Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/43)
  • Patent number: 6339172
    Abstract: A method for analyzing an objective substance, comprsing reacting a labeled probe with an objective substance on a biological sample, said probe comprsing a label substance of the formula (I): wherein A1 is an aromatic group, R1 is a hydrogen or —COCH2COCnF2n+1 and n is an integer of 1-6, which is bonded to a probe selected from the group consisting of nucleic acid, nudeic acid binding potein, low molecular ligand and receptor for ligand (except antibody) to give a fluorescent complex, reacting the complex with an objective substance on a biolgical sample and assaying fluorescence of the resultant fluorescent complex, a labeled nucleic acid probe and a labeled nucleotide. According to the method of the present invention, defects such as hindrance of fluorescence due to contaminant substance, low sensitivity and the like can be resolved, thereby enabling analysis on a tissue.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: January 15, 2002
    Assignees: Toyo Boseki Kabushiki Kaisha
    Inventors: Kazuhiro Matsui, Katsunori Ikeda, Shinichi Teshima, Yoshihisa Kawamura, Kazuko Matsumoto
  • Patent number: 6337346
    Abstract: Compounds useful as cytotoxic agents are selected from the group consisting of compounds of Formula I and compounds of Formula II: wherein: R1, R2, R3 and R4 are each independently selected from the group consisting of: hydrogen, alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, thiophenylcarbonyl; nitro and cyano; thiophenyl and thiophenylthiophenyl, each of which may be unsubstituted or substituted with alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, nitro or cyano; subject to the proviso that at least one of R1, R2, R3 and R4 is not hydrogen; A1 and A2 are each selected from the group consisting of: ═O, alkyl, alkoxy, and alkylcarbonyloxy; and the pharmaceutically acceptable salts thereof. When A1 and A2 are ═O, the center ring has only two, and not three, double bonds.
    Type: Grant
    Filed: August 30, 2000
    Date of Patent: January 8, 2002
    Assignee: University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Sheng-Chu Kuo
  • Patent number: 6300339
    Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, T, X, Y, Z, R5, R6, R7, R8, Ar, k, m, n and p are as defined in the specification. These compounds are useful in treating or preventing conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: October 9, 2001
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6262055
    Abstract: Sulfur-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: July 17, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Steven D. Young, John S. Wai, Mark W. Embrey, Thorsten E. Fisher
  • Patent number: 6251936
    Abstract: This invention provides compounds of Formula I having the structure E is S, SO, SO2, O, or NR1c; X is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkenyl of 2-7 carbon atoms, CN, aryl, aralkyl of 6-12 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, hydroxyaralkyl of 6-12 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy; arylalkoxy, nitro, amino, NR2R2a, NR2COR2a, cycloalkylamino of 3-8 carbon atoms, morpholino, alkylsulfanyl of 1-6 carbon atoms, arylsulfanyl, pyridylsulfanyl, 2-N,N-dimethylaminoethylsulfanyl, —OCH2CO2R2b or —COR2c; Z1 and Z2 are each, independently, hydrogen, halogen, CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, cycloalkyl of 3-8 carbon atoms, nitro, amino, —NR1R1a, —NR1COR1a, cycloalkylamino of 3-8 carbon atoms, morpholino, or OR8, or Z1 and Z2 may be taken together as a diene unit having the formula —CH═CR9—CR10═CR11—; or a pharmaceutically acceptable salt th
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: June 26, 2001
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Arlene J. Dietrich, Madelene M. Antane
  • Patent number: 6211369
    Abstract: Spiro compounds of the formula (I), where X1, X2, X3, X4 are identical or different and are —S—, —O—, —NR5—, —CR5═N— or —CR5═CH—, with the proviso that at least one of the groups X1-4 is different from —CR5═CH—, are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.
    Type: Grant
    Filed: January 3, 2000
    Date of Patent: April 3, 2001
    Assignee: Aventis Research & Technologies GmbH & Co. KG
    Inventors: Josef Salbeck, Donald Lupo
  • Patent number: 6201004
    Abstract: Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the ne
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: March 13, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, Paul Anthony Bradley
  • Patent number: 6174913
    Abstract: Compounds useful as cytotoxic agents are selected from the group consisting of compounds of Formula I and compounds of Formula II: wherein: R1, R2, R3 and R4 are each independently selected from the group consisting of: hydrogen, alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, thiophenylcarbonyl; nitro and cyano; thiophenyl and thiophenylthiophenyl, each of which may be unsubstituted or substituted with alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, nitro or cyano; subject to the proviso that at least one of R1, R2, R3 and R4 is not hydrogen; A1 and A2 are each selected from the group consisting of: ═O, alkyl, alkoxy, and alkylcarbonyloxy; and the pharmaceutically acceptable salts thereof. When A1 and A2 are ═O, the center ring has only two, and not three, double bonds.
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: January 16, 2001
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Sheng-Chu Kuo
  • Patent number: 6172103
    Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.
    Type: Grant
    Filed: November 24, 1999
    Date of Patent: January 9, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Wilfried Schwab, Ruth Raiss
  • Patent number: 6166251
    Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.
    Type: Grant
    Filed: December 31, 1998
    Date of Patent: December 26, 2000
    Assignees: Kazuko Matsumoto, Suzuki Motor Corporation
    Inventors: Kazuko Matsumoto, Jingli Yuan
  • Patent number: 6121271
    Abstract: This invention provides compounds of Formula I having the structure whereinR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, R.sup.9, X, R.sup.6, p, Y, Z, R.sup.7, and R.sub.8 are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: September 19, 2000
    Assignee: American Home Products Corporation
    Inventors: Paul J. Dollings, Arlene J. Dietrich, Jay E. Wrobel
  • Patent number: 6069166
    Abstract: A compound, pharmaceutically acceptable salt thereof, or hydrate thereof having a PGD.sub.2 -antagonistic activity, and an inhibitory activity against infiltration of eosinophils, useful for treating mast cell dysfunction-associated diseases, such as systemic mastocytosis and disorder of systemic mast cell activation, as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, ischemic reperfusion injury, inflammation and atopic dermatitis, which is shown by the formula (I): ##STR1## is provided.
    Type: Grant
    Filed: May 28, 1999
    Date of Patent: May 30, 2000
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
  • Patent number: 6054474
    Abstract: Polycyclic alkaloids of formula (I), ##STR1## wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6 or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X is O, S, SO, SO.sub.2, N--R.sub.5, or C--(R.sub.5).sub.2, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH.sub.2 then R1 is not CH.sub.3, R.sub.2 and R.sub.3 are not both H, R.sub.4 is not OH, m is not 3 and n is not 0.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: April 25, 2000
    Assignee: Biochem Pharma, Inc.
    Inventors: John Dimaio, Dilip M. Dixit
  • Patent number: 6040459
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: March 21, 2000
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 6037361
    Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: March 14, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
  • Patent number: 6022307
    Abstract: The invention provides novel substituted dibenzothiophenes of Formulae (I), (II), (III) and (IV) which have antiangiogenic activity and further provides a method using substituted dibenzothiophenes of Formula (V) as antiangiogenic agents.
    Type: Grant
    Filed: June 28, 1999
    Date of Patent: February 8, 2000
    Assignee: American Cyanamid Company
    Inventors: Mark E. Salvati, Nancy H. Eudy, William A. Hallett, Dennis William Powell
  • Patent number: 6001867
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein: B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms;X is H, or halogen;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, --CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: December 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Arlene J. Dietrich, Zenan Li
  • Patent number: 5990104
    Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: November 23, 1999
    Assignee: Biochem Pharma, Inc.
    Inventors: John Dimaio, Dilip M. Dixit
  • Patent number: 5955619
    Abstract: This invention described novel compounds of formula ##STR1## wherein the general symbols are as defined in claim 1, as stabilisers for protecting organic materials, in particular polymers and lubricants, against thermal, oxidative or light-induced degradation.
    Type: Grant
    Filed: July 23, 1998
    Date of Patent: September 21, 1999
    Inventors: Peter Nesvadba, Samuel Evans, Christoph Krohnke, Jurg Zingg
  • Patent number: 5936127
    Abstract: This invention relates to chiral heterocyclic compounds useful for asymmetric synthesis and catalysis. More particularly, the invention relates to chiral heterocyclic phosphine, sulfur, and nitrogen compounds for asymmetric synthesis and catalysis in the production of enantiomerically pure products.
    Type: Grant
    Filed: January 13, 1998
    Date of Patent: August 10, 1999
    Assignee: The Penn State Research Foundation
    Inventor: Xumu Zhang
  • Patent number: 5905088
    Abstract: Novel pharmaceutically/cosmetically-active heterocyclic biaryl compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(h): ##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 cosmetic applications and for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: May 18, 1999
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventors: Philippe Diaz, Etienne Thoreau
  • Patent number: 5888432
    Abstract: The present invention has for subjects, novel benzopyran derivatives, substituted in position 2 with an adamantyl group as well as the compositions and (co)polymer matrices containing such derivatives. Said derivatives possess interesting photochromic properties.
    Type: Grant
    Filed: December 3, 1997
    Date of Patent: March 30, 1999
    Assignee: Corning Incorporated
    Inventor: You-Ping Chan
  • Patent number: 5859297
    Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: January 12, 1999
    Assignees: Kazuko Matsumoto, Suzuki Motor Corporation
    Inventors: Kazuko Matsumoto, Jingli Yuan
  • Patent number: 5849781
    Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: October 1, 1997
    Date of Patent: December 15, 1998
    Assignee: Adir Et Compagnie
    Inventors: Michel Langlois, Monique Mathe-Allainmat, Philippe Delagrange, Pierre Renard, Beatrice Guardiola
  • Patent number: 5811034
    Abstract: Described are novel 7-methylidene-5-oxo-furo fused naphthopyran compounds having certain substituents at the 2 position of the pyran ring. Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: October 23, 1997
    Date of Patent: September 22, 1998
    Assignee: PPG Industries, Inc.
    Inventor: Jibing Lin
  • Patent number: 5773631
    Abstract: The invention described novel compounds of formula ##STR1## wherein the general symbols are as defined in claim 1, as stabilisers for protecting organic materials, in particular polymers and lubricants, against thermal, oxidative or light-induced degradation.
    Type: Grant
    Filed: February 26, 1996
    Date of Patent: June 30, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Peter Nesvadba, Samuel Evans, Christoph Krohnke, Jurg Zingg
  • Patent number: 5767141
    Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: June 16, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
  • Patent number: 5763609
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.
    Type: Grant
    Filed: March 21, 1996
    Date of Patent: June 9, 1998
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5728846
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist and/or retinoid inverse-agonist-like biological activity.
    Type: Grant
    Filed: December 12, 1996
    Date of Patent: March 17, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
  • Patent number: 5726208
    Abstract: New compounds of formula: ##STR1## wherein: --A--D--E, X, n, Y and Z are as defined in the description, in racemic form and in the form of optical isomers,and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.
    Type: Grant
    Filed: October 11, 1996
    Date of Patent: March 10, 1998
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
  • Patent number: 5707557
    Abstract: Photochromic compounds with a 3H-naphthopyran structure having at least one pyrene moiety in the 3-position, a method for preparing such compounds, and the use of such compounds for producing photochromic articles from an organic synthetic material.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: January 13, 1998
    Assignee: Optische Werke G. Rodenstock
    Inventors: Manfred Melzig, Herbert Zinner
  • Patent number: 5658500
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho-portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. 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: June 14, 1995
    Date of Patent: August 19, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5656206
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. 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: June 14, 1995
    Date of Patent: August 12, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
  • Patent number: 5622546
    Abstract: The application relates to emulsion paints which are protected against fungal infestation by the use of N-alkyl-benzothiophene-2-carboxamide S,S-dioxides.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: April 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Ludwig Elbe, Wilfried Paulus, Heinrich Schrage, Martin Kugler, Franz Kunisch
  • Patent number: 5607624
    Abstract: A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the general symbols are as defined in claim 1, with a compound of formula IV[H].sub.n --R.sub.1 (IV).
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: March 4, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Nesvadba, Samuel Evans, Ralf Schmitt
  • Patent number: 5587486
    Abstract: 1-amino-2-cyclohexene compounds represented by the following formula (I): ##STR1## wherein the substituents are as defined in the specification, a process for preparing the compounds and their use as intermediates in the production of medicinal and agricultural agents is disclosed.
    Type: Grant
    Filed: June 30, 1995
    Date of Patent: December 24, 1996
    Assignee: Kuraray Co., Ltd.
    Inventors: Naoshi Nakagawa, Tadashi Hatanaka, Tatsuhiko Hayashibara, Manzo Shiono
  • Patent number: 5578252
    Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, examples of which are substituted with an oxy-bearing substituent at the number 8 carbon atom and with either an alkyl group at the number 7 carbon atom or with a carbonyl bearing substituent at the number 9 carbon atom and certain substituents at the 3-position of the pyran ring, e.g., 3,3-spirofluoren-9-ylidene 8-methoxy-9-carbomethoxy-3H-naphtho[2,1-b]pyran. 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: November 29, 1995
    Date of Patent: November 26, 1996
    Assignee: Transitions Optical, Inc.
    Inventors: Barry Van Gemert, Anil Kumar
  • Patent number: 5372734
    Abstract: Alkylated benzothiophenes or dibenzothiophenes are high-temperature stable lubricant fluids having extreme pressure and antiwear properties, additive solubility and inherent EP/antiwear properties. These novel fluids may also be used as additives in other lubricant fluids.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: December 13, 1994
    Assignee: Mobil Oil Corporation
    Inventors: Derek A. Law, Carleton N. Rowe, Leslie R. Rudnick
  • Patent number: 5334333
    Abstract: The present invention relates to electroactive compounds capable of undergoing a change in light absorption and refraction due to an applied electric field and a permanent change in refraction due to exposure to predetermined bands of optical radiation. The present invention also relates to electroactive compositions containing such electroactive compounds, electrooptical components comprised of such electroactive compositions and electrooptical devices comprised of such electrooptical components, as well as novel processes of making the same.
    Type: Grant
    Filed: December 17, 1990
    Date of Patent: August 2, 1994
    Assignee: Elf Atochem North America, Inc.
    Inventor: Frederick J. Goetz
  • Patent number: 5315014
    Abstract: The present invention involves monomeric compounds having the structure: ##STR1## Substituents W and Z are independently --CN, --NO.sub.2, --aryl, --aryl--V, --COX, SO.sub.2 R, --H, or --alkyl. Substituent X is --OR, or --NR,R where R and R.sup.1 are independently --alkyl or --H. Substituent V is --halide, --NO.sub.2, --CN, --SO.sub.2 R, or --COX. At least one of W and Z is --NO.sub.2, --SO.sub.2 R, --CN, --COX or --aryl--V. In one preferred embodiment substituents W and Z are both --CN. In another preferred embodiment, substituent X is --NO.sub.2 or --CN and substituent Z is --C.sub.6 H.sub.4 NO.sub.2. These monomers are polymerized to form low bandgap polymers.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: May 24, 1994
    Assignee: Board of Regents, The University of Texas System
    Inventors: John P. Ferraris, Tim L. Lambert, Santiago Rodriguez
  • Patent number: 5292894
    Abstract: A process for the preparation of benzo[b]thiophenes of the general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 independently denote hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, nitro, cyano, halo, C.sub.1 -C.sub.4 alkylcarbonyl, benzoyl, C.sub.1 -C.sub.4 alkylcarbonylamino, benzoylamino,N-(C.sub.1 -C.sub.4 alkyl)phenylamino, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylsulfonyl, phenylsulfonyl, aminosulfonyl, aminocarbonyl, C.sub.1 -C.sub.4 phenylalkyl and nitrobenzyl or R.sup.1 +R.sup.2 or R.sup.2 +R.sup.3 or R.sup.3 +R.sup.4 denote a butadienediyl chain optionally substituted by R.sup.1 to R.sup.4, in whicha) thiophenols of the general formula II ##STR2## in which the substituents R.sup.1 to R.sup.4 have the aforementioned meanings, are reacted with chloroacetaldehyde at a temperature ranging from 0.degree. to 150.degree. C. andb) the resulting (arylthio)acetaldehydes of the general formula III ##STR3## in which the substituents R.sup.
    Type: Grant
    Filed: February 17, 1993
    Date of Patent: March 8, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Ebel, Juergen Schroeder
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5256661
    Abstract: Certain novel compounds having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.
    Type: Grant
    Filed: September 28, 1992
    Date of Patent: October 26, 1993
    Assignee: Whitby Research, Inc.
    Inventor: Alan S. Horn
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5145954
    Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 and R.sup.2, which are the same or different, are optionally substituted alkyl; W, X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryloxyalkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted alkynyl, optionally substituted amino, optionally substituted arylazo, optionally substituted heteroarylalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted acylamino, nitro, cyano, --OR.sup.3, --SR.sup.3, --CO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --COR.sup.7, --CR.sup.8 .dbd.NR.sup.9, --N.dbd.CR.sup.10 R.sup.11, --SOR.sup.12 or --SO.sub.2 R.sup.
    Type: Grant
    Filed: April 17, 1989
    Date of Patent: September 8, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Thomas E. Wiggins, David J. Tapolczay
  • Patent number: 5084476
    Abstract: The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >CO, >CR.sup.8 OR.sup.7, --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --; R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.
    Type: Grant
    Filed: August 17, 1989
    Date of Patent: January 28, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Ekkehard Weiss
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 5068447
    Abstract: Aromatic carbonyl compounds, in particular arylene ether ketones, are prepared by reacting an appropriate reagent system in the presence of free Lewis acid and a complex between a Lewis acid, for example, aluminum trichloride, and an inorganic salt controlling agent, for example, lithium chloride, and, optionally, a diluent, such as methylene chloride. The process is particularly advantageous for the preparation of substantially or all para-linked arylene ether ketones as the presence of the Lewis acid/Lewis base complex markedly reduces alkylation and ensures the substantial absence of ortho substitution.
    Type: Grant
    Filed: July 6, 1990
    Date of Patent: November 26, 1991
    Assignee: Raychem Corporation
    Inventors: Heinrich C. Gors, Patrick J. Horner, Viktors Jansons
  • Patent number: 5066795
    Abstract: A (perfluoroalkyl)dibenzonium salt represented by the following general formula ##STR1## wherein R.sub.f represents a perfluoroalkyl group having 1 to 10 carbon atoms, A represents a sulfur of selenium atom, R.sup.1 and R.sup.2, independently from each other, represent a hydrogen atom or a nitro group, X.sup..crclbar. represents a conjugated base of Bronsted acid, and n is 0 or 1.The said compound is useful as a reagent for introducing a perfluoroalkyl group.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: November 19, 1991
    Assignee: Sagami Chemical Research Center
    Inventors: Teruo Umemoto, Sumi Ishihara
  • Patent number: RE36832
    Abstract: An N-heteroaryl-N'-phenylurea derivative represented by the general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the description of the specification which is useful as a prophylactic and therapeutic agent for hypercholesterolemia, atherosclerosis and diseases caused by them.
    Type: Grant
    Filed: June 19, 1998
    Date of Patent: August 22, 2000
    Assignee: Nihon Nohyaku Co., LTD
    Inventors: Masashi Nagamine, Kenji Yamamoto, Yoshimitsu Matsui, Kenji Horiuchi, Masanori Yoshida