Plural Nitrogens In Acid Moiety Patents (Class 560/13)
  • Patent number: 10369171
    Abstract: The present invention relates to methods for killing neoplastic cells, such as ras-activated cancerous cells, in vitro. In particular embodiments, an attenuated reovirus (e.g., a reovirus lacking a wild-type S1 gene) may be administered to a mixed cellular composition comprising cancerous cells and stem cells such as adult stem cells and/or hematopoietic stem cells; in these embodiments, the attenuated reovirus may result in killing of the cancerous cells with little or no damage to the healthy stem cells.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: August 6, 2019
    Assignee: VIROCURE, INC.
    Inventors: Manbok Kim, Derrick E. Rancourt, Nicole Zur Nieden, Randal N. Johnston
  • Patent number: 8993780
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140315954
    Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
  • Publication number: 20140315906
    Abstract: The present invention relates to 4-aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I) or (Ia).
    Type: Application
    Filed: May 21, 2012
    Publication date: October 23, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Lücking, Rolf Bohlmann, Arne Scholz, Gerhard Siemeister, Mark Jean Gnoth, Ulf Bömer, Dirk Kosemund, Philip Lienau, Gerd Rühter, Carsten Schultz-Fademrecht
  • Publication number: 20140286866
    Abstract: The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: GE HEALTHCARE AS
    Inventors: ALAN CUTHBERTSON, MAGNE SOLBAKKEN
  • Patent number: 8816120
    Abstract: The present invention provides a novel method for preparing compounds N-(4-nitro-2-sulfamoyl-phenyl)-malonamic acid methyl ester and N-(4-amino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, which are novel intermediates for preparing a key intermediate N-(4-methanesulfonylamino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, for the preparation of N-(3-{(1R,2S,7R,8S)-3-[(4-fluorophenyl)methyl]-6-hydroxy-4-oxo-3-azatricyclo[6.2.1.02,7]undec-5-en-5-yl}-1,1-dioxo-1,4-dihydro-1?6,2,4-benzothiadiazin-7-yl)methanesulfonamide, also known commercially as Setrobuvir, a compound useful in treating hepatitis C.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: August 26, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Jiang Zhu
  • Publication number: 20140200362
    Abstract: The present invention provides a novel method for preparing compounds N-(4-nitro-2-sulfamoyl-phenyl)-malonamic acid methyl ester and N-(4-amino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, which are novel intermediates for preparing a key intermediate N-(4-methanesulfonylamino-2-sulfamoyl-phenyl)-malonamic acid methyl ester, for the preparation of N-(3-{(1R,2S,7R,8S)-3-[(4-fluorophenyl)methyl]-6-hydroxy-4-oxo-3-azatricyclo [6.2.1.02,7]undec-5-en-5-yl}-1,1-dioxo-1,4-dihydro-1?6,2,4-benzothiadiazin-7-yl)methanesulfonamide, also known commercially as Setrobuvir, a compound useful in treating hepatitis C.
    Type: Application
    Filed: January 13, 2014
    Publication date: July 17, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Jiang Zhu
  • Patent number: 8742158
    Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: June 3, 2014
    Assignee: TaiMed Biologies, Inc.
    Inventors: Brent R. Stranix, Jean-Francois Lavallee, Nicolas Leberre, Valerie Perron, Dominik Herbart, Guy Milot, Chandra Panchal
  • Publication number: 20140121211
    Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogues, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 1, 2014
    Applicant: INDIAN INSTITUTE OF SCIENCE EDUCATION AND RESEARCH -PUNE
    Inventors: Harinath CHAKRAPANI, Satish Ramesh Malwal
  • Publication number: 20140094614
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 3, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140066504
    Abstract: Novel analogs and prodrugs of the loop diuretic bumetanide are described. Pharmaceutical compositions containing bumetanide analogs and prodrugs are also described. These analogs and prodrugs are particularly useful for the treatment and/or prophylaxis of conditions that involve the NKCC cotransporter family (NKCC1 and NKCC2), or the KCC cotransporter family (KCC1, KCC2, KCC3, KCC4), or GABAa receptors. Such conditions include, but are not limited to anxiety disorders, epilepsy, migraine, non-epileptic seizures, sleep disorders, obesity, eating disorders, autism, depression, edema, glaucoma, stroke, ischemia, neuropathic pain, addictive disorders, schizophrenia, psychosis, and tinnitus.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 6, 2014
    Inventor: Daryl W. HOCHMAN
  • Patent number: 8658803
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: February 25, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140018325
    Abstract: Compounds of Formula I are disclosed wherein R1, R2, R3A, R3B, R4A, R4B, R5A, R5B, R6A, R6B, R8 and R9 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Michael John Boyd, Carmela Molinaro, Amelia Roy, Vouy Linh Truong
  • Patent number: 8609881
    Abstract: The present invention provides compound(s) selected from the group of compounds represented by structural Formula (I): wherein X, Y and R1 are as described herein, use of such compounds as anaerobic cure accelerators, and compostions including such compounds.
    Type: Grant
    Filed: May 7, 2008
    Date of Patent: December 17, 2013
    Assignee: Henkel IP US LCC
    Inventors: Andrew Messana, Anthony F. Jacobine, Steven Thomas Nakos, David M. Glaser
  • Publication number: 20130308219
    Abstract: The present invention relates to a polymerizable composition comprising at least one ethylenically unsaturated, polymerizable compound and at least one oxime sulfonate compound of the formula (I) QAaBbCc where a is 0, 1, 2, 3, 4 or 6, b is 0, 1, 2, 3, 4 or 6, and c is 0, 1, 2, 3, 4 or 6, where the sum of a+b+c is 1, 2, 3, 4 or 6 where (A) is a group (B) is a group (C) is a group where # denotes the point of attachment to Q; X is S or NR14 and Q, R1, R2, R3 and R14 are as defined in claim 1 and in the description. The present invention also relates to the use of the this composition, to novel oxime sulfonates and the use of the oxime sulfonates as thermal curing promoter.
    Type: Application
    Filed: January 27, 2012
    Publication date: November 21, 2013
    Applicant: BASF SE
    Inventors: Kazuhiko Kunimoto, Kaori Sameshima, Yuki Matsuoka, Hisatoshi Kura
  • Patent number: 8546602
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and compounds used to synthesize the compounds of Formula I.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: October 1, 2013
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera, Fritz Blatter, Martin Viertelhaus
  • Publication number: 20130237702
    Abstract: A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.
    Type: Application
    Filed: August 31, 2012
    Publication date: September 12, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masayuki SUGIKI, Toru OKAMATSU, Tetsuo YANO, Shinya TANIGUCHI
  • Publication number: 20130230458
    Abstract: The invention provides compositions and methods for treating cell cycle disorders. Compositions of the invention include proTAME, a prodrug analog of TAME, and, optionally, one or more therapeutic agents.
    Type: Application
    Filed: September 1, 2011
    Publication date: September 5, 2013
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Randall King, Xing Zeng
  • Publication number: 20130225621
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 2, 2011
    Publication date: August 29, 2013
    Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Patrick Gunning
  • Patent number: 8445291
    Abstract: Provide is a method for detecting a target substance, which method can visualize the expression of the target substance at any time point while reducing influences on the functions of the target substance, can use fluorescent dyes having various excitation/emission wavelengths, and can achieve easy staining process. Also provided are a tag, a DNA, a vector, a probe and a detection kit suitable for use in the above-described detection method. Specifically, the method for detecting a target substance, comprises the steps of bringing into contact with each other (a) a tag comprising a polypeptide forming an ?-helix structure, the tag bound to the target substance, and (b) a probe comprising a compound bound to a fluorescent dye; and measuring the fluorescence emitted by the fluorescent dye. The binding of the tag ?-helix structure to the probe compound induces a spectral change in the fluorescence emitted by the fluorescent dye.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: May 21, 2013
    Assignee: National University Corporation Tokyo Medical and Dental University
    Inventors: Hirokazu Tamamura, Hiroshi Tsutsumi
  • Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Publication number: 20130109866
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: October 23, 2012
    Publication date: May 2, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130096127
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 29, 2012
    Publication date: April 18, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Patent number: 8410300
    Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3 -pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO—, R2a being selected from the group consisting of piperonyl, 2-pyrazinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
    Type: Grant
    Filed: September 20, 2007
    Date of Patent: April 2, 2013
    Assignee: TaiMed Biologics, Inc.
