Patents Examined by John M. Ford
  • Patent number: 7026317
    Abstract: The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: April 11, 2006
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Paul J. Gilligan, Richard G. Wilde
  • Patent number: 6894043
    Abstract: Compound selected from those of formula (I): wherein: X represents flourine, bromine, iodine or methyl, each of R1 and R2, which may be identical or different, represents hydrogen or alkyl, its isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid Medicinal products containing the same which are useful as AMPA modulators.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: May 17, 2005
    Assignee: Les Laboratoires Servier
    Inventors: Bernard Pirotte, Pascal De Tullio, Stéphane Boverie, Isabelle Kempen, Pierre Lestage
  • Patent number: 6894044
    Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: May 17, 2005
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, George D. Maynard, Alan Hutchison
  • Patent number: 6894049
    Abstract: The present invention relates to platinum antitumor drugs. In particular, it relates to platinum complexes having formula Ia or Ib or a pharmaceutically acceptable salt thereof wherein: each A is independently an anion; each B is independently halo, hydroxy, carboxylate, carbamate or a carbonate ester, Z is a substituted 5- or 6-membered, heterocyclic moiety wherein at least one substituent sterically hinders access of the Pt atom to a DNA strand of a tumor cell, and wherein Z is other than pyridine; and X is NH3 or mono- or dialkyl substituted NH3. which are active against cancer cells and have improved aqueous solubility and activity.
    Type: Grant
    Filed: October 4, 2000
    Date of Patent: May 17, 2005
    Assignee: AnorMED, Inc.
    Inventors: Ernest S. Y. Wong, Christen M. Giandomenico
  • Patent number: 6878824
    Abstract: The present invention provides a process for preparing N-methylated melamines in simple steps by using inexpensive raw materials in such a manner that the proportion of mono-type, bis-type and tris-type of the N-methylated melamines as prepared can be controlled. The process comprises reacting by heating melamine with methylamine in the presence of an acidic catalyst under pressure to substitute at least one amino group of the melamine by methylamino group.
    Type: Grant
    Filed: March 19, 2003
    Date of Patent: April 12, 2005
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Isao Hashiba, Takayuki Tamura, Hiroyuki Kousaka
  • Patent number: 6878707
    Abstract: Compounds of formula (I) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmaceutically acceptable salts thereof; and enanti
    Type: Grant
    Filed: January 16, 2001
    Date of Patent: April 12, 2005
    Assignee: Novartis AG
    Inventor: Gary Michael Ksander
  • Patent number: 6867217
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: March 15, 2005
    Assignee: Pharmacia Corporation
    Inventors: Michael S. South, Qingping Zeng, Ashton T. Hamme, II, Melvin L. Rueppel
  • Patent number: 6858609
    Abstract: This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H7)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; for the manufacture of a medicine for the treatment o
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: February 22, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Paul A. J. Janssen, Jan Heeres, Henri E. L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
  • Patent number: 6844437
    Abstract: The invention concerns a process for the manufacture of tert-butyl (E)-(6-[2-4-(4-flourophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl)-(4R,6S)-2,2-dimethyl[1,3]-dioxan-4-yl)acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.
    Type: Grant
    Filed: February 15, 2000
    Date of Patent: January 18, 2005
    Assignees: Astrazeneca AB, Shionogi & Co. Ltd.
    Inventors: Nigel P Taylor, Loius J Diorazio, Haruo Koike, Mikio Kabaki
  • Patent number: 6818763
    Abstract: A method of preparing metal mesoporphyrin halide compounds is described. The metal mesoporphyrin halide compound may be formed by forming a novel mesoporphyrin IX intermediate compound and then converting the mesoporphyrin IX intermediate to the metal mesoporphyrin halide through metal insertion. The novel intermediate compound may be formed by a catalytic hydrogenation of hemin in acid and subsequent recovery.
    Type: Grant
    Filed: June 3, 2003
    Date of Patent: November 16, 2004
    Assignee: Wellspring Pharmaceutical Corporation
    Inventors: Robert A. Vukovich, Benjamin Levinson, George S. Drummond, Robert Caroselli, Kazimierz G. Antczak, Christopher Boucher, Richard Mortimer
  • Patent number: 6806267
    Abstract: The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these compounds and to their use as anti-tumour agents.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: October 19, 2004
    Assignees: The Universita'di Siena, The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth Near Dublin
    Inventors: David Clive Williams, Daniela M. Zisterer, Vito Nacci, Giuseppe Campiani
  • Patent number: 6767907
    Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at c
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: July 27, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
  • Patent number: 6765006
    Abstract: The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.
    Type: Grant
    Filed: August 16, 2002
    Date of Patent: July 20, 2004
    Assignee: Euro-Celtique S.A.
    Inventors: Ravi Upasani, Sui X. Cai
  • Patent number: 6762188
    Abstract: Compounds of formula (I) or salts thereof, wherein the dotted Line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —CH═CH— or N═N—, are disclosed as pharmacologic
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: July 13, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
  • Patent number: 6756380
    Abstract: Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon rin
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: June 29, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Patent number: 6753428
    Abstract: Racemates are obtained from one of the enantiomers, or an enantiomerically enriched mixture, of an optically active quinazolinone derivative by reaction of the compound with an alkali alkoxide of a primary alcohol and isolation of the racemate.
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: June 22, 2004
    Assignee: Cytokinetics, Inc.
    Inventors: Gustave Bergnes, Bing Yao, David Morgans, Jr., Whitney W. Smith
  • Patent number: 6750214
    Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 4, 2003
    Date of Patent: June 15, 2004
    Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
  • Patent number: 6750342
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: June 15, 2004
    Assignee: Pharmacia Corporation
    Inventors: Michael South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones, Melvin L. Rueppel
  • Patent number: 6743808
    Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7-membered ring; R8 is hydrogen or alkyl; h
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: June 1, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
  • Patent number: 6743817
    Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: June 1, 2004
    Assignee: Neurogen Corporation
    Inventors: George Maynard, LingHong Xie, Stanislaw Rachwal