Patents Examined by Hong Liu
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Patent number: 7101878Abstract: 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: GrantFiled: August 20, 1999Date of Patent: September 5, 2006Assignee: 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
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Patent number: 6943159Abstract: 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: GrantFiled: August 18, 2000Date of Patent: September 13, 2005Assignee: Neurosearch A/SInventors: Alex Haahr Gouliaev, Mogens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Jørgen Scheel-Krüger, Gunnar M. Olsen, Elsebet Østergaard Nielsen
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Patent number: 6916804Abstract: 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 mType: GrantFiled: December 20, 2002Date of Patent: July 12, 2005Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
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Patent number: 6911447Abstract: 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: GrantFiled: April 12, 2002Date of Patent: June 28, 2005Assignee: The Procter & Gamble CompanyInventors: Wieslaw Adam Mazur, Xinrong Tian, Xiufeng Eric Hu, Frank Hallock Ebetino
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Patent number: 6908919Abstract: 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: GrantFiled: July 15, 2002Date of Patent: June 21, 2005Assignee: Pharmacia CorporationInventors: 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
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Patent number: 6903110Abstract: 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: GrantFiled: July 24, 2002Date of Patent: June 7, 2005Assignee: WyethInventors: Rulin Zhao, Megan Tran, Gary P. Stack, Richard E. Mewshaw
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Patent number: 6903096Abstract: 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: GrantFiled: October 5, 2001Date of Patent: June 7, 2005Assignee: Scios, Inc.Inventors: Sarvajit Chakravarty, Sundeep Dugar, John J. Perumattam, George F. Schreiner, David Y. Liu, John A. Lewicki
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Patent number: 6897313Abstract: The invention relates to a novel, industrial synthesis of 2-ethyl-3-methyl-1,4-diazine.Type: GrantFiled: April 26, 2001Date of Patent: May 24, 2005Assignee: Symrise GmbH & Co. KGInventor: Stefan Lambrecht
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Patent number: 6897214Abstract: 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: GrantFiled: May 2, 2002Date of Patent: May 24, 2005Assignee: Zeneca LimitedInventors: Andrew John Barker, Craig Johnstone
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Patent number: 6894050Abstract: 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 hereinType: GrantFiled: June 5, 2002Date of Patent: May 17, 2005Assignee: 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
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Patent number: 6894049Abstract: 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: GrantFiled: October 4, 2000Date of Patent: May 17, 2005Assignee: AnorMED, Inc.Inventors: Ernest S. Y. Wong, Christen M. Giandomenico
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Patent number: 6894044Abstract: 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: GrantFiled: April 3, 2002Date of Patent: May 17, 2005Assignee: Neurogen CorporationInventors: Jun Yuan, George D. Maynard, Alan Hutchison
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Patent number: 6878707Abstract: 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 enantiType: GrantFiled: January 16, 2001Date of Patent: April 12, 2005Assignee: Novartis AGInventor: Gary Michael Ksander
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Patent number: 6852721Abstract: 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: GrantFiled: May 24, 2001Date of Patent: February 8, 2005Assignee: Targacept, Inc.Inventors: Craig Harrison Miller, Gary Maurice Dull, Lan Miao, Dwo Lynm, Jeffrey Daniel Schmitt, Thomas Jeffrey Clark
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Patent number: 6852725Abstract: 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: GrantFiled: June 8, 1999Date of Patent: February 8, 2005Assignee: 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
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Patent number: 6841552Abstract: 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: GrantFiled: April 20, 2000Date of Patent: January 11, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Scott Dax, James McNally
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Patent number: 6831080Abstract: 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 tType: GrantFiled: May 31, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventors: 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
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Patent number: 6828323Abstract: 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: GrantFiled: February 5, 2001Date of Patent: December 7, 2004Assignee: Gambro, Inc.Inventors: Matthew Stewart Platz, Raymond Paul Goodrich, Jr.
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Patent number: 6828341Abstract: 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: GrantFiled: March 27, 2002Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph DeOrazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer
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Patent number: 6825188Abstract: Compounds having a benzodiazepinyl core structure are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis, angiogenesis, tumor growth and metastasis, atherosclerosis, restenosis and inflammation.Type: GrantFiled: October 22, 2003Date of Patent: November 30, 2004Assignee: SmithKline Beecham CorporationInventors: James Francis Callahan, Russell Donovan Cousins, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Irene Nijole Uzinskas