Only Two Ring Oxygens In The Hetero Ring Which Is Not A Polycyclo Ring System (e.g., Dioxolane, Etc.) Patents (Class 514/467)
  • Publication number: 20090163576
    Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 and R4 together are alkyl having two or three carbon atoms; or R3 and R4 are the same as each other and each is methyl or ethyl; R5 is hydrogen or alkyl having from one to six carbon atoms.
    Type: Application
    Filed: May 11, 2007
    Publication date: June 25, 2009
    Applicant: WELLSTAT THERAPEUTICS CORPORATION
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Publication number: 20090163457
    Abstract: The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.
    Type: Application
    Filed: November 26, 2008
    Publication date: June 25, 2009
    Applicant: pSivida, Inc.
    Inventors: Paul Ashton, Jianbing Chen, Hong Guo, Grazyna Cynkowska, Tadeusz Cynkowski
  • Publication number: 20090163549
    Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.
    Type: Application
    Filed: December 13, 2006
    Publication date: June 25, 2009
    Inventor: Hiroyuki Kai
  • Publication number: 20090137660
    Abstract: A method of treating a patient in need of therapy for a cytokine dysregulation comprising administering to that patient a therapeutically effective dose of a compound of general formula: (I) wherein R1 and R2 together form a group —(CH2)n—CR4R5—(CH2)m— wherein n and m are independently selected integers 0, 1 or 2 and R4 and R5 are independently selected from H, C1-18 alkyl, C1-18 alkoxy, C1-18n hydroxyalkyl, C2-18 alkenyl and C6-18 aryl or aralyalkyl and R3 is the fatty acyl group of an essential polyunsaturated fatty acid.
    Type: Application
    Filed: March 2, 2006
    Publication date: May 28, 2009
    Inventors: Laurence S. Harbige, Michael J. Leach, Paul Barraclough, Anthony P. Dolan
  • Publication number: 20090137393
    Abstract: The invention relates to novel 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) in which X, Y, A, B, Q1, Q2 and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2,4,6-trialkylphenyl-substituted cyclopentane-1,3-diones of the formula (I) and, secondly, at least one crop plant compatibility-improving compound.
    Type: Application
    Filed: January 3, 2007
    Publication date: May 28, 2009
    Applicant: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Ulrich Gorgens, Olga Malsam, Alfred Angermann, Guido Bojack, Alan Graff, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Hein Kehne, Christopher Hugh Rosinger, Jan Dittgen
  • Publication number: 20090082311
    Abstract: The present invention provides a novel compound having few side effects such as bradycardia and the like and having superior peripheral blood lymphocyte-decreasing effect.
    Type: Application
    Filed: April 27, 2007
    Publication date: March 26, 2009
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Masatoshi Kiuchi, Mitsuharu Nakamura, Maiko Hamada, Kunio Sugahara
  • Publication number: 20090076062
    Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: September 13, 2007
    Publication date: March 19, 2009
    Inventors: Juergen Klaus Maibaum, Daniel Kaspar Baeschlin, Holger Sellner
  • Publication number: 20090069416
    Abstract: The present invention is to provide skin cosmetics and anti-wrinkle agents which are excellent in reducing effect on wrinkle caused by photoaging. Skin cosmetics and anti-wrinkle agents which comprise a sugar alcohol derivative represented by the following formula (1): (wherein n is 1 to 5, preferably n=2.).
    Type: Application
    Filed: January 21, 2006
    Publication date: March 12, 2009
    Inventors: Kyoko Miura, Akinori Haratake
  • Patent number: 7468457
    Abstract: Novel biaryl compounds having the structural formula (I): are useful in a variety of pharmaceutical applications, whether human or veterinary, and also in cosmetics.
    Type: Grant
    Filed: November 19, 2004
    Date of Patent: December 23, 2008
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Pascal Collette
  • Publication number: 20080312317
    Abstract: There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R1 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-14 arylcarbonyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom or a hydroxyl group; R5 is a hydrogen atom or a C1-6 alkyl group; R6 is a hydrogen atom or a hydroxyl group; and R7 is an acetyl group or the like.
    Type: Application
    Filed: April 10, 2008
    Publication date: December 18, 2008
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Masayuki Miyano, Daisuke Ito, Norio Murai
  • Publication number: 20080242721
    Abstract: The present disclosure relates to the preparation of ketal compounds from glycerol and levulinic acid and esters, and uses thereof.
    Type: Application
    Filed: May 31, 2007
    Publication date: October 2, 2008
    Applicant: AROMAGEN CORPORATION
    Inventor: Sergey Selifonov
  • Publication number: 20080125483
    Abstract: The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.
    Type: Application
    Filed: November 21, 2007
    Publication date: May 29, 2008
    Inventors: Jenn-Tsang Hwang, Chrong-Shiong Hwang, Yow-Lone Chang, Chung-Niang Yao
  • Publication number: 20080103191
    Abstract: Pharmaceutical composition comprising one or more entacapone derivatives and one or more pharmaceutically acceptable carriers, a process for producing the pharmaceutical composition, specific entacapone derivatives, a process for the preparation of entacapone derivatives, and the use of the entacapone derivatives for the preparation of a medicament.
    Type: Application
    Filed: June 14, 2007
    Publication date: May 1, 2008
    Inventors: Klaus Hansen, Robert Kraemer, Thomas Lauterbach, Dirk Schmidt, Fritz Paar, Petra Pfeiffer, Detlef Geffken, Wolfgang Thimann, Katharina Wehner
  • Patent number: 7339078
    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: March 4, 2008
    Assignee: G.D. Searle LLC
    Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
  • Publication number: 20080033036
    Abstract: The present invention provides a method and composition for promoting hair growth in a mammal which comprises a prostaglandin compound having two hetero atoms at the 15 position as an active ingredient thereof.
    Type: Application
    Filed: August 12, 2004
    Publication date: February 7, 2008
    Inventors: Ryuji Ueno, Tsuyoshi Habe, Takashi Sekida
  • Patent number: 7323493
    Abstract: The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.
    Type: Grant
    Filed: June 19, 1998
    Date of Patent: January 29, 2008
    Assignee: Sanofi-Aventis
    Inventors: Bernard Abramovici, Jean-Claude Gautier, Jean-Claude Gromenil, Jean-Marie Marrier
  • Publication number: 20080020071
    Abstract: A composition protects against, minimizes the effects of, and hastens recovery from the typical symptoms associated with an alcohol induced hangover. The composition includes superoxide dismutase (SOD), and prickly pear cactus (OFI). In addition, sesamin and alpha-lipoic acid work with the SOD and OFI for enhanced antioxidant and therapeutic effects. Other ingredients can be added to the composition for additional treatment of symptoms.
    Type: Application
    Filed: July 24, 2006
    Publication date: January 24, 2008
    Inventor: Victor H. Diaz
  • Patent number: 7307043
    Abstract: An aqueous composition suitable for applying insecticides or acaricides to plant propagation materials comprising water, an insecticidally or acaricidally effective amount of at least one nitroimino- or nitroguanidino-compound in free form or in agrochemically useful salt form and a blend of the following components, by weight: a) 2-10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 4-20% of at least one inorganic solid carrier; and c) 3-25% of at least one antifreeze agent. In one embodiment, the aqueous composition further comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.
    Type: Grant
    Filed: August 17, 2004
    Date of Patent: December 11, 2007
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Christian Schlatter, Ravi Ramachandran
  • Patent number: 7271194
    Abstract: Use of escitalopram (the S-(+)-enantiomer of citalopram) or a pharmaceutically acceptable salt thereof for the preparation of a medicament useful in the treatment of neurotic disorders is provided, including anxiety states, in particular generalised anxiety disorder and social anxiety disorder, post traumatic stress disorder, obsessive compulsive disorder and panic attacks.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: September 18, 2007
    Assignee: H. Lundbeck A/S
    Inventors: Connie Sanchez, Sandra Hogg
  • Patent number: 7271274
    Abstract: The invention relates to compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, wherein the compounds are of the following Formulas: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein the substituents are defined in the application. The invention further provides methods of treatment of inflammatory disorders by administering the compounds.