    Inventors: Brent Richard Stranix, Jean-Francois Lavallee, Nicolas LeBerre, Valerie Perron, Dominik Herbart, Guy Milot, Chandra Panchal
  • Publication number: 20130017603
    Abstract: Compounds having an excellent CaSR agonist activity are in demand. The invention provides glutamate derivatives or salts thereof, pharmaceutical compositions comprising the glutamate derivatives, preventive or therapeutic agents for diarrhea, hyperparathyroidism or peptic ulcer.
    Type: Application
    Filed: September 21, 2012
    Publication date: January 17, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventor: AJINOMOTO CO., INC.
  • Publication number: 20120302744
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and compounds used to synthesize the compounds of Formula I.
    Type: Application
    Filed: August 6, 2012
    Publication date: November 29, 2012
    Applicant: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera, Fritz Blatter, Martin Viertelhaus
  • Publication number: 20120269804
    Abstract: The present invention relates to substituted benzosulphonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 7, 2010
    Publication date: October 25, 2012
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Marion Hitchcock, Ingo Hartung, Florian Pühler
  • Publication number: 20120258935
    Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed
    Type: Application
    Filed: February 21, 2012
    Publication date: October 11, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard P. Polniaszek, Richard Hung Chiu Yu
  • Publication number: 20120234721
    Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.
    Type: Application
    Filed: September 9, 2011
    Publication date: September 20, 2012
    Applicant: Neurotherapeutics Pharma, Inc.
    Inventors: Daryl W. HOCHMAN, John J. Partridge
  • Patent number: 8268885
    Abstract: The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: September 18, 2012
    Assignee: Janssen R&D Ireland
    Inventors: Koenraad Lodewijk August Van Acker, Piet Tom Bert Paul Wigerinck, Lieve Emma Jan Michiels, Abdellah Tahri
  • Publication number: 20120232104
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Publication number: 20120220785
    Abstract: The invention relates to polysultone derivatives used as precursors to radiolabelled macromolecules usable for medicine and in nuclear imaging. The aim of the invention is to provide novel prosthetic compounds or groupings, the synthesis of which is straightforward, easy and automatable, enabling access to economical and effective radiolabelled macromolecules. The aim is achieved by the invention, which involves compounds of formula 10 or 11. Said double-sultone derivatives are produced by opening the sultone rings using a nucleophile radical Ri which may be a radionucleide R* for one of the sultone rings and an active radical peptide Ra for the other sultone ring. The invention also relates to the method for producing the abovementioned compounds, as well as to the drugs or diagnosis products that the latter are capable of forming.
    Type: Application
    Filed: August 10, 2010
    Publication date: August 30, 2012
    Applicant: Advanced Accelerator Applications
    Inventor: Cedric Bouteiller
  • Publication number: 20120208790
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 16, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Patent number: 8242118
    Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: August 14, 2012
    Assignee: Axikin Pharmaceuticals Inc.
    Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
  • Publication number: 20120115948
    Abstract: The invention provides an anti-proliferative composition comprising a non-peptide analog of the C-terminal isoleucine-arginine (IR) tail motif of an activator of an anaphase promoting complex (APC). The invention further provides methods of inhibing the ubiquitination activity of the APC by administering compositions of the invention.
    Type: Application
    Filed: March 8, 2010
    Publication date: May 10, 2012
    Inventors: Randall King, Xing Zeng, Shantanu Gaur
  • Publication number: 20120059055
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: November 15, 2011
    Publication date: March 8, 2012
    Applicant: PANMIRA PHARMACEUTICALS, LLC
    Inventors: John Howard HUTCHINSON, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang
  • Publication number: 20120052488
    Abstract: Compositions, devices, systems and methods for reducing and/or preventing photo-induced damage of one or more reactants in an illuminated analytical reaction by addition of one or more photoprotective compounds to the reaction mixture and allowing the reaction to proceed for a period that is less than a photo-induced damage threshold period.
    Type: Application
    Filed: August 11, 2011
    Publication date: March 1, 2012
    Applicant: Pacific Biosciences of California, Inc.
    Inventors: Stephen Yue, Robert Weber, Xiangxu Kong, Andrei Fedorov, John Lyle
  • Publication number: 20120041196
    Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
    Type: Application
    Filed: September 30, 2011
    Publication date: February 16, 2012
    Applicant: CEPHALON, INC.
    Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassará, Sankar Chatterjee, Germano D'Arasmo, Sergio De Munari, Edmondo Ferretti, Mohamed Iqbal, Ernesto Menta, Patricia A. Messina McLaughlin, Ambrogio Oliva
  • Publication number: 20110319438
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: September 7, 2011
    Publication date: December 29, 2011
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Patent number: 8071650
    Abstract: The present invention relates to novel thiourea derivatives as a modulator for vanilloid receptor (VR) and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: December 6, 2011
    Assignee: Pacific Corporation
    Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
  • Publication number: 20110275619
    Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 10, 2011
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Arun K. Ghosh
  • Publication number: 20110212918
    Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.
    Type: Application
    Filed: November 11, 2010
    Publication date: September 1, 2011
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Vincent S. Hernandez, Xianfeng Li, Suoming Zhang, Tsutomu Akama, Yanchen Zhang, Yang Liu, Jacob J. Plattner, Michael Richard Kevin Alley, Yasheen Zhou, James A. Nieman
  • Patent number: 8008297
    Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: August 30, 2011
    Assignee: Ambrilia Biopharma Inc.
    Inventors: Brent Richard Stranix, Valerie Perron
  • Publication number: 20110190529
    Abstract: The present invention relates to the compound of formula (I) and to the use thereof as an intermediate for the synthesis of the compound of formula (A) or pharmaceutically acceptable salts thereof: formulae (II).
    Type: Application
    Filed: August 18, 2009
    Publication date: August 4, 2011
    Applicant: SANOFI-AVENTIS
    Inventor: Jose Ruiz-Montes
  • Publication number: 20110152522
    Abstract: The present invention relates to a process for preparing 3-phenyl(thio)uracils and -dithiouracils of the formula I where the variables are each as defined in the description, and also intermediates for their preparation.
    Type: Application
    Filed: March 4, 2011
    Publication date: June 23, 2011
    Applicant: BASF Aktiengesselschaft
    Inventors: Sandra Löhr, Joachim Gebhardt, Guido Mayer, Michael Keil, Thomas Schmidt, Bernd Wolf
  • Publication number: 20110136827
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20110130453
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: March 25, 2009
    Publication date: June 2, 2011
    Applicant: AMIRA PHARMACEUTICALS, INC.
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Yen Pham Truong, Thomas Jon Seiders
  • 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
  • Publication number: 20110065631
    Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.
    Type: Application
    Filed: March 29, 2007
    Publication date: March 17, 2011
    Applicant: Gilead Sciences, Inc
    Inventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard Polniaszek, Richard H. Yu
  • Patent number: RE43596
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: August 21, 2012
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw