The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 544/389)
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Publication number: 20150072984
    Abstract: Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 12, 2015
    Inventor: Xiangping Qian
  • Publication number: 20150018335
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 15, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Patent number: 8889685
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful for treating sleep disorders.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: November 18, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8889686
    Abstract: L malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are disclosed for decreasing the bitterness of eszopiclone dosage forms
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: November 18, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Patent number: 8822463
    Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: September 2, 2014
    Assignee: Sk Biopharmaceuticals Co., Ltd.
    Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
  • Publication number: 20140235650
    Abstract: The invention relates to a compound of formula (I), where R1, R2, R7, m, n, and L1 are as defined in claim 1, and to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.
    Type: Application
    Filed: June 22, 2012
    Publication date: August 21, 2014
    Applicant: Metabolys
    Inventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
  • Patent number: 8809332
    Abstract: Besylate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: August 19, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Richard Hsia, H. Scott Wilkinson, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Publication number: 20140213737
    Abstract: A method for enhancing, by at least 10 fold, the antibacterial activity of an antisense oligonucleotide composed of morpholino subunits linked by phosphorus-containing intersubunit linkages. The method includes one or both of: conjugating an arginine-rich carrier to a 3? or 5? end of the oligonucleotide and modifying the oligonucleotide to contain 20%-50% intersubunit linkages that are positively charged at physiological pH. Also disclosed is an antisense oligonucleotide having enhanced antibacterial activity by virtue of one or both modifications.
    Type: Application
    Filed: August 9, 2013
    Publication date: July 31, 2014
    Applicant: Sarepta Therapeutics, Inc.
    Inventors: Dwight D. Weller, Bruce L. Geller, Patrick L. Iversen, Lucas D. Tilley, Jed N. Hassinger
  • Patent number: 8734845
    Abstract: Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: May 27, 2014
    Assignee: Mannkind Corporation
    Inventors: Marshall L. Grant, Grayson W. Stowell, Paul Menkin
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Patent number: 8722939
    Abstract: The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: May 13, 2014
    Assignees: Northwestern University, Cambria Pharmaceuticals, Inc.
    Inventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanites, Richard I. Morimoto, Wei Zhang, Richard B. Silverman
  • Patent number: 8697335
    Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: April 15, 2014
    Assignee: JSR Corporation
    Inventors: Kazuo Nakahara, Mitsuo Sato
  • Publication number: 20140066369
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, 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 condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
    Type: Application
    Filed: April 18, 2012
    Publication date: March 6, 2014
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Dawei Yue, Xiuwen Zhu
  • 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
  • Patent number: 8541416
    Abstract: L-malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl) carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: September 24, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Publication number: 20130225605
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: April 22, 2013
    Publication date: August 29, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130217686
    Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.
    Type: Application
    Filed: September 28, 2011
    Publication date: August 22, 2013
    Applicant: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
  • Patent number: 8497268
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful to provide blood levels of eszopiclone that are independent of fasting state.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: July 30, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8497267
    Abstract: Besylate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: July 30, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Richard Hsia, H. Scott Wilkinson, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Publication number: 20130184222
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Patent number: 8470831
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: June 25, 2013
    Assignee: Cogenia SRL
    Inventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Patent number: 8431577
    Abstract: The present invention discloses a crystalline form of S-zopiclone (Formula I) having a powder X-Ray diffraction spectrum excited by Cu-Ka radiation with characteristic peaks expressed in terms of 2? at about 11.08°, about 12.38°, about 15.86°, about 17.88°, about 19. 98° and about 20.58°; a DSC thermogram with a peak at about 207.7° C. and an infrared absorption spectrum (IR) with characteristic peaks at about 3078 cm?1, about 2942˜2838 cm?1, about 2790 cm?1, about 1716 cm?1, about 1463 cm?1, about 1372 cm?1 and about 757 cm?1. The present invention also discloses a method for preparing the crystalline form of eszopiclone, its pharmaceutical composition and its use in preparing a medicament for treating sleep disorders.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: April 30, 2013
    Assignee: Tianjin Tasly Group Co., Ltd.
    Inventors: Guocheng Wang, Xueyu Xu
  • Publication number: 20130072468
    Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 21, 2013
    Inventors: Eric J. Gilbert, William J. Greenlee, Michael W. Miller, Jack D. Scott, Andrew W. Stamford
  • Publication number: 20130030008
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 1, 2012
    Publication date: January 31, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Patent number: 8357679
    Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: January 22, 2013
    Assignee: MSD Oss B.V.
    Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
  • Patent number: 8343963
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: January 1, 2013
    Assignee: 4SC AG
    Inventor: Stefano Pegoraro
  • Patent number: 8309723
    Abstract: Present invention relates to an improved process for the preparation of Zopiclone and its enantiomerically enriched isomer (Eszopiclone). 6-(5-Chloropyridin-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine is reacted with 1-chloro-carbonyl-4-methylpiperazine in the presence of alkali earth metal carbonates, hydroxides or oxides in a solvent medium to give Zopiclone. It is reacted with optically active acid in a mixture of water and water miscible organic solvent followed by work up to give Eszopiclone. The present invention also relates to process for the conversion of (R) or (S) Zopiclone to 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydro-pyrrolo-[3,4-b]-pyrazine of the intermediate which can be converted to racemic Zopiclone.
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: November 13, 2012
    Assignee: Mylan Laboratories Ltd.
    Inventors: Om Dutt Tyagi, Tushar Kumar Srivastava, Vellanki Siva Ram Prasad, Dnyandev Ragho Rane, Bandi Naga Durga Rao, Daggula Srinivas Reddy
  • Publication number: 20120264765
    Abstract: The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds.
    Type: Application
    Filed: October 29, 2010
    Publication date: October 18, 2012
    Applicants: Cambria Pharmaceuticals, Inc., Northwestern University
    Inventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanties, Richard I. Morimoto, Wei Zhang, Richard B. Silverman
  • Patent number: 8287969
    Abstract: An isosorbide derivative of Formula (I) is provided. In Formula (I), Z is —CH2—CH2—, —CH?CH—, —C?C—, —CH2—O—, —CH2—S—, —CH?N—O—, —CO—O—, —CO—S—, single bond, -ph-, —CO—O-ph- or —CO—O-ph-CO—O—, and ph represents benzene, R1 and R2 are, independently, C1-25 alkyl, —CN, —NCS, —CX3 or —OCX3, and X represents halogen, and m and n are, independently, 0, 1 or 2. The invention also provides a liquid crystal display including the isosorbide derivative.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: October 16, 2012
    Assignee: Industrial Technology Research Institute
    Inventors: Chun-Ming Wu, Kevin Lin, Shih-Hsien Liu, Chih-Lung Chin, An-Cheng Chen, Kung-Lung Cheng, Chien-Hsien Cheng
  • Publication number: 20120252789
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Dirk Wienke
  • Patent number: 8269005
    Abstract: L-malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: September 18, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas
  • Patent number: 8242175
    Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: August 14, 2012
    Assignee: DAC S.R.L.
    Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • Patent number: 8212036
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: July 3, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas
  • Publication number: 20120136002
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: May 18, 2010
    Publication date: May 31, 2012
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Publication number: 20120046293
    Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: October 10, 2011
    Publication date: February 23, 2012
    Applicant: Merck Frosst Canada Ltd.
    Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Patent number: 8088921
    Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: January 3, 2012
    Assignee: Wilex AG
    Inventors: Hugo Ziegler, Peter Wikstroem
  • Publication number: 20110275650
    Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
    Type: Application
    Filed: November 10, 2009
    Publication date: November 10, 2011
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
  • Patent number: 8049011
    Abstract: The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: November 1, 2011
    Assignee: KRKA, Tovarna Zdravil, D.D., Novo Mesto
    Inventors: Jaroslav Tihi, Rok Zupet, Anica Pecavar, Ivanka Kolenc, Darja Pavlin
  • Publication number: 20110251389
    Abstract: The compound of formula (8), in racemic or single enantiomeric form, is useful in making N-(diphenylmethyl)-piperazines such as cetirizine and levocetrizine. wherein Z is preferably phenyl.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 13, 2011
    Inventor: Jie ZHU
  • Patent number: 8012982
    Abstract: The present invention is directed to compounds of formula (I): where X, Y, R1, R2 and R3 are defined therein, which can act as modulators of viral replication and/or virus production, especially of the hepatitis C virus (HCV).
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: September 6, 2011
    Assignee: Istituto di Ricerche Biologia Molecolare P. Angeletti SpA
    Inventors: Immacolata Conte, Caterina Ercolani, Claudio Giuliano, Giovanni Migliaccio, Gessica Filocamo, legal representative, Veronica Suriano, legal representative, Ian Stansfield
  • Publication number: 20110212971
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: May 5, 2011
    Publication date: September 1, 2011
    Inventors: Tao Wang, Yasutsugu Ueda, Lawrence G. Hamann, Zhongxing Zhang, Zhiwei Yin, Alicia Regueiro-Ren, David J. Carini, Jacob Swidorski, Zheng Liu, Nicolas A. Meanwell, John F. Kadow, Barry L. Johnson
  • Publication number: 20110195977
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 23, 2009
    Publication date: August 11, 2011
    Inventors: Daniele Fancelli, Varasi Mario, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Patent number: 7989623
    Abstract: The compound of formula (8), in racemic or single enantiomeric form, is useful in making N-(diphenylmethyl)-piperazines such as cetirizine and levocetrizine. wherein Z is preferably phenyl.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: August 2, 2011
    Assignee: Synthon BV
    Inventor: Jie Zhu
  • Patent number: 7973042
    Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their 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 disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
    Type: Grant
    Filed: December 15, 2008
    Date of Patent: July 5, 2011
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
  • Publication number: 20110152290
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 4, 2010
    Publication date: June 23, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • Publication number: 20110124867
    Abstract: The present invention relates to novel processes for the preparation of the compound of the Formula A45: or a physiologically acceptable salt, solvate or prodrug thereof, which has utility, for example, as a pharmaceutically active compound with CXCR3 antagonist activity, and to novel intermediates useful in the synthesis thereof.
    Type: Application
    Filed: December 16, 2008
    Publication date: May 26, 2011
    Applicant: Schering Corporation
    Inventors: Frank Xing Chen, Timothy D. Cutarelli, Xiayong Fu, Xian Liang, Timothy L. McAllister, Robert K. Orr, Jianguo Yin, Kelvin H. Yong, Man Zhu
  • Publication number: 20110117591
    Abstract: Chemical stain compounds containing a fluorophore and a reducible quenching unit are disclosed. The reducible quenching unit quenches the fluorophore while in its oxidized state. Upon reduction, the quenching properties of the quenching unit are diminished or eliminated. The chemical compounds can be used in a variety of applications, including the detection of bacterial cells, monitoring the electron transport chain function of bacterial cells, monitoring the oxidation state of non-biological systems, and assaying the effectiveness of antibacterial or antimicrobial agents.
    Type: Application
    Filed: October 20, 2010
    Publication date: May 19, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Ching-Ying CHEUNG, Diane R. Gray, Stephen T. Yue