Ring In Alcohol Moiety Patents (Class 560/32)
  • Patent number: 10351519
    Abstract: The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a sulfamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
    Type: Grant
    Filed: February 28, 2017
    Date of Patent: July 16, 2019
    Assignee: BIO-PHARM SOLUTIONS CO., LTD.
    Inventor: Yong Moon Choi
  • Patent number: 9029589
    Abstract: A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: May 12, 2015
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 9018253
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Grant
    Filed: July 1, 2011
    Date of Patent: April 28, 2015
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 9012497
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: April 21, 2015
    Assignee: Symrise AG
    Inventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
  • Publication number: 20150079035
    Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 19, 2015
    Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
  • Patent number: 8946475
    Abstract: The present invention provides methods for preparing a polymeric compound of Formula I: or pharmaceutically acceptable salt thereof. The present invention also provides useful intermediates for preparing the compound of Formula I or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: February 3, 2015
    Assignee: Cellceutix Corporation
    Inventors: Robert W. Kavash, Haizhong Tang, Carol Mulrooney, Dahui Liu
  • Publication number: 20140303344
    Abstract: The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D- mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.
    Type: Application
    Filed: March 12, 2014
    Publication date: October 9, 2014
    Applicant: BCN PÉPTIDES, S.A.
    Inventors: Llorenç RAFECAS JANE, Antoni RIERA ESCALE, Rosario RAMON ALBALATE, Monica ALONSO XALMA
  • Publication number: 20140051753
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 20, 2014
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Publication number: 20140012005
    Abstract: The present invention relates to a process for preparing chiral amino acids with excellent enantiomeric excesses.
    Type: Application
    Filed: December 22, 2011
    Publication date: January 9, 2014
    Applicant: Diverchim
    Inventors: Sylvain Darses, Nicolas Lefevre, Benoit Folleas, Jean-Louis Brayer
  • Publication number: 20130274502
    Abstract: The present invention provides methods for preparing a polymeric compound of Formula I: or pharmaceutically acceptable salt thereof. The present invention also provides useful intermediates for preparing the compound of Formula I or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 19, 2012
    Publication date: October 17, 2013
    Applicant: PolyMedix, Inc.
    Inventors: Robert W. Kavash, Haizhong Tang, Carol Mulrooney, Dahui Liu
  • Publication number: 20130274503
    Abstract: C1-C6Alkyloxy- or benzyloxy-carbonyl esters of -{3-[(E)-(1-phenyl or naphthyl C1-C4alkyl)-imino]-propyl}-amino)-acetic acid, which are intermediates for producing known bridged monobactam compounds useful in the treatment of bacterial infections.
    Type: Application
    Filed: April 26, 2013
    Publication date: October 17, 2013
    Applicant: BASILEA PHARMACEUTICA AG
    Inventors: Marc Muller, Xiaoping Wu, Lin Xu
  • Publication number: 20130261178
    Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C3 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; Z is linear C2-3 alkylene; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10 aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or further substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3;
    Type: Application
    Filed: July 5, 2010
    Publication date: October 3, 2013
    Inventors: Shailesh Mistry, Etienne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Publication number: 20130165509
    Abstract: A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided.
    Type: Application
    Filed: December 27, 2012
    Publication date: June 27, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Bio-Pharm Solutions Co., Ltd.
  • Publication number: 20130156710
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as skin and/or hair lightening (whitening) actives. The invention further relates to compositions and cosmetic, dermatological or therapeutic products comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.
    Type: Application
    Filed: May 25, 2010
    Publication date: June 20, 2013
    Applicant: SYMRISE AG
    Inventors: Gabriele Vielhaber, Heiko Oertling, Nicole Titze, Claudia Gömann, Rahim Brodhage
  • Publication number: 20130137710
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.
    Type: Application
    Filed: May 25, 2010
    Publication date: May 30, 2013
    Applicant: SYMRISE AG
    Inventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
  • Publication number: 20130137720
    Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 30, 2013
    Applicant: The Regents of the University of Colorado, a body corporated
    Inventors: Xiang Wang, Wenqing Xu
  • Publication number: 20130035377
    Abstract: Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.
    Type: Application
    Filed: April 15, 2011
    Publication date: February 7, 2013
    Applicants: UNIVERSITÀ DEGLI STUDI DI ROMA "LA SAPIENZA", UNIVERSITÀ DEGLI STUDI DI MILANO, UNIVERSITÀ DEGLI STUDI DI PAVIA, FONDAZIONE IEO
    Inventors: Saverio Minucci, Antonello Mai, Andrea Mattevi
  • Publication number: 20130005801
    Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.
    Type: Application
    Filed: July 1, 2011
    Publication date: January 3, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Publication number: 20120329945
    Abstract: The present invention relates to a curable composition, comprising specific meta-substituted aromatic compounds and at least one benzoxazine compound. In particular, the invention relates to the use of said meta-substituted aromatic compounds as curatives/catalysts for benzoxazine-containing compositions.
    Type: Application
    Filed: April 27, 2012
    Publication date: December 27, 2012
    Applicant: Henkel AG & Co. KGaa
    Inventors: Atsushi Mori, Atsushi Sudo, Takeshi Endo, Ryoichi Kudoh, Andreas Taden, Rainer Schoenfeld, Thomas Huver, Iris Christa Huver, Stefan Kreiling
  • Patent number: 8329945
    Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: December 11, 2012
    Assignee: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Jack Taunton, Christian A. Hassig, Timothy F. Jamison
  • Publication number: 20120302633
    Abstract: Herein described is a novel crystalline form of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester. In particular, herein described is a polymorph of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester, characterized by a Powder X Ray Diffraction spectrum as indicated in FIG. 1, and/or by a DSC profile as indicated in FIG. 2, and/or by a TGA profile as indicated in FIG. 3 and/or by an IR spectrum as indicated in FIG. 4.
    Type: Application
    Filed: December 3, 2010
    Publication date: November 29, 2012
    Applicant: CHEMI SPA
    Inventors: Stefano Turchetta, Maurizio Zenoni
  • Patent number: 8227636
    Abstract: The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: July 24, 2012
    Assignee: Merck HDAC Research, LLC
    Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
  • Publication number: 20120108515
    Abstract: Novel compounds which may be for treatment, prevention or alleviation of a condition associated with bone loss or low bone density or to inhibit osteoclast differentiation and stimulation, bone resorption, or loosening of a prosthetic device.
    Type: Application
    Filed: June 17, 2010
    Publication date: May 3, 2012
    Applicant: NEOBIOTICS AB
    Inventors: Anders Grubb, Franciszek Kasprzykowski, Ulf Lerner, Beata Zolnowska, Regina Kasprzykowska
  • Publication number: 20120065152
    Abstract: Prodrugs of guanfacine, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for improving the pharmacokinetics of guanfacine or minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration are provided herein.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 15, 2012
    Applicant: SHIRE LLC
    Inventors: Rhys Whomsley, Bernard T. Golding, Robert G. Tyson
  • Patent number: 8058468
    Abstract: The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds around the lead compound (3,4-dichloro-phenyl)-carbamic acid 2-isobutoxycarbonylamino-1-methyl-ethyl ester, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: November 15, 2011
    Assignee: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO
    Inventors: Frank Henri Johan Schuren, Henricus Matheus Wilhelmus Maria Thijssen, Roy Christiaan Montijn
  • Publication number: 20110144177
    Abstract: Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.
    Type: Application
    Filed: February 22, 2011
    Publication date: June 16, 2011
    Inventors: Jeroen C. Verheijen, ShouCheng Du
  • Publication number: 20110039874
    Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
    Type: Application
    Filed: April 16, 2010
    Publication date: February 17, 2011
    Applicant: Northeastern University
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Publication number: 20110009483
    Abstract: Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.
    Type: Application
    Filed: July 13, 2010
    Publication date: January 13, 2011
    Applicant: XenoPort, Inc.
    Inventors: Noa Zerangue, Bernd Jandeleit, Yunxiao Li, Mark A. Gallop
  • Publication number: 20100256229
    Abstract: The present invention is directed to compositions, methods of use, and processes for the synthesis related to 3-((S)-1-(dimethylamino)ethyl)phenyl methyl-((R)-1-phenylpropan-2 yl)carbamate, and its pharmaceutically acceptable salt forms, including the hydrogen fumarate salt. The present invention also relates to a novel form polymorph of 3-((S)-1-(dimethylamino)ethyl)phenylmethyl-((R)-1-phenylpropan-2 yl)carbamate, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
    Type: Application
    Filed: April 2, 2010
    Publication date: October 7, 2010
    Applicant: Colucid Pharmaceuticals, Inc.
    Inventors: Shoucheng Du, Marc W. Andersen, Daniel Coughlin, Alexander Kolchinski
  • Publication number: 20100249123
    Abstract: The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.
    Type: Application
    Filed: March 19, 2008
    Publication date: September 30, 2010
    Applicant: ADDEX PHARMA SA
    Inventors: Beatrice Bonnet, Brice Campo, Luca Raveglia, Mauro Riccaboni
  • Patent number: 7563937
    Abstract: The present invention is directed to a zeolite Y catalyst having a controlled macropore structure. The present invention is also directed to a zeolite Y catalyst composite and a process for preparing the catalyst composite. The catalyst composite exhibits reduced deactivation rates during the alkylation process, thereby increasing the life of the catalyst. The present invention is also directed to processes for the preparation of carbonated, overbased aromatic sulfonates, which processes comprise alkylation, carbonation of aromatic hydrocarbons with one or more olefins.
    Type: Grant
    Filed: February 15, 2006
    Date of Patent: July 21, 2009
    Assignees: Chevron Oronite Company LLC, Chevron Oronite S.A.
    Inventors: Thomas V. Harris, Curt B. Campbell, Paul J. Marcatntonio, Pierre Tequi, Jean-Louis Le Coent
  • Patent number: 7563938
    Abstract: The present invention is directed to novel alkylated aromatic compositions, zeolite catalyst compositions and processes for making the same. The catalyst compositions comprise zeolite Y and mordenite zeolite having a controlled macropore structure. The present invention is also directed to the preparation of the catalyst compositions and their use in the preparation of novel alkylated aromatic compositions. The catalyst compositions of the present invention exhibit reduced deactivation rates during the alkylation process, thereby increasing the life of the catalysts.
    Type: Grant
    Filed: February 15, 2006
    Date of Patent: July 21, 2009
    Assignees: Chevron Oronite Company LLC, Chevron Oronite S.A.
    Inventors: Curt B. Campbell, Thomas V. Harris, Pierre Tequi, Jean-Louis Le Coent
  • Patent number: 7560483
    Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
    Type: Grant
    Filed: June 21, 2005
    Date of Patent: July 14, 2009
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
  • Publication number: 20090048337
    Abstract: Fatty acid amide hydrolase inhibitors of the Formula: I.
    Type: Application
    Filed: July 28, 2006
    Publication date: February 19, 2009
    Applicants: The Regents of the University of California, Universita Degli Studi Du Urbino
    Inventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
  • Patent number: 7429658
    Abstract: A method of synthesis of a N-10 protected PBD compound of formula (I): via an intermediate of formula (II) or formula (V):
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: September 30, 2008
    Assignee: Spirogen Limited
    Inventors: Philip Howard, Luke Masterson
  • Patent number: 7414145
    Abstract: A method of an enantioselective nucleophilic addition reaction to carbonyl, which enables an asymmetric synthesis of an optically active ?-hydroxy-?-keto acid ester, an optically active ?-hydroxy-?-amino acid ester, hydroxydiketone compounds, etc. being useful as a raw material or synthesis intermediate for producing a pharmaceutical preparation, an agricultural chemical, a fragrance, a functional polymer or the like. In this method, the nucleophilic addition reaction of enamide compound accompanied by hydroxyl (—OH) formation to carbonyl is carried out in the presence of a chiral catalyst with copper or nickel.
    Type: Grant
    Filed: January 24, 2005
    Date of Patent: August 19, 2008
    Assignee: Japan Science and Technology Agency
    Inventor: Shu Kobayashi
  • Patent number: 7410965
    Abstract: A delayed release pharmaceutical formulation containing 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol or a pharmaceutically acceptable salt thereof in a matrix; said matrix containing from 1 to 80 wt. % of at least one pharmaceutically acceptable, matrix-forming, hydrophilic or hydrophobic polymer and having the following in vitro dissolution rate relative to 100 wt. % of the 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol contained in the formulation: 3-35 wt. % released after 0.5 hour, 5-50 wt. % released after 1 hour, 10-75 wt. % released after 2 hours, 15-82 wt. % released after 3 hours, 30-97 wt. % released after 6 hours, more than 50 wt. % released after 12 hours, more than 70 wt. % released after 18 hours, and more than 80 wt. % released after 24 hours.
    Type: Grant
    Filed: November 29, 2004
    Date of Patent: August 12, 2008
    Assignee: Gruenenthal GmbH
    Inventors: Johannes Bartholomaeus, Iris Ziegler
  • Publication number: 20080161592
    Abstract: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
    Type: Application
    Filed: March 6, 2008
    Publication date: July 3, 2008
    Applicant: CEPTYR, INC.
    Inventors: Mark Arnold Thomas Blaskovich, Ted Baughman, Thomas Little, William Patt, Maher Qabar, Lauri Marie Schultz, Feng Hong, Gangadhar Nagula, Jennifer Lynn Gage, James Jeffrey Howbert
  • Patent number: 7312245
    Abstract: A fungicide can be provided by using, as an active ingredient, a diamine derivative of the following general formula (1): wherein R1 to R7 represent a specific substituent such as an alkyl group with 1 to 6 carbon atoms, and R8 represents an aryl group, which may be substituted or a heteroaryl group, which may be substituted.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: December 25, 2007
    Assignee: Mitsui Chemical, Inc.
    Inventors: Yutaka Chiba, Hidenori Daido, Tomohisa Akase, Hirozumi Matsuno, Junro Kishi
  • Patent number: 7253318
    Abstract: The invention relates to compounds of the formula and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, n, m, and o are as defined in the specification. The compounds are selective monoamine oxidase ? inhibitors and are useful for the treatment and prevention of Alzheimer's disease and senile dementia, as well as other CNS disorders. The invention also relates to processes for preparing such compounds and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: August 7, 2007
    Assignee: Hoffman-La Roche Inc.
    Inventors: Synese Jolidon, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
  • Patent number: 7041863
    Abstract: The present invention is directed to a zeolite Y catalyst having a controlled macropore structure. The present invention is also directed to a zeolite Y catalyst composite and a process for preparing the catalyst composite. The catalyst composite exhibits reduced deactivation rates during the alkylation process, thereby increasing the life of the catalyst. The present invention is also directed to processes for the preparation of carbonated, overbased aromatic sulfonates, which processes comprise alkylation, carbonation of aromatic hydrocarbons with one or more olefins.
    Type: Grant
    Filed: July 20, 2005
    Date of Patent: May 9, 2006
    Assignees: Chevron Oronite Company LLC, Chevron Oronite S.A.
    Inventors: Thomas V. Harris, Curt B. Campbell, Paul J. Marcantonio, Pierre Tequi, Jean-Louis Le Coent
  • Patent number: 7026515
    Abstract: A readily available and inexpensive natural ?-amino acid is converted into a compound represented by formula (1), which is then reacted with an organometallic reagent represented by formula (2) to give an optically active 5-hydroxyoxazolidine represented by formula (3), which is then treated with an acid to provide an optically active aminoketone represented by formula (4). The product is then converted into an optically active aminoalcohol represented by formula (5) or (6) by, for example reduction.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: April 11, 2006
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hidetoshi Tsunoda, Kunio Okumura, Kengo Otsuka
  • Patent number: 6972292
    Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 6, 2005
    Assignee: Novartis AG
    Inventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
  • Patent number: 6852738
    Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: February 8, 2005
    Assignee: Merck & Co., Inc.
    Inventors: A. Brian Jones, John J. Acton, III
  • Publication number: 20040237837
    Abstract: A lightfast additive and an ink composition including the same include a benzophenone moiety for lightfastness and a moiety for wettability and the ability to stabilize a colorant, wherein the two moieties are covalently bonded. The lightfast additive may exhibit effective ultraviolet (UV) light absorption capacity, effective wettability, and an ability to stabilize a colorant. The ink composition utilizing the light fast additive thus has an improved lightfastness and long-term storage stability.
    Type: Application
    Filed: May 24, 2004
    Publication date: December 2, 2004
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Kyung-hoon Lee, Seung-min Ryu, Yeon-kyoung Jung
  • Publication number: 20040237836
    Abstract: A benzophenone compound, and an ink composition that includes the benzophenone compound can absorb UV light, and thus improve lightfastness of images produced with the ink composition containing the compound. Due to the function of the benzophenone compound as a lightfast dispersant, the dispersibility and the lightfastness of an ink composition are improved with the benzophenone compound, without requiring an additional lightfastness enhancer.
    Type: Application
    Filed: May 24, 2004
    Publication date: December 2, 2004
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Kyung-hoon Lee, Seung-min Ryu, Yeon-kyoung Jung
  • Patent number: 6809207
    Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: October 26, 2004
    Assignee: PharmaCore, Inc.
    Inventors: Sekar Alla, Seung-Yong Choi, Dale Dhanoa, Elso DiFranco, Galina Krokhina, Keqiang Li, Balasubramanian Thiagarajan, Wen-Chun Zhang
  • Patent number: 6803378
    Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: October 12, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
  • Patent number: RE39593
    Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.
    Type: Grant
    Filed: June 17, 2003
    Date of Patent: April 24, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
  • Patent number: RE39616
    Abstract: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 25, 2005
    Date of Patent: May 8, 2007
    Assignees: Teva Pharmaceutical Industries, Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation, Ltd.
    Inventors: Michael Chorev, Tamar Goren, Yacov Herzig, Jeffrey Sterling, Marta Weinstock-Rosin, Moussa B. H. Youdim