Patents Examined by Susannah E. Lee
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Patent number: 7041668Abstract: The present invention discloses and claims benzimidazole compounds of formula (I): in which A is aryl or heteroaryl; R1 is selected from optionally substituted alkyl, alkoxy, aryl or heteroaryl, NH-lower alkyl or NH-cycloalkyl, or halogen, NH2; 1-imidazolyl or SO2Me; R2 is selected from optionally substituted —CO-alkyl, —CO-cycloalkyl, —CO-aralkyl, —CO-aryl, —CO-alkoxy, aryl or aralkyl, or —CO-amino, CO—NHR3 or CO—R3R4 wherein R3 and R4 are selecteded independently from hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, fluoroalkyl, alkynyl, heteroalkyl, alkylheteroalkyl, aryl, aralkyl or together form an alkylene chain optionally containing one to 4 heteroatoms; a pharmaceutically acceptable salt or a prodrug thereof; the use of compounds of formula (I) for the treatment of cancer, and pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents.Type: GrantFiled: March 25, 2004Date of Patent: May 9, 2006Assignee: Aventis Pharma S.A.Inventors: Francois Clerc, Francois Hamy, Isabelle Depaty, Odile Angouillant-Boniface, Stéphanie Deprets, Chantal Carrez, Manfred Roesner
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Patent number: 7034047Abstract: The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.Type: GrantFiled: May 19, 2004Date of Patent: April 25, 2006Assignee: Astellas Pharma, Inc.Inventors: Takahiko Tobe, Takashi Sugane, Wataru Hamaguchi, Itsuro Shimada, Kyoichi Maeno, Junji Miyata, Tetsuya Kimizuka, Takeshi Suzuki, Atsuyuki Kohara, Takuma Morita, Michael Arlt, Hartmut Greiner
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Patent number: 7019011Abstract: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.Type: GrantFiled: September 4, 2003Date of Patent: March 28, 2006Assignee: Aventis Pharma S.A.Inventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney, Gilles Tiraboschi
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Patent number: 7001887Abstract: A compound of Formula (1): ? wherein R1 represents an amidinophenyl group, etc.; R2 represents a hydrogen atom, etc.; R3 represents a carbamoylalkyl group, etc.; R4 represents a hydrogen atom, etc.; R5 represents a benzyl group, etc.; R6 represents a hydrogen atom, etc.; and R7 represents an alkylsulfonyl group, etc. A crystal of a complex between factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor. A medium carrying a part or all of structure coordinate data of a complex between human factor VIIa/human soluble tissue factor and a low-molecular weight reversible factor VIIa inhibitor, obtainable by X-ray crystal structure analysis of the crystal. A method for computationally designing a low-molecular weight reversible factor VIIa inhibitor using the coordinate data.Type: GrantFiled: February 4, 2002Date of Patent: February 21, 2006Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Takuya Shiraishi, Shojiro Kadono, Masayuki Haramura, Haruhiko Sato, Toshiro Kozono, Takaki Koga, Akihisa Sakamoto
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Patent number: 6998420Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.Type: GrantFiled: December 23, 2003Date of Patent: February 14, 2006Assignee: Pharmacia & Upjohn CompanyInventors: William R. Perrault, Robert C. Gadwood
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Patent number: 6998414Abstract: Compounds effective as IP receptor modulators, particularly IP receptor antagonists, that are of the formula I: wherein A, R1, R2, R3 and R4 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: April 29, 2004Date of Patent: February 14, 2006Assignee: Roche Palo Alto LLCInventors: Paul Francis Keitz, Alam Jahangir, Francisco Javier Lopez-Tapia, Counde O'Yang
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Patent number: 6992101Abstract: The present invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein R?, R?, R??, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof in treating diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia.Type: GrantFiled: November 6, 2003Date of Patent: January 31, 2006Assignee: Pfizer, Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill, Jana Polivkova
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Patent number: 6992083Abstract: The invention relates to compounds of formula wherein R is phenyl, unsubstituted or substituted by halogen or —CH2N(CH3)(CH2)nOCH3, or is benzyl, lower alkyl, lower alkoxy, —(CH2)nOCH3, or is pyridin 3 -or 4-yl, unsubstituted or substituted by lower alkyl, halogen, morpholinyl, —(CH2)n-halogen, —(CH2)nOCH3, —(CH2)n-morpholin-4-yl, or —(CH2)n-pyrrolidin-1-yl; R1 is phenyl, unsubstituted or substituted by halogen, tetrahydropyran-4-yl, 3,6-dihydro-2H-pyran-4-yl or morpholin-4-yl; n is independently from each other 1 or 2; and to pharmaceutically acceptable salts thereof for the treatment of diseases related to the adenosine A2A-receptor.Type: GrantFiled: January 9, 2004Date of Patent: January 31, 2006Assignee: Hoffman-La Roche Inc.Inventor: Roger David Norcross
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Patent number: 6979696Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein m, A, X, Y, R1, R2, R3, R4 and R5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: May 7, 2004Date of Patent: December 27, 2005Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Clara Jeou Jen Lin, Amy Geraldine Moore, Counde O'Yang, Yansheng Zhai
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Patent number: 6967253Abstract: Process for the synthesis of 5-(3-pyridylmethyl)imidazolidine-2,4-dione, according to which 5-(3-pyridylmethylene)imidazolidine-2,4-dione is subjected to a hydrogenation reaction.Type: GrantFiled: September 2, 2002Date of Patent: November 22, 2005Assignee: Solvay (Societe Anonyme)Inventor: Roland Callens
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Patent number: 6953860Abstract: A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.Type: GrantFiled: June 12, 2003Date of Patent: October 11, 2005Inventors: Ahmed F. Abdel-Magid, Bruce D. Harris, Cynthia A. Maryanoff
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Patent number: 6953861Abstract: The present invention relates to pyrrolidine compounds of the general structure: where n is an integer 1-6 and R is hydrogen or a C1 to C6 straight chain or branched alkyl group, and wherein when n=1, R=CH3 or H, useful for re-sensitizing vancomycin resistant Gram-positive bacteria in which resistance results from the conversion of an amide bond to an ester bond on the cell wall peptide precursors of the bacteria.Type: GrantFiled: March 18, 2004Date of Patent: October 11, 2005Assignees: The Trustees of Columbia University in the City of New York, The Rockefeller UniversityInventors: Gabriela Chiosis, Ivo G. Boneca, W. Clark Still
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Patent number: 6949563Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C0-4alkyl, are useful in the treatment of cancer.Type: GrantFiled: January 6, 2004Date of Patent: September 27, 2005Inventors: Graham Michael Wynne, Kevin Doyle, Saleh Ahmed, An-Hu Li, John Fraser Keily, Chrystelle Marie Rasamison, Neil Anthony Pegg, Imaad Saba, Claire Thomas, Don Smyth, Shazia Sadiq, Gary Newton, Graham Dawson, Andrew Phillip Crew, Arlindo Lucas Castelhano
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Patent number: 6930124Abstract: The invention relates to compounds of formula (I) in which R5 is chosen from the group consisting of: in which R2 is a C1-C3 alkyl group in which X may be Cl, Br, or F in which n is between 1 and 3, in the E or Z form, or a mixture of the two isomeric forms, possessing antimitotic, antiproliferative and antivascular properties through inhibition of the polymerization of tubulin into microtubulesType: GrantFiled: September 10, 2003Date of Patent: August 16, 2005Assignee: Aventis Pharma S. A.Inventors: Cécile Combeau, Patrick Mailliet, Marielle Chiron
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Patent number: 6927234Abstract: Biologically active xanthone derivatives, as well as compositions prepared from such derivatives, possessing anti-cancer activity, anti-inflammatory activity, anti-obesity activity, and/or hair growth promotion activity, and a method for producing such derivatives and compositions. The derivatives are obtained by utilizing a heating, extracting and condensing system that efficiently recovers the derivatives from a raw material.Type: GrantFiled: November 19, 2003Date of Patent: August 9, 2005Assignee: Kuboyama Bio Ken Inc.Inventor: Henry Aoki
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Patent number: 6927215Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 2 to 10, n represents 0, 1 or 2. y represents unsubstituted or substituted methylene and p represents 1, 2 or 3, and to processes for their preparation and to their use as pesticides.Type: GrantFiled: June 29, 2001Date of Patent: August 9, 2005Assignee: Bayer Cropscience AGInventors: Udo Kraatz, Bernd Gallenkamp, Heiko Rieck, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Peter Lösel, Andreas Turberg, Olaf Hansen, Achim Harder
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Patent number: 6916839Abstract: The present invention relates to pyrazolylarylalkines and to their use, to a process for preparing pyrazolylarylalkines and also to intermediates.Type: GrantFiled: January 5, 2004Date of Patent: July 12, 2005Assignee: Bayer Chemicals AktiengesellschaftInventors: Wolfgang Ebenbeck, Florian Rampf, Albrecht Marhold
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Patent number: 6911463Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.Type: GrantFiled: August 6, 2002Date of Patent: June 28, 2005Assignee: Eli Lilly and CompanyInventors: Daniel Jon Sall, Jolie Anne Bastian, Cynthia Darshini Jesudason, Theo Schotten, Gerd Reuhter, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz