C-c(=x)-x-c Containing (x Is Chalcogen And At Least One X Is Other Than Oxygen) Patents (Class 514/513)
-
Patent number: 6337347Abstract: 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: June 18, 1998Date of Patent: January 8, 2002Assignee: The Research & Development Institute, Inc.Inventor: Tom Livinghouse
-
Patent number: 6337318Abstract: A pharmaceutical and/or veterinary formulation for sustained release of a peptide agonist or analogue, comprising about 2-15% (w/w) of at least one peptide agonist or analogue other than deslorelin (on an active basis), about 0.5-3.5% (w/w) lecithin and the balance stearin. The formulation preferably comprises a GnRH agonist or analogue and is used for the treatment of various conditions where suppression of sex hormone levels is beneficial, particularly prostate cancer, ovarian and breast cancer, and benign prostatic hyperplasia in dogs.Type: GrantFiled: February 19, 1999Date of Patent: January 8, 2002Assignee: Peptech, Ltd.Inventors: Timothy Elliot Trigg, John Desmond Walsh, Paul Adam Schober
-
Publication number: 20020002196Abstract: Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.Type: ApplicationFiled: June 25, 2001Publication date: January 3, 2002Inventors: Raymond E. Conrow, Peter G. Klimko
-
Publication number: 20010056103Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.Type: ApplicationFiled: December 11, 2000Publication date: December 27, 2001Applicant: GPI NIL HOLDINGS, Inc.Inventors: Gregory S. Hamilton, Jia-He Li
-
Publication number: 20010051648Abstract: Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.Type: ApplicationFiled: June 25, 2001Publication date: December 13, 2001Inventors: Raymond E. Conrow, Peter G. Klimko
-
Patent number: 6329422Abstract: Compositions and methods for therapy of cystic fibrosis and other conditions are provided. The compositions comprise one or more compounds such as flavones and/or isoflavones capable of stimulating chloride transport in epithelial tissues. Therapeutic methods involve the administration (e.g., orally or via inhalation) of such compositions to a patient afflicted with cystic fibrosis and/or another condition responsive to stimulation of chloride transport.Type: GrantFiled: October 16, 1998Date of Patent: December 11, 2001Assignee: Children's Hospital Oakland Research InstituteInventors: Horst Fischer, Beate Illek
-
Patent number: 6319948Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation. Also provided by the invention are certain novel substituted (5,6)-dihydronaphthalenyl compounds which are retinoid antagonists and possess the above-mentioned property in addition to their use as antiinflammatory agents for chronic skin inflammatory diseases, as agents for the treatment of rheumatic diseases and as agents for the treatment of various tumors as well as non-malignant proliferative skin conditions.Type: GrantFiled: December 8, 2000Date of Patent: November 20, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Tramposch, Xina Nair, Anne Marinier, Fred Christopher Zusi
-
Patent number: 6303662Abstract: A microemulsion containing (A) a highly polar and fat-soluble oil drug, a highly polar oil and a lowly polar oil, (B) a polyglycerol mono-fatty acid ester and (C) a water-soluble polyhydric alcohol, wherein the amount of (B) is 0.3 to 3 parts by weight based on one part by weight of (A) and the amount of (C) is 0.1 to 3 parts by weight based on one part by weight of the total amount of (A) and (B). The present invention makes it possible to make a microemulsion containing a highly polar and fat-soluble drug which is highly stable.Type: GrantFiled: October 15, 1999Date of Patent: October 16, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Tohru Nagahama, Kazuo Hasegawa
-
Patent number: 6284923Abstract: The invention provides compounds, compositions and methods relating to novel electrophilic aromatic 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: August 22, 1997Date of Patent: September 4, 2001Assignee: Tularik INCInventors: Julio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
-
Patent number: 6251833Abstract: The present invention relates to novel 2-aryl-3-hydroxy-&Dgr;2-cyclopentene-1-one derivatives of the formula (I) in which A, B, D1, D2, G, W, X, Y and Z are each as defined in the description, to processes for their preparation and to their use as herbicides and pesticides.Type: GrantFiled: August 31, 1999Date of Patent: June 26, 2001Inventors: Christoph Erdelen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Norbert Mencke, Andreas Turberg
-
