Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/23)
  • Patent number: 7060425
    Abstract: A color photographic material is described containing a compound of formula (I) wherein, if n=1, R1 is, inter alia, a radical of formula (II), and, if n=2, R1 is unsubstituted or C1–C4alkyl- or hydroxy-substituted phenylene or naphthylene; or —R12—X—R13—, and other residues are as defined in claim 1. The compound of formula (I) is effective as scavenger of the oxidized form of the developer (Dox scavenger), especially when contained in an interlayer between light sensitive layers. Selected compounds of this class can also be used as additives, for example as dye stabilizer, in color photographic materials, or as an antioxidant for organic materials.
    Type: Grant
    Filed: October 11, 1999
    Date of Patent: June 13, 2006
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Suruliappa Gowper Jeganathan, Stéphan Biry, Peter Nesvadba, David George Leppard
  • Patent number: 7053115
    Abstract: The present invention relates to a novel crystalline form of dorzolamide hydrochloride, to processes for its preparation and a pharmaceutical composition containing it.
    Type: Grant
    Filed: April 7, 2003
    Date of Patent: May 30, 2006
    Assignee: Hetero Drugs Limited
    Inventors: Reddy Bandi Parthasaradhi, Reddy Kura Rathnakar, Reddy Rapolu Raji, Reddy Dasari Muralidhara, Reddy Itiyata Srinivas
  • Patent number: 7045514
    Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.
    Type: Grant
    Filed: July 12, 2004
    Date of Patent: May 16, 2006
    Assignee: AstraZeneca AB
    Inventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
  • Patent number: 7030250
    Abstract: The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides (I) wherein R1 is H or C1-5 alkyl, and R2 is C1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-7,7-dioxides, and comprises protecting the alkylamine group, introducing a sulfonamide group and eliminating protecting group.
    Type: Grant
    Filed: March 3, 2003
    Date of Patent: April 18, 2006
    Assignee: Ragatives, S.L.
    Inventors: Pablo García Losada, Luis Octavio Silva Guisasola, Antonio Lorente Bonde-Larsen, Jorge Martín Juárez
  • Patent number: 7018802
    Abstract: Electrochemiluminescent-labels and enzyme substrates, which preferably are conjugated, are used in immunoassays and electrochemiluminescence is generated catalytically. In conventional electrochemiluminescence immunoassays, an anti-analyte antibody molecule can give rise to typically 6–8 electrochemiluminescence-active ruthenium atoms, while in the present invention, each enzyme-labeled anti-analyte molecule can give rise to thousands of electrochemiluminescence-active ruthenium atoms per second. An exemplary immunoassay is based on a catalytic process employing ?-lactamase-conjugated anti-analytes which enzymatically hydrolyze electrochemiluminescent-labeled substrates, making them strongly electrochemiluminescent. The electrochemiluminescence signal generated by each anti-analyte molecule (i.e., each analyte molecule) is much greater than with the conventional method. Accordingly, greater sensitivity can be gained in the measurement of low concentrations of a given immunoassay analyte.
    Type: Grant
    Filed: September 4, 2002
    Date of Patent: March 28, 2006
    Assignee: BioVeris Corporation
    Inventors: Mark T. Martin, Rick Saul, Pam Liang
  • Patent number: 6963002
    Abstract: An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a ?-chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the ?-chloro vinyl carbonyl compound in
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: November 8, 2005
    Assignee: Glenmark Pharmaceuticals Limited
    Inventors: Bobba Venkata Siva Kumar, Vishvas Dattatraya Patil, Changdev Namdev Raut, Shekhar Bhaskar Bhirud, Batchu Chandrasekhar
  • Patent number: 6916831
    Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.
    Type: Grant
    Filed: February 24, 2003
    Date of Patent: July 12, 2005
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
  • Publication number: 20040242901
    Abstract: The present invention relates to sulfonium salts, to methods for their preparation and to radiation curable compositions containing them as photoinitiators.
    Type: Application
    Filed: June 22, 2004
    Publication date: December 2, 2004
    Inventors: Gabriele Norcini, Angelo Casiraghi, Marco Visconti, Giuseppe Li Bassi
  • Publication number: 20040235905
    Abstract: Therapeutically active compounds of formula (I): wherein X is —O—, —CH2— or —C(O)—; Z is —CHR9— or valence bond; Y is —CH2—, —C(O)—, CH(OR10)—, —CH(NR11R12)—, —O—, —S—, —S(O)— or —S(O2)—, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is —CR9— and Y is —CH—, C(OR10)— or —C(NR11R12)—; R1 is —(CH2)nNR4R7 or one of the following groups: n is 1-4; R2 and R3 are independently H, lower alkyl, lower alkoxy, —NO2, halogen, —CF3, —OH, —NHR8 or —COOH, R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, —CF3, —NH2 or —CN; R6 is —NO2, —NR14R19, —CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 a
    Type: Application
    Filed: June 8, 2004
    Publication date: November 25, 2004
    Inventors: Tuula Koskelainen, Leena Otsomaa, Arto Karjalainen, Pekka Kotovuori, Jukka Tenhunen, Sirpa Rasku, Pentti Nore, Eija Tiainen, Olli Tormakangas
  • Publication number: 20040235885
    Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
    Type: Application
    Filed: March 10, 2003
    Publication date: November 25, 2004
    Applicant: SUCAMPO, AG
    Inventors: Ryuji Ueno, Tsuyoshi Habe
  • Patent number: 6818666
    Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: November 16, 2004
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Philippe Diaz
  • Publication number: 20040224928
    Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: May 24, 2004
    Publication date: November 11, 2004
    Applicants: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
  • Patent number: 6812225
    Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: November 2, 2004
    Assignee: AstraZeneca AB
    Inventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
  • Publication number: 20040214801
    Abstract: The present invention pertains, at least in part, to novel 9- substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: May 4, 2004
    Publication date: October 28, 2004
    Applicants: Paratek Pharmaceuticals, Inc., Trustees of Tufts College
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Jimmy Dumornay, Glen Rennie, Gui Liu, Darrell Koza, Paul Sheahan, Karen Stapleton, Paul Hawkins, Beena Bhatia, Atul K. Verma, Laura McIntyre, Tadeusz Warchol, David Messersmith
  • Patent number: 6809206
    Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.
    Type: Grant
    Filed: March 24, 2003
    Date of Patent: October 26, 2004
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Paul Walter Wojtkowski
  • Patent number: 6806288
    Abstract: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
    Type: Grant
    Filed: February 2, 2000
    Date of Patent: October 19, 2004
    Assignee: G.D. Searle & Co.
    Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartman, Cindy L Ludwig, Suzanne Metz, Donald E Korte
  • Publication number: 20040200388
    Abstract: Perylene derivatives of the general formula I 1
    Type: Application
    Filed: May 6, 2004
    Publication date: October 14, 2004
    Applicant: BASF Aktiengesellschaft
    Inventors: Claus Hackmann, Paul Gunthert, Anton Dotter, Peter Blaschka
  • Publication number: 20040202624
    Abstract: The invention relates to compounds of the formula I 1
    Type: Application
    Filed: April 28, 2004
    Publication date: October 14, 2004
    Inventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
  • Patent number: 6803129
    Abstract: The present invention relates to an organic light emitting diode (OLED) device, comprising an anode disposed on a substrate, an organic EL layer disposed on the anode and a cathode disposed on the organic EL layer.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: October 12, 2004
    Assignee: RiTdisplay Corporation
    Inventors: Hsien-Chang Lin, Chih-Hao Kung, Chung-Cheng Pai, Shwu-Ju Shieh, Tzu-Chin Tang
  • Publication number: 20040198805
    Abstract: The present invention relates to a novel crystalline form of dorzolamide hydrochloride, to processes for its preparation and a pharmaceutical composition containing it.
    Type: Application
    Filed: July 2, 2003
    Publication date: October 7, 2004
    Inventors: Reddy Bandi Parthasaradhi, Reddy Kura Rathnakar, Reddy Rapolu Raji, Reddy Dasari Muralidhara, Reddy Itiyata Srinivas
  • Publication number: 20040192723
    Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided.
    Type: Application
    Filed: December 8, 2003
    Publication date: September 30, 2004
    Inventors: Nurulain Zaveri, Wan-Ru Chao, Ahlem Bensari
  • Publication number: 20040180838
    Abstract: The use of bicyclic carbohydrates for the treatment of parasite infections is described. Different bicyclic carbohydrates have been tested in vitro against a number of protozoa. These compounds also have been screened against viruses, tumors, bacteria and fungi. Compound A1, a thiophenyl-containing bicyclic carbohydrate possessed significant activity against Trypanosoma brucei rhodiense, a parasite that causes the lethal sleeping sickness. Compound A2 and Compound A3, bicyclic carbohydrates with halogen containing aryl groups, possessed significant activity against Leishmania donovani, a parasite that causes leishmaniasis. Bicyclic carbohydrates in general, and Compound A1, Compound A2 and Compound A3 more specifically, could be possible treatments for the sleeping sickness and leishmaniasis in the future.
    Type: Application
    Filed: January 7, 2004
    Publication date: September 16, 2004
    Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Bart Ruttens
  • Publication number: 20040176334
    Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.
    Type: Application
    Filed: February 24, 2004
    Publication date: September 9, 2004
    Applicants: Paratek Pharmaceuticals, Inc., Trustees of Tufts College
    Inventors: Mark L. Nelson, Stuart B. Levy, Roger Frechette, Todd E. Bowser, Mohamed Y. Ismail
  • Publication number: 20040176616
    Abstract: A highly efficient process is provided for producing an optically active compound having high optical purity by an asymmetric reaction using as a catalyst a transition metal complex having an optically active nitrogen-containing compound as an asymmetric ligand.
    Type: Application
    Filed: December 31, 2003
    Publication date: September 9, 2004
    Applicant: KANTO KAGAKU KABUSHIKI KAISHA
    Inventors: Masahito Watanabe, Kunihiko Murata, Takao Ikariya
  • Publication number: 20040167151
    Abstract: Compounds are described having a structure according to Formula I or Formula II: 1
    Type: Application
    Filed: February 24, 2003
    Publication date: August 26, 2004
    Inventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
  • Publication number: 20040152761
    Abstract: A compound of the general formula (I) or (II) wherein X is O, NR4 or S and R1-R8 are as defined in the specification.
    Type: Application
    Filed: March 8, 2004
    Publication date: August 5, 2004
    Inventors: Andrew Heaton, Graham Edmund Kelly, Naresh Kumar
  • Publication number: 20040147551
    Abstract: Isoflavone compounds are described and recommended as therapeutic agents. Exemplified and preferred compounds are (a). Indications show compounds have good competitive binding to estrogen receptors. This is exemplified.
    Type: Application
    Filed: November 7, 2003
    Publication date: July 29, 2004
    Applicant: Novogen Research Pty Ltd.
    Inventors: Andrew Heaton, Naresh Kumar, Graham Edmund Kelly, Alan Husband
  • Publication number: 20040138183
    Abstract: The present invention pertains to novel 7,9-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: December 16, 2003
    Publication date: July 15, 2004
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Y. Ismail, Todd Bowser, Laura McIntyre, Beena Bhatia, Paul Hawkins, Laxma Reddy, Karen Stapleton, Tadeusz Warchol, Paul Sheahan
  • Patent number: 6750346
    Abstract: The disclosure is directed to so-called laser-compatible NIR marker dyes based on polymethines for use in optical, in particular, fluorescence optical determination and detection methods, for example, in the fields of medicine, pharmaceutics and in the areas of life science, materials science and environmental science. The disclosure further discusses the aim of the invention which was to create NIR marker dyes based on polymethine which have a high degree of photostability and stability in storage as well as a high fluorescent yield and which can be excited to fluorescence in the easiest possible manner by means of laser radiation in the visible or NIR spectral range, particularly with light of an argon, helium/neon, or diode laser. Dyes based on polymethine of general formula (I) are used.
    Type: Grant
    Filed: January 22, 2002
    Date of Patent: June 15, 2004
    Assignee: Carl Zeiss Jena GmbH
    Inventors: Peter Czerney, Frank Lehmann, Bernd Schweder, Matthias Wenzel
  • Publication number: 20040110790
    Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided.
    Type: Application
    Filed: December 6, 2002
    Publication date: June 10, 2004
    Inventors: Nurulain Zaveri, Wan-Ru Chao, Ahlem Bensari
  • Publication number: 20040102479
    Abstract: The present invention relates to a novel benzopyran or thiobenzopyran derivative represented by formula (1): pharmaceutically acceptable salt or stereoisomer thereof, in which X, R1, R2, R3, R4 and A are defined as described in the specification, and to a process for preparation thereof and a pharmaceutical composition having anti-estrogenic activity which contains the compound (1) as an active component.
    Type: Application
    Filed: August 12, 2003
    Publication date: May 27, 2004
    Applicant: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
  • Publication number: 20040097477
    Abstract: An androgenic steroid compound of the formula: 1
    Type: Application
    Filed: November 4, 2003
    Publication date: May 20, 2004
    Applicant: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
  • Publication number: 20040097733
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: July 2, 2003
    Publication date: May 20, 2004
    Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Publication number: 20040082798
    Abstract: The invention relates to the use of compounds of formula (I) and of their salts and stereoisomers for producing medicaments used in the treatment of cardiovascular diseases.
    Type: Application
    Filed: December 22, 2003
    Publication date: April 29, 2004
    Inventors: Cristina Alonso-Alija, Michael Harter, Michael Hahn, Josef Pernerstorfer, Stefan Weigand, Johannes-Peter Stasch, Frank Wunder
  • Publication number: 20040077882
    Abstract: Bicyclic cyclopropane derivatives of the general Formula (I) 1
    Type: Application
    Filed: September 9, 2003
    Publication date: April 22, 2004
    Inventors: Norbert Moszner, Armin de Meijere, Frank Zeuner, Urs Karl Fischer
  • Publication number: 20040063755
    Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I): 1
    Type: Application
    Filed: August 18, 2003
    Publication date: April 1, 2004
    Inventors: Edmund J. Moran, John R. Jacobsen, Michael R. Leadbetter, Matthew B. Nodwell, Sean G. Trapp, James Aggen, Timothy J. Church
  • Publication number: 20040044226
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Application
    Filed: April 15, 2003
    Publication date: March 4, 2004
    Inventors: Frank P. DiNinno, Seongkon Kim, Jane Y. Wu
  • Publication number: 20040044225
    Abstract: Disclosed are processes for producing a (2S) or (2R) 4-oxo-chroman-2-yl acyl compounds and chroman-2-yl acyl compounds, esters or amides thereof as well as derivatives thereof. Such processes may involve chiral synthesis or achiral synthesis, preferably coupled with a resolution procedure. Such compounds, particularly (2S) or (2R) acetic acid esters, are useful intermedates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are processes for making derivatives of such substantially pure, or enhanced compositions of single (2R) or (2S) enantiomer intermediates or processes for producing final products or salts from such desired enantiomers.
    Type: Application
    Filed: July 3, 2003
    Publication date: March 4, 2004
    Inventors: James Kanter, Charles Marlowe, Anjali Pandey, John J.G. Mullins, Robert Scarborough, Greg Butke, Barry Jacobson, Derek Walker
  • Publication number: 20040029914
    Abstract: Novel compounds are useful as chemotherapeutic, chemopreventative, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones.
    Type: Application
    Filed: April 18, 2003
    Publication date: February 12, 2004
    Inventors: Nurulain Zaveri, Wan-Ru Chao
  • Publication number: 20040016370
    Abstract: Fluorescent functional dyes represented by the following formulas: 1
    Type: Application
    Filed: July 26, 2002
    Publication date: January 29, 2004
    Applicant: 3M Innovative Properties Company
    Inventor: David B. Olson
  • Patent number: 6680332
    Abstract: Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: January 20, 2004
    Assignee: Euro-Celtique S.A.
    Inventors: Christopher S. Konkoy, David B. Fick, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana
  • Patent number: 6677460
    Abstract: An aromatic carboxylic acid bicyclic sulfur compound of the formula (II): wherein X1 is a C1 to C4 alkyl, a halogen, a C1 to C4 haloalkyl, a C2 to C4 alkoxyalkyl, a C1 to C4 alkoxy or a C1 to C4 haloalkoxy; X2 is a hydrogen, a C1 to C4 alkyl or a C1 to C4 haloalkyl, or X2 forms a bond with X5; X3 is a hydrogen, a C1 to C4 alkyl or a C1 to C4 haloalkyl; X4 is a hydrogen, a halogen, a C1 to C4 alkyl, a C1 to C4 haloalkyl or a C1 to C4 alkoxy; X5 forms a bond with X2 or X5 forms a bond with X7; each of X6 and X8 is independently a hydrogen or a C1 to C4 alkyl or forms a bond with X5; p is 1; and n is 0, 1 or 2; or a salt thereof.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: January 13, 2004
    Assignee: Idemitsu Kosan Company, Limited
    Inventors: Kazufumi Nakamura, Masashi Sakamoto, Ichiro Nasuno
  • Patent number: 6677338
    Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: January 13, 2004
    Assignees: President and Fellows of Harvard College, Organix, Inc.
    Inventors: Bertha K. Madras, Peter C. Meltzer
  • Publication number: 20030236410
    Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof wherein: 1
    Type: Application
    Filed: June 2, 2003
    Publication date: December 25, 2003
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Wai Ngor Chan, John Morris Evans, Geoffrey Stemp, Neil Upton, Robert Nicholas Willette
  • Publication number: 20030232819
    Abstract: The present invention provides novel tropane compounds and methods for their use.
    Type: Application
    Filed: March 27, 2003
    Publication date: December 18, 2003
    Inventors: Paul Blundell, Peter C. Meltzer, Bertha K. Madras
  • Publication number: 20030232827
    Abstract: This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders.
    Type: Application
    Filed: February 10, 2003
    Publication date: December 18, 2003
    Inventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Shanghao Lui
  • Publication number: 20030220509
    Abstract: The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides (I) wherein R1 is H or C1-5 alkyl, and R2 is C1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-7,7-dioxides, and comprises protecting the alkylamine group, introducing a sulfonamide group and eliminating protecting group. Some compounds of formula (I) are inhibitors of the carbonic anhydrase and can be used in the treatment of elevated intraocular pressure.
    Type: Application
    Filed: March 3, 2003
    Publication date: November 27, 2003
    Applicant: RAGACTIVES, S.L.
    Inventors: Pablo Garcia Losada, Luis Octavio Silva Guisasola, Antonio Lorente Bonde-Larsen, Jorge Martin Juarez
  • Publication number: 20030216463
    Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.
    Type: Application
    Filed: December 2, 2002
    Publication date: November 20, 2003
    Inventors: Ramesh M. Kanojia, Nareshkumar F. Jain, Raymond Ng, Zhihua Sui, Jiayi Xu
  • Patent number: 6645951
    Abstract: The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: November 11, 2003
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
  • Publication number: 20030203927
    Abstract: Heterocyclic-substituted tricyclics of the formula 1
    Type: Application
    Filed: October 16, 2002
    Publication date: October 30, 2003
    Applicant: Schering Corporation
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Yan Xia