Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/96)
  • Patent number: 9657043
    Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.
    Type: Grant
    Filed: April 23, 2013
    Date of Patent: May 23, 2017
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Maiko Hamada, Kaoru Tashiro, Hiroshi Sakashita, Masatoshi Kiuchi, Shuzo Takeda, Kunitomo Adachi
  • Publication number: 20150148314
    Abstract: There are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer.
    Type: Application
    Filed: January 27, 2015
    Publication date: May 28, 2015
    Inventors: William Fenical, Paul R. Jensen, James J. La Clair, Lynnie Trzoss, Takashi Fukuda
  • Patent number: 9023402
    Abstract: Several classes of in vivo carbon monoxide-releasing compounds are useful for the treatment and/or prevention of diseases, such as chronic inflammatory, e.g., rheumatoid arthritis, and of diseases with a strong inflammatory component, such as atherosclerosis, stroke, coronary disease, and Alzheimers disease. The in vivo carbon monoxide-releasing compounds can be attached to known drug vectors and/or known anti-inflammatory drugs, such as aspirin.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: May 5, 2015
    Assignee: ALFAMA—Investigação e Desenvolvimento de Produtos Farmacêuticos, Lda.
    Inventors: Werner E. Haas, Carlos C. Romao, Beatriz Royo, Ana Cristina Fernandes, Isabel Goncalves
  • Publication number: 20150087620
    Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.
    Type: Application
    Filed: April 23, 2013
    Publication date: March 26, 2015
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Maiko Hamada, Kaoru Tashiro, Hiroshi Sakashita, Masatoshi Kiuchi, Shuzo Takeda, Kunitomo Adachi
  • Patent number: 8853424
    Abstract: The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(1) R3—[—X—B(ZR1)—Y—]n—R4,??(2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(3) R3—[—X—B(ZR1)—]n—R4,??(4) R3—[—B(ZR2)—W—]n—R4,??(5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2,??(6) R3—B(OH)2,??(7) R3—B(ZR1)—X—B(ZR2)—R4,??(8) R3—B(R1)—O—B(R2)—R4,??(9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4,??(10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4,??(11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(12) [R3—X—B(ZR1)—Y]2B(ZR2),??(13) wherein each symbol is as defined in the DESCRIPTION.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 7, 2014
    Assignee: Japan Science and Technology Agency
    Inventors: Katsuhiko Mikoshiba, Nobuyuki Nukina, Shoichiro Ozaki, Kouzo Hamada, Jun-Ichi Goto, Akinobu Suzuki, Etsuko Ebisui, Akiko Terauchi
  • Publication number: 20140100194
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 10, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
  • Patent number: 8680078
    Abstract: Disclosed herein are stable formulations suitable for the treatment of glaucoma and ocular hypertension.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: March 25, 2014
    Assignee: Medivis SRL
    Inventors: Danilo Aleo, Sergio Mangiafico, Maria Grazia Antonietta Saita
  • Patent number: 8546358
    Abstract: The present invention is directed to a method for treating or ameliorating asthma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of compound 17:
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: October 1, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence de Garavilla, Bruce E. Maryanoff
  • Patent number: 8440643
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: May 14, 2013
    Assignee: MethylGene Inc.
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou
  • Publication number: 20120184510
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: January 14, 2011
    Publication date: July 19, 2012
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews, Ning Qin, Laura Reany, Christopher Teleha, Mark A. Youngman
  • Publication number: 20120022022
    Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: September 26, 2011
    Publication date: January 26, 2012
    Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence de Garavilla, Bruce E. Maryanoff
  • Publication number: 20100317625
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.
    Type: Application
    Filed: May 21, 2007
    Publication date: December 16, 2010
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Stephane Raeppel, Michael Mannion, Nancy Z. Zhou, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou
  • Patent number: 7846915
    Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: December 7, 2010
    Assignee: Resverlogix Corporation
    Inventors: Norman C. W. Wong, Joseph E. L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
  • Publication number: 20100279983
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 21, 2007
    Publication date: November 4, 2010
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou
  • Publication number: 20090036409
    Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: August 20, 2008
    Publication date: February 5, 2009
    Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence De Garavilla, Bruce E. Maryanoff
  • Patent number: 7459444
    Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: January 18, 2005
    Date of Patent: December 2, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence de Garavilla, Bruce E. Maryanoff
  • Publication number: 20080287398
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: May 2, 2008
    Publication date: November 20, 2008
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews
  • Publication number: 20080199454
    Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.
    Type: Application
    Filed: December 21, 2007
    Publication date: August 21, 2008
    Inventors: Michael Mortimore, Julian M.C. Golec
  • Patent number: 7030103
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: April 18, 2006
    Assignee: Methylgene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6921756
    Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: July 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6884791
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: April 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Publication number: 20040082546
    Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Application
    Filed: April 8, 2003
    Publication date: April 29, 2004
    Applicant: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6706698
    Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: March 16, 2004
    Assignee: Ilex Products, Inc.
    Inventors: Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Harald Eschenhof, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
  • Publication number: 20030236232
    Abstract: A class of novel benzo(b)thiophene is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
    Type: Application
    Filed: December 3, 2002
    Publication date: December 25, 2003
    Inventors: Michael Dean Kinnick, Ho-Shen Lin, Michael John Martinelli, John Michael Morin, Michael Enrico Richett
  • Patent number: 6632807
    Abstract: This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: October 14, 2003
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
  • Publication number: 20030109500
    Abstract: Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to the highly cytotoxic dephosphorylated form.
    Type: Application
    Filed: August 14, 2002
    Publication date: June 12, 2003
    Inventors: Ronald W. Pero, David Sherris, Kevin G. Pinney, Vani P. Mocharla, Zhi Chen
  • Publication number: 20020123483
    Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as benzopyrone derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokine may for example be interleukin-8 (IL-8), and the relevant chemokine receptors may for example be corresponding chemokine receptors (CXCR-1 and/or CXCR-2). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of [7-[benzopyrone-5′(3′-amino)-thiazole]-phenylalanine-benyl ester in the treatment of disease.
    Type: Application
    Filed: March 5, 2001
    Publication date: September 5, 2002
    Inventors: Geeta Saxena, Christopher R. Tudan, Nick Cheng, Hassan Salari
  • Publication number: 20020107207
    Abstract: The present invention provides an antiproliferative compound having a structural formula 1
    Type: Application
    Filed: November 5, 2001
    Publication date: August 8, 2002
    Inventors: Bob G. Sanders, Kimberly Kline, Weiping Yu
  • Patent number: 6355672
    Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: March 12, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
  • Patent number: 6346521
    Abstract: This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.
    Type: Grant
    Filed: December 28, 1995
    Date of Patent: February 12, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
  • Patent number: 6054448
    Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: April 25, 2000
    Assignee: Eli Lilly and Company Limited
    Inventors: Barry Peter Clark, John Richard Harris
  • Patent number: 5958905
    Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.
    Type: Grant
    Filed: March 26, 1996
    Date of Patent: September 28, 1999
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Erik Joel Verner
  • Patent number: 5910492
    Abstract: This invention provides a pharmaceutical composition comprising a non-peptide osteogenic promoting substance and a biodegradable polymer, which can be safely used as a prophylactic/therapeutic agent for various bone diseases (e.g., bone fractures).
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: June 8, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tetsuo Hoshino, Hiroya Muranishi, Shigehisa Taketomi, Susumu Iwasa
  • Patent number: 5880111
    Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 9, 1999
    Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
  • Patent number: 5578601
    Abstract: Disclosed are nonpeptides having bradykinin antagonist activity of the formulae (I) and (II) ##STR1## or a pharmaceutically acceptable salt thereof therefor.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: November 26, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Peter R. Seoane, Joseph M. Salvino, Brent D. Douty, Mohamed M. A. Awad, Roland E. Dolle, David G. Sawutz, David M. Faunce, Wayne T. Houck
  • Patent number: 5565440
    Abstract: The present invention discloses a methane diphosphonate derivative, a process for producing said derivative and its pharmaceutical applications, said methane diphosphonate derivative indicated with general formula (1): ##STR1## (wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a pharmacologically acceptable cation, a hydrogen atom or a straight chain or branched alkyl group having 1-4 carbon atoms, R.sub.5 is a hydrogen atom or a trialkylsilyl group, m is an integer of 0 to 3, n is an integer of 1 to 3, R.sub.6 and R.sub.7 are independently a hydrogen atom or an alkyl group, and X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group).
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: October 15, 1996
    Assignee: Toray Industries, Inc.
    Inventors: Keijiro Takanishi, Norio Kawabe, Teruo Nakadate
  • Patent number: 5428027
    Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: June 27, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: John P. Daub, George P. Lahm, Bradford S. Marlin
  • Patent number: 5336671
    Abstract: The invention provides fungicidal compositions containing benzyl-tris(aryl)-phosphonium salts of the general formula ##STR1## in which R.sup.1 represents an optionally substituted alkyl or alkoxy group; R.sup.2 represents a hydrogen atom or an optionally substituted alkyl group; R.sup.3, R.sup.4 and R.sup.5 independently represent a hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group; and A.sup.- represents an anion processes for the preparation of such compounds. Certain of the compounds of formula I are novel and the invention therefore also provides processes for the preparation of such compounds and their use as fungicides.
