Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/224)
  • Patent number: 10807953
    Abstract: The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.
    Type: Grant
    Filed: May 28, 2019
    Date of Patent: October 20, 2020
    Assignee: Pliva Hrvatska D.O.O.
    Inventors: Tomislav Biljan, Jasna Dogan, Leonid Metsger, Sara Morasi Pipercic, Marina Ratkaj, Maja Matanovic Skugor, Yi Wang
  • Patent number: 10597363
    Abstract: Disclosed herein are methods for obtaining N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)phenylmethyl) carbamide (pimavanserin) comprising the step of contacting an intermediate according to Formula (A) or a salt thereof, with an intermediate Formula B, or a salt thereof, to produce pimavanserin or a salt thereof wherein Y is —ORi or —NR2aR2b; R3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R4 is substituted or unsubstituted aralkyl; X is —OR22 or —NR23R24; (wherein R22 is hydrogen or substituted or unsubstituted C1-6alkyl and one of R23 and R24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R21 is —OCH2CH(CH3)2 or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.
    Type: Grant
    Filed: July 19, 2016
    Date of Patent: March 24, 2020
    Assignee: ACADIA Pharmaceuticals Inc.
    Inventors: Marlon Carlos, Sagun Tandel, Roger Olsson, Mikael Hillgren, Matthew J. Fleming, Andreas Philipp Boudier, Beat T. Weber
  • Patent number: 9751836
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: September 5, 2017
    Assignee: HELSINN HEALTHCARE SA
    Inventors: Silvina Garcia Rubio, Claudio Pietra, Claudio Giuliano, Zhigang Li
  • Publication number: 20150112070
    Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
    Type: Application
    Filed: January 5, 2015
    Publication date: April 23, 2015
    Applicant: FOREST LABORATORIES HOLDINGS LTD.
    Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew Phillips, Mahendra G. Dedhiya
  • Patent number: 9000174
    Abstract: The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: April 7, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Elfrida R. Benjamin, Zhengming Chen, Deyou Sha, Laykea Tafesse, Samuel F. Victory, John W. F. Whitehead
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Publication number: 20150045389
    Abstract: The present invention is a screening assay for identifying inhibitors of Pseudomonas aeruginosa CFTR Inhibitory Factor as well as compounds identified by the screening assay for use in compositions and methods for ameliorating or treating a respiratory disease such as cystic fibrosis or secondary infection thereof.
    Type: Application
    Filed: April 9, 2013
    Publication date: February 12, 2015
    Inventors: Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
  • Patent number: 8946433
    Abstract: The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques.
    Type: Grant
    Filed: September 15, 2011
    Date of Patent: February 3, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Brian Orr, Joseph P. Haar, Jr., George H. Klemm, Keith G. Tomazi
  • Patent number: 8940743
    Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: January 27, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
  • Patent number: 8937181
    Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: January 20, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Akira Matsumura, Hidenori Mikamiyama, Bin Shao, Naoki Tsuno, Jiangchao Yao
  • Publication number: 20150005328
    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: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Publication number: 20140371238
    Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Application
    Filed: March 13, 2014
    Publication date: December 18, 2014
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Patent number: 8901175
    Abstract: The use of opioids or opioid mimetics is suggested for the manufacture of a medicament for the treatment of resistant cancer patients.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: December 2, 2014
    Assignee: Universität Ulm
    Inventors: Erich Miltner, Claudia Friesen, Andreas Alt
  • Publication number: 20140343288
    Abstract: The present invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable sale thereof, or derivative thereof, suitable for administration to a patient, and methods for treatment with the formulations.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Inventors: S. George Kottayil, Venkat R. Goskonda, Zhongyuan Zhu, Linet Kattookaran, Neha Parikh
  • Publication number: 20140228406
    Abstract: The invention relates to fluorinated fentanyl derivatives that function as opioid receptor agonists, which activate target opioid receptors in a pH-dependent manner, and are thus selective for the receptors in inflamed (acidic) milieu; uses thereof and pharmaceutical compositions comprising them.
    Type: Application
    Filed: August 17, 2012
    Publication date: August 14, 2014
    Applicants: KONRAD-ZUSE-INSTITUT, CHARITÉ UNIVERSITÃTSMEDIZIN BERLIN
    Inventors: Christoph Stein, Marcus Weber, Christian Zöllner, Olga Scharkoi
  • Publication number: 20140171404
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
  • Publication number: 20140163024
    Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 10, 2013
    Publication date: June 12, 2014
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
  • Patent number: 8741894
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 3, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
  • Patent number: 8710049
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: April 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
  • Patent number: 8680282
    Abstract: A CPT1 inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: March 25, 2014
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Peter Brent Sampson, Yong Liu, Radoslaw Laufer, Yunhui Lang, Miklos Feher, Yi Yao, Guohua Pan
  • Publication number: 20140066421
    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: Application
    Filed: May 17, 2012
    Publication date: March 6, 2014
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
  • Patent number: 8658797
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: February 25, 2014
    Assignee: Helsinn Healthcare SA
    Inventors: Silvina Garcia Rubio, Claudio Giuliano, Claudio Pietra, Zhigang Li
  • Patent number: 8642771
    Abstract: The present invention provides methods for the synthesis of polycyclic guanidine compounds. In certain embodiments, provided methods include the step of contacting a described reagent with a triamine compound to provide a polycyclic guanidine compound.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: February 4, 2014
    Assignee: Novomer, Inc.
    Inventor: Alexei Gridnev
  • Patent number: 8642576
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8637547
    Abstract: Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: January 28, 2014
    Assignee: Chroma Therapeutics Ltd.
    Inventors: Alan Hornsby Davidson, David Charles Festus Moffat, Francesca Ann Day, Alistair David Graham Donald
  • Publication number: 20140018317
    Abstract: A compound having a structure of:
    Type: Application
    Filed: February 17, 2012
    Publication date: January 16, 2014
    Applicant: University of Pittsburgh-Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Patent number: 8604207
    Abstract: A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: December 10, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yoshikazu Takaoka, Shiro Shibayama, Rena Nishizawa
  • Patent number: 8592454
    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: November 26, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
  • Publication number: 20130310379
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 21, 2011
    Publication date: November 21, 2013
    Applicant: CONSTELLATION PHARMACEUTICALS
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
  • Patent number: 8575196
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: November 5, 2013
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 8569343
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: October 29, 2013
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Publication number: 20130274476
    Abstract: Inhibitors of the soluble epoxide exemplary hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Application
    Filed: June 14, 2013
    Publication date: October 17, 2013
    Inventors: Bruce D. Hammock, Paul D. Jones, Christophe Morisseau, Huazhang Huang, Hsing-Ju Tsai, Richard Gless, JR.
  • Publication number: 20130261132
    Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: October 3, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Per Vedso, Lars Kristian Albert BlÆher
  • Publication number: 20130231332
    Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.
    Type: Application
    Filed: September 1, 2011
    Publication date: September 5, 2013
    Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
  • Patent number: 8513237
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: August 20, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noëlle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
  • Publication number: 20130210625
    Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Application
    Filed: May 19, 2011
    Publication date: August 15, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Michel Muehlebach, Jurgen Harry Schaetzer
  • Publication number: 20130184262
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Application
    Filed: July 16, 2012
    Publication date: July 18, 2013
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
  • Patent number: 8481743
    Abstract: The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R1, R2, R3, R4 and R5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the activation of opioid receptors, particularly ?-opioid receptors. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: July 9, 2013
    Assignee: Purdue Pharma L.P.
    Inventor: Xiaoming Zhou
  • Patent number: 8466238
    Abstract: The invention aims to provide latent curing agents which exert high low-temperature curing properties when used together with ionically polymerizable compounds and which exhibit high storage stability at room temperature. Latent curing agents for ionically polymerizable compounds which agents each contain a hydroxyl-free amine imide compound having an N—N bond energy of 100 to 210 kJ/mol as determined by B3LYP functional theory method.
    Type: Grant
    Filed: December 26, 2008
    Date of Patent: June 18, 2013
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hiroaki Tamatani, Mitsuaki Chida, Yugo Yamamoto, Yuichi Ito, Takashi Nakano, Naritoshi Yoshimura
  • Publication number: 20130143925
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Application
    Filed: January 28, 2011
    Publication date: June 6, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Bruce D. Hammock, Tristan Rose, Christophe Morisseau, Kin Sing Lee
  • Publication number: 20130102626
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Application
    Filed: September 14, 2012
    Publication date: April 25, 2013
    Inventors: Peter Wipf, Marie Celine Frantz
  • Patent number: 8415369
    Abstract: A compound of the formula (I) wherein the substituents are as defined in the claims, is useful as a pesticide.
    Type: Grant
    Filed: October 13, 2008
    Date of Patent: April 9, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Werner Zambach, Ottmar Franz Hueter, Jean Wenger, Marcela Goeghova, Thomas Pitterna, Peter Maienfisch, Michel Muehlebach
  • Publication number: 20130085275
    Abstract: A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.
    Type: Application
    Filed: November 21, 2012
    Publication date: April 4, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventor: ONO PHARMACEUTICAL CO., LTD.
  • Publication number: 20130079525
    Abstract: The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.
    Type: Application
    Filed: November 21, 2012
    Publication date: March 28, 2013
    Applicant: KANEKA CORPORATION
    Inventor: KANEKA CORPORATION
  • Patent number: 8404693
    Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 26, 2013
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec
  • Patent number: 8399677
    Abstract: The invention provides a method for the preparation of fentanyl comprising: (a) reacting 4-piperidone hydrochloride monohydrate with aniline in presence of reducing environment to produce 4-anilinopiperidine (4-AP), (b) reacting the 4-AP as obtained from step (a) with phenethyl halide under reflux conditions in highly alkaline medium to give 4-anilino-N-phenethylpiperidine, and (c) converting the 4-anilino-N-phenethylpiperidine to fentanyl by reacting with propionyl chloride in presence of halogenated hydrocarbons, then isolating fentanyl by solvent extraction and purifying by crystallization from petroleum ether at a temperature ranging from 60-80° C.
    Type: Grant
    Filed: March 9, 2009
    Date of Patent: March 19, 2013
    Assignee: Defence Research & Development Organisation
    Inventors: Pradeep Kumar Gupta, Laxmi Manral, Kumaran Ganesan, Ramesh Chandra Malhotra, Krishnamurthy Sekhar
  • Publication number: 20130065756
    Abstract: Compounds of the formula I wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Application
    Filed: November 22, 2010
    Publication date: March 14, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Publication number: 20130053392
    Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
    Type: Application
    Filed: February 14, 2011
    Publication date: February 28, 2013
    Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
  • Publication number: 20130030184
    Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naCbH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C3H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg—and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substitute containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.
    Type: Application
    Filed: October 4, 2012
    Publication date: January 31, 2013
    Applicant: PERKINELMER HEALTH SCIENCES, INC.
    Inventor: PerkinElmer Health Sciences, Inc.