Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/233)
  • Patent number: 10179761
    Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: January 15, 2019
    Assignees: UNIVERSITE DE LILLE 2 DROIT ET SANTE, CENTRE HOSPITALIER REGIONAL ET UNIVERSITAIRE DE LILLE (CHRU)
    Inventors: Patricia Melnyk, Patrick Vermersch, Pascal Carato, Bénédicte Oxombre-Vanteghem, Hélène Zephir, Marion Donnier-Marechal
  • Patent number: 10081597
    Abstract: The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic methylphenidate. The process involves the treatment of racemic mixture of dl-threo-methylphenidate base in the presence of di-pivaloyl-D-tartaric acid (D-DPTA) in a solvent to isolate dipivaloyl tartrate salt of d-threo-methylphenidate. The dipivaloyl tartrate salt of d-threo-methylphenidate is treated with a base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent. The d-threo-methylphenidate base is treated with hydrochloric acid-isopropyl alcohol solution to obtain slurry of d-threo-methylphenidate hydrochloride also known as dexmethylphenidate hydrochloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone. The invention also discloses a process for recovery of D-DPTA from the salt mother liquor and from the spent aqueous layer.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: September 25, 2018
    Assignee: Embio Limited
    Inventors: Ashutosh Digambar Gupte, Sunil Vaman Joshi, Amit Hari Pakhurde
  • Patent number: 9458102
    Abstract: Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: October 4, 2016
    Assignee: OREGON HEALTH & SCIENCE UNIVERSITY
    Inventors: Jeffrey Karpen, Sarah Kirk, Adriana Andrade, Michelle Schaffer, Kenneth Melich
  • Patent number: 9278928
    Abstract: The present invention relates to a process for the preparation of d-threo-ritalinic acid salt thereof. More particularly, the present invention relates a process for the preparation of d-threo-ritalinic acid salt via novel organic salts of intermediate thereof.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: March 8, 2016
    Assignee: ZCL CHEMICALS LIMITED
    Inventors: Nand Lal Agarwal, Rahul Arunbhai Bhavsar, Kunal Kamleshbhai Pathak
  • Publication number: 20150148544
    Abstract: A compound of the general formula X—[NR—CO—Ar—CO—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; R represents a hydrogen atom or an alkyl, aryl or alkyl-aryl group; Ar represents an unsubstituted or substituted heteroaryl or aryl group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represents an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.
    Type: Application
    Filed: February 4, 2015
    Publication date: May 28, 2015
    Inventor: Antony Godwin
  • Publication number: 20150065392
    Abstract: A reactive mass label for labelling a biological molecule for detection by mass spectrometry includes the following structure: X-L-M-S-Re, wherein X is a mass marker moiety, L is a cleavable linker, M is a mass normalization moiety, and S is a mass series modifying group including the following group: wherein J is C?O, K is NH, and n is 2 or J and K are both CH2 and n is 1, m is at least 1; and Re is a reactive functionality for attaching the reactive mass label to a biological molecule.
    Type: Application
    Filed: September 15, 2014
    Publication date: March 5, 2015
    Applicant: Electrophoretics Limited
    Inventors: Christian Baumann, Stefan Kienle, Karsten Kuhn, Harald Legner
  • 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
  • Patent number: 8895551
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent 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 2, 2010
    Date of Patent: November 25, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20140336378
    Abstract: Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventor: Doo Hyun Lee
  • Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Publication number: 20140179665
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • 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
  • Publication number: 20140011996
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
    Type: Application
    Filed: August 29, 2013
    Publication date: January 9, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, MIchael Edward Grimwood, Jason Tan, Yuanxi Zhou
  • Publication number: 20140011845
    Abstract: Disclosed are cyclic dione derivatives represented by formula (I), wherein the substituents are as defined in the description. The preparation method, intermediate and use thereof are also provided.
    Type: Application
    Filed: December 30, 2011
    Publication date: January 9, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Stephane Andre Marie Jeanmart, Long Lu, Yaming Wu, Lisheng Mao, Michel Muehlbeach
  • Publication number: 20130303757
    Abstract: One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.
    Type: Application
    Filed: February 25, 2013
    Publication date: November 14, 2013
    Inventors: Duncan H. HUNTER, Mustafa JANABI
  • Patent number: 8541586
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: September 24, 2013
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20130225825
    Abstract: This invention is directed to processes for the preparation of a compound of the formula I or salt thereof, that is useful as a tryptase inhibitor, to intermediates useful in the preparation of such a compound, to processes for the preparation of such intermediates, and to the use of such intermediates for the preparation of such a compound.
    Type: Application
    Filed: April 11, 2013
    Publication date: August 29, 2013
    Applicant: Sanofi-Aventis Deutschland GmbH
    Inventor: Sanofi-Aventis Deutschland GmbH
  • Patent number: 8415354
    Abstract: The present invention relates to inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: April 9, 2013
    Assignee: Abbott Laboratories
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, James T. Link, Yixian Chen, Hwan-soo Jae, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Qi Shuai, Bryan K. Sorensen, Martin Winn, Dariusz Wodka, Hong Yong
  • Publication number: 20130079514
    Abstract: (R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclear leukocytes and monocytes at inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use as inhibitors of chemotaxis of neutrophils and monocytes induced by the C5a fraction of complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of polymorphonuclear leukocytes.
    Type: Application
    Filed: October 15, 2012
    Publication date: March 28, 2013
    Applicant: Dompé S.p.A.
    Inventor: Dompé S.p.A.
  • Patent number: 8372841
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: February 12, 2013
    Assignee: Abbott Laboratories
    Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
  • Publication number: 20120283137
    Abstract: A reactive mass label for labelling a biological molecule for detection by mass spectrometry, which label comprises a reactive functionality for labelling thiol groups or carbonyl groups. Also provided is a reactive mass label for labelling a biological molecule for detection by mass spectrometry, wherein the mass label comprises the following structure: X-L-M-S-Re wherein X is a mass marker moiety, L is a cleavable linker, M is a mass normalization moiety, S is a mass series modifying group comprising the following group: wherein J is C?O, K is NH, and n is 2 or J and K are both CH2 and n is 1, and wherein m is at least 1; and Re is a reactive functionality for attaching the mass label to a biological molecule.
    Type: Application
    Filed: September 8, 2010
    Publication date: November 8, 2012
    Applicant: ELECTROPHORETICS LIMITED
    Inventors: Christian Baumann, Stefan Kienle, Karsten Kuhn, Harald Legner
  • Publication number: 20120283445
    Abstract: The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: June 27, 2012
    Publication date: November 8, 2012
    Applicant: SANOFI
    Inventors: Yong Mi CHOI-SLEDESKI, Nakyen CHOY, Gregory Bernard POLI, John J. SHAY, JR., Patrick Wai-Kwok SHUM, Adam W. SLEDESKI
  • Publication number: 20120271049
    Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.
    Type: Application
    Filed: June 28, 2012
    Publication date: October 25, 2012
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Gerhard Hamprecht, Michael Puhl, Bernd Wolf, Norbert Götz, Michael Keil, Robert Reinhard, Ingo Sagasser, Werner Seitz
  • Publication number: 20120226033
    Abstract: The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I) below: and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 6, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Laurence Clary, Jean-Claude Pascal
  • Patent number: 8258304
    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: January 9, 2009
    Date of Patent: September 4, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Walter Maria Roevens
  • Publication number: 20120156180
    Abstract: Provided are compositions and methods for the treatment of Krabbe and other neurodegenerative diseases, including storage diseases such as GM1 gangliosidosis, Niemann-Pick disease, Tay-Sachs disease, Sandhoff disease, metachromatic leukodystrophy, Canavan disease, Pelizaeus-Merzbacher disease, and storage conditions facilitated by aging of lysosomal functions, which are associated with psychosine (and/or other storage material)-mediated axonal degeneration.
    Type: Application
    Filed: August 10, 2010
    Publication date: June 21, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventor: Ernesto Bongarzone
  • 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
  • Publication number: 20120022069
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent 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: Application
    Filed: April 2, 2010
    Publication date: January 26, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20110306603
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: August 23, 2011
    Publication date: December 15, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Publication number: 20110275670
    Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
    Type: Application
    Filed: June 4, 2009
    Publication date: November 10, 2011
    Inventors: Emma Chapman, Michael Higginbottom, Anne Viet-Anh Horgan (nee Nguyen), Iain Simpson
  • Publication number: 20110263651
    Abstract: The present invention relates to novel piperidine-4-butyramide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: November 19, 2009
    Publication date: October 27, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Tino Dyhring, Elsebet Østergaard Nielsen
  • Patent number: 8039656
    Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Grant
    Filed: March 21, 2005
    Date of Patent: October 18, 2011
    Inventors: Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
  • Publication number: 20110218217
    Abstract: This invention relates to novel piperidine-4-propionamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: August 25, 2009
    Publication date: September 8, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
  • Patent number: 8008305
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20110172174
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: October 31, 2007
    Publication date: July 14, 2011
    Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Patent number: 7968577
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: June 28, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
  • Patent number: 7968707
    Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: June 28, 2011
    Assignee: Abbott Laboratories
    Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
  • Publication number: 20110144108
    Abstract: Novel 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: Application
    Filed: January 17, 2011
    Publication date: June 16, 2011
    Applicant: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec
  • Patent number: 7947714
    Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Grant
    Filed: October 27, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: David Hallett, Craig W. Lindsley, Elizabeth M. Naylor, Zhijian Zhao, Cory R. Theberge, Scott E. Wolkenberg, M. Brad Nolt
  • Publication number: 20110105485
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: July 21, 2010
    Publication date: May 5, 2011
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Patent number: 7897777
    Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride which includes (i) resolving a racemic mixture of racemic threo-methylphenidate hydrochloride with a less than stoichiometric amount of tertiary amine base to obtain a methylphenidate-chiral acid salt, (ii) basifying the methylphenidate-chiral acid salt to obtain methylphenidate free base, and (iii) converting the methylphenidate free base into d-threo-methylphenidate hydrochloride.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: March 1, 2011
    Assignee: Archimica, Inc.
    Inventors: Alexei Kalinin, Guofang Qiu, Thomas J. Marren, James E. Aldred, Jr., Yu Ji
  • Publication number: 20110046106
    Abstract: The present invention relates to compounds of general formula I wherein A, B, R1, R2 and R3 are defined as in claim 1, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Application
    Filed: February 5, 2009
    Publication date: February 24, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Patent number: 7884102
    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: April 28, 2008
    Date of Patent: February 8, 2011
    Assignee: Adolor Corporation
    Inventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
  • Patent number: 7880001
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: February 1, 2011
    Assignee: Abbott Laboratories
    Inventors: James T. Link, Yixian Chen, Hwan-Soo Jae, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Qi Shuai, Bryan K. Sorensen, Martin Winn, Dariusz Wodka, Hong Yong
  • Patent number: 7872028
    Abstract: Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated. levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: January 18, 2011
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty
  • Publication number: 20110003856
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: February 18, 2008
    Publication date: January 6, 2011
    Inventor: Soren Ebdrup
  • Publication number: 20100324025
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Patent number: 7718671
    Abstract: Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.
    Type: Grant
    Filed: July 8, 2004
    Date of Patent: May 18, 2010
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Avinash Phadke, Jesse Quinn, Junko Ohkanda, Andrew Thurkauf, Yiping Shen, Cuixian Liu, Dawei Chen, Shouming Li, Xiangzhu Wang
  • Publication number: 20100093801
    Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.
    Type: Application
    Filed: October 9, 2009
    Publication date: April 15, 2010
    Applicant: SK HOLDINGS CO., LTD.
    Inventors: Coo-Min Chung, Hyung-Jin Jun, Jin-Sung Kim, Hui-Ho Kim, Hye-Kyung Min, Yong-Gil Kim, Jong-Gil Choi, Hongwook Kim
  • Publication number: 20100063292
    Abstract: The present invention relates to an process for the preparation 2,5-bis(2,2,2-trifluoroethoxy)toluene [II]. The compound 2,5-bis(2,2,2-trifluoroethoxy)toluene is useful as intermediate for pharmaceutical industry, especially useful as an intermediate for the preparation of Flecainide and pharmaceutically acceptable salts.
    Type: Application
    Filed: November 2, 2007
    Publication date: March 11, 2010
    Applicant: Grindeks A Joint Stock Company
    Inventors: Daina Zicane, Janis Jaunbergs