Z Radical Contains Sulfur Or Halogen Patents (Class 514/550)
  • Patent number: 6284258
    Abstract: The present invention relates to compounds that are two-part molecules, and compositions containing such compounds, in which one part is designed to become covalently bonded to the skin (bonding agent) and the other part (a characteristic use agent) is designed to impart some characteristic use, such as emolliency, moisturizing effect, anti-acne, anti-wrinkle, anti-pain, antimicrobial, antifungal, antiviral, anti-irritation, skin tanning and skin lightening effects, extended protection of the skin (e.g., from ultraviolet light, by incorporation of a sunscreen component; from toxic and/or irritating substances; from insects and skin parasites, by incorporation of insecticides and/or insect repellants; from free radicals or other agents, as in aging, by incorporation of antioxidants), or dyeing of hair, skin nails, wool or fuir. The covalently bonded part may also be useful to impart skin strengthening effect (e.g., from shear forces) or as wound healing agents.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: September 4, 2001
    Assignee: Arizona Board of Regents
    Inventors: Seth D. Rose, Rosemarie F. Hartman, Carmen Chow, Cathryn M. Rose, K. Daniel Rose
  • Patent number: 6277883
    Abstract: There is disclosed a method of treating male impotence in a person in need of such treatment, which comprises enhancing the effectiveness of the person's immune system by the administration to such person of at least one aliphatic sulfur compound, preferably a sulfur-containing amino-acid derivative having the formula (I) in which A is hydrogen or a carboxymethylene -CH2CO2H group, B is hydrogen or an alkyl group having 1 to 3 carbon atoms, and X is hydrogen, or an acyl group —CO—R in which R is an alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable salt of such compound.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: August 21, 2001
    Inventor: Arthur Vanmoor
  • Publication number: 20010008904
    Abstract: The present invention relates to a method for supplying bioavailable methionine to a cow which comprises supplying to the cow an ester of methionine or methionine amide and/or an ester of the hydroxy analogue of methionine or a salt thereof.
    Type: Application
    Filed: February 28, 2001
    Publication date: July 19, 2001
    Applicant: RHONE-POULENC ANIMAL NUTRITION
    Inventors: Jean-Claude Robert, Robert Bennett, Georges Gros
  • Publication number: 20010000784
    Abstract: A method of suppressing immune responses, comprising administering to a patient in need thereof an effective amount of a composition comprising a substance capable of reducing the content of reductive glutathione in macrophages.
    Type: Application
    Filed: December 8, 2000
    Publication date: May 3, 2001
    Applicant: AJINOMOTO CO. INC.
    Inventors: Junji Hamuro, Yukie Murata
  • Patent number: 6221909
    Abstract: The present invention relates to a method for supplying bioavailable methionine to a cow which comprises supplying to the cow an ester of methionine or methionine amide and/or an ester of the hydroxy analogue of methionine or a salt thereof.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: April 24, 2001
    Assignee: Rhône-Poulenc Animal Nutrition
    Inventors: Jean-Claude Robert, Robert Bennett, Georges Gros
  • Patent number: 6187944
    Abstract: Acrylonitrile compounds having pesticidal activity of formula (I) and salts thereof. wherein Q is Y is ═C(R4)— or ═N—, R1 is alkyl, haloalkyl, etc., each of R2 and R3 is halogen, alkyl which may be substituted, alkenyl which may be substituted, etc., R4 is hydrogen, halogen, alkyl or haloalkyl, 1 is from 1 to 4, m is from 0 to 5, n is from 0 to 3, q is from 0 to 4, when 1 is 2 or more, a plurality of R2 may be the same or different, when each of m, n and q is 2 or more, a plurality of R3 may be the same or different.
    Type: Grant
    Filed: August 16, 1999
    Date of Patent: February 13, 2001
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Koji Sugimoto, Tsuyoshi Ikeda, Munekazu Ogawa
  • Patent number: 6153609
    Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: November 28, 2000
    Assignee: Pfizer Inc
    Inventors: Ralph P. Robinson, Todd A. Blumenkopf
  • Patent number: 6136331
    Abstract: A cosmetic containing fluorine-containing oil represented by the following formula do not inhibit the oil repellency of powder treated with a fluorine-containing compound, is excellent in affinity for the skin, and is inexpensive.
    Type: Grant
    Filed: December 29, 1998
    Date of Patent: October 24, 2000
    Assignee: Daikin Industries LTD
    Inventors: Masamichi Morita, Eiji Seki, Motonobu Kubo
  • Patent number: 6130250
    Abstract: Use of the compound of formula I (as described in the specification) in the therapy of veterinary diseases, the expression of which is enhanced by increasing stock density.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: October 10, 2000
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: David George Sidney Burch, Paul Howard Ripley, Erich Zeisl
  • Patent number: 6096762
    Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel .alpha.,.alpha.-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: May 21, 1999
    Date of Patent: August 1, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Gene M. Dubowchik, Bireshwar Dasgupta, Dolatrai M. Vyas
  • Patent number: 6069169
    Abstract: The present invention is directed to the use of compounds of Formula (I), depicted below, as active principals for treating skin conditions; compositions containing these compounds; and methods of treating skin conditions using these compounds and compositions. ##STR1## wherein R.sub.4 is (CR.sub.5 R.sub.6 --CR.sub.7 R.sub.8 --X.sub.1).sub.n --CR.sub.9 R.sub.10 R.sub.11, n is an integer from 1 to 18; R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, are independently, hydrogen or non-hydrogen substituents; and X, X.sub.1, Y and Z are independently, 0, NH, or S.
    Type: Grant
    Filed: June 2, 1997
    Date of Patent: May 30, 2000
    Assignee: Avon Products, Inc.
    Inventors: Dmitri Ptchelintsev, Neil Scancarella, Robert Kalafsky
  • Patent number: 6046237
    Abstract: There are disclosed compounds of the general formula (I): alkyl-X-CH.sub.2 COOR wherein alkyl represents a saturated or unsaturated hydrocarbon of 8-26 carbon atoms, X represents a sulfur atom or a selenium atom and R is hydrogen or C.sub.1 -C.sub.4 alkyl. Said compounds are used for the manufacturing of medicaments for the treatment of hyperlipidemic conditions, (arteriosclerotic disease), coronary artery disease and for reducing the concentration of lipids in blood of mammals, for inhibiting oxidative modification of LDL, and for reducing proliferation of cancer cells. Methods for preparing the compounds are also disclosed.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: April 4, 2000
    Inventors: Rolf Berge, Jon Songstad
  • Patent number: 6046236
    Abstract: (1) Prostaglandin (PG) E.sub.2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): ##STR1## cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient,(2) carbocyclic sulfonamides represented by the compound of the formula (II): ##STR2## cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore,(4) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient.The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.
    Type: Grant
    Filed: May 5, 1997
    Date of Patent: April 4, 2000
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Nobuyuki Hamanaka, Tsumoru Miyamoto
  • Patent number: 5977160
    Abstract: The invention involves a method for treating a human survivor of a heart attack and provides further improvement in survival following the heart attack by the early initiation and long-term administration of an angiotensin converting enzyme inhibitor. The angiotensin converting enzyme inhibitor may be used on its own, or in conjunction with other therapeutic compounds such as data blockers and thrombolytic agents. The preferred angiotensin converting enzyme inhibitor is captopril.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: November 2, 1999
    Assignee: Brigham and Women's Hospital, Inc.
    Inventors: Marc A. Pfeffer, Janice M. Pfeffer, Eugene Braunwald
  • Patent number: 5968727
    Abstract: The invention comprises a novel pyruvate compound for the treatment of prevention of reperfusion injury following ischemia, diabetic effects, cholesterol levels, injured organs ethanol intoxication oras s foodstuff. The novel pyruvate compound is particularly a puruvate thiolester, a glucerol-pyruvate ester or a dihydoxyacetone-pyruvate ester.
    Type: Grant
    Filed: March 1, 1999
    Date of Patent: October 19, 1999
    Assignee: Case Western Reserve University
    Inventors: Henri Brunengraber, Catherine Bomont, France David, Peter T. Hallowell
  • Patent number: 5932229
    Abstract: Described are the use of compounds of Formula (I), depicted below, as active principals for treating skin conditions; compositions containing these compounds; and methods of treating skin conditions using these compounds and compositions. ##STR1## wherein R.sub.4 is (CR.sub.5 R.sub.6 --CR.sub.7 R.sub.8 --X.sub.1).sub.n --CR.sub.9 R.sub.10 --C(.dbd.X.sub.2)X.sub.3 R.sub.11, n is an integer from 1 to 18; R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, are independently, hydrogen or non-hydrogen substituents; and X, X.sub.1, X.sub.2, X.sub.3, Y and Z are independently, O, NH, or S.
    Type: Grant
    Filed: May 2, 1997
    Date of Patent: August 3, 1999
    Assignee: Avon Products, Inc.
    Inventors: Dmitri Ptchelintsev, Neil Scancarella, Robert Kalafsky
  • Patent number: 5925668
    Abstract: The present invention provides compounds with antioxidant activity effective in treating free radical mediated diseases.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: July 20, 1999
    Assignee: ASTA Medica Aktiengesellschaft
    Inventors: Gerreke Biewenga, Guido R. M. M. Haenen, Aalt Bast
  • Patent number: 5889056
    Abstract: A compound of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group, each optionally substituted by one to three groups independently selected from: --CN; --NO.sub.2 ; a group --COR.sup.2 wherein R.sup.2 is hydrogen, C.sub.1-6 alkyl, --OR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-6 alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected from hydrogen or C.sub.1-6 alkyl; a group --S(O).sub.m R.sup.6 wherein m is 0, 1 or 2, R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxy or NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-6 alkyl; a group PO(OR.sup.9).sub.2 wherein R.sup.9 is hydrogen or C.sub.1-6 alkyl; a group NR.sup.10 R.sup.11 wherein R.sup.10 and R.sup.11 are independently selected from hydrogen, C.sub.1-6 alkyl, --COR.sup.12 wherein R.sup.12 is hydrogen or C.sub.
    Type: Grant
    Filed: December 27, 1996
    Date of Patent: March 30, 1999
    Assignee: Glaxo Wellsome Inc.
    Inventors: Harold Francis Hodson, Richard Michael John Palmer, David Alan Sawyer, Richard Graham Knowles, Karl Witold Franzmann, Martin James Drysdale, Patricia Ifeyinwa Davies, Helen Alice Rebecca Clark, Barry George Shearer, Steven Smith
  • Patent number: 5874469
    Abstract: Fluoroalkyl hydrocarbons as vehicles for pharmaceutical drugs are disclosed. These vehicles are particularly well-suited for delivering drugs which are insoluble in water or chemically unstable in aqueous media. Pharmaceutical solution compositions based on these vehicles have long shelf lives and provide improved drug bioavailability. In addition, the pharmaceutical compositions of the present invention are nonaqueous, and therefore do not require preservatives or tonicity agents. The invention is particularly useful in the field of ophthalmology.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: February 23, 1999
    Assignee: Alcon Laboratories, Inc.
    Inventors: Manoj L. Maniar, John C. Lang
  • Patent number: 5874468
    Abstract: Novel brain targeted low molecular weight, hydrophobic antioxidants and use of antioxidants in treatment of central nervous system neurodegenerative disorders such as Parkinson's, Alzheimer's and Creutzfeldt-Jakob's diseases and in treatment of conditions of peripheral tissues, such as acute respiratory distress syndrome, amyotrophic lateral sclerosis, atheroscierotic cardiovascular disease and multiple organ disfunction, in which oxidants are overproduced.
    Type: Grant
    Filed: December 26, 1996
    Date of Patent: February 23, 1999
    Assignees: Yissum, Mor
    Inventors: Daphne Atlas, Eldad Melamed, Daniel Ofen
  • Patent number: 5863931
    Abstract: Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: January 26, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: Richard Mansfield Beams, Harold Francis Hodson, Richard Michael John Palmer
  • Patent number: 5861435
    Abstract: A method for preventing settlement of aquatic fouling organisms on surface of an aquatic structure without environmental hazard is provided. The method is based upon absolutely novel concept to prevent the settlement by means of thick slime layer, i.e. bio-jelly, deposited on said surface. The present invention also provides a bio-jelly producing agent and a bio-jelly producing paint both useful for the present method. Further, the present invention provides a novel low toxic antifouling agent.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: January 19, 1999
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Junji Yokoi, Isao Nakamura, Ryoji Hamade, Naoki Yamamori, Hiroharu Ohsugi, Akio Harada
  • Patent number: 5843755
    Abstract: A mold belonging to the genus Ascochyta is cultivated with a medium to obtain a culture. A compound having a structure represented by the following formula and having an antitumor activity, which is capable of forming a tautomeric equilibrium mixture composed of tautomers, is collected from the culture, or a mixture of the tautomers is collected from the culture.
    Type: Grant
    Filed: June 10, 1997
    Date of Patent: December 1, 1998
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yoko Obayashi, Toshihiko Yoshimura, Yuka Ikenoue, Ryosuke Fudo, Masahiro Murata, Toshihiko Ando
  • Patent number: 5827883
    Abstract: A method of using vitamin D derivatives of the formula ##STR1## wherein X is .dbd.CH.sub.2 or H,H;Y is a moiety--CH(CH.sub.3)--(A).sub.n --C(O)--OR.sup.1 (a)--CH(CH.sub.3)--CH.sub.2 --O--C(O)--R.sup.2 (b)or--C(O)--OR.sup.1 (c);A is --CH.dbd.CH-- or CH.sub.2 --CH.sub.2 --R.sup.1 is lower alkyl, cycloalkyl, cycloalkylmethyl, --CH.sub.2 R.sup.3 or --CH.sub.2 --CH.sub.2 R.sup.3 ;R.sup.2 is lower alkyl, cycloalkyl or R.sup.3 ;R.sup.3 is hydroxy-lower alkyl, hydroxy-cycloalkyl or trifluoromethyl-hydroxy-lower-alkyl;n is 0 or 1;and the dotted bond in the five membered ring is optional;in the treatment of dermatological conditions, in particular keratinization disorders such as psoriasis, as well as acne and photodamaged skin, is described.Vitamin D derivatives of the formula I above, wherein X, Y, A, R.sup.1, R.sup.2, R.sup.3 and n are as set forth above; with the proviso that X is H,H when Y is --CH(CH.sub.3)--CH.sub.2 --OC(O)--C(OH)(CH.sub.3).sub.
    Type: Grant
    Filed: July 21, 1997
    Date of Patent: October 27, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Marc Muller, Josef Stadlwieser
  • Patent number: 5821237
    Abstract: The subject invention relates to compositions which are useful for improving the visual appearance of skin, especially facial skin. The composition contains certain primary actives including at least one cyclic polyanionic polyols at least one sulfhydryl compound and at least one zwitterionic surfactant. The subject invention further relates to methods of improving the visual appearance of skin.
    Type: Grant
    Filed: December 11, 1995
    Date of Patent: October 13, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Donald Lynn Bissett, Gerald Bruce Kasting, Kay Lesley Powers
  • Patent number: 5801274
    Abstract: N-?Mercaptoacyl(amino acid or peptide)! compounds and S-lipophilic aliphatic carbonyl derivatives thereof, and pharmaceutical compositions comprising such compounds, as well as the use of these compounds as antihypertensives by the inhibition of neutral endopeptidase and/or peptidyldipeptidase A are disclosed. Methods for preparing such compounds and derivatives are disclosed also.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 1, 1998
    Assignee: Institut National de la Sante et de la Recherche Medicale
    Inventors: Marie-Claude Fournie-Zaluski, Bernard-Pierre Roques
  • Patent number: 5780489
    Abstract: The invention provides a method for treating amyotrophic lateral sclerosis in a patient which comprises administering to the patient an effective amount of a non-cysteine glutathione precursor or a glutathione derivative so as to increase the intracellular glutathione levels and alleviate a symptom of amyotrophic lateral sclerosis. The non-cysteine substrate may be a thiazolidine-4-carboxylate analog, a thiazolidine-4-carboxylate analogs ester, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 21, 1996
    Date of Patent: July 14, 1998
    Inventor: Benjamin Rix Brooks
  • Patent number: 5760076
    Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: October 10, 1995
    Date of Patent: June 2, 1998
    Assignees: G.D Searle & Co., Monsanto Company
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5700840
    Abstract: Fluorinated alkene compounds useful for controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the formula BrCF.sub.2 CFClCH.sub.2 CO--R where R is R.sub.1 or R.sub.2. R.sub.1 is --SR.sub.5, halogen, --NHOH or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic or aromatic group; an aliphatic amine group; an aliphatic carboxylic acid group; or R.sub.5 and R.sub.6 when taken with the N of R.sub.1 are an amino acid or a cyclic group or R.sub.1 is --OR.sub.5, where R.sub.5 is an aliphatic or aromatic group; an aliphatic amine group; or an aliphatic carboxylic acid group. R.sub.2 is --SR.sub.5 or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic, aromatic or heterocyclic group; an aliphatic amine group; an aliphatic carboxylic acid group; R.sub.5 and R.sub.6 when taken with the N of R.sub.2 are an amino acid or a cyclic group; R.sub.5 and R.sub.6 when taken with the N of R.sub.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: December 23, 1997
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Peter Gerrard Ruminski, Gopichand Yalamanchili
  • Patent number: 5679332
    Abstract: The hair shaping composition for permanent shaping of hair contains a cysteine ester of the formula (I):HS--CH.sub.2 --CH(NH.sub.2)--COO--CH.sub.2 --CH.sub.2 --R (I)as a keratin-reducing material, wherein R is a hydroxy group, alkoxy groups, a poly(alkoxy) group or a hydroxypoly(alkoxy) group, or one of its acid additional salts. Cysteine ester compounds and their methods of preparation are also described. Preferred embodiments of the hair shaping composition have a pH of from 4.5 to 9.0 and contain from 4 to 30% by weight of the cysteine ester or its acid addition salt and provide a safe and uniform shaping of hair without allergic or sensitizing reactions.
    Type: Grant
    Filed: November 16, 1995
    Date of Patent: October 21, 1997
    Assignee: Wella Aktiengesellschaft
    Inventors: Hans-Juergen Braun, Guenther Lang, Gerhard Maresch
  • Patent number: 5667776
    Abstract: Damage to cells, tissue and other body parts in a mammalian host may be treated by using a tumor necrosis factor in conjunction with at least one biological modifier, which may be a free radical scavenger or a metabolic inhibitor. The biological modifier is preferably uric acid, buthionine sulphoximine, vitamin C, aspirin, or nordihydroguaiaretic acid. Such a combination may be used to treat, for example, cancer, infectious diseases, and damage caused by radiation therapy, high oxygen tension, and chemotherapy.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: September 16, 1997
    Assignee: Chiron Corporation
    Inventors: Robert Zimmerman, Benedict J. Marafino, Jr.
  • Patent number: 5637619
    Abstract: The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhy drazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.
    Type: Grant
    Filed: July 5, 1995
    Date of Patent: June 10, 1997
    Assignee: Yale University
    Inventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh
  • Patent number: 5602164
    Abstract: Obesity is treated by the administration to a subject of a compound having the general formula (I): R.sub.4 --(CH.sub.2).sub.n --CO--N(R.sub.1)--CH(R.sub.2)--CO(--R.sub.3), wherein R.sub.1 represents H or CH.sub.3 ; R.sub.2 represents a side chain of a naturally occurring amino acid; R.sub.3 represents OH, OCH.sub.2 CH.sub.3 and NH.sub.2 ; n is 6-18; and R.sub.4 represents CH.sub.3 or a group having the general formula (II): R.sub.3 --CO--CH(R.sub.2)--N(R.sub.1)--CO--, wherein R.sub.1, R.sub.2 and R.sub.3 have the above meanings. The compounds of formula (I) wherein R.sub.4 is a group of formula (II), are novel compounds.
    Type: Grant
    Filed: March 18, 1996
    Date of Patent: February 11, 1997
    Assignee: Senyorina Ltd.
    Inventors: Meir Shinitzky, Avner Shenfeld
  • Patent number: 5571794
    Abstract: A cosmetic treatment for inducing upper and lower lip augmentation in humans, wherein an active ingredient encouraging vasodilatation, preferably an ultra highly diluted homeopathic, ultra highly diluted element, local irritant or direct local vasodilator or a combination of two or more is administered by topical application or sublingually or gum by chewing. The vasodilators singly or in combinations of preferably ultra highly diluted elements, homeopathics, local irritant or vasodilators are diluted to preferably ten to fifteen percent for topical administration in a cosmetic cream or cosmetic gel or oral sublingual drops diluted in a 2% alcohol base or a five percent fructose-coated chewing gum. The treatment results in a significant non-invasive augmentation of both the upper and lower lip that onsets within a few moments and is effective for a duration on an average of four and one half hours.
    Type: Grant
    Filed: June 22, 1995
    Date of Patent: November 5, 1996
    Inventor: Bruce M. Frome
  • Patent number: 5536723
    Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: July 16, 1996
    Assignee: Brigham & Women's Hospital
    Inventors: Joseph Loscalzo, John Cooke
  • Patent number: 5491170
    Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is --O--, --S--, or --NR.sub.2 --, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: February 13, 1996
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 5491169
    Abstract: Compounds having the properties of morphinic substances, particularly anasia, with beneficial effects on behaviour and with peripheral effects without their major drawbacks (tolerence, addiction), the blood-brain barrier and having the following formula :H.sub.2 N--CH(R.sub.1)--CH(R.sub.2)--S--S--CH(R.sub.3)--CH(R.sub.4)--A--B--Zwherein: AB preferably represents a CO amide bond, R.sub.2 et R.sub.3 preferably represent a hydrogen atom, R.sub.1 et R.sub.4 preferably represent, independently of each other, a benzyl grouping, --CH.sub.2 CH.sub.2 SCH.sub.3, --CH.sub.2 --CH.sub.2 --S(O)--CH.sub.3 or --CH.sub.2 --CH(CH.sub.3) .sub.2, Z may represent a --CH(R.sub.5)[CH(R.sub.6)].sub.n --COO(R.sub.7) grouping wherein: R.sub.5 may represent a hydrogen atom, a methyl grouping, a benzyl grouping or a phenyl grouping, R.sub.6 may represent a hydrogen atom and may also form a hydrocarbon cycle with R.sub.5, or Z may represent a heterocyclic grouping, and preferably a morpholinyl grouping. No drawings.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: February 13, 1996
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Bernard Roques, Marie C. Fournie-Zaluski
  • Patent number: 5441748
    Abstract: An aqueous agent for disintegrating gallstones containing an alkali metal carbonate such as sodium or potassium hydrogen carbonate and optionally N-acetylcysteine.
    Type: Grant
    Filed: November 10, 1993
    Date of Patent: August 15, 1995
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventor: Akihito Moyiyasu
  • Patent number: 5411991
    Abstract: A method of reducing the rate of mammalian hair growth includes topically applying a composition containing a sulfhydryl reactive compound to the skin.
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: May 2, 1995
    Inventors: Douglas Shander, Gurpreet S. Ahluwalia, Diana M-D. Grosso
  • Patent number: 5393764
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5391571
    Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: February 21, 1995
    Assignee: American Home Products Corporation
    Inventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
  • Patent number: 5378692
    Abstract: A method of lowering lipids is disclosed wherein a patient is administered a lipid metabolism improving composition characterized by comprising a compound of the following formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group; R.sub.2 and R.sub.3 are the same or different and each represents a hydroxyl group, a lower alkoxy group or an amino group, or a pharmacologically acceptable salt thereof as an active ingredient.Since the compound of the present invention lowers blood triglyceride, cholesterol and .beta.-lipoprotein levels, it is of value for ameliorating hyperlipidemia in arteriosclerotic diseases, e.g. myocardinal infarction, angina pectoris, cerebral infarction, cerebral arteriosclerosis, etc., nephrosis, hypertension, diabetes, obesity and other diseases, and prevention of various circulatory diseases.
    Type: Grant
    Filed: July 6, 1993
    Date of Patent: January 3, 1995
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Shinji Ohmori, Kazumi Ogata, Hideki Tsuruoka, Takahiro Sakaue, Yuuichi Isowaki, Yasuko Umegaki
  • Patent number: 5262436
    Abstract: Mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: August 6, 1991
    Date of Patent: November 16, 1993
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 5242681
    Abstract: The present invention relates to contrast enhancing agents, conjugates thereof, pharmaceutical compositions thereof, and methods for diagnostic analysis, particularly NMR image analysis using these agents. The contrast enhancing agents are chelates of paramagnetic, ferromagnetic or diamagnetic metal ion(s) complexed with new lipophilic complexing acids related to polyaminopolycarboxylic acids.
    Type: Grant
    Filed: August 4, 1992
    Date of Patent: September 7, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Gabriel A. Elgavish, Sung K. Kim
  • Patent number: 5202347
    Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.
    Type: Grant
    Filed: January 17, 1992
    Date of Patent: April 13, 1993
    Inventor: Nicholas S. Bodor
  • Patent number: 5200549
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl; ##STR2## wherein R.sub.2 is lower alkyl; R.sub.3 is phenyl, or phenyl substituted by 1 to 3 substituents selected from the group consisting of halo, lower alkyl, and lower alkoxy; and R.sub.4 is hydrogen or methyl or the corresponding hydroxy acid of formula ##STR3## and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as described above; or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, an acetylamino-substituted-C.sub.1-4 alkyl ester of said acid, a phenyl-dimethylamino ester of said acid or a .alpha.-monoglyceride of said acid.The compounds of formulas I and II are useful as agents for the treatment of hyperproliferative skin diseases such as psoriasis.
    Type: Grant
    Filed: September 24, 1991
    Date of Patent: April 6, 1993
    Assignee: Hoffman-La Roche Inc.
    Inventors: Peter M. Wovkulich, Milan R. Uskokovic, Ann Goldstein, John A. McLane
  • Patent number: 5187183
    Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.
    Type: Grant
    Filed: June 14, 1991
    Date of Patent: February 16, 1993
    Assignee: Brigham & Women's Hospital
    Inventors: Joseph Loscalzo, John Cooke
  • Patent number: 5185355
    Abstract: Synergistic microbicidal compositions are disclosed, comprising 4,5-dichloro-2-cyclohexyl-3-isothiazolone and one or more known microbicides for more effective, and broader control of microorganisms in various systems.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: February 9, 1993
    Assignee: Rohm and Haas Company
    Inventor: Jemin C. Hsu
  • Patent number: 5147893
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts and stereoisomers or geometric isomers thereof.
    Type: Grant
    Filed: May 9, 1991
    Date of Patent: September 15, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: RE34805
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: December 6, 1994
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon