Patents Issued in November 6, 2001
  • Patent number: 6313103
    Abstract: Pectic substance from Aloe Vera and other sources is used as a stabilizer and a delivery vehicle for pectin/heparin-binding proteins, such as pectin/heparin binding growth factors. Aloe pectin, a naturally occurring LM (low methoxyl) pectin, binds to pectin/heparin-binding growth factors, i.e., bFGF, aFGF, and KGF of fibroblast growth factor (FGF) family and TGF-&bgr;1 of transforming growth factor-&bgr; (TGF-&bgr;) family. Commercial LM or HM (high methoxyl) citrus pectins tested did not exhibit any binding activity with bFGF. A weak binding to bFGF was observed with a de-esterified pectin (polygalacturonic acid) prepared from citrus. The binding protected the growth factor from protease digestion. The calcium gel beads prepared with Aloe pectin also bound to these pectin/heparin-binding growth factors. The growth factor could also be encapsulated in the pectin calcium gel and Aloe pectin sodium gel. Pectin/heparin-binding growth factor stabilized by pectin is used for wound healing.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: November 6, 2001
    Assignee: Carrington Laboratories, Inc.
    Inventors: Yawei Ni, Kenneth M. Yates
  • Patent number: 6313104
    Abstract: The invention relates to the use of polysulfated glycosaminoglycans having a sulfur content of at least 12.5% for producing pharmaceutical preparations for inhibiting the &ggr;-interferon-induced upregulation of the MHC Class I and MHC Class II proteins and ICAM-1. The invention furthermore relates to organoprotective solutions comprising polysulfated glycosaminoglycans and to a process for the ex-vivo protection of transplant organs.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: November 6, 2001
    Assignee: Abbott Laboratories
    Inventors: F. J. van der Woude, Benito Yard, Dieter Herr, Volker Laux
  • Patent number: 6313105
    Abstract: Homogeneous mixtures are described and can be processed to give shaped biodegradable and physiologically nonhazardous articles, such as packagings for food or drink or pharmaceutical products, sausage casings and the like. The mixtures comprise dialdehyde starch with a degree of oxidation of greater than 30%, starch which does not exhibit any iodine-starch reaction, and/or modified starch, water and other plasticizers, and also, if desired, other biopolymers and additives.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: November 6, 2001
    Assignee: Aventis Research and Technologies GmbH & Co KG
    Inventors: Holger Bengs, Arnold Schneller, Gitte Böhm, Silke Schuth, Jürgen Grande
  • Patent number: 6313106
    Abstract: The present invention relates to compounds, which are phospholipid derivatives of valproic acid, to compositions comprising said compounds and their use for treating epilepsy, migraine, bipolar disorders and pain.
    Type: Grant
    Filed: July 12, 2000
    Date of Patent: November 6, 2001
    Assignee: D-Pharm Ltd.
    Inventor: Alexander Kozak
  • Patent number: 6313107
    Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: November 6, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
  • Patent number: 6313108
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: July 11, 2000
    Date of Patent: November 6, 2001
    Assignee: Akzo Nobel N.V.
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6313109
    Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: November 6, 2001
    Assignee: Societe de Conseils de Recherches d'Applications Scientifiques, Sas
    Inventor: Sun H. Kim
  • Patent number: 6313110
    Abstract: The present invention relates to a compound of Formula (I): or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as inhibitors of HIV protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
    Type: Grant
    Filed: June 1, 2000
    Date of Patent: November 6, 2001
    Assignee: Dupont Pharmaceuticals Company
    Inventor: George V. DeLucca
  • Patent number: 6313111
    Abstract: Substitued 6H-1,3,4-thiadiazin-2-amines of the following general formula: wherein Ar is phenyl optionally substituted with one or more chloro, bromo atoms, C1-C4 alkoxy, or C1-C4 alkyl groups; and represents a morpholino, thimomorpholino, piperidino, pyrrolidino, or hexamethylenimino moieties, the pharmaceutically acceptable salts thereof and the use of them anasethetic, cardiovascular and hypometabolic agents and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: November 6, 2001
    Assignees: The Procter & Gamble Company, Nauchno-Tekhnologicheskoe Predpriyatie “Ligand” (Tovarischestvo S Ogranichennoi Otvetstvennostiju)
    Inventors: Oleg Nikolaevich Chupakhin, Larisa Petrovna Sidorova, Emma Afanasievna Tarakhty, Antonina Petrovna Novikova, Natalya Mikhailovna Perova, Valentin Antonovich Vinogradov, Michiel Franciscus van Ginkel
  • Patent number: 6313112
    Abstract: The present invention is generally directed to potassium adenosine triphosphate (“KATP”) channel opening compositions. The present invention also relates to the use of KATP channel openers in therapeutic applications. The KATP channel opening compositions of the present invention include diazoxide (7-chloro-3-methyl-2H-1,2,4-benzo-thiadiazine 1,1-dioxide) and aprikalim. According to the present invention, diazoxide and aprikalim can be used independently, or in combination. The present also relates to therapeutic methods for protecting neuronal function utilizing KATP channel openers. Methods of the present invention may be advantageous for protecting neuronal function, prior to medical procedures, after stroke-like events or other events associated with reductions in blood flow, and/or for preserving tissues or organs against cellular injury and death during removal, storage, transplantation or reattachment.
    Type: Grant
    Filed: October 20, 2000
    Date of Patent: November 6, 2001
    Assignee: Wake Forest University
    Inventor: David W. Busija
  • Patent number: 6313113
    Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
    Type: Grant
    Filed: December 2, 1997
    Date of Patent: November 6, 2001
    Assignees: Reddy-Cheminor, Inc., Dr. Reddy's research foundation
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Rajagopalan Ramanujam, Ranjan Chakrabarti
  • Patent number: 6313114
    Abstract: Compounds are provided which have the following formula: wherein: R is hydrogen, alkyl of 1 to 6 carbon atoms, phenyl, or substituted phenyl; X and Y are each, independently, hydrogen, halogen, cyano, or alkoxy of 1 to 6 carbon atoms; and m is 1 to 5; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 30, 1999
    Date of Patent: November 6, 2001
    Assignee: American Home Products Corp
    Inventors: Richard E. Mewshaw, Dahui Zhou, Ping Zhou
  • Patent number: 6313115
    Abstract: Compounds of general structural formula (I) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior.
    Type: Grant
    Filed: October 4, 1999
    Date of Patent: November 6, 2001
    Assignee: The Regents of the University of California
    Inventors: Gary A. Rogers, Christopher M. Marrs
  • Patent number: 6313116
    Abstract: Compounds that are inhibitors of phosphodiesterase and have therapeutic utility, are of formula (i) wherein R1 is C3-6 cycoalkyl, or C1-3 alkyl optionally substituted with one or more fluorine atoms; R2 is C1-6 alkyl, C3-6 cycloalkyl, CF3, CH2CF3, C2F5 or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, are each H, C1-3 alkyl, halogen, CF3 or CN, provided that both are not H; or a pharmaceutically-acceptable salt thereof
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: November 6, 2001
    Assignee: Darwin Discovery, Ltd.
    Inventors: Hazel Joan Dyke, Andrew Sharpe, Hannah Jayne Kendall, Richard John Davenport, Verity Margaret Sabin, George Martin Buckley, Marianna Dilani Richard, Alan Findlay Haughan
  • Patent number: 6313117
    Abstract: Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: November 6, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Rajashehar Betageri, Michel Jose Emmanuel, Eugene Richard Hickey, Weimin Liu, Usha R. Patel, Denice Mary Spero, David S. Thomson, Yancey David Ward, Erick Richard Roush Young, Sanxing Sun
  • Patent number: 6313118
    Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable sal
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: November 6, 2001
    Assignee: Astra Aktiebolag
    Inventors: Stefan Berg, Mats Linderberg, Svante Ross, Seth-Olov Thorberg, Bengt Ulff
  • Patent number: 6313119
    Abstract: Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: November 6, 2001
    Assignees: Adventis Pharma Deutschland GmbH, Genentech, Inc.
    Inventors: Anuschirwan Peyman, David William Will, Jochen Knolle, Karlheinz Scheunemann, Denis Carniato, Jean-Francois Gourvest, Thomas R. Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
  • Patent number: 6313120
    Abstract: The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in Claim 1. These compounds are pharmacologically active.
    Type: Grant
    Filed: June 13, 2000
    Date of Patent: November 6, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
  • Patent number: 6313121
    Abstract: Metalaxyl having a high content of R-enantiomer of more than 70% by weight, or pure R-metalaxyl, in admixture with 4-[3-(4-chloropheny)-3-(3,4-dimethoxyphenyl)acryloyl]morpholine (“dimethomorpho”) or 3-anilino-5-methyl-5-(4-phenoxyphenyl)-1,3-oxazolidine-2,4-dione (“famoxadone”), exhibits a clearly enhanced fungicidal action against plant diseases compared with a mixture of the same kind in which metalaxyl is used in the form of a racemate.
    Type: Grant
    Filed: August 31, 1999
    Date of Patent: November 6, 2001
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Ruth Beatrice Küng, Micha Wicki, Cosima Nuninger, Martin Weiss
  • Patent number: 6313122
    Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: November 6, 2001
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6313123
    Abstract: The compounds of formula B: which are useful in disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: November 6, 2001
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, James M. Chen
  • Patent number: 6313124
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
    Type: Grant
    Filed: January 28, 1998
    Date of Patent: November 6, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
  • Patent number: 6313125
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives are ligands for GABAA receptors useful in the treatment of disorders of dementing illnesses.
    Type: Grant
    Filed: January 14, 2000
    Date of Patent: November 6, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Kevin William Moore, Austin John Reeve
  • Patent number: 6313126
    Abstract: Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, alkylaryl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is carbon or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 30, 1999
    Date of Patent: November 6, 2001
    Assignee: American Home Products Corp
    Inventors: Richard E. Mewshaw, Ping Zhou, Dahui Zhou, Kristin L. Meagher, Magda Asselin, Deborah A. Evrard, Adam M. Gilbert
  • Patent number: 6313127
    Abstract: Compounds of formula (I) in which all variables are defined in the description and their salts inhibit the enzyme oxido squalene cyclase and are useful in treating hypercholesterolemia and also as anti-fungal agents. Processes for their preparation are also described together with their use in medicine.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: November 6, 2001
    Assignee: Zeneca Limited
    Inventors: David Waterson, Elaine Sophie Elizabeth Stokes, George Robert Brown, John Graham Cumming, Nicholas John Newcombe, Robin Wood, William John Watkins
  • Patent number: 6313128
    Abstract: This invention relates to a cosmetic composition containing at least one NPY-antagonist component mixed with an excipient for cosmetic preparations.
    Type: Grant
    Filed: February 9, 2000
    Date of Patent: November 6, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Elisabeth Blanc-Ferras, Francoise Bono-Colombie, Bernard Breda, Jean Courregelongue, Catherine Ducasse, Remy Mounier, Paul Raymond, Michel Sabadie, Claudine Serradeil-Le-Gal, Vilain Pol, Jean-Marie Pereillo
  • Patent number: 6313129
    Abstract: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.
    Type: Grant
    Filed: August 20, 1999
    Date of Patent: November 6, 2001
    Assignee: Hughes Institute
    Inventors: Fatih M. Uckun, Elise A. Sudbeck, Marina Cetkovic, Ravi Malaviya, Xing-Ping Liu
  • Patent number: 6313130
    Abstract: Inhibitors of JAK3 kinase for the treatment of allergy inhibit mast cell degranulation an dmediator release.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: November 6, 2001
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Ravi Malaviya, Elise A. Sudbeck
  • Patent number: 6313131
    Abstract: A method of treating and/or preventing renal dysfunction in a patient, such as renal colic or contrast nephropathy by administering to a patient, a compound of the formula: is described herein. Administration of dyphylline in a sustained release oral dosage form is preferred.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: November 6, 2001
    Assignee: Upsher-Smith Laboratories, Inc.
    Inventor: Carl H. Lawyer
  • Patent number: 6313132
    Abstract: The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary tract incontinence, and methods for preparing the compounds of Formula (I).
    Type: Grant
    Filed: September 27, 1999
    Date of Patent: November 6, 2001
    Assignee: Pharmacia AB
    Inventors: Rolf Johansson, Martin Haraldsson, Erik Ringberg, Ian Vagberg, Katarina Beierlein, Rikard Emond, Birger Sjoberg
  • Patent number: 6313133
    Abstract: Methods for re-establishing normal sleep patterns in adults with age-related sleep disorders are provided. In particular, methods are disclosed wherein a compound that stimulates growth hormone and/or prolactin secretion is orally administered to subjects just prior to retiring.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: November 6, 2001
    Assignee: Arch Development Corporation
    Inventors: Eve Van Cauter, Georges Copinschi
  • Patent number: 6313134
    Abstract: The present invention discloses thaliporphine and its derivatives for the treatment and/or prophylaxis of cardiac diseases, including cardiac arrhythmia, myocardial ischemia or myocardial infarction, and sudden death caused by cardiac arrhythmia or acute myocardial infarction.
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: November 6, 2001
    Assignee: National Science Council
    Inventors: Ming-Jai Su, Shoei-Sheng Lee
  • Patent number: 6313135
    Abstract: A compound of the formula wherein the substituents are as defined in the specification and a method of inhibiting tumors.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: November 6, 2001
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gerard Ulibarri
  • Patent number: 6313136
    Abstract: The present invention relates to imidazo pyridine derivatives of the formula (I), in which the phenyl moiety is substituted, and in which the imidazo pyridine moiety is substituted with a carboxamide group in 6-position, which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: November 6, 2001
    Assignee: AstraZeneca AB
    Inventors: Kosrat Amin, Mikael Dahlström, Peter Nordberg, Ingemar Starke
  • Patent number: 6313137
    Abstract: The present invention relates to imidazo pyridine derivatives of the formula (I), in which the phenyl moiety is substituted, and in which the imidazo pyridine moiety is substituted with a carboxamide group in 6-position, which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: November 6, 2001
    Assignee: AstraZeneca AB
    Inventors: Kosrat Amin, Mikael Dahlström, Peter Nordberg, Ingemar Starke
  • Patent number: 6313138
    Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: November 6, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, George D. Hartman, Randall W. Hartman
  • Patent number: 6313139
    Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: November 6, 2001
    Assignee: Akzo Nobel N. V.
    Inventors: Fredericus Antonius Dijcks, Dirk Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn
  • Patent number: 6313140
    Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.
    Type: Grant
    Filed: June 13, 2000
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc.
    Inventors: Philip A Carpino, Paul A DaSilva-Jardine, Bruce A Lefker, John A Ragan
  • Patent number: 6313141
    Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein: A represents an optionally substituted alkylene group of from 2-5 carbon atoms; W is COH or CH; Y and Z are nitrogen or CH; and R1, R2, R3, R4, R5, R6 are defined herein. Pharmaceutical compositions and preparations containing such compounds are also provided. The invention further relates to the use of such compounds in the treatment of neuropsychological diseases such as schizophrenia and other central nervous system diseases.
    Type: Grant
    Filed: March 8, 2000
    Date of Patent: November 6, 2001
    Assignee: Neurogen Corporation
    Inventor: Xiao-Shu He
  • Patent number: 6313142
    Abstract: Methods of preparing CETP inhibitors are disclosed.
    Type: Grant
    Filed: October 10, 2000
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc.
    Inventors: David B. Damon, Robert W. Dugger
  • Patent number: 6313143
    Abstract: Disclosed are novel substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and methods for the treatment and/or control of cancer.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: November 6, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Nader Fotouhi, Emily Aijun Liu, Allen John Lovey, John Guilfoyle Mullin, Jr., Giuseppe Federico Weber
  • Patent number: 6313144
    Abstract: Compositions are disclosed utilizing the optically pure (−) isomer of norcisapride. This compound is a potent drug for the treatment of gastro-esophageal reflux disease, emesis, dyspepsia and other conditions while substantially reducing the concomitant liability of adverse effects associated with cisapride. The (−) isomer of norcisapride also avoids the adverse drug interactions associated with racemic cisapride and other therapeutic agents.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: November 6, 2001
    Assignee: Sepracor, Inc.
    Inventors: John R. McCullough, A. K. Gunnar Aberg
  • Patent number: 6313145
    Abstract: Indoline derivatives useful as 5HT2C receptor antagonists and methods of using them to treat various CNS disorders are provided.
    Type: Grant
    Filed: December 21, 1998
    Date of Patent: November 6, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventor: Steven Mark Bromidge
  • Patent number: 6313146
    Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 6, 2001
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Bradford C. Van Wagenen, Manuel F. Balandrin, Eric G. DelMar, Edward F. Nemeth
  • Patent number: 6313147
    Abstract: Compounds with fungicidal properties having formula X is CH or nitrogen; R is (C1-C12)alkyl, halo(C1-C12)alkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, (C1-C12)alkoxy(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C3-C7)cycloalkyl(C1-C4)alkyl, aralkyl, aryloxy(C1-C4)alkyl or heterocyclic; R1 is aryl, heterocyclic or C(R6R7R8).
    Type: Grant
    Filed: March 8, 2000
    Date of Patent: November 6, 2001
    Assignee: Dow Agrosciences LLC
    Inventors: Steven Howard Shaber, Lixin Zhang, Edward Michael Szapacs, James Allen Quinn
  • Patent number: 6313148
    Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a —CH(R3)N(R2)B—R1 and —OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is an optionally-substituted pyridyl ring and the group R1 is positioned on B in a 1,3 or 1,4 relationship with the —CH(R3)N(R2)B- linking group. R1, R2 and R3 and D can be a number of different organic or halogen moieties. N-oxides of —NR2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: November 6, 2001
    Assignee: Zeneca Limited
    Inventor: Gloria Anne Breault
  • Patent number: 6313149
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: November 6, 2001
    Assignee: American Home Products Corporation
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen
  • Patent number: 6313150
    Abstract: An &agr;-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 R1 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), NR2 (R2 being hydrogen, alkyl or acyl) or a single bond; and n represents 0, 1 or 2.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: November 6, 2001
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshikazu Ohtsuka, Takami Murashi, Shinji Suzuki, Michio Masuko, Hideyuki Takenaka
  • Patent number: 6313151
    Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: November 6, 2001
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6313152
    Abstract: Disclosed are compounds which inhibit &bgr;-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 &bgr;-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: Grant
    Filed: September 7, 1999
    Date of Patent: November 6, 2001
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Jing Wu, Eugene D. Thorsett, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Lawrence Y. Fang, James E. Audia