Benzene Ring Bonded Directly To The Carbonyl Patents (Class 558/415)
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Publication number: 20110003998Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; X is Br or Cl; and R5, R6, R7 and R8 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 4 wherein R11, R12, R13 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.Type: ApplicationFiled: March 4, 2009Publication date: January 6, 2011Inventor: Donald J. Dumas
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Patent number: 7863327Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.Type: GrantFiled: May 3, 2005Date of Patent: January 4, 2011Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Tadashi Honda, Michael B. Sporn, Nanjoo Suh
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Publication number: 20100249424Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.Type: ApplicationFiled: August 4, 2008Publication date: September 30, 2010Applicant: E.I.DuPont De Nemours and CompanyInventors: Gary David Annis, Brenton Todd Smith
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Patent number: 7754919Abstract: The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5 and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: GrantFiled: October 18, 2006Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: Tania Silva, Zachary Kevin Sweeney
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20100145060Abstract: Embodiments of the invention provide a method of using Schwartz Reagent, Cp2Zr(H)Cl, without accumulating or isolating it. Methods provide mixtures of Cp2ZrCl2, reductants that selectively reduce Cp2ZrCl2, and substrates. After reaction of Cp2ZrCl2 and the reductant, an intermediate reduction product is formed, apparently Schwartz Reagent. The in situ Schwartz Reagent then selectively reduces certain functional groups on the substrate. Substrates include tertiary amides, tertiary benzamides, aryl O-carbamates, and heteroaryl N-carbamates, which are reduced to aldehydes, benzaldehydes, aromatic alcohols, and heteroaromatics, respectively. Compared to prior methods, reagents are inexpensive and stable, reaction times are short, and reaction temperature in certain cases is conveniently room temperature. It has been estimated that using the in situ method described herein instead of synthesized or commercially obtained Schwartz Reagent provides a 50% reduction in cost.Type: ApplicationFiled: December 3, 2009Publication date: June 10, 2010Inventors: Yigang Zhao, Victor A. Snieckus
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Publication number: 20100130601Abstract: A compound of formula (I), wherein A1, A2, A3, A4, R1, R2, R3, G1, G2, G3 and Q are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: February 26, 2008Publication date: May 27, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Pierre Jung, Christopher Richard Ayles Godrey, William Lutz, Peter Maienfisch, Andre Stoller, Werner Zambach
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Publication number: 20100078607Abstract: There is provided a non-resonant two-photon absorption recording material including (a) a non-resonant two-photon absorption compound; and (b) a recording component capable of changing at least either one of a refractive index and a fluorescent intensity. The non-resonant two-photon absorption compound (a) is represented by the following formula (1): In the formula (1), both of X and Y represent a substituent having a Hammett sigma para value (?p value) of 0 or more and they may be the same as or different from each other; n represents an integer of 1 to 4; R represents a substituent and each R may be the same as or different from every other R; and m represents an integer of 0 to 4.Type: ApplicationFiled: September 30, 2009Publication date: April 1, 2010Applicant: FUJIFILM CORPORATIONInventors: Masaharu AKIBA, Eri TAKAHASHI, Hiroo TAKIZAWA, Hidehiro MOCHIZUKI, Hirokazu HASHIMOTO
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Publication number: 20100075932Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.Type: ApplicationFiled: November 24, 2009Publication date: March 25, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Preben Olesen, Thomas Kruse Hansen, Lise Brown Christiansen, Holger Claus Hansen
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Patent number: 7683201Abstract: Compounds of Formula I including all geometric and stereoisomers, N-oxides, and agriculturally suitable salts thereof, are disclosed which are useful as invertebrate pest control agents wherein A, B, J, K, L and R3 are as defined in the disclosure. Also disclosed are compositions for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula I an N-oxide thereof or a suitable salt thereof and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, its N-oxide or a suitable salt of the compound (e.g., as a composition described herein).Type: GrantFiled: May 4, 2006Date of Patent: March 23, 2010Assignee: E. I. du Pont de Nemours and CompanyInventor: George Philip Lahm
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Publication number: 20100056639Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: December 12, 2007Publication date: March 4, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Pierre Jung, Christopher Richard Syles Godfrey, William Lutz, Peter Maienfisch, Andre Stoller, Werner Zambach
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Publication number: 20100009397Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.Type: ApplicationFiled: June 8, 2009Publication date: January 14, 2010Applicants: UNIVERSITY OF SOUTH FLORIDA, YALE UNIVERSITYInventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
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Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
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Patent number: 7541071Abstract: The compound of the invention is represented by Formula (1a) or Formula (1b) wherein R1 is a monovalent group; P1 and P2 are a monovalent group having an acrylic group and a hydroxyl group; A1, A2, and B1 are a divalent cyclic group; X1, X2, X3, X4, Y1 and Y2 are a bonding group.Type: GrantFiled: December 22, 2004Date of Patent: June 2, 2009Assignees: Chisso Corporation, Chisso Petrochemical CorporationInventors: Ryushi Shundo, Tomohiro Eto
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Publication number: 20080319055Abstract: A method of providing a cooling sensation to the skin or the mucous membranes of the body by applying thereto a compound of Formula I in which X is H or (CH2)n—R, n is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, phenyl, C1-C4 straight or branched alkyl, or, a C1-C4 straight or branched alkoxy, or X and Y form together a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— which forms together with the carbon atoms to which they are attached a 5-membered ring; and R is a group with non-bonding electrons, R1 is H or C1-C5 branched alkyl, R2 and R3 are C1-C4 branched alkyls, or R2 and R3 taken together form a monocyclic, bicyclic or tricyclic radical of up to 10 carbons provided that R1, R2 and R3 together comprise at least 6 carbons. The compounds may be incorporated into products such as dentifrices, foodstuffs, confectionery, beverages, and cosmetic and medicinal preparations.Type: ApplicationFiled: March 15, 2006Publication date: December 25, 2008Applicant: GIVAUDAN SAInventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
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Patent number: 7449594Abstract: A process for preparing 4-pentafluorosulfanylbenzoylguanidines of formula I wherein R1 to R4 have the meanings indicated in the specification. The compounds of formula I are NEH1 inhibitors and can be employed, for example, for the treatment of cardiovascular disorders.Type: GrantFiled: October 6, 2006Date of Patent: November 11, 2008Assignee: Sanofi-aventis Deutschland GmbHInventors: Gerrit Schubert, Heinz-Werner Kleemann
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Patent number: 7449599Abstract: The present invention is directed to phenyl carboxamide compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: May 9, 2005Date of Patent: November 11, 2008Assignee: Merck + Co Inc.Inventors: Craig A. Coburn, Thomas G. Steele, Joseph P. Vacca, David Allen Annis, Jr., Gergely M. Makara, Huw M. Nash, Praveen K. Tadikonda, Tong Wang
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Patent number: 7414152Abstract: Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy, X is (CH2)n—R, where n is 0 or 1 and R is a group with non-bonding electrons, with the provisos that: (a) when Y and Z are H, X is not F, OH, MeO or NO2 in the 4-position and is not OH in the 2 or 6-position (b) when Y or Z is H then X, Y and Z are such that (i) the groups in the 3- and 4-positions are not both OMe, (ii) the groups in the 4- and 5-positions are not both OMe, (iii) the groups in 3- and 5-positions are not OMe if the group in the 4-position is OH, and (iv) the groups in the 3- and 5-positions are not OH if the group in the 4-position is methyl.Type: GrantFiled: May 19, 2006Date of Patent: August 19, 2008Assignee: Givaudan, SAInventors: Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack, Lori W. Tigani
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Publication number: 20080139505Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.Type: ApplicationFiled: November 15, 2005Publication date: June 12, 2008Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
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Patent number: 7332629Abstract: Disclosed are compounds of the formulae: and method of using the compounds to treat cancer, AIDS, HIV infection, and asthma.Type: GrantFiled: December 12, 2003Date of Patent: February 19, 2008Assignee: Jawaharlal Nehru Centre for Advanced Scientific ResearchInventors: Tapas Kumar Kundu, Karanam Balasubramanyam, Vankatesh Swaminathan
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Patent number: 7268248Abstract: The present invention relates to 3-cyano-2,4,5-trifluorobenzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5-fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3-dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene (VI).Type: GrantFiled: December 31, 2003Date of Patent: September 11, 2007Assignee: Bayer AktiengesellschaftInventors: Albrecht Marhold, Peter Wolfrum
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Patent number: 7126026Abstract: A process for preparing 4-pentafluorosulfanylbenzoylguanidines of formula I wherein R1 to R4 have the meanings indicated in the specification. The compounds of formula I are NHE1 inhibitors and can be employed, for example, for the treatment of cardiovascular disorders.Type: GrantFiled: November 15, 2004Date of Patent: October 24, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Gerrit Schubert, Heinz-Werner Kleemann
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Patent number: 7078565Abstract: Disclosed are phenyl-alkylene benzamides useful as orexin antagonistsType: GrantFiled: October 30, 2002Date of Patent: July 18, 2006Assignee: SmithKline Beecham plcInventors: Wai Ngor Chan, Amanda Johns, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Mythily Vimal
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Patent number: 7045660Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: March 3, 2004Date of Patent: May 16, 2006Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 7030261Abstract: Disclosed is a method for preparing a 2-hydroxy-6-ureidocarbonyl naphthalene derivative. The method comprises the step of reacting 2-hydroxy-6-aminocarbonyl naphthalene and a isocyanate in an organic solvent at a temperature of 90–200° C. According to the present invention, 2-hydroxy-6-ureidocarbonyl naphthalene derivative can easily be obtained within relatively short time and high yield.Type: GrantFiled: February 3, 2005Date of Patent: April 18, 2006Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Masaya Kitayama, Hiroyuki Wakamori, Nobuhiro Yonetani
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Patent number: 7026498Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.Type: GrantFiled: October 23, 2001Date of Patent: April 11, 2006Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
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Patent number: 6960688Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.Type: GrantFiled: October 23, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
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Patent number: 6951884Abstract: The invention relates to fluorobenzamide derivatives of the formula wherein R1, R2, R3 R4, R5, R6 and R7 are as defined herein. =, The compounds of the invention are selective monoamine oxidase B inhibitors and therefore they are suitable for the treatment of diseases mediated by monoamine oxidase B, such as Alzheimer's disease or senile dementia.Type: GrantFiled: June 6, 2003Date of Patent: October 4, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 6924307Abstract: Aminobutylic acid derivatives of the formula (I): wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.Type: GrantFiled: April 22, 2003Date of Patent: August 2, 2005Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6903092Abstract: Compounds having the general formula wherein R1, R2, R3, R4, R5, X1 and X2 are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: April 5, 2001Date of Patent: June 7, 2005Inventor: Peter Bernstein
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Patent number: 6861448Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 22, 2002Date of Patent: March 1, 2005Assignees: Virtual Drug Development, Inc., The UAB Research FoundationInventors: Wayne J. Brouillette, Lawrence DeLucas, Christie Brouillette, Sadanandan E. Velu, Yong-Chul Kim, Liyuan Mou, R. Stephen Porter
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Patent number: 6849648Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.Type: GrantFiled: October 4, 2002Date of Patent: February 1, 2005Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, William Glen Harter, James Lester Hicks, Patrick Michael O'Brien, Ly Pham, Joseph Armand Picard, William Howard Roark
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Publication number: 20040235908Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: June 16, 2004Publication date: November 25, 2004Applicant: Schering CorporationInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
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Patent number: 6821963Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: June 4, 2002Date of Patent: November 23, 2004Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Publication number: 20040220147Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.Type: ApplicationFiled: June 10, 2004Publication date: November 4, 2004Inventors: Johan Malm, Peter Brandt, Karin Edvinsson, Thomas Ericsson, Sandra Gordon
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Patent number: 6806365Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: April 5, 2002Date of Patent: October 19, 2004Assignee: Hoffmann-La Rocher Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Publication number: 20040176445Abstract: The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.Type: ApplicationFiled: March 9, 2004Publication date: September 9, 2004Applicant: Bayer Pharmaceuticals CorporationInventors: Klaus Urbahns, Michael Woltering, Susanne Nikolic, Josef Pernerstorfer, Berthold Hinzen, Elke Dittrich-Wengenroth, Hilmar Bischoff, Claudia Hirth-Dietrich, Klemens Lustig
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Publication number: 20040171680Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.Type: ApplicationFiled: October 17, 2003Publication date: September 2, 2004Inventors: Xiiaoli Chen, Keith T. Demarest, Jung Lee, Jay M. Matthews, Philip Rybczynski
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Publication number: 20040167350Abstract: The present invention relates to 3-cyano-2,4,5-trifluoro-benzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5-fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3-dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene (VT).Type: ApplicationFiled: December 31, 2003Publication date: August 26, 2004Inventors: Albrecht Marhold, Peter Wolfrum
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Publication number: 20040143006Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR&dgr; suptype.Type: ApplicationFiled: September 4, 2003Publication date: July 22, 2004Inventors: Lone Jeppesen, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
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Publication number: 20040122064Abstract: The present invention is directed to benzophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.Type: ApplicationFiled: February 5, 2004Publication date: June 24, 2004Inventor: Joseph Howing Chan
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Patent number: 6753433Abstract: Method for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) comprising the reaction of a compound of formula wherein X is a halogen, with organometallic dimethylaminopropyl halide. Other aspects of the invention are new compounds of formula II and formula III and their preparation.Type: GrantFiled: February 24, 2003Date of Patent: June 22, 2004Assignee: Orion Corporation, FERMIONInventors: Leif Hilden, Tuomas Huuhtanen, Petteri Rummakko, Arne Grumann, Pekka Pietikaeinen
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Publication number: 20040087491Abstract: A class of compounds is described which can be used for the treatment of viral infections.Type: ApplicationFiled: October 30, 2003Publication date: May 6, 2004Inventors: Daniel L. Flynn, Kenneth Williams, Susan L. Hockerman, Jeffrey Zablocki
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Publication number: 20040082625Abstract: The compounds of the invention are represented by the following general structure 1Type: ApplicationFiled: May 22, 2003Publication date: April 29, 2004Inventors: Michael G. Kelly, Shimin Xu, Ning Xi, Philip Miller, John F. Kincaid, Chiara Ghiron, Thomas Coulter
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Publication number: 20040077870Abstract: A process for the preparation of 1-(4′-fluorophenyl)-1-(3-dimethylamino-propyl)-5-phthalanecarbonitrile of formula (I), or a pharmaceutically acceptable salt thereof, 1Type: ApplicationFiled: October 22, 2002Publication date: April 22, 2004Applicant: Sekhsaria Chemicals LimitedInventors: Nandkumar Chodankar, Ajit Bhobe, G.M. Oak, Philip Eappan
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Publication number: 20040030130Abstract: A method of synthesizing pure enantiomers of acylanalides such as Casodex® (bicalutamide) and its derivatives includes contacting a compound having a ring structure that, when opened, provides a substituent having the structure of Formula I: 1Type: ApplicationFiled: May 23, 2003Publication date: February 12, 2004Inventor: Nnochiri Nkem Ekwuribe
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Publication number: 20040014809Abstract: A compound of the formula 1Type: ApplicationFiled: January 21, 2003Publication date: January 22, 2004Inventor: Peter Bernstein
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Patent number: 6670400Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.Type: GrantFiled: April 8, 2002Date of Patent: December 30, 2003Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Jacques Pommier, Christiane Martin, Pierre Roubert, Jean Pierre Defaux
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Publication number: 20030232882Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.Type: ApplicationFiled: November 18, 2002Publication date: December 18, 2003Inventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Publication number: 20030207894Abstract: Compounds of formula I: 1Type: ApplicationFiled: January 29, 2003Publication date: November 6, 2003Inventors: George Theodoridis, Edward Barron, Daniel H. Cohen, Ellen M. Crawford, Thomas G. Cullen, Hongyan Qi, Elizabeth Rowley, Syed F. Ali, Walter H. Yeager, Christina B. Duggan