Patent number: 6242464Abstract: Single isomer methylphenidate, selected from the d- and l-threo-enantiomers, has been obtained in purified form, to the extent of less than 2% by weight of a contaminant selected from resolving agent and ritalinic acid. This is achieved by resolution of a mixture of enantiomers using an O,O′-diaroyltartaric acid as resolving agent.Type: GrantFiled: January 22, 1997Date of Patent: June 5, 2001Assignee: Chiroscience LimitedInventors: Michael Christopher James Harris, Hooshang Zavareh
-
Patent number: 6201023Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.Type: GrantFiled: June 10, 1997Date of Patent: March 13, 2001Assignee: Agrogene Ltd.Inventors: Yuji Oka, Yitzhak Spiegel, Yigal Cohen
-
Patent number: 6156299Abstract: Topical compositions and methods are disclosed for the treatment of pseudofolliculitis barbae and ingrown hair. The compositions comprise acetylsalicylic acid, propylene glycol, glycerine, and isopropyl alcohol. The method involves the step of applying the composition to the beard areas of the face after shaving. The acetylsalicylic acid is dissolved in a solvent mixture comprising propylene glycol, glycerine, and isopropyl alcohol. The acetylsalicylic acid is present in the range of between about 5 percent by weight per unit volume of the solvent mixture up to saturation of the solvent mixture. The solvent mixture comprises propylene glycol in the range of about 5 to 15 percent by volume, glycerine in the range of about 1 to 10 percent by volume, and the balance of the volume made up with isopropyl alcohol alone or a solution comprising at least 50 percent by volume of isopropyl alcohol.Type: GrantFiled: September 3, 1999Date of Patent: December 5, 2000Assignee: Tend Skin International, Inc.Inventors: Steven E. Rosen, Robert Lee Brown
-
Patent number: 6153655Abstract: The present invention is directed to polymeric- prodrug transport forms of the formula: ##STR1## wherein: B is a leaving group, OH, a residue of a hydroxyl-containing moiety or ##STR2## wherein B.sub.1 is a leaving group, OH or a residue of a hydroxyl-containing moiety;Y.sub.1-2 are independently O or S;M is selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2); R.sub.2-5 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls and substituted C.sub.1-6 heteroalkyls;(m) is zero or one;(n) is a positive integer;(p) is zero or a positive integer;Z is an electron withdrawing group; andR.sub.Type: GrantFiled: April 17, 1998Date of Patent: November 28, 2000Assignee: Enzon, Inc.Inventors: Anthony J. Martinez, Annapurna Pendri, Richard B. Greenwald, Yun H. Choe
-
Patent number: 6143734Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a compound comprising an enolic anilide non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO.sub.2 group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: January 31, 2000Date of Patent: November 7, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
-
Patent number: 6124352Abstract: A method of treating fungal diseases as well as pharmaceutical, veterinary and agricultural compositions useful in such treatment. The method includes administering an effective antifungal amount of a compound of the formula (I): ##STR1## wherein S is a spacer selected from a nitrogen, an oxygen, an alkyl, an alkenyl, an alcohol, an ester, a polyester, an amino acid, a carbohydrate, or a nitrogen-containing positively charged group;L is a ligand selected from a hydrogen, a hydroxyl residue, an alkyl residue, an alkenyl residue, a benzyl residue, an alcohol residue, an ester residue, a polyester residue, an alkyl acid residue, a carbohydrate, a steroid, a lipid, an organic polymer, a nitrogen-containing positively charged group or a vitamin;R.sub.1 and R.sub.3 are halogen or hydroxyl; andR.sub.2 is hydrogen or alkyl.Type: GrantFiled: July 27, 1994Date of Patent: September 26, 2000Assignee: Jemlan, LLCInventor: Vladimir Z. Gurevich
-
Patent number: 6117902Abstract: The present invention provides 6,8-Dimercaptooctanoic acid derivatives substituted at the 6-S and/or 8-S position with the (3-methylthiopropanoyl) radical, wherein they correspond to the following formula (I): ##STR1## in which: R represents OR.sub.3 or ##STR2## R.sub.3 representing a hydrogen atom, a linear or branched alkyl radical, or a radical of the formula ##STR3## n being an integer from 1 to 10 and r' and r", which are identical or different, representing a hydrogen atom, a linear or branched alkyl radical or, taken together, form with the nitrogen atom, a nitrogen-containing heterocycle optionally substituted with an optionally substituted oxygen or nitrogen atom,R.sub.5 and R.sub.4, identical or different, represent a hydrogen atom or a linear or branched alkyl radical,R.sub.1 and R.sub.2, which are identical or different, represent a hydrogen atom, a radical --COCH.sub.3 or a radical of formula:--CO(CH.sub.2).sub.2 SCH.sub.3 (II)with the proviso that at least one of the radicals R.sub.1 or R.sub.Type: GrantFiled: March 30, 1999Date of Patent: September 12, 2000Assignee: Galderman Research & Development, S.N.C. Sophia AbtipolisInventors: Gerard Anthony Quash, Jacques Gore, Guy Fournet
