Hetero Ring Is Five-membered Consisting Of One Nitrogen And Four Carbons (e.g., Halopyrrolidines, Etc.) Patents (Class 548/400)
  • Patent number: 7750166
    Abstract: The present invention relates to novel ionic liquids comprising a docusate, docusate variant, or other sulfonate anion. The ionic liquids may be conveniently made via, for example, metathesis. The ionic liquids are often hydrophobic and useful in many hydrocarbon compositions, polymer compositions, and in supercritical carbon dioxide applications. The ionic liquids are capable of hindering static electricity buildup in the hydrocarbon compositions and can therefore minimize flammability and/or explosiveness.
    Type: Grant
    Filed: August 15, 2003
    Date of Patent: July 6, 2010
    Assignees: University of South Alabama, Sachem, Inc.
    Inventors: Roger Moulton, James H. Davis, Jr.
  • Patent number: 7741357
    Abstract: Reaction of nordihydroguaiaretic acid with various alkyl chlorides, 1-piperidinecarbonyl chloride, methyl chloroformate, or 1,1?-carbonyldiimidazole under alkaline conditions produced the corresponding phenol ethers, carbamates and carbonates, respectively, in 67-83% yields (Scheme 1 and Scheme 2). Among these derivatives, the nitrogen-containing compounds were converted to the corresponding hydrochloride salts. Having good solubility, these NDGA derivatives were found to be stable in aqueous solution. These new compounds exerted potent activities against HIV Tat-regulated transactivation in cos-7 cells. The most active transcription inhibitor compound of this series 5b (P4N, Tetrapiperidino NDGA, meso-2,3-dimethyl-1,4-bis(3,4-[2-(piperidino)ethoxyphenyl])butane tetrakishydrochloride salt) has an IC50 of 0.88 ?M.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: June 22, 2010
    Assignee: Johns Hopkins University
    Inventors: Ru Chih C. Huang, Apostolos Gittis, Evangelos Moudrianakis, Julie A. Dohm, Jih Ru Hwu, Ming-Hua Hsu
  • Patent number: 7736396
    Abstract: Provided is a hair dyeing composition, containing a first part containing (a) a nitrogen-containing compound expressed by the general formula (1) or a salt thereof and a second part containing a component (b) of an oxidizing agent, wherein a pH upon use is 7.5 to 12, wherein R1 and R3 to R5 represent H, a hydroxy group, and an alkyl group with C12 or less optionally having a substituent, R2 represents a hydroxy group, —R or —OR, in which R means the same as R3 to R5, and two or more of R1 to R5 may be taken together to form a 3 to 8 membered-ring optionally having a substituent.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: June 15, 2010
    Assignee: Kao Corporation
    Inventors: Masaki Fukuhara, Takafumi Nishi, Yasuyuki Fujii
  • Patent number: 7737241
    Abstract: The invention is a system for initiating free radical polymerization comprising: a) in one part, one or more amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms and optionally containing one or more heteroatoms or heteroatom containing functional moieties, and one or more cationic counter ions and b) in a second part, a liberating compound which reacts with the nitrogen atom(s) bound to the boron atom(s) upon contact with the amido-borate to form an organoborane radical.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: June 15, 2010
    Assignee: Dow Global Technologies Inc.
    Inventors: Shaoguang Feng, Gary L. Jialanella, Peter Nickias, Toni Ristoski
  • Patent number: 7728148
    Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 6, 2007
    Date of Patent: June 1, 2010
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Ying Sun, Yat Sun Or, Zhe Wang
  • Publication number: 20100130749
    Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren Inter alia the invention relates to a process for the manufacture of a compound of the formula I. or a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.
    Type: Application
    Filed: April 1, 2008
    Publication date: May 27, 2010
    Inventor: Gottfried Sedelmeier
  • Patent number: 7723530
    Abstract: The present invention relates to the use of polymerisable diketopyrrolopyrroles in colour filters, which can themselves be used for example in electro-optical systems such as TV screens, liquid crystal displays, charge coupled devices, plasma displays or electroluminescent displays and the like. In contrast to conventional pigments the polymerisable diketopyrrolopyrroles do not tend to aggregate and, hence, show very good dispersibility. Color filters prepared by using the polymerisable diketopyrrolopyrroles have high transparence and pure hue. In addition, they facilitate adjustment of color points and enable a large choice of shades.
