Patents Examined by Hong Liu
  • Patent number: 7101878
    Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
    Type: Grant
    Filed: August 20, 1999
    Date of Patent: September 5, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Mark Brian Anderson, Haresh N. Vazir, David Robert Luthin, Genevieve DeGuzman Paderes, Ved P. Pathak, Lance Christopher Christie, Yufeng Hong, Eileen Valenzuela Tompkins, Haitao Li, James Faust
  • Patent number: 6943159
    Abstract: The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C?O of CH2; Y represents —CH(R4)—, —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.
    Type: Grant
    Filed: August 18, 2000
    Date of Patent: September 13, 2005
    Assignee: Neurosearch A/S
    Inventors: Alex Haahr Gouliaev, Mogens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Jørgen Scheel-Krüger, Gunnar M. Olsen, Elsebet Østergaard Nielsen
  • Patent number: 6916804
    Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl m
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: July 12, 2005
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
  • Patent number: 6911447
    Abstract: Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: June 28, 2005
    Assignee: The Procter & Gamble Company
    Inventors: Wieslaw Adam Mazur, Xinrong Tian, Xiufeng Eric Hu, Frank Hallock Ebetino
  • Patent number: 6908919
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone 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: July 15, 2002
    Date of Patent: June 21, 2005
    Assignee: Pharmacia Corporation
    Inventors: Michael S. South, Brenda L. Case, Thomas A. Dice, Ricky L. Fenton, Gary W. Franklin, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, Carrie L. Kusturin, Richard J. Lindmark, Scott A. Long, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Matthew W. Mahoney, John J. Parlow, Melvin L. Rueppel
  • Patent number: 6903096
    Abstract: The invention is directed to methods to inhibit TGF-? and/or p38-? kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar? is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: June 7, 2005
    Assignee: Scios, Inc.
    Inventors: Sarvajit Chakravarty, Sundeep Dugar, John J. Perumattam, George F. Schreiner, David Y. Liu, John A. Lewicki
  • Patent number: 6903110
    Abstract: Compounds of the formula useful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: June 7, 2005
    Assignee: Wyeth
    Inventors: Rulin Zhao, Megan Tran, Gary P. Stack, Richard E. Mewshaw
  • Patent number: 6897214
    Abstract: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: May 24, 2005
    Assignee: Zeneca Limited
    Inventors: Andrew John Barker, Craig Johnstone
  • Patent number: 6897313
    Abstract: The invention relates to a novel, industrial synthesis of 2-ethyl-3-methyl-1,4-diazine.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: May 24, 2005
    Assignee: Symrise GmbH & Co. KG
    Inventor: Stefan Lambrecht
  • Patent number: 6894050
    Abstract: Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein
    Type: Grant
    Filed: June 5, 2002
    Date of Patent: May 17, 2005
    Assignee: Pfizer Inc.
    Inventors: Phoebe Chiang, William A. Novomisle, Willard M. Welch, Jr., Angel Guzman-Perez, Paul A. DaSilva-Jardine, Ravi S. Garigipati, Kevin K. Liu
  • 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: 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: 6852721
    Abstract: The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridinyl diazabicyclic compounds, such as (1S,4S)-2-(5-(3-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. Other exemplary compounds of the present invention include (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(3-thienyl)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(4-fluorophenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, and (1S,4S)-2-(5-benzoyl-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: February 8, 2005
    Assignee: Targacept, Inc.
    Inventors: Craig Harrison Miller, Gary Maurice Dull, Lan Miao, Dwo Lynm, Jeffrey Daniel Schmitt, Thomas Jeffrey Clark
  • Patent number: 6852725
    Abstract: The present invention is directed to imidazolyl derivatives of the formula: where the substituents are defined in the specification, or a pharmaceutically acceptable salt thereof. The derivatives bind selectively to the somatostatin subtype receptors and elicit either an agonist or antagonist effect from the somatostatin subtype receptors.
    Type: Grant
    Filed: June 8, 1999
    Date of Patent: February 8, 2005
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S. A. S.
    Inventors: Christophe Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Christophe Philippe Moinet, Thomas D. Gordon, Barry A. Morgan
  • Patent number: 6841552
    Abstract: Compounds of the formula: are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system.
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: January 11, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Scott Dax, James McNally
  • Patent number: 6831080
    Abstract: There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken t
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: December 14, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
  • Patent number: 6828341
    Abstract: Described are cyclohexylamine derivatives of Formula I and pharmaceutically acceptable salts thereof, wherein R1, g, *, R, V, B, E, Y, G, H, X1, and d are as defined in the description. The compounds of Formulas I, VI, and VIa are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, trauma, hypoglycemia, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, chronic pain, or urinary incontinence.
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: December 7, 2004
    Assignee: Warner-Lambert Company
    Inventors: Russell Joseph DeOrazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer
  • Patent number: 6828323
    Abstract: Methods are provided for neutralization of microorganisms in fluids or on surfaces. Preferably the fluids contain blood or blood products and comprise biologically active proteins. Preferred methods include the steps of adding an activation-effective amount of a microorganism neutralizer with an isoalloxazine backbone to a fluid and exposing the fluid to a triggering event. Preferred triggering events include light of a suitable wavelength and intensity to activate the microorganism neutralizer or a pH sufficient to activate the microorganism neutralizer. Other fluids, including juices, water and the like, may also be decontaminated by these methods as may surfaces of foods, animal carcasses, wounds, food preparation surfaces and bathing and washing vessel surfaces. Compounds with an isoalloxazine backbone are also provided.
    Type: Grant
    Filed: February 5, 2001
    Date of Patent: December 7, 2004
    Assignee: Gambro, Inc.
    Inventors: Matthew Stewart Platz, Raymond Paul Goodrich, Jr.
  • Patent number: 6825198
    Abstract: Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein.
    Type: Grant
    Filed: May 28, 2002
    Date of Patent: November 30, 2004
    Assignee: Pfizer Inc
    Inventors: Phoebe Chiang, William A. Novomisle, Willard M. Welch, Jr.