The Benzene Ring Is Attached To Nitrogen Through An Acyclic Carbon Or Carbon Chain Patents (Class 514/487)
  • Publication number: 20010056106
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Application
    Filed: March 9, 2001
    Publication date: December 27, 2001
    Inventors: Robert H. Chen, Min A. Xiang
  • Patent number: 6316496
    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: November 13, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
  • 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
  • Patent number: 6191157
    Abstract: The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: February 20, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Ulrich Müller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grützmann, Martin Beuck
  • Patent number: 6187821
    Abstract: A benzene compound of the formula: wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient.
    Type: Grant
    Filed: May 12, 1999
    Date of Patent: February 13, 2001
    Assignee: Welfide Corporation
    Inventors: Tetsuro Fujita, Kunitomo Adachi, Toshiyuki Kohara, Masatoshi Kiuchi, Kenji Chiba, Koji Teshima, Tadashi Mishina
  • Patent number: 6143788
    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: November 7, 2000
    Assignee: G.D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. Decrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Belekudru Devadas, Srinivasan RAJ Nagarajan, David L. Brown, Joseph J. McDonald
  • Patent number: 6114325
    Abstract: A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2)n-NR.sup.2 R.sup.3, wherein when A is R.sup.1, B is --(CH.sub.2)n-NR.sup.2 R.sup.3 and when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, B is R.sup.1 ; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.1 is a hydrocarbon group of C.sub.10-30 ; R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, or together represent a heterocyclic ring having 3-7 members; when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.5 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: September 5, 2000
    Assignee: Shiseido Co., Ltd.
    Inventors: Hirotada Fukunishi, Kenichi Umishio, Masahiro Tajima, Koji Kobayashi
  • 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: 6057363
    Abstract: New active compound combinations of valinamide derivatives of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 has the meaning given in the description,with known fungicidal active substances, and their use for combating phytopathogenic fungi are described.
    Type: Grant
    Filed: July 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Wilhelm Dehne, Wilhelm Brandes, Karl-Heinz Kuck, Thomas Seitz
  • Patent number: 6004565
    Abstract: The methods and compositions of the invention and the compounds used in the invention involve a novel immunosuppression mechanism, accelerated lymphocyte homing immunosuppression (ALH-immunosuppression). For example, the compound FTY720 specifically directs lymphocytes to the peripheral lymph nodes, mesenteric lymph nodes, and Peyer's patches. By reversibly sequestering lymphocytes in these tissues, the compounds can inhibit an immune response in a mammal. Understanding these mechanisms provides a novel immunosuppression therapy that can synergistically interact with other immunosuppressive compounds. Screening methods for identifying similar ALH-immunosuppression compounds are also described. The invention allows better treatments and therapies wherever an immunosuppression regimen is desired.
    Type: Grant
    Filed: September 23, 1997
    Date of Patent: December 21, 1999
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Kenji Chiba, Kunitomo Adachi
  • Patent number: 5948820
    Abstract: A benzene compound of the formula ##STR1## wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient.The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Beh.cedilla.
    Type: Grant
    Filed: February 20, 1997
    Date of Patent: September 7, 1999
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tetsuro Fujita, Kunitomo Adachi, Toshiyuki Kohara, Masatoshi Kiuchi, Kenji Chiba, Koji Teshima, Tadashi Mishina
  • Patent number: 5856354
    Abstract: The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: January 5, 1999
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
  • Patent number: 5854283
    Abstract: The optically pure forms of monoocarbamates of halogenated 2-phenyl-1,2-ethanediol and dicarbamates of 2-phenly-1,2-ethaniediol have been found to be effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: December 29, 1998
    Assignee: Yukong Limited
    Inventors: Yong Moon Choi, Min Woo Kim, Jeonghan Park
  • Patent number: 5821260
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 13, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5811456
    Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.
    Type: Grant
    Filed: August 6, 1996
    Date of Patent: September 22, 1998
    Assignees: Laboratoires Mayoly Spindler, Michel Seman
    Inventors: Michel Seman, Suzanne Bernard, Rene Milcent, Catherine Paillat
  • Patent number: 5807884
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: October 4, 1994
    Date of Patent: September 15, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5807891
    Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: September 15, 1998
    Assignee: Novartis AG
    Inventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
  • Patent number: 5792787
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 11, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Margaret K. Offermann
  • Patent number: 5783596
    Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 21, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
  • Patent number: 5773231
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 30, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • 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: 5773209
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 30, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5762963
    Abstract: Methods and compositions are provided for the oral delivery of temporally increasing concentrations of capsaicin, its derivatives, and analogs (collectively, "capsaicinoids"), to provide oral or pharyngeal analgesia while minimizing sensations of nausea and burning associated with the oral administration of capsaicinoids. The methods and compositions described herein soothe and relieve oral or pharynx pain. In one embodiment, one or more capsaicinoids are dispersed within a lollipop, with successively decreasing concentrations of capsaicin from the center out to the periphery, and administered to a patient in need of amelioration of oral pain. Alternatively, the capsaicinoid can be dispersed, with decreasing concentrations from the center to the periphery, in a tablet, caplet, lozenge, troche, pill, candy, or similar formulation.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 9, 1998
    Assignee: Emory University
    Inventor: Michael G. Byas-Smith
  • Patent number: 5763474
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 and R.sub.5 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, fluoroalkyl, alkoxy, perfluoroalkoxy, fluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen, with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen; or a pharmaceutically acceptable salt thereof, relaxes smooth muscles.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: June 9, 1998
    Assignee: American Home Products Corporation
    Inventors: David R. Herbst, Madelene M. Antane, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
  • Patent number: 5750351
    Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 12, 1998
    Assignee: Emory University
    Inventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
  • Patent number: 5744481
    Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: April 28, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5728729
    Abstract: 3-Methoxy-2-phenyl-acrylic esters of the formula ##STR1## in which R represents optionally substituted alkyl, cycloalkyl or aryl andn represents a number 0 or 1,a process for their preparation and their use as pesticides.
    Type: Grant
    Filed: November 13, 1995
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Peter Gerdes, Heinz-Wilhelm Dehne
  • 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: 5684018
    Abstract: This invention relates to novel acyloxyisopropyl carbamates as bioreversible prodrug moieties for amino drugs and to methods of synthesizng these compounds.
    Type: Grant
    Filed: December 13, 1994
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventor: Jose Alexander
  • Patent number: 5663200
    Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.
    Type: Grant
    Filed: October 19, 1995
    Date of Patent: September 2, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
  • 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: 5602175
    Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: February 11, 1997
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Kathryn L. Reed
  • Patent number: 5574029
    Abstract: The present invention provides a method for treating anxiety in a human in need thereof, comprising administering an antianxiety amount of a muscarinic agonist compound of the general formula ##STR1## wherein X R.sup.43, R.sup.44, R.sup.45 and R.sup.46 are defined in the disclosure.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: November 12, 1996
    Assignee: Eli Lilly and Company
    Inventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
  • Patent number: 5523325
    Abstract: This invention relates to amidrazones, insecticidal amidrazone compositions, and methods of using such compositions.
    Type: Grant
    Filed: September 9, 1993
    Date of Patent: June 4, 1996
    Inventor: Richard M. Jacobson
  • Patent number: 5510378
    Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: April 23, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Kathryn L. Reed
  • Patent number: 5482972
    Abstract: There are described new amino acid amides of the formula (I) ##STR1## in which n, R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X.sup.1, X .sup.2 and X.sup.3 having the meaning given in the description, and a process for their preparation.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: January 9, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Heinz-Wilhelm Dehne
  • Patent number: 5416117
    Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: February 28, 1994
    Date of Patent: May 16, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5364850
    Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: November 15, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
  • Patent number: 5360783
    Abstract: A water-based pesticidal composition contains 100 weight parts of substantially water-insoluble pesticide and 1.7-200 weight parts of a surface active agent. The surface active agent contains Component A and Component B at weight ratio of A/B=80/20-20/80. Component A is polyalkylene glycol ether derivative of polyethylene polyamine shown by the following general formula and having molecular weight of 20,000-100,000: ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, alkyl group with 1-4 carbon atoms, alkanoyl group with 2-18 carbon atoms, alkenoyl group with 2-18 carbon atoms and polyoxyalkylene glycol group containing oxyethyne unit and oxypropylene unit at weight ratio of (oxyethyne unit/oxypropylene unit=)100/0-50/50, at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 being the polyoxyalkylene glycol group, and n is an integer 2-250.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: November 1, 1994
    Assignee: Takemoto Yushi Kabushiki Kaisha
    Inventors: Shinichi Itoh, Kenji Kuno, Akio Hoshino
  • 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: 5331006
    Abstract: Novel unnatural dipeptoids useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. The compounds are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, and opioids. The compounds are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: July 19, 1994
    Assignee: Warner-Lambert Company
    Inventors: David C. Horwell, Julian Aranda, Corinne Augelli-Szafran, Hans-Jurgen Betche, Ann Holmes, Michael D. Mullican, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, Bruce D. Roth, Bradley D. Tait, Bharat K. Trivedi, Uwe Trostmann, Paul C. Unangst
  • Patent number: 5328909
    Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: July 12, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5272175
    Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: December 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
  • Patent number: 5217994
    Abstract: Compounds of the general formula ##STR1## and the pharmaceutically acceptable salts thereof whereinn is an integer of from 0 to 6;Y is CH.sub.2, O, SO.sub.2, --CONH--, --NHCO--, or ##STR2## R.sup.1 and R.sup.2 are independently hydrogen,C.sub.1-8 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,amino C.sub.1-4 alkyl,C.sub.1-4 alkylamino C.sub.1-4 alkyl, orC.sub.3-8 cycloalkylwherein R.sup.1 and R.sup.2 may be unsubstituted or substituted with one or more groups chosen from R.sup.3, whereR.sup.3 ishydrogen,C.sub.1-6 alkyl,hydroxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,C.sub.1-4 alkyloxy C.sub.0-4 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,halogen, orCF.sub.3 ;R.sup.4 isC.sub.1-6 alkyl,heterocyclyl C.sub.0-4 alkyl, oraryl C.sub.0-4 alkyl;R.sup.5 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-3 alkyl, orC.sub.1-6 alkylcarbonyloxymethylare used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: June 8, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Melissa S. Egbertson, Robert J. Gould, George D. Hartman
  • 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: 5180420
    Abstract: The water dispersible granule of the present invention contains (a) a pesticidal active ingredient which is solid at room temperature, (b) an anionic surface active agent, and (c) a kaolin series clay having a volume median diameter of 2 .mu.m or more, and it exhibits a good disintegrability-in-water and a high dispersion stability.
    Type: Grant
    Filed: March 11, 1991
    Date of Patent: January 19, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yasuyuki Katayama, Yasuhiko Ishimoto, Fumio Horide, Shigenori Tsuda, Fumio Nishioka
  • Patent number: 5173506
    Abstract: Novel N-(mercaptoalkyl)urea or carbamates of the formulae I and II ##STR1## wherein A is a monocyclic or bicyclic arylene or heteroarylene;Q is hydrogen or R.sub.9 CO--;Y is --O--, --S-- or --NR.sub.8 --;R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 and R.sub.8 are independently hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sub.3 is --OR.sub.5 or --NR.sub.5 R.sub.6 ;R.sub.4 is --(CH.sub.2).sub.q R.sub.7 ; or R.sub.2 and R.sub.4 and the carbons to which they are attached complete a 5-, 6- or 7-membered carbocyclic ring;R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;R.sub.
    Type: Grant
    Filed: August 16, 1990
    Date of Patent: December 22, 1992
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Alan Bronnenkant
  • Patent number: 5149709
    Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.
    Type: Grant
    Filed: July 3, 1990
    Date of Patent: September 22, 1992
    Assignee: Schering Corporation
    Inventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro
  • Patent number: 5141956
    Abstract: Ethyl 2-[4-(3-chlorophenoxy)phenoxy]ethylcarbamate is suitable controlling phytophagous cicadas in rice crops and fruit pests such as leaf rollers, citrus fruit pests such as scale insects, and vegetable and cotton pests such as white flies and noctuids.
    Type: Grant
    Filed: June 19, 1990
    Date of Patent: August 25, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 5112859
    Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## NR.sup.5,--O-- or --S--; where R.sup.3, R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl of gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.
    Type: Grant
    Filed: September 14, 1990
    Date of Patent: May 12, 1992
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Richard E. Mewshaw, Donald P. Strike