Nitrogen Attached Directly Or Indirectly To The Tricyclo Ring System By Nonionic Bonding Patents (Class 549/48)
  • Patent number: 8969593
    Abstract: Organic dyes and photoelectric conversion devices are provided. The Organic dye has the structure represented by formula (I), wherein, n is an integral of 2-11; the plurality of X is independent and elected from the group consisting of and combinations thereof; R, R1, and R2 comprise hydrogen, halogen, C1-18 alkyl group, C1-18 alkoxy group, C3-18 heteroalkyl group, C3-20 aryl group, C3-20 heteroaryl group, C3-20 cycloaliphatic group or C3-20 cycloalkyl group, or R1 is connected to R2 to form a ring having 5-14 members; R3 comprise hydrogen, halogen, nitro group, amino group, C1-18 alkyl group, C1-18 alkoxy group, C1-18 sulfanyl group, C3-18 heteroalkyl group, C3-20 aryl group, C3-20 heteroaryl group, C3-20 cycloaliphatic group or C3-20 cycloalkyl group; and Z is hydrogen, alkali metal, or quaternary ammonium salt.
    Type: Grant
    Filed: December 31, 2009
    Date of Patent: March 3, 2015
    Assignee: Industrial Technology Research Institute
    Inventors: Yung-Liang Tung, Jia-Yin Wu, Jen-An Chen, Hsin-Yi Hsu, Chun-Guey Wu, Min-Fong Jhong, Song-Yeu Tsai
  • Publication number: 20140221664
    Abstract: The inventions disclosed and described herein relate to new and efficient generic methods for making a wide variety of compounds having HAr—Z-Har tricyclic cores, wherein HAr is an optionally substituted five or six membered heteroaryl ring, and Hal is a halogen, and Z is a bridging radical, such as S, Sc, NR5, C(O), C(O)C(O), Si(R5)2, SO, SO2, PR5, BR5, C(R5)2 or P(O)R5 and both HAr are covalently bound to one another. The synthetic methods employ a “Base-Catalyzed Halogen Dance” reaction to prepare a metallated compound comprising a five or six membered heteroaryl ring comprising a halogen atom, and then oxidatively coupling the reactive intermediate compound. The compounds of Formula (II) and/or oligomer or polymers comprising repeat units having Formula (II) can be useful for making semi-conducting materials, and/or electronic devices comprising those materials. Acyl compounds can be prepared. Heteroarylene substituents can be used. The core tricyclic core can be coupled to itself.
    Type: Application
    Filed: August 9, 2012
    Publication date: August 7, 2014
    Applicant: GEORGIA TECH RESEARCH CORPORATION
    Inventors: Yulia A. Getmanenko, Seth Marder, Do Kyung Hwang, Bernard Kippelen
  • Patent number: 8703970
    Abstract: Disclosed herein are compounds having photoremovable protecting groups which are removed after the compounds absorbs light of a given wavelength and undergo an electrocyclic reaction between a chromophore in the compound attached via an anilide to a benzothiophene ring.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: April 22, 2014
    Assignee: Marquette University
    Inventors: Mark G. Steinmetz, Majher I. Sarker, Tasnuva Shahrin
  • Patent number: 8652752
    Abstract: Compounds of the Formula (I), wherein L1, L?1, L?1, L2, L?2, L?2, L3, L?3, L?3, L4, L?4 and L?4 for example are hydrogen or COT; R, R? and R? for example are hydrogen, C6-C12aryl or C3-C20heteroaryl; X, X? and X? for example are O, S, single bond, NRa or NCORa, T is for example hydrogen, C1-C20alkyl, C3-C12cycloalkyl, C2-C20alkenyl, C5-C12cycloalkenyl, C7-C18cycloalkylenaryl, C5-C18cycloalkylenheteroaryl, C6-C14aryl, providedthat at least one of R, R? or R? is unsubstituted or substituted C3-C20heteroaryl; and Y is an inorganic or organic anion; are suitable as photolatent acid generators.
    Type: Grant
    Filed: September 22, 2008
    Date of Patent: February 18, 2014
    Assignee: BASF SE
    Inventors: Pascal Hayoz, Hitoshi Yamato, Toshikage Asakura
  • Publication number: 20130167930
    Abstract: The invention relates to compounds of general formula IIIa and their use in optoelectronic components.
    Type: Application
    Filed: December 29, 2011
    Publication date: July 4, 2013
    Applicant: Heliatek Gmbh
    Inventors: Dirk Hildebrandt, Gunter Mattersteig, Olga Gerdes, Serge Vetter, Andre Weiss
  • Publication number: 20130123265
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 4, 2013
    Publication date: May 16, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
  • Patent number: 8058550
    Abstract: This disclosure relates to a polymer that includes a first comonomer repeat unit containing a benzothiadiazole moiety, a thiophene oxide moiety, a cyclopentadithiophene oxide moiety, a thiadiazoloquinoxaline moiety, a benzoisothiazole moiety, a benzothiazole moiety, a thienothiophene moiety, a thienothiophene oxide moiety, a dithienothiophene moiety, a dithienothiophene oxide moiety, or a tetrahydroisoindole moiety. The polymer can be used as a photoactive material in a photovoltaic cell. This disclosure also relates to such photovoltaic cells, as well as modules containing such photovoltaic cells.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: November 15, 2011
    Assignee: Konarka Technologies, Inc.
    Inventors: Russell Gaudiana, Richard Kingsborough, Xiaobo Shi, David Waller, Zhengguo Zhu
  • Patent number: 7910653
    Abstract: Aromatic sulfonimide ionene polymers useful as membranes in electrochemical cells are prepared.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: March 22, 2011
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Mark F. Teasley
  • Patent number: 7868086
    Abstract: Aromatic sulfonimide ionene polymers useful as membranes in electrochemical cells are prepared.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: January 11, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Mark F. Teasley
  • Patent number: 7838594
    Abstract: Aromatic sulfonimide ionene compositions useful as monomers for polymers in electrochemical cells are prepared.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: November 23, 2010
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Mark F. Teasley
  • Patent number: 7838612
    Abstract: Described herein are aromatic sulfonimide compositions that can be used to prepare polymers useful as membranes in electrochemical cells.
    Type: Grant
    Filed: October 1, 2007
    Date of Patent: November 23, 2010
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Mark F. Teasley
  • Patent number: 7781673
    Abstract: This disclosure relates to a polymer containing a first comonomer repeat unit and a second comonomer repeat unit. The first comonomer repeat unit includes a cyclopentadithiophene moiety. The second comonomer repeat unit includes a thienothiophene moiety, a thienothiophene tetraoxide moiety, a dithienothiophene moiety, a dithienothiophene dioxide moiety, a dithienothiophene tetraoxide moiety, or a tetrahydroisoindole moiety. The polymer can be used as a photoactive material in a photovoltaic cell. This disclosure also relates to such photovoltaic cells, as well as modules containing such photovoltaic cells.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: August 24, 2010
    Assignee: Konarka Technologies, Inc.
    Inventors: Russell Gaudiana, Richard Kingsborough, David Waller, Zhengguo Zhu
  • Patent number: 7772407
    Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
    Type: Grant
    Filed: February 26, 2007
    Date of Patent: August 10, 2010
    Assignees: Astellas Pharma Inc., Kotobuki Pharmaceuticals Co., Ltd.
    Inventors: Masakazu Imamura, Takeshi Murakami, Ryota Shiraki, Kazuhiro Ikegai, Takashi Sugane, Fumiyoshi Iwasaki, Eiji Kurosaki, Hiroshi Tomiyama, Atsushi Noda, Kayoko Kitta, Yoshinori Kobayashi
  • Patent number: 7750040
    Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
    Type: Grant
    Filed: July 20, 2005
    Date of Patent: July 6, 2010
    Inventors: Martin Bolli, Daniel Bur, Martine Clozel, Walter Fischli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Michael Scherz, Thomas Weller
  • Patent number: 7674822
    Abstract: This invention relates to modulating (e.g., inhibiting) protein tyrosine phosphatase 1B (PTP1B).
    Type: Grant
    Filed: November 22, 2005
    Date of Patent: March 9, 2010
    Assignee: Wyeth
    Inventors: Jinbo Lee, Michael J. Smith, Alessandro Fabio Moretto, Zhao-Kui Wan, Eva Deanna Binnun, Weixin Xu, Kenneth W. Foreman, Diane M. Joseph-McCarthy, David V. Erbe, Steve Y. Tam
  • Patent number: 7671081
    Abstract: Compounds of formula (I): wherein the substituents are as defined herein.
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: March 2, 2010
    Assignee: Sun Chemical Corporation
    Inventors: Shaun Lawrence Herlihy, Brian Rowatt, Robert Stephen Davidson
  • Patent number: 7465825
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: December 16, 2008
    Assignee: The Institute for Pharmaceutical Discovery, LLC
    Inventors: Michael C. Van Zandt, Haiquan Fang, Shaojing Hu, Darren Whitehouse
  • Publication number: 20080177088
    Abstract: Described herein are aromatic sulfonimide compositions that can be used to prepare polymers useful as membranes in electrochemical cells.
    Type: Application
    Filed: October 1, 2007
    Publication date: July 24, 2008
    Inventor: MARK F. TEASLEY
  • Patent number: 7393846
    Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: July 1, 2008
    Assignee: Glenmark Pharmaceuticals, S.A.
    Inventors: Balasubramanian Gopalan, Laxmikant Atmaram Gharat, Aftab Dawoodbhai Lakdawala, Usha Karunakaran
  • Publication number: 20080146810
    Abstract: The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.
    Type: Application
    Filed: June 27, 2007
    Publication date: June 19, 2008
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Gopalan Balasubramanian, Laxmikant A. Gharat, Aftab D. Lakdawala, Raghu R. Anupindi
  • Patent number: 7332615
    Abstract: The present invention discloses hydrophilic derivatives of 4,8-dihydrobenzodithiophene-4,8-diones, which are active as anticancer agents, along with pharmaceutical formulations containing the same.
    Type: Grant
    Filed: September 28, 2005
    Date of Patent: February 19, 2008
    Assignees: Industrial Technology Research Institute, Yung Shin Pharm. Ind. Co., Ltd.
    Inventors: Pi-Tsan Huang, Yen-Fang Wen, Wuu-Chian Shin, Mei-Hwai Chen, Sheng-Chu Kuo, Kuo-Hsiung Lee
  • Patent number: 7238725
    Abstract: The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.
    Type: Grant
    Filed: October 8, 2003
    Date of Patent: July 3, 2007
    Assignee: Glenmark Pharmaceuticals Ltd.
    Inventors: Gopalan Balasubramanian, Laxmikant A. Gharat, Aftab D. Lakdawala, Raghu R. Anupindi
  • Patent number: 7223789
    Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 9, 2004
    Date of Patent: May 29, 2007
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Balasubramanian Gopalan, Laxmikant Atmaram Gharat, Aftab Dawoodbhai Lakdawala, Usha Karaunakaran
  • Patent number: 7175961
    Abstract: Bistable molecules are provided with at least one photosensitive functional group. As thus constituted, the bistable molecules are photopatternable, thereby allowing fabrication of micrometer-scale and nanometer-scale circuits in discrete areas without relying on a top conductor as a mask. The bistable molecules may comprise molecules that undergo redox reactions, such as rotaxanes and catenanes, or may comprise molecules that undergo an electric-field-induced band gap change that causes the molecules, or a portion thereof, to rotate, bend, twist, or otherwise change from a substantially fully conjugated state to a less conjugated state. The change in states in the latter case results in a change in electrical conductivity.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: February 13, 2007
    Assignee: Hewlett-Packard Development Company, L.P.
    Inventors: Patricia A. Beck, Xiao-An Zhang, Zhang-Lin Zhou
  • Patent number: 7101905
    Abstract: New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.
    Type: Grant
    Filed: March 29, 2002
    Date of Patent: September 5, 2006
    Assignee: King Pharmaceuticals Research & Development, Inc.
    Inventors: Allan R. Moorman, Romeo Romagnoli, Pier Giovanni Baraldi
  • Patent number: 6818260
    Abstract: The invention relates to new thienothiophene derivatives, their use as semiconductors or charge transport materials, in optical, electrooptical or electronic devices like for example organic field effect transistors (FET or OFET) for thin film transistor liquid crystal displays and integrated circuit devices such as RFID tags, electroluminescent devices in flat panel displays, and in photovoltaic and sensor devices, and to a field effect transistor, light emitting device or ID tag comprising the thienothiophene derivatives.
    Type: Grant
    Filed: July 9, 2002
    Date of Patent: November 16, 2004
    Assignee: Merck Patent GmbH
    Inventors: Louise Farrand, Marcus Thompson, Mark Giles, Martin Heeney, Steven Tierney, Maxim Shkunov, David Sparrowe, Iain McCulloch
  • Patent number: 6693136
    Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: February 17, 2004
    Assignee: Abbott Laboratories
    Inventors: Chih-Hung Lee, Meiqun Jiang, Richard A. Perner, Arthur Gomtsyan, Erol K. Bayburt, Guo Zhu Zheng
  • Publication number: 20030225097
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: November 5, 2002
    Publication date: December 4, 2003
    Inventors: Michael Howard Block, Craig Samuel Donald, David Robert Brittain, Kevin Michael Foote
  • Publication number: 20030220340
    Abstract: This invention provides novel compounds possessing antibacterial and/or antifungal and/or antitumor activity. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
    Type: Application
    Filed: May 15, 2003
    Publication date: November 27, 2003
    Inventors: Christoher Don Roberts, Jesse Daniel Keicher, Mikail Hakan Gazginci, Mark Douglas Velligan
  • Patent number: 6605632
    Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: August 12, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Frédérique Klupsch, Gérald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6602901
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: August 5, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Publication number: 20030018065
    Abstract: This invention provides processes for preparing a group of novel bridged tricyclic compounds having the formula: 1
    Type: Application
    Filed: June 27, 2002
    Publication date: January 23, 2003
    Applicant: Wyeth
    Inventors: Alexander Alexei Greenfield, John Anthony Butera
  • Patent number: 6509499
    Abstract: The invention concerns novel compound of general formula (1) in which: P, T1, T2, X and n are as defined in claim 1, their tautomeric forms, and their additive salts with pharmaceutically acceptable bases. The invention also concerns methods for preparing these compounds and their applications as medicines. These compounds inhibit the aldose reductase enzyme and can be used in the treatment or prevention of peripheral and autonomous neurological diabetic complications, renal and ocular disorders such as cataract and retinopathy.
    Type: Grant
    Filed: March 17, 2000
    Date of Patent: January 21, 2003
    Assignee: Merck PatentGesellschaft mit
    Inventors: François Collonges, Hervé Dumas, Claude Lardy, Philippe Durbin
  • Patent number: 6495701
    Abstract: The present invention is directed to processes for the preparation of a compound useful for treating diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R6 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R6 is not a hydrogen atom, and to intermediates useful for the said processes. The processes of the present invention are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: December 17, 2002
    Assignee: Asahi Kasei Kabushiki Kaisha
    Inventors: Koki Matsubara, Hitoshi Kida
  • Publication number: 20020151524
    Abstract: The invention provides fungicidal compounds of formula I and salts thereof: 1
    Type: Application
    Filed: August 6, 2001
    Publication date: October 17, 2002
    Applicant: Aventis CropScience S.A.
    Inventors: Vincent Gerusz, Darren James Mansfield, Joseph Perez, Jean-Pierre Vors
  • Patent number: 6429312
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R5 is hydrogen or C1-C6 alkyl; and R 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 19, 2001
    Date of Patent: August 6, 2002
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • 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
  • Publication number: 20010044461
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: March 19, 2001
    Publication date: November 22, 2001
    Inventors: Jun Yuan, Xi Chen
  • 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: 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: 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: 6172104
    Abstract: Methods of treating Pneumocystis carinii pneumonia comprise administering a therapeutically effective amount of a dicationic dibenzofuran compound described by Formula (I). Methods of treating Pneumocystis carinii pneumonia also comprise administering a therapeutically effective amount of a dicationic dibenzothiophene compound described by Formula (II). Novel compounds are also disclosed, and are represented by the Formulae (I) and (II).
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: January 9, 2001
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Richard R. Tidwell, James Edwin Hall
  • Patent number: 6172099
    Abstract: Compounds represented by general formula (I) or their salts, having &bgr;3-adrenoceptor agonism and being efficacious when employed in drugs for treating and preventing diabetes, obesity, hyperlipemia, etc. wherein R represents hydrogen or methyl; R1 represents hydrogen, halogeno, hydroxy, benzyloxy, amino or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4 ′ or nitro (wherein R3 represents hydrogen, methyl, SO2R5, formyl or CONHR6′; R5 represents lower alkyl, benzyl or NR4R4′; R4 and R4′ may be the same or different and each represents hydrogen, lower alkyl or benzyl; and R6′ represents hydrogen or lower alkyl); R6 represents hydrogen or lower alkyl; n is 1 or 2; X represents secondary nitrogen, oxygen or sulfur; and when n is 1, then one of R7 and R8 represents hydrogen while another represents hydrogen, amino, acetylamino or hydroxy, or when n is 2, then R8 represents hydrogen while R7 represents hydrogen, amino, acetylamino or hydroxy.
    Type: Grant
    Filed: March 27, 2000
    Date of Patent: January 9, 2001
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Shiro Miyoshi, Kohei Ogawa
  • Patent number: 6080338
    Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the pyran portion or on the pyran portion and the naphtho- or benzo-portion thereof. These compounds may be represented by one of the following graphic formula: ##STR1## wherein B and/or B' is an alkylaminoalkylamino-substituted aryl group and R.sub.1 may also be an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: June 27, 2000
    Assignee: Transitions Optical, Inc.
    Inventor: Anil Kumar
  • 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: 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: 5917057
    Abstract: This invention relates to N-hydroxy-dibenz?b,e!oxepinalkylamines, N-hydroxy-dibenz?b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R.sup.1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R.sup.2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.
    Type: Grant
    Filed: February 27, 1998
    Date of Patent: June 29, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Richard C. Allen, Grover C. Helsley, R. Richard L. Hamer, Brian S. Freed, John I. White, Lawrence L. Martin
  • Patent number: 5879592
    Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the naphtho- or benzo-portions and/or pyran portions thereof. These compounds may be represented by one of the following graphic formulae: ##STR1## wherein R.sub.1 is an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.
    Type: Grant
    Filed: December 10, 1997
    Date of Patent: March 9, 1999
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5840980
    Abstract: A diamine compound of the following formula (1): ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group, each of A.sub.1, A.sub.2 and A.sub.3 which are independent of one another, is a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a group of the following formula (2): ##STR2## wherein R.sub.1 is as defined above, and X is a substituted or unsubstituted arylene group or a substituted or unsubstituted heterocyclic bivalent group.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: November 24, 1998
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Mitsutoshi Anzai, Atsushi Takesue, Takanobu Watanabe, Chieko Inayoshi