Thioureas (i.e., N-c(=s)-n Patents (Class 514/580)
  • Publication number: 20040092487
    Abstract: The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension.
    Type: Application
    Filed: October 27, 2003
    Publication date: May 13, 2004
    Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE GOVERNMENT OF THE U.S., as represented by the Sec. of the Dept. of Health and Human Services
    Inventors: Deanna L. Kroetz, Darryl C. Zeldin, Bruce D. Hammock, Christophe Morisseau
  • Publication number: 20040082626
    Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism:
    Type: Application
    Filed: July 25, 2003
    Publication date: April 29, 2004
    Inventors: Hiroshi Takemoto, Masami Takayama, Yutaka Yoshida
  • Publication number: 20040044034
    Abstract: Compounds are described which modulate the tzrosine kinase activity of p56lck and signal transduction pathways in which this enzyme is involved. The invention also relates to compounds which have immunomodulatory activity, e.g., which have immunosuppressant or immunostimulatory activity, and/or which have an antineoplastic effect. The invention further relates to compositions comprising these compounds, and methods of using them.
    Type: Application
    Filed: January 22, 2003
    Publication date: March 4, 2004
    Inventors: Jun Hayashi, Alexander D. Mackerell
  • Publication number: 20040043082
    Abstract: Methods and preparations for treating disorders of the eye and/or causing dissolution of corneal proteoglycans and organized healing of corneal stroma, softening of the cornea for non-surgical refractive correction of eyesight, removing corneal haze and opacification, inhibiting fibroblasts and preventing corneal fibrosis and scar formation, treating pterigiums and treating corneal neovascularization as well as iris neovascularization. Preparations containing a) urea, b) urea derivatives (e.g., hydroxyurea, thiourea), c) antimetabolites, e) urea, urea derivatives, non-enzymatic proteins, nucleosides, nucleotides and their derivatives (e.g.
    Type: Application
    Filed: March 14, 2003
    Publication date: March 4, 2004
    Applicant: Vitreo-Retinal Technologies, Inc.
    Inventors: Vicken H. Karageozian, David Castillejos, John Park, Gabriel Arthuro Carpio Aragon, Jose Luis Gutierres Floress
  • Publication number: 20040034069
    Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.
    Type: Application
    Filed: August 8, 2003
    Publication date: February 19, 2004
    Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
  • Publication number: 20040006044
    Abstract: S-alkylsiothiouronium derivatives such as S-ethylisothiouronium diethylphosphate are used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of nausea and vomiting. The compositions of the invention are also effective in preventing or alleviating emesis associated with migraines or other medical conditions such as chemotherapy or radiotherapy, as well as other symptoms of migraines including phonophobia and photophobia.
    Type: Application
    Filed: March 5, 2003
    Publication date: January 8, 2004
    Applicant: MEDITOR PHARMACEUTICALS LTD.
    Inventors: Raphael Barkan, Alexander Mirimsky
  • Patent number: 6660284
    Abstract: The present invention relates to novel compounds corresponding to formula (I) below: The invention also relates to the process for manufacturing them, to their use as pigments and to a cosmetic composition comprising them.
    Type: Grant
    Filed: April 9, 2002
    Date of Patent: December 9, 2003
    Assignee: L'Oreal
    Inventors: Thierry Bordier, Michel Philippe
  • Publication number: 20030203944
    Abstract: The present invention relates to an antagonist against vanilloid receptor and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fevescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.
    Type: Application
    Filed: February 3, 2003
    Publication date: October 30, 2003
    Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Young Ho Park, Jung Bum Yi
  • Publication number: 20030199574
    Abstract: Methods for treating disorders of the eye and/or disorders of a nerve in a human or veterinary patient by delivering to the patient a therapeutically effective amount of a compound selected from the group of; urea, urea derivatives, thiourea, thiourea derivatives, guanidine, guanidine derivatives and compounds having General Formula I as set forth herein. For ophthalmic applications, the compound may be delivered by intravitreal injection such that the compound causes vitreal liquefaction, posterior vitreoretinal detachment and other affects.
    Type: Application
    Filed: February 13, 2003
    Publication date: October 23, 2003
    Applicant: Vitreo-Retinal Technologies, Inc.
    Inventors: Vicken H. Karageozian, David Castillejos, John Park
  • Publication number: 20030195202
    Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Application
    Filed: January 24, 2003
    Publication date: October 16, 2003
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: David M. Armistead, Michael C. Badia, Guy W. Bemis, Randy S. Bethiel, Catharine A. Frank, Perry M. Novak, Steven M. Ronkin, Jeffrey O. Saunders
  • Publication number: 20030180388
    Abstract: The present invention relates to compositions and methods for the protection and restoration of hearing. In particular, the present invention relates to methods and compositions for the prevention of chemical (e.g., cisplatin) induced deafness. The present invention thus provides methods of improving the outcome of subjects treated with cisplatin.
    Type: Application
    Filed: January 16, 2003
    Publication date: September 25, 2003
    Applicant: The Regents of the University of Michigan
    Inventors: Goran Laurell, Andreas Ekborn, Josef Miller, Hans Ehrsson
  • Patent number: 6608227
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: August 19, 2003
    Assignee: Bristol-Myers Squibb Pharma
    Inventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
  • Publication number: 20030153596
    Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.
    Type: Application
    Filed: July 9, 2002
    Publication date: August 14, 2003
    Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
  • Publication number: 20030119905
    Abstract: The present invention is based on the discovery that nitric oxide (NO) is an important growth regulator in an intact developing organism. In particular, the present invention relates to a method of increasing in a mammal a population of hematopoietic stem cells in bone marrow which are capable of undergoing normal hematopoiesis and differentiation, wherein the bone marrow is contacted with an inhibitor of NO, such as an inhibitor of nitric oxide synthase (NOS), thereby producing bone marrow having an increased population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis and differentiation. The present invention also relates to a method of increasing a population of cells in S phase in a tissue of a mammal, comprising contacting the tissue with an inhibitor of NO, such as an inhibitor of NOS. The invention also pertains to a method of regenerating tissue in an adult mammal comprising contacting a selected tissue (e.g.
    Type: Application
    Filed: November 4, 2002
    Publication date: June 26, 2003
    Applicant: Cold Spring Harbor Laboratory
    Inventors: Grigori N. Enikolopov, Natalia I. Peunova, Boris A. Kuzin, Hollis Cline, Tatiyana Michurina
  • Patent number: 6545052
    Abstract: A method is provided for inhibiting free radical degradation in the skin of a human or nonhuman animal comprising contacting the skin with a skin treatment composition having a concentration of a 1-(3-methoxybenzyl)-3-substituted thiourea compound effective for inhibiting free radical generation. Skin protecting compositions comprising a free radical inhibiting concentration of a 1-(3-methoxybenzyl)-3-substituted thiourea compound, and optionally a sunscreeen composition, are also provided.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: April 8, 2003
    Assignee: Fan Tech, Ltd.
    Inventors: Alan Wohlman, Anthony J. O'Lenick, Jr.
  • Patent number: 6534542
    Abstract: Compounds of formula (i) and of formula (ii) wherein the symbols have the meaning disclosed in the specification, specifically or selectively modulate &agr;2B and/or &agr;2C adrenergic receptors in preference over &agr;2A adrenergic receptors, and as such are useful for alleviating chronic pain and allodynia and have no or only minimal cardivascular and/or sedatory activity.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: March 18, 2003
    Assignee: Allergen Sales, Inc.
    Inventors: Ken Chow, Daniel W. Gil, Wenkui Ken Fang, Michael E. Garst
  • Publication number: 20030008884
    Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: 1
    Type: Application
    Filed: August 6, 2001
    Publication date: January 9, 2003
    Applicant: Aventis CropScience S.A.
    Inventors: Vincent Gerusz, Darren James Mansfield, Jose Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
  • Publication number: 20020183315
    Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), 1
    Type: Application
    Filed: May 23, 2002
    Publication date: December 5, 2002
    Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
  • Publication number: 20020177627
    Abstract: This patent discloses the use of poly-substituted isothiouronium salts (T1 where R1, R2, R3, R4=hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl, etc. and X−=Cl−, Br−, NO3−, CH3CO2−, or any other common anion), poly-substituted guanidinium salts (G1 where R1, R2, R3, R5, R6=hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl, etc. and X−=Cl−, Br, NO3−, CH3CO2−, or any other common anion), or mixtures of two or more of the above compounds, as the biocidal component of microbiocidal or anti-fouling formulations.
    Type: Application
    Filed: June 28, 2002
    Publication date: November 28, 2002
    Applicant: RhoCraft Research Development, Ltd.
    Inventors: Thomas M. Fyles, Robert D. Rowe
  • Patent number: 6479458
    Abstract: A method for preventing retinal ganglion cell depth, associated with glaucoma, in an animal of the mammalian species, including humans, comprising the step of administering to ganglion cells and their axons (optic nerve) of said mammal a pharmaceutical composition which comprises as its active ingredient one or more compounds having activity for blocking a reverse mode of the sodium/calcium exchanger.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: November 12, 2002
    Assignee: Allergan, Inc.
    Inventors: Joseph S. Adorante, George R. Ehring, Kara L. Kopper
  • Patent number: 6476076
    Abstract: The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: November 5, 2002
    Assignees: Pacific Corporation, Digital Biotech Co., Ltd.
    Inventors: Jeewoo Lee, Uhtaek Oh, Young-Ho Park, Young-Ger Suh, Hyeung-Geun Park, Hee-Doo Kim
  • Publication number: 20020161051
    Abstract: Compounds of formula (i) and of formula (ii) 1
    Type: Application
    Filed: February 27, 2001
    Publication date: October 31, 2002
    Applicant: ALLERGAN SALES, INC.
    Inventors: Ken Chow, Daniel W. Gil, Wenkui Ken Fang, Michael E. Garst
  • Patent number: 6469034
    Abstract: Novel CycloHexenyl-Ethyl-Thiourea (CHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: October 22, 2002
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Ventatachalam
  • Publication number: 20020072518
    Abstract: The present invention relates to a class of compounds represented by the Formula I 1
    Type: Application
    Filed: August 29, 2001
    Publication date: June 13, 2002
    Inventors: Ish Kumar Khanna, Yi Yu, Balekudru Devadas, Hwang-Fun Lu, Nizal S. Chandrakumar, Renee M. Huff, Bipinchandra N. Desai, Srinivasan Raj Nagarajan
  • Patent number: 6395189
    Abstract: A process is provided for both removing and controlling biofilms present in industrial cooling and process waters. The process provides a composition which includes the reaction products of an amino base, a formaldehyde, an alkylenepolyamine, and the ammonium salt of an inorganic or organic acid. The composition may be used to remove existing biofilms from process water equipment. Further, lower maintenance dosages may be used to maintain the equipment in a substantially biofilm-free condition.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: May 28, 2002
    Assignee: Polymer Ventures, Inc.
    Inventors: Jon O. Fabri, Walter D. Heslep
  • Patent number: 6342499
    Abstract: The present invention provides a method to control parasitic and saprophagous mites on beneficial insects such as honeybees via the application of a parasiticidally or saprophagouscidally effective amount of a mitochondrial electron transport inhibitor or a pyrimidine compound of formula I.
    Type: Grant
    Filed: July 12, 1999
    Date of Patent: January 29, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Bruce Christian Black, William R. Baumbach, Michael P. Beluch
  • Publication number: 20010039276
    Abstract: Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.
    Type: Application
    Filed: December 20, 2000
    Publication date: November 8, 2001
    Applicant: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Ventatachalam
  • Patent number: 6313172
    Abstract: Methods and compositions for the treatment of pain using this area derivatives. Particularly disclosed are new compositions for the treatment of chronic pain, and methods for their use.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: November 6, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Ken Chow, Daniel W. Gil, Wenkui Ken Fang, Michael E. Garst, Larry A. Wheeler
  • Publication number: 20010021378
    Abstract: There are described a flowable composition for controlling harmful insects and representatives of the order Acarina, comprising at least one pesticidally active compound, one or more signal substances selected from the group consisting of pheromones, kairomones and attractants, a UV absorber or a UV absorber mixture and, if appropriate, one or more additives selected from the group consisting of viscosity-regulating thickeners, fillers, solvents and other formulation auxiliaries,
    Type: Application
    Filed: February 22, 2001
    Publication date: September 13, 2001
    Inventors: Dieter Hofer, Max Angst, Pierre-Joseph Charmillot
  • Patent number: 6207715
    Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: March 27, 2001
    Assignee: American Home Products Corporation
    Inventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
  • Patent number: 6149822
    Abstract: A process is provided for both removing and controlling biofilms present in industrial cooling and process waters. The process provides a composition which includes the reaction products of an amino base, a formaldehyde, an alkylenepolyamine, and the ammonium salt of an inorganic or organic acid. The composition may be used to remove existing biofilms from process water equipment. Further, lower maintenance dosages may be used to maintain the equipment in a substantially biofilm-free condition.
    Type: Grant
    Filed: March 1, 1999
    Date of Patent: November 21, 2000
    Assignee: Polymer Ventures, Inc.
    Inventors: Jon O. Fabri, Walter D. Heslep
  • Patent number: 6075022
    Abstract: The present invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one thiourea to inhibit bacterial adhesion to the submergible surface. The present invention also relates to a method for controlling biofouling of an aqueous system. This method adds an effective amount of at least one thiourea to inhibit bacteria from adhering to a submerged surface within the aqueous system. This method effectively controls biofouling without substantially killing the bactaria. The thiourea used in the method of the invention has the following formula a compound of the formula: The present invention also relates to compositions containing thiourea compounds and useable in the above methods. The compositions comprise at least one thiourea in an amount effective to inhibit bacteria from adhering to submergible or submerged surfaces.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: June 13, 2000
    Assignee: Buckman Laboratories International Inc.
    Inventors: Mark L. Zollinger, Stephen D. Bryant
  • Patent number: 6036992
    Abstract: Enteral formulas that contain long-chain polyunsaturated fatty acids (PUFAs) and a process for making such enteral compositions are described. More particularly, the invention relates to enteral compositions which provide long chain PUFAs arachidonic acid (AA) and docosahexaenoic acid (DHA) essentially free of cholesterol and may be derived from egg yolk lipids, and thus are predominantly in a phospholipid form. The process of making such a composition provides improved organoleptic and stability properties. Enteral compositions according to this invention may be used to feed infants, particularly pre-term infants, to promote neural development and development of visual acuity, and to reduce the incidence of necrotizing enterocolitis.
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: March 14, 2000
    Assignee: Abbott Laboratories
    Inventors: David A. Borror, David V. Diodato, Debra L. Ponder, Margaret H. Dohnalek
  • Patent number: 5952386
    Abstract: 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: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5871950
    Abstract: The present invention provides methods for treating autoimmune diseases in mammals and for preventing or treating transplantation rejection in a transplant recipient. The methods of treatment involve the use of drugs capable of suppressing expression of MHC Class I molecules. In particular the use of the drug methimazole to suppress expression of MHC Class I molecules in the treatment of autoimmune diseases and the prevention or treatment of rejection in a transplant recipient is disclosed. In addition in vivo and in vitro assays are provided for the assessment and development of drugs capable of suppressing MHC Class I molecules.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 16, 1999
    Inventors: Dinah S. Singer, Leonard Kohn, Edna Mozes, Motoyasu Saji, Jocelyn Weissman, Giorgio Napolitano, Fred D. Ledley
  • Patent number: 5591775
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein for use in the treatment of a disorder of the melatoninergic system.
    Type: Grant
    Filed: December 6, 1994
    Date of Patent: January 7, 1997
    Assignee: Adir et Compagnie
    Inventors: Patrick Depreux, Hamid A. Mansour, Daniel Lesieur, Fran.cedilla.ois Lefoulon, Pierre Renard, Gerard Adam, Philippe Delagrange
  • Patent number: 5574054
    Abstract: Novel quaternary ammonium salts having utility in the medical field for treating gastrointestinal disorders.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: November 12, 1996
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Osamu Kitagawa, Katsuyuki Ishii, Seiichi Niwa, Sigeru Ueki, Masao Seiki
  • Patent number: 5449690
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, and medicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: September 12, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick DePreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5449689
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: September 12, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5416117
    Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: February 28, 1994
    Date of Patent: May 16, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5371102
    Abstract: Methods of using N,N'-disubstituted thiocarbamide compounds for reversibly inhibiting hyperthyroidism are provided. Active compounds reversibly inhibit catalytic iodination without producing sulfenic acid intermediates which can permanently inactivate thyroid peroxidase. By preventing sulfenic acid formation, side effects due to toxicity in liver and bone marrow can be reduced compared to currently used drugs. The compounds can be formulated for administration to a hyperthyroid patient until remission occurs with less risk of possible everdosing.
    Type: Grant
    Filed: August 6, 1993
    Date of Patent: December 6, 1994
    Assignee: University of Hawaii
    Inventor: Daniel Doerge
  • Patent number: 5328909
    Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: July 12, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5318768
    Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and a crystalline contrast agent in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
    Type: Grant
    Filed: February 17, 1993
    Date of Patent: June 7, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Carl R. Illig, Eugene R. Cooper
  • Patent number: 5198012
    Abstract: A biocide composition comprises an effective amount of a biocide and an effective amount of a biocide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a hydroxyalkyl phosphate, a polyoxyalkylene alkyl ether phosphate, a salt thereof, a polyoxyalkylene alkenyl ether phosphate, a salt thereof, a polyoxyalkylene hydroxyalkyl ether phosphate and a salt thereof.
    Type: Grant
    Filed: May 21, 1991
    Date of Patent: March 30, 1993
    Assignee: Kao Corporation
    Inventor: Tetsuji Iwasaki
  • Patent number: 5075110
    Abstract: A process for stabilizing attenuated lyophilized vaccines with a compound having the general formula: ##STR1## wherein R1 is an oxygen atom or a sulphur atom and R2 is a NH.sub.2 group or a linear chain, unsaturated or not, selected from the group consisting of --O--C . . . , --NH--C . . . , and --C . . . .
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: December 24, 1991
    Assignee: Institut Merieux
    Inventors: Alain J. Francon, Bernard J. Montagnon
  • Patent number: 5043008
    Abstract: A biocide composition comprises an effective amount of a biocide and an effective amount of a biocide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a hydroxyalkyl phosphate, a polyoxyalkylene alkyl ether phosphate, a salt thereof, a polyoxyalkylene alkenyl ether phosphate, a salt thereof, a polyoxyalkylene hydroxyalkyl ether phosphate and a salt thereof.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: August 27, 1991
    Assignee: Kao Corporation
    Inventor: Tetsuji Iwasaki
  • Patent number: 5006539
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: March 6, 1989
    Date of Patent: April 9, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4707478
    Abstract: This invention relates to methods for the prophylactic and curative treatment of gastrointestinal and cardiovascular disorders and parasitic infections in humans and animals, using a class of hetrocyclic amidino substituted urea and thiourea compounds, a novel class of heterocyclic amidino substituted urea and thiourea compounds and pharmaceutical compositions and animal feed additives including the same.
    Type: Grant
    Filed: September 16, 1982
    Date of Patent: November 17, 1987
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: William L. Studt, Harry K. Zimmerman, Stuart A. Dodson
  • Patent number: 4701457
    Abstract: Amidinoureas are disclosed as useful for the treatment of irritable bowel syndrome.
    Type: Grant
    Filed: January 13, 1984
    Date of Patent: October 20, 1987
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John Yelnosky, Ghulam N. Mir
  • Patent number: 4628061
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: August 23, 1983
    Date of Patent: December 9, 1986
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson