The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/237)
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Patent number: 9334223Abstract: Process for the preparation of 2-phenyl-2-methyl propanoic acid derivatives, useful as intermediates in the preparation of fexofenadine hydrochloride.Type: GrantFiled: October 3, 2014Date of Patent: May 10, 2016Assignee: Dipharma Francis S.r.l.Inventors: Pietro Allegrini, Vittorio Lucchini, Davide Rossi, Mauro Mittino, Gabriele Razzetti
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Publication number: 20150105552Abstract: 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: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
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Publication number: 20150057443Abstract: 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: ApplicationFiled: August 21, 2014Publication date: February 26, 2015Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
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Patent number: 8916587Abstract: 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: GrantFiled: April 10, 2012Date of Patent: December 23, 2014Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Patent number: 8772291Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.Type: GrantFiled: December 8, 2009Date of Patent: July 8, 2014Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
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Patent number: 8653106Abstract: 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: GrantFiled: July 30, 2010Date of Patent: February 18, 2014Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Patent number: 8481527Abstract: 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: GrantFiled: October 27, 2007Date of Patent: July 9, 2013Assignee: Richter Gedeon Nyrt.Inventors: Istvan Vago, Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Monika Vastag
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Publication number: 20130117941Abstract: 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: ApplicationFiled: June 21, 2011Publication date: May 16, 2013Applicant: BASF SEInventors: Markus Frey, Hauke Rohwer, Frédérique Wendeborn, Menno Hazenkamp
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Publication number: 20130096151Abstract: 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: ApplicationFiled: March 29, 2011Publication date: April 18, 2013Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Yanmin Hu, Anthony M.R. Coates
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Patent number: 8420622Abstract: 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: GrantFiled: December 14, 2007Date of Patent: April 16, 2013Assignee: Merck, Sharp & Dohme, Corp.Inventors: Benito Munoz, Jed Hubbs, Christopher L. Hamblett, Hua Zhou, Michelle Martinez
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Patent number: 8389547Abstract: Compounds of formula (I) are modulators of gamma-secretase, and hence are useful in treatment of Alzheimer's disease.Type: GrantFiled: April 25, 2007Date of Patent: March 5, 2013Inventors: Yudith Garcia, Joanne Clare Hannam, Timothy Harrison, Christopher L. Hamblett, Jed L. Hubbs, Janusz Josef Kulagowski, Andrew Madin, Mark Peter Ridgill, Eileen Seward
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Patent number: 8372979Abstract: 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: GrantFiled: April 24, 2008Date of Patent: February 12, 2013Assignee: SANOCHEMIA Pharmazeutika AGInventors: Stefan Welzig, Jan Rothenburger, Beate Kälz, József Gungl, Klaus Gerdes, Federico Gaeta
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Publication number: 20120196895Abstract: 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: ApplicationFiled: January 11, 2010Publication date: August 2, 2012Applicant: Bionevia Pharmaceuticals, Inc.Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Jason A. Hanko
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Publication number: 20120183498Abstract: 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: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Publication number: 20120149900Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.Type: ApplicationFiled: January 8, 2010Publication date: June 14, 2012Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
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Patent number: 8153657Abstract: 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: GrantFiled: October 22, 2004Date of Patent: April 10, 2012Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Jia Zhou
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Publication number: 20120046247Abstract: 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: ApplicationFiled: August 16, 2011Publication date: February 23, 2012Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
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Publication number: 20120022086Abstract: 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: ApplicationFiled: March 17, 2010Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Patent number: 8067605Abstract: 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: GrantFiled: November 30, 2010Date of Patent: November 29, 2011Assignee: Albany Molecular Research, Inc.Inventors: Harold Meckler, Benjamin J. Littler, Prasad Raje, Michael Van Brundt, Paul Vogt
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Publication number: 20110281911Abstract: 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: ApplicationFiled: August 3, 2009Publication date: November 17, 2011Applicant: Bionevia Pharmaceuticals, Inc.Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Jason A. Hanko, Jeffrey P. Kiplinger
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Publication number: 20110263428Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: July 1, 2009Publication date: October 27, 2011Applicant: 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
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Publication number: 20110118312Abstract: 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: ApplicationFiled: January 20, 2011Publication date: May 19, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
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Publication number: 20110082295Abstract: 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: ApplicationFiled: May 27, 2009Publication date: April 7, 2011Applicants: Tokyo Institute of Technology, Kyoto UniversityInventors: Hachiro Sugimoto, Takashi Takahashi, Ichiro Hijikuro, Michiaki Okuda
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Publication number: 20110071295Abstract: 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: ApplicationFiled: November 30, 2010Publication date: March 24, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Harold MECKLER, Ben Littler, Prasad Raje, Michael Van Brunt, Paul F. Vogt
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Publication number: 20100324090Abstract: 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: ApplicationFiled: April 24, 2008Publication date: December 23, 2010Inventors: Federico Gaeta, Klaus Gerdes, Stefan Welzig, Beate Kätz, Jan Rothenburger, József Gungl
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Publication number: 20100298329Abstract: 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: ApplicationFiled: September 19, 2008Publication date: November 25, 2010Applicant: Massachusette Institute of TechnologyInventors: Alice T. Shaw, Tyler E. Jacks, Nicola Tolliday
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Patent number: 7812035Abstract: 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: GrantFiled: December 11, 2002Date of Patent: October 12, 2010Assignee: Sepracor Inc.Inventors: Heike Radeke, Liming Shao
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Patent number: 7781459Abstract: 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: GrantFiled: December 20, 2006Date of Patent: August 24, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Elisabeth DeFossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger, Alfons Enhsen
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Patent number: 7763639Abstract: 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: GrantFiled: December 8, 2006Date of Patent: July 27, 2010Assignee: NSAB, Filial AF Neurosearch Sweden AB, SverigeInventors: Clas Sonesson, Lars Swanson, Nicholas Ross Waters
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Publication number: 20100160376Abstract: 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: ApplicationFiled: May 24, 2007Publication date: June 24, 2010Inventor: Marshall Anlauf Thompson
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Publication number: 20100152238Abstract: 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: ApplicationFiled: March 5, 2008Publication date: June 17, 2010Applicant: Yissum Research Development Company of The Hebrew University of JerusalemInventors: Raphael Mechoulam, Natalya Kogan
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Publication number: 20100150995Abstract: 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: ApplicationFiled: April 24, 2008Publication date: June 17, 2010Applicant: SANOCHEMIA PHARMAZEUTIKA AGInventors: Stefan Welzig, Jan Rothenburger, Beate Kalz, Jozsef Gungl, Klaus Gerdes, Federico Gaeta
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Publication number: 20100113496Abstract: 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: ApplicationFiled: September 22, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Patent number: 7700587Abstract: 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: GrantFiled: September 7, 2004Date of Patent: April 20, 2010Assignee: Florida A&M UniversityInventors: Seth Y. Ablordeppey, Donald M. N. Sikazwe
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Patent number: 7649095Abstract: 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: GrantFiled: April 12, 2006Date of Patent: January 19, 2010Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Katsuya Kishikawa
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Publication number: 20090253743Abstract: 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: ApplicationFiled: November 26, 2008Publication date: October 8, 2009Applicants: Avigen, Inc., Sanochemia Pharmazeutika, AGInventors: Federico Gaeta, Stefan Welzig, Jan Rothenburger, Beate Kalz, Jozsef Gungl, Klaus Gerdes
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Patent number: 7517892Abstract: 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: GrantFiled: September 12, 2001Date of Patent: April 14, 2009Assignee: 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
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Patent number: 7511147Abstract: The present invention relates to a shortened process for preparing L-lobeline by rhodium-catalysed asymmetric hydrogenation on an industrial scale.Type: GrantFiled: July 8, 2005Date of Patent: March 31, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Franz-Dietrich Klingler, Rainer Sobotta
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Publication number: 20090076081Abstract: 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: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian, Xihan Wu
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Publication number: 20090069378Abstract: The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 12, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Publication number: 20080293948Abstract: 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: ApplicationFiled: May 15, 2008Publication date: November 27, 2008Applicant: DIPHARMA FRANCIS s.r.l.Inventors: Tiziano Scubla, Pietro Allegrini, Eliana Rocchini, Caterina Napoletano
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Publication number: 20080227814Abstract: 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: ApplicationFiled: January 18, 2005Publication date: September 18, 2008Inventors: Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Owen Brendan Wallace
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Publication number: 20080227983Abstract: 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: ApplicationFiled: May 29, 2008Publication date: September 18, 2008Applicant: AMR TECHNOLOGY, INC.Inventor: Thomas E. D'Ambra
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Publication number: 20080221106Abstract: 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: ApplicationFiled: August 5, 2005Publication date: September 11, 2008Inventors: Liya Zhu, Wenjie Wang, Halhong Huang, Ziyun Lin, Liyuan Mou, Zhengui Nie, Yu He, Xueyu Ouyang, Shanying Peng, Dongfong Zhang, Jun Wei
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Patent number: 7385060Abstract: 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: GrantFiled: March 31, 2003Date of Patent: June 10, 2008Assignee: Sanochemia Pharmazeutika AGInventors: Laszlo Czollner, Beate Kälz, Jan Rothenburger, Stefan Welzig
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Publication number: 20080132751Abstract: 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: ApplicationFiled: November 30, 2006Publication date: June 5, 2008Inventors: Brian C. Keller, Camilo Rey, Jorge Useche
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Patent number: 7381734Abstract: 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: GrantFiled: July 22, 2005Date of Patent: June 3, 2008Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Publication number: 20080125412Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: ApplicationFiled: October 30, 2007Publication date: May 29, 2008Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Patent number: 7365082Abstract: 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: GrantFiled: December 8, 2003Date of Patent: April 29, 2008Assignee: Bayer CropScience AGInventors: 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
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Patent number: 7307091Abstract: 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: GrantFiled: April 29, 2002Date of Patent: December 11, 2007Assignee: BDD Berolina Drug Development GmbHInventors: Rudolf-Gisbert Alken, Thomas Stabingis