Nitrogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/229)
  • Patent number: 11903917
    Abstract: The present invention relates to PD-0184264 for use in a method for the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza vims infection or a viral or bacterial infection alone. Also provided are compositions comprising such inhibitors for use in the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza virus infection or a bacterial or viral infection alone.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: February 20, 2024
    Assignee: ATRIVA THERAPEUTICS GMBH
    Inventors: Stephan Ludwig, Oliver Planz
  • Patent number: 11427540
    Abstract: Described herein, in part, are dosage forms and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a T-type calcium channel, such as epilepsy and epilepsy syndromes (e.g., absence seizures, juvenile myoclonic epilepsy, or a genetic epilepsy), tremor (e.g., essential tremor), and psychiatric disorder (e.g., mood disorders (e.g., major depressive disorder)). The present invention further comprises methods for modulating the function of a T-type calcium channel.
    Type: Grant
    Filed: July 28, 2021
    Date of Patent: August 30, 2022
    Assignee: PRAXIS PRECISION MEDICINES, INC.
    Inventors: Kiran Reddy, Margaret S. Lee, Gabriel Maurice Belfort, Sapna Makhija Garad, Mahesh Padval, Randall Wagner
  • Patent number: 10174025
    Abstract: The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided are a method for manufacturing a 4-heteroaryl-N-(2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxylic acid amide derivative; and an intermediate for this manufacturing method.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: January 8, 2019
    Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Tsutomu Satoh, Takashi Kudoh, Tetsuo Iwama
  • Patent number: 9150555
    Abstract: The present invention relates to a novel amide derivative. More specifically, the present invention provides a medicinal agent useful as a prophylactic or therapeutic agent for diseases, which relies on the production of cytokines from T cells, and which comprises an amide derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or the pharmacologically acceptable salt as an active ingredient. Provided is an amide derivative represented by general formula (I) [wherein each symbol is as defined in the description] or a pharmacologically acceptable salt thereof, or a solvate of the derivative or the pharmacologically acceptable salt.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: October 6, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroyuki Ushio, Maiko Hamada, Masayuki Watanabe, Atsushi Numata, Naoto Fujie, Tooru Takashima, Hiroyuki Furukawa, Junki Ando
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Publication number: 20140371176
    Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 18, 2014
    Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
  • 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: 8796460
    Abstract: The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: August 5, 2014
    Assignee: Mercky Sharp & Dohme Corp.
    Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana, Angie R. Angeles
  • Patent number: 8772494
    Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: July 8, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Lieven Meerpoel, Marcel Viellevoye, Joannes Theodorus Maria Linders
  • Patent number: 8759528
    Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Thorsten Lehmann-Lintz, Bernd Nosse
  • Patent number: 8759519
    Abstract: This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Julius W. J. Dickens, Ioannes Nicolaos Houpis, Yolande Lydia Lang, Carina Leys, Sigrid Carl Maria Stokbroekx, Johan Erwin Edmond Weerts
  • Patent number: 8735590
    Abstract: The present invention provides bicyclo-heptan-2-amines that selectively bind to the sigma-2 receptor and are useful in the treatment of diseases related to the sigma-2 receptor, for example, cancer and neurological disorders.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: May 27, 2014
    Inventors: Adeboye Adejare, Zeynep Ates-Alagoz, Boyenoh Gaye
  • Patent number: 8686021
    Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.
    Type: Grant
    Filed: May 3, 2006
    Date of Patent: April 1, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
  • Patent number: 8653108
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: February 18, 2014
    Assignee: Southwest Research Institute
    Inventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
  • Patent number: 8642623
    Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical compositions containing such compounds, a method for producing the compounds, and the use of such compounds to treat pain and various other conditions.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: February 4, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Jeewoo Lee
  • 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: 8580821
    Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: November 12, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christophe Grundschober, Patrick Schnider
  • Patent number: 8519139
    Abstract: The present invention relates to compounds of formula (II)
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: August 27, 2013
    Assignee: Aziende Chimeche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Angelo Guglielmotti, Guido Furlotti, Giuseppe Luna, Lorenzo Polenzani
  • Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Patent number: 8415476
    Abstract: An intermediate of formula (II)
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 9, 2013
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani
  • Patent number: 8367835
    Abstract: Provided is a compound useful as a therapeutic drug for pain and inflammation caused by various pathological conditions such as neuropathic pain and rheumatoid arthritis. The compound of the formula (I) or a salt thereof [wherein R1 is a methyl group or a hydrogen atom, R2 represents a hydrogen atom, an alkyl group, an alkylcarbonyl group or an aryl carbonyl group, A represents a cycloalkyl group, a cycloalkenyl group, an aryl group or a heteroaryl group (each group may be substituted with a substituent selected from the group consisting of alkyl, alkenyl, cycloalkyl and halogen), n and m each represent an integer of 1, 2 or 3, and p represents an integer of 0, 1, 2 or 3].
    Type: Grant
    Filed: May 7, 2009
    Date of Patent: February 5, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Yasunori Tsuzuki, Toshiya Morie, Takanori Nakamura, Isao Shimizu, Masanori Miyauchi
  • Publication number: 20130012485
    Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.
    Type: Application
    Filed: December 20, 2007
    Publication date: January 10, 2013
    Inventors: Daniel Kaspar Bäschlin, Richard Sedrani, Stefanie Flohr, Kenji Namoto, Nils Ostermann, Finton Sirockin, François Gessier, Garry Fenton, Mandy Christine Beswick, David Edward Clark, Bohdan Waszkowycz
  • 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: 20120283266
    Abstract: The invention relates to a compound of Formula (I): (A?)x-(A)-(B)-(Z)-(L)-(D), wherein: (A) is heteroaryl or aryl; each (A?), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is chosen from —N(—R1)—R2, —O—R3, and —S—R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and
    Type: Application
    Filed: April 19, 2010
    Publication date: November 8, 2012
    Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
  • Publication number: 20120270885
    Abstract: The use of a compound of formula I Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and Z? are provided that both are not N; R1, R2, R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Application
    Filed: February 10, 2012
    Publication date: October 25, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Peter Maienfisch, Louis-Pierre Molleyres, Jérôme Cassayre, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
  • Patent number: 8263583
    Abstract: This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenyl-hexanamide or derived form thereof and its use as a medicament.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: September 11, 2012
    Assignee: Pfizer Limited
    Inventors: Paul Alan Glossop, Kim James
  • Patent number: 8258305
    Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: September 4, 2012
    Assignee: Prexa Pharmaceuticals, Inc.
    Inventor: James R. Hauske
  • Patent number: 8252816
    Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical composition s containing such compounds, a method for producing the compounds, and the use of such compounds to treat pain and various other conditions.
    Type: Grant
    Filed: April 11, 2008
    Date of Patent: August 28, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Jeewoo Lee
  • Patent number: 8211916
    Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.
    Type: Grant
    Filed: January 22, 2008
    Date of Patent: July 3, 2012
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Patent number: 8173157
    Abstract: A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally substituted C3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: May 8, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventor: Hiroshi Nishikawa
  • 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
  • Publication number: 20120004208
    Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.
    Type: Application
    Filed: September 15, 2011
    Publication date: January 5, 2012
    Inventors: Luca Gobbi, Georg Jaeschke, Thomas Luebbers, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Lucinda Steward
  • Publication number: 20110046129
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
    Type: Application
    Filed: September 9, 2010
    Publication date: February 24, 2011
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
  • Patent number: 7872022
    Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.
    Type: Grant
    Filed: March 23, 2007
    Date of Patent: January 18, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christophe Grundschober, Patrick Schnider
  • Patent number: 7834185
    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: February 21, 2008
    Date of Patent: November 16, 2010
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • Publication number: 20100267946
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Application
    Filed: July 1, 2010
    Publication date: October 21, 2010
    Applicant: XenoPort, Inc.
    Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
  • Patent number: 7786307
    Abstract: The application relates to novel amino alcohols of general formula (I) where R, R1, R2, R3, R4, R5, X1 and X2 each have the definitions illustrated in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: August 31, 2010
    Assignee: Novartis AG
    Inventors: Peter Herold, Stefan Stutz, Aleksandar Stojanovic, Vincenzo Tschinke, Christiane Marti, Michael Quirmbach
  • Patent number: 7786140
    Abstract: A piperidine derivative of the formula (I) is found to bind specifically with the NR1/NR2B receptor and usable as an analgesic (pain treatment drug). wherein X is OH or lower alkylsulfonyloxy; Ar is optionally substituted aryl or optionally substituted heteroaryl; n is an integer of 1 to 4; m is an integer of 0 to 1; R1 is hydrogen; R2 is OH or R1 and R2 taken together may form a single bond; excluding that 1) n is 2; m is 0; R1 and R2 taken together may form a single bond; and Ar is optionally substituted phenyl and 2) n is 3; m is 0; R1 and R2 taken together may form a single bond; and Ar is phenyl.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: August 31, 2010
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshisada Yano, Toshiyuki Kanemasa, Shoichi Yamamoto
  • Patent number: 7781613
    Abstract: Disclosed are compounds of the general formula (I), with the definitions of the substituents R1 to R5, A and X being detailed in the text, and to their physiologically tolerated salts, to processes for preparing these compounds and to the use thereof as inhibitors of hormone-sensitive lipase (HSL).
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: August 24, 2010
    Assignee: Sanofi-Aventis
    Inventors: Karl Schoenafinger, Stefan Petry, Guenter Mueller, Karl-Heinz Baringhaus
  • Patent number: 7781590
    Abstract: The present invention comprises peridinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
    Type: Grant
    Filed: August 21, 2006
    Date of Patent: August 24, 2010
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Jean Jeunesse
  • Patent number: 7772223
    Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
    Type: Grant
    Filed: September 18, 2006
    Date of Patent: August 10, 2010
    Assignee: Pfizer Inc.
    Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
  • Publication number: 20100197732
    Abstract: The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.
    Type: Application
    Filed: June 5, 2008
    Publication date: August 5, 2010
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Sonny Sebastian, Sasidhar Venkata Balla, Ramamurthy Katikareddy, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • 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
  • Patent number: 7728145
    Abstract: There is described a process for the purification of an impure preparation containing fentanyl by means of a reverse phase preparative chromatography process. A chromatographic column is loaded with a stationary phase, typically a silica particle having an organic ligand bound thereto. With a loading ratio of from about 50 to about 150 the impure preparation is acidified and passed through the column. The column is eluted with typically an aqueous solution of acetonitrile and the purified fentanyl is obtained in a specified cut.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: June 1, 2010
    Assignee: Mallinckrodt Inc.
    Inventor: Enrico Anthony Antonini
  • Patent number: 7718675
    Abstract: The application relates to novel amino alcohols of the general formula (I) where R, R1, R2, R3, R4, R5 and R6 each have the definitions illustrated in detail in the description, to a process for their preparation, and to the use of these compounds as medicines, in particular as renin inhibitors.
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: May 18, 2010
    Assignee: Speedel Experimenta AG
    Inventors: Peter Herold, Stefan Stutz, Aleksandar Stojanovic, Vincenzo Tschinke, Christiane Marti, Michael Quirmbach
  • Patent number: 7700629
    Abstract: The present invention describes a new method for the separation of bupivacaine enantiomers consisting in a continuous separation process performed without heating, by the selective precipitation of their diastereomeric salts with tartaric acid. This heatless process avoids the degradation of the reagents granting a continuous process feature to the procedure. Another embodiment of the present invention is related to the enantiomeric manipulation of bupivacaine enantiomers in order to obtain pharmaceutical compositions presenting several enantiomeric excess of levobupivacaine to quantify and determinate the role of the dextrobupivacaine on its anesthetic and cardiotoxic effects. These enantiomeric manipulated compositions showed to present an expressive improvement on its anesthetic properties that had shown to be similar to racemic bupivacaine presenting a cardiotoxic profile similar to enantiomeric pure levobupivacaine.
    Type: Grant
    Filed: June 1, 2007
    Date of Patent: April 20, 2010
    Assignee: Cristalia Productos Quimicos Farmaceuticos Ltda
    Inventors: Roberto T. Sudo, Valter F. T. Russo, Elisa M. S. Russo
  • Publication number: 20100094015
    Abstract: An intermediate of formula (II)
    Type: Application
    Filed: December 15, 2009
    Publication date: April 15, 2010
    Applicant: AZIENDE CHIM. RIUN. ANGEL. FRA. A.C.R.A.F. S.p.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani
  • Publication number: 20100076024
    Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in claim 1; to compositions comprising said compounds and to their use as pharmaceutical agents, in particular as inhibitors of serine proteases.
    Type: Application
    Filed: February 20, 2008
    Publication date: March 25, 2010
    Inventors: Kaspar Zimmermann, Daniel Kaspar Baeschlin, Saliha Moussaoui
  • Patent number: 7674806
    Abstract: Amidines and derivatives thereof of formula (I) are described. The process for their preparation and pharmaceutical compositions thereof are also described. The amidines of the invention are useful in the inhibition of chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatement of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: March 9, 2010
    Inventors: Marcello Allegretti, Maria Candida Cesta, Giuseppe Nano, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta