Hetero Ring Is Six-membered Consisting Of Two Nitrogens And Four Carbons Patents (Class 514/85)
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Publication number: 20020193314Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.Type: ApplicationFiled: May 7, 2002Publication date: December 19, 2002Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
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Patent number: 6495553Abstract: This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.Type: GrantFiled: August 7, 1998Date of Patent: December 17, 2002Assignee: NewBiotics, Inc.Inventor: H. Michael Shepard
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Patent number: 6486165Abstract: Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided.Type: GrantFiled: March 13, 2001Date of Patent: November 26, 2002Assignee: Adolor CorporationInventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, Deqi Guo
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Publication number: 20020173515Abstract: Novel derivatives of 5-thia- and 5-selenopyrimidinone are found to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.Type: ApplicationFiled: October 23, 2001Publication date: November 21, 2002Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
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Publication number: 20020173490Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: 1Type: ApplicationFiled: December 22, 2000Publication date: November 21, 2002Applicant: METABASIS THERAPEUTICS, INC.Inventors: Tao Jiang, Srinivas Rao Kasibhatla, K. Raja Reddy
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Publication number: 20020165218Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.Type: ApplicationFiled: August 28, 2001Publication date: November 7, 2002Inventors: James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G Schiro, Hongmei Huang, Michael Evans, Yongxin Han
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Patent number: 6455530Abstract: A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (S,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and to their use for the treatment of fungal infection are also disclosed.Type: GrantFiled: September 18, 2000Date of Patent: September 24, 2002Assignee: Sepracor Inc.Inventors: Patrick Koch, John R. McCullough, Chris H. Senanayake, Gerald J. Tanoury, Yaping Hong
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Patent number: 6399782Abstract: Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is describedType: GrantFiled: April 11, 2000Date of Patent: June 4, 2002Assignee: Metabasis Therapeutics, Inc.Inventors: Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, Qun Dang, Gerard R. Scarlato, M. Rami Reddy
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Patent number: 6391884Abstract: This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.Type: GrantFiled: August 7, 1998Date of Patent: May 21, 2002Assignee: NewBiotics, Inc.Inventor: H. Michael Shepard
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Publication number: 20020042399Abstract: Compounds having kappa opioid agonist activity, compositions containing them and 5 method of using them as analgesics and pruritic agents are provided.Type: ApplicationFiled: January 26, 2001Publication date: April 11, 2002Applicant: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
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Publication number: 20020040014Abstract: Novel FBPase inhibitors of the formula I 1Type: ApplicationFiled: March 7, 2001Publication date: April 4, 2002Applicant: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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Patent number: 6362172Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.Type: GrantFiled: January 10, 2001Date of Patent: March 26, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Yasutsugu Ueda, John D. Matiskella, Jerzy Golik, Thomas W. Hudyma, Chung-Pin Chen
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Publication number: 20020035092Abstract: Propanoic acid derivatives of formula (1) are described:Type: ApplicationFiled: September 18, 2001Publication date: March 21, 2002Applicant: Celltech Therapeutics LimitedInventors: Rikki Peter Alexander, Barry John Langham, James Thomas Reuberson, Emma Louise Trown, Graham John Warrellow
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Publication number: 20020028814Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.Type: ApplicationFiled: April 17, 2001Publication date: March 7, 2002Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
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Publication number: 20020013296Abstract: Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided.Type: ApplicationFiled: March 13, 2001Publication date: January 31, 2002Inventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, Deqi Guo
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Patent number: 6337324Abstract: The invention relates to pharmaceutical compositions for topical administration comprising a topically acceptable antiviral substance and an antiinflammatory glucocorticoid in a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the prophylactic and curative treatment of herpesvirus infections in mammals including man. The invention also relates to the use of a combination of a topically acceptable antiviral substance and an antiinflammatory glucocorticoid for the manufacture of a medicament for said prophylactic and curative treatment.Type: GrantFiled: March 8, 1996Date of Patent: January 8, 2002Assignee: Medivir, ABInventors: Johan Georg Harmenberg, Ann Harriet Margareta Kristofferson
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Publication number: 20010051614Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g.Type: ApplicationFiled: November 29, 2000Publication date: December 13, 2001Inventors: Jeremy Ian Levin, Frances Christy Nelson
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Publication number: 20010041691Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided.Type: ApplicationFiled: January 10, 2001Publication date: November 15, 2001Inventors: Yasutsugu Ueda, John D. Matiskella, Jerzy Golik, Thomas W. Hudyma, Chung-Pin Chen
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Patent number: 6310051Abstract: The invention provides the use of dipyridoxyl or aminopolycarboxylic acid based chelating agents, metal chelates and salts thereof, in the manufacture of a therapeutic agent for use in the treatment or prophylaxis of atherosclerosis and related conditions in the human or non-human animal body.Type: GrantFiled: June 23, 2000Date of Patent: October 30, 2001Assignee: Nycomed Imaging ASInventors: Jan Olof Gustav Karlsson, Rolf Goran Gustav Andersson, Anders Olsson, Bo Zieden, Per Jynge, Tudor Griffith, Derek Grant, Robertson Towart, Helge Refsum
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Patent number: 6307047Abstract: The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).Type: GrantFiled: October 27, 1999Date of Patent: October 23, 2001Assignee: Abbott LaboratoriesInventors: Lawrence A. Black, Anwer Basha, Teodozyj Kolasa, Michael E. Kort, Huaqing Liu, Catherine M. McCarty, Meena Patel, Jeffrey J. Rohde, Michael J. Coghlan, Andrew O. Stewart
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Patent number: 6300356Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.Type: GrantFiled: August 10, 2000Date of Patent: October 9, 2001Assignee: Merck & Co., Inc.Inventors: Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
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Patent number: 6294672Abstract: The present invention is directed towards novel azaindole compounds which bind to the AMP site and are potent FBPase inhibitors. The present invention also is directed towards the clinical use of the novel FBPase inhibitors as a method of treatment or prevention of diseases responsive to lowered blood glucose levels.Type: GrantFiled: January 5, 2000Date of Patent: September 25, 2001Assignee: Metabasis Therapeutics, Inc.Inventors: K. Raja Reddy, Gerard R. Scarlato, Qun Dang, Mark D. Erion, Srinivas Rao Kasibhatla, M. Rami Reddy
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Patent number: 6248729Abstract: A method is provided for preventing a cerebral infarction by administering to a patient a combination of an ADP-receptor blocking antiplatelet drug, such as clopidogrel, in combination with an antihypertensive agent such as an angiotensin AII antagonist (for example, irbesartan), an ACE inhibitor (for example, fosinopril) or a NEP/ACE inhibitor such as omapatrilat.Type: GrantFiled: June 9, 1999Date of Patent: June 19, 2001Assignees: Bristol-Myers Squibb Co., Sanofi-SynthelaboInventors: Anthony A. Coniglio, Francis R. Plat, Melvin S. Blumenthal
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Patent number: 6201002Abstract: Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce mortality and sudden cardiac death in this patient population. Additionally, losartan potassium has been shown to reduce the need for hospitalization of symptomatic heart failure patients.Type: GrantFiled: January 6, 1998Date of Patent: March 13, 2001Assignee: Merck & Co., Inc.Inventors: Polly A. Beere, Paul I. Chang, Bertram Pitt, Eva J. Rucinska, Robert Segal, Divakar Sharma, Duane B. Snavely
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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: 6156790Abstract: The present invention provides a two-step procedure for the replacement of the pyranose anomeric 10-OH group in dihydroartemisinin by a variety of carbon nucleophiles, resulting in the novel C-10 carbon-substituted trioxanes of structure: ##STR1## wherein, when n is 1, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, acetylenics, or benzoylmethylenes, or alkanoylmethylenes; or when n is 2, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes.Type: GrantFiled: December 30, 1997Date of Patent: December 5, 2000Assignees: Hauser, Inc., Johns Hopkins UniversityInventors: Gary H. Posner, Soon Hyung Woo, Poonsakdi Ploypradith, Michael H. Parker, Theresa A. Shapiro, Qun Y. Zheng, Christopher Murray, Randall J. Daughenbaugh
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Patent number: 6143733Abstract: Quinoxalinedione derivatives ##STR1## as well as their production and use in pharmaceutical agents are described.Type: GrantFiled: May 29, 1997Date of Patent: November 7, 2000Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Martin Kruger, Eckhard Ottow, Dieter Seidelmann, Graham H Jones, Herbert Schneider, Lechoslaw Turski
