N-c(=x)x Containing (x Is Chalcogen) Doai Patents (Class 514/476)
- With an additional active ingredient (Class 514/479)
- Polycyclo ring system attached by nonionic bonding (Class 514/480)
- N-C(=X)-N, N-C(=N)N, N-N, nitrogen directly bonded to oxygen by nonionic bonding or cyano containing (Class 514/482)
- Plural N-C(=X)-X groups (Class 514/483)
- Ring in acid moiety (Class 514/484)
- Ring in alcohol moiety (Class 514/489)
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Publication number: 20040171678Abstract: Dithiocarbamate, particularly tetraethylthiuram disulfide, and thiocarbamate anions strongly inhibit the growth of cancer cells of a variety of cell types. Such inhibitory effect is enhanced by heavy metal ions such as copper ions, cytokines and ceruloplasmin. A method is presented for using tetraethylthiuram disulfide to reduce tumor growth, and to potentiate the effect of other anticancer agents.Type: ApplicationFiled: February 25, 2004Publication date: September 2, 2004Applicant: Charlotte-Mecklenburg Hospital Authority d/b/a Carolinas Medical CenterInventor: Thomas Preston Kennedy
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Patent number: 6774180Abstract: High molecular weight derivatives of activated poly(ethylene glycol) and the like polymers are prepared in high purity by conjugating a large PEG molecule to a small PEG molecule. Most of the reaction steps can be accomplished on the more readily purified small molecule to avoid laborious purification of the high molecular weight derivatives.Type: GrantFiled: December 18, 2001Date of Patent: August 10, 2004Assignee: Nektar Therapeutics AL, CorporationInventors: Antoni Kozlowski, Xiaoming Shen, Michael David Bentley, Zhihao Fang
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Patent number: 6765021Abstract: This invention provides compounds of formula I having the structure wherein: B, D, C, and R1 as defined herein.Type: GrantFiled: August 9, 2002Date of Patent: July 20, 2004Assignee: WyethInventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
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Publication number: 20040138176Abstract: The invention relates to a compositions useful in the field of agricultural chemistry and methods for making and using the compositions. The compositions include (i) a permeabilizing agent, and (ii) a active component, for example, a pesticide or plant growth regulator, and can include additional components as well, for example, flow agents. The permeabilizing agent, or a mixture of permeabilizing agents, acts as an adjuvant to the active component or chemicals to improve the degree of efficacy of the active component or speed of action of the active component. The permeabilizing agents are typically one or more chelating agents, cationic materials, anionic materials, and zwitterionic materials, and include polyphosphate salts. Examples of cationic materials include polyamines such as ethylenediamine and quaternary ammonium salts. The active components can be pesticides, herbicides, insecticides, fungicides, virucides, bacteriocides, and acaricides.Type: ApplicationFiled: January 26, 2004Publication date: July 15, 2004Applicant: CJB Industries, Inc.Inventor: David Miles
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Patent number: 6730700Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.Type: GrantFiled: July 15, 2002Date of Patent: May 4, 2004Assignee: Renovis, Inc.Inventors: L. David Waterbury, Allan L. Wilcox, John M. Carney, Farah Mavandadi, Albert Danielzadeh
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Publication number: 20040039039Abstract: Fungicidal mixtures, comprisingType: ApplicationFiled: July 3, 2003Publication date: February 26, 2004Inventors: Arne Ptock, Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegried Strathmann, Maria Scherer, Klaus Schelberger, Achim Reddig
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Patent number: 6696487Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.Type: GrantFiled: August 6, 2001Date of Patent: February 24, 2004Assignee: Bayer Cropscience S.A.Inventors: Vincent Gerusz, Darren James Mansfield, José Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
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Patent number: 6689774Abstract: The present invention provides methods and compositions comprising one or more zinc ionophores for protecting tissue from the harmful effects of apoptosis in patients in need thereof. Concentrations of zinc-pyrithione and diethyldithiocarbamate in the picomolar to nanomolar range have a strong protective effect against apoptosis.Type: GrantFiled: July 26, 2002Date of Patent: February 10, 2004Assignee: Zinc Therapeutics, Canada Inc.Inventor: Henry Fliss
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Publication number: 20040019103Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II).Type: ApplicationFiled: July 10, 2003Publication date: January 29, 2004Applicant: Biorex Research & Development Co.Inventors: Laszlo Vigh, Peter Literati Nagy, Jeno Szilbereky, Laszlo Urogdi, Andrea Jednakovits, Laszlo Jaszlits, Katalin Biro, Ede Marvanyos, Mihaly Barabas, Erzsebet Hegedus, Laszlo Koranyi, Maria Kurthy, Gabor Balogh, Ibolya Horvath, Zsolt Torok, Eva Udvardy, Gyorgy Dorman, Denes Medzihradszky, Bea Mezes, Eszter Kovacs, Erno Duda, Beatrix Farkas, Attila Glatz
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Publication number: 20040019102Abstract: There is provided a method for inhibiting ATF/CREB and cancer cell growth using disulfiram, administered in combination with heavy metals. It was found that disulfiram disrupts transcription factor DNA binding by forming mixed disulfides with thiols within the DNA-binding region, and that this process is facilitated by metal ions. Disulfiram administered to melanoma cells in combination with copper (II) or zinc(II) decreased expression of cyclin A, reduced proliferation in vitro, and inhibited growth of melanoma cells. The combination of oral zinc gluconate and disulfiram at currently approved doses for alcoholism stabilized tumor growth in two of three patients with Stage IV metastatic melanoma, with 12 and 17 month survivals, respectively, to date, and produced a >50% reduction in hepatic metastases in one individual.Type: ApplicationFiled: May 14, 2003Publication date: January 29, 2004Applicant: Charlotte-Mecklenburg Hospital Authority d/b/a Carolinas Medical CenterInventor: Thomas Preston Kennedy
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Patent number: 6677308Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.Type: GrantFiled: August 28, 1998Date of Patent: January 13, 2004Assignee: G. D. Searle & Co.Inventors: Nizal Chandrakumar, Michael Clare, Wendell Doubleday, Alan F. Gasiecki, Mark A. Russell
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Patent number: 6673788Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II: wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; wherein Y is selected from fluoroalkyl, and and wherein R9 is alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.Type: GrantFiled: November 25, 2002Date of Patent: January 6, 2004Assignee: G. D. Searle & Co.Inventors: Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
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Publication number: 20030229064Abstract: Dithiocarbamate, particularly tetraethylthiuram disulfide, and thiocarbamate anions strongly inhibit the growth of cancer cells of a variety of cell types. Such inhibitory effect is enhanced by heavy metal ions such as copper ions, cytokines and ceruloplasmin. A method is presented for using tetraethylthiuram disulfide to reduce tumor growth, and to potentiate the effect of other anticancer agents.Type: ApplicationFiled: March 3, 2003Publication date: December 11, 2003Applicant: Charlotte-Mecklenburg Hospital Authority d/b/a Carolinas Medical CenterInventor: Thomas Preston Kennedy
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Patent number: 6653309Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: October 30, 2000Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeffrey O. Saunders, Daniel Elbaum, Perry M. Novak, Douglas Naegele, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Catharine Frank, Dean P. Stamos, William Walters, David Pearlman
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Patent number: 6649591Abstract: In accordance with the present invention, there is provided a new class of drugs for therapeutic treatment of such indications as cerebral stroke and other ischemia/reperfusion injury. Thus, in accordance with the present invention, dithiocarbamates are linked to the surface of a non-immunogenic, non-targeting macromolecule other than an antibody (e.g., albumin protein) either by using cross-linking reagents or by nonspecific binding to produce polydithiocarbamate-macromolecule-containing compositions, which represent a new class of drugs for therapeutic treatment of such indications as cerebral stroke and other ischemia/reperfusion injury. In accordance with another aspect of the present invention, combinational therapeutic methods have been developed for the in vivo inactivation or inhibition of formation (either directly or indirectly) of species which induce the expression of inducible nitric oxide synthase, as well as reducing nitric oxide levels produced as a result of .NO synthase expression.Type: GrantFiled: October 1, 1999Date of Patent: November 18, 2003Assignee: Medinox, Inc.Inventor: Ching-San Lai
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Publication number: 20030203887Abstract: In accordance with the present invention, there are provided methods for the in vivo reduction of free radical levels in mammalian subjects in need thereof. In contrast to the inhibitory approach described in the prior art (i.e., wherein the function of the species responsible for free radical production is inhibited), the present invention employs a scavenging approach whereby overproduced free radical is bound in vivo to a suitable free radical scavenger. An exemplary free radical scavenger contemplated for use in the practice of the present invention is a dithiocarbamate-ferrous iron complex. This complex binds to free radicals, forming a stable, water-soluble free radical-containing complex. When administered to a subject afflicted with a disorder associated with free radical overproduction (e.g.Type: ApplicationFiled: May 7, 2003Publication date: October 30, 2003Applicant: MCW Research Foundation, Inc.,Inventor: Ching-San Lai
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Patent number: 6630509Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, which compounds have utility in treating clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: June 3, 2002Date of Patent: October 7, 2003Assignee: AstraZeneca ABInventors: Jonas Fägerhag, Lanna Li, Eva-Lotte Lindstedt Alstermark
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Publication number: 20030181495Abstract: The present invention provides novel combinations of dithiocarbamate disulfide dimers with other active agents. In one method, the disulfide derivative of a dithiocarbamate is coadministered with a thiazolidinedione for the treatment of diabetes. In another embodiment, In another embodiment, invention combinations further comprise additional active agents such as, for example, metformin, insulin, sulfonylureas, and the like. In another embodiment, the present invention relates to compositions and formulations useful in such therapeutic methods.Type: ApplicationFiled: March 21, 2003Publication date: September 25, 2003Applicant: Medinox, Inc.Inventors: Ching-San Lai, Vassil P. Vassilev
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Patent number: 6620798Abstract: Methods for the repair, reconstruction and protection of tissue using compositions containing flavonoids and/or flavonols, including simultaneous administration of agents in order to obtain synergistic effects from the combinations taught and claimed herein. The administration of the flavonols and /or flavonoids in conjuction with compositions containing vitamin C and/or salts and esters of vitamin C provides advantageous sparing of autocoids (internal steroids). The simultaneous administration of flavonols and /or flavonoids to compositions containing glucosamine and or glucosamine sulfate and chondroitin stimulates rapid improvement in joint function. The addition to the flavonoids and/or flavonols to previously administered compositions is a most convenient method of achieving enhanced benefits. The use of combinations of flavonoids and flavonols for use in relieving pain is also a part of the invention.Type: GrantFiled: June 6, 2000Date of Patent: September 16, 2003Inventor: Russell Jaffe
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Publication number: 20030134897Abstract: Compositions including an aromatic compound for inhibiting the production of exoproteins by Gram positive bacteria are disclosed.Type: ApplicationFiled: October 2, 2001Publication date: July 17, 2003Applicant: Kimberly-Clark Worldwide, Inc.Inventors: Rae Ellen Syverson, Richard A. Proctor
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Patent number: 6573297Abstract: A (2-substituted oxyphenyl)alkanamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C3-30 expressed by R1 and the other is —(CH2)n-NR2R3; Z is —CO— or —CONR6—; R2 and R3 individually represent H, lower alkyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members; wherein —CONR5—(CH2)n-NR2R3 or —CONR6—(CH2)n-NR2R3 may be the following Group (II): wherein ring Y is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, lower alkyl, lower acyl and etc; R5 and R6 are individually H, lower alkyl, lower acyl or lower alkylcarbamoyl, or may form a part of said Group(II); 1 is 0 or 1; m is 1 or 2; and n is an integer of 0-5.Type: GrantFiled: October 29, 2001Date of Patent: June 3, 2003Assignee: Shiseido Co., Ltd.Inventors: Koji Kobayashi, Hirotada Fukunishi, Tokuro Iwabuchi
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Publication number: 20030087840Abstract: In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or “DC”) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.Type: ApplicationFiled: June 18, 2002Publication date: May 8, 2003Applicant: Medinox, Inc.Inventors: Ching-San Lai, Tingmin Wang
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Patent number: 6548540Abstract: Dithiocarbamate, particularly tetraethylthiuram disulfide, and thiocarbamate anions strongly inhibit the growth of cancer cells of a variety of cell types. Such inhibitory effect is enhanced by heavy metal ions such as copper ions, cytokines and ceruloplasmin. A method is presented for using tetraethylthiuram disulfide to reduce tumor growth, and to potentiate the effect of other anticancer agents.Type: GrantFiled: December 12, 2000Date of Patent: April 15, 2003Assignee: Charlotte-Mecklenburg Hospital AuthorityInventor: Thomas Preston Kennedy
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Publication number: 20030065026Abstract: Dithiocarbamate, particularly tetraethylthiuram disulfide strongly inhibits the growth of cancer cells of a variety of cell types. Such inhibitory effect is enhanced by heavy metal ions such as copper ions, cytokines and ceruloplasmin. A method is presented for using tetraethylthiuram disulfide to reduce tumor growth, and to potentiate the effect of other anticancer agents.Type: ApplicationFiled: September 8, 1999Publication date: April 3, 2003Inventor: THOMAS P. KENNEDY
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Patent number: 6534541Abstract: The present invention is in particular related to the use of rivastigmine in the manufacture of a medicament for the treatment of ocular disorders.Type: GrantFiled: October 11, 2000Date of Patent: March 18, 2003Assignee: Novartis AGInventor: David Goldblum
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Publication number: 20030040511Abstract: In accordance with the present invention, there are provided methods for the in vivo reduction of free radical levels in mammalian subjects in need thereof. In contrast to the inhibitory approach described in the prior art (i.e., wherein the function of the species responsible for free radical production is inhibited), the present invention employs a scavenging approach whereby overproduced free radical is bound in vivo to a suitable free radical scavenger. An exemplary free radical scavenger contemplated for use in the practice of the present invention is a dithiocarbamate-ferrous iron complex. This complex binds to free radicals, forming a stable, water-soluble free radical-containing complex. When administered to a subject afflicted with a disorder associated with free radical overproduction, the water-soluble free radical-containing complex is produced and then filtered through the kidneys, concentrated in the urine, and eventually excreted by the subject, thereby reducing in vivo free radical levels.Type: ApplicationFiled: October 8, 2002Publication date: February 27, 2003Applicant: MCW Research Foundation, Inc.Inventor: Ching-San Lai
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Patent number: 6524564Abstract: The present invention relates to free-radically polymerizable, siloxane-containing urethane (meth)acrylates which comprise, in incorporated form, a) at least one compound which contains at least one active hydrogen atom and at least one free-radically polymerizable &agr;,&bgr;-ethylenically unsaturated double bond per molecule, b) at least one diisocyanate, c) at least one compound which contains two active hydrogen atoms per molecules, d) at least one compound which contains at least one active hydrogen atom and at least one siloxane group per molecule, to water-soluble or water-dispersible polymers which comprise these urethane (meth)acrylates in copolymerized form, to the use of these polymers, and to cosmetic compositions which comprise these polymers.Type: GrantFiled: February 14, 2001Date of Patent: February 25, 2003Assignee: BASF AktiengesellschaftInventors: Son Nguyen Kim, Axel Sanner, Volker Schehlmann
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Patent number: 6506794Abstract: An aqueous dispersion comprising a halopropargyl compound (HPC) and a partially hydrolysed polyvinyl alcohol (PHPVA). The aqueous dispersions are useful for inhibiting the growth of micro-organisms on or in a medium, especially an industrial medium such as paint films, metal working fluids, wood, latices and plastic materials.Type: GrantFiled: September 26, 2001Date of Patent: January 14, 2003Assignee: Avecia Inc.Inventors: Emerentiana Sianawati, John Edward Yates
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Patent number: 6500849Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: January 26, 1999Date of Patent: December 31, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: John Joseph Tegeler, Barbara Seavey Rauckman, Russell Richard Lee Hamer, Brian Scott Freed, Gregory Harold Merriman
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Patent number: 6498188Abstract: Methods for the treatment of cancers or viral infections in mammals are disclosed that include administration of an N-chlorophenylcarbamate, or an N-chlorophenylthiocarbamate, or a salt thereof. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: August 24, 2000Date of Patent: December 24, 2002Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6495538Abstract: The present invention provides methods and compositions comprising one or more zinc ionophores for protecting tissue from the harmful effects of apoptosis in patients in need thereof. Concentrations of zinc-pyrithione and diethyldithiocarbamate in the picomolar to nanomolar range have a strong protective effect against apoptosis.Type: GrantFiled: January 12, 2001Date of Patent: December 17, 2002Assignee: Zinc Therapeutics, Canada Inc.Inventor: Henry Fliss
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Publication number: 20020177583Abstract: Methods and compositions for altering the viability of cells, particularly cancers in animals and humans are disclosed. The compositions of the present invention are formed from a set of components comprising one or more of the following: a dithiocarbonyl, preferably dithiocarbamate, compound; a divalent metal ion; a modulator of cellular glutathione levels; and an inhibitor of the phosphorylation of choline. The compositions described herein induce a relatively selective and rapid effect on the viability of cancer cells by inducing a mixture of apoptotic and necrotic cell death, with the dominant pathway being apoptosis. Particularly preferred active compositions comprise all four components, although combinations of fewer components can be fully effective in certain tumors.Type: ApplicationFiled: May 24, 2001Publication date: November 28, 2002Inventor: Zoltan Kiss
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Publication number: 20020151540Abstract: The present invention provides a novel dithiocarbamamte disulfide dimer useful in various therapeutic treatments, either alone or in combination with other active agents. In one method, the disulfide derivative of a dithiocarbamate is coadministered with an agent that inactivates (or inhibits the production of) species that induce the expression of nitric oxide synthase to reduce the production of such species, while, at the same time reducing nitric oxide levels in the subject. In another embodiment, free iron ion levels are reduced in a subject by administration of a disulfide derivative of a dithiocarbamate(s) to scavenge free iron ions, for example, in subjects undergoing anthracycline chemotherapy. In another embodiment, cyanide levels are reduced in a subject by administration of a disulfide derivative of a dithiocarbamate so as to bind cyanide in the subject. In a further aspect, the present invention relates to compositions and formulations useful in such therapeutic methods.Type: ApplicationFiled: January 11, 2002Publication date: October 17, 2002Applicant: Medinox, Inc.Inventors: Ching-San Lai, Vassil Vassilev
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Patent number: 6444701Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: November 8, 2001Date of Patent: September 3, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini
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Patent number: 6414019Abstract: Novel synergistic fungicidal compositions used for protecting seeds, plants and other vegetative material against fungi contain a mixture of one or more compounds selected from group A and one or more compounds selected from group B. Compounds from group A are selected from Beta-Amino butyric acid and its N-benzoyl-octyl ester derivatives. Compounds from group B are selected from the group of fosetyl aluminum, dimethomorph, a mixture of folpet and ofurace (45:5), folpet fencaramid (Bayer SZX), mancozeb, cymoxynil, methalaxyl, the single optical isomer of metalaxyl, a mixture of cymoxamil and mancozeb (4:1), copper sulfate, copper hydroxide, copper sulfate hydrate, azoxystrobin, and acidenzolar-s-methyl.Type: GrantFiled: October 12, 1999Date of Patent: July 2, 2002Assignee: Agrogene Ltd.Inventors: Yigal Cohen, Moshe Korat, Dan Zvi-Tov
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Publication number: 20020082400Abstract: Chemically-defined, non-polymeric valency platform molecules and conjugates comprising chemically-defined valency platform molecules and biological or chemical molecules including polynucleotide duplexes of at least 20 base pairs that have significant binding activity-for human lupus anti-dsDNA autoantibodies.Type: ApplicationFiled: December 29, 2000Publication date: June 27, 2002Inventors: Stephen M. Coutts, David S. Jones, Douglas Alan Livingston, Lin Yu
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Patent number: 6407090Abstract: The present invention provides methods and compositions comprising one or more zinc ionophores for blocking apoptosis in patients in need thereof. Concentrations of zinc-pyrithione and diethyldithiocarbamate in the picomolar to nanomolar range have a strong protective effect against apoptosis.Type: GrantFiled: June 23, 2000Date of Patent: June 18, 2002Assignee: Zinc Therapeutics Canada, Inc.Inventor: Henry Fliss
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Publication number: 20020045573Abstract: In accordance with the present invention, there is provided a new class of drugs for therapeutic treatment of such indications as cerebral stroke and other ischemia/reperfusion injury. Thus, in accordance with the present invention, dithiocarbamates are linked to the surface of a non-immunogenic, non-targeting macromolecule other than an antibody (e.g., albumin protein) either by using cross-linking reagents or by nonspecific binding to produce polydithiocarbamate-macromolecule-containing compositions, which represent a new class of drugs for therapeutic treatment of such indications as cerebral stroke and other ischemia/reperfusion injury. In accordance with another aspect of the present invention, combinational therapeutic methods have been developed for the in vivo inactivation or inhibition of formation (either directly or indirectly) of species which induce the expression of inducible nitric oxide synthase, as well as reducing nitric oxide levels produced as a result of .NO synthase expression.Type: ApplicationFiled: October 1, 1999Publication date: April 18, 2002Inventor: CHING-SAN LAI
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Patent number: 6369073Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: October 2, 2000Date of Patent: April 9, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini
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Patent number: 6344472Abstract: A fungicidal composition comprising a compound A having the formula: wherein M is an oxygen or sulphur atom, n is 0 and 1, and Y is a fluorine or chlorine atom or a methyl radical; and at least one fungicidal compound B. A method for preventing or controlling phytopathogenic fungi on crops by applying an effective and non-plant-poisonous amount of said compound on the exposed parts of the plants is also disclosed.Type: GrantFiled: April 18, 2000Date of Patent: February 5, 2002Assignee: Rhone-Poulenc, Inc.Inventor: Marie-Pascale Latorse
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Patent number: 6344485Abstract: Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.Type: GrantFiled: June 18, 1999Date of Patent: February 5, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker
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Patent number: 6331531Abstract: Method for controlling harmful organisms in genetically modified cotton plants which contain a gene derived from Bacillus thuringiensis which encodes and expresses an insecticidally active protein, which comprises applying an insecticisally effective amount of one or more compounds from the following groups and a-f, described herein, to the plants, to their seeds or propagation stock and/or to the area in which they are cultivated. The method according to the invention makes it possible to reduce the application rate of crop protection agents which act synergistically with the transgenic plants, and also to increase and widen the efficacy of the transgenic plants, and therefore offers both economical and ecological advantages.Type: GrantFiled: June 3, 1999Date of Patent: December 18, 2001Assignee: Aventis CropScience GmbHInventor: Manfred Kern
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Patent number: 6329424Abstract: A phytomicrobicidal composition comprising such an amount of at least two active ingredient components that a synergistic effect is achieved, together with a suitable carrier material, wherein component I is a compound of the formula I in which: X is CH or N; R is CH3 or cyclopropyl; Y is H, F, Cl, Br, CF3, CF3O, propargyloxy; Z is H, F, Cl, CF3, CF3O; or Y and Z together are a methylenedioxy, a (difluoromethylene)dioxy, an ethylenedioxy, a (trifluoroethylene)dioxy or a benzo group; and wherein component II is a compound selected from the group consisting of II A) metalaxyl, II B) R-metalaxyl, II C) furalaxyl, II D) benalaxyl, II E) ofurace, II F) oxadixyl, II G) cymoxanil and II H) mancozeb.Type: GrantFiled: October 29, 1999Date of Patent: December 11, 2001Assignee: Bayer AktiengesellschaftInventors: Gertrude Knauf-Beiter, Ronald Zeun
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Patent number: 6309633Abstract: The invention provides a drug-oligomer conjugate having the following general formula: wherein D is a therapeutic drug moiety; H and H′ are each a hydrophilic moiety, independently selected from the group consisting of straight or branched PEG polymers having from 2 to 130 PEG subunits, and sugars; L is a lipophilic moiety selected from the group consisting of alkyl groups having 2-26 carbon atoms, cholesterol, adamantane and fatty acids; o is a number from 1 to the maximum number of covalent bonding sites on H; m+n+p together have a value of at least one and not exceeding the total number of covalent bonding sites on D for the —H′, —L and —H—L substituents; the H—L bond(s) are hydrolyzable and the D—L′ bond(s), when present, are hydrolyzable; the conjugate being further characterized by one of the following: (i) m is 0 and p is at least 1; (ii) n is 0 and p is at least 1; (iii) m and n are each 0 and p is at least 1; (iv) p isType: GrantFiled: June 19, 1999Date of Patent: October 30, 2001Assignee: Nobex CorporationInventors: Nnochiri Ekwuribe, Muthukumar Ramaswamy, Jayanthi Sethuraman Rajagopalan
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Patent number: 6303649Abstract: A compound of formula (I), wherein R1 is carboxy or protected carboxy, R2 and R3 are each independently hydrogen, hydroxy, or protected hydroxy, R4 is hydrogen or halogen, R5 is aryl substituted with halogen, amino, hydroxy or protected hydroxy, R6 is aryl optionally substituted with halogen, amino, hydroxy or protected hydroxy, A1 and A2 are each independently lower alkylene, and (II) is (III), (IV), (V) or (VI) or its salt, process for preparing it, a pharmaceutical composition including it, and a use thereof.Type: GrantFiled: August 4, 2000Date of Patent: October 16, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kouji Hattori, Hiromichi Itani, Akira Tanaka, Toshifumi Shiraga
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Publication number: 20010021378Abstract: There are described a flowable composition for controlling harmful insects and representatives of the order Acarina, comprising at least one pesticidally active compound, one or more signal substances selected from the group consisting of pheromones, kairomones and attractants, a UV absorber or a UV absorber mixture and, if appropriate, one or more additives selected from the group consisting of viscosity-regulating thickeners, fillers, solvents and other formulation auxiliaries,Type: ApplicationFiled: February 22, 2001Publication date: September 13, 2001Inventors: Dieter Hofer, Max Angst, Pierre-Joseph Charmillot
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Patent number: 6248762Abstract: When used in admixture with mancozeb, chlorothalonil, a copper salt, folpet, fluazinam or cymoxanil (it being possible for the latter to be used also together with one of the other five components), metalaxyl having a high R-enantiomer content of more than 70% by weight, or pure R-metalaxyl, exhibits a markedly increased fungicidal action against plant diseases as compared with a similar mixture in which metalaxyl is used in the form of the racemate.Type: GrantFiled: May 17, 2000Date of Patent: June 19, 2001Assignee: Syngenta Investment CorporationInventors: Cosima Nuninger, John Edward Nicholas Goggin, Dino Sozzi
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Patent number: 6172094Abstract: A composition comprising effective amounts of a) a carbamate of the formula I where X is CH or N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different if n is 2, and b) a dithiocarbamate (II) selected from the group consisting of manganese ethylenebis(dithiocarbamate) (zinc complex) (IIa), manganese ethylenebis(dithiocarbamate) (IIb), zinc ammoniate ethylenebis(dithiocarbamate) (IIc) and zinc ethylenebis(dithiocarbamate) (IId) and optionally c) 1-(2-cyano-2-methoxyiminoacetyl)-3-ethylurea (III) H3CCH2—NHCONH—CO—C(CN)═NOCH3 (III) which exhibits a synergistically enhanced fungicidal effect is described.Type: GrantFiled: October 22, 1998Date of Patent: January 9, 2001Assignee: BASF AktiengesellschaftInventors: Bernd M{umlaut over (u)}ller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Maria Scherer, Klaus Schelberger, Joachim Leyendecker
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Patent number: 6124349Abstract: The present invention provides methods for producing pharmaceutical-grade particulate dithiocarbamates from secondary amines by vigorously contacting at least one secondary amine and a pharmaceutically acceptable diluent that is a solvent for the carbon disulfide, but not for the secondary amine in an inert gas atmosphere, cooling the mixture so as to precipitate the dithiocarbamate therefrom, and separating the precipitated dithiocarbamate from the cooled mixture. The preferred solvent contains absolute ethanol. In alternative embodiments, the invention further provides methods for purifying a dithiocarbamate to obtain a pharmaceutical-grade dithiocarbamate particulate from a dithiocarbamate feed and methods for producing a sterile pharmaceutical-grade dithiocarbamate from a dithiocarbamate feed.Type: GrantFiled: February 18, 1999Date of Patent: September 26, 2000Assignee: Medinox, Inc.Inventors: Vassil P. Vassilev, Wei-Cheng Liaw, Ching-San Lai
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Patent number: 6114378Abstract: A fungicidal mixture comprisinga) an oxime ether of the formula I ##STR1## where the substituents have the following meaning: X is oxygen or amino (NH);Y is CH or N;Z is oxygen, sulfur, amino (NH) or C.sub.1 -C.sub.4 -alkylamino (N--C.sub.1 -C.sub.4 -alkyl);R' is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -haloalkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -haloalkynyl, C.sub.3 -C.sub.6 -cycloalkylmethyl, or benzyl which may be partially or fully halogenated and/or may carry one to three of the following radicals: cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy and C.sub.1 -C.sub.Type: GrantFiled: October 21, 1998Date of Patent: September 5, 2000Assignee: BASF AktiengesellschaftInventors: Ruth Muller, Herbert Bayer, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, Maria Scherer