N-c(=x)-n, N-c(=n)n, N-n, Nitrogen Directly Bonded To Oxygen By Nonionic Bonding Or Cyano Containing Patents (Class 514/482)
  • Patent number: 6410574
    Abstract: The present invention relates to a fungicidal composition obtained by mixing a 1,2,3-thiadiazole derivative of general formula (I) useful as a plant disease controller with at least one fungicide selected from the compounds having a fungicidal activity against plant diseases, and to a method for using the same: wherein R1 is hydrogen, alkyl or cycloalkyl and R2 is CO—Y—R3, wherein Y is O, S, NR4 or the like and R3 is hydrogen, alkyl, phenyl, 5- or 6-membered heterocycle or the like.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: June 25, 2002
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Tsutomu Nishiguchi, Tsuyoshi Takemoto, Sohkichi Tajima, Yoshinobu Yamamoto
  • Patent number: 6395763
    Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs 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 and compositions of this invention.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: May 28, 2002
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean P. Stamos, Randy S. Bethiel
  • Patent number: 6387949
    Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
    Type: Grant
    Filed: June 1, 2000
    Date of Patent: May 14, 2002
    Assignee: AstraZeneca Canada Inc.
    Inventors: Daniel Delorme, Vlad Gregor, Niklas Plobeck, Edward Roberts, Eric Sun
  • Patent number: 6331542
    Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: December 18, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Thomas Joseph Carr, Renee Louise Desjarlais, Timothy Francis Gallagher, Stacie Marie Halbert, Hye-Ja Oh, Scott Kevin Thompson, Daniel Frank Veber, Dennis Shinji Yamashita, Jack Hwekwo Yen
  • Patent number: 6297275
    Abstract: A method for controlling fungi using a phenylhydrazine derivative compound of the formula: wherein: X is phenyl, phenylalkoxy, phenoxy, or benzyl, alone or in combination with one or more halogen, alkyl, or alkylthio; Y is hydrogen, alkanoyl, haloalkanoyl, or alkoxy carbonyl; and R is hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, or phenylalkoxy.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: October 2, 2001
    Assignees: Uniroyal Chemical Company, Inc., Crompton Co./Cie
    Inventors: Mark Achiel Dekeyser, Kenneth Wesley Seebold, Jr., Gaik-Lean Chee
  • Patent number: 6294581
    Abstract: The production of IgA is selectively inhibited by orally administering 15-deoxyspergualin or pharmacologically acceptable salts thereof, thus preventing and treating IgA-associated immunological diseases such as IgA nephropathy.
    Type: Grant
    Filed: September 18, 2000
    Date of Patent: September 25, 2001
    Assignee: Takara Shuzo Co., Ltd.
    Inventors: Kazutoh Takesako, Hideharu Saito, Ikunoshin Kato
  • 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: 6284777
    Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, inducing osteoporosis; gingival disease including gingivitis and periodontists; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: September 4, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Stacie Marie Halbert, Scott Kevin Thompson
  • Patent number: 6239151
    Abstract: The invention provides hydrazine derivatives of the formula wherein R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is an acyl group derived from an &agr;-, &bgr;-, &ggr;- or &dgr;-(amino, hydroxy or thiol)carboxylic acid in which the amino, hydroxy or thiol group is optionally lower alkylated or the amino group is optionally acylated, sulphonylated or amidated and in which any functional group present in a side-chain is optionally protected, or a group of the formula Het(CH2)mCO; R3 is hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl-lower alkenyl, aryl or heterocyclyl; R4 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a groupin
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: May 29, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
  • Patent number: 6147120
    Abstract: A synergistic composition and a synergistic system for use in treating the skin and hair of people and animals comprises separate treatment compositions (solution, dispersions, emulsions, suspensions or other liquid or liquefiable materials). One treatment with a first composition that may comprise at least 0.1% by weight of antimicrobially active aliphatic phenol derivative and treatment with another composition being selected from the group consisting of:a) a solution comprising an antimicrobially active cationic species;b) a comprising antimicrobially active aliphatic phenol derivative, preferably in a different weight percentage of antimicrobially active aliphatic phenol derivative than said one composition, comprising greater than 0.3% antimicrobially active aliphatic phenol derivative;c) a solution comprising an alcohol provides a synergistic antimicrobial action.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: November 14, 2000
    Assignee: Ecolab Inc.
    Inventors: Sally K. Swart, John Hilgren, William Feil, Mary Bennett
  • Patent number: 6110968
    Abstract: Methods are provided for measuring the accumulation of advanced glycosylation endproducts (AGEs), and for lowering the accumulation of advanced glycosylation endproducts, which are predicated on the discovery that such AGEs and their precedent glycotoxins are present in tobacco and its byproducts. More particularly, the methods focus on the observation that individuals who smoke or otherwise use tobacco have increased levels of AGEs relative to non-smoking individuals. The present methods relate to the measurement of AGE levels in both individuals and in tobacco and its byproduct, smoke, and to the treatment of such individuals with agents capable of reacting with glycosylation products to either avert or diminish the accretion of AGEs in the body.
    Type: Grant
    Filed: November 10, 1998
    Date of Patent: August 29, 2000
    Assignee: The Picower Institute for Medical Research
    Inventors: Richard J. Bucala, Helen Vlassara, Anthony Cerami, Carla J. Cerami, Henry W. Founds
  • Patent number: 6077866
    Abstract: Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.
    Type: Grant
    Filed: May 10, 1996
    Date of Patent: June 20, 2000
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Yoshinori Kitagawa, Katsuaki Wada, Yoshiko Kyo, Yuichi Otsu, Yumi Hattori, Toru Obinata, Takahisa Abe, Katsuhiko Shibuya, Wolfram Andersch
  • Patent number: 6043284
    Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: February 5, 1998
    Date of Patent: March 28, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
  • Patent number: 6040338
    Abstract: The present invention relates to a compound of the formula wherein R.sup.1 and R.sup.2 are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R.sup.3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R.sup.4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.
    Type: Grant
    Filed: November 3, 1997
    Date of Patent: March 21, 2000
    Assignee: Yale University
    Inventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh, Shu-Hui Chen
  • Patent number: 6022891
    Abstract: Compounds with fungicidal properties are presented having the formula ##STR1## wherein m and n are 0 or 1; X is hydrogen, halo, C.sub.1 -C.sub.4) alkyl or alkoxy; Z is (C.sub.1 -C.sub.12) alkyl or haloalkyl; R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen, a halogen, lower alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, arylcycloalkyl, or heterocyclyl, optionally substituted with one or more halogen atoms.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: February 8, 2000
    Assignee: Rohm and Haas Company
    Inventors: Ronald Ross, Ted Tsutomo Fujimoto, Steven Howard Shaber
  • Patent number: 5998470
    Abstract: Disclosed herein is a compound of the formula ##STR1## known as 2-[N-(N-benzyloxycarbonyl-L-leucinyl)]-2'-[N'-[4-(N,N-dimethylaminomethyl) benzyloxy]carbonyl-L-leucinyl]carbohydrazide; and pharmaceutically acceptable salts, hydrates and solvates thereof.
    Type: Grant
    Filed: April 13, 1999
    Date of Patent: December 7, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Stacie Marie Halbert, Scott Kevin Thompson, Daniel Frank Veber
  • Patent number: 5965619
    Abstract: Substituted indene derivatives are useful for treating patients having precancerous lesions and for inhibiting the growth of neoplastic cells.
    Type: Grant
    Filed: December 23, 1997
    Date of Patent: October 12, 1999
    Assignee: Cell Pathways Inc.
    Inventors: Rifat Pamukcu, Gary A. Piazza, Paul Gross, Gerhard Sperl, Klaus Brendel
  • 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: 5874465
    Abstract: Compounds having the structural formula: ##STR1## wherein: R is C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.9 aralkyl, or nitroso; R' is C.sub.1 -C.sub.4 alkyl; and R" is C.sub.1 -C.sub.4 alkyl. These compounds exhibit insecticidal and miticidal activity.
