSITY
    Inventors: Xingming Deng, Jia Zhou, Chunyong Ding
  • Patent number: 8709308
    Abstract: 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: Grant
    Filed: January 26, 2012
    Date of Patent: April 29, 2014
    Assignee: Tokuyama Corporation
    Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Mitsuyoshi Sando, Shinobu Izumi
  • Patent number: 8691120
    Abstract: 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: Grant
    Filed: September 15, 2010
    Date of Patent: April 8, 2014
    Assignee: Tokuyama Corporation
    Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Mitsuyoshi Sando, Kazuhiro Teranishi
  • Patent number: 8691977
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 8, 2014
    Assignee: Neupharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20130310558
    Abstract: 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: Application
    Filed: March 15, 2013
    Publication date: November 21, 2013
    Inventor: Key M. Brummond
  • Publication number: 20130274240
    Abstract: 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: Application
    Filed: November 5, 2012
    Publication date: October 17, 2013
    Inventor: JAPAN TOBACCO INC.
  • Publication number: 20130210785
    Abstract: This disclosure relates to progesterone derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation resulting from traumatic brain injury or stroke.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 15, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: Emory University
  • Publication number: 20130203712
    Abstract: 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: Application
    Filed: May 19, 2011
    Publication date: August 8, 2013
    Applicant: University of Iowa Research Foundation
    Inventors: Christopher M. Adams, Steven D. Kunkel
  • Patent number: 8492365
    Abstract: 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: Grant
    Filed: June 9, 2009
    Date of Patent: July 23, 2013
    Assignees: 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
  • Publication number: 20130184263
    Abstract: 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: Application
    Filed: December 14, 2012
    Publication date: July 18, 2013
    Applicant: GlaxoSmithKline LLC
    Inventor: GlaxoSmithKline LLC
  • Publication number: 20130102779
    Abstract: 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: Application
    Filed: November 27, 2012
    Publication date: April 25, 2013
    Applicant: PARATEK PHARMACEUTICALS, INC.
    Inventor: Paratek Pharmaceuticals, Inc.
  • Publication number: 20130040954
    Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:
    Type: Application
    Filed: April 3, 2012
    Publication date: February 14, 2013
    Inventors: Rosemarie MANG, Werner HEILMAYER, Rudolf BADEGRUBER, Dirk B. STRICKMANN, Rodger NOVAK, Mathias FERENCIC, Atchyuta Rama Chandra Murty BULUSU
  • Patent number: 8343972
    Abstract: 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: Grant
    Filed: July 26, 2006
    Date of Patent: January 1, 2013
    Assignee: Nabriva Therapeutics AG
    Inventors: Rosemarie Mang, Heinz Berner
  • Patent number: 8318706
    Abstract: 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: Grant
    Filed: December 21, 2007
    Date of Patent: November 27, 2012
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Oak Kim, Haregewein Assefa, Laura Honeyman
  • Publication number: 20120252776
    Abstract: 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: Application
    Filed: March 12, 2012
    Publication date: October 4, 2012
    Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
  • Publication number: 20120251492
    Abstract: 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: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Makoto Ishikawa, Shigeki Suzuki, Makoto Aoki, Nobuto Minowa, Kokichi Suzuki
  • Publication number: 20120170098
    Abstract: 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: Application
    Filed: September 15, 2010
    Publication date: July 5, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Mitsuyoshi Sando, Kazuhiro Teranishi
  • Publication number: 20120135968
    Abstract: 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: Application
    Filed: May 7, 2010
    Publication date: May 31, 2012
    Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
  • Publication number: 20120115818
    Abstract: 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: Application
    Filed: April 30, 2010
    Publication date: May 10, 2012
    Applicant: President and Felows of Harvard College
    Inventors: Andrew G. Myers, David A. Kummer, Derun Li, Evan Hecker, Amelie Dion, Peter M. Wright
  • Publication number: 20120115819
    Abstract: 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: Application
    Filed: May 13, 2010
    Publication date: May 10, 2012
    Inventors: Roger B. Clark, Diana Katharine Hunt, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus P. Rönn
  • Publication number: 20120115862
    Abstract: 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: Application
    Filed: October 9, 2009
    Publication date: May 10, 2012
    Inventors: Stefan Laufer, Wolfgang Albrecht
  • Publication number: 20120052019
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Application
    Filed: August 22, 2011
    Publication date: March 1, 2012
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20120046291
    Abstract: 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: Application
    Filed: November 2, 2007
    Publication date: February 23, 2012
    Inventors: Theodore J. Nitz, Christian Montalbetti, Richard Mears, Xinjie Gai, Edward Glenn
  • Publication number: 20110182828
    Abstract: 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: Application
    Filed: December 18, 2008
    Publication date: July 28, 2011
    Applicant: Schering Corporation
    Inventors: 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
  • Publication number: 20110086822
    Abstract: 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: Application
    Filed: October 8, 2010
    Publication date: April 14, 2011
    Inventors: 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
  • Publication number: 20110077251
    Abstract: 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: Application
    Filed: August 16, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
  • Publication number: 20110021480
    Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.
    Type: Application
    Filed: September 28, 2010
    Publication date: January 27, 2011
    Applicant: Solvay Pharmaceuticals GmbH
    Inventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
  • Publication number: 20100327735
    Abstract: 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: Application
    Filed: June 29, 2009
    Publication date: December 30, 2010
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: James Anthony Cella, Joseph John Shiang
  • Publication number: 20100305129
    Abstract: 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: Application
    Filed: August 11, 2010
    Publication date: December 2, 2010
    Applicant: Burnham Institute for Medical Research
    Inventors: Zéev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
  • Publication number: 20100305072
    Abstract: 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: Application
    Filed: December 21, 2007
    Publication date: December 2, 2010
    Inventors: 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
  • Publication number: 20100105671
    Abstract: 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: Application
    Filed: August 7, 2009
    Publication date: April 29, 2010
    Inventors: Jingye Zhou, Xiao-Yi Xiao, Louis Plamondon, Diana Katharine Hunt, Roger B. Clark, Robert B. Zahler
  • Publication number: 20100048892
    Abstract: 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: Application
    Filed: April 20, 2009
    Publication date: February 25, 2010
    Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
  • Patent number: 7655653
    Abstract: 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: Grant
    Filed: October 25, 2007
    Date of Patent: February 2, 2010
    Assignee: N.V. Organon
    Inventor: Hubert Jan Jozef Loozens
  • Patent number: 7557208
    Abstract: Described are naphthols useful in the manufacture of novel indeno-fused photochromic naphthopyran materials.
    Type: Grant
    Filed: November 11, 2008
    Date of Patent: July 7, 2009
    Assignee: Transitions Optical, Inc.
    Inventors: Robert W. Walters, Anil Kumar, Clara E. Nelson, Anu Chopra
  • Publication number: 20090118267
    Abstract: 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: Application
    Filed: February 13, 2006
    Publication date: May 7, 2009
    Inventors: Dirk Finsinger, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Kai Schiemann, Wolfgang Staehle, Christiane Amendt, Nina Heiss, Frank Zenke
  • Patent number: 7517982
    Abstract: Described are naphthols useful in the manufacture of novel indeno-fused photochromic naphthopyran materials.
    Type: Grant
    Filed: March 1, 2007
    Date of Patent: April 14, 2009
    Assignee: Transitions Optical, Inc.
    Inventors: Robert W. Walters, Anil Kumar, Clara E. Nelson, Anu Chopra
  • Patent number: RE42700
    Abstract: 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: Grant
    Filed: July 25, 2008
    Date of Patent: September 13, 2011
    Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State University
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs