Patents Examined by N. Wright
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Patent number: 6426357Abstract: The present invention provides a compound of the formula: and methods for using the same, wherein R1, R2, R3, R4 and X are those defined herein.Type: GrantFiled: July 31, 2000Date of Patent: July 30, 2002Assignee: Affymax, Inc.Inventors: Randall A. Scheuerman, Stephen D. Yanofsky, Christopher P. Holmes, Derek MacLean, Beatrice Ruhland, Ronald W. Barrett, Jay E. Wrobel, Ariamala Gopalsamy
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Patent number: 6417369Abstract: Copper pyrazolate precursor compositions useful for the formation of copper in semiconductor integrated circuits, e.g., interconnect metallization in semiconductor device structures, as an adhesive seed layer for plating, for the deposition of a thin-film recording head and for circuitization of packaging components. The copper pyrazolate precursor compositions include fluorinated and non-fluorinated pyrazolate copper (I) complexes and their Lewis base adducts. Such precursors are usefully employed for liquid delivery chemical vapor deposition of copper or copper-containing material on a substrate.Type: GrantFiled: March 13, 2000Date of Patent: July 9, 2002Assignee: Advanced Technology Materials, Inc.Inventors: Chongying Xu, Thomas H. Baum, Ziyun Wang
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Patent number: 6399631Abstract: Carbazoles of the formula which are effective in treating conditions associated with neuropeptide Y-5 neurotransmission.Type: GrantFiled: July 21, 2000Date of Patent: June 4, 2002Assignee: Pfizer Inc.Inventors: Richard L. Elliott, David A. Griffith, Marlys Hammond
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Patent number: 6399771Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, 2 and 3, to a plurality of processes for their preparation and to their use as pesticides.Type: GrantFiled: September 9, 2000Date of Patent: June 4, 2002Assignee: Bayer AktiengesellschaftInventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
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Patent number: 6380191Abstract: Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.Type: GrantFiled: June 16, 2000Date of Patent: April 30, 2002Assignee: Merck & Co. Inc.Inventors: Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
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Patent number: 6372742Abstract: 5-(3-Isatinylidinyl)thiazolidineones and 3-(thiazolidinon-5-yl)indoles compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are novel methods for assaying or screening for inhibitors of telomerase activity.Type: GrantFiled: June 30, 2000Date of Patent: April 16, 2002Assignee: Geron CorporationInventors: Allison C. Chin, Richard L. Tolman, Mark Q. Nguyen, Ryan Holcomb
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Patent number: 6372913Abstract: 2-substituted 5-formylthiazoles are prepared in an advantageous manner by reacting halogenomalonaldehydes in the presence of a solvent and a C1-compound of the formula (III) in which X represents oxygen or sulfur and R1 is as defined in the description, the reaction mixture comprising less than 5% by weight of water.Type: GrantFiled: August 17, 1998Date of Patent: April 16, 2002Assignee: Bayer AGInventor: Helmut Kraus
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Patent number: 6369241Abstract: The present invention relates to methods for preparing 2,2-dimethyl-5-acyloxy-10-propyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-8-one (5) and 2,2-dimethyl-5-hydroxy-10-propyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-8-one (6) and their use as intermediates for the synthesis of antiviral calanolide compounds. For example, Fries rearrangement on compound 5 or Friedel-Crafts reaction on 6, yields intermediate 2,2-dimethyl-5-hydroxy-6-propionyl-10-propyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-8-one (4), which, in turn, can be converted to (+)-calanolide A and (−)-calanolide B. The coupling of compound 6 with the appropriate chiral molecule under Mitsunobu or nucleophilic displacement leads to the asymmetric synthesis of antiviral calanolide compounds.Type: GrantFiled: April 25, 2000Date of Patent: April 9, 2002Assignee: Sarawak Medichem Pharmaceuticals, Inc.Inventors: Ze-Qi Xu, Hongwei Yuan, Jennifer Crabb, Raghu Samy, Ailing Li, Hua Cao
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Patent number: 6355648Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1 and R2 are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl; 1-propynyl; or 3-propynyl; or R1 and R2 are joined to form an alkyl, alkenyl or heterocyclic ring; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, substituted alkynyl, or CORA; RA is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NH2, NO2, C1 to C6 alkyl, or substituted C1 to C6 alkyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; R5 is optionally substituted and selected from a benzene riType: GrantFiled: April 19, 2000Date of Patent: March 12, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6350747Abstract: The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.Type: GrantFiled: February 28, 2000Date of Patent: February 26, 2002Assignee: Glaxo Wellcome Inc.Inventors: Kimberley Caroline Glennon, Lee Frederick Kuyper, Karen Elizabeth Lackey, Robert Walton Mcnutt, Jr.
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Patent number: 6348601Abstract: N-Methyl-2-pyrrolidone (NMP) is prepared by preparing a mixture comprising monomethylamine, dimethylamine and trimethylamine and ammonia in a first process step by reacting ammonia with methanol at elevated temperature in the presence of a catalyst, separating 10 off the ammonia, reacting the mixture comprising the methylamines with gamma-butyrolactone (&ggr;-BL), in a molar ratio of monomethylamine to &ggr;-BL of at least 1 in a second process step at elevated temperature and superatmospheric pressure, separating NMP and unreacted methylamines from the reaction product and returning unreacted methylamines to the first process step for reaction with methanol and ammonia.Type: GrantFiled: February 1, 2001Date of Patent: February 19, 2002Assignee: BASF AktiengesellschaftInventors: Frank Ohlbach, Johann-Peter Melder, Karl-Heinz Ross, Martin Rudloff, Jörg Liebe
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Patent number: 6344563Abstract: process is described for preparing a compound of Formula (1.3.0): comprising: establishing a reaction mixture consisting of in an aprotic solvent; in the presence of a strong base in solid form selected from the group consisting of sodium hydroxide, NaOH; and potassium hydroxide, KOH;—and optionally—in the presence of a catalytic amount of cesium carbonate, Cs2CO3, or of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt—followed by—heating said reaction mixture under a nitrogen atmosphere; whereby there is produced a compound of Formula (1.3.Type: GrantFiled: June 29, 2000Date of Patent: February 5, 2002Inventors: Timothy Norris, Megan E. Hnatow, John F. Lambert
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Patent number: 6339085Abstract: Pyridoxal analogues can be useful for treating B6 efficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula: or a pharmaceutically acceptable acid addition salt thereof, in which R1 is alkyl, alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy; alkoxy; dialkylamino; alkanoyloxy; alkanoyloxyaryl; alkoxyalkanoyl; alkoxycarbonyl; dialkylcarbamoyloxy; or aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nito, or alkanoyloxy. These analogues can be administered, either alone or concurrently with known medications, to treat the above-described diseases.Type: GrantFiled: March 7, 2000Date of Patent: January 15, 2002Assignees: The University of Manitoba, Medicore Inc.Inventor: Wasimul Haque
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Patent number: 6339094Abstract: This invention provides a series of substituted propanamines useful as tachykinin receptor antagonists. This invention also provides methods employing these substituted propanamines as well as pharmaceutical formulations comprising these compounds.Type: GrantFiled: January 27, 2000Date of Patent: January 15, 2002Assignee: Eli Lilly and CompanyInventors: James E Fritz, Philip A Hipskind, Stephen W Kaldor, Karen L Lobb, James A Nixon
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Patent number: 6337405Abstract: A process for preparing a compound represented by general formulae (5) and (6) in the following reaction scheme or salts thereof, wherein R1 represents a protective group for a nitrogen atom; R2 represents a methanesulfonyl group or p-toluenesulfonyl group; R3 represents a hydrogen atom, an aralkyl group, or an alkyl group having 1 to 6 carbon atoms; and X represents a halogen atom. Reaction Scheme: The above process is useful as an industrial process for preparing intermediates of anticoagulant aromatic amidine derivatives described in Japanese Patent Application Laid-Open (kokai) No. 208946/1993.Type: GrantFiled: December 22, 2000Date of Patent: January 8, 2002Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Yukio Yokoyama, Tatsuya Kobayashi, Takeo Koyama
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Patent number: 6320050Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: March 15, 2000Date of Patent: November 20, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Ramakanth Sarabu
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Patent number: 6316616Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.Type: GrantFiled: April 22, 1998Date of Patent: November 13, 2001Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Matthew S. Sigman
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Patent number: 6313315Abstract: There is disclosed a method for producing an essentially enantiomerically pure N-protected-azetidine-2-carboxylic acid of formula (1): which method is characterized by: subjecting a crude enantiomerically excess N-protected-azetidine-2-carboxylic acid comprising said enantiomer represented by formula (1) in excess to the other enantiomer thereof to crystallization in an organic solvent selected from aromatic hydrocarbon, aliphatic ether, aliphatic alcohol, aliphatic ketone, aliphatic nitrile, aliphatic amide, aliphatic sulfoxide, aliphatic ester and a mixed solvent thereof, wherein R is: an optionally substituted alkyl, alicyclic or alicyclicalkyl group, an optionally substituted alkenyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, or a dialkylamino group, and absolute configuration of the asterisked asymmetric carbon atom is S or R.Type: GrantFiled: June 1, 2000Date of Patent: November 6, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Kazuhiro Yamauchi, Hideki Ushio, Isao Kurimoto
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Patent number: 6313175Abstract: Novel meta substituted arylalkylamine compounds are disclosed. These compounds can be administered as small molecule drugs to treat diseases or conditions associated with insufficient serotonin mediated nerve transmission (e.g., depression and obesity).Type: GrantFiled: August 13, 1999Date of Patent: November 6, 2001Assignee: Biostream, Inc.Inventors: David R. Elmaleh, Alan J. Fischman
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Patent number: 6310216Abstract: 6-Amino-3-azabicyclo[3.1.0]hexanes of the formula wherein R1 and R2 independently of one another are C3-C4-alkenyl or Ar—CH(R′)— where R′ is hydrogen or C1-C4-alkyl and Ar is an optionally substituted C6-C10-aryl and R3 is hydrogen, C3-C4-alkenyl, Ar—CH(R′)— where R′ is hydrogen or C1-C4-alkyl and Ar is an optionally substituted C6-C10-aryl or COOR4 where R4 is C1-C4-alkyl or C2-C4-alkenyl. The invention also relates to a method for making these compounds and a method for using them.Type: GrantFiled: February 18, 2000Date of Patent: October 30, 2001Assignee: Bayer AktiengesellschaftInventors: Elmar Vilsmaier, Torsten Goerz, Gunther Milch, Uwe Petersen, Axel Dalhoff, Gabriele Schmuck