    Type: Grant
    Filed: January 3, 2008
    Date of Patent: May 25, 2010
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Jean-Marie Adam, Gerardus De Keyzer
  • Patent number: 7718683
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: May 18, 2010
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M. K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
  • Patent number: 7714012
    Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: May 11, 2010
    Assignee: Trustees of Dartmouth University
    Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
  • Publication number: 20100105753
    Abstract: One aspect of the present invention relates to synthetic peptide derivatives that inhibit fibroblast activation protein ? (FAP) activity. Another aspect of the invention relates to methods for treating a mammal suffering from cancer by administering a therapeutically effective amount of synthetic peptides derivatives that inhibit FAP activity.
    Type: Application
    Filed: March 20, 2008
    Publication date: April 29, 2010
    Applicant: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-Sen Lai
  • Patent number: 7692028
    Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: April 6, 2010
    Assignee: UCB Pharma, S.A.
    Inventors: Edmond Differding, Benoît Kenda, Bénédicte Lallemand, Alain Matagne, Philippe Michel, Patrick Pasau, Patrice Talaga
  • Publication number: 20100076034
    Abstract: The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.
    Type: Application
    Filed: December 18, 2007
    Publication date: March 25, 2010
    Applicant: DOMPE PHA.R.MA S.P.A.
    Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta
  • Patent number: 7683097
    Abstract: The present invention provides compounds that are effective against inhibiting topoisomerase (i.e., topoisomerase I and/or topoisomerase II). These compounds are used for treating cell-proliferative disorders. In some instances, these compounds have anticancer activity, e.g., against multi-drug resistant cancers.
    Type: Grant
    Filed: May 25, 2005
    Date of Patent: March 23, 2010
    Assignee: Propharmacon Inc.
    Inventors: Martin A. Murphy, John Robert Schullek, John S. Ward, Gary C. Look, Brian Siesel
  • Patent number: 7678818
    Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 19, 2007
    Date of Patent: March 16, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
  • Patent number: 7674807
    Abstract: Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: March 9, 2010
    Assignee: Bayer CropScience AG
    Inventors: Katsuaki Wada, Takuya Gombuchi, Yasushi Yoneta, Yuichi Otsu, Katsuhiko Shibuya, Norihiko Nakakura, Rüdiger Fischer, Tetsuya Murata, Eiichi Shimojo
  • Publication number: 20100048549
    Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein A, D, E, J, Q1 R1, R2, R3, p and j are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes sst1 and/or sst4 and can be used for the treatment or diagnosis of diseases or conditions wherein sst1 and/or sst4 agonists or antagonists are indicated to be useful.
    Type: Application
    Filed: May 16, 2006
    Publication date: February 25, 2010
    Inventors: Jussi Tomperi, Harri Salo, Oili Kallatsa, Pia Knuuttila, Päivi Laakso, Iisa Höglund, Anna-Marja Hoffrén, Kurt Kokko, Pauli Saarenketo, Mia Engström, Siegfried Wurster
  • Patent number: 7659299
    Abstract: Use of an agent capable of inhibiting SAP ligand binding activity or depleting SAP from the plasma of a subject for the production of a medicament for treatment or prevention of osteoarthritis in the subject.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: February 9, 2010
    Assignee: Pentraxin Therapeutics Limited
    Inventors: Mark B. Pepys, Philip Nigel Hawkins
  • Publication number: 20100029639
    Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.
    Type: Application
    Filed: April 15, 2009
    Publication date: February 4, 2010
    Applicant: CARDIOME PHARMA CORP.
    Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M. C. Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
  • Patent number: 7622491
    Abstract: The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulinemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity and eating disorders.
    Type: Grant
    Filed: August 11, 2005
    Date of Patent: November 24, 2009
    Assignee: Metabolex Inc.
    Inventors: Yan Zhu, Jingyuan Ma, Peng Cheng, Zuchun Zhao, Francine M. Gregoire, Vera A. Rakhmanova
  • Patent number: 7615645
    Abstract: The invention relates to a method for the continuous production of aldehydes by the isomerising hydroformylation in a homogenous phase of olefin compositions by means of a synthesis gas, in the presence of a homogeneous rhodium catalyst that is complexed with an organophosphorus ligand containing oxygen atoms and/or nitrogen atoms and a free ligand. The production is carried out at high temperature and high pressure in a multi-stage reaction system consisting of at least two reaction zones. According to the method, the olefin composition is first reacted in a first reaction zone or a group of several first reaction zones at a total pressure of between 10 and 40 bar, using a synthesis gas with a CO/H2 molar ratio of between 4:1 and 1:2 until a 40 to 95% conversion of the ?-olefins is obtained.
