Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/32)
  • Patent number: 6605632
    Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: August 12, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Frédérique Klupsch, Gérald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6583161
    Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: June 24, 2003
    Assignee: Tularik Inc.
    Inventor: Julio C. Medina
  • Patent number: 6525040
    Abstract: The invention is directed to novel cyclic organoselenium compounds useful as antioxidants, pharmaceutical compositions containing them, and methods for their preparation.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: February 25, 2003
    Assignee: Oxis Isle of Man, Limited
    Inventors: Irene Erdelmeier, Catherine Tailhan-Lomont, Marc Moutet, Jean Chaudiere, Jean-Claude Yadan
  • Patent number: 6492405
    Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound is a) a compound containing one or more sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; b) a 5-membered ring heterocyclic compound containing a sulfur atom and a nitrogen atom, which ring is substituted by one or more substituents bearing a terminal —ONO2 group; c) a 5-membered ring compound containing two conjugate S-atoms, which ring is linked to one or more substituents bearing a terminal —ONO2 group; or d) a compound containing an acyclic —S—S group, linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing a terminal —ONO2 group.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: December 10, 2002
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventor: Abdullah Haj-Yehia
  • Patent number: 6472488
    Abstract: Polymerizable compositions from novel monomers that correspond to the formula: in which: Z represents H or CH3 and X represents O or S, and Y is a 5- to 8-membered heterocycle consisting of hydrogen, carbon and sulphur atoms and at least two endocyclic sulphur atoms.
    Type: Grant
    Filed: September 20, 2001
    Date of Patent: October 29, 2002
    Assignee: Essilor International Compagnie Generale D'Optique
    Inventors: Florence Caye, Michèle Sindt, Daniel Paquer, Dorothée Jury, Michel Schneider, Jean-Luc Mieloszynski
  • Patent number: 6444833
    Abstract: A class of metallocene compounds is disclosed having the general formula (I): wherein Y is a moiety of formula (II) wherein A, B and D, same or different from each other, are selected from an element of the groups 14 to 16 of the Periodic Table of the Elements (new IUPAC version), with the exclusion of nitrogen and oxygen; R1, R2, R3, R4 and R5 are hydrogen or hydrocarbon groups, Z is selected from a moiety of formula (II) as described above and from a moiety of formula (III): wherein R6, R7, R8 and R9, are hydrogen or hydrocarbon groups; L is a divalent bridging group; M is an atom of a transition metal selected from those belonging to group 3, 4, 5, 6 or to the lanthanide or actinide groups in the Periodic Table of the Elements (new IUPAC version), X, same or different, is hydrogen, a halogen, a R10, OR10, OSO2CF3, OCOR10, SR10, NR102 or PR102 group, wherein the substituents R10 are hydrogen or alkyl groups; p is an integer of from 0 to 3, being equal to
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: September 3, 2002
    Assignee: Basell Technology Company BV
    Inventors: John A. Ewen, Michael J. Elder, Robert L. Jones
  • Patent number: 6433188
    Abstract: Glucokinase activating amides as herein disclosed are useful for increasing insulin secretion in the treatment of type II diabetes.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: August 13, 2002
    Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
  • Patent number: 6391901
    Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: May 21, 2002
    Assignee: Eli Lilly and Company
    Inventors: Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Alan D Palkowitz, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
  • Patent number: 6380235
    Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitut
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: April 30, 2002
    Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.
    Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 6369098
    Abstract: The present invention describes methods for synthesizing novel dithiolane derivatives, ligands with high affinity for the nuclear hormone receptors, peroxisome proliferator-activated receptor-&ggr; (PPAR&ggr;) and/or PPAR&agr;. Methods for using these compounds in the treatment of endocrine, skin, cardiovascular, immunological, neurological, neuropsychiatric, neoplastic and chronic viral diseases of various organs, including the eye are described. Methods of treating proliferative and inflammatory diseases, degenerative diseases, and age-related dysregulations, caused by an hereditary (genetic) condition or an environmental insult are also provided.
    Type: Grant
    Filed: October 4, 2000
    Date of Patent: April 9, 2002
    Assignee: Bethesda Pharmaceuticals, Inc.
    Inventors: Harrihar A. Pershadsingh, Mitchell A. Avery
  • Publication number: 20020001774
    Abstract: A hemicyanine dye having formula (1) and an optical recording medium using the hemicyanine dye as an optical recording medium are provided: 1
    Type: Application
    Filed: April 3, 2001
    Publication date: January 3, 2002
    Inventors: Jong-tae Je, Kyu-youn Lee, Young-jae Huh
  • Patent number: 6323214
    Abstract: The present invention relates to compounds of formulas (IA), (IB), and (IC): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.
    Type: Grant
    Filed: September 17, 1998
    Date of Patent: November 27, 2001
    Assignee: Medco Research, Inc
    Inventor: Pier Giovanni Baraldi
  • Patent number: 6307062
    Abstract: The novel monomers correspond to the formula: in which: Z represents H or CH3 and X represents O or S, and Y is a 5- to 8-membered heterocycle consisting of hydrogen, carbon and sulphur atoms and at least two endocyclic sulphur atoms.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: October 23, 2001
    Assignee: Essilor International Compagnie Generale d'Optique
    Inventors: Florence Caye, Michèle Sindt, Daniel Paquer, Dorothée Jury, Michel Schneider, Jean-Luc Mieloszynski
  • Patent number: 6245828
    Abstract: The present invention is directed to polymerizable dental compositions containing a) 3 to 80 wt. % of cycloaliphatic epoxides; b) 0 to 80 wt. % of an epoxide or a mixture of epoxides which are different from a); c) 3 to 85 wt. % of a filer material; d) 0.01 to 25 wt. % of initiators, inhibitors and/or accelerators; e) 0 to 25 wt. % of auxiliary agents, the individual percentages of which are in relation to the total weight. The new polymerizable agents are particularly suited as dental material.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: June 12, 2001
    Assignee: ESPE Dental AG
    Inventors: Wolfgang Weinmann, Oswald Gasser, Rainer Guggenberger, Gunther Lechner, Wolfgang Soglowek, Joachim Zech
  • Patent number: 6028069
    Abstract: Cyclic sulphones of formula (I) are disclosed, in which: R.sup.1 and R.sup.2 each independently of one another stand for H, A, CF.sub.3, CH.sub.2 F, CHF.sub.2, C.sub.2 F.sub.5, Hal, OH, OA, NH.sub.2, NHA, NA.sub.2, NO.sub.2 or CN; X stands for CR.sup.4 R.sup.5, C.dbd.Z, O, S, NH, NA or NR.sup.3 ; Y stands for CR.sup.6 R.sup.7, C.dbd.Z, O, NH, NA, or NR.sup.3 ; Z stands for O, S, NH, NA, NOH, NOA, CH.sub.2, CHA or CA.sub.2 ; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently of one another stand for H, A, R.sup.3, Hal, OH, OA, SH, SA, NH.sub.2, NHA or NA.sub.2, or alternatively, R.sup.5 and R.sup.6 or R.sup.7 and R.sup.8 can together represent a bond, only one such bond being present in each molecule; R.sup.4 and R.sup.5 together can also stand for O--(CH.sub.2).sub.2 --O or O--(CH.sub.2).sub.3 --O; R.sup.8 and R.sup.9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R.sup.
    Type: Grant
    Filed: March 30, 1999
    Date of Patent: February 22, 2000
    Assignee: Merck Patent Gesellschaft mit berschranker Haftung
    Inventors: Manfred Baumgarth, Rolf Gericke, Klaus-Otto Minck, Norbert Beier
  • Patent number: 6015808
    Abstract: Pharmaceutical compositions with heretofore unknown and enhanced physical, chemical, and biological properties are prepared by combining known biologically active parent compounds with oxo thia azabicyclo compounds, such as lactam and .beta.-lactam compounds, capable of rapidly transporting the parent compounds in undegraded form to their target sites of action. A process for combining the parent compound with .beta.-lactam compounds consists of dissolving the parent compound in a polar solvent, adding a .beta.-lactam compound, incubating the resulting mixture, followed by drying, and subjecting the remaining solid material to solvent washing or extraction to further purify the new pharmaceutical composition. The new pharmaceutical composition possesses the biological and therapeutic activity of the parent compound and the barrier penetrating characteristics of the .beta.
    Type: Grant
    Filed: August 22, 1995
    Date of Patent: January 18, 2000
    Inventors: Mandayam Jeersannidhi Thirumalachar, Mandayam Jeersannidhi Narasimhan, Jr.
  • Patent number: 5998408
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5972950
    Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: October 26, 1999
    Assignee: Laboratories UPSA
    Inventors: Eric Nicolai, Jean-Marie Teulon
  • Patent number: 5955491
    Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: September 21, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
  • Patent number: 5856503
    Abstract: Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: January 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Hans-Peter Marki, Hans Lengsfeld, Olivier Morand, Gerard Schmid, Yu-Hua Ji
  • Patent number: 5728696
    Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 17, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5718845
    Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: February 17, 1998
    Assignee: Enichem S.p.A.
    Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
  • Patent number: 5716624
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5709867
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--, and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: January 20, 1998
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5646147
    Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: July 8, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5637262
    Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, of the following graphic formula: ##STR1## wherein R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen or preferably a carboalkoxy group and R.sub.3 is hydrogen or preferably an alkyl group, provided that either R.sub.1 or R.sub.2 is hydrogen, and B and B' are the aryl groups phenyl or naphthyl, a heterocyclic aromatic group or together form a spiro adamantylene group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(oxazine) type compounds, are also described.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: June 10, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Barry Van Gemert, Anil Kumar
  • Patent number: 5591848
    Abstract: New intramolecular charge-transfer organic dyes are described. The design of these molecules is based on the phenomenon of spiroconjugation, and it provides a modular approach to the preparation of unique materials with interesting optical properties. In the dyes of the invention, the lowest unoccupied molecular orbital (LUMO) of the acceptor part (based on indandione) is spiroconjugated with the highest unoccupied molecular orbital (HOMO) of the donor part (amines, alcohols and thiols). The interaction between the donor and acceptor is controlled by the energy and symmetry of the frontier orbitals. The novel dyes described herein, with predictable and tunable optical properties, can be used in many optical applications including nonlinear optics (NLO).
    Type: Grant
    Filed: October 7, 1994
    Date of Patent: January 7, 1997
    Assignee: The Penn State Research Foundation
    Inventor: Przemyslaw B. Maslak
  • Patent number: 5514799
    Abstract: Nonlinear optical compounds having structures with delocalized resonance configurations corresponding to: ##STR1## wherein A.sub.1 and A.sub.2 are independently selected from electron withdrawing moieties; R.sub.1 and R.sub.2 are independently selected from aromatic rings, heteroaromatic rings and fused ring systems consisting of two or three aromatic or heteroaromatic rings; n and m are integers from one to five, and D.sub.1 and D.sub.2 are independently selected from hydrogen, electron donating groups and polymer attachment groups, with the proviso that at least one of D.sub.1 and D.sub.2 is an electron donating group. Polymers blended with, cured with, or having pendant side chains of the disclosed nonlinear optical materials and exhibiting second order nonlinear optical properties are also disclosed.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: May 7, 1996
    Assignee: Enichem S.p.A.
    Inventors: Pushkara R. Varanasi, Kwan-Yue A. Jen, King Y. Wong, Robert M. Mininni
  • Patent number: 5510538
    Abstract: A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: April 23, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Marco Frigerio, Simona Sputore, Marco Santagostino
  • Patent number: 5482962
    Abstract: This invention relates to N,N'-disubstituted-N,N'-diacylhydrazines which are useful as insecticides, compositions containing those compounds and methods of their use. This invention also relates to the production of intermediates useful in the production of such compounds.The compounds of this invention may be represented by the formula ##STR1## wherein R.sup.1 is cyano or H,R.sup.2 is branched alkyl,B is aryl or substituted aryl,R.sup.a is H or a variety of substituents, andZ forms a fused 5-member heterocyclic ring.
    Type: Grant
    Filed: July 22, 1994
    Date of Patent: January 9, 1996
    Assignee: Rohm and Haas Company
    Inventor: Robert E. Hormann
  • Patent number: 5466398
    Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, of the following graphic formula: ##STR1## wherein R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen or preferably a carboalkoxy group and R.sub.3 is hydrogen or preferably an alkyl group, provided that either R.sub.1 or R.sub.2 is hydrogen, and B and B' are the aryl groups phenyl or naphthyl, a heterocyclic aromatic group or together form a spiro adamantylene group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(oxazine) type compounds, are also described.
