Chalcogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/236)
  • Patent number: 11439634
    Abstract: An object of the present invention is mainly to provide a medical skin external preparation that is suitable for treating superficial skin infections, in particular, superficial skin infections accompanied by blister or erosion, etc. For example, the present invention can provide a medical skin external preparation containing 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid and/or a pharmaceutically acceptable salt thereof as an active ingredient, and an alcohol and/or a fatty acid having 12 or more carbon atoms.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: September 13, 2022
    Assignee: Maruho Co., Ltd.
    Inventors: Tomoki Sakaguchi, Masumi Kawaguchi, Ayako Nakamura
  • Patent number: 11296733
    Abstract: A communication apparatus and a communication method are provided. The communication apparatus includes an antenna configured to receive a wireless signal, an oscillator driven by a driving current and configured to generate an oscillating signal based on the wireless signal, a measurer configured to measure an oscillation degree of the oscillating signal, and an accumulator configured to accumulate a difference between a target value and a measurement value of the oscillation degree. A value of the wireless signal is determined based on a cumulative signal corresponding to the accumulated difference.
    Type: Grant
    Filed: July 16, 2020
    Date of Patent: April 5, 2022
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Seok Ju Yun, Joonseong Kang
  • Patent number: 11147796
    Abstract: It is to provide an agent for preventing or improving hearing loss, which comprises a low molecular compound which can be produced relatively easily and inexpensively as an active ingredient. One or more compounds selected from the group consisting of compounds represented by the following formulas (I0), (II), and (III) and a pharmaceutically acceptable salt of the compounds when R3 is OH are used as an agent for preventing or improving hearing loss.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: October 19, 2021
    Assignees: TOHOKU UNIVERSITY, KAKE EDUCATIONAL INSTITUTION
    Inventors: Takaaki Abe, Yukio Katori, Yohei Honkura, Fumika Nanto, Kenichiro Hayashi
  • Patent number: 11065229
    Abstract: This invention relates to a method for treating atopic dermatitis, comprising administering an effective amount of N-acyltryptamine represented by Formula (I): wherein R represents a saturated aliphatic hydrocarbon group having 2 to 29 carbon atoms; or a pharmaceutically acceptable salt, hydrate or solvate thereof to a subject in need thereof.
    Type: Grant
    Filed: May 30, 2019
    Date of Patent: July 20, 2021
    Inventors: Masanori Somei, Kazuko Somei, Hiizu Somei
  • Patent number: 10584127
    Abstract: Disclosed are chemical entities of Formula (I), wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
    Type: Grant
    Filed: May 31, 2016
    Date of Patent: March 10, 2020
    Assignee: Rugen Holdings (Cayman) Limited
    Inventor: Gideon Shapiro
  • Patent number: 10376500
    Abstract: The invention relates to a gel composition containing pirfenidone, which is advantageous over other cutaneously administered pharmaceutical forms known in the prior art and which can be used in treatment for the restoration of tissues with fibrotic lesions and for the prevention of fibrotic lesions.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: August 13, 2019
    Assignee: CELL THERAPY AND TECHNOLOGY S.A. DE C.V.
    Inventors: José Agustin Rogelio Magaña Castro, Laura Vázquez Cervantes, Juan Socorro Armendáriz Borunda
  • Patent number: 10294230
    Abstract: Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: May 21, 2019
    Assignee: Rugen Holdings (Cayman) Limited
    Inventor: Gideon Shapiro
  • Patent number: 10206913
    Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: February 19, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Lori Jean Patterson, Eric L. Stangeland
  • Patent number: 9675598
    Abstract: The present disclosure relates to tolperisone, or a pharmaceutically acceptable salt or hydrate thereof, with 10 ppm 2-methyl-1-(4-methylphenyl)-propenone (4-MMPPO) or less, methods of producing the same, as well as compositions related thereto. The disclosure further relates to methods of treating a subject with tolperisone under conditions that limit exposure of the subject to tolerable levels of 4-MMPPO.
    Type: Grant
    Filed: August 1, 2016
    Date of Patent: June 13, 2017
    Assignee: Sanochemia Pharmazeutika AG
    Inventors: Federico Gaeta, Klaus Gerdes, Stefan Welzig, Beate Katz, Jan Rothenburger, Jozsef Gungl
  • Patent number: 9662317
    Abstract: The present disclosure relates to methods of administering tolperisone to subjects in need thereof. In certain aspects, the present disclosure relates to methods of administering tolperisone to subjects in need thereof, said methods limiting the exposure of the subject to 4-MMPPO.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: May 30, 2017
    Assignee: SANOCHEMIA PHARMAZEUTIKA AG
    Inventors: Federico Gaeta, Klaus Gerdes, Stefan Welzig, Beate Katz, Jan Rothenburger, Jozsef Gungl
  • Patent number: 9187423
    Abstract: The invention relates to processes and intermediates for preparing compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: November 17, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Miroslav Rapta
  • Patent number: 9012476
    Abstract: This invention relates to a new salt of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides the pharmaceutically acceptable hydrobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: April 21, 2015
    Assignee: Ivax International GmbH
    Inventors: Anne Zimmermann, Brian Frøstrup
  • Patent number: 9006445
    Abstract: This invention relates to a new crystalline form of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides polymorphic Form II of the Pridopidine hydrochloride salt, a process for the preparation of this polymorphic form, pharmaceutical compositions comprising polymorphic Form II, and methods of uses of this polymorphic form.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: April 14, 2015
    Assignee: Ivax International GmbH
    Inventors: Clas Sonesson, Thomas Pittelkow, Brian Frøstrup, Anne Zimmermann
  • Publication number: 20150073018
    Abstract: Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided, e.g., for the treatment of neuropathic pain.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: Benny Bang-Andersen, Andre Faldt, Tine Bryan Stensbol, Silke Miller, Heidi Lopez De Diego
  • Publication number: 20140329746
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20140315951
    Abstract: This invention relates to a new crystalline form of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides polymorphic Form II of the Pridopidine hydrochloride salt, a process for the preparation of this polymorphic form, pharmaceutical compositions comprising polymorphic Form II, and methods of uses of this polymorphic form.
    Type: Application
    Filed: September 6, 2012
    Publication date: October 23, 2014
    Applicant: IVAX INTERNATIONAL GMBH
    Inventors: Clas Sonesson, Thomas Pittelkow, Brian Frøstrup, Anne Zimmermann
  • Patent number: 8802856
    Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: October 22, 2013
    Date of Patent: August 12, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • Patent number: 8802857
    Abstract: The invention relates to processes and intermediates for preparing compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors.
    Type: Grant
    Filed: July 10, 2012
    Date of Patent: August 12, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Miroslav Rapta
  • Publication number: 20140018371
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 16, 2014
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Robert M. Jones, Sangdon Han, Juerg Lehmann, Lars Thoresen
  • Patent number: 8604058
    Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: December 10, 2013
    Assignee: Theravance, Inc.
    Inventors: Lori Jean Patterson, Eric L. Stangeland, Sheila Zipfel, Daniel D. Long
  • Publication number: 20130324507
    Abstract: The present invention concerns novel (aza)benzhydryl ether derivatives which exhibit H4-receptor binding activity. The present invention also concerns their process of preparation and their therapeutical uses.
    Type: Application
    Filed: June 5, 2013
    Publication date: December 5, 2013
    Applicant: BIOPROJET
    Inventors: Isabelle BERREBI-BERTRAND, Xavier BILLOT, Thierry CALMELS, Marc CAPET, Stéphane KRIEF, Olivier LABEEUW, Jeanne-Marie LECOMTE, Nicolas LEVOIN, Xavier LIGNEAU
  • Patent number: 8598359
    Abstract: The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
    Type: Grant
    Filed: June 11, 2008
    Date of Patent: December 3, 2013
    Assignee: Decode Genetics EHF
    Inventors: Vincent Sandanayaka, Jasbir Singh, Mark Gurney, Bjorn Mamat, Peng Yu, Louis Bedell, Lei Zhao, Rama K. Mishra
  • Patent number: 8592596
    Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: November 26, 2013
    Assignee: Theravance, Inc.
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • Patent number: 8592453
    Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: November 26, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • Patent number: 8557998
    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: Grant
    Filed: June 20, 2012
    Date of Patent: October 15, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd
    Inventor: Tomohiro Toyoda
  • Patent number: 8507526
    Abstract: The use of 4-[2-(4-methylphenylsulfanyl)phenyl]piperidine or a pharmaceutically acceptable salt thereof in the treatment of irritable bowl syndrome.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: August 13, 2013
    Assignee: H. Lundbeck A/S
    Inventor: Silke Miller
  • Publication number: 20130197032
    Abstract: The present invention relates to a novel use of both enantiomers of the phenylpiperidine derivative OSU6162, i.e. (?) and (+)-OSU6162 as partial agonists on 5-hydroxytryptamine (5hHT) receptors. As a result, both (?) OSU6162 and (+)-OSU6162 may be used for the treatment and/or prevention of one or more diseases associated with a need for modulation of monoaminergic neurotransmitter receptors, wherein at least one of the monoaminergic neurotransmitter receptors is a 5-hydroxytryptamine receptor (5-HT receptor). Thus, said compounds act as stabilizers not only on dopaminergic, but also on serotonergic brain signaling and will act as partial agonists on such monoaminergic neurotransmitter receptors.
    Type: Application
    Filed: September 20, 2011
    Publication date: August 1, 2013
    Applicant: A. CARLSSON RESEARCH AB
    Inventors: Lizzie Maria Carlsson, Angélica Kloberg, Ethan S. Burstein, Per Arvid Emil Carlsson
  • Publication number: 20130197031
    Abstract: The present invention provides novel deuterated analogs of Pridopidine, i.e. 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine. Pridopidine is a drug substance currently in clinical development for the treatment of Huntington's disease. In other aspects the invention relates to pharmaceutical compositions comprising a deuterated analog of Pridopidine of the invention, and to therapeutic applications of these analogs.
    Type: Application
    Filed: August 31, 2011
    Publication date: August 1, 2013
    Applicant: IVAX INTERNATIONAL GMBH
    Inventor: Clas Sonesson
  • Publication number: 20130190352
    Abstract: Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided e.g. for the treatment of neuropathic pain.
    Type: Application
    Filed: October 25, 2012
    Publication date: July 25, 2013
    Applicant: H. LUNDBECK A/S
    Inventor: H. LUNDBECK A/S
  • Publication number: 20130150406
    Abstract: This invention relates to a new salt of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides the pharmaceutically acceptable hydrobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Applicant: Ivax International GmbH
    Inventor: Ivax International GmbH
  • Publication number: 20130131079
    Abstract: The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Applicant: FAES FARMA, S.A.
    Inventors: Francisco Ledo Gómez, Ana Muñoz Muñoz, Carmen Pumar Durán
  • Publication number: 20130045165
    Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.
    Type: Application
    Filed: April 29, 2011
    Publication date: February 21, 2013
    Applicant: KINENTIA BIOSCIENCES, LLC
    Inventor: David J. Fairfax
  • 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
  • Patent number: 8362255
    Abstract: A process for the manufacture of (un)substituted phenylsulfanylphenyl-piperidines comprising the use of benzyl as N-piperidine protecting group is disclosed.
    Type: Grant
    Filed: March 2, 2009
    Date of Patent: January 29, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Michael Rock, Sebastian Brandes
  • Patent number: 8354430
    Abstract: A method is provided for the treatment of sleep apnea and other conditions wherein an effective amount of crystalline 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine monohydrochloride of formula (I): optionally comprising water up to 6%, and having an X-ray diffractogram that comprises characteristic peaks (2?) at 11.2°, 19.9°, 20.7° and 34.1°±0.2° is administered to a patient in need thereof.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: January 15, 2013
    Assignee: Bioprojet
    Inventors: Manuel Raga, Juan Sallares, Marta Guerrero, Antonio Guglietta, Jean-Michel Arrang, Jean-Charles Schwartz, Holger Stark, Walter Schunack, Xavier Ligneau, Jeanne-Marie Lecomte, Charon Ganellin
  • Patent number: 8324251
    Abstract: The present application describes modulators of MIP-1? or CCR-1 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, ring A, T, V, X, R1, R2 and R8, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: December 4, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Percy H. Carter
  • Publication number: 20120302553
    Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
    Type: Application
    Filed: February 6, 2012
    Publication date: November 29, 2012
    Applicant: H. LUNDBECK A/S
    Inventors: Thomas Ruhland, Garrick P. Smith, Benny Bang-Anderson, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
  • Patent number: 8304433
    Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: November 6, 2012
    Assignee: Theravance, Inc.
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • Patent number: 8304432
    Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: November 6, 2012
    Assignee: Theravance, Inc.
    Inventors: Lori Jean Patterson, Eric L. Stangeland, Sheila Zipfel, Daniel D. Long
  • Patent number: 8299095
    Abstract: Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided e.g. for the treatment of neuropathic pain.
    Type: Grant
    Filed: June 15, 2007
    Date of Patent: October 30, 2012
    Assignee: H. Lundbeck A/S
    Inventors: Benny Bang-Andersen, Andre Faldt, Tine Bryan Stensbol, Silke Miller, Heidi Lopez De Diego
  • Publication number: 20120259122
    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: June 20, 2012
    Publication date: October 11, 2012
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
  • Patent number: 8207197
    Abstract: The invention relates to new crystalline 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine monohydrochloride, the respective manufacture and methods of use, and compositions containing such a compound.
    Type: Grant
    Filed: February 6, 2006
    Date of Patent: June 26, 2012
    Assignee: Bioprojet
    Inventors: Manuel Raga, Juan Sallares, Marta Guerrero, Antonio Guglietta, Jean-Michel Arrang, Jean-Charles Schwartz, Holger Stark, Walter Schunack, Xavier Ligneau, Jeanne-Marie Lecomte, Charon Ganellin
  • 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: 20120035214
    Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: April 1, 2010
    Publication date: February 9, 2012
    Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Daniel J. McKay, Melissa Arbour, Renee Aspiotis, Austin Chen, Pierre-Andre Fournier, Michel Gallant, Yongxin Han, Helene Juteau, Patrick Lacombe, Sebastien Laliberte, Sophie Lauzon, Carmela Molinaro, Paul O'Shea, Yeeman Ramtohul, Daniel Simard, Dwight MacDonald, Bruce Mackay, Christophe Mellon, Krista Morley, Chit Tsui, Sarah Jennifer Dolman, Greg Hughes, Jacob Janey
  • Patent number: 8076329
    Abstract: The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
    Type: Grant
    Filed: April 25, 2006
    Date of Patent: December 13, 2011
    Assignee: Bioprojet
    Inventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
  • Publication number: 20110281844
    Abstract: Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.
    Type: Application
    Filed: December 15, 2010
    Publication date: November 17, 2011
    Inventors: Jean-Charles SCHWARTZ, Jean-Michel ARRANG, Monique GARBARG, Jeanne-Marie LECOMTE, Xavier LIGNEAU, Walter G. SCHUNACK, Holger STARK, Charon Robin GANELLIN, Fabien LEURQUIN, Elz Sigurd
  • Publication number: 20110281890
    Abstract: Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Application
    Filed: July 25, 2011
    Publication date: November 17, 2011
    Inventor: Connie L. Sun
  • Publication number: 20110206782
    Abstract: The present invention relates to new piperidine modulators of dopamine receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 15, 2011
    Publication date: August 25, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventor: Chengzhi Zhang
  • Publication number: 20110200935
    Abstract: The present invention provides a photoresist composition having a sulfonium salt comprising an anion represented by the formula (IA): wherein R1 and R2 independently represent a hydrogen atom, a C1-C12 aliphatic hydrocarbon group, a C3-C20 saturated cyclic hydrocarbon group, a C6-C20 aromatic hydrocarbon group or a C7-C21 aralkyl group, and the aliphatic hydrocarbon group, the saturated cyclic hydrocarbon group, the aromatic hydrocarbon group and the aralkyl group can have one or more substituents selected from the group consisting of a hydroxyl group, a cyano group, a fluorine atom, a trifluoromethyl group and a nitro group, and one or more —CH2— in the aliphatic hydrocarbon group can be replaced by —O— or —CO—, or R1 and R2 are bonded each other to form a C4-C20 nitrogen-containing ring together with the nitrogen atom to which they are bonded, an acrylic resin having an acid-labile group and being insoluble or poorly soluble in an aqueous alkali solution but becoming soluble in an aqueous alkali solutio
    Type: Application
    Filed: February 11, 2011
    Publication date: August 18, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tatsuro MASUYAMA, Satoshi YAMAGUCHI
  • Publication number: 20110160247
    Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereo. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.
    Type: Application
    Filed: June 8, 2009
    Publication date: June 30, 2011
    Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
    Inventors: Jianqi Li, Kai Gao, Wangping Cai, Yongyong Zheng