N-c(=x)-x-n Containing Patents (Class 514/477)
  • Patent number: 11414396
    Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
    Type: Grant
    Filed: August 26, 2020
    Date of Patent: August 16, 2022
    Assignees: Exelixis, Inc., Genentech, Inc.
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava, Neel Kumar Anand
  • Patent number: 11173120
    Abstract: The present invention related to aqueous lipid and/or liposome formulations with an increased chemical stability, to methods of preparing such aqueous formulations as well as to kits comprising them. The present invention further relates to methods of preparing lipid-based pharmaceutical compositions, to pharmaceutical compositions prepared by such methods and to methods of chemically stabilizing aqueous lipid and/or liposome formulations.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: November 16, 2021
    Assignee: BioNTech RNA Pharmaceuticals GmbH
    Inventors: Heinrich Haas, Isaac Hernan Esparza Borquez
  • Patent number: 8957060
    Abstract: Disclosed herein are solutions and kits for tumescent antibiotic delivery. Embodiments of the solution comprise an antibiotic component, an anesthetic component and a vasoconstrictor component. In addition, a method of use is disclosed comprising subcutaneous delivery of the solution. The disclosed solution, kit and method of subcutaneous delivery can be used for a variety of surgical procedures including liposuction, mastectomy and others. The tumescent antibiotic solution can be administered to a patient in situations where establishing IV access is difficult, impossible, or undesirable. A variety of delivery methods appropriate for surgical settings, as well as for use by first responders are likewise disclosed.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: February 17, 2015
    Inventor: Jeffrey Alan Klein
  • Publication number: 20150033418
    Abstract: A first aspect of the invention is an agricultural composition comprising nanoparticles, an agrochemical active ingredient in the nanoparticles, and optionally (but in some embodiments preferably) a carrier for the nanoparticles. In some embodiments, the nanoparticles are viral particles or capsids, particularly plant viral particles or capsids. In some embodiments, the carrier comprises an inert or biodegradable carrier (e.g., a solid carrier) to which the nanoparticles are bound or in which the nanoparticles are suspended. In some embodiments, the carrier comprises inert or biodegradable polymer fibers.
    Type: Application
    Filed: April 16, 2013
    Publication date: January 29, 2015
    Inventors: Steven A. Lommel, Julie Willoughby, Richard Guenther
  • Patent number: 8916500
    Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: December 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Heike Hungenberg, Peter Dahmen
  • Patent number: 8846567
    Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from the class of the organophosphates or carbamates, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: September 30, 2014
    Assignee: Bayer CropScience AG
    Inventors: Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
  • Publication number: 20140274685
    Abstract: The disclosure provides for methods for reducing dust by treating a seed with a dust reducing composition described herein. The disclosure also provides for methods of reducing exposure to vacuum planter dust released during seed planting by applying a composition described herein to a seed. Methods for increasing seed lubricity by coating a seed with a composition described herein are also provided for. Compositions and seeds useful in these methods are also described.
    Type: Application
    Filed: March 5, 2014
    Publication date: September 18, 2014
    Applicant: BAYER CROPSCIENCE LP
    Inventors: Yaodong HUANG, William HANSON, Philip M. Mathew, Smita PATEL, Justin ELDRIDGE
  • Publication number: 20130178490
    Abstract: The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and one or more carbamate compound(s) selected from Group (A) shows an excellent controlling activity on a pest.
    Type: Application
    Filed: October 13, 2011
    Publication date: July 11, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: So Kiguchi, Soichi Tanaka
  • Patent number: 8398759
    Abstract: An ecologically compatible anti-microbial-adhesion agent is described, which is particularly suitable for use in anti-fouling paints, preferably for boats, characterized in that it comprises a compound selected from eugenol, vanillin, benzaldehyde substituted with one or two substituents selected from the groups —OH (hydroxy) and —OCH3 (methoxy), or any combination thereof. An anti-fouling paint is also described, particularly for boats, comprising the anti-microbial-adhesion agent mentioned above and other components selected from conventional biocides, solvents, resins, pigments, charges and fillings, and combinations thereof.
    Type: Grant
    Filed: May 12, 2009
    Date of Patent: March 19, 2013
    Assignee: Biopaint S.R.L.
    Inventors: Cecilia Calisti, Giulio Zanaroli, Fabio Fava, Alessandra Bontempi Di Roccaspada, Maurizio Ruzzi
  • Publication number: 20120283095
    Abstract: The present invention relates to synergistic mixtures comprising, as active components, one insecticidal compound I selected from the group consisting of carbamates; and one fungicidal compound II selected from the group of strobilurines in synergistic effective amounts.
    Type: Application
    Filed: November 29, 2010
    Publication date: November 8, 2012
    Applicant: BASF SE
    Inventors: Markus Gewehr, Egon Haden, Lutz Brahm
  • Publication number: 20110311503
    Abstract: The novel active ingredient combinations which consist of the compounds of the formula (I) in combination with further active insecticidal ingredients (II) are very suitable for control of animal pests such as insects and/or unwanted acarids.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Christian FUNKE, Heike HUNGENBERG, Rüdiger FISCHER
  • Patent number: 8003119
    Abstract: The use of the polyamine known as spermidine, i.e., N-(3-aminopropyl)tetraminethylenediamine, as an active principle in the preparation of a composition for pharmaceutical or dietetic use in man for combating hair loss is disclosed.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: August 23, 2011
    Assignee: Giuliani S.p.A.
    Inventors: Fabio Rinaldi, Elisabetta Sorbellini, Valter Gatti, Danila Ingrid Marchioretto
  • Patent number: 7999006
    Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: August 16, 2011
    Assignee: Exelixis, Inc.
    Inventor: Peter Lamb
  • Publication number: 20110160251
    Abstract: The present invention provides an animal ectoparasite control composition containing an insecticidal component and an adipate, and a method of controlling an animal ectoparasite which comprises administering an effective amount of the animal ectoparasite control composition to an animal.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 30, 2011
    Inventors: Naonobu NISHIGUCHI, Takahisa Hirayama, Kaori Ikari
  • Patent number: 7935727
    Abstract: Compounds having a biphenyl group substituted with a phenyl or heteroaromatic group, as shown in Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: May 3, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yi-Heng Chen, Zhijian Lu, Peter J. Sinclair
  • Publication number: 20100255997
    Abstract: Compositions useful in the field of agricultural chemistry and methods for making and using the compositions are provided. Methods of improving the degree of efficacy of an active component or speed of action of an active component are also provided.
    Type: Application
    Filed: June 18, 2010
    Publication date: October 7, 2010
    Applicant: CJB Industries
    Inventor: David Miles
  • Patent number: 7803839
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Grant
    Filed: October 5, 2006
    Date of Patent: September 28, 2010
    Assignee: Exelixis, Inc.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Publication number: 20100113268
    Abstract: The invention relates to active compound combinations of chloronicotinyls with oxamyl and to the use of these mixtures for controlling animal pests.
    Type: Application
    Filed: December 12, 2007
    Publication date: May 6, 2010
    Applicant: Bayer CropScience AG
    Inventors: Wolfram Andersch, Heike Hungenberg, Roland Gallow
  • Publication number: 20090099135
    Abstract: Embodiments of the present invention provide compositions for controlling a target pest including a pest control product and at least one active agent, wherein: the active agent can be capable of interacting with a receptor in the target pest; the pest control product can have a first activity against the target pest when applied without the active agent and the compositions can have a second activity against the target pest; and the second activity can be greater than the first activity.
    Type: Application
    Filed: January 16, 2008
    Publication date: April 16, 2009
    Applicant: TyraTech, Inc.
    Inventor: Essam Enan
  • Publication number: 20090099127
    Abstract: A nematicidal composition includes (a) at least one carbamate and (b) at least one neonicotinoid and/or chloronicotinyle. In one exemplary embodiment, the carbamate can be an oxime carbamate, such as thiodicarb and the neonicotinoid can be a nitroguanidine. In one specific embodiment, the nitroguanidine includes imidacloprid and/or clothianidin. An exemplary method of the invention includes applying a composition of the invention to either soil or a plant (e.g., seeds or foliarly) to combat nematode damage and/or increase crop yield.
    Type: Application
    Filed: October 31, 2006
    Publication date: April 16, 2009
    Applicant: BAYER CROPSCIENCE LP
    Inventors: Michael R. Schwarz, John E. Curtis
  • Publication number: 20080306026
    Abstract: An encapsulated composition of (a) a pesticide at least active via ingestion that is photolabile, and (b) at least one photoprotectant, wherein the encapsulating polymeric barrier is base triggerable is disclosed. A method for controlling damage of a material by a pest by the use of such encapsulated compositions is likewise disclosed. The composition as disclosed gives protection for beneficial arthropods and reduces workers exposure.
    Type: Application
    Filed: February 23, 2006
    Publication date: December 11, 2008
    Inventors: Ian Malcolm Shirley, Tanya Wright, Robert Michael Perrin, Patrick Mulqueen, Anne Waller, Andy Pierce
  • Publication number: 20080287534
    Abstract: Disclosed is a method for protecting a plant planted in a growing medium from foliar insect pests comprising applying an insecticidally effective amount of a mixture comprising methomyl and oxamyl to the growing medium.
    Type: Application
    Filed: February 14, 2006
    Publication date: November 20, 2008
    Inventors: Jon Stuart Claus, Gale Edwin Drake, Robert Mark Leighty, Frederick Walters Marmor
  • Publication number: 20080101409
    Abstract: A method and apparatus analyze a compressed image code stream to determine logical boundaries of segments and parse the data stream into packets, wherein the packets are configured to reduce a number of partial logical segments in individual packets
    Type: Application
    Filed: October 26, 2006
    Publication date: May 1, 2008
    Inventors: Matthew J. West, Paul S. Everest, John G. Apostolopoulos, Susie J. Wee
  • Patent number: 7312244
    Abstract: Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: December 25, 2007
    Assignee: Cellgate, Inc.
    Inventors: Linda Clifford, legal representative, Laurence J. Marton, Aldonia L. Valasinas, Venodhar K. Reddy, Benjamin Frydman, deceased
  • Patent number: 6949574
    Abstract: The present invention relates to novel oxime carbamyl derivatives and pharmaceutical compositions comprising said derivatives which inhibit fatty acid amide hydrolase. These pharmaceutical compositions are useful for the treatment of conditions which can be effected by inhibiting fatty acid amide hydrolase including, but not limited to, neuropathic pain, emesis, anxiety, altering feeding behaviors, movement disorders, glaucoma, brain injury, and cardiovascular disease.
    Type: Grant
    Filed: February 4, 2003
    Date of Patent: September 27, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sing-Yuen Sit, Kai Xie, Hongfeng Deng
  • Patent number: 6825014
    Abstract: The present invention relates to the preparation of compounds of formula (I): from the corresponding hydantoins by means of an enzymatic process. The L-compound is preferably formed.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: November 30, 2004
    Assignee: Degussa AG
    Inventors: Hans-Peter Krimmer, Oliver May, Ingo Klement, Karlheinz Drauz, Dietmar Reichert
  • Patent number: 6692754
    Abstract: The present invention relates to skin aging inhibitors and/or skin quality-improving agents comprising hydroxyproline, its N-acyl derivatives or salts thereof, and cosmetic compositions for inhibiting skin aging and/or improving skin quality comprising said skin aging inhibitors and/or skin quality-improving agents.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: February 17, 2004
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yutaka Makimoto, Asako Kobayashi, Toshihiro Sakakibara, Chiemi Takaboshi, Ayako Kamimura, Tomoya Takahashi, Minako Tajima, Yoichiro Takekoshi
  • Publication number: 20030220352
    Abstract: The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
    Type: Application
    Filed: March 18, 2003
    Publication date: November 27, 2003
    Applicant: Inflazyme Pharmaceuticals Ltd.
    Inventors: Ronald W. Lauener, David L. Burgoyne, Patrick J. Rebstein, Lloyd F. MacKenzie, Yuanlin Zhou, Yaping Shen
  • Patent number: 6593362
    Abstract: This invention relates to pharmaceutical compositions and methods of using non-peptidic cyclophilin-binding compounds in medical conditions involving breakdown of mitochondrial energy metabolism induced by calcium overload, in treating alopecia and promoting hair growth, in treating infections with filarial and helmintic parasites, and in treating and preventing infections with the human immunodeficiency virus.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: July 15, 2003
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Joseph P. Steiner, Gregory S. Hamilton
  • Publication number: 20020091150
    Abstract: The present invention is a compound of formula 1
    Type: Application
    Filed: December 10, 2001
    Publication date: July 11, 2002
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6414031
    Abstract: There are disclosed bisoxime ether derivatives of the formula I in which the variables have the following meanings: R1 is halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; n is 1 to 5, it being possible for the radicals R1 to be different if n is other than 1; R2 is C1-C4-alkyl, C3-C6-alkenyl or C3-C6-alkynyl, it being possible for these groups to be partially or fully halogenated; Q is C(═CHOCH3)—COOCH3, C(═CHCH3)—COOCH3, C(═NOCH3)—COOCH3 or C(═NOCH3)13 CONHCH3; and salts thereof, processes and intermediates for the preparation of these compounds, and their use for controlling animal pests and harmful fungi.
    Type: Grant
    Filed: November 2, 2000
    Date of Patent: July 2, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Bayer, Roland Götz, Michael Keil, Hubert Sauter, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Andreas Gypser, Bernd Müller, Arne Ptock, Eberhard Ammermann, Thomas Grote, Gisela Lorenz, Siegfried Strathmann, Volker Harries
  • Patent number: 6290992
    Abstract: A method of termite control consists of injecting a foam formulation above ground into the walls of a structure infested with termites or other undesirable pests. The inner spaces of affected walls are flooded at and above ground level to ensure that the foam formulation reaches all passages open to the soil under the structure and establishes an above-ground layer of pest-control chemicals. The foam penetrates all porous material exposed to the injection and impregnates it with active ingredients that remain embedded in the material long after the foam disappears, thereby retaining the insecticidal, repellant and preservative properties of the active agents for a long time without exposure to normal degrading forces. The pest-control formulation preferably comprises pesticide, repellant and preservative components, and a foaming agent in a liquid carrier.
    Type: Grant
    Filed: July 10, 1998
    Date of Patent: September 18, 2001
    Inventor: Shelby J. Magnuson-Hawkins
  • Patent number: 6235729
    Abstract: The present invention provides a method of inhibiting tumor progression in an individual in need of such treatment, comprising the step of administering to said individual a pharmacologically effective dose of a phospholipase C inhibitor. Also provided is a method of inhibiting metastasis in an individual in need of such treatment, comprising the step of administering to said individual a pharmacologically effective dose of a phospholipase C inhibitor. Further provided are pharmaceutical compositions, comprising a phospholipase C inhibitor of tumor invasiveness and metastasis and a pharmaceutically acceptable carrier and a pharmaceutical composition, comprising a phospholipase C inhibitor of tumor invasiveness and metastasis, a antineoplastic agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 25, 1997
    Date of Patent: May 22, 2001
    Assignee: UAB Research Foundation
    Inventors: Philip Chen, Timothy Turner, Alan Wells
  • Patent number: 6221885
    Abstract: Pesticidal compositions containing as active ingredients 3,5-dichloro-1-(3,3-dichloro-2-propenyloxy)-4-[3-(5-trifluoromethylpyridin-2-yloxy)pro poxy]benzene of the formula: and at least one carbamate compound selected from thiodicarb, methomyl and alanycarb have excellent pesticidal activity by their synergistic cooperative action.
    Type: Grant
    Filed: August 23, 1999
    Date of Patent: April 24, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Shigeru Saito
  • Patent number: 6150406
    Abstract: A method for suppressing plant damage by nematodes which comprises the concurrent administration, to the locus, soil or seeds of plants in need of such treatment, of (a) a metabolite of the fungus Myrothecium verrucaria and (b) a chemical pesticide, as well as synergistic nematocidal compositions useful therein.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: November 21, 2000
    Assignee: Valent BioSciences, Inc.
    Inventors: Prem Warrior, Daniel F. Heiman, Linda A. Rehberger
  • Patent number: 6114285
    Abstract: A method of chemically suckering trees of the families Musaceae (banana) and Plantaginaceae (plantains) which comprises introducing into a mother tree an amount of a composition effective to arrest apical dominance in the mother tree.A method of protection of two or more trees of the families Musaceae (banana) and Plantaginaceae (plantains) which share a common root system.
    Type: Grant
    Filed: February 18, 1999
    Date of Patent: September 5, 2000
    Assignee: Rhone Poulenc Agro
    Inventors: Marvin Donaldo Mora Padilla, Juan Bocanegra, Jorge Cepeda
  • Patent number: 6034137
    Abstract: This invention provides novel cationic lipids, particularly guanidino lipids, and methods for their preparation. Also provided are polyanionic-lipid complexes comprising the lipids of the invention, their preparation and use to deliver biologically active substances, particularly nucleic acids to cells.
    Type: Grant
    Filed: October 20, 1997
    Date of Patent: March 7, 2000
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Paula N. Belloni, Donald R. Hirschfeld, John O. Link, John J. Nestor, Jr., Gary A. Peltz
  • Patent number: 5952316
    Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.
    Type: Grant
    Filed: August 14, 1997
    Date of Patent: September 14, 1999
    Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.
    Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
  • Patent number: 5910323
    Abstract: This invention provides a novel aqueous pesticide formulation having a fungicidal bicarbonate-containing inorganic salt ingredient which enhances the efficacy of an insecticidal ingredient for treatment of cultivated crops. An invention pesticide formulation also contains a water-soluble organic compound which functions as a compatibility enhancing ingredient in the aqueous pesticide formulation, and improves the spreadability and adhesiveness of the composition ingredients when applied to foliage.
    Type: Grant
    Filed: October 21, 1993
    Date of Patent: June 8, 1999
    Assignee: Church & Dwight Co., Inc.
    Inventors: M. Stephen Lajoie, Amy L. Joseph, Keith A. Jones, Anthony E. Winston
  • Patent number: 5889059
    Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sub.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: March 30, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5851988
    Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## whereineach A is independently a proton-accepting substituent;each R is independently a noninterfering substituent;n is 0, 1, or 2; andeach linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--.Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
    Type: Grant
    Filed: January 15, 1997
    Date of Patent: December 22, 1998
    Assignee: Terrapin Technologies, Inc.
    Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M. Kauvar, Wayne R. Spevak
  • Patent number: 5821260
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 13, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5807884
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: September 15, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5783596
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 21, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5750351
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 12, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5747514
    Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: May 5, 1998
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller, Fionna Mitchell Martin
  • Patent number: 5723490
    Abstract: The present invention relates to a class of THF-containing sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.
    Type: Grant
    Filed: April 19, 1995
    Date of Patent: March 3, 1998
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Roger D. Tung
  • Patent number: 5716979
    Abstract: The invention concerns tachykinin antagonists. The compounds are nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included.The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
    Type: Grant
    Filed: October 8, 1996
    Date of Patent: February 10, 1998
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
  • Patent number: 5599803
    Abstract: Insecticidal compositions, comprising normally-employed insecticides but comprising also an effective activity-enhancing amount of capsaicin or other capsaicinoid, especially in the form of capsicum, exhibit synergistic effects against numerous insects, including especially bud worms, boll worms, cabbage loopers, army worms, beet army worms, and beetles, and are especially effective on cotton, soybeans, common garden vegetables, and flowers, when sprayed on the insect or its habitat, especially as an aqueous solution, suspension, or emulsion. Larger crop stands may be effectively treated by aerial spraying from the usual crop-dusting airplane.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: February 4, 1997
    Assignee: Kalamazoo Holdings, Inc.
    Inventors: Gary C. Hainrihar, James G. Dubberly, John T. Greenlee
  • Patent number: RE38915
    Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N?N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: December 6, 2005
    Assignee: Telik, Inc.
    Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M. Kauvar, Wayne R. Spevak