Benzene Ring Containing Patents (Class 514/107)
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Patent number: 6645774Abstract: This invention provides methods of modifying feeding behavior, including increasing or decreasing food consumption, e.g., in connection with treating obesity, bulimia or anorexia. These methods involve administration of compounds that are selective agonists or antagonists for the Y5 receptor. One such compound has the structure: In addition, this invention provides an isolated nucleic acid molecule encoding a Y5 receptor, an isolated Y5 receptor protein, vectors comprising an isolated nucleic acid molecule encoding a Y5 receptor, cells comprising such vectors, antibodies directed to the Y5 receptor, nucleic acid probes useful for detecting nucleic acid encoding Y5 receptors, antisense oligonucleotides complementary to any unique sequences of a nucleic acid molecule which encodes a Y5 receptor, and nonhuman transgenic animals which express DNA encoding a normal or a mutant Y5 receptor.Type: GrantFiled: November 23, 1999Date of Patent: November 11, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Christophe P. G. Gerald, Richard L. Weinshank, Mary W. Walker, Theresa Branchek
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Patent number: 6579860Abstract: An interleukin-6 production inhibitor is provided containing a methanebisphosphonic acid derivative as an active component, which has inhibitory effects on interleukin-6 production and is useful in prevention and treatment of diseases due to abnormal production of the interleukin-6. This pharmaceutical is anticipated to have effects in prevention and treatment of diseases related to the interleukin-6, for example, thrombocytosis, inflammatory diseases, abnormal immune response diseases, osteoporosis, rheumatoid arthritis, hypercalcemia, multiple myeloma, cachexia, and nephritis.Type: GrantFiled: September 27, 2000Date of Patent: June 17, 2003Assignee: Toray Industries, Inc.Inventors: Junzo Koike, Yuriko Funaba, Masahiko Tanahashi, Seiji Okazaki, Masatoshi Ito
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Patent number: 6558702Abstract: The present invention relates to a method for the sustained release in vivo of a biologically active agent comprising administering to a subject in need of treatment an effective amount of a sustained release composition comprising a biocompatible polymer having the biologically active agent incorporated therein, and a bisphosphonate wherein the bisphosphonate compound is present in an amount sufficient to modify the release profile of the biologically active agent from the sustained release composition. Pharmaceutical compositions suitable for use in the method of the invention are also disclosed.Type: GrantFiled: April 13, 2001Date of Patent: May 6, 2003Assignee: Alkermes Controlled Therapeutics, Inc.Inventors: James R. Dasch, M. Gary I. Riley
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Patent number: 6509324Abstract: Compounds able to chelate bi- and trivalent paramagnetic metal ions, their chelated complexes with these metal ions and physiologically compatible salts thereof and therein magnetic resonance imaging.Type: GrantFiled: September 24, 2001Date of Patent: January 21, 2003Assignee: Bracco S.p.A.Inventors: Maurizio Franzini, Andrea Beltrami, Luisella Calabi, Alessandro Maiocchi, Mario Virtuani, Pier Lucio Anelli, Kondareddiar Ramalingam, Ramachandran S. Ranganathan
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Patent number: 6506733Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.Type: GrantFiled: March 15, 2000Date of Patent: January 14, 2003Assignee: Axys Pharmaceuticals, Inc.Inventors: Ann M. Buysse, Rohan V. Mendonca, James T. Palmer, Zong-Qiang Tian, Shankar Venkatraman
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Patent number: 6498151Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.Type: GrantFiled: March 21, 2001Date of Patent: December 24, 2002Assignee: Merck Frosst Canada & Co.Inventors: Chun Sing Li, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Cheuk Kun Lau, Patrick Roy, Michel Therien, Zhaoyin Wang, Claude Dufresne, Rejean Fortin
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Publication number: 20020156301Abstract: Triphenylmethane derivatives represented by the general formula: 1Type: ApplicationFiled: February 11, 2002Publication date: October 24, 2002Applicant: Sumitomo Chemical Co., Ltd.Inventors: Hideo Kaneko, Yoshitaka Tomigahara, Norihisa Ooe, Haruyuki Matsunaga, Iwao Nakatsuka
