At 2-position Patents (Class 544/315)
  • Patent number: 6020491
    Abstract: Cyclic amine monomers and polymers and N-halamine biocidal polymer compounds are provided. Representative monomers have the structure: ##STR1## wherein R.sup.1 is selected from the group consisting of hydrogen and from C.sub.1 to C.sub.4 alkyl; R.sup.10 is a bond or parasubstituted phenyl; and R.sup.11 is cyclic amine unit of a 5- to 6-membered heterocyclic ring selected from the group consisting of: (a) 1,3,5-triazine-2,4-dione; (b) 3,4,5,6-tetrahydro(1H)pyrimidin-2-one; and (c) 2-oxazolidinone; R.sup.10 is attached to a linkage carbon of R.sup.11, wherein said linkage carbon of R.sup.11 is a carbon located on the ring of R.sup.11 and is substituted with a substituent selected from the group consisting of C.sub.1 -C.sub.4 alkyl, benzyl, and alkyl-substituted benzyl; from 0 to 2 non-linkage carbon members are a carbonyl group; and from 0 to 1 non-linkage carbon member is substituted with a moiety selected from the group consisting of C.sub.1 -C.sub.
    Type: Grant
    Filed: July 7, 1998
    Date of Patent: February 1, 2000
    Assignee: Auburn University
    Inventors: Shelby D. Wonley, Gang Sun, Wanying Sun, Tay-Yuan Chen
  • Patent number: 6013651
    Abstract: The present invention is directed to compounds of the formula ##STR1## and pharmaceutically acceptable salts and isomers thereof.
    Type: Grant
    Filed: March 4, 1998
    Date of Patent: January 11, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Thomas E. Rogers, Peter G. Ruminski
  • Patent number: 6005106
    Abstract: Naphthalene derivatives of the formula [I]: wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.
    Type: Grant
    Filed: June 14, 1996
    Date of Patent: December 21, 1999
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
  • Patent number: 5998456
    Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.
    Type: Grant
    Filed: January 16, 1998
    Date of Patent: December 7, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kozo Aoki, Kazuhiro Aikawa
  • Patent number: 5981537
    Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sup.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.
    Type: Grant
    Filed: May 9, 1996
    Date of Patent: November 9, 1999
    Assignee: Pharmacia & Upjohn Company
    Inventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Fritz Reusser, Gary J. Cleek, Irene W. Althaus
  • Patent number: 5977027
    Abstract: The present invention provides a nitrogen-containing cyclic compound represented by the formula (1): ##STR1## wherein R.sup.1 represents an alkyl group; R represents a hydrogen atom or an alkyl group; X represents an oxygen or sulfur atom or NR.sup.3 ; Q.sup.1 represents a hydrogen atom, or an alkyl, cycloalkyl, alkenyl or alkynyl group or a phenyl, naphthyl or heterocyclic group etc.; Q.sup.2 represents an alkyl, cycloalkyl or alkenyl group, or a phenyl or thienyl group etc.; A.sup.1 represents a carbon or nitrogen atom; A.sup.2 represents CR.sup.2 or NR.sup.2, or an oxygen or sulfur atom, or SO or SO.sub.2 ; A.sup.3 represents a single bond, or an oxygen or sulfur atom, or CR.sup.5 or NR.sup.5) and a herbicide comprising the same, which herbicide exhibits very high herbicidal activity at very low application rate and has selectivity against crops.
    Type: Grant
    Filed: September 4, 1998
    Date of Patent: November 2, 1999
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yasuo Kawamura, Eiichi Oya, Kaoru Itoh, deceased, Hiroshi Kita, Hisashi Nakata, Kanji Sawada, Yoshitake Tamada, Tsutomu Nawamaki, Kimihiro Ishikawa, Kenichi Shiojima, Chiaki Kawaguchi, Kunimitsu Nakahira
  • Patent number: 5972949
    Abstract: There are disclosed novel ether compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen or the like; A is a group of the general formula: ##STR2## B is a group of the general formula: ##STR3## and X is oxygen or sulfur; and harmful-organism controlling agents containing them as active ingredients.
    Type: Grant
    Filed: October 16, 1998
    Date of Patent: October 26, 1999
    Assignee: Sumito Chemical Co., Ltd.
    Inventors: Akira Shuto, Hirosi Kisida, Toru Tsuchiya, Yoji Takada, Hiroaki Fujimoto
  • Patent number: 5965576
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: October 12, 1999
    Assignee: Zeneca Limited
    Inventors: Ashokkumar Bhikkappa Shenvi, Robert Toms Jacobs, Scott Carson Miller, Cyrus John Ohnmacht, Jr., Chris Allan Veale
  • Patent number: 5952354
    Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: September 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
  • Patent number: 5942516
    Abstract: Novel pyridines, pyrimidines, pyrazines, pyridazines and triazines, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Grant
    Filed: September 27, 1996
    Date of Patent: August 24, 1999
    Inventors: John Duncan Elliott, Deborah Lynne Bryan
  • Patent number: 5932730
    Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: August 3, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
  • Patent number: 5929075
    Abstract: The present invention provides novel compounds of formula ##STR1## the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula:--N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d), --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: July 27, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Leo Jacobus Jozef Backx, Robert Jozef Maria Hendrickx, Luc Alfons Leo Van der Eycken, Didier Robert Guy Gabriel de Chaffoy de Courcelles
  • Patent number: 5919792
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
  • Patent number: 5919930
    Abstract: Process for cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates.In a process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates under palladium catalysis in the presence of at least one water-soluble complex ligand, the reaction medium comprises an aqueous and an organic phase and the palladium is added in the form of a palladium compound soluble in the organic phase.Polycyclic aromatic compounds can thus be prepared economically and in very good yields and simultaneously very high purity, in particular without contamination by the complexing ligands.
    Type: Grant
    Filed: July 26, 1995
    Date of Patent: July 6, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Steffen Haber, Javier Manero
  • Patent number: 5919788
    Abstract: The present invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R.sup.1 and R.sup.2 are each independently hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.3 and R.sup.4 are each independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)-amino, carboxyl, C.sub.1-6 alkyloxycarbonyl and C.sub.1-6 alkylcarbonyl; Alk is C.sub.1-4 alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: July 6, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
  • Patent number: 5889006
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: March 30, 1999
    Assignee: Schering Corporation
    Inventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle
  • Patent number: 5883096
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds of formula I ##STR1## wherein one of Y and Z is N and the other is N, CH, or C-alkyl;X is --O--, --SO.sub.0-2 --, amino, substituted amino, --CO--, --CH.sub.2 --, mono or di-substituted methylene, --CS--, --CONR.sup.20 --, --NR.sup.20 --SO.sub.2 --, --NR.sup.20 CO--, --SO.sub.2 NR.sup.20 --, --CH.dbd.CH--, --C.tbd.C-- or --NHC(O)NH--;R is optionally substituted phenyl, aryl or cycloalkyl, or other substituents as defined in the specification;R.sup.1 and R.sup.21 are H, CN or optionally substituted alkyl, or other substituents as defined in the specification;R.sup.2 is optionally substituted cycloalkyl or piperidyl, or other substituents as defined in the specification; andR.sup.3, R.sup.4, R.sup.5, R.sup.20, R.sup.27 and R.sup.
    Type: Grant
    Filed: February 16, 1996
    Date of Patent: March 16, 1999
    Assignee: Schering Corporation
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Patent number: 5877312
    Abstract: This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: March 2, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Prabhakar Kondaji Jadhav, George Clautice Emmett, Michael Ernest Pierce
  • Patent number: 5866577
    Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: February 2, 1999
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
  • Patent number: 5847149
    Abstract: Thiadiazole derivatives of the formula (I)X-B-A.sup.1 -(M.sup.1 -A.sup.2 -).sub.m (M.sup.2 -A.sup.3).sub.n -R.sup.1(I )in which the symbols and indices have the following meanings:X is Cl, Br or I;B is 1,3,4-thiadiazole-2,5-diyl;A.sup.1, A.sup.2 and A.sup.3 are identical or different and are substituted or unsubstituted 1,4-phenylene, pyrazine-2,5-diyl, pyridazine-3,6-diyl, pyridine-2,5-diyl, pyrimidine-2,5-diyl, trans-1,4-cyclohexylene, 1,3,4-thiadiazole-2,5-diyl, 1,3-dioxane-2,5-diyl, 1,3-dithiane-2,5-diyl, 1,3-thiazole-2,4-diyl, 1,3-thiazole-2,5-diyl, thiophene-2,4-diyl, thiophene-2,5-diyl, piperazine-1,4-diyl, piperazine-2,5-diyl, naphthalene-2,6-diyl, bicyclo?2.2.2!octane-1,4-diyl, or 1,3-dioxaborinane-2,5-diyl;M.sup.1 and M.sup.2 are identical or different and are --CO--O--, --O--CO--, --O--CO--O--, --O--CS--O--, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or a single bond;R.sup.
    Type: Grant
    Filed: July 16, 1996
    Date of Patent: December 8, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Robert Walter Fuss, Javier Manero, Hubert Schlosser, Rainer Wingen
  • Patent number: 5840751
    Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: November 24, 1998
    Assignee: Warner-Lambert Company
    Inventors: Edmund Lee Ellsworth, Elizabeth Lunney, Bradley Dean Tait
  • Patent number: 5808068
    Abstract: There is disclosed a genus of compounds that have anti-HIV infection therapeutic activity and inhibit nuclear localization of the HIV preintegration complex.
    Type: Grant
    Filed: August 15, 1997
    Date of Patent: September 15, 1998
    Assignee: The Picower Institute for Medical Research
    Inventors: Senliang Pan, Michael Bukrinsky, Omar K. Haffar
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
  • Patent number: 5780465
    Abstract: 4-Substituted 5-polycyclylpyrimidine compounds in which the 5-substituent is polycyclic and is attached to the pyrimidine moiety through an aliphatic carbon atom, such as 5-(2,2-dimethylindan-1-yl)-4-methylthiopyrimidine, were prepared and found to possess excellent herbicidal activity. The compounds are especially useful for the control of undesirable vegetation in paddy rice.
    Type: Grant
    Filed: April 3, 1997
    Date of Patent: July 14, 1998
    Assignee: Dow AgroSciences LLC
    Inventors: Lowell D. Markley, Kim E. Arndt, Patricia G. Ray, Terry W. Balko, Erik N. K. Cressman, David G. Ouse, Johnny L. Jackson, Jacob Secor
  • Patent number: 5773451
    Abstract: Described are compounds of formula (I) in which R1,R2,R3,R4,R5,R6,R7, m,n,p, and q are as defined in the description. Such compounds are suitable for use against Helicobacter bacteria.
    Type: Grant
    Filed: December 20, 1995
    Date of Patent: June 30, 1998
    Assignee: BYK Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Bernhard Kohl
  • Patent number: 5763447
    Abstract: A method of promoting drainage of mucous secretions in the congested airways of a bedridden/immobilized patient or an intubated/mechanically-ventilated patient is disclosed. The method comprises administering to the airways of the patient a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5')tetraphosphate, an analog of UTP, or any other analog, in an amount effective to promote drainage of fluid in the congested airways, including sinuses, by hydrating mucous secretions or by stimulating ciliary beat frequency in the airways. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or eye drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.
    Type: Grant
    Filed: July 23, 1996
    Date of Patent: June 9, 1998
    Assignee: Inspire Pharmaceuticals
    Inventors: Karla M. Jacobus, H. Jeff Leighton
  • Patent number: 5763461
    Abstract: Compounds of the formula ##STR1## wherein Pyr is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two substitutents chosen from alkyl, alkoxy, hydroxy, halo, cyano, nitro, hydroxyalkyl, alkoxyalkyl, alkanoyl, fluoroalkyl or the N-oxide of any of these;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylaikyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.
    Type: Grant
    Filed: March 21, 1997
    Date of Patent: June 9, 1998
    Assignee: Sanofi
    Inventors: David J. Aldous, Thomas R. Bailey, Guy Dominic Diana, Gee-Hong Kuo, Theodore J. Nitz
  • Patent number: 5756532
    Abstract: The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: May 26, 1998
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Richard E. Mewshaw, Byron A. Bravo, Young H. Kang
  • Patent number: 5733920
    Abstract: The invention provides novel inhibitors of cyclin-dependent kinases, in particular inhibitors of the CDK/cyclin complexes such as CDK4/cyclin D1. The novel compounds are analogs of chromones. These compounds can be used for inhibiting excessive or abnormal cell proliferation. Thus, the novel compounds are useful for treating a subject with a disorder associated with excessive cell proliferation, such as cancer.
    Type: Grant
    Filed: October 31, 1995
    Date of Patent: March 31, 1998
    Assignee: Mitotix, Inc.
    Inventors: Muzammil M. Mansuri, Krishna K. Murthi, Kollol Pal
  • Patent number: 5723473
    Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: March 3, 1998
    Assignee: Zeneca Limited
    Inventor: Brian Leslie Pilkington
  • Patent number: 5723610
    Abstract: Disclosed in this invention are the phenylpyrimidine derivatives represented by the general formula I: ##STR1## the alcohols represented by the formula: ##STR2## usable as starting material for the preparation of the phenylpyrimidine derivatives, and the processes for preparing such derivatives. The phenylpyrimidine derivatives of the formula I according to the present invention have very excellent properties as a liquid crystal compound and can be utilized effectively for the production of liquid crystal elements.
    Type: Grant
    Filed: April 12, 1996
    Date of Patent: March 3, 1998
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takayuki Higashii, Masayoshi Minai, Isao Kurimoto, Shoji Toda, Takeshi Tani, Chizu Sekine, Koichi Fujisawa
  • Patent number: 5712285
    Abstract: A class of pyrrolo?2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are ligands for dopamine receptorsubtypes within the body, in particular the D.sub.4 subtype, and are accordingly of use in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia and depression.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: January 27, 1998
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Mark Peter Ridgill
  • Patent number: 5691369
    Abstract: The cyclic ureas, and the pharmaceutically-acceptable salts and esters thereof, of the present invention are useful as antiarrhythmic and antifibrillatory agents and have the following general structure: ##STR1## wherein X, Y, A, L, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are defined as in the Specification.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 25, 1997
    Assignee: The Proctor & Gamble Company
    Inventors: Stanford Salvatore Pelosi, Jr., Chia-Nien Yu
  • Patent number: 5684011
    Abstract: The invention provides novel compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their preparation: ##STR1## wherein R.sup.1 is --S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.2 ;n is selected from 0, 1 and 2;R.sup.2, R.sup.3, and R.sup.4 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted aryloxy, optionally substituted arylalkoxy, alkoxy, alkenyloxy, alkynyloxy, hydroxyalkyl, alkoxyalkyl, alkylthio, alkenylthio, alkynylthio, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkenyloxy, haloalkynyloxy, haloalkylthio, haloalkenylthio, haloalkynylthio, halogen, hydroxy, cyano, nitro, --NR.sup.5 R.sup.6, --NR.sup.7 COR.sup.8, --NR.sup.9 SO.sub.2 R.sup.10, --N(SO.sub.2 --R.sup.11)(SO.sub.2 --R.sup.12), --COR.sup.13, --CONR.sup.14 R.sup.15, --COOR.sup.16, --OCOR.sup.17, --OSO.
    Type: Grant
    Filed: May 24, 1996
    Date of Patent: November 4, 1997
    Assignee: Zeneca Limited
    Inventors: Steven Fitzjohn, Michael Peter Robinson, Michael Drysdale Turnbull
  • Patent number: 5679792
    Abstract: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are, for example, an alkyl chain,A is a mesogenic group, andM is a spacer group,are highly suitable as components of liquid-crystal mixtures.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: October 21, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Claus Escher, Gerhard Illian, Hubert Schlosser, Rainer Wingen
  • Patent number: 5670492
    Abstract: Provided are DC-89 derivatives represented by the formula: ##STR1## wherein X represents Cl or Br, R represents hydrogen or COR.sup.1, and W represents ##STR2## and pharmaceutically acceptable salts thereof. The compounds of the present invention have excellent anti-tumor activity and are useful as anti-tumor agents.
    Type: Grant
    Filed: November 28, 1995
    Date of Patent: September 23, 1997
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Nobuyoshi Amishiro, Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Akihiko Okamoto, Katsushige Gomi
  • Patent number: 5667722
    Abstract: An antiferroelectric liquid crystal compound represented by the following general formula (I): ##STR1## wherein R.sup.1 represents an alkyl group having 6 to 16 carbon atoms; R.sup.2 represents a straight chain alkyl group having 3 to 8 carbon atoms or a branched alkyl group having 4 to 10 carbon atoms; and * means an asymmetric carbon atom, and an antiferroelectric liquid crystal composition comprising at least one liquid crystal compound as defined above. The optically active compound of the present invention is highly miscible with a number of known antiferroelectric liquid crystal compounds and thus capable of providing liquid crystal materials having improved temperature properties. A liquid crystal composition containing the optically active compound of the present invention is applicable to electro-optical devices with the use of antiferroelectric liquid crystals.
    Type: Grant
    Filed: May 23, 1996
    Date of Patent: September 16, 1997
    Assignee: Takasago International Corporation
    Inventors: Yukiharu Iwaya, Mamoru Yamada, Hitoshi Kondo, Toshimitsu Hagiwara
  • Patent number: 5635509
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: June 3, 1997
    Assignee: Zeneca Limited
    Inventors: Robert T. Jacobs, Scott C. Miller, Ashokkumar B. Shenvi, Cyrus J. Ohnmacht, Jr., Chris A. Veale
  • Patent number: 5624916
    Abstract: 2-Aryl or 2-heterocyclyl-2, 2-disubstituted ethyl-1,2,4-triazoles have been shown to have fungicidal activity.
    Type: Grant
    Filed: June 12, 1995
    Date of Patent: April 29, 1997
    Assignee: Rohm and Haas Company
    Inventors: Steven H. Shaber, Luong T. Nguyen
  • Patent number: 5602129
    Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: February 11, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
  • Patent number: 5599770
    Abstract: A herbicidal composition comprising a herbicidally effective amount of a 2-benzyloxypyrimidine derivative represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are each independently H, a halogen, hydroxyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.3 -C.sub.5 alkenyloxy, C.sub.3 -C.sub.5 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, or phenyl;n is an integer of 0 to 5; andeach X which may be identical or different if n is greater than 1, is a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.7 -C.sub.9 aralkyloxy, phenyl, hydroxymethyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or nitro, andan adjuvant.
    Type: Grant
    Filed: June 21, 1995
    Date of Patent: February 4, 1997
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Yoshikazu Kubota, Hisashi Kanno, Tsutomu Sato, Masato Arahira
  • Patent number: 5596001
    Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and natiatherosclerosis agents.
    Type: Grant
    Filed: October 25, 1993
    Date of Patent: January 21, 1997
    Assignee: Pfizer Inc.
    Inventor: Ernest S. Hamanaka
  • Patent number: 5576443
    Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: November 19, 1996
    Assignee: Sterling Diagnostic Imaging, Inc.
    Inventors: Dietrich M. Fabricius, Gregory C. Weed
  • Patent number: 5576320
    Abstract: The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT.sub.3 agonist activity of formula (I): ##STR1## in which A is --CH.dbd.N-- or --N.dbd.CH--; R is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, cyano, carboxamido, trifluoromethyl, a vinyl group, a formyl group, a carboxyl group in free, salt or esterified form, hydroxyl, hydroxymethyl, mercapto, amine, mono- or di-(C.sub.1-4 alkyl)amino, aminomethyl, mono- or di(C.sub.1-4 alkyl)aminomethyl, 1-piperido, 1-pyrrolidino, 1-piperazino or 4-(C.sub.1-4 alkyl)-1-piperazino, where R may replace any one of the hydrogen atoms of the heteroaryl nucleus;R.sub.1 is hydrogen or a methyl group;R.sub.2 and R.sub.3, which are identical or different, are hydrogen or C.sub.1-4 alkyl;n is 1 or 2; m is 0 or 1; and m+n.gtoreq.2;and addition salts with inorganic or organic acids of the compounds of formula (I).
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 19, 1996
    Assignee: Sanofi
    Inventors: Marco Baroni, Umberto Guzzi, Antonina Giudice, Marco Landi, Vivian Mazza
  • Patent number: 5556859
    Abstract: N-(4-Pyrimidinyl)amide pesticides of the formulas ##STR1## and N-oxides and salts thereof, wherein the variable groups are as defined in the specification, are active against nematodes, insects, mites, and plant pathogens.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: September 17, 1996
    Assignee: DowElanco
    Inventor: Peter L. Johnson
  • Patent number: 5552409
    Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.
    Type: Grant
    Filed: March 31, 1994
    Date of Patent: September 3, 1996
    Assignee: Rohm and Haas Company
    Inventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
  • Patent number: 5552090
    Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds substituted at the 3 position of the pyran ring with (i) an aryl substituent and (ii) a phenyl substituent having a 5- or 6-member heterocyclic ring fused at the number 3 and 4 carbon atoms of the phenyl substituent, and at the 6 position of the naphthyl portion of the naphthopyran compound with a nitrogen-containing heterocyclic ring. 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(indoline) type compounds, are also described.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: September 3, 1996
    Assignee: PPG Industries, Inc.
    Inventors: Barry Van Gemert, David B. Knowles
  • Patent number: 5550236
    Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boronic acids with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium, if desired applied to a support material, as catalyst, wherein the coupling is carried out in the presence of a ligand and a base. The process of the invention allows the yield of polycyclic aromatic compounds to be significantly increased in comparison with processes not using a ligand and thus allows a yield optimum for the Pd(0)-catalyzed cross-coupling of aromatic boronic acids with aromatic halogen compounds to be achieved.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hubert Schlosser, Rainer Wingen, Javier Manero
  • Patent number: 5548078
    Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: August 20, 1996
    Assignee: Shionogi Seiyaku Kabushiki Kaisha
    Inventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
  • Patent number: 5539115
    Abstract: Disclosed in this invention are the phenylpyrimidine derivatives represented by the general formula I: ##STR1## the alcohols represented by the formula: ##STR2## usable as starting material for the preparation of the phenylpyrimidine derivatives, and the processes for preparing such derivatives. The phenylpyrimidine derivatives of the formula I according to the present invention have very excellent properties as a liquid crystal compound and can be utilized effectively for the production of liquid crystal elements.
    Type: Grant
    Filed: October 8, 1993
    Date of Patent: July 23, 1996
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takayuki Higashii, Masayoshi Minai, Isao Kurimoto, Shoji Toda, Takeshi Tani, Chizu Sekine, Koichi Fujisawa