    Type: Grant
    Filed: June 21, 1993
    Date of Patent: November 14, 1995
    Assignee: Transitions Optical, Inc.
    Inventors: Barry Van Gemert, Anil Kumar
  • Patent number: 5463088
    Abstract: A process for preparing perfluoroalkoxy(alkylthio)benzenes from perfluorochloroalkoxy(alkylthio)-benzenes by reaction with hydrogen fluoride in the gas phase and in the presence of a catalyst.
    Type: Grant
    Filed: April 26, 1994
    Date of Patent: October 31, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Norbert Lui, Albrecht Marhold, Karl-Rudolf Gassen
  • Patent number: 5399710
    Abstract: Novel labeling reagents are useful for radiolabeling proteins such as antibodies with radionuclide metals such as .sup.99m Tc, .sup.186 Re, and .sup.188 Re. The reagents are of the following formula: ##STR1## wherein: each X is independently chosen from O, S, NH, or NR.sub.2, wherein R.sub.2 is a protecting group or an electron withdrawing group;R.sub.1 represents a protecting group, wherein each R.sub.1 is a separate protecting group or the two R.sub.1 symbols are taken together to represent a single protecting group; andeach T is independently chosen from hydrogen, lower alkyl groups of from 1 to about 6 carbon atoms, electron withdrawing groups, and lower alkyl groups of from 1 to about 6 carbon atoms substituted with electron withdrawing group(s).
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: March 21, 1995
    Assignee: NeoRx Corporation
    Inventors: Sudhakar Kasina, Ananthachari Srinivasan, James Sanderson, Alan R. Fritzberg
  • Patent number: 5397791
    Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: March 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh, Wasyl Halczenko, Melissa Egbertson, Nathan Ihle
  • Patent number: 5369158
    Abstract: Described are novel reversible photochromic naphthopyran compounds substituted at the number eight carbon atom on the naphtho portion of the naphthopyran ring with, for example, a methoxy group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds are also described.
    Type: Grant
    Filed: June 2, 1993
    Date of Patent: November 29, 1994
    Assignee: Transitions Optical, Inc.
    Inventor: David B. Knowles
  • Patent number: 5356924
    Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 each independently represents a halogen atom or an alkyl, alkoxy, haloalkyl, haloalkoxy, alkoxycarbonyl, alkenoxy, cyano or nitro group; R.sub.3 and R.sub.4 each independently represents a hydrogen atom or an alkyl group; R.sub.5 represents a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonylalkyl group; X and Y each independently represents an oxygen or sulphur atom or a group N--R, in which R is a hydrogen atom or an alkyl group; n is 0-3; r is 0 or 1; m is 0-4; and A or B represents a group of the general formula: ##STR2## wherein R.sub.6 represents a hydrogen or halogen atom, or an alkyl group; and R.sub.7 represents a halogen atom or an alkyl group; the other of A and B being a hydrogen atom or as for R.sub.1 or R.sub.2, have useful pesticidal activity.
    Type: Grant
    Filed: February 22, 1993
    Date of Patent: October 18, 1994
    Assignee: Shell Research Limited
    Inventors: Martin Anderson, Antony G. Brinnand, Roger E. Woodall
  • Patent number: 5312913
    Abstract: An electrically conductive complex obtained by reacting a thia-and/or selenafulvalenyl group-containing compound as an electron donor with an electron acceptor, and having an electron donar/electron acceptor molar ratio of 1/0.1 to 1/10, the thia-and/or selenafulvalenyl group-containing compound having the formula (I), ##STR1## wherein each of X.sub.1, X.sub.2, X.sub.3, X.sub.4, X'.sub.1, X'.sub.2, X'.sub.3 and X'.sub.4 is independently S or Se, Y is an electron donating or electron accepting group having a size which is not so large as to prevent molecular overlapping, m is an integer of 0 to 4, each of Z.sub.1, Z.sub.2, Z'.sub.1 and Z'.sub.2 is independently a hydrogen atom, C.sub.n H.sub.2n+1 in which n is an integer of 1 to 5, or alternatively, a combination of Z.sub.1 with Z.sub.2 or Z'.sub.2 and is C.sub.n H.sub.2n in which n is an integer of 1 to 5, or X(C.sub.n H.sub.2n).sub.n' X in which X is S or Se and n' is an integer of 1 to 3, and each of R.sub.1, R.sub.2, R.sub.3, R'.sub.1, R'.sub.2 and R'.sub.