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Patent number: 6284730Abstract: The invention relates to a combined pharmaceutical preparation comprising parathyroid hormone and a bone resorption inhibitor, said preparation being adapted for (a) the administration of parathyroid hormone during a period of approximately 6 to 24 months; (b) after the administration of parathyroid hormone has been terminated, the administration of a bone resorption inhibitor during a period of approximately 12 to 36 months.Type: GrantFiled: August 14, 1998Date of Patent: September 4, 2001Assignee: NPS Allelix Corp.Inventors: John Dietrich, Sverker Ljunghall, Sven Sjögren
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Patent number: 6214812Abstract: Bisphosphonate conjugates capable of releasing antibacterial and/or cytotoxic components upon binding with bone tissue. Such conjugates are useful in the treatment and prevention of bone cancer, bone infections and other bone-related diseases. Bisphosphonate conjugates are also delivery vehicles for use in delivering pharmaceutical compositions to bone tissue. Methods of synthesizing novel bisphosphonates and pharmaceutical compositions incorporating the same, and medical uses for such compositions, are provided. Compositions of the present invention include bone-seeking radio isotope conjugates for use in imaging and therapy.Type: GrantFiled: April 1, 1999Date of Patent: April 10, 2001Assignee: MBC Research, Inc.Inventors: Marat Karpeisky, Nelly Padioukova, Sergey Mikhailov, H. B. F. Dixon, Grigorii Tzeitline
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Patent number: 6207655Abstract: The present invention relates to conjugates of 3-carboxy-4,4′-dihydroxyphosphorylbutenoic acids with alkylating agents, derivatives are endowed with marked antitumor activity, especially against multiple myeloma. The present invention relates as well to a process for the preparation thereof and to pharmaceutical compositions containing them.Type: GrantFiled: January 13, 2000Date of Patent: March 27, 2001Assignee: Novuspharma S.p.A.Inventors: Valeria Livi, Silvano Spinelli, Marco Conti, Simonetta D'Alo', Ernesto Menta
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Patent number: 6200961Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.Type: GrantFiled: December 16, 1998Date of Patent: March 13, 2001Assignee: Aquatrols Corporation of America, Inc.Inventors: Stanley J. Kostka, Rennan Pan
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Patent number: 6174874Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.Type: GrantFiled: September 17, 1999Date of Patent: January 16, 2001Assignee: Merck Frosst Canada & Co.Inventors: Zhaoyin Wang, Claude Dufresne, Yves Leblanc, Chun Sing Li, Jacques Y. Gauthier, Cheuk K. Lau, Michel Therien, Patrick Roy
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Patent number: 6127350Abstract: A method of treating or preventing neoplastic disease and a method of preventing transformation of a normal cell into a tumor cell by mutated ras activities, utilizing a compound of formula I are disclose.Type: GrantFiled: January 28, 1998Date of Patent: October 3, 2000Assignee: Symphar S.A.Inventors: Eric Niesor, Craig Leigh Bentzen, Lan Mong Nguyen, Jean-Luc Thuillard, Hieu Trung Phan, Jean Flach
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Patent number: 6121253Abstract: This invention relates to prostaglandin-bisphosphonate conjugates. These conjugates are effective for treating or preventing bone diseases such as osteoporosis. These conjugates simultaneously deliver a prostaglandin agent for increasing bone formation and a bisphosphonate agent for inhibiting bone resorption.Type: GrantFiled: November 15, 1999Date of Patent: September 19, 2000Assignee: Merck Frosst Canada & Co.Inventors: Yongxin Han, Robert N. Young, Laurent Gil, Rejean Ruel
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Patent number: 6114340Abstract: An improved fungicidal composition is a mixture of (a) fungicide used to combat phytopathogenic fungi and (b) at least one phosphonate or phosphinate of formula R.sup.1 R.sup.2 P(O)OR.sup.3 where R.sup.1 is C.sub.6-20 alkyl, C.sub.6-20 alkoxy or optionally substituted phenyl, R.sup.2 is benzyl, C.sub.6-20 alkyl optionally interrupted by NH or O, di-C.sub.6-20 alkylamino or the group --CH.sub.2 CH.sub.2 --R.sup.1 P(O)OR.sup.3, and R.sup.3 C.sub.6-20 alkyl. Some of the compounds of formula (I) are novel.Type: GrantFiled: February 3, 1999Date of Patent: September 5, 2000Assignee: AgrEvo UK LimitedInventors: Hans-Jerg Kleiner, Martin Mach, Heinz Hagemeister, Dieter Regnat, Herbert Buschhaus, Hans-Peter Jende, David Stock, Geoffrey Gower Briggs
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Patent number: 6114316Abstract: Tissue-destructive conditions related to excess protemase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.Type: GrantFiled: September 2, 1999Date of Patent: September 5, 2000Assignee: Research Foundation of S.U.N.Y.Inventors: Nungavarm S. Ramamurthy, Lorne M. Golub, Timo A. Sorsa, Olli P. Teronen, Tuula A. Salo
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Patent number: 6096730Abstract: Phosphonic acid agents are synthesized and characterized which are potent inhibitors of angiogenesis, tumorigenesis and metalloproteinase activity. Their method of use for the inhibition of angiogenesis and metalloproteinase and the treatment of tumors is also shown.Type: GrantFiled: July 23, 1998Date of Patent: August 1, 2000Assignee: University of Kentucky Research FoundationInventors: Delwood C. Collins, Antonio R. Gagliardi, Peter Nickel
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Patent number: 6008205Abstract: The present invention is directed to presqualene diphosphate (PSDP) analogs having an active region of natural PSDP and a metabolic transformation region resistant to rapid intracellular inactivation in vivo. For example, PSDP and its stable analogs can inhibit neutrophil signal transduction events in cellular activation that result in the generation of active oxygen species, regulation of leukocyte adherence, both homotypic (leukocyte-leukocyte) or heterotypic adherence with leukocytes and epithelial cells of mucosal origin or endothelial cells of vascular origin. These analogs can also be used to regulate leukocyte-dependent tissue injury.Type: GrantFiled: April 4, 1997Date of Patent: December 28, 1999Assignee: The Brigham & Women's Hospital, Inc.Inventors: Charles N. Serhan, Bruce D. Levy
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Patent number: 5998390Abstract: Tissue-destructive conditions related to excess proteinase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.Type: GrantFiled: September 28, 1998Date of Patent: December 7, 1999Assignee: The Research Foundation of State University of New YorkInventors: Nungavarm S. Ramamurthy, Lorne M. Golub, Timo A. Sorsa, Olli P. Teronen, Tuula A. Salo
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Patent number: 5962438Abstract: A novel estrogen derivative represented by the formula: ##STR1## is useful for treating or preventing diseases caused by estrogen deficiency.Type: GrantFiled: October 17, 1997Date of Patent: October 5, 1999Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Michihiro Yamamoto, Akira Sasaki, Takashi Katsumata, Naomi Tsushima, Hideyuki Harada
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Patent number: 5935945Abstract: A method of treating or preventing supraventricular tachyarrhythmias is disclosed which comprises the use of a compound which selectively blocks the ultra-rapidly-activating delayed rectifier K.sup.+ current (I.sub.Kur) of the human atrium.Type: GrantFiled: October 28, 1997Date of Patent: August 10, 1999Assignee: Merck & Co., Inc.Inventors: Joseph J. Lynch, Jr., Richard J. Swanson, Joseph J. Salata, Bernard Fermini
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Patent number: 5843993Abstract: A complex and method for making same for use as a diagnostic or therapeutic pharmaceutical includes a ligand comprising at least one hydroxyalkyl phosphine donor group bound to a gold atom to form a gold-ligand complex that is stable in aqueous solutions containing oxygen, serum and other body fluids.Type: GrantFiled: March 14, 1997Date of Patent: December 1, 1998Assignee: The Curators of the University of MissouriInventors: Kattesh V. Katti, Douglas E. Berning, Wynn A. Volkert, Alan R. Ketring
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Patent number: 5824661Abstract: Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N;(c) Q is covalent bond; O; or S;(d) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is C.sub.1 -C.sub.8 alkyl;(e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims.are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.Type: GrantFiled: September 7, 1994Date of Patent: October 20, 1998Assignee: The Procter & Gamble CompanyInventors: Marion David Francis, Susan Mary Kaas, Frank Hallock Ebetino
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Patent number: 5712261Abstract: A method is provided for preventing and/or treating hypertriglyceridemia, and/or atherosclerosis and/or pancreatitis resulting from hypertriglyceridemia, employing a squalene synthetase inhibitor.Type: GrantFiled: June 21, 1995Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5683992Abstract: The present invention relates to a methanediphosphonate derivative, its manufacturing process, and pharmaceutical applications, that is represented with the following formula: ##STR1## wherein, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2, or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to carbon atoms or pharmaceutically allowable cations. .function.The compounds of the present invention have excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and are useful as antiinflammatory agents, antirheumatic agents, bone metabolic disease drugs, autoimmune disease drugs, or osteoporosis drugs.Type: GrantFiled: March 15, 1996Date of Patent: November 4, 1997Assignee: Toray Industries, Inc.Inventors: Norio Kawabe, Hiromi Uchiro, Teruo Nakadate, Masahiko Tanahashi, Masatoshi Ito
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Patent number: 5670493Abstract: A compound of formula (I): ##STR1## in which: R.sub.1, R.sub.2, which may be identical or different, represent hydrogen or halogen, or alkyl, alkoxy, nitro or trihalomethyl,X represents CO, SO.sub.2 or CH.sub.2,A.sub.1 represents any one of the groups as defined in the description,A.sub.2 represents --(CH.sub.2).sub.n or --CH.dbd.CH--,R.sub.3, R.sub.4, which may be identical or different, represent hydrogen or alkyl,its isomers as well as its addition salts with a pharmaceutically acceptable base and medicinal product containing the same are useful as angiogenesis inhibitors.Type: GrantFiled: July 19, 1996Date of Patent: September 23, 1997Assignee: Adir et CompagnieInventors: Alex Cordi, Patrice Desos, Angela D. Morris, Ghanem Atassi
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Patent number: 5661139Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a bis-(2-aryl)hydrazone capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Alteon Inc.Inventors: Michael E. Lankin, David H. Shih, Dilip R. Wagle, San-Bao Hwang
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Patent number: 5624917Abstract: There is provided a squalene inhibitory composition containing a 1,1-bisphosphonic acid compound, a lower alkyl ester thereof, or a salt thereof, which is useful for treating hypercholesterolemia. There are also provided novel compounds having squalene synthetase inhibitory activity and a pharmaceutical composition for treating hypercholesterolemia containing a 1,1-bisphosphonic compound, a lower alkyl ester thereof or a salt thereof.Type: GrantFiled: January 16, 1996Date of Patent: April 29, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kazuaki Kitano, Takashi Sohda, Ryuichi Tozawa, Hitoshi Ikeda, Tsuneo Oda
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Patent number: 5616571Abstract: Bisphosphonate, particularly alendronate, can prevent or treat bone loss associated with immunosuppressive therapy, whether or not the immunosuppressive therapy is associated with an organ transplant.Type: GrantFiled: June 6, 1995Date of Patent: April 1, 1997Assignee: Merck & Co., Inc.Inventors: Anastasia G. Daifotis, Ashley J. Yates
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Patent number: 5593980Abstract: This invention provides a new use of acids, esters, and salts of arylmethylphosphonates of Formula I, ##STR1## or a phosphonic acid of Formula II ##STR2## and derivatives as anti-inflammatory and anti-arthritic agents. Representative compounds include 4-dodecyloxybenzylphosphonic acid dimethyl ester, (2-naphthalenylmethyl)phosphonic acid dimethyl ester, and ([1,1'-biphenyl]-2-ylmethyl)phosphonic acid dimethyl ester.Type: GrantFiled: November 13, 1995Date of Patent: January 14, 1997Assignee: The Upjohn CompanyInventor: Roy A. Johnson
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Patent number: 5583124Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.Type: GrantFiled: June 6, 1995Date of Patent: December 10, 1996Assignee: Rohm and Haas CompanyInventors: Richard M. Jacobson, Luong T. Nguyen
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Patent number: 5543561Abstract: Compounds of the formula I ##STR1## in which R.sup.1 signifies hydrogen, a straight-chained, branched, saturated or unsaturated alkyl radical with 1-9 carbon atoms possibly substituted by phenyl or a phenyl ring which is possibly substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 -alkoxy or halogen, R.sup.2 signifies hydrogen or C.sub.1 -C.sub.3 -alkyl, whereby the two radicals can be the same or different, R represents hydrogen or a straight-chained or branched alkyl radical with 1-4 carbon atoms, X signifies an alkylene chain with 1-6 carbon atoms which can be substituted one or more times by C.sub.1 -C.sub.Type: GrantFiled: March 28, 1995Date of Patent: August 6, 1996Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Frieder Bauss
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Patent number: 5536711Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.Type: GrantFiled: June 6, 1995Date of Patent: July 16, 1996Assignee: Rohm and Haas CompanyInventors: Richard M. Jacobson, Luong T. Nguyen
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Patent number: 5431920Abstract: The present invention relates to a novel oral dosage form of a bisphosphonic active ingredient for use in treatment of diseases involving bone resorption and formulated in an enteric-coated form for administration to subjects exhibiting upper gastrointestinal tract sensitivity to bisphosphonic acid compounds.Type: GrantFiled: September 21, 1993Date of Patent: July 11, 1995Assignee: Merck Frosst, Canada, Inc.Inventor: Simon R. Bechard
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Method for lowering cholesterol employing a phosphonomethylphosphinate squalene synthetase inhibitor
Patent number: 5428028Abstract: A method is provided for inhibiting cholesterol biosynthesis by inhibiting de novo squalene production employing methylene phosphonoalkylphosphinate compounds.Type: GrantFiled: June 11, 1992Date of Patent: June 27, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: Scott A. Biller, David R. Magnin -
Patent number: 5395826Abstract: Compounds of the tautomeric formula Ia, Ib or Ic, ##STR1## where R is a radical of the formula ##STR2## are effective compounds for the treatment and prophylaxis of degenerative bone disorders. They are used as pharmaceuticals.Type: GrantFiled: November 30, 1993Date of Patent: March 7, 1995Assignee: Hoechst AktiengesellschaftInventors: Christoph Naumann, Hans-Jochen Lang, Jurgen Sandow, Anne-Marie Moura
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Patent number: 5393748Abstract: Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R.sup.1 -R.sup.4 independently are C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl, silyl SiR.sub.3 or hydrogen, whereby in formula (I) at least one of the groups R.sup.1 -R.sup.4 is hydrogen and at least one of the groups R.sup.1 -R.sup.4 is different from hydrogen, Q.sup.1 is hydrogen, hydroxyl, halogen, amino NH.sub.2, or OR'.sub.1, wherein R'.sub.1 is C.sub.1 -C.sub.4 -alkyl or acyl, Q.sup.2 is the group (.alpha.) wherein Y is a six-membered heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR'", wherein R'" is hydrogen, lower alkyl, or acyl, n is the integer 0 to 6, and R' and R" are hydrogen or lower alkyl provided that as a ring atom of the ring Y and/or a chain atom of the group X, there is always at least one heteroatom from the group O, N and S, including the steroisomers and the salts of the compounds.Type: GrantFiled: October 20, 1993Date of Patent: February 28, 1995Assignee: Leiras OyInventors: Esko Pohjala, Marjaana Heikkila-Hoikka, Hannu Nikander, Hannu Hanhijarvi
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Patent number: 5374628Abstract: Phosphonic acid squalene synthetase inhibitors are provided which are effective in lowering serum cholesterol and have the formula ##STR1## wherein m is 0 to 3, n is 1 to 5, Y.sup.1 and Y.sup.2 are H or halogen, R.sup.2, R.sup.3 and R.sup.4 are H, metal ion, C.sub.1 to C.sub.8 alkyl, C.sub.3 to C.sub.12 alkenyl, or prodrug ester, and R.sup.1 is a substituted or unsubstituted heteroaryl group or a substituted phenyl group.Type: GrantFiled: October 18, 1993Date of Patent: December 20, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: Scott A. Biller
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Patent number: 5366965Abstract: Methods for treating or preventing osteoporosis, including regimens for intermittent dosing of bone resorption inhibiting polyphosphonate compound or a pharmaceutically acceptable salt or ester of any such compound.Type: GrantFiled: January 29, 1993Date of Patent: November 22, 1994Assignee: Boehringer Mannheim GmbHInventor: Klaus Strein
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Patent number: 5360797Abstract: Novel acids, esters, and salts of phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonic acids and 1,2-oxaphosphepins are described. These compounds are useful as antiinflammatory and anti-arthritic agents. Also described are known compounds of the phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonate classes which are also useful as antiinflammatory and anti-arthritic agents. Representative compounds include [1,2-phenyldiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [2,3-quinoxalindiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [[3-(propyl)-4-(methoxy)-1,8-naphthalenediyl]bis(methylene)]bisphosphonic acid tetramethyl ester, [2,6-naphthalenediylbis(methylene)bisphosphonic acid tetraethyl ester, and [2,2'-biphenylenebis(methyl)]bisphosphonic acid tetramethyl ester. Representative oxaphosphepins include the preferred 3,4-dihydro-3-methoxy-7-(phenylmethoxy)-1H-naphth[1,8de][1,2]oxaphosphepin -3-oxide.Type: GrantFiled: November 1, 1993Date of Patent: November 1, 1994Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Herman W. Smith
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Patent number: 5332728Abstract: A method is provided for treating a fungal infection which includes the step of administering a therapeutically effective amount of a phosphorus-containing squalene synthetase inhibitor.Type: GrantFiled: November 23, 1992Date of Patent: July 26, 1994Assignee: Bristol-Myers Squibb CompanyInventor: Scott A. Biller
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Patent number: 5317015Abstract: This invention relates to a method of lowering abnormally high serum cholesterol levels in the body without significantly reducing mevalonic metabolite synthesis and to novel pharmacological compositions containing as an active ingredient bisphosphonic acid and ester compounds containing a mono-, bi- or tricyclic ring linked with a bisphosphonate moiety through a basic amino alkylene group. This invention also provides novel bisphosphonate compounds and the processes for their preparation.Type: GrantFiled: May 1, 1992Date of Patent: May 31, 1994Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John W. Ullrich, Raymond D. Youssefyeh, Daniel L. Cheney, Christopher J. Burns
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Patent number: 5278153Abstract: Phosphonic acid squalene synthetase inhibitors are provided which are effective in lowering serum cholesterol and have the formula ##STR1## wherein m is 0 to 3, n is 1 to 5, Y.sup.1 and Y.sup.2 are H or halogen, R.sup.2, R.sup.3 and R.sup.4 are H, metal ion, C.sub.1 to C.sub.8 alkyl, C.sub.3 to C.sub.12 alkenyl, or prodrug ester, and R.sup.1 is a substituted or unsubstituted heteroaryl group or a substituted phenyl group.Type: GrantFiled: May 18, 1992Date of Patent: January 11, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: Scott A. Biller
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Patent number: 5254544Abstract: Hydroxyphosphinyl phosphonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, metal ion or a prodrug ester; and R.sup.1 is a lipophilic group which contains at least 6 carbons and is alkyl, alkenyl, alkynyl, mixed alkenylalkynyl, a hetero-containing moiety as defined herein, or a phenylalkyl or phenylalkenyl group including those containing a biphenyl group.Type: GrantFiled: September 25, 1992Date of Patent: October 19, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Scott A. Biller, John K. Dickson, Jr.
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Patent number: 5242908Abstract: The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.Type: GrantFiled: February 1, 1991Date of Patent: September 7, 1993Assignee: Hoechst AktiengesellschaftInventors: Anuschirwan Peyman, Eugen Uhlmann, Karlheinz Budt, Jochen Knolle, Irvin Winkler, Matthias Helsberg
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Patent number: 5204336Abstract: Substituted gem-diphosphonate compounds having use as cholesterol lowering agents are disclosed. A compound of the invention is tetraethyl-2-[3-t-butyl-4-hydroxynaphthyl]ethenylidene-1,1-diphosphonate.Type: GrantFiled: May 6, 1992Date of Patent: April 20, 1993Assignee: Symphar S.A.Inventors: Lawrence I. Kruse, Virendra P. Shah
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Patent number: 5190930Abstract: Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolsim disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorus trichloride and hydrolysing the primary product.Type: GrantFiled: December 20, 1991Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5162310Abstract: Phenylaliphatylaminoalkanediphosphonic acids of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical having 4 and not more than 7 C atoms and substituted by phenyl, R.sub.2 is a monovalent aliphatic hydrocarbon radical having 1 and not more than 4 C atoms and alk is a divalent aliphatic hydrocarbon radical having 2 and not more than 4 C atoms, and their salts, have a particularly pronounced regulating action on calcium metabolism and can be used as medicaments for the treatment of diseases to be attributed to disturbances thereof. They are prepared, for example, for reacting a compound of the formula ##STR2## in which X.sub.3 denotes carboxyl, with a phosphorylating agent and hydrolyzing the primary product.Type: GrantFiled: November 15, 1989Date of Patent: November 10, 1992Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5157027Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## and analogs thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester;R.sup.5 is H, halogen or lower alkyl;Zq is substituted alkenyl, substituted alkynyl, mixed alkenyl-alkynyl or substituted phenylalkyl or, phenylalkenyl or phenylalkynyl, or alkyl, including all stereoisomers thereof.New methods for using such compounds to inhibit cholesterol biosynthesis are also provided.Type: GrantFiled: May 13, 1991Date of Patent: October 20, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: Scott A. Biller, David R. Magnin
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Patent number: 5153183Abstract: This invention relates to a methylenediphosphonic acid compound expressed by the formula (1). The compound has a marked effect as an anti-inflammatory agent or, more particularly, against inflammations accompanying disturbances in bone metabolism.Type: GrantFiled: May 6, 1991Date of Patent: October 6, 1992Assignee: Toray Industries, Inc.Inventors: Norio Kawabe, Keijiro Takanishi, Shu Matsumoto