Benzene Ring In A Substituent Attached To The Ring Nitrogen Of The Five Membered Hetero Ring By Nonionic Bonding Patents (Class 548/578)
  • Patent number: 9023869
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: May 5, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20150031726
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: October 15, 2014
    Publication date: January 29, 2015
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20140303232
    Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Jeremy Lee BARYZA, Rohan Eric John BECKWITH, Keith BOWMAN, Crystal BYERS, Tanzina FAZAL, Gabriel Grant GAMBER, Cameron Chuck-munn LEE, Ritesh Bhanudasji TICHKULE, Chandra VARGEESE, Shuangxi WANG, Laura Ellen West, Thomas ZABAWA, Junping ZHAO
  • Patent number: 8853390
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Publication number: 20140275005
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Application
    Filed: May 5, 2014
    Publication date: September 18, 2014
    Applicant: Sanofi
    Inventor: Zhongli GAO
  • Publication number: 20140275569
    Abstract: The present application provides methods for decarboxylation of amino acids via imine formation with a catalyst under superheated conditions in either a microwave or oil bath.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Richard W. Morrison, Douglas Michael Jackson
  • Patent number: 8809591
    Abstract: The present invention is directed to a process for the manufacture of 2,3,5-trimethyl-hydro-p-benzoquinone comprising the following steps: a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone; b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formal-dehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone; c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone; wherein the organic solvent in all steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, methyl tert.-amyl ether, methoxycyclopentane and any mixtures thereof. Preferably the organic solvent used in all steps a), b) and c) is the same.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: August 19, 2014
    Assignee: DSM IP Assets B.V.
    Inventors: Werner Bonrath, Thomas Netscher, Jan Schütz, Bettina Wüstenberg
  • Patent number: 8735385
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • Publication number: 20140046054
    Abstract: The invention relates to a process for preparing amines (A) by alcohol amination of alcohols (Al) by means of an aminating agent (Am) with elimination of water, wherein the alcohol amination is carried out in the presence of a complex catalyst comprising iridium and an amino acid.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 13, 2014
    Applicant: BASF SE
    Inventors: Alexander WETZEL, Michael Limbach, Marion Brinks, Mathias Schelwies
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Patent number: 8642780
    Abstract: The present invention relates to N-carbomethoxy-N-methoxy-(2-chloromethyl)-aniline compounds of the formula I, wherein: n is 0, 1, 2 or 3, each R1 is independently selected from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy. The invention also relates to processes and intermediates for preparing such compounds of formula I. The invention furthermore relates to processes for preparing 2-(pyrazol-3?-yloxymethylene)-anilides in which compounds of formula I are applied as precursors.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: February 4, 2014
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Bernd Mueller
  • Publication number: 20130245018
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).
    Type: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Applicant: PIMCO 2664 LIMITED
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Publication number: 20130211080
    Abstract: The present invention is directed to a process for the manufacture of 2,3,5-trimethyl-hydro-p-benzoquinone comprising the following steps: a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone; b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formal-dehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone; c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone; wherein the organic solvent in all steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, tert.-amyl ether, methoxycyclopentane and any mixtures thereof. Preferably the organic solvent used in all steps a), b) and c) is the same.
    Type: Application
    Filed: August 25, 2011
    Publication date: August 15, 2013
    Applicant: DSM IP ASSETS B.V.
    Inventors: Werner Bonrath, Thomas Netscher, Jan Schütz, Bettina Wüstenberg
  • Publication number: 20130184238
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Patent number: 8476336
    Abstract: The invention relates to an ophthalmologic composition including a dye of the general formula I in which R1=substituted or unsubstituted hydrocarbon radical, R2=substituted or unsubstituted hydrocarbon radical with at least one polymerizable double bond, R3?H or substituted or unsubstituted hydrocarbon radical, R4?H, electron-withdrawing substituent or substituted or unsubstituted hydrocarbon radical and X?O, S, NH or NR5, wherein R5 is a substituted and/or unsubstituted hydrocarbon radical. Moreover, the invention relates to another ophthalmologic composition and an ophthalmologic lens.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 2, 2013
    Assignee: Acri.Tec GmbH
    Inventor: Juergen Nachbaur
  • Publication number: 20130131034
    Abstract: The instant invention relates to derivatives of formula (I) and their application in therapeutics.
    Type: Application
    Filed: March 1, 2011
    Publication date: May 23, 2013
    Applicant: SANOFI
    Inventors: Markus Follmann, Pascale Goberville, Stéphanie Hachtel, Gerhard Hessler, Heinz-Werner Kleemann, Thomas Maier, Gary MC Cort, Carsten Struebing, Bérangère Thiers, Li-Hsing Wang
  • Publication number: 20130117941
    Abstract: The present invention relates to the use of a composition comprising specific a-amino-ketones, H2O2, a H2O2 precursor or a peracid and optionally an activator as a bleaching mixture for textile materials or dishes either manually or in an automatic washing machine or dish washer. Further aspects of the invention are the composition comprising specific a-aminoketones and H2O2, a H2O2 precursor or a peracid and a process for bleaching of stains or of soiling on textile materials or dishes in the context of a washing process either manually or in an automatic washing machine or dish washer. Also aspects of the invention are detergent formulations comprising such a composition and novel compounds.
    Type: Application
    Filed: June 21, 2011
    Publication date: May 16, 2013
    Applicant: BASF SE
    Inventors: Markus Frey, Hauke Rohwer, Frédérique Wendeborn, Menno Hazenkamp
  • Publication number: 20130079372
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: November 26, 2012
    Publication date: March 28, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20130065877
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Application
    Filed: November 6, 2012
    Publication date: March 14, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Patent number: 8389743
    Abstract: This invention is directed to a compound of formula I, wherein R1, R2, R4, R5, R6, R7, R8 and n are as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a process of preparation of a compound of formula I, a method of treatment of a disorder or condition such as depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as descri
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: March 5, 2013
    Assignee: Pfizer Inc.
    Inventors: Travis T. Wager, Ramalakshmi Yegna Chandrasekaran, Todd William Butler
  • Patent number: 8389559
    Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 5, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Jianguo Ma
  • Publication number: 20130005986
    Abstract: The present invention relates to N-carbomethoxy-N-methoxy-(2-chloromethyl)-aniline compounds of the formula I, wherein: n is 0, 1, 2 or 3, each R1 is independently selected from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy. The invention also relates to processes and intermediates for preparing such compounds of formula I. The invention furthermore relates to processes for preparing 2-(pyrazol-3?-yloxymethylene)-anilides in which compounds of formula I are applied as precursors.
    Type: Application
    Filed: March 17, 2011
    Publication date: January 3, 2013
    Applicant: BASF SE
    Inventors: Maximilian Dochnahl, Bernd Mueller
  • Patent number: 8343963
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: January 1, 2013
    Assignee: 4SC AG
    Inventor: Stefano Pegoraro
  • Publication number: 20120220568
    Abstract: This invention is directed to a compound of formula I, wherein R1, R2, R4, R5, R6, R7, R8 and n are as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a process of preparation of a compound of formula I, a method of treatment of a disorder or condition such as depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as descri
    Type: Application
    Filed: March 9, 2012
    Publication date: August 30, 2012
    Inventors: Travis T. Wager, Ramalakshmi Y. Chandrasekaran, Todd William Butler
  • Publication number: 20120149693
    Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.
    Type: Application
    Filed: May 5, 2010
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: Raymond G. Booth
  • Patent number: 8193228
    Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: June 5, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Michael M. C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
  • Publication number: 20120129906
    Abstract: The present invention relates to novel diphenylethyne derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 24, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Michael E. Garst, Wha Bin Im
  • Publication number: 20120129860
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 27, 2012
    Publication date: May 24, 2012
    Applicant: Acucela, Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Anna Gall, Mark W. Orme, Jennifer Gage, Thomas L. Little, JR., Qin Jiang, Lana Michele Rossiter, Kevin F. McGee, JR., Ryo Kubota
  • Patent number: 8183275
    Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: May 22, 2012
    Assignees: Merck Sharp & Dohme Corp., Albany Molecular Research, Inc.
    Inventors: Peter H. Dobbelaar, Christopher L. Franklin, Allan Goodman, Cheng Guo, Peter R. Guzzo, Mark Hadden, Shuwen He, Alan J. Henderson, Tianying Jian, Linus S. Lin, Jian Liu, Ravi P. Nargund, Megan Ruenz, Bruce J. Sargent, Iyassu K. Sebhat, Larry Yet
  • Patent number: 8178574
    Abstract: The present invention is directed to the tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide Formula (I): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: May 15, 2012
    Assignee: Pfizer Inc.
    Inventors: Travis T. Wager, Todd W. Butler
  • Publication number: 20120071651
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 22, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Publication number: 20120022039
    Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.
    Type: Application
    Filed: February 12, 2010
    Publication date: January 26, 2012
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • 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
  • Publication number: 20120010403
    Abstract: A production method of a compound containing a primary, secondary, or tertiary aminomethyl aromatic ring of the present invention includes: using a fluoroboron compound or a dimer thereof, or solvates thereof, which are represented by a formula (I): Ra(Rb)N—CH2—BF3M??(I) as an aminomethylating agent for an aromatic ring; and reacting the aminomethylating agent with an aromatic ring-containing compound, which can react with the aminomethylating agent, under the presence of a metal catalyst such as a palladium compound so as to perform the direct aminomethylation of the aromatic ring.
    Type: Application
    Filed: September 21, 2011
    Publication date: January 12, 2012
    Inventor: Keigo TANAKA
  • Patent number: 8080541
    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: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20110243865
    Abstract: Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole), and/or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: December 22, 2009
    Publication date: October 6, 2011
    Applicant: POLA CHEMICAL INDUSTRIES INC.
    Inventors: Kouji Yokoyama, Makoto Kimura, Masashi Tamai, Yuko Saitoh, Tomomi Kato, Yu Ikeda
  • Publication number: 20110245244
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.
    Type: Application
    Filed: April 4, 2011
    Publication date: October 6, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
  • Patent number: 7915427
    Abstract: Novel intermediates for the production of aminoacetyl pyrrolidine carbonitrile derivatives ensure the safe and efficient production of the compounds. Specifically, the present invention provides a sulfonyloxyacetyl pyrrolidine derivative, represented by the following formula: (Chemical Formula 1) (wherein R1 is a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted arylmethyl group, a substituted or unsubstituted aromatic hydrocarbon, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted aliphatic heterocyclic ring; R2 is CONH2 or CN; and X is CH2, CHF or CF2.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: March 29, 2011
    Assignee: Kyorin Pharmaceuticals Co., Ltd.
    Inventors: Yoshikazu Asahina, Yasumichi Fukuda, Futoshi Shiga
  • Patent number: 7906501
    Abstract: Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
    Type: Grant
    Filed: April 27, 2005
    Date of Patent: March 15, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Roberto Artusi, Antonio Giordani, Simona Zanzola, Lucio Claudio Rovati
  • Publication number: 20110053904
    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: August 19, 2010
    Publication date: March 3, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20100292288
    Abstract: The present invention is directed to novel salts of (R)-1-{2-[4?-(3-methoxy-propane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine, and crystalline forms, and compositions thereof that modulate the activity of the histamine H3-receptor and are useful in the treatment of histamine H3-receptor associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, pain, dementia, Alzheimer's disease and the like.
    Type: Application
    Filed: June 6, 2008
    Publication date: November 18, 2010
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Anthony C. Blackburn, John A. DeMattei, Ryan M. Hart, Young Mi Khulman, Michael Mesleh, Jeffrey Smith
  • Publication number: 20100292279
    Abstract: The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
    Type: Application
    Filed: May 12, 2010
    Publication date: November 18, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Johan Bylund, Maria E. Ek, Jörg Holenz, Annika Kers, Liselotte Öhberg
  • Publication number: 20100291299
    Abstract: Cyclopentadienyl and Indenyl barium/strontium metal precursors and Lewis base adducts thereof are described. Such precursors have utility for forming Ba- and/or Sr-containing films on substrates, in the manufacture of microelectronic devices or structures.
    Type: Application
    Filed: August 3, 2008
    Publication date: November 18, 2010
    Applicant: ADVANCED TECHNOLOGY MATERIALS, INC.
    Inventors: Thomas M. Cameron, Chongying Xu
  • Patent number: 7812040
    Abstract: This invention is directed to a compound of the formula Ia or Ib, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-i
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: October 12, 2010
    Assignee: Pfizer Inc.
    Inventor: Travis T Wager
  • Publication number: 20100256213
    Abstract: The present invention is directed to the tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide Formula (I): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.
    Type: Application
    Filed: December 4, 2008
    Publication date: October 7, 2010
    Inventors: Travis T. Wager, Todd W. Butler
  • Publication number: 20100249075
    Abstract: The present invention relates to novel tetralin ER-? agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-? mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis.
    Type: Application
    Filed: February 10, 2006
    Publication date: September 30, 2010
    Applicant: ELI LILLY AND COMPANY
    Inventors: Venkatesh Krishnan, Julian Stanley Kroin, Bryan Hurst Norman, Elizabeth Marie Thomas
  • Publication number: 20100240653
    Abstract: The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.
    Type: Application
    Filed: October 16, 2007
    Publication date: September 23, 2010
    Inventors: Vincent J. Santora, Ryan M. Hart, Jason B. Ibarra, Douglas M. Park, Albert S. Ren, Graeme Semple, Jeffrey A. Schultz, Brian M. Smith, Jeffrey Smith
  • Publication number: 20100125076
    Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.
    Type: Application
    Filed: April 20, 2008
    Publication date: May 20, 2010
    Applicant: Unimed Pharma, Spol. S R.O.
    Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
  • Patent number: 7700585
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: April 20, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
  • Patent number: 7687536
    Abstract: Aminocycloalkyl cinnamide compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of local analgesia and anesthesia.
    Type: Grant
    Filed: April 11, 2006
    Date of Patent: March 30, 2010
    Assignee: Cardiome Pharma Corp.
    Inventors: Gregory N. Beatch, Cindy J. Longley, Michael J. A. Walker, Richard A. Wall