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Patent number: 6121251Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is ##STR2## n is 0 or 1; Y is O, S, NR.sub.1, or R.sub.6 ;the ring bond containing R.sub.4 and R.sub.5 is a single or double bond;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and --HC.dbd.CH--CH.dbd.CH-- thereby forming a napthyl ring;R is independently selected from (C.sub.1 -C.sub.12)alkyl and halo(C.sub.1 -C.sub.12)alkyl;R.sub.1 is independently selected from (C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl and aryl;R.sub.2 is independently selected from hydrogen, (C.sub.1 -C.sub.12)alkyl (C.sub.1 -C.sub.12)alkoxy, halo(C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkoxy, hydroxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxycarbonyl(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl, halo(C.sub.2 -C.sub.8)alkenyl, (C.sub.3 -C.sub.10)alkynyl, halo(C.sub.3 -C.sub.10)alkynyl, (C.sub.3 -C.sub.Type: GrantFiled: September 26, 1997Date of Patent: September 19, 2000Assignee: Rohm and Haas CompanyInventors: Steven Howard Shaber, Edward Michael Szapacs, Ronald Ross
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Patent number: 6110904Abstract: A method for suppressing plant damage by nematodes which comprises the concurrent administration, to the locus, soil or seeds of plants in need of such treatment, of (a) a metabolite of the fungus Myrothecium verrucaria and (b) a chemical pesticide, as well as synergistic nematocidal compositions useful therein.Type: GrantFiled: August 28, 1997Date of Patent: August 29, 2000Assignee: Valent BioSciences, Inc.Inventors: Prem Warrior, Daniel F. Heiman, Linda A. Rehberger
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Patent number: 6057323Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X; and ArY, Z and n are as described in the specification.Type: GrantFiled: October 30, 1998Date of Patent: May 2, 2000Assignee: Adolor CorporationInventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
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Patent number: 6043245Abstract: A compound of the formula I ##STR1## wherein G is H or PO.sub.3 H.sub.2 or a pharmaceutical acceptable salt thereof, pharmaceutical compositions containing such compounds and method of using such compounds or pharmaceutical compositions containing them to treat or prevent fungal infection are disclosed.Type: GrantFiled: September 25, 1998Date of Patent: March 28, 2000Assignee: Schering CorporationInventors: Frank Bennett, Viyyoor M. Girijavallabhan, Naginbhai M. Patel, Anil K. Saksena, Ashit Ganguly
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Patent number: 6015800Abstract: A novel series of substituted quinoxaline 2-ones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.Type: GrantFiled: May 15, 1998Date of Patent: January 18, 2000Assignee: Warner-Lambert CompanyInventor: Sham Shridhar Nikam
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Patent number: 6004964Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.Type: GrantFiled: November 2, 1998Date of Patent: December 21, 1999Assignee: Adolor CorporationInventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
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Patent number: 5985856Abstract: The present invention is drawn to water soluble derivatives aliphatic acid aromatic secondary and tertiary amine containing drugs. The present invention is further drawn to methods of making water soluble derivatives of aliphatic and aromatic secondary and tertiary amine containing drugs.Type: GrantFiled: December 30, 1998Date of Patent: November 16, 1999Assignee: University of KansasInventors: Valentino Stella, Jeffrey P. Krise, Jan J. Zygmunt, Ingrid Gunda Georg
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Patent number: 5985858Abstract: A phosphonic diester derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen-substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R.sup.2 represents a hydrogen atom or a phenyl lower alkyl group; R.sup.3 and R.sup.Type: GrantFiled: June 26, 1998Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuyoshi Miyata, Yasuhiro Sakai, Yasuo Shoji, Yoshihiko Tsuda, Yasuhide Inoue, Keigo Sato, Shinya Miki
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Patent number: 5958905Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.Type: GrantFiled: March 26, 1996Date of Patent: September 28, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Erik Joel Verner
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5880111Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
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Patent number: 5846971Abstract: A pharmaceutical composition comprising:i) substantially inert beads; wherein said beads are coated withii) an antifungal agent which is (-)-(2R-cis)-4-?4-?4-?4-??-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-tr iazol-1-ylmethyl)furan-3-yl!methoxy!phenyl!-1-piperazinyl!phenyl!-2,4-dihyd ro-2-?(S)-1-ethyl-2(S)-hydroxypropyl!-3H-1,2,4-triazol-3-one;iii) a binder to enables the antifungal compound to adhere to said beads.The composition enables the antifungal compound, which has very low water solubility, to have enhanced bioavailability in mammals, such as humans.Type: GrantFiled: June 20, 1997Date of Patent: December 8, 1998Assignee: Schering CorporationInventors: Surendra A. Sangekar, Winston A. Vadino, Ping I. Lee
