Nitrogen Containing Patents (Class 514/471)
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Patent number: 7179840Abstract: This invention relates to novel furancarboxamides of the formula (I) in which R, R1 and m are as defined in the disclosure, to a plurality of processes for preparing these substances and to their use for controlling unwanted micro-organisms.Type: GrantFiled: May 15, 2003Date of Patent: February 20, 2007Assignee: Bayer CropScience AGInventors: Heiko Rieck, Ralf Dunkel, Hans-Ludwig Elbe, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck
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Patent number: 7176201Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which theyType: GrantFiled: October 7, 2003Date of Patent: February 13, 2007Assignees: The Regents of the University of California, Universita Degli Studi di Parma, Universita Degli Studi di UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Patent number: 7160923Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: November 14, 2000Date of Patent: January 9, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7160916Abstract: This invention features a method for enhancing bone growth or inhibiting bone resportion. The method includes administering to a subject in need thereof a compound of the following formula: A is H, R, or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, halogen, R, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3.Type: GrantFiled: September 1, 2004Date of Patent: January 9, 2007Assignee: Yung Shin Pharmaceutical Ind. Co., Ltd.Inventors: Wen-Mei Fu, Chih-Hsin Tang, Rong-Sen Yang, Che-Ming Teng, Sheng-Chu Kuo, Fang-Yu Lee
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Patent number: 7157078Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: February 2, 2004Date of Patent: January 2, 2007Assignee: The University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garren, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Patent number: 7157604Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: August 9, 2002Date of Patent: January 2, 2007Assignee: Merck & Co., Inc.Inventors: Dongfang Meng, Dann LeRoy Parker, Jr., Robert R. Wilkening, Ronald W. Ratcliffe
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7148225Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: November 19, 2004Date of Patent: December 12, 2006Assignee: Neurogen CorporationInventors: Yang Gao, Alan J. Hutchinson, Wallace C. Pringle, Taeyoung Yoon, He Zhao
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Patent number: 7135499Abstract: The present invention relates to novel insecticidally and acaricidally active compound combinations of N2-[1,1-dimethyl-2-(methylsulphonyl)ethyl]-3-iodo-N1-{2-methyl-4-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl}phthalamide of the formula (I) and active compounds identified in the disclosure.Type: GrantFiled: October 6, 2003Date of Patent: November 14, 2006Assignee: Bayer CropScience AGInventors: Jörg Konze, Wolfram Andersch, Dietrich Stübler, Rüdiger Fischer
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Patent number: 7132445Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: GrantFiled: July 30, 2003Date of Patent: November 7, 2006Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Jr., Laura L. Rokosz, James P. Jakway, Gaifa Lai, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
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Patent number: 7132441Abstract: This invention is in the field of a combination comprising a therapeutically-effective amount of a cyclooxygenase-2 inhibitor, a 5-lipoxygenase inhibitor and an immunosuppressive drug selected from antiproliferative agents, antiinflammatory-acting compounds and inhibitors of leukocyte activation. This combination may be used, for example, to suppress the immune response associated with organ transplantation, graft versus host disease, and conditions with underlying autoimmune or inflammatory reactivities or responses.Type: GrantFiled: March 15, 2002Date of Patent: November 7, 2006Assignee: G.D. Searle & Co.Inventors: Susan A. Gregory, Peter C. Isakson, Gary Anderson
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Patent number: 7132448Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative or a chloronicotinyl insecticide and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: August 3, 2004Date of Patent: November 7, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Albert Ahn, Richard Fisher, Christine M. Monro, Pierre R. Joseph
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Patent number: 7129238Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.Type: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 7122571Abstract: Compounds useful as inhibitors of cyclooxygenase-2 activity have the formulae I or Ia: wherein: Q1, Q2, n, m, X, Y and R are as defined herein.Type: GrantFiled: December 10, 2002Date of Patent: October 17, 2006Assignee: Temple University - Of The Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M.V. Ramana Reddy
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Patent number: 7115758Abstract: The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.Type: GrantFiled: November 26, 2002Date of Patent: October 3, 2006Assignee: Schering AGInventors: Andreas Steinmeyer, Katica Schwarz, Claudia Giesen, Martin Haberey, Marianne Fähnrich
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7105545Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkyType: GrantFiled: April 2, 2002Date of Patent: September 12, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Walter Kunz, Clemens Lamberth, Fredrik Cederbaum, Martin Zeller
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7101912Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.Type: GrantFiled: December 8, 2003Date of Patent: September 5, 2006Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Kenneth C. Cundy, Jianhua Li, Feng Xu, Cindy X. Zhou, Laxminarayan Bhat
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Patent number: 7094414Abstract: The present invention exhibits a remarkable effect of making it possible to provide a famotidine injection solution containing famotidine at a high concentration, being stable for a long period of time at room temperature, and having a low viscosity without impairing the absorption of famotidine, which can be hardly provided so far.Type: GrantFiled: December 20, 2001Date of Patent: August 22, 2006Assignee: Astellas Pharma Inc.Inventors: Katsunori Nakata, Hiroshi Yatabe, Tsukasa Nishikawahara
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Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
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Patent number: 7094806Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.Type: GrantFiled: June 10, 2004Date of Patent: August 22, 2006Assignee: Trustees of Tufts CollegeInventors: Mark L. Nelson, Darrell J. Koza, Glen Rennie
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Patent number: 7087639Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.Type: GrantFiled: January 20, 2004Date of Patent: August 8, 2006Assignee: LKT Laboratories, Inc.Inventors: Luke K. T. Lam, Nayaz Ahmed
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Patent number: 7078400Abstract: 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: GrantFiled: July 1, 2003Date of Patent: July 18, 2006Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 7078435Abstract: Autoinducer compounds which enhance gene expression in a wide variety of microorganisms, therapeutic compositions and therapeutic methods wherein gene expression within microorganisms is regulated are disclosed.Type: GrantFiled: October 10, 2003Date of Patent: July 18, 2006Assignee: Montana State UniversityInventor: Tom Livinghouse
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Patent number: 7067542Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: July 10, 2002Date of Patent: June 27, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert A. Chrusciel
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Patent number: 7060718Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: March 11, 2003Date of Patent: June 13, 2006Assignee: Amgen Inc.Inventor: Jonathan B. Houze
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Patent number: 7056946Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: November 24, 2003Date of Patent: June 6, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7053109Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: July 10, 2002Date of Patent: May 30, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Patent number: 7049334Abstract: A method for enhancing learning and memory or treating amnesia. The method includes administrating to a subject in need thereof a compound of the formula (I): A is H, R, or ?each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, nitro, halogen, R, OH, OR, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, ROC(O)R?OH, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3. The compound is in an effective amount for enhancing learning and memory or treating amnesia.Type: GrantFiled: September 13, 2002Date of Patent: May 23, 2006Assignee: Carlsbad Technology, Inc.Inventors: Wen-Mei Fu, Keng-Chen Liang, Wei-Lin Chien, Sheng-Chu Kuo, Fang-Yuan Lee, Che-Ming Teng
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Patent number: 7049308Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.Type: GrantFiled: September 27, 2001Date of Patent: May 23, 2006Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
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Patent number: 7045551Abstract: The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, R7 and A are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said aryl hydroxyethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: May 16, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Li-Qiang Sun, Huan He, Alexandre L'Heureux
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Patent number: 7045532Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.Type: GrantFiled: October 31, 2001Date of Patent: May 16, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown, Michael Patane, Vivek J. Kadambi, Michael Solomon, Alain Stricker-Krongrad
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Patent number: 7041702Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
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Patent number: 7034015Abstract: 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: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7034053Abstract: The present invention disclosed compounds of Formula I. The present invention also discloses beta-3 agonists of formula I and methods for treating beta-3 mediated diseases and condition using the compounds of formula I, in particular methods for treating diabetes or obesity.Type: GrantFiled: December 17, 2001Date of Patent: April 25, 2006Assignee: SmithKline Beecham CorporationInventors: David N. Deaton, Barry George Shearer, David Edward Uehling
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Patent number: 7026351Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.Type: GrantFiled: March 20, 2003Date of Patent: April 11, 2006Assignee: Xenoport, Inc.Inventors: Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 7012094Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: April 19, 1995Date of Patent: March 14, 2006Assignee: G.D. Searle, LLCInventors: Stephen R. Bertenshaw, John J. Talley
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Patent number: 6992104Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: December 22, 2003Date of Patent: January 31, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6989383Abstract: The present invention relates to methods of treating cancer using a combination of a compound which is an antineoplastic agent and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at lest two therapeutic agents selected from a group consisting of a compound which is an antineoplastic agent and a compound which is an inhibitor or prenyl-protein transferase. The invention also relates to methods of preparing such compositions.Type: GrantFiled: June 4, 1998Date of Patent: January 24, 2006Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Neal Rosen, Laura Sepp-Lorenzino, Mark M. Moasser, Allen I. Oliff, Jackson B. Gibbs, Nancy Kohl, Samuel L. Graham, George C. Prendergast
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Patent number: 6984662Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: November 3, 2003Date of Patent: January 10, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Christine M. Monro, Pierre R. Joseph, Albert Ahn, Richard Fisher
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Patent number: 6982279Abstract: Compounds of the formulae IA and Ib. in which X, R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel antiarrhythmic active compounds, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: GrantFiled: December 12, 2001Date of Patent: January 3, 2006Assignee: Aventis Pharm Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Patent number: 6958416Abstract: The invention relates to derivatives of valproyltaurinamide of formula (I) in which R1 and R2 are independently hydrogen, a C1-C6-alkyl group, an arylalkyl group or an aryl group. The derivatives are especially useful for the treatment of epilepsy, affective illness, cognitive disorders, neurodegenerative disease, neuropathic pain syndrome, migraine, stroke, brain ischemia, or head trauma injury.Type: GrantFiled: March 5, 2002Date of Patent: October 25, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Meir Bialer, Boris Yagen, Nina Isoherranen
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Patent number: 6949567Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.Type: GrantFiled: February 26, 2002Date of Patent: September 27, 2005Assignee: 4SC AGInventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
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Patent number: 6936602Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.Type: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
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Patent number: 6936627Abstract: The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent.Type: GrantFiled: October 29, 2002Date of Patent: August 30, 2005Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, Chia-En Lin, Tiansheng Wang
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Patent number: 6916956Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.Type: GrantFiled: August 10, 2001Date of Patent: July 12, 2005Assignee: Japan Tobacco, Inc.Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
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Patent number: 6916481Abstract: The invention relates to an active substance vector multiparticulate system and to the production and use thereof. The object of the invention is an active-substance vector multiparticulate system comprising one or several active substances included in a hydrophilic organic matrix comprising at least one hydrosoluble and/or hydrodispersable anionic polymer which is insolubilized by a metallic cation. The invention can be specifically used in the food industry, detergents and agrochemistry.Type: GrantFiled: April 12, 2000Date of Patent: July 12, 2005Assignees: Aventis CropScienceInventors: Christian Prud'Homme, Etienne Fleury, Jean-Paul Michalon, Robert Zerrouk