The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 544/399)
  • Patent number: 6599903
    Abstract: Intermediate compounds having the formula wherein the substituents are defined as set forth in the disclosure.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: July 29, 2003
    Assignee: Societe de Conseils de Recherches d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Publication number: 20030109523
    Abstract: This invention provides novel bicyclic compounds of Formula (I): 1
    Type: Application
    Filed: June 6, 2002
    Publication date: June 12, 2003
    Applicant: Wyeth
    Inventors: Arie Zask, Diane B. Hauze, Kenneth L. Kees, Richard D. Coghlan, John Yardley
  • Publication number: 20030100750
    Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
    Type: Application
    Filed: May 3, 2002
    Publication date: May 29, 2003
    Inventors: Bing Wang, Satyanarayana Janagani, Wyeth B. Callaway, Jonathan L. Sessler
  • Patent number: 6562965
    Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: May 13, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Publication number: 20030088095
    Abstract: A first process for producing an optically active perfluoroalkylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfluoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro 3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybutanoic aryl ester derivatives.
    Type: Application
    Filed: August 7, 2002
    Publication date: May 8, 2003
    Applicant: CENTRAL GLASS COMPANY, LIMITED
    Inventors: Akihiro Ishii, Masatomi Kanai, Takashi Hayami, Katsuyoshi Shibata, Masaki Matsui, Kazumasa Funabiki, Yokusu Kuriyama, Manabu Yasumoto
  • Publication number: 20030078418
    Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.
    Type: Application
    Filed: March 15, 2002
    Publication date: April 24, 2003
    Inventors: James M. Balkovec, Mark L. Greenlee, Steven H. Olson, Gregory P. Rouen
  • Publication number: 20030069418
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
    Type: Application
    Filed: April 11, 2002
    Publication date: April 10, 2003
    Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
  • Patent number: 6541471
    Abstract: A compound of formula (I): wherein: G represents a group such as: wherein R1 and R2 independently represent a hydrogen atom or an alkyl, cycloalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl or heteroarylalkyl group, or, R1 and R2 together with the nitrogen atom form a heterocycloalkyl group, R3 represents a hydrogen atom or an alkyl or optionally substituted phenyl group, Ra represents a hydroxy group, a linear or branched (C1-C6)alkoxy group or an amino group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, m is an integer of from 0 to 1 inclusive, n and q are integers of from 0 to 6 inclusive, p and r are integers of from 1 to 6 inclusive, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base; and medicinal products containing the same which are useful as a TXA2 recept
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: April 1, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Gilbert Lavielle, Thierry Dubuffet, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Christine Vayssettes-Courchay
  • Publication number: 20030060625
    Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
    Type: Application
    Filed: September 26, 2002
    Publication date: March 27, 2003
    Inventors: Fred Thomas Bizzarro, Nancy-Ellen Haynes, Ramakanth Sarabu
  • Publication number: 20030060472
    Abstract: New compounds of formula I are described: 1
    Type: Application
    Filed: June 20, 2001
    Publication date: March 27, 2003
    Inventors: David Alexander Learmonth, Patricio Manuel Vieira Araujo Soares da Silva
  • Publication number: 20030060459
    Abstract: The present application describes modulators of MCP-1 of formula (I): 1
    Type: Application
    Filed: December 20, 2001
    Publication date: March 27, 2003
    Inventors: Percy Carter, Robert Cherney
  • Publication number: 20030060624
    Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: 1
    Type: Application
    Filed: April 17, 2002
    Publication date: March 27, 2003
    Inventor: Robert A. Singer
  • Patent number: 6515159
    Abstract: An S,S-ethylenediamine-N,N′-disuccinic acid iron alkali salt which contains a lactam compound represented by the following general formula (1): wherein M is an ammonium ion or an alkali metal ion, and an ethylenediaminemonosuccinic acid represented by the following general formula (2): wherein M is an ammonium ion or an alkali metal ion, in an amount of 7 wt % or less, respectively.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: February 4, 2003
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Toshitake Yamakawa, Haruo Sakai
  • Publication number: 20020193591
    Abstract: The present invention provides a process for producing intermediates of antibacterial agents in accordance with the following steps and intermediates in the production thereof.
    Type: Application
    Filed: July 11, 2002
    Publication date: December 19, 2002
    Applicant: DAIICHI PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Takemura, Hisashi Takahashi
  • Patent number: 6479518
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.
    Type: Grant
    Filed: September 21, 2001
    Date of Patent: November 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
  • Patent number: 6472397
    Abstract: The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen. wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III): wherein D represents the group —V—(CH2)p—COOR.
    Type: Grant
    Filed: November 3, 2000
    Date of Patent: October 29, 2002
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazumi Ota, Kazuko Kobayashi, Tomoaki Miura, Takahiro Imai, Kazumasa Aizawa, Hisashi Suzuki, Shokichi Ohuchi, Kiyoaki Katano, Takashi Ando
  • Patent number: 6458957
    Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.
    Type: Grant
    Filed: July 12, 2000
    Date of Patent: October 1, 2002
    Assignee: Geneva Pharmaceuticals, Inc.
    Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
  • Publication number: 20020123493
    Abstract: The present invention relates to cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: January 3, 2002
    Publication date: September 5, 2002
    Inventors: Michael Mullican, David Lauffer
  • Publication number: 20020107240
    Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: January 3, 2002
    Publication date: August 8, 2002
    Inventors: David Lauffer, Brian Ledford, Michael Mullican
  • Patent number: 6420561
    Abstract: An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: July 16, 2002
    Assignee: Japan Tobacco Inc.
    Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe
  • Publication number: 20020091089
    Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
    Type: Application
    Filed: April 16, 2001
    Publication date: July 11, 2002
    Inventors: Donald S. Karanewsky, Vincent J. Kalish, Edward D. Robinson, Brett R. Ullman
  • Patent number: 6413987
    Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: July 2, 2002
    Assignee: Bridge Pharma, Inc.
    Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
  • Patent number: 6395738
    Abstract: The present invention relates to benzofuran derivatives represented by following general formula (I): wherein R1 represents lower alkyl, R2 represents hydrogen or substituted or unsubstituted lower alkyl, R3, R4, R5 and R6 independently represent hydrogen or lower alkyl, X represents CH2 or C═O, and Y represents CH2 or NH, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 29, 2000
    Date of Patent: May 28, 2002
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Tohru Matsuzaki, Haruhiko Manabe
  • Patent number: 6388022
    Abstract: The present invention provides a linker binding carrier for organic synthesis represented by the formula: —Z—W—(SO2X)m wherein  is a carrier, X is a leaving group, Y is a bond or spacer, Z is a bivalent group, when Z is a bivalent electron attractive group, W is an aromatic ring which may be substituted and when Z is a bivalent non-electron attractive group, W is an aromatic ring which is substituted by an electron attractive group and may be further substituted and m is 1 or 2, or a salt thereof, which is useful for synthesizing a novel organic compound.
    Type: Grant
    Filed: August 30, 1999
    Date of Patent: May 14, 2002
    Assignee: Takeda Chemical Industires, Ltd.
    Inventors: Katsunori Nagai, Tetsuo Miwa
  • Patent number: 6369225
    Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: April 9, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
  • Patent number: 6365587
    Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
    Type: Grant
    Filed: May 13, 1999
    Date of Patent: April 2, 2002
    Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
  • Publication number: 20020016463
    Abstract: Novel compounds of the general formula: 1
    Type: Application
    Filed: February 22, 2001
    Publication date: February 7, 2002
    Inventors: Jeff Zablocki, Elfatih Elzein, Grigory Nudelman, Tim Marquart, Brent K. Blackburn, Venkata P. Palle
  • Publication number: 20020010176
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
    Type: Application
    Filed: July 28, 2001
    Publication date: January 24, 2002
    Inventors: Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
  • Patent number: 6335445
    Abstract: A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of and the other substituents are defined in the specification having an inhibitory activity of NO-synthase enzymes producing nitrogen mono-oxide and/or an activity which traps the reactive oxygen species.
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: January 1, 2002
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Patent number: 6303612
    Abstract: Processes for the preparation of derivatives of hydroxyphenylsulfanylbenzoic and hydroxyphenylsulfanylarylacetic acids of Formula (I) and pharmaceutical compositions including these compounds are provided: wherein X is H, halogen or NO2 group, n is 0 or 1, and m is 2 to 4 if Z is either 4-acetyl-3 -hydroxy-2-propylphenoxy of Formula (II): or a piperazinyl residue, or m is 1 if Z is quinolin-2-yl or 6-chloroquinoli-2-yl.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: October 16, 2001
    Assignee: Leciva, A.S.
    Inventors: Miroslav Kucha{haeck over (r)}, Vojt{haeck over (e)}ch Kmoní{haeck over (c)}ek, Vladimíra Panajotová, Bohumila Br{haeck over (u)}nová, Antonín Jandera, Hana Ji{haeck over (r)}í{haeck over (c)}ková, V{haeck over (e)}ra Bucharová
  • Patent number: 6300510
    Abstract: An S,S-ethylenediamine-N,N′-disuccinic acid iron alkali salt which contains a lactam compound represented by the following general formula (1): wherein M is an ammonium ion or an alkali metal ion, and an ethylenediaminemonosuccinic acid represented by the following general formula (2): wherein M is an ammonium ion or an alkali metal ion, in an amount of 7 wt % or less, respectively.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: October 9, 2001
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Toshitake Yamakawa, Haruo Sakai
  • Publication number: 20010025105
    Abstract: Disclosed are compounds of formula I: 1
    Type: Application
    Filed: April 9, 2001
    Publication date: September 27, 2001
    Applicant: Molecular Geriatarics Corporation
    Inventors: John DeBernardis, Daniel Kerkman, Raymond Zinkowski
  • Patent number: 6252071
    Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of &dgr;-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-&ggr;-tocopherols.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: June 26, 2001
    Assignee: Roche Vitamins Inc.
    Inventors: Robert Karl Müller, Heinz Schneider
  • Patent number: 6239277
    Abstract: A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula where m and n are individually an integer of from 1 to 6, R and R′ are the same or different and are hydrogen, C1 to C6 alkyl or aryl or heteroaryl that is unsubstituted or is substituted with at least one substituent that is halo, C1 to C6 alkyl or C1 to C6 alkoxy and R″ is C3 to C12 branched alkyl or an organic or inorganic cation. The process comprises treating a solution comprising a compound of the formula wherein m, R and R′ are as defined above and an aliphatic ester of the formula X—(CH2)n—O—CH2—CO(O)R″ where X is a leaving group and n and R″ are as defined above, with an effective amount of a base for a time and at a temperature sufficient to form a piperazine-substituted aliphatic carboxylate.
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: May 29, 2001
    Assignee: Salsbury Chemicals, Inc.
    Inventors: Pedro E. Hernandez, David John Fairfax, Erik T. Michalson
  • Patent number: 6221898
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
    Type: Grant
    Filed: August 29, 1997
    Date of Patent: April 24, 2001
    Assignee: Astra Aktiebolag
    Inventor: Thomas Antonsson
  • Patent number: 6214994
    Abstract: Disclosed are compounds of formula I: wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1 and Ar2 independently represent aryl groups; and Y is hydrogen; or Y and R1 or R2 together represent CH2;CH2CH2; CH2O; CH2S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; or the pharmaceutically acceptable salts thereof, useful in the treatment of neoplastic diseases, and bacterial or fungal infections, and in preventing or decreasing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore, useful for treating Alzheimer's Disease.
    Type: Grant
    Filed: July 13, 1999
    Date of Patent: April 10, 2001
    Assignee: Molecular Geriatrics Corporation
    Inventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
  • Patent number: 6180619
    Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.
    Type: Grant
    Filed: June 16, 1998
    Date of Patent: January 30, 2001
    Assignee: Biomeasure, Incorporated
    Inventor: Sun H. Kim
  • Patent number: 6166050
    Abstract: Compounds of the formula ##STR1## which inhibit leukocyte adhesion mediated by interaction of the .alpha..sub.4 .beta..sub.1 integrin (VLA-4) with its counterreceptor VCAM-1, and their use for the treatment of inflammatory and autoimmune diseases.
    Type: Grant
    Filed: December 10, 1999
    Date of Patent: December 26, 2000
    Assignee: American Home Products Corporation
    Inventors: Louis J. Lombardo, Joan Sabalski
  • Patent number: 6159979
    Abstract: Novel bicyclic aryl/bicyclic heterocyclic ring containing compounds having a combined 5HT.sub.1A, 5HT.sub.1B and 5HT.sub.1D receptor antagonistic activity are provided.
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: December 12, 2000
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 6140501
    Abstract: Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds.The present invention related to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of formula ##STR1## in which R.sub.1 represents a --CONH.sub.2, --CN, --COOH, --COOM or --COOR.sub.3 group, M being an alkali metal and R.sub.3 being an alkyl radical having from 1 to 4 carbon atoms; andR.sub.2 represents a hydrogen atom or a group --COR.sub.4 or --R.sub.5, where R.sub.4 is chosen from the groups --OR.sub.6 or --R.sub.7, in whichR.sub.5 represents an allyl or alkylaryl radical,R.sub.6 represents a linear or branched alkyl radical having from 1 to 4 carbon atoms, a haloalkyl, alkylaryl, alkylnitroaryl or alkylhaloaryl radical, andR.sub.
    Type: Grant
    Filed: October 9, 1998
    Date of Patent: October 31, 2000
    Assignee: UCB, S.A.
    Inventors: Guy Duchene, Michel Deleers, Guy Bodson, Genevieve Motte, Francoise Lurquin
  • Patent number: 6017918
    Abstract: The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: January 25, 2000
    Assignee: Warner-Lambert Company
    Inventors: Helen Tsenwhei Lee, Mark Alan Massa, William Chester Patt, Bruce David Roth
  • Patent number: 6002002
    Abstract: The present invention provides novel hydroxylamine derivatives represented by the general formula: wherein:X is O, --NH, or a group of formula NR', wherein R and R' are independently selected from alkyl, cycloalkyl, phenylalkyl, phenyl optionally substituted with halo, haloalkyl,alkyl, alkoxy or nitro; and a N-containing heterocyclic ring;R.sup.1 is H or alkanoyl,R.sup.2 is H or hydroxy optionally acylated with alkanoyl, andR.sup.3 is a group of the formula --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected fromH, alkyl, and a group of the formula --CO--NH--R wherein R is as defined above, orwherein R.sup.4 and R.sup.5 when taken together form a 5- to 7-membered heterocyclic ring which may optionally contain one additional hetero atom selected from nitrogen, oxygen and sulfur and which is optionally substituted with alkyl or phenylalkyl.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: December 14, 1999
    Assignee: Biorex Research & Development Co.
    Inventors: Laszlo Urogdi, Ede Marvanyos, Mihaly Barabas, Laszlo Jaszlits, Katalin Biro, Andrea Jednakovits, Erzsebet Radvanyne, Maria Kurthy, Istvanne Udvardy Nagy
  • Patent number: 5998414
    Abstract: Described herein are compounds of the general formula: ##STR1## a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, wherein:R.sub.1 is H, halo, aryl or aryl substituted with one or two groups independently selected from halo, C.sub.1-4 alkyl, C.sub.1-4 -alkoxy, nitro, trifluoromethyl, trifluoromethoxy or cyano;R.sub.2 is C.sub.4-9 alkyl; phenyl or phenyl substituted with one or two groups selected independently from OH, cyano, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, trifluoromethyl, trifluoromethoxy, nitro or phenyl; naphthyl;phenyl fused to a 5 or 6-membered heterocycle; the coumarin moiety ##STR2## wherein R.sub.3 and R.sub.4 are selected independently from H, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;or 1,2-methylenedioxy phenyl;with the proviso that R.sub.2 is not phenyl or 3,4-dimethoxyphenyl when R.sub.1 is H.Also described is their use as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia and anxiety.
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: December 7, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Xin Wang, Jian-min Fu, Adi M. Treasurywala
  • Patent number: 5986095
    Abstract: A process is described for preparing a compound of the formula or the S-enantiomer thereof,wherein:R is alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl,R.sup.1 is halogen;R.sup.2 is halogen, alkyl, cycloalkyl, aryl or ##STR1## wherein the process comprises treating the associated racemic alcohol with an acylatingagent ##STR2## (wherein L is a leaving group) and an enzyme or microorganism capable of enantioselective acylation. This process may also be used to isolate the unreacted R- or S-alcohol. The acylated product may be enantioselectively hydrolyzed with a lipase or lipase-supplying microorganism to the S- or R-alcohol. Compounds prepared by this invention are useful antipsychotic agents or useful intermediates therefor.
    Type: Grant
    Filed: January 6, 1992
    Date of Patent: November 16, 1999
    Assignee: E.R. Squibb & Sons, Inc.
    Inventors: Ronald L. Hanson, Ramesh N. Patel, Laszlo J. Szarka
  • Patent number: 5972940
    Abstract: A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and --NO.sub.2, E is --O-- or a covalent bond, n is an integer from 1 to 12, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms or taken together with the nitrogen to which they are attached form an optionally unsaturated 5 to 6-member ring of the formula --NX and X is selected from the group consisting of oxygen, sulfur, methylene and >N--R', R' being hydrogen or an alkyl of 1 to 6 carbon atoms, and their pharmaceutically acceptable acid addition salts useful to inhibit --NO synthase.
    Type: Grant
    Filed: September 10, 1997
    Date of Patent: October 26, 1999
    Assignee: Societe de Conseils Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Colette Broquet, Pierre Etienne Chabrier De Lassauniere
  • Patent number: 5935958
    Abstract: Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein Q, n, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetyl-cholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.
    Type: Grant
    Filed: June 26, 1997
    Date of Patent: August 10, 1999
    Assignee: Schering Corporation
    Inventors: Joseph A. Kozlowski, Derek B. Lowe, Wei K. Chang, Sundeep Dugar
  • Patent number: 5919777
    Abstract: The present invention relates to novel compounds of the general formula I ##STR1## which can be used for treating medical disorders resulting from a deficiency in growth hormone.
    Type: Grant
    Filed: April 23, 1997
    Date of Patent: July 6, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Thomas Kruse Hansen, Bernd Pesche, Knud Erik Andersen
  • Patent number: 5908843
    Abstract: Novel piperazine derivatives of formula I:Y--(C.sub.m H.sub.2m --CHR.sup.1).sub.n --CO--(NH--CHR.sup.2 --CO).sub.r -- Zwherein ##STR1## R.sup.1, R.sup.2 and R.sup.7 are each, independently, --C.sub.t H.sub.2t --R.sup.9, benzyl, hydroxybenzyl, imidazolylmethyl or indolylmethyl;R.sup.3 is H or H.sub.2 N--C(.dbd.NH)--;R.sup.4 and R.sup.6 are each, independently, (H,H) or .dbd.O;R.sup.5 is H, H.sub.2 N--C(.dbd.NH)-- or H.sub.2 N--C(.dbd.NH)--NH;R.sup.8 is OH, OA or NHOH;R.sup.9 is H, OH, NH.sub.2, SH, SA, COOH, CONH.sub.2 or NH--C(.dbd.NH)--NH.sub.2 ;A is in each case, independently, alkyl having 1-4 C atoms;m and t are each, independently, 0, 1, 2, 3 or 4;n and r are each, independently, 0 or 1; andp is 0, 1 or 2,inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for the treatment of thrombosis, apoplexy, cardiac infarctus, inflammation, arteriosclerosis and tumors.
    Type: Grant
    Filed: January 31, 1994
    Date of Patent: June 1, 1999
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Joachim Gante, Peter Raddatz, Horst Juraszyk, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 5874436
    Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.
    Type: Grant
    Filed: April 23, 1997
    Date of Patent: February 23, 1999
    Inventors: James P. Demers, Sigmond Johnson, Michele Ann Weidner-Wells, Ramesh M. Kanojia, Stephanie A. Fraga, Dieter Klaubert
  • Patent number: 5872117
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: November 4, 1997
    Date of Patent: February 16, 1999
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita