C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/354)
At 3-position (Class 514/355)
  • Substituted pyridines useful for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6794396
    Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: September 21, 2004
    Assignee: Pharmacia Corporation
    Inventors: Len F. Lee, Kevin C. Glenn, Daniel T. Connolly, David G. Corley, Daniel L. Flynn, Ashton T. Hamme, Shridhar G. Hegde, Michele A. Melton, Roger J. Schilling, James A. Sikorski, Nancy N. Wall, Jeffery A. Zablocki
  • Activated iododerivatives for the treatment of cancer and aids
    Patent number: 6780995
    Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.
    Type: Grant
    Filed: November 25, 2002
    Date of Patent: August 24, 2004
    Assignee: Isotechnika Inc.
    Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
  • Benzoylpyridine derivative or its salt, fungicide containing it as an active ingredient, its production process and intermediate for producing it
    Patent number: 6770662
    Abstract: The present invention relates to a fungicide containing a novel benzoylpyridine derivative or its salt. The present invention provides a fungicide containing a benzoylpyridine derivative represented by the formula (I) or its salt: wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group; n is 1, 2, 3 or 4; R1 is a substitutable alkyl group; R2 is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: August 3, 2004
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Hisaya Nishide, Munekazu Ogawa, Hidemasa Kominami, Koji Higuchi, Akihiro Nishimura
  • Active substance combinations having insecticidal and acaricidal properties
    Patent number: 6762183
    Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: July 13, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
  • Methods for increasing leptin levels using nicotinic acid compounds
    Patent number: 6750234
    Abstract: The invention relates to the use of nicotinic acid and nicotinic acid esters, such as nicotinic acid alkyl esters, to increase the amount of leptin in a subject. As a result, one can treat conditions, such as conditions characterized by wounds, by administering sufficient amounts of nicotinic acid or nicotinic acid ester to increase leptin levels to alleviating amounts. Various conditions and modes of treatment are disclosed.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: June 15, 2004
    Assignees: University of Kentucky Research Foundation, Arizona Board of Regents on Behalf of University of Arizona
    Inventors: Elaine Jaccobson, Myron Jacobson, Hyuntae Kim
  • Heterocyclic dicarboxylic acid diamide derivatives, agricultural/horticultural insecticides and method of using the same
    Patent number: 6747041
    Abstract: Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Het represents a 5- or 6-membered heterocycle; X and Y represent each halocyano, nitro, optionally halogenated C3-6, cycloalkyl, optionally substituted phenyl, an optionally substituted heterocycle, etc; n is from 0 to 3; m is from 1 to 5; Z1 and Z2 represent each O or S; and B1 to B4 represent each C or N. Agricultural/horticultural insecticides having an excellent controlling effect on pest insects such as diamond-back moth (Pluntella xylostella) and tobacco cutworm (Spodoptera litura).
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: June 8, 2004
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Takeshi Katsuhira, Takashi Furuya, Makoto Gotoh, Masanori Tohnishi, Hideo Takaishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
  • Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use
    Patent number: 6743790
    Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: June 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
  • Methods of using CCR1 antagonists as immunomodulatory agents
    Publication number: 20040087571
    Abstract: The present invention relates to methods of using CCR1 antagonists as immunomodulatory agents.
    Type: Application
    Filed: October 16, 2003
    Publication date: May 6, 2004
    Applicant: Pfizer Inc
    Inventors: Matthew F. Brown, Anderson S. Gaweco, Ronald P. Gladue, John C. Kath, Christopher S. Poss
  • Compounds useful as reversible inhibitors of cathespin S
    Patent number: 6730671
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: May 4, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Inhibitors of bacterial NAD synthetase
    Patent number: 6727237
    Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: April 27, 2004
    Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanadan E. Velu
  • Abc expression promoters
    Publication number: 20040077689
    Abstract: The ABCA1 mRNA expression-promoting agent, LXR&agr; mRNA expression-promoting agent, ABCG1 mRNA expression-promoting agent, cholesterol efflux-promoting agent, cholesteryl ester accumulation-inhibiting agent, ACAT-1 mRNA expression-inhibiting agent and CEH mRNA expression-promoting agent of the present invention are excellent in the ability to control cholesterol distribution in the body and have low toxicity.
    Type: Application
    Filed: October 16, 2003
    Publication date: April 22, 2004
    Inventors: Yasuo Sugiyama, Hiromatsu Fuse, Masao Hirakata, Ryuichi Tozawa
  • Capsaicin receptor ligands
    Patent number: 6723730
    Abstract: Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: April 20, 2004
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Alan Hutchinson, Robert W. DeSimone, Kevin J. Hodgetts, James E. Krause, Geoffrey G. White
  • Methods for inhibiting diabetic complications
    Patent number: 6716858
    Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions. The instant invention also teaches new methods to treat or prevent diabetic nephropathy, oxidative stress, and protein crosslinking, comprising administering an amount effective of one of the compounds of the invention to treat or prevent the disorder.
    Type: Grant
    Filed: October 13, 1999
    Date of Patent: April 6, 2004
    Assignee: Kansas University Medical Center
    Inventors: Raja Khalifah, Billy G. Hudson
  • Devices and methods for eliminating termite colonies
    Patent number: 6716421
    Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.
    Type: Grant
    Filed: March 5, 2001
    Date of Patent: April 6, 2004
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Philip Frederick Brode, III, Garry Steven Garrett, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
  • N-acyloxylated cycloalkyl compounds, composition containing the same and methods of use therefor
    Patent number: 6713492
    Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: March 30, 2004
    Assignees: Daiichi Radioisotope Laboratories, Ltd., Yamagata Public Corporation for the Development of Industry
    Inventors: Osamu Itoh, Heitaro Obara, Hidekatsu Yokoyama, Masaaki Aoyama
  • Thiolesters and uses thereof
    Patent number: 6706729
    Abstract: This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: March 16, 2004
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James A. Turpin, Yongsheng Song, Ettore Appella, John K. Inman, David G. Covell, William G. Rice, Anders Wallqvist, Andrew Maynard, Mingjun Huang
  • Vitamin D analogues
    Patent number: 6706725
    Abstract: The invention relates to novel bicyclic compounds having the general formula (I): as well as to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, in carcinology and in the field of autoimmune diseases and that of organ or tissue transplants in particular), or alternatively in cosmetic compositions.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: March 16, 2004
    Assignee: Galderma Research & Development, S.N.C.
    Inventor: Jean-Michel Bernardon
  • Fungicidal heterocyclic aromatic amides and their compositions, methods of use and preparation
    Patent number: 6706740
    Abstract: Heterocyclic aromatic amides (HAA) according to Formula I: wherein X1-X4, M, Z, and A are herein defined. The invention also encompasses hydrates, salts and complexes thereof. These compounds are useful as antifungal agents.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: March 16, 2004
    Assignee: Dow AgroSciences LLC
    Inventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Matthew J. Henry, Jenifer L. Adamski Butz, Robert P. Gajewski
  • Antipsychotic sulfonamide-heterocycles, and methods of use thereof
    Patent number: 6703383
    Abstract: One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Sepracor, Inc.
    Inventors: Xinhe Wu, Brian M. Aquila, Liming Shao, Heike Radeke, Gregory D. Cuny, James R. Hauske, Roger L. Xie
  • Benzene derivatives and pharmaceutical use thereof
    Patent number: 6703379
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Novel pharmaceutical compositions having an antidiabetic action, and process for their preparation
    Publication number: 20040039031
    Abstract: The present invention relates to the field of therapeutic chemistry and more particularly to the preparation of novel medicinal products for treating diabetes. Specifically, a subject of the invention is novel antidiabetic medicinal products consisting of a combination of two active principles that are effective via the oral route, at subliminal doses, formed from an antidiabetic biguanide and an antidiabetic sulfonamide, in combination or as a mixture with one or more inert, pharmaceutically acceptable excipients. The invention also relates to a process for the preparation of such medicinal products formed from a biguanide and a sulfonamide.
    Type: Application
    Filed: May 21, 2003
    Publication date: February 26, 2004
    Inventors: Nathalie Cugnardey, Nicolas Wiernsperger
  • Treatment of mycobacterium tuberculosis with antisense polynucleotides
    Publication number: 20040033972
    Abstract: Methods of inhibiting the proliferation of Mycobacterium tuberculosis comprising contacting Mycobacterium tuberculosis with an effective amount of a polynucleotide complementary to an mRNA transcript expressed by Mycobacterium tuberculosis are provided. Typical methods of the invention utilize phosphorothioate modified antisense polynucleotides (PS-ODNs) against the mRNA of M.tuberculosis genes such as glutamine synthetase, aroA,ask, groES, and the genes of the Antigen 85 complex.
    Type: Application
    Filed: August 29, 2002
    Publication date: February 19, 2004
    Inventors: Marcus A. Horwitz, Gunter Harth, Paul C. Zamecnik
  • Nitrogen-containing compounds and their use as glycine transport inhibitors
    Publication number: 20040034069
    Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.
    Type: Application
    Filed: August 8, 2003
    Publication date: February 19, 2004
    Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
  • Fungicidal mixtures based on amide compounds
    Publication number: 20040029930
    Abstract: Fungicidal mixtures, comprising
    Type: Application
    Filed: June 11, 2003
    Publication date: February 12, 2004
    Inventors: Karl Eicken, Arne Ptock, Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegfried Strathmann, Maria Scherer, Klaus Schelberger, Manfred Hampel
  • Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme
    Patent number: 6689801
    Abstract: Novel thiol derivatives of formula I or of the formula Ia wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: February 10, 2004
    Assignee: Novartis AG
    Inventors: Cynthia A. Fink, Faribroz Firooznia
  • Aromatic diamide derivatives, chemicals for agricultural or horticultural use and usage thereof
    Publication number: 20040009982
    Abstract: The present invention relates to an aromatic diamide derivative represented by the general formula (I): 1
    Type: Application
    Filed: September 20, 2002
    Publication date: January 15, 2004
    Inventors: Masanori Tohnishi, Eiji Kohno, Hayami Nakao, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka
  • Electrophilic ketones for the treatment of herpesvirus infections
    Patent number: 6673784
    Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: January 6, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
  • Insecticidal anthranilamides
    Publication number: 20030229050
    Abstract: This invention provides compounds of Formula (1), their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n are as defined in the disclosure. Also disclosed are methods for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula (1) and compositions containing the compounds of Formula (1).
    Type: Application
    Filed: August 28, 2002
    Publication date: December 11, 2003
    Inventors: George P. Lahm, Brian J. Myers, Thomas P. Selby, Thomas M. Stevenson
  • Substituted diaryl or diheteroaryl methans, ethers and amines having retinoid agonist, antagonist or inverse agonist type biological activity
    Patent number: 6660755
    Abstract: Compounds of the formula Y3(R4)—X—Y1(R1R2)—Z—Y2(R2)—A—B where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 9, 2003
    Assignee: Allergan, Inc.
    Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
  • Benzoylpyridine derivative or its salt, fungicide containing it as an active ingredient, its production process and intermediate for producing it
    Publication number: 20030216444
    Abstract: The present invention relates to a fungicide containing a novel benzoylpyridine derivaitive or its salt. The present invention provides a fungicide containing a benzoylpyridine derivative represented by formula (I) or its salt: wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cyclo(alkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may he esterified or amidated, or at substitutable amino group; n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2 is a substitutable alkyl group, it substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.
    Type: Application
    Filed: December 23, 2002
    Publication date: November 20, 2003
    Inventors: Hisaya Nishide, Munekazu Ogawa, Hidemasa Kominami, Koji Higuchi, Akihiro Nishimura
  • Novel aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity
    Publication number: 20030212113
    Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity.
    Type: Application
    Filed: December 24, 2002
    Publication date: November 13, 2003
    Inventors: Natalia B. Dyatkina, Dong-Fang Shi, Christopher Don Roberts, Mark Douglas Velligan, Sebastian Johannes Reinhard Liehr, Janos Botyanszki, Wentao Zhang, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
  • Polyamine analogues as therapeutic and diagnostic agents
    Patent number: 6646149
    Abstract: Novel “bispolyamine” inhibitor compounds of polyamine transport are disclosed. These compounds are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. These compounds display desirable activities both for diagnostic and research assays and therapy.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: November 11, 2003
    Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
  • Acid derivatives useful as serine protease inhibitors
    Patent number: 6642252
    Abstract: Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(═O)NR4R5, L is a linker group, X2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: November 4, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory S. Bisacchi, James C. Sutton, William A. Slusarchyk, Uwe D. Treuner, Guohua Zhao, Daniel L. Cheney, Yan Shi, Shung C. Wu
  • Unsaturated derivatives at the 4-position of 6-tert-butyl-1,1-dimethylindane and their use in human and veterinary medicine and in cosmetics
    Patent number: 6642273
    Abstract: An unsaturated derivative at the 4-position of 6-tert-butyl-1,1-dimethylindane corresponding to the following formula: in which: X represents: a divalent radical of formula: and Y represents a divalent radical of following formula: R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue selected from the group consisting of residues deriving from glucose, galactose, mannose and glucuronic acid or an amino acid residue deriving from lysine, glycine and aspartic acid, r′ and r″, which are identical or different, represent H, low
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: November 4, 2003
    Assignee: Galderma Research & Development
    Inventors: Angel De Lera, Beatriz Dominguez
  • Method for treatment of bacterial infections with once or twice-weekly administered rifalazil
    Publication number: 20030203903
    Abstract: A method for treatment of bacterial infections with rifalazil administered once-weekly, or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections caused by Mycobacterium avium complex, infections caused by Chlamydia pneumoniae and infections caused by Helicobacter pylori by administering to a patient suffering from the bacterial infection 1-100 mg of rifalazil once or twice a week. In this dose regimen, the treatment is fast, efficacious and eliminates undesirable secondary symptoms observed with daily doses of 1-50 mg of rifalazil.
    Type: Application
    Filed: September 14, 2002
    Publication date: October 30, 2003
    Inventors: Lynn M. Rose, David J. Porubek, Alan B. Montgomery
  • Hydroxamic acid and its derivatives as inhibitors of melanocyte tyrosinase for topical skin lighteners
    Publication number: 20030199558
    Abstract: Methods, compounds, and formulations are provided to reduce pigmentation in mammalian skin, comprising hydroxamic acid and its derivatives, and especially benzohydroxamic acid and its derivatives. The compounds preferably inhibit pigment synthesis in melanocytes through inhibition of melanocyte tyrosinase. The methods can be used for lightening skin, and for treating uneven skin complexions, which result from hyperpigmentation-related medical conditions such as melasma, age spots, freckles, ochronosis, and lentigo. The compounds can be used medically or cosmetically, and preferably as topical formulations.
    Type: Application
    Filed: December 23, 2002
    Publication date: October 23, 2003
    Applicant: Integriderm, Inc.
    Inventors: Thomas P. Dooley, Lin Cheng
  • Substituted amine derivatives and methods of use
    Publication number: 20030195230
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: January 10, 2002
    Publication date: October 16, 2003
    Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
  • Picolinic acid derivatives and their use as fungicides
    Publication number: 20030191113
    Abstract: The invention concerns compounds of general formula (1) wherein: n, G, Q1, Q2, X1, X2, Y and Z are as defied in the description, the method for preparing said compounds, fungicide compositions comprising said compounds and methods for treating plants using said compounds or compositions.
    Type: Application
    Filed: July 8, 2002
    Publication date: October 9, 2003
    Inventors: Francisco Nieto-Roman, Jean-Pierre Vors, Alain Villier, Helene Lachaise, Adeline Mousques, Benoit Hartmann, Pierre Hutin, Jose Lorenzo Molina, Benoit Muller
  • Heterocyclically substituted amides, their preparation and use
    Patent number: 6630493
    Abstract: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: October 7, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Lymphocyte function antigen-1 antagonists
    Patent number: 6630492
    Abstract: Mevinolin compounds for use in the treatment or prevention of autoimmune diseases, inflammation, ischemia/reperfusion injury and graft rejection. Such compounds bind to the LFA-1 I-domain and thereby inhibit LFA-1/ICAM-1 or LFA-1/ICAM-3 interactions.
    Type: Grant
    Filed: February 24, 2000
    Date of Patent: October 7, 2003
    Assignee: Novartis AG
    Inventors: Wilfried Bauer, Sylvain Cottens, Dieter Geyl, Gabriele Weitz-Schmidt, Jörg Kallen, Ulrich Hommel
  • Admantane derivatives
    Publication number: 20030187031
    Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
    Type: Application
    Filed: December 6, 2002
    Publication date: October 2, 2003
    Inventors: Lilian Alcaraz, Mark Furber
  • Appetite suppressant for oral ingestion
    Publication number: 20030185883
    Abstract: A method of suppressing human appetite, and a material therefore, are disclosed in the claims. The method includes the step of inducing body weight loss in a human by providing that human with material containing, as an active ingredient, 2-AcetylPyridine for human oral consumption. The material can be provided in the form of a lozenge. A related aspect of the invention relates to material for human ingestion to encourage body weight loss, the material comprising about 1% 2-AcetylPyridine volume/volume.
    Type: Application
    Filed: March 28, 2002
    Publication date: October 2, 2003
    Inventor: Ronald S. Nietupski
  • Compounds for the management of aging-related and diabetic vascular complications, process for their preparation and therapeutic uses thereof
    Patent number: 6624178
    Abstract: The invention discloses novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, wherein, R1, R2, R3, X and m are as defined in the specification.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: September 23, 2003
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventor: Alangudi Sankaranarayanan
  • Use of compounds for decreasing activity of hormone-sensitive
    Publication number: 20030166690
    Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
    Type: Application
    Filed: December 13, 2002
    Publication date: September 4, 2003
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Certain thiol inhibitors of endothelin-converting enzyme
    Patent number: 6613782
    Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: September 2, 2003
    Assignee: Novartis AG
    Inventors: Stéphane De Lombaert, Cynthia Anne Fink, Fariborz Firooznia, Denton Wade Hoyer, Arco Yingcheu Jeng
  • Acylsulfonamide derivative
    Publication number: 20030162818
    Abstract: This invention provides a novel acylsulfonamide derivative which can be used as an ACC activity inhibitor effective for the treatment of visceral fat syndrome that becomes the risk-factor of diseases of adult people such as myocardial infarction, cerebral infarction and diabetes.
    Type: Application
    Filed: March 4, 2003
    Publication date: August 28, 2003
    Applicant: AJINOMOTO CO. INC.
    Inventors: Hiroshi Ikawa, Masato Nishimura, Keiji Okada, Takashi Nakamura
  • Cathecol hydrazone derivatives, process for preparing the same and pharmaceutical composition containing the same
    Patent number: 6610715
    Abstract: The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or —CH2CH2C(═O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, —C(═X)—R5, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, —NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: August 26, 2003
    Assignee: Cheil Jedang Corporation
    Inventors: Yong Sik Youn, Myung Xik Xiang, Byoung Chol Suh, Jong Hoon Kim, Kwang Hyuk Lee, Eui Kyung Kim, Jae Kyu Shin, Chung Keun Rhee
  • Inhibitors of p38
    Patent number: 6608060
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: August 19, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
  • Bisaryl compound and medicament for cancer treatment comprising the same
    Patent number: 6608061
    Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.
    Type: Grant
    Filed: February 14, 2000
    Date of Patent: August 19, 2003
    Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.
    Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi
  • Compounds for the management of aging-related and diabetic vascular complications, process for their preparation and therapeutic uses thereof
    Patent number: 6608094
    Abstract: Novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular and neurovascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, inflammatory disorders, immunological disorders, oxidative stress, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, wherein, R1, R2, R3, X and m are as defined in the specification. Also disclosed is a method for preparation of the compounds of general formula (I) and pharmaceutical composition containing one or more compounds as defined above as active ingredients. Also disclosed is a method of treatment of a diabetic patient by administering the compounds as defined above, either singly or in combination with drugs for antidiabetic therapy.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: August 19, 2003
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventor: Alangudi Sankaranarayanan