-
Patent number: 6117901Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: November 21, 1997Date of Patent: September 12, 2000Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Eugene D. Thorsett, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Lawrence Y. Fang, James E. Audia
-
Patent number: 6114372Abstract: Compounds of formula (I) having MMP and TNF inhibitory activity.Type: GrantFiled: October 2, 1998Date of Patent: September 5, 2000Assignee: Darwin Discovery LimitedInventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson, John Fraser Keily
-
Patent number: 6110908Abstract: Stable antiseptic compositions having broad spectrum, fast acting, and profound persistent effect without significant irritation of the tissue to which they are applied are disclosed. The broad spectrum, fast acting component of the present invention comprises one or more antimicrobial alcohols, antimicrobial lipids, or mixtures thereof. The persistent component of the present invention comprises one or more antimicrobial lipids, pyridine-containing compounds, nitrogen-containing antibitics, preservatives, or mixtures thereof, which preferably bind to either or both of the skin surface and intracellular structures within the epidermis. Additional components include antioxidants, emulsifying agents, acidifiers, thickeners, and coloring and texturing compounds. Preferred antiseptic formulations comprise an antimicrobial alcohol such as 70% n-propanol, an antimicrobial lipid such as free fatty acids and/or fatty acid esters, and zinc omadine.Type: GrantFiled: May 5, 1997Date of Patent: August 29, 2000Inventor: B. Eugene Guthery
-
Patent number: 6090847Abstract: The invention relates to the use of EP.sub.2 receptor agonists as neuroprotective agents. In particular said compounds are represented by the formulae: ##STR1## wherein the broken line attachment to the cyclopentane ring or the omega chain indicates the .alpha. configuration and the solid line attachment to the cyclopentane ring or the omega chain indicates the .beta. configuration, R is hydrogen or a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.1 wherein m is 0-10, and R.sub.1 is an aliphatic ring having from about 3 to about 7 carbon atoms, or an aryl or heteroaryl ring having from about 4 to about 10 carbon atoms and wherein the heteroatom is selected from the group consisting of N, O and S.Type: GrantFiled: November 3, 1998Date of Patent: July 18, 2000Assignee: Allergan Sales, Inc.Inventor: David F. Woodward
-
Patent number: 6077866Abstract: Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.Type: GrantFiled: May 10, 1996Date of Patent: June 20, 2000Assignee: Nihon Bayer Agrochem K.K.Inventors: Yoshinori Kitagawa, Katsuaki Wada, Yoshiko Kyo, Yuichi Otsu, Yumi Hattori, Toru Obinata, Takahisa Abe, Katsuhiko Shibuya, Wolfram Andersch
-
Patent number: 6071962Abstract: Disclosed the use of compounds of Formula (I) depicted below, as active principals for treating skin conditions, compositions containing these compounds, and methods of treating skin conditions using these compounds and compositions. ##STR1## where R.sub.4 is (CR.sub.5 R.sub.6 --CR.sub.7 R.sub.8 --X.sub.1).sub.n --CR.sub.9 R.sub.10 R.sub.11 ; n is an integer from 1 to 18; R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are, independently, hydrogen or non-hydrogen substituents comprising alkyls, alkenyls, oxa-alkyls, aralkyls and aryls; and X, X.sub.1, Y and Z are, independently, oxygen, amine or sulfur, with preferred compounds being those in which X, X.sub.1, Y and Z are oxygen, and R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are hydrogen.Type: GrantFiled: September 14, 1998Date of Patent: June 6, 2000Assignee: Avon Products, Inc.Inventors: Dmitri Ptchelintsev, Neil D. Scancarella, Robert Kalafsky
-
Patent number: 6063817Abstract: The present invention relates to methods of preventing, or reducing the severity of, an ischemic injury originating in an animal's dermal tissue by applying to the animal a composition comprising a compound of formula I*: ##STR1## or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in whichX is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 --NH--, --COCH.sub.2 --, --NHCS--, --CH.sub.2 S--, --CH.sub.2 O--, --OCH.sub.2 --, --NHCH.sub.2 -- or --CR.sup.5 .dbd.CR.sup.6 --;n is 1 or 0;R.sup.m and R.sup.k are independently hydrogen, halogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy or nitro;R.sup.4 is --(CH.sub.2).sub.t --Y.sup.b, C.sub.1-6 alkyl, or C.sub.3-6 cycloalkyl;R.sup.1 is --CO.sub.2 Z, C.sub.1-6 alkyl, CH.sub.2 OH, --CONHR.sup.y, or CHO;R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl, or R.sup.a and R.sup.Type: GrantFiled: February 19, 1998Date of Patent: May 16, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Shannon, Karyn A. Monte, Kenneth Tramposch
-
Patent number: 6060454Abstract: Methods are provided for conducting surgical procedures in a patient wherein, during the surgical procedure, autonomous ventricular electrical conductivity and escape beats are reversibly and transiently suppressed to facilitate the surgical procedure. Also provided are compositions which are capable of inducing ventricular asystole in a patient. The compositions may include an AV node blocker. In one embodiment, compositions including an atrioventricular (AV) node blocker and a .beta.-blocker are provided, wherein the .beta.-blocker is present in an amount sufficient to substantially reduce the amount of AV node blocker required to induce ventricular asystole in the patient. The compositions and methods may be used for inducing temporary ventricular asystole in a beating heart, and to facilitate the performance of a variety of surgical techniques, including minimally invasive microsurgical techniques.Type: GrantFiled: August 7, 1998Date of Patent: May 9, 2000Assignee: Duke UniversityInventor: Francis G. Duhaylongsod
-
Patent number: 6043232Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a compound comprising an enolic anilide non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO.sub.2 group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: January 22, 1999Date of Patent: March 28, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
-
Patent number: 6011000Abstract: The invention relates to compositions containing chemical compounds and compositions containing steel factor which stimulate the expression of hemoglobin or globin protein such as embryonic or fetal globin, or the proliferation of hemoglobin expressing and other cells. These compositions can be used to treat or prevent the symptoms associated with anemia, sickle cell diseases, thalassemia and other blood disorders. The invention also relates to methods for administering these compositions to patients and to medical aids for the treatment and prevention of blood and other disorders.Type: GrantFiled: June 6, 1995Date of Patent: January 4, 2000Inventors: Susan P. Perrine, Douglas V. Faller
-
Patent number: 6004569Abstract: A pesticide and a method of using the pesticide to kill invertebrates, especially insects, arachnids and larvae. The method is to prepare a mixture of a carrier with the pesticide and apply the mixture to the insects, arachnids and larvae and their habitat. The pesticide is a neurotransmitter affector utilizing octopamine receptor sites in the insects, arachnids and larvae. The affector agent is a chemical having a six membered carbon ring having substituted thereon at least one oxygenated functional group. The affector agent is a chemical component of a plant essential oil and is naturally occurring. Deposition of the chemicals of the present invention on a surface provides residual toxicity for up to 30 days. Various carriers for the affector agent are disclosed. The chemicals of the present invention deter feeding of insects, arachnids and larvae and also retard growth of the larvae of the insects and arachnids.Type: GrantFiled: June 6, 1997Date of Patent: December 21, 1999Assignee: Ecosmart Technologies, Inc.Inventors: Steven M. Bessette, Myron A. Beigler
-
Patent number: 6001340Abstract: Topical compositions and methods are disclosed for the treatment of pseudofolliculitis barbae and ingrown hair. The compositions comprise acetylsalicylic acid, propylene glycol, glycerine, and isopropyl alcohol. The method involves the step of applying the composition to the beard areas of the face after shaving. The acetylsalicylic acid is dissolved in a solvent mixture comprising propylene glycol, glycerine, and isopropyl alcohol. The acetylsalicylic acid is present in the range of between about 5 percent by weight per unit volume of the solvent mixture up to saturation of the solvent mixture. The solvent mixture comprises propylene glycol in the range of about 5 to 15 percent by volume, glycerine in the range of about 1 to 10 percent by volume, and the balance of the volume made up with isopropyl alcohol alone or a solution comprising at least 50 percent by volume of isopropyl alcohol.Type: GrantFiled: March 30, 1993Date of Patent: December 14, 1999Assignee: Steven E. RosenInventors: Steven E. Rosen, Robert Lee Brown
-
Patent number: 5994539Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.Type: GrantFiled: December 18, 1997Date of Patent: November 30, 1999Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro
-
Patent number: 5985921Abstract: Compounds of the formula ##STR1## in which n, q, A, X, G, Y, Z, R, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.9 are as defined in claim 1, and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers thereof, in each case in the free form or in an agrochemically suitable salt form, can be used as agrochemical active compounds and can be prepared in a manner known per se.Type: GrantFiled: December 6, 1996Date of Patent: November 16, 1999Assignee: Novartis CorporationInventors: Saleem Farooq, Stephen Trah, Hugo Ziegler, Rene Zurfluh, Alfons Pascual, Henry Szczepanski, Roger Graham Hall
-
Patent number: 5972995Abstract: Compositions and methods for therapy of cystic fibrosis and other conditions are provided. The compositions comprise one or more flavones and/or isoflavones capable of stimulating chloride transport in epithelial tissues. Therapeutic methods involve the administration (e.g., orally or via inhalation) of such compositions to a patient afflicted with cystic fibrosis and/or another condition responsive to stimulation of chloride transport.Type: GrantFiled: October 16, 1997Date of Patent: October 26, 1999Assignee: Children's Hospital Medical Center of Northern CaliforniaInventors: Horst Bernhard Fischer, Beate Illek
-
Patent number: 5968727Abstract: The invention comprises a novel pyruvate compound for the treatment of prevention of reperfusion injury following ischemia, diabetic effects, cholesterol levels, injured organs ethanol intoxication oras s foodstuff. The novel pyruvate compound is particularly a puruvate thiolester, a glucerol-pyruvate ester or a dihydoxyacetone-pyruvate ester.Type: GrantFiled: March 1, 1999Date of Patent: October 19, 1999Assignee: Case Western Reserve UniversityInventors: Henri Brunengraber, Catherine Bomont, France David, Peter T. Hallowell
-
Patent number: 5962487Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.Type: GrantFiled: December 16, 1997Date of Patent: October 5, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine
-
Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
-
Patent number: 5948819Abstract: An .alpha.-substituted phenylacetic acid derivative useful as an agricultural fungicide, represented by general formula (I), or a salt thereof, a process for producing the same, an intermediate for the production thereof, and an agricultural fungicide containing the same as the active ingredient, wherein R.sup.1 represents halogen, alkyl, OH, alkylthio, alkylsulfinyl, alkylsulfonyl, amino or nitro; Q represents aryl, heterocycle, mono- or disubstituted methyleneamino, (substituted amino-)methyl, alkyl, alkenyl, alkynyl, substituted carbonyl or substituted sulfonyl; X represents hydrogen, halogen, alkyl or OH; Y represents OH, alkylthio or amino; Z represents oxygen or sulfur; M represents oxygen, S(O)i (i being 0, 1 or 2), NR.sup.2 (R.sup.2 being hydrogen, alkyl or acyl) or a single bond; and n represents 0, 1 or 2.Type: GrantFiled: October 7, 1996Date of Patent: September 7, 1999Assignee: Shionogi & Co., LtdInventors: Toshikazu Ohtsuka, Takami Murashi, Shinji Suzuki, Michio Masuko, Hideyuki Takenaka
-
Patent number: 5929114Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: May 15, 1997Date of Patent: July 27, 1999Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
-
Patent number: 5927283Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in a wide variety of treatments including hypoxia, hypothermia, ischemia, stroke, ARDS, COPD, surgical blood loss, acute nonvolemic hemodilutions, wounds, diabetic ulcers, chronic leg ulcers, pressure sores, tissue transplants, and sepsis. The compounds are capable of acting on hemoglobin in whole blood.Type: GrantFiled: May 8, 1997Date of Patent: July 27, 1999Assignee: Virginia Commonwealth UniversityInventors: Donald J. Abraham, Michael Gerber
-
Patent number: 5925674Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.Type: GrantFiled: October 26, 1995Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
-
Patent number: 5925367Abstract: A composition for controlling harmful insects and representatives of the order Acarina, containing as biologically active components a) a substance that modifies the behavior of the pests and b) at least one pesticidally active compound, wherein the biologically active components are contained in a flowable or viscous non-hardening matrix that is resistant to water and weather, is protected against light and is suitable for distribution in the form of droplets or droplet-like units or spots that adhere to a substrate, by means of which matrix the behavior-modifying substance is protected against UV radiation and from which it is slowly released in a biologically effective amount over a prolonged period, and wherein the pesticidally active compound can be taken up in a pesticidally effective amount from the surface of the droplets or droplet-like units or spots by the pests to be controlled; as well as a method of controlling the said pests, especially plant-destructive insects.Type: GrantFiled: January 19, 1995Date of Patent: July 20, 1999Assignee: Ciba-Geigy CorporationInventors: Max Angst, Fran.cedilla.ois Gugumus, Gunther Rist, Manfred Vogt, Jean Rody
-
Patent number: 5883123Abstract: This invention relates to butyrate prodrugs derived from lactic acid and pharmaceutical compositions and methods employing them, either alone or in combination with other agents, for increasing gamma globin and fetal hemoglobin in a patient. These compounds, compositions and methods are particularly effective in treating .beta.-hemoglobinopathies, including sickle cell syndromes and .beta.-thalassemia syndromes. In addition, this invention relates to the use of these prodrugs, alone or in combination with other agents, to stimulate cell differentiation which prevents proliferation of malignant cells. These methods are particularly useful in treating cancer, especially malignant hematological disorders.Type: GrantFiled: October 6, 1995Date of Patent: March 16, 1999Assignee: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Biqin Li
-
Patent number: 5876916Abstract: The invention comprises a novel pyruvate compound for the treatment or prevention of reperfusion injury following ischemia, diabetic effects, cholesterol levels, injured organs, ethanol intoxication or as a foodstuff. The novel pyruvate compound is particularly a pyruvate thiolester, a glycerol-pyruvate ester or a dihydoxyacetone-pyruvate ester.Type: GrantFiled: February 27, 1997Date of Patent: March 2, 1999Assignee: Case Western Reserve UniversityInventors: Henri Brunengraber, Catherine Bomont, France David, Peter T. Hallowell
-
Patent number: 5852056Abstract: Methods of inhibiting IL-6 in a cell by administering a therapeutically effective amount of phenylacetate or pharmaceutically acceptable derivatives thereof.Type: GrantFiled: April 10, 1996Date of Patent: December 22, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Dvorit Samid
-
Patent number: 5843994Abstract: Compositions and methods of treating anemia, cancer, AIDS, or severe .beta.-chain hemoglobinopathies by administering a therapeutically effective amount of phenylacetate or pharmaceutically acceptable derivatives thereof or derivatives thereof alone or in combination or in conjunction with other therapeutic agents including retinoids, hydroxyurea, and flavonoids. Intravesicle methods of treatment of cancers phenylacetate. Pharmacologically-acceptable salts alone or in combinations and methods of preventing AIDS and malignant conditions, and inducing cell differentiation are also aspects of this invention. A product as a combined preparation of phenylacetate and a retinoid, hydroxyurea, or flavonid (or other mevalonate pathway inhibitor) for simultaneous, separate, or sequential use in treating a neoplastic condition in a subject. Methods of modulating lipid metabolism and/or reducing serum triglycerides in a subject using phenylacetate.Type: GrantFiled: June 7, 1995Date of Patent: December 1, 1998Assignee: The United States of America as represeneted by the Department of Health and Human ServicesInventor: Dvorit Samid
-
Patent number: 5840661Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.Type: GrantFiled: December 31, 1996Date of Patent: November 24, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
-
Patent number: 5821260Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.Type: GrantFiled: June 7, 1995Date of Patent: October 13, 1998Assignee: Emory UniversityInventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
-
Patent number: 5792787Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.Type: GrantFiled: June 7, 1995Date of Patent: August 11, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Margaret K. Offermann
-
Patent number: 5783596Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.Type: GrantFiled: June 7, 1995Date of Patent: July 21, 1998Assignee: Emory UniversityInventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
-
Patent number: 5773231Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
-
Patent number: 5773209Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan