Morpholine Ring Bonded Directly To The Carbocyclic Ring Patents (Class 544/166)
  • Publication number: 20150141416
    Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 21, 2015
    Inventors: Frank Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20150099714
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Publication number: 20150031663
    Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.
    Type: Application
    Filed: October 13, 2014
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
  • Publication number: 20140378682
    Abstract: The invention discloses processes for the preparation of rivaroxaban and its pharmaceutically acceptable salts, solvates, and hydrates thereof. The invention also relates to novel intermediates for the preparation of rivaroxaban.
    Type: Application
    Filed: September 10, 2012
    Publication date: December 25, 2014
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Daya Ram Pal, Mukul Hari Prasad Sharma, Kuldeep Natwarlal Jain, Naitik Bharatbhai Patel
  • Patent number: 8901295
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: December 2, 2014
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Montpellier 1, Universite Paris-EST Creteil val de Marne, Assistance Publique-Hopitaux de Paris, Centre National de la Recherche Scientifique
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20140213784
    Abstract: The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as well as intermediates are additionally claimed.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 31, 2014
    Applicant: SANDOZ AG
    Inventors: Hubert Sturm, Kerstin Knepper
  • Publication number: 20140179687
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 26, 2014
    Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
  • Publication number: 20140100224
    Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
    Type: Application
    Filed: June 26, 2013
    Publication date: April 10, 2014
    Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of California
    Inventors: Frank M. Longo, Stephen M. Massa
  • Publication number: 20140094445
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. 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: August 15, 2012
    Publication date: April 3, 2014
    Applicant: University of Utah Research Foundation
    Inventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Patent number: 8653304
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20130345213
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: LUPIN LIMITED
    Inventors: Manojkumar Ramprasad Shukla, Vinod Dinkar Chaudhari, Majid Bashir Sayyed, Ramesh Dattatraya Phadtare, Navnath Bajirao Walke, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130203745
    Abstract: The present invention relates to bisaryl(thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl and —NH—CO-(1-4C)alkyl, or substituted with phenoxy, benzyl, benzyloxy, phenylethyl or morpholinyl, each optionally substituted with (1-4C)alkyl, and (8-10C)bicyclic group, bicyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms or oxo; A is selected from —CO—, —NH—, —O—, —S—, —SO— or —SO2—; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substit
    Type: Application
    Filed: July 8, 2011
    Publication date: August 8, 2013
    Applicant: AbbVie B.V.
    Inventors: Wouter I. Iwema Bakker, Raymond Bronger
  • Publication number: 20130190296
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: November 20, 2012
    Publication date: July 25, 2013
    Applicant: Dendreon Corporation
    Inventor: Dendreon Corporation
  • Publication number: 20130172554
    Abstract: The present invention provides processes for the preparation of 4-{4-[5(S)-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one which are simple, eco-friendly, cost-effective, reproducible, robust and are well amenable on industrial scale.
    Type: Application
    Filed: August 1, 2011
    Publication date: July 4, 2013
    Applicant: SYMED LABS LIMITED
    Inventors: Dodda Mohan Rao, Pingili Krishna Reddy, Ambati Anna Reddy, Buthukuri Venkat Reddy
  • Patent number: 8338413
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: December 25, 2012
    Assignee: Novartis AG
    Inventor: Heinrich Rueeger
  • Publication number: 20120322799
    Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.
    Type: Application
    Filed: November 30, 2010
    Publication date: December 20, 2012
    Applicant: PHARMATROPHIX, INC.
    Inventor: Gopal Damodara
  • Publication number: 20120214808
    Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: Prosidion Limited
    Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
  • Publication number: 20120196849
    Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.
    Type: Application
    Filed: April 10, 2012
    Publication date: August 2, 2012
    Applicant: IRM LLC
    Inventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
  • Publication number: 20120184735
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Application
    Filed: September 30, 2010
    Publication date: July 19, 2012
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20120165325
    Abstract: Polymorphic forms of N-(2,6-dimethyl-4-morpholin-4-yl-phenyl)-3,3-dimethyl-butyramide are provided together with a process for the manufacture of said compound.
    Type: Application
    Filed: March 2, 2012
    Publication date: June 28, 2012
    Applicant: H. Lundbeck A/S
    Inventors: Svend Treppendahl, Karin Liltorp, Heidi Lopez de Diego
  • Patent number: 8207164
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: June 26, 2012
    Assignee: Novartis AG
    Inventors: Philipp Holzer, Rainer Machauer, Marina Tintelnot-Blomley
  • Publication number: 20120149687
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: October 31, 2011
    Publication date: June 14, 2012
    Applicant: AVILA THERAPEUTICS, INC.
    Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
  • Patent number: 8158825
    Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of 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: June 21, 2006
    Date of Patent: April 17, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
  • Publication number: 20120022042
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Application
    Filed: September 30, 2011
    Publication date: January 26, 2012
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 8101609
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: January 24, 2012
    Assignee: Apotex Pharmachem Inc.
    Inventors: Prabhudas Bodhuri, Gamini Weeratunga
  • Publication number: 20110230479
    Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
    Type: Application
    Filed: October 22, 2010
    Publication date: September 22, 2011
    Inventors: Frank M. Longo, Stephen M. Massa
  • Publication number: 20110135650
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: June 1, 2010
    Publication date: June 9, 2011
    Inventors: Samuel CHACKALAMANNIL, Tin-Yau CHAN, Mariappan V. CHELLIAH, Martin C. CLASBY, Michael DWYER, William J. GREENLEE, Tomokazu HIRABAYASHI, Santhosh NEELAMKAVIL, Hidemitsu NISHIDA, Fumihiko SAITOH, Unmesh SHAH, Yan XIA
  • Publication number: 20110021520
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: July 23, 2010
    Publication date: January 27, 2011
    Inventors: Sangamesh BADIGER, Murali CHEBROLU, Mathias FREDERIKSEN, Philipp HOLZER, Konstanze HURTH, Rainer Martin LUEOEND, Rainer MACHAUER, Henrik MOEBITZ, Ulf NEUMANN, Rita RAMOS, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
  • Publication number: 20110009626
    Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (VI?), (VII?) and (VIII?) and their preparation.
    Type: Application
    Filed: August 11, 2010
    Publication date: January 13, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
  • Patent number: 7868004
    Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: January 11, 2011
    Assignee: Givaudan S.A.
    Inventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Adam Mazur, Jay Patrick Slack
  • Publication number: 20100331329
    Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.
    Type: Application
    Filed: September 10, 2010
    Publication date: December 30, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
  • Publication number: 20100298328
    Abstract: 1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.
    Type: Application
    Filed: March 30, 2007
    Publication date: November 25, 2010
    Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
  • Publication number: 20100286138
    Abstract: Polymorphic forms of N-(2,6-dimethyl-4-morpholin-4-yl-phenyl)-3,3-dimethyl-butyramide are provided together with a process for the manufacture of said compound.
    Type: Application
    Filed: May 11, 2010
    Publication date: November 11, 2010
    Applicant: H. LUNDBECK A/S
    Inventors: Svend Treppendahl, Karin Liltorp, Heidi Lopez de Diego
  • Publication number: 20100273798
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
    Type: Application
    Filed: April 28, 2009
    Publication date: October 28, 2010
    Applicant: APOTEX PHARMACHEM INC.
    Inventors: Prabhudas BODHURI, Gamini Weeratunga
  • Publication number: 20100273790
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8: .
    Type: Application
    Filed: April 26, 2010
    Publication date: October 28, 2010
    Applicant: Apotex Pharmachem Inc.
    Inventors: Prabhudas BODHURI, Gamini Weeratunga
  • Patent number: 7816355
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: October 19, 2010
    Assignee: Apotex Pharmachem Inc
    Inventors: Prabhudas Bodhuri, Gamini Weeratunga
  • Publication number: 20100158996
    Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.
    Type: Application
    Filed: February 12, 2010
    Publication date: June 24, 2010
    Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
  • Publication number: 20100160327
    Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of 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: Application
    Filed: June 21, 2006
    Publication date: June 24, 2010
    Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
  • Publication number: 20100160247
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: June 17, 2009
    Publication date: June 24, 2010
    Applicant: CoNCERT Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Publication number: 20100152098
    Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
    Type: Application
    Filed: November 5, 2009
    Publication date: June 17, 2010
    Applicant: Mpex Pharmaceuticals, Inc.
    Inventors: Tomasz Glinka, Olga Rodny, Keith A. Bostian, David M. Wallace, Robert I. Higuchi, Chun Chow, Chi Ching Mak, Gavin Hirst, Brian Eastman
  • Patent number: 7687624
    Abstract: The invention relates to a method for production of compounds of formula (I), where X has the meaning given in claim 1 and precursors for the same.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: March 30, 2010
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Hanns Wurziger
  • Patent number: 7598378
    Abstract: The present invention relates to a process for preparing 4-(4-aminophenyl)-3-morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with hydrogen in the presence of a hydrogenation catalyst, characterized in that the reaction is effected in an aliphatic alcohol.
    Type: Grant
    Filed: September 9, 2004
    Date of Patent: October 6, 2009
    Assignee: Bayer Schering Pharma AG
    Inventors: Christian Thomas, Mathias Berwe, Alexander Straub
  • Publication number: 20090239841
    Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
    Type: Application
    Filed: October 24, 2005
    Publication date: September 24, 2009
    Inventors: Alan J. Hutchison, Jun Yuan
  • Patent number: 7544716
    Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.
    Type: Grant
    Filed: November 28, 2003
    Date of Patent: June 9, 2009
    Assignee: Xention Limited
    Inventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
  • Publication number: 20090137571
    Abstract: The present invention relates to morpholine and thiomorpholine derivatives or the general formula I or pharmaceutically acceptable salts thereof and their use.
    Type: Application
    Filed: January 28, 2009
    Publication date: May 28, 2009
    Applicant: H. LUNDBECK A/S
    Inventors: Christian Wenzel Tornoe, Mario Rottlander, Nikolay Khanzhin, Andreas Ritzen, William Patrick Watson
  • Publication number: 20090105237
    Abstract: A method of conferring a cooling effect on the skin or mucous membranes by applying thereto at least one compound of the Formula I: (a) wherein B is selected from H, CH3, C2H5, OCH3, OC2H5; and OH; and (b) wherein A is a moiety of the formula —CO-D, wherein D is selected from the following moieties: (i) —NR1R2, wherein R1 and R2 are independently selected from H and C1-C8 straight or branched-chain aliphatic, alkoxyalkyl, hydroxyalkyl, araliphatic and cycloalkyl groups, or R1 and R2 together with the nitrogen atom to which they are attached form part of an optionally-substituted, five- or six-membered heterocyclic ring; (ii) —NHCH2COOCH2CH3, —NHCH2CONH2, —NHCH2CH2OCH3, —NHCH2CH2OH, —NHCH2CH(OH)CH2OH and (iii) a moiety selected from the group consisting of: The compounds are useful for providing cooling effects in a variety of products, such as foodstuffs, confectionery, tobacco products, beverages, cosmetics, dentifrices, medicinal preparations, mouthwashes and toiletries.
    Type: Application
    Filed: May 24, 2006
    Publication date: April 23, 2009
    Inventors: Karen Ann Bell, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
  • Publication number: 20090105474
    Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.
    Type: Application
    Filed: March 14, 2006
    Publication date: April 23, 2009
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
  • Patent number: 7514431
    Abstract: The present invention is directed to compounds of the formula I: I (wherein R1, R2, R3, R4, R5, R6, X, Z and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: April 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Changyou Zhou, Alexander Pasternak, Lihu Yang