Amine Addition Salt Of Organic Phosphorus Containing Acid Patents (Class 514/76)
  • Patent number: 6794371
    Abstract: A method for preventing loss of bone mineral in mammals which method comprises administering to a mammal an amount of an aminoalkylenephosphonate which is effective to prevent or minimize loss of bone material density. The aminoalkylenephophonates of the present invention should have at least one R-N(Alk-PO3H2)2 group or at least two RRN-Alk-PO3H2 groups wherein R and R can be, same or different, aliphatic or cyclic moiety, and Alk is an alkylene group having from 1 to 4 carbon atoms.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: September 21, 2004
    Assignee: The Dow Chemical Company
    Inventor: R. Keith Frank
  • Patent number: 6784168
    Abstract: A synergistic biocide comprises a tris(hydroxymethyl)phosphine or a tetrakis (hydroxymethyl)phosphonium salt and at least one non-surfactant biopenetrant, such as a polymer or copolymer having a plurality of quaternary ammonium groups, a hydrotrope or a syntan, together optionally with a surfactant.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: August 31, 2004
    Assignee: Rhodia Consumer Specialties Limited
    Inventors: Christopher Raymond Jones, Robert Eric Talbot
  • Patent number: 6673378
    Abstract: An anti-catabolic dietary supplement, phosphatidylserine, and diet and exercise programs using phosphatidylserine for lean muscle development and optimized conditioning.
    Type: Grant
    Filed: November 1, 1995
    Date of Patent: January 6, 2004
    Inventor: Robert Fritz
  • Patent number: 6624152
    Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: September 23, 2003
    Assignee: Biogen, Inc.
    Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
  • Patent number: 6593312
    Abstract: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: July 15, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Husson-Robert, Olivier Nosjean, Michelle Boulanger
  • Patent number: 6541462
    Abstract: Cytotoxic tumor therapy in a patient is enhanced by co-administration of sphingomyelin. The invention most likely enhances a tumor cell's ability to undergo ceramide-induced apoptosis by increasing the levels of sphingomyelin in all cellular compartments, thereby providing sufficient substrate for activated sphingomyelinase. A method of treating rheumatoid arthritis also is provided.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: April 1, 2003
    Assignee: Center for Molecular Medicine and Immunology
    Inventor: David Modrak
  • Patent number: 6476006
    Abstract: The present invention provides compacted pharmaceutical composition for oral administration to a patient which expands upon contact with gastric fluid to retain a dosage form in the patient's stomach for an extended period of time, the formulation comprising a non-hydrated hydrogel, a superdisintegrant and tannic acid. The present invention further provides a pharmaceutical dosage form containing an active ingredient, and the compacted pharmaceutical composition. The invention further provides a dosage form suitable for delivering a therapeutic bis-phosphonate such as alendronate to the stomach of a patient over and extended period.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: November 5, 2002
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Moshe Flashner-Barak, Vered Rosenberger, Mazal Dahan, Yitzhak Lerner
  • Publication number: 20020099033
    Abstract: Application of synthetic or naturally occurring lung surfactant to the posterior pharyngeal region prior to a period of sleep significantly reduces episodes of sleep disturbance resulting in apnea or hypopnea. The present invention provides lung surfactant in a convenient applicator container for easy use and storage. Incidents of oxygen desaturation are reduced, thereby lowering the risks of apnea-associated pathologies.
    Type: Application
    Filed: December 10, 2001
    Publication date: July 25, 2002
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Keith C. Meyer, M. Safwan Badr
  • Patent number: 6380174
    Abstract: Disclosed is a slime-removing composition comprising polyhexamethyleneguanidine phosphate and 2-bromo-2-nitro-1, 3-propanediol, represented by the following formulas I and II, respectively. With a synergistic effect, the composition has potent sterilizing activity against a broad spectrum of microorganisms which cause the formation of slime during paper manufacture, including bacteria and fungi. In addition to being excellent in rapid action and persistency of the sterilizing activity, the composition generates resistant mutants at an extremely low frequency, so that there can be obtained an economical favor of maintaining high antimicrobial activity even at a small amount. Also, by virtue of the availability in various phases, numerous applications of the microbicide exist in the various industries including cooling water and sterilizer industries in addition to paper and pulp making industries. wherein m is an integer of 4 to 7 and n is an integer of 1 to 14.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: April 30, 2002
    Assignee: SK Corporation
    Inventors: Hong-Shin Ju, Won-Seong Song
  • Patent number: 6353022
    Abstract: Compositions containing one or more HETE derivative(s) and an effective concentration of ethanol and methods of use for treating dry eye are disclosed.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: March 5, 2002
    Assignee: Alcon Universal Ltd.
    Inventors: L. Wayne Schneider, Daniel A. Gamache, Lori K. Weimer, Timothy L. Kessler, Zhongyou Wei, Terri Pasquine, John M. Yanni, Haresh G. Bhagat
  • Patent number: 6348491
    Abstract: An oil-in-water emulsion for encapsulating paclitaxel including (a) triglyceride , (b) emulsifier including phosphatidyl choline (PC), non-ionic surfactant and polyethyleneglycol-modified disteaoyl phosphatidylethanolamine (PEG-M-DSPE), and (c) pharmaceutically acceptable aqueous solution.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: February 19, 2002
    Assignee: National Science Council
    Inventors: I-Ming Chu, Tzy-Rong Wang
  • Patent number: 6329352
    Abstract: Application of synthetic or naturally occurring lung surfactant to the posterior pharyngeal region prior to a period of sleep significantly reduces episodes of sleep disturbance resulting in apnea or hypopnea. The present invention provides lung surfactant in a convenient applicator container for easy use and storage. Incidents of oxygen desaturation are reduced, thereby lowering the risks of apnea-associated pathologies.
    Type: Grant
    Filed: May 17, 1999
    Date of Patent: December 11, 2001
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Keith C. Meyer, M. Safwan Badr
  • 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: 6300323
    Abstract: A compound Wherein x, y, and z are integers from 0 to 3; and the (poly)ethereal amine is at least one selected from compounds of formula II1 through II5:
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: October 9, 2001
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Takahiro Haga, Kevin E. Crosby, Jeffrey R. Schussler
  • Patent number: 6162427
    Abstract: The invention relates to the use of G-CSF in combination with a chemotherapeutic agent (in particular, cyclophosphamide) to produce a pharmaceutical preparation for boosting the mobilization of hematopoietic stem cells from bone marrow in the treatment of diseases requiring peripheral stem cell transplantation. The claimed combination results in more efficient leukapheresis, e.g. before myeloblative or myelotoxic therapy.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: December 19, 2000
    Assignee: Roche Diagnostics GmbH
    Inventors: Matthias Baumann, Peter-Paul Ochlich
  • Patent number: 6077837
    Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.
    Type: Grant
    Filed: October 23, 1998
    Date of Patent: June 20, 2000
    Assignee: D-Pharm Ltd.
    Inventor: Alexander Kozak
  • Patent number: 6071919
    Abstract: A method of treating a disease in a mammal by administering a therapeutic effective amount of an amphoteric zwitterion compound as an active ingredient. A pharmaceutical composition which comprises an amphoteric zwitterionic compound as an active ingredient in combination with a carrier and other adjunctive pharmaceutical agents.
    Type: Grant
    Filed: November 2, 1998
    Date of Patent: June 6, 2000
    Assignee: T. Ronald Theodore
    Inventors: T. Ronald Theodore, Roscoe L. Van Zandt
  • Patent number: 5958977
    Abstract: A novel phosphoric acid-amino acid complex salt is provided which manifests insolubility in a neutral or alkaline aqueous solution and solubility in an acidic aqueous solution and has a basic amino acid, an alkaline earth metal, and phosphoric acid as main components thereof. An additive composition containing the complex salt and used in a feed for ruminant mammals excels in protection in the first compartment of the stomach of a ruminant mammal and solubility in the fourth compartment of the stomach. This additive composition improves the nutrition of the feed with respect to such a basic amino acid as lysine, a substance frequently missing in the feed for ruminant mammals.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: September 28, 1999
    Assignee: Ajinomoto Co., Inc.
    Inventors: Toru Ikeda, Toshihide Yukawa
  • Patent number: 5958902
    Abstract: Application of synthetic or naturally occurring lung surfactant to the posterior pharyngeal region prior to a period of sleep significantly reduces episodes of sleep disturbance resulting in apnea or hypopnea. The present invention provides lung surfactant in a convenient applicator container for easy use and storage. Incidents of oxygen desaturation are reduced, thereby lowering the risks of apnea-associated pathologies.
    Type: Grant
    Filed: April 16, 1997
    Date of Patent: September 28, 1999
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Keith C. Meyer, M. Safwan Badr
  • Patent number: 5902804
    Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition is also effective against viruses. The composition contains N-phosphonoglycine derivatives which are systemic herbicides.
    Type: Grant
    Filed: February 18, 1997
    Date of Patent: May 11, 1999
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 5902802
    Abstract: Cationic amphiphiles are provided that are alkyl or alkoxyalkyl O-phosphate esters of diacylphosphatidyl zwitterionic compounds such as phosphatidylcholine or phosphatidyl ethanolamine. The amphiphiles can be used as carriers for delivering macromolecules intracellularly.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: May 11, 1999
    Assignee: Megabios Corporation
    Inventor: Timothy D. Heath
  • Patent number: 5897860
    Abstract: The present invention relates to a hemostatic composition comprising at least 0.1 NIH U/ml of thrombin, about 0.01 mU/ml of casein kinase II, and from 10 ng/ml to 100 ng/ml of sphingosine or a sphingosine derivative. The composition is effective in treating patients suffering from hemophilia, ulcers, or microbial infections. In addition, the composition is effective in reducing clotting time during the surgical procedure of suturing blood vessels.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: April 27, 1999
    Assignee: Korea Institute of Science Technology
    Inventors: Seung-Ho Kim, Jin Young Lee, Moon Hi Han
  • Patent number: 5888405
    Abstract: The 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 amino methyl phosphonic acid or salt thereof to inhibit bacterial adhesion to the submergible surface. The invention also relates to a method for controlling biofouling of an aqueous system. This method adds an effective amount of at least one amino methyl phosphonic acid or salt thereof to inhibit bacteria from adhering to a submerged surface within the aqueous system. This method effectively controls biofouling without substantially killing the fouling organisms. The amino methyl phosphonic acid used in the methods of the invention has the formula R.sup.1 R.sup.2 NCH.sub.2 P(O)(OH).sub.2. In this formula, R.sup.1 and R.sup.2 are independently a C.sub.6 -C.sub.20 alkyl group or a CH.sub.2 P(O)(OH).sub.2 group. However, R.sup.1 and R.sup.2 are not both a CH.sub.2 P(O)(OH).sub.2 group. Alternatively, R.sup.1 and R.sup.
    Type: Grant
    Filed: July 29, 1997
    Date of Patent: March 30, 1999
    Assignee: Buckman Laboratories International Inc.
    Inventors: Thomas E. McNeel, Marilyn S. Whittemore, Stephen D. Bryant, Graciela H. Vunk
  • Patent number: 5869338
    Abstract: A method and pharmaceutical for protecting against mutational damage in mammalian cells, irrespective of the nature of the mutagenic event or source of radiational or chemical insult or the like.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 9, 1999
    Assignee: Arch Development Corporation
    Inventor: David J. Grdina
  • Patent number: 5854231
    Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains N-phosphonoglycine derivatives which are systemic herbicides in combination with chemotherapeutic agents for treatment of cancers and tumors. N-phosphonoglycine derivatives can be used to treat viral infections, particularly herpes infections. Optionally potentiators can be included.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: December 29, 1998
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 5716959
    Abstract: A substituted piperazine zwitterion composition containing, for example, as an active ingredient, HEPES (N-2 Hydroxyethylpiperazine-N'-2 Ethane Sulfonic Acid), and method useful for treatment of cancer, autoimmune, arthritis and other mammalian diseases.
    Type: Grant
    Filed: February 13, 1996
    Date of Patent: February 10, 1998
    Assignee: T. Ronald Theodore
    Inventors: T. Ronald Theodore, Roscoe L. Van Zandt
  • Patent number: 5681829
    Abstract: Certain phosphocholine derivatives having substantial antifungal therapeutic activity are disclosed. The phosphocholine derivatives may be chemically synthesized, enzymatically prepared or extracted from the plant Irlbachia alata. The phosphocholine derivatives are useful in treating fungal infections including those which are dermatophytic, systemic, ophthalmic and vaginal.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: October 28, 1997
    Assignee: Shaman Pharmaceuticals, Inc.
    Inventors: Michael Tempesta, Shivanand D. Jolad, Steven King, Guohua Mao, Reimar C. Bruening, John E. Kuo, Thien V. Troung, Donald E. Bierer, Jeffrey M. Dener
  • Patent number: 5665713
    Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition is also effective against viruses. The composition contains N-phosphonoglycine derivatives which are systemic herbicides.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: September 9, 1997
    Assignee: Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 5656615
    Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains a 10:1 to 1:10 mixture of (1) N-chlorophenyl carbamates and N-chlorophenylthiocarbamates and (2) N-phosphonoglycine derivatives which are systemic herbicides. This composition can also be used to treat viral infections.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: August 12, 1997
    Assignee: The Procter & Gamble Company
    Inventor: James Berger Camden
  • Patent number: 5654290
    Abstract: Drug compositions comprised of therapeutically effective amounts of at least one compound selected from the group consisting of:DHA esterified in the form of lysophosphatidyl-choline (lyso-PCDHA) in position sn-2;DHA-phosphatidylcholines (PCDHAs) in which DHA is esterified in position sn-2 and which have an acyl group of [very short length] 2 to 6 carbon atoms in position sn-1;and triglycerides in which DHA is esterified in position sn-2 and which have acyl groups of [very short length] 2 to 6 carbon atoms in positions sn-1 and sn-3.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: August 5, 1997
    Assignees: Institut National de la Sante et de la Recherche Medicale, Imedex
    Inventors: Yves Bayon, Martine Croset, Michel Lagarde, Jean Lecerf, Frank Thies, Jean-Louis Tayot, Veronique Chirouze
  • Patent number: 5627174
    Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the general structure: ##STR1## These Polar compounds are particularly useful for systemic control of pests.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: May 6, 1997
    Assignee: Monsanto Company
    Inventors: Dennis P. Phillion, Peter G. Ruminski, Gopichand Yalamanchili
  • Patent number: 5624917
    Abstract: There is provided a squalene inhibitory composition containing a 1,1-bisphosphonic acid compound, a lower alkyl ester thereof, or a salt thereof, which is useful for treating hypercholesterolemia. There are also provided novel compounds having squalene synthetase inhibitory activity and a pharmaceutical composition for treating hypercholesterolemia containing a 1,1-bisphosphonic compound, a lower alkyl ester thereof or a salt thereof.
    Type: Grant
    Filed: January 16, 1996
    Date of Patent: April 29, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kazuaki Kitano, Takashi Sohda, Ryuichi Tozawa, Hitoshi Ikeda, Tsuneo Oda
  • Patent number: 5593980
    Abstract: This invention provides a new use of acids, esters, and salts of arylmethylphosphonates of Formula I, ##STR1## or a phosphonic acid of Formula II ##STR2## and derivatives as anti-inflammatory and anti-arthritic agents. Representative compounds include 4-dodecyloxybenzylphosphonic acid dimethyl ester, (2-naphthalenylmethyl)phosphonic acid dimethyl ester, and ([1,1'-biphenyl]-2-ylmethyl)phosphonic acid dimethyl ester.
    Type: Grant
    Filed: November 13, 1995
    Date of Patent: January 14, 1997
    Assignee: The Upjohn Company
    Inventor: Roy A. Johnson
  • Patent number: 5585118
    Abstract: The present invention is directed to methods in which a lithium source and a choline source act synergistically to reduce or eliminate the symptoms associated with bipolar disorder.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 17, 1996
    Assignee: Brigham and Women's Hospital
    Inventor: Andrew L. Stoll
  • Patent number: 5578586
    Abstract: A method and composition for reducing evaporation of an aqueous layer from the surface of the eye. The method comprises applying an admixture of a charged phospholipid and a non-polar oil over the eye, preferably in the form of a meta-stable oil in water emulsion in a dosage not exceeding 100 microliters.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: November 26, 1996
    Assignee: Ocular Research of Boston, Inc.
    Inventors: Thomas Glonek, Jack V. Greiner, Donald R. Korb
  • Patent number: 5516798
    Abstract: Described is a method of treating diarrhea in a warm-blooded vertebrate animal, and a composition therefor. The method involves administering to the animal an effective amount of a methylamine, such as betaine. Also described is the use of a composition for the manufacture of a medicament for treatment of diarrhea in a warm-blooded vertebrate animal, wherein the composition contains an effective amount of a methylamine, such as betaine.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: May 14, 1996
    Assignee: North Carolina State University
    Inventor: Peter R. Ferket
  • Patent number: 5500417
    Abstract: This invention provides a new use of acids, esters, and salts of arylmethylphosphonates of Formula I, ##STR1## or phosphonic acid derivatives of Formula II ##STR2## as anti-inflammatory and anti-arthritic agents. Representative compounds include 4-dodecyloxybenzylphosphonic acid dimethyl ester, (2-naphthalenylmethyl)phosphonic acid dimethyl ester, and ([1,1 '-biphenyl]-2-ylmethyl)phosphonic acid dimethyl ester. The invention also provides novel acids, esters, and salts of arylmethylphosphonic acid, phosphonic acid and derivatives.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: March 19, 1996
    Assignee: The Upjohn Company
    Inventor: Roy A. Johnson
  • Patent number: 5496811
    Abstract: An ocular drug delivery vehicle of an oil-in-water submicron emulsion comprising about 0.5 to 50% of a first component of an oil, about 0.1 to 10% of a second component of an emulsifier, about 0.05 to 5% of a non-ionic surfactant and an aqueous component, with the mean droplet size being in the submicron range, i.e., below about 0.5 .mu.m and preferably between about 0.1 and 0.3 .mu.m. Also, topical pharmaceutical compositions containing a drug such as an anti-glaucoma drug, beta adrenergic blocker or other autonomic system drug, a local anesthetic, a steroid, a non-steroidal anti-inflammatory drug, an antibiotic drug, an antifungal drug, an antiviral drug or combinations thereof and the vehicle described above. Methods of administering such vehicles or compositions to the eye of a patient while reducing irritation thereof and providing increased bioavailability of the drug.
    Type: Grant
    Filed: January 5, 1993
    Date of Patent: March 5, 1996
    Assignee: Pharmos Corp.
    Inventors: Haim Aviv, Doron Friedman, Amir Bar-Ilan, Micha Vered
  • Patent number: 5466682
    Abstract: Compounds of formula (I) ##STR1## in which A is (CH.sub.2).sub.n in which n is 1-10, preferably 3 or 5, and R is the acyl group from a known anti-inflammatory agent, exhibit high anti-inflammatory activity. The mechanism of action is novel because they do not release the anti-inflammatory agent in the body but exhibit an activity superior to the activity of the known anti-inflammatory agent. The compounds are also active in combating bone calcium loss.
    Type: Grant
    Filed: July 26, 1993
    Date of Patent: November 14, 1995
    Assignee: Istituto Gentili S.p.A.
    Inventors: Sergio Rosini, Maurizio Mian
  • Patent number: 5461040
    Abstract: P-substituted aminoalkylphosphinic acids of the formula ##STR1## wherein R denotes an optionally fluorinated methyl group, R.sub.1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.sub.2 and R.sub.3 denote hydrogen or R.sub.2 denotes hydroxy, lower alkoxy or halogen and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together represent an oxo group, and their pharmaceutically acceptable salts are active as GABA.sub.b -agonists and can be used in the treatment of spinal spasticity, multiple sclerosis and cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain. They can be manufactured by methods known per se and suitable such methods are described.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: October 24, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Roger G. Hall, Ludwig Maier, Wolfgang Frostl
  • Patent number: 5447922
    Abstract: .alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is alkyl, arylalkyl or aryl; R.sup.4 is H or pharmaceutically acceptable cation;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: September 5, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: R. Michael Lawrence, Scott A. Biller, Olga M. Fryszman
  • Patent number: 5434144
    Abstract: The subject invention relates to methods of regulating skin wrinkles and/or atrophy in mammalian skin comprising topically applying to the skin of a mammal in need of treatment a composition comprising a safe and effective amount of a cyclic polyanionic polyol derivative having the structure: ##STR1## wherein n is an integer from 1 to 3; and each X is, independently, selected from the group consisting of OSO.sub.3.sup.-, OPO.sub.3.sup..dbd., SO.sub.3.sup.--, PO.sub.3.sup..dbd., CO.sub.2.sup.--, and OH; with at least 3 X's being other than OH.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: July 18, 1995
    Assignee: The Procter & Gamble Company
    Inventors: Gerald B. Kasting, John M. Gardlik
  • Patent number: 5407921
    Abstract: A method for suppressing a bitter taste of material to be placed in mouth or in contact with mouth, such as foods, drinks, pharmaceuticals, comprises adding an acidic phospholipid or an acidic lysophospholipid to the material.
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: April 18, 1995
    Assignee: Kao Corporation
    Inventors: Yoshihisa Katsuragi, Takeshi Yasumasu, Tomoshige Umeda, Susumu Yamasawa, Yuki Mitsui
  • Patent number: 5294607
    Abstract: A method and composition for reducing evaporation of an aqueous layer from the surface of the eye. The method comprises applying an admixture of a charged phospholipid and a non-polar oil over the eye, preferably in the form of a meta-stable oil in water emulsion in a dosage not exceeding 100 microliters.
    Type: Grant
    Filed: June 9, 1992
    Date of Patent: March 15, 1994
    Assignee: Ocular Research of Boston, Inc.
    Inventors: Thomas Glonek, Jack V. Greiner, Donald R. Korb
  • Patent number: 5292497
    Abstract: A method of decreasing the toxicity of chemical therapeutic agents administered in cancer chemotherapy including adminstration to a patient undergoing chemotherapy. This reduction in toxicity can be accomplished by administering an effective amount of S-3-(3-methylaminopropylamino)propyl dihydrogen phosphorothioate. Methods of inducing mucolytic activity and reducing toxicity of acetominophen overdose are also discussed. Such activities are induced through the administration of S-3-(3-methylaminopropylamino)propyl dihydrogen phosphorothioate.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: March 8, 1994
    Assignee: U.S. Bioscience, Inc.
    Inventors: Philip S. Schein, James R. Piper
  • Patent number: 5284835
    Abstract: This invention encompasses pharmaceutical compositions and a dietary supplement for treating or preventing alcoholic cirrhosis of the liver which comprises administering about 1 to 3 grams per day of dilinoleoylphosphatidylcholine (DLPC).
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: February 8, 1994
    Inventor: Charles S. Lieber
  • Patent number: 5278152
    Abstract: The compound of the formula I ##STR1## in which R is an aldehyde group or a group which can be converted into an aldehyde, R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium or triethylamnonium, orR.sup.1 and R.sup.2 together form a cyclic diester,R.sup.3 and R.sup.4 are alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R.sup.5 and R.sup.8 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, and X, Y or Z are oxygen or sulfur, or prodrug forms of the compound of the formula I can be used for the treatment of diseases caused by viruses.The preparation of these compounds and pharmaceutical preparations containing them and their use is described.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: January 11, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Anuschirwan Peyman, Eugen Uhlmann, Irvin Winkler, Matthias Helsberg, Christoph Meichsner
  • Patent number: 5278151
    Abstract: A method and composition for reducing evaporation of an aqueous layer from the surface of the eye. The method comprises applying an admixture of a charged phospholipid and a non-polar oil over the eye, preferably in the form of a finely divided oil in water emulsion.
    Type: Grant
    Filed: June 9, 1992
    Date of Patent: January 11, 1994
    Assignee: Ocular Research of Boston, Inc.
    Inventors: Donald R. Korb, Thomas Glonek, Jack Greiner
  • Patent number: 5262405
    Abstract: A composition for use in the treatment of the obstruction of air ways comprising one or more phospholipids, alone or in association with excipients. This composition can be used in a method of treating the obstruction of air ways in a patient.
    Type: Grant
    Filed: February 20, 1991
    Date of Patent: November 16, 1993
    Assignees: Synthelabo, Inserm
    Inventors: Sophie Girod-Vaquez, Edith Puchelle, Claude Galabert, Jean-Marie Zam, Denis Pierrot
  • Patent number: 5229376
    Abstract: Encapsulated PI compositions such as liposomes containing plant PI and th use to prevent mitogenic transformation of normal splenic lymphoid cells (including lymphocytes transformed induced by treatment of cells with lipid A) by exposing the cells thereto.
    Type: Grant
    Filed: March 12, 1991
    Date of Patent: July 20, 1993
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Carl R. Alving, Earl C. Richardson