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Method of treating neurodegenerative diseases using an AMPA excitatory amino and an uricosuric agent
Patent number: 5767119Abstract: The present invention is a pharmaceutical composition having a combination of an uricosuric agent such as probenecid or the like and an excitatory amino acid antagonist useful for treating a disease advantageously affected by treatment with an excitatory amino acid antagonist.Type: GrantFiled: December 31, 1996Date of Patent: June 16, 1998Assignee: Warner-Lambert CompanyInventors: Christopher Franklin Bigge, Graham Johnson, Charles Price Taylor, Jr., Devin Franklin Welty -
Patent number: 5763445Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compounds of formular I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ;R.sub.1, R.sub.2, R.sub.3, R.sub.4 ; andY, Z and n are as described in the specification.Type: GrantFiled: July 14, 1997Date of Patent: June 9, 1998Assignee: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
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Patent number: 5750697Abstract: A channel protein having a Na.sup.+ /K.sup.+ selectivity of approximately 100 and capable of affecting Na.sup.+ membrane transport is disclosed. Amiloride derivatives, and amiloride gel materials incorporating such derivatives, useful in treating membrane transport, cellular volume and cellular pressure disorders and in isolating the channel protein are also disclosed. These amiloride derivatives may be prepared by mixing the amiloride with an alkanediol in the presence of a base followed by addition of an acid. Use of the channel protein in diagnostic assays and screening assays is described.Type: GrantFiled: July 20, 1992Date of Patent: May 12, 1998Inventor: Bruce D. Cherksey
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Patent number: 5741784Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; ....... represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## ,or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: August 30, 1996Date of Patent: April 21, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5714490Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two amino acid ester groups (e.g., an amino acid ester group convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: February 3, 1998Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5710154Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two groups convertible in vivo into hydroxy moieties, (e.g., a polyether ester, amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: January 20, 1998Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5707977Abstract: A compound of formula (I), ##STR1## an acid or base addition salt thereof or a stereochemically isomeric form thereof, wherein A and B taken together form --N.dbd.CH--, --CH.dbd.N--, --CH.sub.2 --CH.sub.2, CH.dbd.CH--, --C(.dbd.O)--CH.sub.2 --, --CH.sub.2 --C(.dbd.O); D is a radical of formula ##STR2## L is a radical of formula ##STR3## Alk is a C.sub.1-4 alkanediyl radical; R.sup.1 is halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.4 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, or R.sup.5 and R.sup.6 taken together with the nitrogen atom to which they are attached form a heterocyclic ring. Active intermediates, compositions and methods of preparing compounds, compositions are described.Type: GrantFiled: June 20, 1996Date of Patent: January 13, 1998Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Luc Alfons Leo Van der Eycken, Frank Christopher Odds, Jean Louis Mesens
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Patent number: 5693626Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two phosphate ester groups (e.g., a phosphate ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: December 2, 1997Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5681830Abstract: Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, cough, and apnea, respiratory depression, cognitive disorders, emesis and gastrointestinal disorders.Type: GrantFiled: August 3, 1994Date of Patent: October 28, 1997Assignee: Delta Pharmaceuticals, Inc.Inventors: Kwen-Jen Chang, Dulce G. Bubacz, Ann O. Davis, Robert W. McNutt, Jr., Mark A. Collins, Michael J. Bishop
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Patent number: 5661151Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether or ester thereof (e.g., a polyether ester amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: August 26, 1997Assignee: Schering CorporationInventors: Anil K. Saksena, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Russell E. Pike, Haiyan Wang, Yi-Tsung Liu, Ashit K. Ganguly, Frank Bennett
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Patent number: 5646151Abstract: Compounds, compositions and method of treating hyperalgesia comprising a compound of formula I, II, III and IV as defined in the specification.Type: GrantFiled: March 8, 1996Date of Patent: July 8, 1997Assignee: Adolor CorporationInventors: Lawrence I. Kruse, Virendra Kumar, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Alan L. Maycock