Spiro Patents (Class 540/543)
  • Patent number: 6916807
    Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: July 12, 2005
    Assignee: Pfizer Inc.
    Inventors: Kevin D. Freeman-Cook, Mark C. Noe
  • Patent number: 6908926
    Abstract: Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.
    Type: Grant
    Filed: April 12, 2000
    Date of Patent: June 21, 2005
    Assignee: Novo Nordisk A/S
    Inventors: Florencio Zaragoza Dörwald, Knud Erik Andersen, Tine Krogh Jørgensen, Bernd Peschke, Birgitte Schjellerup Wulff, Ingrid Pettersson, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Müller, Bernd Krist
  • Patent number: 6900201
    Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: May 31, 2005
    Assignee: Pfizer Inc.
    Inventors: Mark C. Noe, Kevin Freeman-Cook
  • Patent number: 6887867
    Abstract: Substituted benzodiazepine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compounds are generally 7- or 8-mono substituted 5H-2,3-benzodiazepines. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: May 3, 2005
    Assignee: Transgenomic, Inc.
    Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
  • Patent number: 6867204
    Abstract: Compounds of the formula: or pharmaceutically acceptable salts or prodrugs thereof, where each of n and p independently is 2 or 3, Y is —SO2— or —SO2—N(R10)—, Z1 is CH or N, and R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. The compounds have selective 5-HT6 affinity and are useful in the treatment of certain CNS disorders. Also provided are compositions comprising, methods for using, and methods for preparing Compounds of Formula I.
    Type: Grant
    Filed: May 9, 2003
    Date of Patent: March 15, 2005
    Assignee: Roche Palo Alto LLC
    Inventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
  • Patent number: 6858599
    Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.
    Type: Grant
    Filed: December 27, 2001
    Date of Patent: February 22, 2005
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
  • Publication number: 20040266752
    Abstract: The invention is directed to nonpeptide substituted benzazepines of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension, among others disclosed. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Application
    Filed: June 16, 2004
    Publication date: December 30, 2004
    Inventors: Mona Patel, Philip J. Rybczynski, Min Amy Xiang
  • Publication number: 20040266753
    Abstract: A compound selected from those of formula (I): 1
    Type: Application
    Filed: June 18, 2004
    Publication date: December 30, 2004
    Inventors: Michel Koch, Francois Tillequin, Sylvie Michel, John Hickman, Alain Pierre, Stephane Leonce, Bruno Pfeiffer, Pierre Renard
  • Publication number: 20040259857
    Abstract: Novel spirobenzoazepine compounds, novel processes for the preparation of nonpeptide substituted spirobenzoazepine derivatives, and novel processes for the preparation of intermediates in the preparation of such derivatives. Novel intermediates in the preparation of nonpeptide substituted spirobenzoazepine derivatives.
    Type: Application
    Filed: June 16, 2004
    Publication date: December 23, 2004
    Inventors: Xiaohu Deng, Birdella Kenney, Jimmy T. Liang, Neelakandha Mani, Frank J. Villani, Fan Zhang-Plasket, Hua Zhong
  • Patent number: 6812358
    Abstract: A novel process for making estra-4,9(10)-diene-3,17-dione steroids from readily available 19-nor-androst-4-ene-3-one steroids by a straightforward three-step process. Products of this process are important intermediates in the preparation of biologically active substances.
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: November 2, 2004
    Assignee: Bridge Organics Co.
    Inventors: Verlan H. Van Rheenen, Edward J. Hessler
  • Patent number: 6797819
    Abstract: The present invention provides novel alkaloid compounds and collections of these compounds, and provides methods for the synthesis of these compounds using biomimetic synthetic strategies. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as bacterial infections, proliferative diseases, and reproductive disorders, to name a few.
    Type: Grant
    Filed: May 22, 2001
    Date of Patent: September 28, 2004
    Assignees: President and Fellows of Harvard College, CBR Institute for Biomedical Research, Inc.
    Inventors: Matthew Shair, Nicholas Westwood, Henry Efrem Pelish
  • Publication number: 20040167331
    Abstract: The present invention provides compounds with activity as inhibitors of acyl glucosaminylinositol amidases with amidase activity against S-conjugate amides, particularly mycothiol-derived S-conjugate amides. Certain of the invention compounds are naturally occurring compounds obtained from marine sponges and other organisms. The invention further provides methods for using the compounds to inhibit virulence and reduce antibiotic resistance of mycothiol-producing bacteria.
    Type: Application
    Filed: March 15, 2004
    Publication date: August 26, 2004
    Inventors: Robert C Fahey, Gerald L Newton, Carole A Bewley, Gillian Nicholas
  • Patent number: 6762177
    Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.
    Type: Grant
    Filed: November 5, 2002
    Date of Patent: July 13, 2004
    Assignee: Sepracor, Inc.
    Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
  • Publication number: 20040087574
    Abstract: Disclosed are novel spiro derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases.
    Type: Application
    Filed: March 25, 2003
    Publication date: May 6, 2004
    Inventors: Toshiya Takahashi, Takeshi Ishigaki, Miyuki Funahashi, Koji Taniguchi, Masayuki Kaneko, Mie Kainoh, Hiroyuki Meguro
  • Patent number: 6706878
    Abstract: A compound of formula wherein n, m, p, X, Y, W, A, G and D are as defined in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
    Type: Grant
    Filed: March 24, 2003
    Date of Patent: March 16, 2004
    Assignee: Astrazeneca AB
    Inventors: Eifion Phillips, Robert Mack, John Macor, Simon Semus
  • Patent number: 6703502
    Abstract: A compound of formula wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2; A is N or C(R2); G is N or C(R3); D is N or C(R4); with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO; R1 is hydrogen or C1 to C4 alkyl; R2, R3, and R4 are independently hydrogen, halogen, C1, C4 alkyl, C2, C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1, C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3 or R2 and R3, or R3 and R4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3; R5 and
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: March 9, 2004
    Assignee: AstraZeneca AB
    Inventors: Eifion Phillips, Robert Mack, John Macor, Simon Semus
  • Patent number: 6693101
    Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: February 17, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
  • Publication number: 20040010141
    Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1
    Type: Application
    Filed: April 25, 2003
    Publication date: January 15, 2004
    Applicant: Pfizer Inc.
    Inventors: Mark C. Noe, Kevin Freeman-Cook
  • Patent number: 6677332
    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: Grant
    Filed: May 25, 2000
    Date of Patent: January 13, 2004
    Assignee: Sepracor, Inc.
    Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
  • Publication number: 20030225057
    Abstract: The present invention relates to novel compounds of Formula (I): 1
    Type: Application
    Filed: April 10, 2003
    Publication date: December 4, 2003
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Jeffrey Smith, Brian Smith
  • Publication number: 20030225056
    Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1
    Type: Application
    Filed: April 25, 2003
    Publication date: December 4, 2003
    Applicant: Pfizer Inc.
    Inventors: Kevin D. Freeman-Cook, Mark C. Noe
  • Patent number: 6638925
    Abstract: New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) and new compounds of the general formula (III) Drugs, containing compounds of formulas (I) and/or (III), which can be used successfully for the treatment of Alzheimer's disease and related dementia conditions, as well as for the treatment of Langdon-Down syndrome, are also described.
    Type: Grant
    Filed: February 11, 1999
    Date of Patent: October 28, 2003
    Assignee: Sanochemia Ltd.
    Inventors: Laszlo Czollner, Johannes Frohlich, Ulrich Jordis, Bernhard Kuenburg
  • Patent number: 6627634
    Abstract: Bicyclic heterocycles of general formula wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: September 30, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Publication number: 20030171355
    Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.
    Type: Application
    Filed: November 5, 2002
    Publication date: September 11, 2003
    Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
  • Patent number: 6579869
    Abstract: The present invention concerns a compound of formula (I) wherein: W represents O or NH, Q represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarbon radical containing 1 to 30 carbon atoms including or not heteroatom(s), R1 is H, OH, or OMe, O-(C1-C30)-alkyl, O-aryl-(C1-C30)-alkyl, O-(C2-C30)-alkenyl, O-(C3-C30)-cycloalkyl or null, and R2 is H or OH, or R1 and R2 form together —O—, R3=R4=OMe or R3 and R4 form together —OCH2O—, R is H, C1-C30 alkyl or O-protecting group and R6 represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarbon radical containing 1 to 30 carbon atoms including or not heteroatom(s), or R and R6 form together —CMe2—, n is 0 to 8, R5 is H, OH, OMe, O-(C1-C30)-alkyl, O-aryl-(C1-C30)-alkyl, O-(C2-C30)-alkenyl, O-(C3-C30)-cycloalkyl or O-aryl, the dotted line is null or forms a double bond dep
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: June 17, 2003
    Assignee: Oncopharm Corporation
    Inventors: Jean-Pierre Robin, Robert Dhal, Freddy Drouye, Jean-Pierre Marie, Nina Radosevic, Julie Robin, Karine Souchaud, Patricia Bataille
  • Publication number: 20030096803
    Abstract: The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1
    Type: Application
    Filed: October 23, 2001
    Publication date: May 22, 2003
    Inventors: Mark C. Noe, Martin J. Wythes, Brian S. Bronk
  • Patent number: 6566357
    Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; two R2 units on the same carbon atom are taken together to form a spirocyclic ring having from 4 to 7 atoms, the balance of the R2 units are independently selected from the group consisting of: a) hydrogen; b) —O(CH2)jR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —CH2)jCON(R10)2; and g) two R2 units can be taken together to form a carbonyl unit; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 uni
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: May 20, 2003
    Assignee: The Procter & Gamble Co.
    Inventors: Matthew John Laufersweiler, Michael Philip Clark, Jane Far-Jine Djung, Adam Golebiowski, Todd Andrew Brugel, Biswanath De
  • Publication number: 20030087882
    Abstract: The present application describes novel spiro-cyclic &bgr;-amino acid derivatives of formula I: 1
    Type: Application
    Filed: March 12, 2002
    Publication date: May 8, 2003
    Inventors: Gregory R. Ott, Xiao Tao Chen, Jingwu Duan, Matthew E. Voss
  • Publication number: 20030064978
    Abstract: There are provided novel compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the Specification and optical isomers, racemates and tautomers thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme nitric oxide synthase.
    Type: Application
    Filed: August 9, 2002
    Publication date: April 3, 2003
    Inventors: Christopher Walpole, Hua Yang
  • Publication number: 20030045517
    Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I, 1
    Type: Application
    Filed: July 2, 2001
    Publication date: March 6, 2003
    Inventors: Robert H.K. Chen, Min A. Xiang
  • Patent number: 6512112
    Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.
    Type: Grant
    Filed: June 28, 2001
    Date of Patent: January 28, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Robert C. Gadwood, Bharat V. Kamdar
  • Patent number: 6509334
    Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, N02, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 a
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: January 21, 2003
    Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.
    Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Publication number: 20020198188
    Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
    Type: Application
    Filed: January 10, 2002
    Publication date: December 26, 2002
    Applicant: Children's Medical Center Corporation
    Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
  • Publication number: 20020183307
    Abstract: Compounds, pharmaceutical compositions, and methods for the treatment of a hyperlipidemic condition in a subject. The compounds of the present invention are apical sodium co-dependent bile acid transport inhibitors and are 1,4-benzothiazepine and 1,5-benzothiazepine compounds corresponding to Formula I: 1 wherein j, m, Y, Z, R1A, R1B, R2A, R2B and R6 are as defined in the specification.
    Type: Application
    Filed: July 25, 2001
    Publication date: December 5, 2002
    Inventors: Samuel J. Tremont, Kevin J. Koeller, William L. Neumann
  • Patent number: 6476019
    Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: November 5, 2002
    Assignee: Sepracor Inc.
    Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
  • Publication number: 20020160996
    Abstract: Compounds represented by the formula: 1
    Type: Application
    Filed: April 11, 2002
    Publication date: October 31, 2002
    Inventors: Shigenori Ohkawa, Yasuyoshi Arikawa, Kouki Kato, Masahiro Okura, Masaki Setoh
  • Patent number: 6444819
    Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: September 3, 2002
    Assignee: Neurogen Corporation
    Inventors: Renata Xavier Kover, Salva Terdjanian, Jennifer Tran, Andrew Thurkauf
  • Patent number: 6410526
    Abstract: The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, Robert S. Meissner, James J. Perkins
  • Patent number: 6407229
    Abstract: The invention relates to processes for the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine, or derivatives thereof. Furthermore, the invention also relates to the compounds formed during the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: June 18, 2002
    Assignee: Sanochemia Pharmazeutika AG
    Inventors: Laszlo Czollner, Johannes Fröhlich, Ulrich Jordis, Bernhard Küenburg
  • Patent number: 6399598
    Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptacle salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: June 4, 2002
    Assignee: The Procter & Gamble Company
    Inventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
  • Patent number: 6392038
    Abstract: A process for the preparation of substantially single enantiomer (−)-narwedine comprises seeding a solution of racemic narwedine dissolved in a solvent with substantially single enantiomer (−)-narwedine, provided that if an added amine base is present the ratic solvent:added amine base is greater than 15:1.
    Type: Grant
    Filed: January 10, 2000
    Date of Patent: May 21, 2002
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Gerard Andrew Potter, Peter David Tiffin
  • Patent number: 6387893
    Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
  • Publication number: 20020019540
    Abstract: Novel substituted amino acids of formula 1
    Type: Application
    Filed: August 8, 2001
    Publication date: February 14, 2002
    Inventors: Justin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
  • Patent number: 6340753
    Abstract: A novel optically active quarternary ammonium salt with an axial chirality is provided. The quarternary ammonium salt can act as a phase-transfer catalyst to convert glycine derivatives into optically active &agr;-amino acid derivatives by stereoselectively alkylating the glycine derivatives. Furthermore, according to the present invention, intermediates useful for producing the novel quarternary ammonium can be produced.
    Type: Grant
    Filed: July 13, 2000
    Date of Patent: January 22, 2002
    Assignee: Nagase & Co., Ltd.
    Inventor: Keiji Maruoka
  • Patent number: 6316437
    Abstract: Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: November 13, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Jacob M. Hoffman
  • Patent number: 6288059
    Abstract: A compound of formula (I), a pharmaceutically acceptable salt or ester or other derivative thereof: R1 is optionally substituted cycloalkyl or optionally substituted saturated heterocyclic group. R2 is optionally substituted aryl or optionally substituted heteroaryl. A is methylene, carbonyl or sulfonyl. B is a single bond, alkylene or alkenylene. D is oxygen or sulfur. G is alkylene or alkenylene. L is —N(R3)— or —C(R4)(R5)—. R3 is optionally substituted aryl or optionally substituted heteroaryl. R4 is H, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl or optionally substituted saturated heterocyclic group. R5 is alkyl optionally substituted with amino, amino, optionally substituted acylamino, OH, optionally substituted hydroxyalkyl, alkoxy or —CO—R6. R6 is alkyl, alkoxy or amine residue. R4 together with R5 forms a cycloalkane ring, cycloalkene ring, or saturated heterocyclic ring. R7 is alkyl.
    Type: Grant
    Filed: June 5, 2000
    Date of Patent: September 11, 2001
    Assignee: Sankyo Company, Limited
    Inventors: Takahide Nishi, Takeshi Yamaguchi
  • Patent number: 6251890
    Abstract: The present invention relates to carbapenem antibacterial agents of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 represents: in formula I, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: June 26, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Timothy A. Blizzard, Ronald W. Ratcliffe, Jerry D. Morgan, II, Robert R. Wilkening
  • Patent number: 6207668
    Abstract: The present invention relates to novel substituted pyridines/pyrimidines of the formula I where A is CH or N; X is NH, oxygen or S(O)q where q is 0, 1 or 2; Y is a direct bond or CH2; Z is oxygen, NR7 or S(O)m is 0, 1 or 2, and the radicals R1, R2, R3, R4, R5, R6 and R7 are as defined in the description, to processes for their preparation, and to their use as pesticides, fungicides, ovicides or as veterinary medicaments.
    Type: Grant
    Filed: April 1, 1997
    Date of Patent: March 27, 2001
    Assignee: Hoechst Schering
    Inventors: Ralf Braun, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin
  • Patent number: 6174940
    Abstract: The present invention relates to mixtures comprising the compound I in a proportion of 65-95% by weight, the compound II in a proportion of 5-35% by weight and the compound III in a proportion of 0-10% by weight wherein the substituents are as defined in the description, and to mixtures with other compounds. The mixtures are suitable for stabilizing organic material against the effect of light and heat.
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: January 16, 2001
    Assignee: Clariant GmbH
    Inventors: Thomas St{umlaut over (a)}hrfeldt, Mathias Mehrer, Matthias Z{umlaut over (a)}h, Gerhard Pfahler
  • Patent number: 6156747
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or trihalomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: December 5, 2000
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jose Ignacio Andres-Gil, Pedro Martinez-Jimenez, Francisco Javier Fernandez-Gadea, Victor Karel Sipido