Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/332)
  • Patent number: 8138350
    Abstract: The present application relates to novel substituted N?-cyano-N-halogenalkylimidamide derivatives, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: July 7, 2007
    Date of Patent: March 20, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Peter Jeschke, Robert Velten, Rüdiger Fischer, Achim Hense, Michael Edmund Beck, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Erich Sanwald, Christian Arnold
  • Patent number: 8101640
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: January 24, 2012
    Assignees: Novartis Vaccines and Diagnostics, Inc., University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20120015987
    Abstract: The present invention provides a novel crystalline form of atazanavir sulfate, process for its preparation and to pharmaceutical composition containing it. In accordance with the present invention atazanavir sulfate was dissolved in methanol, to the solution was added ethyl acetate, the solid obtained was collected by filtration and dried to give atazanavir sulfate crystalline form H1.
    Type: Application
    Filed: January 12, 2009
    Publication date: January 19, 2012
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
  • Publication number: 20120010172
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 31, 2009
    Publication date: January 12, 2012
    Applicant: McDERMOTT WILL & EMERY LLP
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Patent number: 8088772
    Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: January 3, 2012
    Assignee: The Genetics Company, Inc.
    Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Frank Jaschinski, Guy Lemaillet, Cornelia Marty-Ernst, Elena Marzi, Leonardo Scapozza
  • Patent number: 8088921
    Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: January 3, 2012
    Assignee: Wilex AG
    Inventors: Hugo Ziegler, Peter Wikstroem
  • Publication number: 20110306639
    Abstract: The present invention discloses hydrocarbylidene nitrohydrozinecarboximidamides and the use thereof as well as a method for making the same. The structural general formula of the compounds are shown in formula I, wherein, R1 is C1-C10 saturated and/or unsaturated aliphatic hydrocarbonyl, benzyl, substituted benzyl, halogenated picolyl, halogenated thiazolyl methyl, tetrahydrofuryl methyl or oxazolyl methyl; R2 is hydrogen, C1-C5 saturated and/or unsaturated aliphatic hydrocarbonyl, phenyl, substituted phenyl, pyridyl or substituted pyridyl; R3 is hydrogen, C1-C10 saturated and/or unsaturated aliphatic hydrocarbonyl, furyl, phenyl, substituted phenyl, benzyl or substituted benzyl. The tests of insecticidal activity show that the hydrocarbylidene nitrohydrozinecarboximidamides shown by formula (I) have high preventive efficiency against insect pests of plants, such as aphid, plant hopper, cotton bollworm, asparagus caterpillar, and the like, and can be used as plant insecticides.
    Type: Application
    Filed: November 25, 2008
    Publication date: December 15, 2011
    Inventors: ZhaoHai Qin, Yongqiang Ma, Wangcang Su, Lei Wang, Zheng Zhang, Bengbin Zhao, Jiangsheng Fang
  • Publication number: 20110306621
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: December 15, 2011
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Nobuyuki Shiraishi, Yuichiro Kawamoto, Takuya Washio
  • Publication number: 20110288133
    Abstract: This invention relates to novel Histone deacetylases inhibitors. Also disclosed is a method for treating mucositis or cancer with these inhibitors.
    Type: Application
    Filed: May 18, 2010
    Publication date: November 24, 2011
    Applicant: Taipei Medical University
    Inventors: Hui-po Wang, On Lee, Yu-Wen Cheng, Chun-li Wang, Feng-Shuo Chang, Hsiao Che-Chih
  • Publication number: 20110269677
    Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.
    Type: Application
    Filed: March 12, 2008
    Publication date: November 3, 2011
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
  • Publication number: 20110269751
    Abstract: The heterocyclic nitrogenous or oxygenous compounds of formula (A), (B), (C) or (D) formed from dialdehydes, their optical isomers, cis- and trans- isomers, or agrochemically acceptable salts, their preparation methods, agrochemical compositions comprising the compounds and the uses thereof are provided. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm, armyworm and so on.
    Type: Application
    Filed: December 18, 2009
    Publication date: November 3, 2011
    Applicants: SHANGHAI SHENGNONG PESTICIDE CO., LTD., EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Zhong Li, Xuhong Qian, Xusheng Shao, Xiaoyong Xu, Liming Tao, Gonghua Song
  • Publication number: 20110257199
    Abstract: Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.
    Type: Application
    Filed: June 17, 2011
    Publication date: October 20, 2011
    Inventors: Richard R. Tidwell, David W. Boykin, W. David Wilson, Reto Brun, Karl Werbovetz, Mohamed A. Ismail, Reem K. Arafa, Laixing Hu
  • Publication number: 20110195939
    Abstract: HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo.
    Type: Application
    Filed: July 30, 2009
    Publication date: August 11, 2011
    Applicant: GANIAL IMMUNOTHERAPEUTICS INC.
    Inventors: Ferdinando Nicoletti, Yousef Al-Abed, Gianni Garotta
  • Publication number: 20110195940
    Abstract: Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature. Exemplary potent HIV protease inhibitors are mono-m-PEG3-atazanavir, mPEGn-N-darunavir (wherein n is 3 or 5), mPEGn-NHCO-saquinavir (wherein n is 5 or 7), and di-mPEG3-atazanavir.
    Type: Application
    Filed: September 17, 2009
    Publication date: August 11, 2011
    Applicant: Nektar Therapeutics
    Inventors: C. Simone Jude-Fishburn, Laurie A. Vander Veen, Timothy A. Riley
  • Publication number: 20110184184
    Abstract: A method for purifying an ?-unsaturated amine compound represented by Formula (1), the method comprising a step of extracting with water the compound of Formula (1) from a crude product of the ?-unsaturated amine compound represented by Formula (1), and a step of extracting with a pyridine solvent the ?-unsaturated amine compound of Formula (1) from the aqueous solution containing the compound of Formula (1) obtained in the previous step to obtain a pyridine solvent solution of the compound of Formula (1): wherein R1 represents a hydrogen atom, a C1-4 alkyl group, a halo C1-4 alkyl group, a C1-4 alkoxy-C1-4 alkyl group, a C7-9 aralkyl group, or an optionally substituted phenyl group, R2 represents a hydrogen atom, a C1-4 alkyl group, or a C7-9 aralkyl group, and R3 represents a hydrogen atom, a C1-5 alkyl group, a halo C1-4 alkyl group, a hydroxy C1-4 alkyl group, a C1-4 alkoxy-C1-4 alkyl group, C2-4 alkenyl group, or a C7-9 aralkyl group.
    Type: Application
    Filed: August 8, 2008
    Publication date: July 28, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Hiroshi Souda
  • Publication number: 20110144114
    Abstract: Triazinone derivatives represented by formula (I) wherein: Z, R1, R2, R3, R4, and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.
    Type: Application
    Filed: December 15, 2010
    Publication date: June 16, 2011
    Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
  • Publication number: 20110124689
    Abstract: A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.
    Type: Application
    Filed: October 8, 2010
    Publication date: May 26, 2011
    Inventors: Soojin Kim, Bruce T. Lotz, Mary F. Malley, Jack Z. Gougoutas, Martha Davidovich, Sushil K. Srivastava
  • Publication number: 20110118234
    Abstract: The present invention provides compounds Formula (I) that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: May 4, 2009
    Publication date: May 19, 2011
    Inventors: Kaustav Biswas, Jian J. Chen, James R. Falsey, Vijay Keshav Gore, Qingyian Liu, Vu Van Ma, Stephanie J. Mercede, Robert M. Rzasa, Christopher M. Tegley, Jiawang Zhu
  • Patent number: 7943803
    Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: May 17, 2011
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
  • Patent number: 7923461
    Abstract: A compound having the following formula wherein A is —O—; B is alkylene or alkenylene optionally containing —O—, —S—, —(NR7)—, —CO— or —N?; R1 and R2 are alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is unsubstituted or substituted by halogen, cycloalkyl, aryl, adamantyl or amino; R3 is a substituted or unsubstituted pyridine ring; R5 and R6 are hydrogen or alkyl; R7 is hydrogen or alkyl; X is O or S; and each hydrogen of the said amino is unsubstituted or substituted by alkyl, alkoxycarbonyl, cycloalkyloxycarbonyl, arylalkoxycarbonyl or halogenoalkyloxycarbonyl. The compound is a TNF-? production inhibitor that is useful for treating autoimmune diseases such as rheumatoid arthritis.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: April 12, 2011
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Masakazu Ban, Hiroshi Suhara, Masato Horiuchi, Noriyoshi Yamamoto, Hiroshi Enomoto, Hiroyuki Inoue
  • Publication number: 20110077160
    Abstract: Compounds having the following generic formula are disclosed.
    Type: Application
    Filed: December 7, 2010
    Publication date: March 31, 2011
    Inventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette V. Brown, Ronald Ross, JR., William C. Lo, Matthias S. Ober
  • Publication number: 20110071178
    Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
    Type: Application
    Filed: April 16, 2010
    Publication date: March 24, 2011
    Applicant: Northeastern University
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Publication number: 20110071093
    Abstract: Oligomeric reagents are provided comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble, non-peptidic oligomer and a pharmaceutically active agent. The oligomeric reagents are useful for, among other things, forming oligomer active agent conjugates. Related methods, compositions, preparations, and so forth are also provided.
    Type: Application
    Filed: March 12, 2009
    Publication date: March 24, 2011
    Applicant: Nektar Therapeutics
    Inventor: Franco J. Duarte
  • Publication number: 20110064657
    Abstract: The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.
    Type: Application
    Filed: June 26, 2008
    Publication date: March 17, 2011
    Applicant: The Johns Hopkins University
    Inventors: Martin Gilbert Pomper, Ray Sangeeta, Ronnie C. Mease, Catherine Foss
  • Publication number: 20110065710
    Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Application
    Filed: December 2, 2004
    Publication date: March 17, 2011
    Inventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
  • Patent number: 7897779
    Abstract: The present invention relates to novel 1,4-dihydropyridine derivatives, to novel cosmetic or dermatological sunscreen compositions containing these derivatives and the use of these derivatives for photoprotecting human skin and/or hair against UV radiation, in particular solar radiation.
    Type: Grant
    Filed: February 11, 2005
    Date of Patent: March 1, 2011
    Assignee: DSM IP Assets B.V.
    Inventors: Katja Berg-Schultz, Ulrich Huber, Daniel Sprenger
  • Patent number: 7884206
    Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidinophenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: February 8, 2011
    Assignee: Wilex AG
    Inventors: Hugo Ziegler, Peter Wikstroem
  • Publication number: 20110009355
    Abstract: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.
    Type: Application
    Filed: April 6, 2010
    Publication date: January 13, 2011
    Inventors: Scott L. Harbeson, Roger D. Tung
  • Publication number: 20100304966
    Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.
    Type: Application
    Filed: October 9, 2008
    Publication date: December 2, 2010
    Applicant: BASF SE
    Inventors: Joachim Rheinheimer, Barbara Nave, Doris Kremzow, Stefan Redlich, Christian Pilger, Claudia Rosenbaum, Wassilios Grammenos
  • Patent number: 7838678
    Abstract: A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: November 23, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Soojin Kim, Bruce T. Lotz, Mary F. Malley, Jack Z. Gougoutas, Martha Davidovich, Sushil K. Srivastava
  • Publication number: 20100292482
    Abstract: The present invention relates to a Compound of the formula (I), wherein X represents CN, COOR, wherein R represents hydrogen or a carboxyl protecting group, CONR?2, wherein R? represents hydrogen or a carboxyl protecting group, or nitro; R1, R2, R3, R4, R5 independently of each other represent hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; Y represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C7-C13 alkaryl, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; and wherein the stereochemically unspecified double bonds in the above formula (I) represent either the E,E; E,Z; Z,E or Z,Z configuration.
    Type: Application
    Filed: October 24, 2008
    Publication date: November 18, 2010
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss
  • Publication number: 20100286182
    Abstract: A method of identification of compounds that modulate thyroid hormone activity, and the use of such compounds and compositions thereof for such purposes are disclosed. The compounds may be selected from the group consisting of: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to aberrant thyroid hormone activity, such as hyperthyroidism and thyrotoxicosis.
    Type: Application
    Filed: April 18, 2008
    Publication date: November 11, 2010
    Inventors: Herbert H. Samuels, Ruben Abagyan, Matthieu Schapira, Maxim Totrov, Bruce M. Raaka, Stephen R. Wilson, Li Fan, Zhiguo Zhou
  • Patent number: 7829720
    Abstract: A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.
    Type: Grant
    Filed: May 2, 2005
    Date of Patent: November 9, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Soojin Kim, Bruce T. Lotz, Mary F. Malley, Jack Z. Gougoutas, Martha Davidovich, Sushil K. Srivastava
  • Publication number: 20100274006
    Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.
    Type: Application
    Filed: May 4, 2010
    Publication date: October 28, 2010
    Applicant: NIPPON SODA CO., LTD
    Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
  • Patent number: 7812037
    Abstract: Compounds with antiplatelet aggregation and anticoagulant characteristics for the treatment of cardiovascular, cerebrovascular, and cardiovascular related diseases and symptoms, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxine and/or substituted pyridoxine analogs.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: October 12, 2010
    Assignee: Medicure International, Inc.
    Inventors: Wasimul Haque, James Diakur, Vinh Pham, Atiq Rehman, Tara Whitney, Mohammed Omar, Seng Yi, A. Qasim Khan
  • Patent number: 7807677
    Abstract: Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A? and A? are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.
    Type: Grant
    Filed: February 9, 2006
    Date of Patent: October 5, 2010
    Assignee: Medivir AB
    Inventors: Jenny Ekegren, Anders Hallberg, Hans Wallberg, Bertil Samuelsson, Mahalingam Kannan
  • Publication number: 20100249101
    Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Application
    Filed: January 7, 2010
    Publication date: September 30, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
  • Publication number: 20100249135
    Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of
    Type: Application
    Filed: December 11, 2007
    Publication date: September 30, 2010
    Applicant: THE GENETICS COMPANY, INC.
    Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Jaschinskin Frank, Guy Lemaillet, Cornelia Marty-Ernest, Elena Marzi, Leonardo Scapozza
  • Patent number: 7794907
    Abstract: A hydrazone compound capable of realizing an electrophotographic photoreceptor having good electric properties such as good sensitivity and light responsibility, good electric and mechanical durability and good environment stability, is provided. The hydrazone compound is represented by the following general formula (1). The compound is contained in the charge transporting layer of the electrophotographic photoreceptor.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: September 14, 2010
    Assignee: Sharp Kabushiki Kaisha
    Inventors: Akihiro Kondoh, Takatsugu Obata
  • Patent number: 7786043
    Abstract: The invention relates to 2-(pyridin-2-yl)-pyrimidine compounds of general formula (I) and their use for controlling pathogenic fungi and as plant protection products that, as an active constituent, contain compounds of this type: In general formula (I), k represents 0, 1, 2, 3; m represents 0, 1, 2, 3, 4 or 5; n represents 1, 2, 3, 4 or 5; R1, independent of one another, represents halogen, OH, CN, NO2, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, C2-C4 alkenyl, C2-C4 alkynyl, C3-C8 cycloalkyl, C1-C4 alkoxy-C1-C4 alkyl, amino, phenoxy, which is optionally substituted by halogen or C1-C4 alkyl, NHR, NR2, C(Ra)?N—ORb, S(?O)pA1 or C(?O)A2, or two radicals R1 bound to adjacent carbon atoms can, together, also represent a group —O-Alk-O—, wherein Alk represents a linear or branched C1-C4 alkylene, and 1, 2, 3 or 4 hydrogen atoms can also be replaced by halogen; R2 represents C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, hydroxy, halogen, CN or NO2; whereby R2 can also represent
    Type: Grant
    Filed: July 22, 2005
    Date of Patent: August 31, 2010
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Thomas Grote, Carsten Blettner, Markus Gewehr, Udo Hünger, Bernd Müller, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Ulrich Schöfl, Harald Köhle, Siegfried Strathmann, Maria Scherer, Reinhard Stierl, Jan Rether
  • Publication number: 20100197735
    Abstract: Novel phenylurea compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.
    Type: Application
    Filed: March 5, 2010
    Publication date: August 5, 2010
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Thibaud Portal
  • Patent number: 7750049
    Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: July 6, 2010
    Assignee: Pharmeste S.R.L.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
  • Publication number: 20100113276
    Abstract: The use of N2-phenylamidines of formula (I) as herbicides is described. In this formula (I), R2, R3, R4, R5 and R6 are different radicals and A is a bond or various 1- or polyatomic bridging elements.
    Type: Application
    Filed: March 4, 2008
    Publication date: May 6, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Birgit Kuhn, Harald Jakobi, Thomas Mueller, Joerg Tiebes, Heinz Kehne, Dirk Schmutzler, Martin Hills, Christopher Rosinger, Klaus Kunz, Mark Wilheim Drewes, Dieter Feucht, Thomas Seitz, Benoit Hartmann, Ralf Dunkel, Joerg Nico Greul, Oliver Guth, Kerstein Ilg, Darren James Mansfeld, Wahed Ahmed Moradi, Peter Dahmen, Ulrike Wachendorf-Neumann, Arnd Voerste, Dale Robert Mitchell, Jean-Pierre Andre Vors, Dale Robert Mitchell, Tom Hough
  • Patent number: 7709507
    Abstract: Compounds of the formula or a pharmaceutically acceptable salt thereof or a tautomer thereof, wherein A and B are as described herein, are useful for treating conditions afflicting mammals.
    Type: Grant
    Filed: May 10, 2007
    Date of Patent: May 4, 2010
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
  • Publication number: 20100048646
    Abstract: The present application relates to novel substituted N?-cyano-N-halogenalkylimidamide derivatives, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Application
    Filed: July 7, 2007
    Publication date: February 25, 2010
    Applicant: Bayer CropScience AG
    Inventors: Peter Jeschke, Robert Velten, Rüdiger Fischer, Achim Hense, Michael Edmund Beck, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Erich Sanwald, Christian Arnold
  • Publication number: 20100035930
    Abstract: The invention relates to compounds of the formula I as defined herein, which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. The compounds of the formula I are suitable for manufacturing medicaments for the prophylaxis, secondary prevention and therapy of one or more disorders which are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: June 8, 2009
    Publication date: February 11, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Christopher KALLUS, Mark BROENSTRUP, Werngard CZECHTIZKY, Andreas EVERS, Markus FOLLMANN, Nis HALLAND, Herman SCHREUDER
  • Publication number: 20100029588
    Abstract: The present invention relates to oxime ether-, hydrazone- or azomethine-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the amidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.
    Type: Application
    Filed: March 8, 2008
    Publication date: February 4, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Thomas Seitz, Klaus Kunz, Wahed Ahmed Moradi, Jörg Nico Greul, Darren James Mansfield, Urlich Heinemann, Amos Mattes, Oswald Ort, Jean-Pierre Vors, Peter Dahem, Ulrike Wachendorff-Neumann, Arnd Voerste
  • Publication number: 20100016380
    Abstract: A compound having the following formula wherein A is —O—; B is alkylene or alkenylene optionally containing —O—, —S—, —(NR7)—, —CO— or —N?; R1 and R2 are alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is unsubstituted or substituted by halogen, cycloalkyl, aryl, adamantyl or amino; R3 is a substituted or unsubstituted pyridine ring; R5 and R6 are hydrogen or alkyl; R7 is hydrogen or alkyl; X is O or S; and each hydrogen of the said amino is unsubstituted or substituted by alkyl, alkoxycarbonyl, cycloalkyloxycarbonyl, arylalkoxycarbonyl or halogenoalkyloxycarbonyl. The compound is a TNF-? production inhibitor that is useful for treating autoimmune diseases such as rheumatoid arthritis.
    Type: Application
    Filed: September 23, 2009
    Publication date: January 21, 2010
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Masakazu Ban, Hiroshi Suhara, Masato Horiuchi, Noriyoshi Yamamoto, Hiroshi Enomoto, Hiroyuki Inoue
  • Publication number: 20090300856
    Abstract: One subject of the present invention is monocationic monochromophoric compounds of formula (I) and/or (II) below: in which: R1 represents a hydrogen or an alkyl, phenyl, benzyl, alkylcarbonyl, alkylsulphonyl, aminosulphonyl or aminocarbonyl radical; R5 represents an alkyl, phenyl or benzyl radical; R2 and R3, represent a halogen or an alkyl, aryloxy, arylamino, hydroxyl, alkoxy, (poly)hydroxyalkoxy, alkoxycarbonyl, alkylcarbonyloxy, amino, alkylcarbonylamino, aminocarbonyl, ureido, aminosulphonyl, alkylthio, alkylsulphonylamino, cyano, trifluoromethyl, thio, alkylsulphinyl or alkylsulphonyl radical; R4 represents a hydrogen or an alkyl, amino, alkylcarbonylamino, ureido, alkylsulphonylamino, hydroxycarbonyl, alkoxycarbonyl, cyano, phenyl or benzyl radical; R6 and R7, represent a hydrogen or an alkyl, alkylcarbonyl, alkoxycarbonyl, alkoxyaryl, aminoaryl, aminocarbonyl or alkylsulphonyl radical; and n is between 0 and 4, n? is between 0 and 4, the electroneutrality of the compounds of formulae (I) and (II)
    Type: Application
    Filed: April 13, 2007
    Publication date: December 10, 2009
    Inventors: Herve David, Nadege Murguet, Andrew Greaves
  • Publication number: 20090300857
    Abstract: Disclosed are thiol dyes of formula (1), wherein R1, R2, R3, R4 and R5 independently from each other are hydrogen; unsubstituted or substituted, straight-chain or branched, monocyclic or polycyclic, interrupted or uninterrupted C1-C14alkyl; C2-C14alkenyl; C6-C10aryl; C6-C10aryl-C1-C10alkyl; or C5-C10alkyl(C5-C10aryl); A is a residue of an organic dye; and Y1 is the direct bond; C1-C10alkylene; C5-C10cycloalkylene; C5-C12arylene; or C5-C12arylene-(C1-C10alkylene). The compounds are used to dye hair with or without reducing agents. Furthermore, the present invention relates to compositions comprising thiol dyes of formula (1) and to process for the preparation of theses compounds.
    Type: Application
    Filed: August 21, 2006
    Publication date: December 10, 2009
    Applicant: CIBA CORPORATION
    Inventors: Victor Paul Eliu, Beate Fröhling, Dominique Kauffmann