    Type: Grant
    Filed: October 14, 2004
    Date of Patent: November 10, 2009
    Assignee: BASF Aktiengesellschaft
    Inventors: Martin Volland, Thomas Mackewitz, Wolfgang Ahlers, Ansgar Schäfer, Wolfgang Richter, Rocco Paciello
  • Patent number: 7612213
    Abstract: A compound represented by the general formula (I): (I) wherein R represents linear, branched, or cyclic alkyl or aryl; a process for producing the compound; and an antitumor agent containing the compound as an active ingredient.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: November 3, 2009
    Assignee: Riken
    Inventors: Hiroyuki Osada, Hideaki Kakeya, Yujiro Hayashi
  • Patent number: 7605176
    Abstract: Compounds of formula I wherein the groups and residues A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one amide according to the invention. As a result of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes.
    Type: Grant
    Filed: March 3, 2005
    Date of Patent: October 20, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Philipp Lustenberger, Dirk Stenkamp, Stephan Georg Mueller, Thorsten Lehmann-Lintz, Marcus Schindler, Leo Thomas, Ralf R. H. Lotz, Marco Santagostino
  • Publication number: 20090253671
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Application
    Filed: March 2, 2006
    Publication date: October 8, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Shanta Bist, Sheila Irene Hauck, Kenneth Gregory Hull
  • Patent number: 7598395
    Abstract: The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, provided that the ring is not 1,2,3-triazole, the ring being substituted by groups R8, R9 and R10; X is a single or double bond; Y is O, S, N(R11) or (CR12R13)(CR14R15)m(CR16R17)n; m is 0 or 1; n is 0 or 1; and R1 to R17 each, independently, have a range of values; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: October 6, 2009
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Josef Ehrenfreund, Hans Tobler, Harald Walter
  • Patent number: 7589119
    Abstract: This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.
    Type: Grant
    Filed: February 22, 2008
    Date of Patent: September 15, 2009
    Assignee: Signal Pharmaceutical, LLC
    Inventors: Glenn Friedman, Jeffrey McKie, Jonathan Wright, Sophie Perrin-Ninkovic, Bernd M. Stein
  • Publication number: 20090220407
    Abstract: Disclosed are methods for forming carbon nano-onions. The methods include annealing a carbon nanodiamond starting material in an inert atmosphere. The method can be carried out at ambient pressure. Also disclosed are methods for functionalizing carbon nano-onions. For instance, carbon nano-onions can be functionalized so as to be soluble in aqueous or organic solvents, as desired. Also disclosed are methods for separating mixtures of carbon nano-onions. In particular, mixtures of carbon nano-onions can be separated from one another based upon differences in electrochemical characteristics of the different nano-onions.
    Type: Application
    Filed: August 15, 2006
    Publication date: September 3, 2009
    Inventors: Luis Echegoyen, Amit J. Palkar, Arno S. Rettenbacher, Frederic Melin, Bevan Elliot
  • Patent number: 7582124
    Abstract: Provided is a hair dyeing composition, containing a first part containing (a) a nitrogen-containing compound expressed by the general formula (1) or a salt thereof and a second part containing a component (b) of an oxidizing agent, wherein a pH upon use is 7.5 to 12, wherein n=1 or 2, R1 and R3 to R5 represent H, a hydroxy group, and an alkyl group with C12 or less optionally having a substituent, R2 represents a hydroxy group, —R or —OR, in which R means the same as R1 to R5, and two or more of R1 to R5 may be taken together to form a 3 to 8 membered-ring optionally having a substituent.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: September 1, 2009
    Assignee: Kao Corporation
    Inventors: Masaki Fukuhara, Takafumi Nishi, Yasuyuki Fujii
  • Patent number: 7582770
    Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.
