Patents Examined by C. S. Aulakh
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Patent number: 6713507Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: GrantFiled: October 11, 2001Date of Patent: March 30, 2004Assignee: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6710042Abstract: Compounds of formula (I) are useful as human NK3 receptor antagonists.Type: GrantFiled: September 18, 2001Date of Patent: March 23, 2004Assignee: Sanofi-SynthelaboInventors: Daniel Bichon, Xavier Edmonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 6689888Abstract: The present invention provides processes useful in the preparation of certain &bgr;3-adrenergic receptor agonists of the structural formula the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.Type: GrantFiled: February 20, 2003Date of Patent: February 10, 2004Assignee: Pfizer Inc.Inventors: Robert J. Chambers, Robert W. Dugger, Ming Kang, Yong Tao, John W. Wong
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Patent number: 6686373Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein the dashed lines represent optional double bonds; C1, C2, C3 and C4 are carbon atom; R1 is C1-4 alkyl; R2 is H, amino, etc.; R3 is H, halo-CH2—, C2-8 alkyl or Q1-, wherein said C2-8 alkyl is optionally substituted with up to 3 substituents selected from halo, C1-3 alkyl, R4(R5)N, etc.; R4 is H, C1-7 alkyl, etc.; R5 is H, C1-7alkyl, etc.; R6 and R7 are independently selected from H and C1-4 alkyl; R8 is aryl or heteroaryl; Q1 is a 4-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 4 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4 alkyl, etc.; Y5, Y6, Y7 and Y8 are hydrogen; Y1, Y2, Y3 and Y4 are independently selected from hydrogen, halo, etc.Type: GrantFiled: July 9, 2002Date of Patent: February 3, 2004Assignee: Warner-Lambert Company LLCInventors: Kiyoshi Kawamura, Sachiko Mihara, Seiji Nukui, Chikara Uchida
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Patent number: 6680326Abstract: Novel polycyclic compounds of the formula [I], wherein R1, R2, R3, R4, R5, R6, R7, ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts thereof. These compounds have antitumor activity and useful for the treatment of cancer.Type: GrantFiled: September 25, 2002Date of Patent: January 20, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Tsunehisa Aoyama, Kenichi Kawasaki, Miyako Masubuchi, Tatsuo Ohtsuka, Kiyoaki Sakata
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Patent number: 6670379Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1,Type: GrantFiled: April 17, 2003Date of Patent: December 30, 2003Assignee: Novartis AGInventors: Trevor John Howe, Gurdip Bhalay, Darren Mark Le Grand, Thomas Storz
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Patent number: 6664263Abstract: The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.Type: GrantFiled: March 3, 2003Date of Patent: December 16, 2003Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wieslaw M. Cholody, Teresa Kosakowska-Cholody, Christopher J. Michejda
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Patent number: 6649626Abstract: The invention concerns compounds of general formula (I) wherein: Z represents a sulphur or oxygen atom, NH, N-alkyl or Nboc; group R′, identical or different, represent each a hydrogen atom, a OCH3 group or a OCH2O group; group R″ represents a hydrogen or a CH3 group; group X represents a carbonyl, sulphonyl or CO2 group; and group R represents an alkyl, aryl, alkenyl or aralkyl group. The invention also concerns the preparation of said compounds, pharmaceutical compositions containing them and their use for stimulating &ggr;-amino-butyric acid activity and as medicine for treating nervous disorders.Type: GrantFiled: August 15, 2002Date of Patent: November 18, 2003Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de Bern, Innovationsagentur GmbHInventors: Robert Dodd, Rodolphe Razet, Pierre Jean-Paul Potier, Werner Sieghart, Frantisek Jursky, Roman Furtmuller, Erwin Sigel, Urs Thomet
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Patent number: 6642247Abstract: The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.Type: GrantFiled: June 11, 1999Date of Patent: November 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Geo Adam, Andrea Cesura, François Jenck, Sabine Kolczewski, Stephan Röver, Jürgen Wichmann
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Patent number: 6610747Abstract: A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: A—X, wherein A=—CH═CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(═O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered hetType: GrantFiled: August 27, 2001Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: Mavis Diane Adam, Mark David Andrews, Mark Leonard Elliott, Geoffrey Edward Gymer, David Hepworth, Harry Ralph Howard, Jr., Donald Stuart Middleton, Alan Stobie
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Patent number: 6608076Abstract: Polymeric conjugates of camptothecin derivatives having increased circulating half-lives are disclosed. In preferred aspects, the E ring lactone of the camptothecin derivative is opened and functionalized to allow attachment of a polymer such as PEG in the 17- or 20-position thereof. A representative example of such compounds is Methods of preparing and using the same are also disclosed.Type: GrantFiled: May 16, 2002Date of Patent: August 19, 2003Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Hong Zhao
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Patent number: 6593348Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.Type: GrantFiled: March 19, 2002Date of Patent: July 15, 2003Assignee: Research Triangle InstituteInventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6573273Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain urea, thiourea, acylurea, or sulfonylurea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: GrantFiled: December 21, 2001Date of Patent: June 3, 2003Assignee: 3M Innovative Properties CompanyInventors: Stephen L. Crooks, George W. Griesgraber, Kyle J. Lindstrom, Bryon A. Merrill, Michael J. Rice
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Patent number: 6566522Abstract: The present invention provides a rhodamine dye for recording layer of the high density optical recording disc, which has a chemical structure as shown in (I): where X− represents an acid anion and R represents a benzoic acid group, benzene sulfonic acid group or benzoic ester group. The dye of the present invention is applicable to recording layer of the high density optical recording disc after prepared appropriately. The dye of the present invention is cost efficient and simple in synthesis and purification.Type: GrantFiled: July 29, 2002Date of Patent: May 20, 2003Assignee: Industrial Technology Research InstituteInventors: Song-Yeu Tsai, Tien-Tsan Hung, Shih-Peng Hsu, Hao-Hsien Chiang
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Patent number: 6559161Abstract: The invention provides compounds of formula (I) wherein R1 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a hydroxy group, an alkoxy group having from 1 to 6 carbon atoms, a halogen atom, a nitro group, an amino group, a monoalkylamino group wherein the alkyl moiety has from 1 to 6 carbon atoms, a dialkylamino group wherein each alkyl moiety may be the same or different and each has from 1 to 6 carbon atoms, a dialkoxyamino group wherein each alkoxy moiety may be the same or different and each has from 1 to 6 carbon atoms, an alkanoyalmino group having from 1 to 20 carbon atoms or an alkanesulfonylamino group having from 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms; and R3 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or an alkoxy group having from 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 9, 2002Date of Patent: May 6, 2003Assignee: Universidad de BarcelonaInventors: Mercedes Alvarez, Lidia Feliu, Dolores Garcia Gravalos, Jose Luis Fernandez-Puentes
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Patent number: 6548500Abstract: Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.Type: GrantFiled: December 19, 2000Date of Patent: April 15, 2003Assignee: Molecumetics Ltd.Inventors: Michael Kahn, Masakatsu Eguchi, Hwa-Ok Kim, Marcin Stasiak
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Patent number: 6511989Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which A, R(1), R(2), X, Y, and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: November 2, 2001Date of Patent: January 28, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert
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Patent number: 6509361Abstract: The present invention contemplates 1,5-diaryl-substituted pyrazole compounds that, inter alia, inhibit the activity of p38 MAP kinase. Also contemplated by the invention are processes for the preparation of the contemplated compounds and for the use of a contemplated compound in treating a mammalian host having a p38 kinase- or TNF-mediated disease.Type: GrantFiled: February 12, 2001Date of Patent: January 21, 2003Assignee: Pharmacia CorporationInventors: Richard M. Weier, Joyce Z. Crich, Xiang Dong Xu, Paul W. Collins
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Patent number: 6506773Abstract: Pharmacologically active compounds are provided as well as pharmaceutical compositions and methods for treating cancer; inflammation; an autoimmune, infectious or ocular disease; or age-related macular degeneration in a mammal.Type: GrantFiled: May 15, 2001Date of Patent: January 14, 2003Assignee: Darwin Discovery Ltd.Inventors: Duncan Robert Hannah, Hazel Joan Dyke, Robert John Watson, John Fraser Keily, Andrew Douglas Baxter
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Patent number: 6503922Abstract: Pharmaceutical compounds comprising bridged nicotine analogs of N-octylnicotinium iodide (NONI) having selective antagonist properties at &agr;3&bgr;2-containing nicotinic receptor subtypes, and compositions containing these compounds. The compounds and compositions are used to treat central nervous system pathologies.Type: GrantFiled: August 30, 2001Date of Patent: January 7, 2003Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Linda P. Dwoskin, Rui Xu, Vladimir P. Grinevich