    Type: Grant
    Filed: September 29, 1992
    Date of Patent: May 17, 1994
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Makoto Mizutani, Kazushige Kawabata, Keiji Tanaka
  • Patent number: 5288749
    Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: February 22, 1994
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
  • Patent number: 5274072
    Abstract: Provided are certain novel substituted 2(5H)furanone compounds which are useful as ultraviolet/visible light absorbing compounds. Also provided are polyester compositions having such compounds copolymerized therein and shaped or formed articles comprised of such polyester compositions.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: December 28, 1993
    Assignee: Eastman Kodak Company
    Inventors: Max A. Weaver, James J. Krutak, Clarence A. Coates, Jr., William W. Parham, Wayne P. Pruett, Samuel D. Hilbert
  • Patent number: 5268386
    Abstract: A novel heterocyclic compound capable of lowering the uric acid levels in plasma and urine having the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl, phenyl or substituted phenyl, or R.sup.1 and R.sup.2 may form a four- to eight-membered carbon ring together with the carbon atom to which they are attached; R.sup.3 is hydrogen or lower alkyl; R.sup.4 is one or two radicals selected from a group consisting of hydrogen, halogen, nitro, lower alkyl, phenyl, substituted phenyl, --OR.sup.5 and --SO.sub.2 NR.sup.6 R.sup.6' ; R.sup.5 is hydrogen, lower alkyl, phenyl-substituted lower alkyl, carboxymethyl or ester thereof, hydroxyethyl or ether thereof, or allyl; R.sup.6 and R.sup.6' are independently hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: July 26, 1990
    Date of Patent: December 7, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroshi Harada, Eiichi Ohsugi, Yukio Yonetani, Toshihiro Shinosaki
  • Patent number: 5175280
    Abstract: A thia- and/or selenafulvalenyl group-containing compound of the formula (I), ##STR1## wherein each of X.sub.1, X.sub.2, X.sub.3, X.sub.4, X'.sub.1, X'.sub.2, X'.sub.3 and X'.sub.4 is independently S or Se, Y is an electron donating or electron accepting group having a size which is not so large as to prevent molecular overlapping, m is an integer of 0 to 4, each of Z.sub.1, Z.sub.2, Z'.sub.1 and Z'.sub.2 is independently a hydrogen atom, C.sub.n H.sub.2n+1 in which n is an integer of 1 to 5, or alternatively, a combination of Z.sub.1 with Z.sub.2 and Z'.sub.1 with Z'.sub.2 is C.sub.n H.sub.2n in which n is an integer of 1 to 5, or X(C.sub.n H.sub.2n).sub.n', X in which X is S or Se and n' is an integer of 1 to 3, and each of R.sub.1, R.sub.2, R.sub.3, R'.sub.1, R'.sub.2 and R'.sub.3 is independently a hydrogen atom or C.sub.n H.sub.2n+1 in which n is an integer of 1 to 5. The compound has an electron donating nature and can be used to make electrically conductive complexes.
    Type: Grant
    Filed: June 17, 1991
    Date of Patent: December 29, 1992
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Makoto Mizutani, Kazushige Kawabata, Keiji Tanaka
  • Patent number: 5157182
    Abstract: A dehydrocyclization process is described for producing polynuclear organic compounds by contacting a starting organic material having at least one ring moiety comprising at least two adjacent ring carbon atoms each bonded to an independently selected monovalent radical comprising at most about eight carbon atoms provided at least one of the monovalent hydrocarbon radicals comprises more than one carbon atom with a crystalline copper aluminum borate catalyst. The preferred catalyst comprises at least one member selected from the group consisting of (a) crystalline copper aluminum borate and (b) zero valent copper on a support comprising at least one member selected from the group consisting of Al.sub.4 B.sub.2 O.sub.9 and the crystalline copper aluminum borate, the zero valent copper on the support being formed by the reduction of the crystalline copper aluminum borate.
    Type: Grant
    Filed: June 19, 1991
    Date of Patent: October 20, 1992
    Assignee: Amoco Corporation
    Inventors: Patrick E. McMahon, Larry C. Satek
  • Patent number: 5116874
    Abstract: This invention provides certain N-[(phenyl)amino]carbonyl-bicyclicsulfonamide sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: May 26, 1992
    Assignee: Eli Lilly and Company
    Inventor: Gerald A. Poore
  • Patent number: 4996142
    Abstract: The invention relates to an adduct of a basic macromoleculer and biotin having the general formula: ##STR1## in which MM is the residue of a basic macromolecule formed by substituting the H-atom of one or more primary amino groups;alk represents an optionally substituted alkylene group having from 1 to 10 C-atoms;m is 0 or 1; andn is a positive integer,with the proviso that, where MM represents cytochrome C or histone, m is not 0.The adduct is useful in constructing non-radioactive nucleic acid hydridization probes.
    Type: Grant
    Filed: September 4, 1987
    Date of Patent: February 26, 1991
    Assignee: Agricultural Genetics Company Limited
    Inventors: Ali H. Al-Hakim, Roger Hull
  • Patent number: 4978476
    Abstract: This invention provides novel side chain polymers which exhibit nonlinear optical response, and which have utility as a transparent optical component in all-optical and electrooptical light switch and light modulator devices.
    Type: Grant
    Filed: April 2, 1990
    Date of Patent: December 18, 1990
    Assignee: Hoechst Celanese Corp.
    Inventors: Diane E. Allen, Ronald N. DeMartino
  • Patent number: 4975451
    Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; and Ar.sup.1 is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 2-methyl[1-1'-biphenyl]-3-yl, or 6-phenoxy-2-pyridyl, exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively nontoxic to fish.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: December 4, 1990
    Assignee: FMC Corporation
    Inventors: Thomas G. Cullen, Scott McN. Sieburth, Gary A. Meier, John F. Engel, Leslie W. Stratton, Alan W. Fritz
  • Patent number: 4965264
    Abstract: A thienocinnoline compound of the general formula ##STR1## wherein R stands for hydrogen, a halogen or a lower alkyl, Ar stands for an aryl, a heteroaryl, or an aryl or a heteroaryl having as a substituent at least a halogen, a lower alkyl, a lower alkoxy, nitro, amino, hydroxy, trifluoromethyl and/or a lower alkanoylamino; and the bond between 5a-position and 6-position represents a single bond or a double bond, which is useful as an antianxiety agent, amnesia-treating drug, a brain function-activating drug, an antidementiac drug or a potentiating agent of biological protection.
    Type: Grant
    Filed: November 18, 1988
    Date of Patent: October 23, 1990
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Toru Nakao, Kenji Morita, Masao Hisadome, Shuzo Takehara
  • Patent number: 4960886
    Abstract: A charge transfer complex formed between a benzoquinone derivative represented by formula ##STR1## wherein at least one of the rings A and B represents a heterocyclic ring as defined in the specification, and an electron donor, and a salt of an anion or anion radical of the benzoquinone derivative of the above formula are disclosed. The charge transfer complex and the salt are useful as electronic materials.
    Type: Grant
    Filed: December 11, 1987
    Date of Patent: October 2, 1990
    Assignees: Fuji Xerox Co., Ltd., Toshio Mukai
    Inventors: Toshio Mukai, Yoshiro Yamashita, Takanori Suzuki
  • Patent number: 4945178
    Abstract: Acetoacetic esters of the formula R--OOCCH.sub.2 COCH.sub.3 are reacted with an unsaturated ester of the formula R.sup.1 R.sup.2 C.dbd.CHCOOR.sup.3 in the presence of basic catalyst such as ethanolic sodium ethoxide to give compound I of the formula ##STR1## and the alcohol by-product HOR.sup.3. By known hydrolysis and decarboxylation procedures, compound I is convertible to compound II of the formula ##STR2## In the above formulas, R is alkyl, R.sup.1 and R.sup.2 are each selected independently from H, alkyl, alkylthioalkyl, cycloalkyl, alkyl substituted cycloalkyl, aryl, substituted aryl, heterocyclic, or substituted heterocyclic, and R.sup.3 is alkyl or cycloalkyl. These compounds I and II are intermediates in the preparation of known herbicides.
    Type: Grant
    Filed: February 24, 1989
    Date of Patent: July 31, 1990
    Assignee: Eastman Kodak Company
    Inventor: Charles A. McCombs
  • Patent number: 4913721
    Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: April 3, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey