Sulfamides (i.e., N-(o=)s(=o)-n) Patents (Class 514/600)
  • Publication number: 20080051330
    Abstract: Novel compositions and methods of treating and preventing a viral infection are provided. A method of blocking a viral infection facilitated by a serine proteolytic (SP) activity is disclosed, which involves administering to a subject suffering or about to suffer from a viral infection a therapeutically effective amount of a substance having serine protease inhibitory activity or serpin activity. Among the substances found to be useful are ?1-antitrypsin (AAT), peptide derivatives from the carboxy terminal end of AAT and synthetic drugs mimicking the action of such substances. The invention is particularly well suited for checking a viral infection mediated by members of herpesviridae family.
    Type: Application
    Filed: April 14, 2006
    Publication date: February 28, 2008
    Inventor: Leland Shapiro
  • Patent number: 7291620
    Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: November 6, 2007
    Assignee: Merck + Co., Inc.
    Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca, Harold G. Selnick
  • Publication number: 20070238710
    Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 11, 2007
    Applicant: ARDEA BIOSCIENCES
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
  • Publication number: 20070191451
    Abstract: The present invention is a methods for neuroprotection, for treating an acute neurodegenerative disorder, for treating a chronic neurodegenerative disorder and/or for preventing neuron death or damage following brain, head and/or spinal cord trauma or injury comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-heteroaryl sulfamide derivatives of formula (I) as herein defined.
    Type: Application
    Filed: February 12, 2007
    Publication date: August 16, 2007
    Inventor: Virginia L. Smith-Swintosky
  • Publication number: 20070191452
    Abstract: The present invention is a method for the treatment of pain comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-heteroaryl sulfamide derivatives of formula (I) as herein defined. The present invention is further directed to methods for the treatment of pain comprising co-therapy with analgesic agent(s) and a compound of formula (I) as described herein.
    Type: Application
    Filed: February 12, 2007
    Publication date: August 16, 2007
    Inventor: Virginia L. Smith-Swintosky
  • Publication number: 20070191450
    Abstract: The present invention is a method for the treatment of mania and/or bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-heteroaryl sulfamide derivatives of formula (I) as herein defined.
    Type: Application
    Filed: February 12, 2007
    Publication date: August 16, 2007
    Inventor: Virginia L. Smith-Swintosky
  • Publication number: 20070191449
    Abstract: The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-heteroaryl sulfamide derivatives of formula (I) as herein defined. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one antidepressant.
    Type: Application
    Filed: February 12, 2007
    Publication date: August 16, 2007
    Inventor: Virginia L. Smith-Swintosky
  • Publication number: 20070191453
    Abstract: The present invention is a method for the treatment of substance abuse and/or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-heteroaryl sulfamide derivatives of formula (I) as herein defined.
    Type: Application
    Filed: February 12, 2007
    Publication date: August 16, 2007
    Inventor: Virginia L. Smith-Swintosky
  • Patent number: 7199158
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 18, 2005
    Date of Patent: April 3, 2007
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 7192940
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: March 20, 2007
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Patent number: 7105569
    Abstract: New active compound combinations of valinamide derivatives of the formula (I) in which R1 and R2 has the meaning given in the description, with known fungicidal active substances, and their use for combating phytopathogenic fungi are described.
    Type: Grant
    Filed: May 6, 2002
    Date of Patent: September 12, 2006
    Assignee: Bayer Aktiengesellsachft
    Inventors: Heinz-Wilhelm Dehne, Wilhelm Brandes, Karl-Heinz Kuck, Thomas Seitz
  • Patent number: 7022701
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: April 20, 2004
    Date of Patent: April 4, 2006
    Assignee: Wyeth
    Inventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
  • Patent number: 6951886
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: October 4, 2005
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 6939867
    Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with ?-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseases
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: September 6, 2005
    Assignee: Pfizer Inc.
    Inventors: Robert L. Dow, Ernest S. Paight
  • Patent number: 6908947
    Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: June 21, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
  • Patent number: 6906099
    Abstract: The present invention relates to the use of a composition that increases central nervous system GABA levels in a mammal, for the treatment of addiction to drugs of abuse and modification of behavior associated with addiction to drugs of abuse in said mammal.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: June 14, 2005
    Assignee: Brookhaven Science Associates, LLC
    Inventors: Stephen L. Dewey, Jonathan D. Brodie, Charles R. Ashby, Jr.
  • Patent number: 6852738
    Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: February 8, 2005
    Assignee: Merck & Co., Inc.
    Inventors: A. Brian Jones, John J. Acton, III
  • Patent number: 6776994
    Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: August 17, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Brandes, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Krüger
  • Publication number: 20040106583
    Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1
    Type: Application
    Filed: October 27, 2003
    Publication date: June 3, 2004
    Applicant: Aventis Pharma Deutschland GmBH
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Publication number: 20040092489
    Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.
    Type: Application
    Filed: October 27, 2003
    Publication date: May 13, 2004
    Applicant: Aventis Pharma Deutschland GmBH
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Publication number: 20040044047
    Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: July 22, 2002
    Publication date: March 4, 2004
    Applicant: G.D. Searle & Co.
    Inventors: Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
  • Publication number: 20040014758
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: July 3, 2003
    Publication date: January 22, 2004
    Inventors: Dean A. Wacker, John V. Duncia, Joseph B. Santella, Daniel S. Gardner
  • Patent number: 6653347
    Abstract: This invention relates to the novel use of diphenyl sulfamido in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: August 30, 2002
    Date of Patent: November 25, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
  • Patent number: 6620829
    Abstract: The invention relates to a method of treating non inflammatory cartilage damage by administering a GABA analog of Formula: and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: September 16, 2003
    Assignee: Warner-Lambert Company
    Inventors: Denis Schrier, Howard Glenn Welgus, David Juergen Wustrow
  • Publication number: 20030166717
    Abstract: Disclosed are compounds of formula X, 1
    Type: Application
    Filed: May 31, 2002
    Publication date: September 4, 2003
    Inventors: John Freskos, David L. Brown, Yvette M. Fobian, Larry Fang, Arthur Glenn Romero, Varghese John
  • Publication number: 20030158236
    Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: 1
    Type: Application
    Filed: June 25, 2002
    Publication date: August 21, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Publication number: 20030144342
    Abstract: &agr;-and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: May 6, 2002
    Publication date: July 31, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 6596771
    Abstract: A series of imidodisulfamide derivatives have been prepared and are useful to treat antiviral infections, especially infections caused by orthopox viruses.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: July 22, 2003
    Assignee: Schering Corporation
    Inventor: Vassil S. Georgiev
  • Publication number: 20030134898
    Abstract: The present invention provides a method of inhibiting sebum production and treating sebaceous gland disorders comprising administering to a patient in need of said treatment an effective amount of a compound that inhibits both acyl-Coenzyme A:cholesteryl acyltransferase (ACAT), and acyl-Coenzyme A:fatty alcohol acyltransferase (AFAT), provided that the compound is not [(2,4,6-triisopropyl-phenyl)-acetyl]-sulfamic acid 2,6-diisopropyl-phenyl ester or a pharmaceutically acceptable salt or solvate thereof. The method of the invention is useful to treat sebaceous gland disorders caused or exacerbated by the overproduction of sebum, including oily skin, acne, seborrhea, perioral dermatitis, rosacea, and corticosteroid-induced acneiform lesions.
    Type: Application
    Filed: July 31, 2002
    Publication date: July 17, 2003
    Inventor: Reynold Homan
  • Publication number: 20030119876
    Abstract: The invention relates to new diphenylurea having the formula (I) 1
    Type: Application
    Filed: February 26, 2002
    Publication date: June 26, 2003
    Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jurgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
  • Patent number: 6583172
    Abstract: Anticonvulsant derivatives useful in treating chronic neurodegenerative conditions are disclosed.
    Type: Grant
    Filed: March 30, 2000
    Date of Patent: June 24, 2003
    Inventor: Richard P. Shank
  • Patent number: 6576632
    Abstract: The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R1, R2, R3, R4, R5, R10, R11, b, m, n, p and v are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and methods of treating hyperproliferative disorders in mammals by administering the above compounds.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: June 10, 2003
    Assignee: Pfizer Inc
    Inventors: Steven W. Goldstein, Kelly P. Longo, James F. Blake, Mohamed M. A. Awad, Kenneth P. Raiche, Kevin W. Kramer
  • Patent number: 6545053
    Abstract: Compounds having a &bgr;-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4′, or nitro; R6 represents hydrogen or lower alkyl; and X represents methylene, R9 represents hydrogen, one of R7 and R8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.
    Type: Grant
    Filed: November 16, 2000
    Date of Patent: April 8, 2003
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Shiro Miyoshi, Kohei Ogawa
  • Patent number: 6538159
    Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkenyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alk
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: March 25, 2003
    Assignee: Syngenta Participations AG
    Inventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
  • Patent number: 6538016
    Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4al
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: March 25, 2003
    Assignee: Syngenta Participations AG
    Inventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
  • Patent number: 6525099
    Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: February 25, 2003
    Assignee: Eli Lilly and Company
    Inventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Patent number: 6515024
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: February 4, 2003
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 6509353
    Abstract: Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: January 21, 2003
    Assignee: Sepracor Inc.
    Inventor: Paul D. Rubin
  • Publication number: 20020193443
    Abstract: A series of imidodisulfamide derivatives have been prepared and are useful to treat antiviral infections, especially infections caused by orthopox viruses.
    Type: Application
    Filed: July 1, 2002
    Publication date: December 19, 2002
    Inventor: Vassil S. Georgiev
  • Patent number: 6495358
    Abstract: Compounds of the general formula I are provided: and pharmaceutically acceptable salts thereof, wherein, Z is a chemical species or Ri capable of binding at a primary specificity site of a protease; Y is a chemical species reactive to a specific class of protease; each of R2, R3, R5 and R7 is independently selected from the group consisting hydrogen, alkyls, aryls, substituted aryls, alkylaryls and arylalkyls; R4 and R6 are independently selected from the group consisting of: (a) H, alkyl, aryl, arylalkyl, alkylaryl, substituted derivatives thereof, and Ri; (b) —C(O)OH and derivatives thereof, said derivatives selected from the group consisting of —C(O)OQ, —C(O)NRYRZ, —C(O)[NHCHRi(q)C(O)]qOQ, and —C(O)[NHCHRi(q)C(O)]qNRYRZ; and (c) —CHRiNH2 and derivatives thereof, said derivatives selected from the group consisting of —CHRiNHW, —CHRiNHC(O)OQ, —CHRiNHC(O)R, —CHRiNHC(O)NRYRZ, —CHRiNHC(O)[NHCHRi(q
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: December 17, 2002
    Assignee: Wichita State University
    Inventor: William C. Groutas
  • Publication number: 20020183315
    Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), 1
    Type: Application
    Filed: May 23, 2002
    Publication date: December 5, 2002
    Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
  • Patent number: 6482859
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are ea
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: November 19, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Martin Zeller, André Jeanguenat
  • Patent number: 6440963
    Abstract: The treatment of neuromuscular dysfunction of the lower urinary tract by compounds which selectively inhibit the COX-2 isozyme is described. The compounds concerned inhibit the COX-2 isozyme with a potency at least 10-fold, and preferably at least 100-fold, greater than their potency on the COX-1 isozyme.
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: August 27, 2002
    Assignee: Recordati S.A., Chemical and Pharmaceutical Company
    Inventors: Amedeo Leonardi, Rodolfo Testa, Luciano Guarneri
  • Patent number: 6433016
    Abstract: A series of substituted sulfonamide derivatives have been prepared and may be used to treat antiviral infections, especially infections caused by orthopoxviruses.
    Type: Grant
    Filed: July 2, 2001
    Date of Patent: August 13, 2002
    Inventor: Vassil Stefanov Georgiev
  • Patent number: 6391918
    Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-p
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: May 21, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: André Jeanguenat, Martin Zeller
  • Patent number: 6369073
    Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.
    Type: Grant
    Filed: October 2, 2000
    Date of Patent: April 9, 2002
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini
  • Patent number: 6369032
    Abstract: Use of cathepsin S inhibitors for the treatment of an allergic condition, in particular an atopic allergic condition, more specifically for the treatment of hay fever, asthma, atopic dermatitis or a food allergy.
    Type: Grant
    Filed: September 5, 2001
    Date of Patent: April 9, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Yin Gu, Lars Karlsson, Siquan Sun, Robin L. Thurmond
  • Patent number: 6340709
    Abstract: This invention provides a method for treating and preventing neurological disorder such as Alzheimer's disease, and for promoting wound healing comprising administering a compound characterized as being a matrix metalloproteinase inhibitor.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: January 22, 2002
    Assignee: Warner-Lambert Company
    Inventors: Thomas Michael Andrew Bocan, Peter Alan Boxer, Joseph Thomas Peterson, Jr., Denis Schrier, Andrew David White
  • Patent number: 6277849
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: August 21, 2001
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Martin Zeller
  • Publication number: 20010006964
    Abstract: New active compound combinations of valinamide derivatives of the formula (I) 1
    Type: Application
    Filed: February 5, 2001
    Publication date: July 5, 2001
    Inventors: Heinz-Wilhelm Dehne, Wilhelm Brandes, Karl-Heinz Kuck, Thomas Seitz