Additional Ring Containing Patents (Class 546/337)
  • Patent number: 6277849
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: August 21, 2001
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Martin Zeller
  • Patent number: 6268384
    Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compounds and the compositions and methods that utilize them can be used, either alone or in conjunction with a neurotrophic factor, such as nerve growth factor, to promote repair of neuronal damage caused by disease or physical trauma.
    Type: Grant
    Filed: May 27, 1998
    Date of Patent: July 31, 2001
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Perry M. Novak, Michael Mullican
  • Patent number: 6268379
    Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-2 heteroatoms selected from N, 0, and S, which are useful as metalloprotease inhibitors.
    Type: Grant
    Filed: May 13, 1999
    Date of Patent: July 31, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Chu-Biao Xue, Carl P. Decicco, Ruth R. Wexler
  • Patent number: 6262104
    Abstract: Compounds, or solvates or salts thereof, of formula (I): selective delta opioid agonists and antagonists and may be of therapeutic utility as analgesics, immunosuppressants to prevent rejection in organ transplant and skin graft, anti-allergic and anti-inflammatory agents, brain cell protectants, agents for treating drug and alcohol abuse, gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness, epilepsy and, in general, agents for the treatment of those pathological conditions which, customarily, can be treated with agonists and antagonists of the delta opioid receptor.
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: July 17, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Giulio Dondio, Silvano Ronzoni
  • Patent number: 6251917
    Abstract: Compounds of the formula where R1, R2, R3, X and n are as defined in the description, are inhibitors of cysteine protease.
    Type: Grant
    Filed: May 26, 1999
    Date of Patent: June 26, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber
  • Patent number: 6221888
    Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: April 24, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Malcolm Maccoss, Sander G. Mills, Richard A. Mumford
  • Patent number: 6172064
    Abstract: A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5 and R6 are as described in the specification, or a pharmaceutically acceptable salt, solvate, biohydrolyzable ester, biohydrolyzable amide, affinity reagent, or prodrug thereof. Also described are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine.
    Type: Grant
    Filed: August 25, 1999
    Date of Patent: January 9, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: Robert Carl Andrews, Marc Werner Andersen, David John Cowan, David Norman Deaton, Scott Howard Dickerson, David Harold Drewry, Michael David Gaul, Michael Joseph Luzzio, Brian Edward Marron, Michael Howard Rabinowitz
  • Patent number: 6172057
    Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: January 9, 2001
    Assignee: American Cyanamid Company
    Inventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
  • Patent number: 6166052
    Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: December 26, 2000
    Assignee: Warner-Lambert Company
    Inventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
  • Patent number: 6166051
    Abstract: Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
    Type: Grant
    Filed: June 23, 1998
    Date of Patent: December 26, 2000
    Assignee: Zambon Group S.p.A.
    Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
  • Patent number: 6143789
    Abstract: Compound of formula (I): ##STR1## wherein: T represents alkylene,A and B together form a naphthalene, dihydronaphthalene, or tetrahydronaphthalene group,R represents hydrogen, hydroxy, R' or OR', R' being as defined in the description,G.sub.1 represents halogen, a radical R.sub.1 or a group --O--CO--R.sub.1, R.sub.1 being as defined in the description,G.sub.2 represents a group selected from: ##STR2## X, R.sub.2 and R.sub.21 being as defined in the description, and medicinal products containing the same which are useful in the treatment of a condition related to the melatoninergic system.
    Type: Grant
    Filed: November 25, 1998
    Date of Patent: November 7, 2000
    Assignee: Adir et Compagnie
    Inventors: Fran.cedilla.ois Lefoulon, Luc Demuynck, Daniel Lesieur, Patrick Depreux, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6140353
    Abstract: N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: ##STR1## in which E, g.sup.1, g.sup.2, Q, R and X.sup.1 to X.sup.4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.
    Type: Grant
    Filed: December 2, 1998
    Date of Patent: October 31, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Katrin Grobke, Yu-Hua Ji, Sabine Wallbaum, Lutz Weber
  • Patent number: 6133442
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: October 17, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 6127372
    Abstract: This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: ##STR1## This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
    Type: Grant
    Filed: April 1, 1996
    Date of Patent: October 3, 2000
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Mark Andrew Murcko, Perry Michael Novak, Govinda Rao Bhisetti
  • Patent number: 6127545
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: September 18, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Pye, Kai Rossen, Ashok Maliakal, Ralph P. Volante, Jess Sager, Jean-Francois Marcoux, Ian Davies, Edward G. Corley, Daniel Richard Sidler, Robert D. Larsen
  • Patent number: 6124332
    Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: September 26, 2000
    Assignee: British Biotech Pharmaceuticals Ltd.
    Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
  • Patent number: 6124333
    Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: September 26, 2000
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
  • Patent number: 6100263
    Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;and their salts, processes and intermediates for their preparation, and their use are described.
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: August 8, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 6063930
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 2, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J Dinsmore, Neville J. Anthony, Gerald E. Stokker, Robert P. Gomez
  • Patent number: 6063816
    Abstract: A compound selected from those of formula (I): ##STR1## wherein: R.sub.1 represents optionally substituted alkyl, acyl, cycloalkyl, aryl, aminocarbonylalkyl, or heterocycle,R.sub.2 represents alkylene,R.sub.3 represents X or Y as defined in the description,R.sub.4 represents--either alkyl, cycloalkyl, aryl, arylalkyl, cycloalkylalkyl, heterocycloalkylene, or heterocycle when R.sub.3 represents Y,or biaryl, arylheteroaryl or heteroarylaryl, when R.sub.3 represents X or Y,their isomers and also pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as metalloprotease inhibitors in the treatment of cancers.
    Type: Grant
    Filed: August 9, 1999
    Date of Patent: May 16, 2000
    Assignee: Adir et Compagnie
    Inventors: Stephen Hanessian, Ghanem Atassi, Gordon Tucker, Daniel-Henri Caignard, Pierre Renard
  • Patent number: 6060476
    Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: March 2, 1994
    Date of Patent: May 9, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
  • Patent number: 6040450
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: September 15, 1998
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Michel Journet, Linda Gerena, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Patent number: 6013836
    Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: January 11, 2000
    Assignee: Rohm and Haas Company
    Inventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
  • Patent number: 6010980
    Abstract: Substituted 2-phenylpyridines I and their salts ##STR1## where n=0, 1;R.sup.1 =halogen, C.sub.1 -C.sub.4 -haloalkyl;R.sup.2 and R.sup.3 =H, halogen;R.sup.4 =CN, halogen;R.sup.5 =--CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--OR.sup.6, --CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--N(R.sup.7)R.sup.8, --O-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--OR.sup.6, --O-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--N(R.sup.7) R.sup.8, --S-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--OR.sup.6 or --S-(C.sub.1 -C.sub.4 -alkylene)-CO--O-(C.sub.1 -C.sub.4 -alkylene)-CO--N(R.sup.7)R.sup.8 ;R.sup.6 =H, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.3 -C.sub.4 -alkynyl;R.sup.7 =H, C.sub.1 -C.sub.4 -alkyl, carboxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.4 -alkyl;R.sup.8 =H or C.sub.1 -C.sub.4 -alkyl,are used as herbicides and for the desiccation/defoliation of plants.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: January 4, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Schafer, Gerhard Hamprecht, Elisabeth Heistracher, Olaf Menke, Cyrill Zagar, Michael Rack, Norbert Gotz, Albrecht Harreus, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz
  • Patent number: 5994507
    Abstract: A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold --CO--NH--C(.dbd.C--)--CO--, and conjugates that are capable of binding albumin and exhibiting the scaffold --CO--NH--C(.dbd.C--)--CO--.
    Type: Grant
    Filed: December 31, 1997
    Date of Patent: November 30, 1999
    Assignee: Amersham Pharmacia Biotech AB
    Inventors: .ANG.ke Pilotti, Tor Regberg, Christel Ellstrom, Charlotta Lindqvist, Ann Eckersten, Lars Fagerstam
  • Patent number: 5990314
    Abstract: This invention relates to a compound of formula I ##STR1## These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.
    Type: Grant
    Filed: June 7, 1996
    Date of Patent: November 23, 1999
    Assignee: SmithKline Beecham Corporation
    Inventor: Robert A. Daines
  • Patent number: 5985886
    Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.
    Type: Grant
    Filed: June 16, 1998
    Date of Patent: November 16, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Deborah Lynne Bryan
  • Patent number: 5977074
    Abstract: This invention relates to compounds and pharmaceutical compositions, and methods for inhibiting or preventing the amyloid protein deposits in the brain which are associated with Alzheimer's disease and aged Down's syndrome patients. More particularly, it relates to the treatment of Alzheimer's disease.
    Type: Grant
    Filed: March 28, 1996
    Date of Patent: November 2, 1999
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Barbara Cordell, Daniel Schirlin, Norton P. Peet, Jeffrey N. Higaki, Viviane Van Dorsselaer, Michael R. Angelastro
  • Patent number: 5965741
    Abstract: The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R.sup.1, and R.sup.3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof, pharmaceutically acceptable salts thereof, and in vivo hydrolizable esters and amides thereof, that are useful to relieve pain. The invention also provides pharmaceutical compositions as well as synthetic and therapeutic methods relating to such compounds.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: October 12, 1999
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, Howard Tucker, John Oldfield, Peter Warner
  • Patent number: 5962682
    Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: October 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5952341
    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: September 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 5948778
    Abstract: This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.
    Type: Grant
    Filed: May 19, 1998
    Date of Patent: September 7, 1999
    Assignee: Merrel Pharmaceuticals Inc.
    Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
  • Patent number: 5945436
    Abstract: Compounds of of the formula ##STR1## wherein R is a C.sub.6 -C.sub.10 aryl group, optionally substituted with one or more halogen atoms, phenoxy, or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, or C.sub.1 -C.sub.6 haloalkyl; R.sup.1 is C.sub.3 -C.sub.6 cycloalkyl or, linear or branched, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 haloalkenyl, C.sub.2 -C.sub.8 alkoxyalkyl or C.sub.1 -C.sub.6 haloalkyl; n is 1, 2 or 3; and R.sup.2 is CN, C(O)NH.sub.2 or C(S)NH.sub.2, or the physiologically acceptable salts thereof with organic and inorganic acids. These compounds are useful as fungicides.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: August 31, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./Cie.
    Inventors: Hoi Kiong Lai, Douglas Irving Relyea, Robert Allan Davis
  • Patent number: 5912350
    Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: June 15, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5891896
    Abstract: Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): ##STR1## wherein L is preferably --OR.sup.1 ; R.sup.a is preferably optionally substituted alkyl; R.sup.1 is preferably optionally substituted indanyl; R.sup.3 is preferably hydrogen, fluorine, hydroxy or an optionally substituted straight or branched chain alkyl group; R.sup.4 and R.sup.5 are preferably independently --(CH.sub.2).sub.t Ar, where t is zero or an integer 1, 2 or 3 wherein Ar is preferably optionally substituted monocyclic or bicyclic aryl or optionally substituted monocyclic or bicyclic heteroaryl; and R.sup.6 and R.sup.7 are preferably independently hydrogen, fluorine or optionally substituted alkyl.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: April 6, 1999
    Assignee: Celltech Therapeutics Ltd.
    Inventors: Graham John Warrellow, Julien Alistair Brown
  • Patent number: 5889031
    Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.
    Type: Grant
    Filed: February 9, 1998
    Date of Patent: March 30, 1999
    Assignee: Bristol-Myers Squibb Compnay
    Inventors: Daniel J. Keavy, Michael F. Parker, Ronald J. Mattson, Graham Johnson
  • Patent number: 5874436
    Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.
    Type: Grant
    Filed: April 23, 1997
    Date of Patent: February 23, 1999
    Inventors: James P. Demers, Sigmond Johnson, Michele Ann Weidner-Wells, Ramesh M. Kanojia, Stephanie A. Fraga, Dieter Klaubert
  • Patent number: 5863950
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-viral agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: January 26, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Siegfried H. Reich, Kathleen Lewis, Michael Melnick, Mary Ann M. Fuhry, Stephen Warren Kaldor
  • Patent number: 5859033
    Abstract: A series of pyridinyl tri-substituted benzamide derivatives of general structure ##STR1## wherein the symbols R.sup.1, R.sup.2, X and n are described in detail in the specification, are useful as anticonvulsants agents.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: January 12, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: Katherine S. Takaki, Astrid Ortiz, Brett T. Watson
  • Patent number: 5849732
    Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: December 15, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
  • Patent number: 5849771
    Abstract: Compounds of formula (I), wherein Ar, R.sub.1, R.sub.2, Y and R are as defined in claim 1, are effective as traps for free radicals.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: December 15, 1998
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Abdelhamid Zeghdaoui, Jean-Pierre Finet, Beatrice Tuccio, Viviane Cerri, Paul Tordo
  • Patent number: 5847123
    Abstract: Imide compounds having a propioloyl group or pharmaceutically acceptable salts thereof which exhibit potent activities to inhibit the production of Interleukin 1-.beta. and also the production of Tumor Necrosis Factor .alpha.. These imide compounds are useful as a prophylactic or therapeutic agent for inhibiting the production of Interleukin 1-.beta. and the production of Tumor Necrosis Factor .alpha., typically for such diseases as chronic rheumatism, sepsis, ulcerative colitis, Crohn's disease and many other related diseases in which Interleukin 1-.beta. and/or Tumor Necrosis Factor .alpha. would participate.
    Type: Grant
    Filed: July 1, 1997
    Date of Patent: December 8, 1998
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Shinji Yokoyama, Noriyoshi Sueda, Hiroaki Yamada, Ryotaro Kojima, Koichi Katsuyama
  • Patent number: 5830897
    Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 3, 1998
    Assignees: G. D. Searle & Co., Monsanto Company
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5830915
    Abstract: The invention provides compounds which are useful as inhibitors of matrix metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are described in the claims, a stereoisomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester acyloxyamide, imide or derivative thereof.Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by matrix metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: November 3, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Biswanath De, Yetunde Olabisi Taiwo
  • Patent number: 5831094
    Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 3, 1998
    Assignee: Merrell Pharamceuticals Inc.
    Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
  • Patent number: 5808124
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: June 21, 1996
    Date of Patent: September 15, 1998
    Assignee: Allergan
    Inventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5808082
    Abstract: A process for the preparation of Phosphodiesterase IV inhibitors is described. The process consists of eight chemical steps involving five isolations to prepare the title compound from readily available isovanillin in 35% overall yield (Scheme 1). The process is highlighted by: a) a highly diastereoselective Michael addition of phenyllithium using (1R, 2S) cis-aminoindanol as a chiral auxiliary, b) highly crystalline intermediates providing for efficient purifications, c) crystallization of the final compound as its CSA salt for excellent enantiomeric purity.
    Type: Grant
    Filed: April 22, 1997
    Date of Patent: September 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Woo-Baeg Choi, Hywyn R. D. Churchill, Joseph E. Lynch, Paul J. Reider, Ralph P. Volante
  • Patent number: 5783522
    Abstract: Substituted 2-phenylpyridines I ##STR1## R.sup.1,R.sup.3 =H, halogen, alkyl, haloalkyl, alkoxyalkyl, alkoxy, alkoxyalkoxy, OH, haloalkoxy, alkylcarbonyloxy, haloalkylcarbonyloxy, SH, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, CHO, CN, CO.sub.2 H, alkoxycarbonyl, alkoxyalkoxycarbonyl, haloalkoxycarbonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxyalkylcarbonyl, CONH.sub.2, alkyl-aminocarbonyl, dialkylaminocarbonyl, pyrrolidinyl-carbonyl piperidylcarbonyl, morpholinylcarbonyl, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, pyrrolidinyl, piperidinyl, morpholinyl, alkylcarbonylamino, haloalkylcarbonylamino, alkylsulfonylamino;R.sup.2 =halogen, CN, NO.sub.2, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio; orR.sup.1 +R.sup.2 or R.sup.2 +R.sup.3 =trimethylene or tetramethylene chain;R.sup.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: July 21, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Schaefer, Gerhard Hamprecht, Elisabeth Heistracher, Hartmann Koenig, Ralf Klintz, Peter Muenster, Harald Rang, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5770624
    Abstract: Particularly the invention relates to the compounds of formula I ##STR1## wherein Ar represents carbocyclic aryl, heterocyclic aryl or biaryl;R.sub.1 represents lower alkyl, cycloalkyl, aryl-lower alkyl, lower alkoxy-lower alkyl, aryl, cycloalkyl-lower alkyl, halo-lower alkyl;R.sub.2 represents hydrogen or lower alkyl;R.sub.3 and R.sub.4 represent independently hydrogen, lower alkyl, lower alkoxy, halo, hydroxy, acyloxy, lower alkoxy-lower alkoxy, trifluoromethyl or cyano; or R.sub.3 and R.sub.4 together represent lower allylenedioxy;n represents an integer from 1 to 5;pharmaceutically acceptable prodrug derivatives; and pharmaceutically acceptable salts thereof; methods for preparation thereof;pharmaceutical compositions comprising said compounds; and a method of inhibiting TNF-alpha activity and matrix-degrading metalloproteinases in mammals using such compounds.
    Type: Grant
    Filed: December 10, 1996
    Date of Patent: June 23, 1998
    Assignee: Novartis Corp.
    Inventor: David Thomas Parker
  • Patent number: H1992
    Abstract: The present invention relates to compounds of formula I: wherein Ar is an aryl group or a heteroaryl group; X is —NH—OH or —OH; R1 is H, —CH(R3)(R4), —C(O)R3, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, wherein R3 is H or any suitable substituent and R4 is H, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group; R2 is CH2-R5, wherein R5 is H or any suitable substituent, or wherein R5 and R4 are optionally substituted carbon atoms singly- or double-bonded to one another; and pharmaceutically acceptable prodrugs, salts, and solvates thereof. The invention further relates to methods of using these compounds, particularly as metalloproteinase inhibitors.
    Type: Grant
    Filed: August 11, 1999
    Date of Patent: September 4, 2001
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Steven L. Bender, Arlindo L. Castelhano