    Type: Grant
    Filed: April 20, 2005
    Date of Patent: September 18, 2007
    Assignee: AhteroGenics, Inc.
    Inventors: Charles Q. Meng, M. David Weingarten
  • Patent number: 7264822
    Abstract: One aspect of the invention is a system for treating vascular conditions, including a catheter, a stent coupled to the catheter, and a polymeric coating on the stent comprising at least one conjugated drug. Each conjugated drug includes a control agent and a bioactive agent, where the control agent controls the elution rate of the bioactive agent.
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: September 4, 2007
    Assignee: Poly-Med, Inc.
    Inventors: Shalaby W. Shalaby, Todd Campbell
  • Patent number: 7196089
    Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: March 27, 2007
    Assignee: Asterand UK Limited
    Inventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
  • Patent number: 7105552
    Abstract: Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.
    Type: Grant
    Filed: April 27, 2001
    Date of Patent: September 12, 2006
    Assignee: Theracos, Inc.
    Inventors: Bishwajit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
  • Patent number: 7078400
    Abstract: The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.
    Type: Grant
    Filed: July 1, 2003
    Date of Patent: July 18, 2006
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Patent number: 7034015
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 7026315
    Abstract: Fungicidal mixtures, comprising as active components a) a morpholine or piperidine derivative I selected from the group of the compounds Ia, Ib, Ic and Id and b) compounds of the formula II in a synergistically effective amount are described.
    Type: Grant
    Filed: December 11, 1999
    Date of Patent: April 11, 2006
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Schelberger, Maria Scherer, Reinhold Saur, Karl Eicken, Egon Haden, Eberhard Ammermann, Thomas Grote, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 7001924
    Abstract: The present invention features compounds useful for inhibiting RNase P activity. These compounds can be used as therapeutics for treating or preventing a variety of bacterial infections. The compounds belong to several classes including mono- and bis-guanylhydrazones, guanylhydrazone mimetics, and benzothiazolium compounds. Exemplary compounds are compounds of formula I: Y—(NR?)k—U1—(NR?)I—A—(NR1)m—U2—(NR2)n—Z??I with substituents as described herein.
    Type: Grant
    Filed: September 23, 2002
    Date of Patent: February 21, 2006
    Assignee: Message Pharmaceuticals
    Inventors: Tony Giordano, Michael A. Sturgess, Samala J. Rao
  • Patent number: 6926913
    Abstract: The invention provides a composition of matter comprising molecular iodine and tetraglycol.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: August 9, 2005
    Assignees: Ben Gurion University of the Negev Research & Development Authority, Yissum Research Development Company of the Hebrew
    Inventors: Uri Wormser, Amnon Sintov
  • Patent number: 6903086
    Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: June 7, 2005
    Assignee: SYNTEX (U.S.A.) LLC
    Inventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
  • Patent number: 6894074
    Abstract: The invention relates to insecticidal mixtures comprising compounds of the formula (I) in which X?, Y?, Z?, n, G?, A? and B? are as defined above and agonists and/or antagonists of nicotinic acetylcholine receptors, for protecting plants against attack by pests.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: May 17, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Bretschneider, Reiner Fischer, Christoph Erdelen, Ernst Brück
  • Patent number: 6890955
    Abstract: The invention concerns aryloxypropanolamine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive.
    Type: Grant
    Filed: January 3, 2003
    Date of Patent: May 10, 2005
    Assignee: Virbac SA
    Inventors: Ahmed El Hadri, Philippe Archimbault, Gérard Leclerc, Arthur Donny Strosberg, France Pietri-Rouxel
  • Patent number: 6864254
    Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 8, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Patent number: 6861539
    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: August 12, 2003
    Date of Patent: March 1, 2005
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
  • Patent number: 6849626
    Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: February 1, 2005
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
  • Patent number: 6825231
    Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endot
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: November 30, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang, Heinz-Werner Kleemann, Jan-Robert Schwark, Klaus Wirth, Hans-Willi Jansen
  • Patent number: 6800658
    Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: October 5, 2004
    Assignees: Children's Medical Center Corporation, President & Fellows of Harvard College, Nuchem Pharmaceuticals, Inc.
    Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
  • Patent number: 6790463
    Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: September 14, 2004
    Inventors: Robert F. Hofmann, Robert H. Carpenter
  • Patent number: 6777440
    Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1, R2 and B1 are as defined herein.
    Type: Grant
    Filed: December 6, 2002
    Date of Patent: August 17, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Jacques Banville, Roger Remillard, Serge Plamondon
  • Publication number: 20040138296
    Abstract: The present invention provides compositions and methods for the treatment or prevention of Alzheimer's disease. More particularly, the invention provides a combination therapy for the treatment or prevention of Alzheimer's disease, wherein the therapy comprises administering to a subject an amyloid beta vaccine in combination with a cyclooxygenase-2 selective inhibitor.
    Type: Application
    Filed: July 25, 2003
    Publication date: July 15, 2004
    Applicant: Pharmacia Corporation
    Inventors: David W. Robertson, Grant A. Krafft
  • Patent number: 6730783
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: May 4, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
  • Publication number: 20040019038
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Application
    Filed: July 21, 2003
    Publication date: January 29, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John Robert Proudfoot, Alan D. Swinamer, Hidenori Takahashi, Thomas A. Gilmore, Rajiv Sharma
  • Patent number: 6683210
    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: March 15, 2002
    Date of Patent: January 27, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
  • Patent number: 6677330
    Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded). wherein R1 and R2 represent substituents.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: January 13, 2004
    Assignee: Eisai Co., Ltd.
    Inventors: Yoichi Iimura, Takashi Kosasa, Yoshiharu Yamanishi, Hachiro Sugimoto, Yoshio Takeuchi, Tetsuo Shibata, Emiko Suzuki
  • Publication number: 20040006130
    Abstract: A compound of the formula [I] 1
    Type: Application
    Filed: February 10, 2003
    Publication date: January 8, 2004
    Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
  • Publication number: 20040006050
    Abstract: Compounds of Formula I, 1
    Type: Application
    Filed: June 9, 2003
    Publication date: January 8, 2004
    Applicants: Wyeth, ArQule Inc.
    Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
  • Publication number: 20030225091
    Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1
    Type: Application
    Filed: November 15, 2002
    Publication date: December 4, 2003
    Inventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
  • Patent number: 6653322
    Abstract: The present invention provides compositions and methods for treating an animal, preferably a human, suffering from or predisposed to a physical disorder by administering an effective amount of a composition comprising at least one RAR antagonist, preferably an RAR&agr; antagonist, and at least one RXR agonist. The combination of an RXR agonist, which has no therapeutic effects alone, with an RAR antagonist allows the use of lower doses of the RAR antagonist than were previously thought to be efficacious; this approach obviates many of the undesirable physiological side-effects of treatment with RAR antagonists.
    Type: Grant
    Filed: July 19, 2000
    Date of Patent: November 25, 2003
    Assignees: Bristol-Myers Squibb Company, Institut National de la Sante et de la Recherche Medicale, Centre National de la Recherche Scientifique, Universite Louis Pasteur
    Inventors: Pierre Chambon, Hinrich Gronemeyer, Peter R. Reczek, Jacek Ostrowski
  • Patent number: 6653318
    Abstract: The present invention relates to pyrimidine nucleoside compounds and their use to treat viral infections of Varicella Zoster virus and Epstein Barr Virus, as well as cancers which are complications of Epstein Barr virus.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: November 25, 2003
    Assignees: Yale University, The University of Georgia Research Foundation, Inc.
    Inventors: Yung-Chi Cheng, Chung K. Chu, Ling Li, Yongseok Chai
  • Patent number: 6649652
    Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I)
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: November 18, 2003
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall
  • Patent number: 6638931
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: October 28, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro