The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/237)
  • Patent number: 9334223
    Abstract: Process for the preparation of 2-phenyl-2-methyl propanoic acid derivatives, useful as intermediates in the preparation of fexofenadine hydrochloride.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: May 10, 2016
    Assignee: Dipharma Francis S.r.l.
    Inventors: Pietro Allegrini, Vittorio Lucchini, Davide Rossi, Mauro Mittino, Gabriele Razzetti
  • Publication number: 20150105552
    Abstract: This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
  • Publication number: 20150057443
    Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
    Type: Application
    Filed: August 21, 2014
    Publication date: February 26, 2015
    Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
  • Patent number: 8916587
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: December 23, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Patent number: 8772291
    Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
  • Patent number: 8653106
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Patent number: 8481527
    Abstract: The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Grant
    Filed: October 27, 2007
    Date of Patent: July 9, 2013
    Assignee: Richter Gedeon Nyrt.
    Inventors: Istvan Vago, Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Monika Vastag
  • 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: 20130096151
    Abstract: The present invention relates to the use of an anesthetic agent for killing clinically latent microorganisms associated with microbial infections and to novel combinations comprising an anesthetic agent and an antimicrobial agent for the treatment of microbial infections.
    Type: Application
    Filed: March 29, 2011
    Publication date: April 18, 2013
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Yanmin Hu, Anthony M.R. Coates
  • Patent number: 8420622
    Abstract: Compounds of formula I: I wherein at least one of R4 and R5 comprises Si(R6)3 as a substituent selectively attenuate production of A?(1-42) and hence find use in treatment of Alzheimer's disease and related conditions.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: April 16, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Benito Munoz, Jed Hubbs, Christopher L. Hamblett, Hua Zhou, Michelle Martinez
  • Patent number: 8389547
    Abstract: Compounds of formula (I) are modulators of gamma-secretase, and hence are useful in treatment of Alzheimer's disease.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: March 5, 2013
    Inventors: Yudith Garcia, Joanne Clare Hannam, Timothy Harrison, Christopher L. Hamblett, Jed L. Hubbs, Janusz Josef Kulagowski, Andrew Madin, Mark Peter Ridgill, Eileen Seward
  • Patent number: 8372979
    Abstract: The invention relates to a method for producing highly pure 2,4?-dimethyl-3-piperidino-propiophenone (tolperisone) (formula I) and the pharmaceutically acceptable salts, hydrochlorides, and hydrates thereof. The method allows the content of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) to be kept significantly lower than in previously known methods. The invention further relates to active substance formulations which contain tolperisone and are suitable, among other things, for producing combination preparations used for treating patients suffering from Alzheimer's disease. The invention also relates to topical formulations, controlled release (CR) formulations, and transdermal therapeutic systems, such as active substance patches, which contain less than 50 ppm, preferably less than 10 ppm, more preferably less than 7 ppm, and most preferably less than 3 ppm or 0 ppm (i.e.
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: February 12, 2013
    Assignee: SANOCHEMIA Pharmazeutika AG
    Inventors: Stefan Welzig, Jan Rothenburger, Beate Kälz, József Gungl, Klaus Gerdes, Federico Gaeta
  • Publication number: 20120196895
    Abstract: The invention relates to novel crystalline forms of (2RS)-1-(4-ethylphenyl)-2-methyl-3-piperidin-1-yl-propan-1-one. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotonic conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.
    Type: Application
    Filed: January 11, 2010
    Publication date: August 2, 2012
    Applicant: Bionevia Pharmaceuticals, Inc.
    Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Jason A. Hanko
  • Publication number: 20120183498
    Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 19, 2012
    Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
  • Publication number: 20120149900
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: June 14, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • Patent number: 8153657
    Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: April 10, 2012
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Jia Zhou
  • Publication number: 20120046247
    Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 23, 2012
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Publication number: 20120022086
    Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 26, 2012
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Patent number: 8067605
    Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: November 29, 2011
    Assignee: Albany Molecular Research, Inc.
    Inventors: Harold Meckler, Benjamin J. Littler, Prasad Raje, Michael Van Brundt, Paul Vogt
  • Publication number: 20110281911
    Abstract: The invention relates to substantially enantiopure crystalline salt forms of (2RS)-I-(4-Ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one. The preparation and characterization of the substantially enantiopure crystalline salt forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the substantially enantiopure crystalline salt forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotome conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.
    Type: Application
    Filed: August 3, 2009
    Publication date: November 17, 2011
    Applicant: Bionevia Pharmaceuticals, Inc.
    Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Jason A. Hanko, Jeffrey P. Kiplinger
  • Publication number: 20110263428
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: July 1, 2009
    Publication date: October 27, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Stephane Andre Marie Jeanmart, Russell Colin Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Mangala Govenkar, Matthew Robert Cordingley, Claire Janet Russell, Melloney Tyte
  • Publication number: 20110118312
    Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.
    Type: Application
    Filed: January 20, 2011
    Publication date: May 19, 2011
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
  • Publication number: 20110082295
    Abstract: To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH?CH.
    Type: Application
    Filed: May 27, 2009
    Publication date: April 7, 2011
    Applicants: Tokyo Institute of Technology, Kyoto University
    Inventors: Hachiro Sugimoto, Takashi Takahashi, Ichiro Hijikuro, Michiaki Okuda
  • Publication number: 20110071295
    Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.
    Type: Application
    Filed: November 30, 2010
    Publication date: March 24, 2011
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Harold MECKLER, Ben Littler, Prasad Raje, Michael Van Brunt, Paul F. Vogt
  • Publication number: 20100324090
    Abstract: The present disclosure is directed to methods for providing tolperisone having extremely low levels of 4-MMPPO (2-methyl-1-(4-methylphenyl)-propenone), as well as related compositions. The invention further relates to methods of treating a subject with tolperisone under conditions that limit exposure of the subject to tolerable levels of 4-MMPPO, among other features.
    Type: Application
    Filed: April 24, 2008
    Publication date: December 23, 2010
    Inventors: Federico Gaeta, Klaus Gerdes, Stefan Welzig, Beate Kätz, Jan Rothenburger, József Gungl
  • Publication number: 20100298329
    Abstract: The invention provides compositions and methods for treating cancer. Aspects of the invention relate to therapeutic compositions comprising tolperisone and related compounds. Aspects of the invention relate to methods and compositions for treating Ras-associated cancers.
    Type: Application
    Filed: September 19, 2008
    Publication date: November 25, 2010
    Applicant: Massachusette Institute of Technology
    Inventors: Alice T. Shaw, Tyler E. Jacks, Nicola Tolliday
  • Patent number: 7812035
    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: October 12, 2010
    Assignee: Sepracor Inc.
    Inventors: Heike Radeke, Liming Shao
  • Patent number: 7781459
    Abstract: The invention relates to acyl-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and the physiological tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example for the treatment of type II diabetes.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: August 24, 2010
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Elisabeth DeFossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger, Alfons Enhsen
  • Patent number: 7763639
    Abstract: The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho, meta-disubstituted phenyl)-1-alkypiperidines and piperazines. wherein R1, R2, R3 and X are as defined.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: July 27, 2010
    Assignee: NSAB, Filial AF Neurosearch Sweden AB, Sverige
    Inventors: Clas Sonesson, Lars Swanson, Nicholas Ross Waters
  • Publication number: 20100160376
    Abstract: A method for producing a consumable nicotine-alternative composition includes measuring a quantity of a cigarette nicotine-alternative alkaloid and/or a larger quantity of lobeline. The quantities of cigarette nicotine-alternative alkaloid and/or lobeline are diluted into one or more successive intermediate solutions, a last of which constitutes a final solution. The final solution is apportioned so that each portion contains a precise quantity of cigarette nicotine-alternative alkaloid and/or lobeline appropriate for consumption in a single use by a single person. Each portion is introduced into a separate single-serving dispenser.
    Type: Application
    Filed: May 24, 2007
    Publication date: June 24, 2010
    Inventor: Marshall Anlauf Thompson
  • Publication number: 20100150995
    Abstract: The invention relates to a method for producing highly pure 2,4?-dimethyl-3-piperidino-propiophenone (tolperisone) (formula I) and the pharmaceutically acceptable salts, hydrochlorides, and hydrates thereof. The method allows the content of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) to be kept significantly lower than in previously known methods. The invention further relates to active substance formulations which contain tolperisone and are suitable, among other things, for producing combination preparations used for treating patients suffering from Alzheimer's disease. The invention also relates to topical formulations, controlled release (CR) formulations, and transdermal therapeutic systems, such as active substance patches, which contain less than 50 ppm, preferably less than 10 ppm, more preferably less than 7 ppm, and most preferably less than 3 ppm or 0 ppm (i.e.
    Type: Application
    Filed: April 24, 2008
    Publication date: June 17, 2010
    Applicant: SANOCHEMIA PHARMAZEUTIKA AG
    Inventors: Stefan Welzig, Jan Rothenburger, Beate Kalz, Jozsef Gungl, Klaus Gerdes, Federico Gaeta
  • Publication number: 20100152238
    Abstract: Novel cannabinoid-derived quinone derivatives (quinonoid derivatives) having a substituted hydroxyl group, pharmaceutical compositions comprising same and uses thereof as anti-proliferative agents, are provided.
    Type: Application
    Filed: March 5, 2008
    Publication date: June 17, 2010
    Applicant: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventors: Raphael Mechoulam, Natalya Kogan
  • Publication number: 20100113496
    Abstract: The present invention relates to new piperidine modulators of VMAT2, nicotinic acetylcholine receptors, and/or ?-opioid receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: September 22, 2009
    Publication date: May 6, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventor: Thomas G. Gant
  • Patent number: 7700587
    Abstract: Haloperidol analogs that conforms to the structural formulae: wherein: R is H, or —(CH2)n—OH, n is an integer from 0 to 2, and A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP+ like species, (2) has an affinity for the D2 receptor subtype of 15<D2<250 and (3) functions as a dopamine receptor antagonist, or the structural formulae: wherein: R1 is H, or —(CH2)n—OH, n is an integer from 0 to 2, B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP+ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: April 20, 2010
    Assignee: Florida A&M University
    Inventors: Seth Y. Ablordeppey, Donald M. N. Sikazwe
  • Patent number: 7649095
    Abstract: Piperidine derivatives represented by formula (I) or nontoxic salts thereof (wherein symbols are defined in the description): Since the compound represented by formula (I) has a PDE4 inhibitory activity, it is useful for preventing and/or treating inflammatory diseases, diabetic diseases, allergic diseases, autoimmune diseases, osteoporosis, bone fracture, obesity, depression, Parkinson's disease, dementia, ischemia-reperfusion injury, leukemia and the like.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: January 19, 2010
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Nakai, Katsuya Kishikawa
  • Publication number: 20090253743
    Abstract: The present disclosure is directed to methods for providing tolperisone having extremely low levels of 4-MMPPO (2-methyl-1-(4-methylphenyl)-propenone), as well as related compositions. The invention further relates to methods of treating a subject with tolperisone under conditions that limit exposure of the subject to tolerable levels of 4-MMPPO, among other features.
    Type: Application
    Filed: November 26, 2008
    Publication date: October 8, 2009
    Applicants: Avigen, Inc., Sanochemia Pharmazeutika, AG
    Inventors: Federico Gaeta, Stefan Welzig, Jan Rothenburger, Beate Kalz, Jozsef Gungl, Klaus Gerdes
  • Patent number: 7517892
    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: April 14, 2009
    Assignee: Sepracor Inc.
    Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
  • Patent number: 7511147
    Abstract: The present invention relates to a shortened process for preparing L-lobeline by rhodium-catalysed asymmetric hydrogenation on an industrial scale.
    Type: Grant
    Filed: July 8, 2005
    Date of Patent: March 31, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Franz-Dietrich Klingler, Rainer Sobotta
  • Publication number: 20090076081
    Abstract: The invention relates to a compound of formula wherein Ar1, Ar2, R1, R2, R3, R4, R5, and R5? or to a pharmaceutically active salt thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: September 10, 2008
    Publication date: March 19, 2009
    Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian, Xihan Wu
  • Publication number: 20090069378
    Abstract: The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 12, 2009
    Applicant: Protia, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20080293948
    Abstract: A process for the preparation of 4-[1-oxo-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-?,?-dimethylbenzeneacetic acid, useful as an intermediate for the preparation of fexofenadine, is provided.
    Type: Application
    Filed: May 15, 2008
    Publication date: November 27, 2008
    Applicant: DIPHARMA FRANCIS s.r.l.
    Inventors: Tiziano Scubla, Pietro Allegrini, Eliana Rocchini, Caterina Napoletano
  • Publication number: 20080227814
    Abstract: The present invention relates to a selective estrogen receptor modulator selected from the group consisting of: (I) or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.
    Type: Application
    Filed: January 18, 2005
    Publication date: September 18, 2008
    Inventors: Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Owen Brendan Wallace
  • Publication number: 20080227983
    Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings, each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.
    Type: Application
    Filed: May 29, 2008
    Publication date: September 18, 2008
    Applicant: AMR TECHNOLOGY, INC.
    Inventor: Thomas E. D'Ambra
  • Publication number: 20080221106
    Abstract: Disclosed Arylamine ketones of formula (I), their preparation methods, the pharmaceutical compositions containing them and their use in preventing and/or treating the diseases related to the plaque-activating factors, especially in anti-inflammation and immunization, more especially in the treatment of the acute or chronic inflammation, such as, osteoarthritis, oarthritis deformans, etc.
    Type: Application
    Filed: August 5, 2005
    Publication date: September 11, 2008
    Inventors: Liya Zhu, Wenjie Wang, Halhong Huang, Ziyun Lin, Liyuan Mou, Zhengui Nie, Yu He, Xueyu Ouyang, Shanying Peng, Dongfong Zhang, Jun Wei
  • Patent number: 7385060
    Abstract: The invention relates to a method for producing an addition salt of 2,4?-dimethyl-3-piperidino-propiophenone (tolperisone) with a pharmaceutically acceptable acid, of formula (I).
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: June 10, 2008
    Assignee: Sanochemia Pharmazeutika AG
    Inventors: Laszlo Czollner, Beate Kälz, Jan Rothenburger, Stefan Welzig
  • Publication number: 20080132751
    Abstract: The present invention provides compositions and methods for treating pain by the administration of analgesics. The analgesics are encapsulated in diacylglycerol-polyethyleneglycol (DAG-PEG) liposomes and delivered sublingually as aerosols.
    Type: Application
    Filed: November 30, 2006
    Publication date: June 5, 2008
    Inventors: Brian C. Keller, Camilo Rey, Jorge Useche
  • Patent number: 7381734
    Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
    Type: Grant
    Filed: July 22, 2005
    Date of Patent: June 3, 2008
    Assignee: Tularik Limited
    Inventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
  • Publication number: 20080125412
    Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.
    Type: Application
    Filed: October 30, 2007
    Publication date: May 29, 2008
    Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
  • Patent number: 7365082
    Abstract: It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is CH or N; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: December 8, 2003
    Date of Patent: April 29, 2008
    Assignee: Bayer CropScience AG
    Inventors: Ping Ding, Robert N. Henrie, II, Daniel H. Cohen, John W. Lyga, David S. Rosen, George Theodoridis, Qun Zhang, Walter H. Yeager, Stephen F. Donovan, Steven Shunxiang Zhang, Inna Shulman, Seong Jae Yu, Guozhi Wang, Y. Larry Zhang, Ariamala Gopalsamy, Dennis L. Warkentin, Paul E. Rensner, Ian R. Silverman, Thomas G. Cullen
  • Patent number: 7307091
    Abstract: The invention discloses deuterated 3-piperidinopropiophenones as well as their physiologically tolerated salts. Furthermore, the invention concerns the use of deuterated 3-piperidinopropiophenones for the treatment of muscular illnesses as well as for the preparation of pharmaceutical drugs for the treatment of muscular illnesses. In addition, the invention discloses pharmaceutical formulations containing deuterated 3-piperidinopropiophenones as well as their physiologically tolerated salts for the treatment of muscular illnesses in addition to containing pharmaceutically tolerated adjuvants and/or additives.
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: December 11, 2007
    Assignee: BDD Berolina Drug Development GmbH
    Inventors: Rudolf-Gisbert Alken, Thomas Stabingis