    Type: Grant
    Filed: February 18, 2005
    Date of Patent: September 1, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
  • Patent number: 7572817
    Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: August 11, 2009
    Assignee: AstraZeneca AB
    Inventor: Magnus Polla
  • Patent number: 7569079
    Abstract: The present disclosure relates to polycationic monochromophoric hydrazone compounds of following formula (I): wherein W1 is a heteroaromatic radical comprising 5 or 6 ring members, optionally condensed with an aromatic ring comprising 6 ring members, comprising a quaternized nitrogen atom and optionally another heteroatom which may or may not be identical to nitrogen; X, which may or may not be identical, is a nitrogen atom or a CR2 group; Z is a cationic group comprising at least one quaternized nitrogen atom. 1The present disclosure also relates to a composition for dyeing human keratin fibers comprising the polycationic compounds disclosed herein, and to a dyeing process using the composition of the present disclosure, and ever further to multicompartment device.
    Type: Grant
    Filed: April 14, 2008
    Date of Patent: August 4, 2009
    Assignee: L'Oreal S.A.
    Inventors: Hervé David, Nadège Murguet
  • Patent number: 7553864
    Abstract: This invention relates to compounds of the Formulae (I)-(IX): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.
    Type: Grant
    Filed: November 29, 2006
    Date of Patent: June 30, 2009
    Assignee: Schering Corporation
    Inventors: M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga Adulla P. Reddy, Vincent S. Madison
  • Patent number: 7553977
    Abstract: A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the group consisting of dialkyl phosphono, diaryl phosphono, and dialkylaryl phosphono. Additional methods, intermediates and products are also described.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: June 30, 2009
    Assignees: North Carolina State University, ZettaCore, Inc.
    Inventors: Jonathan S. Lindsey, Robert S. Loewe, Kannan Muthukumaran, Arounaguiry Ambroise
  • Patent number: 7550491
    Abstract: The present invention relates to salts comprising bis(trifluoromethyl)imide anions and saturated, partially or fully unsaturated, heterocyclic cations, to a process for the preparation thereof, and to the use thereof as ionic liquids.
    Type: Grant
    Filed: November 17, 2003
    Date of Patent: June 23, 2009
    Assignee: Merck Patent GmbH
    Inventors: Nikolai Ignatyev, Urs Welz-Biermann, Michale Schmidt, Helge Willner, Andriy Kucheryna
  • Patent number: 7550604
    Abstract: Disclosed herein are novel pyrroloterpene compounds and methods for obtaining these compounds. Also disclosed are methods of treating cancer and bacterial infections using the novel pyrroloterpene compounds.
    Type: Grant
    Filed: August 17, 2005
    Date of Patent: June 23, 2009
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventor: Venkata Rami Reddy Macherla
  • Patent number: 7550499
    Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
    Type: Grant
    Filed: May 10, 2005
    Date of Patent: June 23, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Tuerdi, Hannguang J. Chao, Jennifer X. Qiao, Tammy C. Wang, Timur Gungor
  • Patent number: 7528264
    Abstract: Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: May 5, 2009
    Assignee: The Procter & Gamble Company
    Inventors: Michael Patrick Hayes, Tammy Talbot Schunk
  • Patent number: 7528261
    Abstract: A small molecule compound including at least one type of an optionally substituted indolocarbazole moiety and at least one divalent linkage.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: May 5, 2009
    Assignee: Xerox Corporation
    Inventors: Yuning Li, Beng S Ong, Yiliang Wu, Ping Liu
  • Patent number: 7517990
    Abstract: The present invention relates to a method for deuteration of a heterocyclic ring, which comprises subjecting a compound having a heterocyclic ring to sealed refluxing state in a deuterated solvent in the presence of an activated catalyst selected form a palladium catalyst, a platinum catalyst, a rhodium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst. In accordance with a method of the present invention, a hydrogen atom belonging to a heterocyclic ring of a compound having a heterocyclic ring can be very efficiently deuterated because temperature of deuteration reaction can be maintained at higher than boiling point of the solvent. Further, a method for deuteration of the present invention can be applied widely to deuteration of various compounds having a heterocyclic ring which are liable to decomposition under supercritical conditions or acidic conditions, leading to industrial and efficient deuteration of a compound having a heterocyclic ring.
    Type: Grant
    Filed: November 7, 2003
    Date of Patent: April 14, 2009
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Nobuhiro Ito, Tsuneaki Maesawa, Kazushige Muto, Kosaku Hirota, Hironao Sajiki
  • Patent number: 7514431
    Abstract: The present invention is directed to compounds of the formula I: I (wherein R1, R2, R3, R4, R5, R6, X, Z and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: April 7, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Changyou Zhou, Alexander Pasternak, Lihu Yang
  • Patent number: 7511070
    Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.
    Type: Grant
    Filed: November 9, 2005
    Date of Patent: March 31, 2009
    Assignee: Poniard Pharmaceuticals, Inc.
    Inventors: David J. Grainger, James C. Metcalfe, Sudhakar Kasina
  • Patent number: 7510700
    Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: March 31, 2009
    Assignee: Mallinckrodt Inc
    Inventors: Samuel Achilefu, Richard B. Dorshow, Raghavan Rajagopalan, Joseph B. Bugaj
  • Patent number: 7507700
    Abstract: This invention relates to organic catalysts comprising iminium or oxaziridinium moieties, cleaning compositions comprising such catalysts; and processes for making and using such catalysts and cleaning products.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: March 24, 2009
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, George Douglas Hiler, II, Susumu Murata, Rebecca Massie Grey
  • Patent number: 7504520
    Abstract: The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: March 17, 2009
    Assignee: Abbott Laboratories
    Inventors: Arthur Gomtsyan, Richard J. Perner, John R. Koenig, Margaret Chi-Ping Hsu, Dilinie P. Fernando, Chih-Hung Lee
  • Patent number: 7498447
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: March 3, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7498436
    Abstract: This present invention relates to prodrug compounds of the formula (Y) and pharmaceutical salts thereof: where RN, R1, R2, R3R4 and RC are defined herein, which are useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: March 3, 2009
    Assignees: Pharmacia & Upjohn Company LLC, Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Barbara Jagodzinska, Michel Maillard, James P. Beck, Ruth E. TenBrink, Daniel Getman
  • Patent number: 7498421
    Abstract: A pharmaceutical composition comprising a compound of formula (I) wherein X is an electron withdrawing group, Y1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R4, —CO2R4, —CONHR4 or —COR4, and each of R1, R2 and R4, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, or a compound of formula (II) wherein each of Y2 and Y3, which may be the same or different, is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R9, —CO2R9, —CONHR9 or —COR9, Z is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclyl, —CH?C(NHR10)CH((CH2)m CO2R11)(C?O)CH3 or —CH2(C?O)CH((CH2)mCO2R11)(C?O)CH3, R8 is —(CH2)nCO2R12, each of R5 to R7 and R9 to R12, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, and each of m and n, which may be the same or different, is 1 to 6 or a compound of formula (III) wherein each of Y4 to Y6, which may be the same or
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: March 3, 2009
    Assignee: Medical Research Council
    Inventors: Joseph Floyd Clark, Thomas Andrew Daniel Cadoux-Hudson, Christopher Joseph Schofield
  • Patent number: 7495111
    Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.
    Type: Grant
    Filed: June 15, 2006
    Date of Patent: February 24, 2009
    Assignee: Wyeth
    Inventors: P. Sivaramakrishnan Ramamoorthy, Zhongqi Shen, Boyd L. Harrison
  • Patent number: 7495112
    Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: February 24, 2009
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Patent number: 7491831
    Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: February 17, 2009
    Assignee: Plexxikon, Inc.
    Inventors: Dean R. Artis, Prabha N. Ibrahim, Jack Lin, Chao Zhang
  • Patent number: 7488468
    Abstract: A near infrared fluorescent contrast agent comprising a compound having three or more sulfonic acid groups in a molecule, and a method of fluorescence imaging comprising introducing the near infrared fluorescent contrast agent of the present invention into a living body, exposing the body to an excitation light, and detecting near infrared fluorescence from the contrast agent. The near infrared fluorescent contrast agent of the present invention is excited by an excitation light and emits near infrared fluorescence. This infrared fluorescence is superior in transmission through biological tissues. Thus, detection of lesions in the deep part of a living body has been made possible. In addition, the inventive contrast agent is superior in water solubility and low toxic, and therefore, it can be used safely.
    Type: Grant
    Filed: September 16, 1999
    Date of Patent: February 10, 2009
    Assignees: Schering AG, Fuji Photo Film Co., Ltd.
    Inventors: Naoto Miwa, Michihito Inagaki, Hiroaki Eguchi, Masafumi Okumura, Yoshio Inagaki, Toru Harada