    Type: Grant
    Filed: October 24, 1996
    Date of Patent: February 23, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Mark Achiel Dekeyser, Paul Thomas McDonald
  • Patent number: 5798383
    Abstract: The prevent invention provides a compound of formula (I): ##STR1## wherein Ar is (a) phenyl, naphthyl and biphenyl, each optionally substituted with C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 hydroxyalkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.2-4 alkoxyalkoxy, C.sub.1-4 alkylthio, hydroxy, halo, cyano, amino, C.sub.1-4 alkylamino, di (C.sub.2-8) alkylamino, C.sub.2-6 alkanoylamino, carboxy, C.sub.2-6 alkoxycarbonyl, or optionally substituted phenyl, phenoxy, phenylthio or phenylsulfinyl or (b) furyl, benzo?b!furyl, thienyl, benzo?b!thienyl, pyridyl or quinolyl, each optionally substituted with C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halo, C.sub.1-4 alkoxy, optionally-substituted phneyl, phenoxy or phenylthio, X is C.sub.1 -C.sub.4 alkylene, C.sub.2 -C.sub.4 alkenylene, --(CHR.sup.1).sub.m --Q.sup.1 --(CHR.sup.2).sub.n --, --O--(CHR.sup.1).sub.j --Q.sup.2 -- and --(CHR.sup.1)--O--N.dbd. in which the N.dbd. moiety is attached to the cycloalkene ring; and in which Q.sup.1 is O, S, SO, SO.sub.2, NR.
    Type: Grant
    Filed: May 8, 1997
    Date of Patent: August 25, 1998
    Assignee: Pfizer Inc.
    Inventors: Akiyoshi Kawai, Makoto Kawai, Rodney W. Stevens
  • Patent number: 5773469
    Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: June 30, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
  • Patent number: 5709890
    Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: January 20, 1998
    Assignee: Donlar Corporation
    Inventor: J. Larry Sanders
  • Patent number: 5656660
    Abstract: The present invention describes compounds, methods and compositions effective to treat mast cell mediated inflammatory conditions, such as conjunctivitis, asthma and allergic rhinitis. The compounds of the invention comprise novel mono- and di-aminomethylbenzyl, aminobenzyl, guanidylbenzyl and benzyl tryptase inhibitors. The compositions for treating mast cell mediated inflammatory conditions include oral, inhalant and topical preparations as well as devices comprising such preparations.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: August 12, 1997
    Assignee: Arris Pharmaceutical Corporation
    Inventors: Robert T. Lum, Heinz W. Gschwend, Barr E. Bauer, Elaine Kuo, Ken Rice
  • Patent number: 5646133
    Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: July 8, 1997
    Assignee: Donlar Corporation
    Inventor: J. Larry Sanders
  • Patent number: 5626883
    Abstract: A vitamin C supplement comprising ascorbic acid, ascorbyl palmitate, niacinamide ascorbate, calcium ascorbate, magnesium ascorbate, potassium ascorbate, and sodium ascorbate which together can be administered to a human to avoid the transitory initial suppression of human NK cell activity which is present when ascorbic acid alone is administered. Also included is xylitol, lysine acetate, tetrasodium pyrophosphate, ribose, cysteine, and hesperidin which further prolongs the biological activity of ascorbic acid and promotes the uptake of ascorbic acid by human tissue.
    Type: Grant
    Filed: April 15, 1994
    Date of Patent: May 6, 1997
    Assignee: Metagenics, Inc.
    Inventor: Stephen M. Paul
  • Patent number: 5482947
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: January 9, 1996
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
  • Patent number: 5476870
    Abstract: The present invention relates, by way of novel industrial products, to compounds which are structurally related to 15-deoxyspergualin. These novel compounds have the formula ##STR1## in which: n is equal to 6 or 8 andA is a single bond, CH.sub.2, CHF, CH(OH), CH(OCH.sub.3), CH.sub.2 NH or CH.sub.2 O,and their addition salts.
    Type: Grant
    Filed: December 2, 1993
    Date of Patent: December 19, 1995
    Assignee: Fournier Industrie ET Sante
    Inventors: Patrice Renaut, Luc Lebreton, Patrick Dutartre, Philippe Derrepas, Soth Samreth
  • Patent number: 5475027
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: December 12, 1995
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
  • Patent number: 5356931
    Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.
    Type: Grant
    Filed: January 4, 1993
    Date of Patent: October 18, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
  • Patent number: 5214061
    Abstract: This invention relates to p-acylaminophenoxycarbamates having the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, aryl and arylloweralkyl; R.sub.3 is hydrogen, loweralkyl, arylloweralkyl; R.sub.4 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkyl, phenylcarbonyl, arylloweralkylcarbonyl, substituted phenylcarbonyl, pyridylcarbonyl, and substituted pyridylcarbonyl with the proviso that if R.sub.4 contains a carbonyl group directly attached to the oxygen of the N-O moiety, R.sub.3 cannot be hydrogen; or R.sub.3 and R.sub.4 taken together from a heterocyclic ring selected from the group consisting of imidazole or loweralkylimidazole; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; and p is an integer selected from 0 and 1; the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and stereoisomers and racemic mixtures thereof.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: May 25, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Allen, Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5208236
    Abstract: Novel glutarylamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: R.sup.1 and R.sup.3 are independently hydroxy, lower alkoxy, aryllower alkoxy, amino, lower alkylamino and di-(lower alkyl)amino;R.sup.2 is H or hydroxy;R.sup.4 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;R.sup.6 is H or R.sup.7 --(CH.sub.2).sub.3 --, wherein R.sup.7 is amino or (aryllower alkoxy)carbonylamino;Q is --C(O)-- or --SO.sub.2 --;Y is lower alkyl, lower alkoxy, aryllower alkoxy, amino, lower alkylamino, di-(lower alkyl)amino, or a group of the formula ##STR2## wherein A is a bond, --N(R.sup.5)--, or --O--; and R.sup.5 is H or lower alkyl;B is H or Z--(CH.sub.2).sub.m --Z is amino, lower alkylamino, di-(lower alkyl)amino, (aryllower alkoxy)carbonylamino, 1-pyrrolidino or 1-piperidino;m=1,2,3,4 or 5; and n=1,2 or 3; oror a pharmaceutically acceptable addition salt thereof; useful in the treatment of cardiovascular disorders, are disclosed.
    Type: Grant
    Filed: September 23, 1992
    Date of Patent: May 4, 1993
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 5192537
    Abstract: Immunoreactive cells sensitized for an antigenic marker associated with a malignant tumor are prepared in vitro by collecting the tumor patient's own mononuclear cells, depleting suppressor T-cells, suspending the mononuclear cells with serum, preferably autologous, and culturing the cells under conditions to activate and immunize the patient's mononuclear cells against the patient's tumor. Methods of treatment and immunized cells in pharmaceutical presentations are described.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: March 9, 1993
    Assignee: Cellcor Inc.
    Inventor: Michael E. Osband
  • Patent number: 5166153
    Abstract: Novel N-acylated 2-[4-(halophenoxy)-phenoxy]-ethylcarbamic acid esters of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.8 alkyl or C.sub.3 -C.sub.5 alkenyl,R.sub.2 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, --CO--R.sub.7 or --NR.sub.8 R.sub.9,R.sub.3 and R.sub.4 independently of one another are hydrogen or methyl,R.sub.5 is chlorine or fluorine,R.sub.6 is either the same substituent as R.sub.5 or is hydrogen,R.sub.7 is C.sub.1 -C.sub.8 alkoxy or --NR.sub.10 R.sub.11,R.sub.8 is C.sub.1 -C.sub.4 alkyl,R.sub.9 is C.sub.1 -C.sub.4 alkyl orR.sub.8 and R.sub.9 together form a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.3 --,R.sub.10 is hydrogen or C.sub.1 -C.sub.4 alkyl andR.sub.11 is hydrogen or C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or phenyl substituted by halogen or by methyl, orR.sub.10 and R.sub.11 together form a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.
    Type: Grant
    Filed: April 24, 1990
    Date of Patent: November 24, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 5118709
    Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: June 2, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Erfinders J. Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
  • Patent number: 5114968
    Abstract: Novel N-acylated 2-[4-(4-fluorophenoxy)phenoxy]ethylcarmabates of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.4 alkenyl or C.sub.3 -C.sub.4 alkynyl,R.sub.2 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, --CO--R.sub.5 or --NR.sub.6 R.sub.7,R.sub.3 and R.sub.4 are each independently of the other hydrogen or methyl,R.sub.5 is C.sub.1 -C.sub.8 alkoxy or --NR.sub.8 R.sub.9,R.sub.6 is C.sub.1 -C.sub.4 alkyl,R.sub.7 is C.sub.1 -C.sub.4 alkyl orR.sub.6 and R.sub.7 together are a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.3 --,R.sub.8 is hydrogen or C.sub.1 -C.sub.4 alkyl, andR.sub.9 is hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, phenyl or phenyl which is substituted by halogen or methyl, orR.sub.8 and R.sub.9 together are a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.3 --.
    Type: Grant
    Filed: April 18, 1990
    Date of Patent: May 19, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 5017604
    Abstract: The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: May 21, 1991
    Assignee: Warner-Lambert Company
    Inventors: Thomas R. Belliotti, Catherine R. Kostlan
  • Patent number: 4981865
    Abstract: The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective inhibitors of cyclooxygenase and 5-lipoxygenase.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: January 1, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Thomas R. Belliotti, Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, James B. Kramer, Jagadish C. Sircar
  • Patent number: 4971994
    Abstract: Novel N-phenyl-N-carbonylthioureas of the formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.10 alkyl, phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl or phenyl-C.sub.1 -C.sub.7 alkyl each of which is monohalogenated or polyhalogenated or interrupted once or more than once by oxygen and/or sulfur; C.sub.3 -C.sub.8 cycloalkyl; C hd 3-C.sub.8 cycloalkyl which is monosubstituted or polysubstituted by halogen or C.sub.1 -C.sub.5 alkyl; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 is C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, phenyl, phenyl-C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.8 cycloalkyl; C.sub.1 14 C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl each of which is monohalogenated or polyhalogenated or interrupted once or more than once by oxygen and/or sulfur; C.sub.3 -C.sub.8 cycloalkyl; phenyl or C.sub.3 -C.sub.8 cycloalkyl each of which is monosubstituted or polysubstituted by halogen or C.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: November 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Jozef Drabek, Manfred Boger, Josef Ehrenfreund
  • Patent number: 4945111
    Abstract: Fungicidal N,N'-diacylaminals of the formula ##STR1## in which R.sup.1 is optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or cycloalkenyl,R.sup.2 and R.sup.3 are hydrogen or various organic radicals, andX is oxygen or sulphur.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: July 31, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Winfried Lunkenheimer, Dieter Berg, Wilhelm Brandes
  • Patent number: 4939170
    Abstract: Fungicidal substituted aminophenyl carbamates of the formula ##STR1## in which X represents --CO--NR.sup.8 R.sup.9 ; --CO--OR.sup.9 ; --CO--SR.sup.9 ; --CO.sup.R.sup.10 ; --SO.sub.2 R.sup.9 or hydrogen, in whichR.sup.8 represents hydrogen or alkyl,R.sup.9 represents optionally substituted aryl, optionally substituted aralkyl, optionally substituted alkyl, alkenyl, halogenoalkenyl, or in each case optionally substituted cycloalkyl, cycloalkenyl or cycloalkylalkyl, andR.sup.10 has the meaning of R.sup.9 or represents an optionally substituted heterocyclic ring,Y.sup.1 to Y.sup.4 are identical or different and represent hydrogen, halogen, nitro, cyano, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, alkylsulfonyl or halogenoalkythio,R.sup.1 to R.sup.7 are identical or different and represent hydrogen, alkyl, halogenoalkyl or alkoxyalkyl,n represents 0 or 1, andZ represents alkyl, halogenoalkyl or a ##STR2## radical, in which R.sup.11 to R.sup.
    Type: Grant
    Filed: May 20, 1988
    Date of Patent: July 3, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Klaus Sasse, Peter Heitkamper, Klaus Konig, Wilhelm Brandes, Gerd Hanssler, Albrecht Marhold
  • Patent number: 4908383
    Abstract: Novel N-phenyl-N-carboxythioureas of the formula I ##STR1## in which R.sub.1 and R.sub.2 each represents C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.3 represents hydrogen, halogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 alkylthio,R.sub.4 represents C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl each mono- or poly-substituted by halogen or interrupted one or several times by oxygen and/or sulphur; C.sub.3 -C.sub.8 cycloalkyl; or C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by halogen or by C.sub.1 -C.sub.5 alkyl, andR.sub.5 represents C.sub.1 -C.sub.10 alkyl; phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl or phenyl-C.sub.1 -C.sub.7 alkyl each mono- or poly-substituted by halogen or interrupted one or several times by oxygen and/or sulphur; C.
    Type: Grant
    Filed: May 23, 1989
    Date of Patent: March 13, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Jozef Drabek, Josef Ehrenfreund
  • Patent number: 4829089
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: May 9, 1989
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4824670
    Abstract: The present invention relates to new carbazates of the general formula (I), ##STR1## wherein A is C.sub.3-10 alkyl, C.sub.3-10 alkenyl, C.sub.2-10 haloalkyl, trifluoromethyl, phenyl-C.sub.1-3 alkyl, phenyl-C.sub.2-3 -alkenyl, naphthyl-C.sub.1-3 alkyl; phenyl optionally substituted by one or more identical or different substituent(s) selected from C.sub.1-4 alkyl, halogen, C.sub.1-4 alkoxy and hydroxy; C.sub.3-7 cycloalkyl-C.sub.1-3 alkyl; optionally nitro-substituted furyl; diphenyl-hydroxy-methyl or indazolyl optionally substituted by one or more C.sub.1-4 alkoxy group(s) andR represents C.sub.1-4 alkyl,with the proviso that if R stands for ethyl, A is other than tertiary butyl, and acid addition salts thereof, a process for the preparation thereof and feed-additives comprising the same.The compounds of the general formula (I) may be used in animal husbandry due to their weight-gain increasing and fodder utilization improving effect.
    Type: Grant
    Filed: December 11, 1985
    Date of Patent: April 25, 1989
    Assignee: Egis Gyogyszergyar
    Inventors: Ildiko Ratz nee Simonek, Pal Benko, Edit Bernenyi nee Poldermann, Karoly Magyar
  • Patent number: 4748160
    Abstract: There are described compounds of formula I,ZCHRCON(--N.dbd.CR.sub.4 R.sub.5)CHR.sub.6 (CH.sub.2).sub.n COY Iwhere the substituents are defined in the disclosure.There are also described methods for making the compounds, formulations containing them and their use, e.g. as antihypertensives.
    Type: Grant
    Filed: November 14, 1985
    Date of Patent: May 31, 1988
    Assignee: Fisons plc
    Inventors: Colin Bennion, David P. Marriott, Anthony R. Cook, David H. Robinson
  • Patent number: 4735959
    Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
    Type: Grant
    Filed: May 14, 1985
    Date of Patent: April 5, 1988
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
  • Patent number: 4717736
    Abstract: Compounds having the formula: ##STR1##are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory agents and cytoprotective agents.
    Type: Grant
    Filed: November 21, 1984
    Date of Patent: January 5, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joshua Rokach, Robert N. Young
  • Patent number: 4698365
    Abstract: Compounds of the formula ##STR1## in which "halogen" represents chlorine or fluorine and n is zero, one, two or three, that have useful pesticidal activity.
    Type: Grant
    Filed: November 25, 1986
    Date of Patent: October 6, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Martin Anderson
  • Patent number: 4666939
    Abstract: A stabilized febantel formulation comprising febantel, a water-miscible organic diluent and an acid, base or buffer salt in an amount such that when diluted 1:10 with water the formulation has a pH value of about 3 to 5. The formulation is far more stable than in the absence of the acid, base or buffer salt.
    Type: Grant
    Filed: March 20, 1985
    Date of Patent: May 19, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Voege, Hubert Rast
  • Patent number: 4649148
    Abstract: The invention is insecticidal diaminoguanidine hydrazone compounds which are also effective antifeeding agents for insects and methods for their preparation.
    Type: Grant
    Filed: October 17, 1985
    Date of Patent: March 10, 1987
    Assignee: American Cyanamid Company
    Inventors: Roger W. Addor, Donald P. Wright, Jr., Jack K. Siddens, John J. Hand
  • Patent number: 4647583
    Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, and particularly against strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.
    Type: Grant
    Filed: April 15, 1983
    Date of Patent: March 3, 1987
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Ishiguri, Shigeo Yamamoto, Katsuzo Kamoshita