    Type: Grant
    Filed: October 18, 1991
    Date of Patent: August 9, 1994
    Assignee: Shell Research Limited
    Inventors: Heinz-Manfred Becher, Guido Albert, Jurgen Curtze
  • Patent number: 5268385
    Abstract: This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D.sub.2 receptors without appreciably activating postsynaptic dopamine receptors which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting essentially of the stereoisomers of mixtures thereof of compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of pyridyl and ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3, R.sub.2 is H, R.sub.
    Type: Grant
    Filed: November 18, 1991
    Date of Patent: December 7, 1993
    Assignee: Whitby Research, Inc.
    Inventor: Alan S. Horn
  • Patent number: 5268388
    Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: December 7, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: John P. Daub, George P. Lahm, Bradford S. Marlin
  • Patent number: 5229375
    Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: July 20, 1993
    Assignee: Scripps Clinic and Research Foundation
    Inventors: Peter E. Maligres, Kyriacos C. Nicolaou
  • Patent number: 5204334
    Abstract: Benzoheterocyclylalkylaminoalkanediphosphonic acids of formula I ##STR1## wherein R.sub.1 and R.sub.2, independently of one another, are hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or lower alkyl, X and Y, independently of one another, are oxy or thio, alk.sub.1 and alk.sub.2 are identical or different lower alkylene radicals, n is 0 or 1 and m and m', independently of one another, are 0, 1 or 2, the sum of n, m and m' being 1, 2 or 3, and their salts exhibit a pronounced regulatory action on the calcium metabolism of warm-blooded animals. They are prepared, for example, as follows: in a compound of the formula ##STR2## wherein R.sub.1, R.sub.2, n, m, m', X, Y, alk.sub.1 and alk.sub.2 are as defined above, R'.sub.3 is one of the groups R.sub.3 mentioned above or is an amino-protecting group R.sub.0, Z.sub.1 is a functionally modified phosphono group, and Z.sub.2 is a free or functionally modified phosphono group, converting functionally modified phosphono Z.sub.
    Type: Grant
    Filed: September 25, 1991
    Date of Patent: April 20, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Wolfgang Frostl, Knut A. Jaeggi
  • Patent number: 5190929
    Abstract: Cyclophosphamides possessing anti-tumor activity and having the formula ##STR1## and salts thereof; wherein R is lower alkyl, aryl, aryl-lower alkyl or a nitrogen, sulfur or oxygen containing heterocyclic or heterocyclic lower alkyl, andR' is hydrogen, hydroxy or OOH with the proviso that when R' is hydrogen, R is other than methyl or phenyl and when R' is hydroxy, R is other than methyl.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: March 2, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Gregory W. Canute
  • Patent number: 5158943
    Abstract: A sulfur-containing hetrocyclic compound of the formula (I) ##STR1## wherein the ring A is an optionally substituted benzene ring, R is a hydrogen atom or an optionally substituted hydrocarbon residue, B is a carboxyl group which may be esterified or amidated, X is --CH(OH)-- or --CO--, and n is an integer of 0, 1 or 2, or its salt, which is useful in the prevention or treatment of osteoporosis.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: October 27, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Iwao Yamazaki
  • Patent number: 5145990
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.
    Type: Grant
    Filed: January 9, 1991
    Date of Patent: September 8, 1992
    Assignee: Merck & Co., Inc.
    Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett
  • Patent number: 5071841
    Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: December 10, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
  • Patent number: 5021404
    Abstract: Angiostatic compounds are potentiated by collagen matrix metabolism modulators including:a) proline analogs which inhibit proline hydroxylation when substituted for proline in collagen;b) inhibitors of proline hydroxylase;c) inhibitors of collagen cross-linking; andd) all trans-retinoic acid.In methods and therapeutic compositions for inhibiting angiogenesis in a mammal, the collagen matrix modulator is administered with an angiostatic steroid or with heparin (including angiostatic heparin fragments of six or more sugar units, and synthetic fragments).
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: June 4, 1991
    Assignee: The Children's Medical Center Corporation
    Inventors: Judah Folkman, Donald Ingber
  • Patent number: 4963536
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 -A- is a group of the formula: ##STR2## in which R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, andX is O or S, andR.sup.2 is hydrogen or lower alkyl, provided that when R.sup.1 is lower alkyl, thenR.sup.1 -A- is a group of the formula: ##STR3## in which R.sup.1 and X are each as defined above, processes for the preparation thereof and pharmaceutical composition comprising the same.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: October 16, 1990
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Teruo Oku, Eishiro Todo, Chiyoshi Kasahara, Katsuya Nakamura, Hiroshi Kayakiri, Masashi Hashimoto
  • Patent number: 4963537
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: April 26, 1989
    Date of Patent: October 16, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill