Plural Nitrogens In The Heterocyclic Ring Patents (Class 540/545)
  • Patent number: 7973031
    Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.
    Type: Grant
    Filed: October 29, 2002
    Date of Patent: July 5, 2011
    Assignees: Novartis AG, Dana-Farber Cancer Institute Inc
    Inventors: James Douglas Griffin, Paul William Manley
  • Publication number: 20110136753
    Abstract: Glycosylated indolocarbazoles, method for obtaining same and uses thereof. This invention relates to rebeccamycin and staurosporine derivatives obtained by fermentation of recombinant bacterial strains. The invention also relates to the methods used to obtain the recombinant strains and the production of rebeccamycin and staurosporine derivatives. The invention also relates to bacterial strains that are of use for the production of rebeccamycin and staurosporine derivatives. Lastly, the rebeccamycin and staurosporine derivatives described herein are applicable to the field of human health, specifically for manufacturing drugs that are of use in the treatment of tumour, neurological and inflammatory diseases.
    Type: Application
    Filed: April 6, 2009
    Publication date: June 9, 2011
    Applicants: UNIVERSIDAD DE OVIEDO, ENTRECHEM S.L.
    Inventors: Aaroa Pêrez Salas, César Sánchez Reillo, Alfredo Fernández Braña, Carmen Méndez Fernández, Jose Antonio Salas Fernández, Francisco Morís Varas
  • Publication number: 20110124629
    Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3 -fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
    Type: Application
    Filed: January 3, 2011
    Publication date: May 26, 2011
    Applicant: CEPHALON, INC.
    Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
  • Publication number: 20110112067
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 12, 2011
    Applicant: Universitat des Saarlandes
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20110098274
    Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: January 7, 2011
    Publication date: April 28, 2011
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
  • Patent number: 7915199
    Abstract: A selective herbicidal composition for controlling grasses and weeds in crops of cultivated plants, comprising a) a herbicidally effective amount of a compound of formula I wherein the substituents are defined as given in claim 1; b) a herbicidally synergistic amount of at least one herbicide selected from the classes of phenoxy-phenoxypropionic acids, hydroxylamines, sulfonylureas, imidazolinones, pyrimidines, triazines, ureas, PPO, chloroacetanilides, phenoxyacetic acids, triazinones, dinitroanilines, azinones, carbamates, oxyacetamides, thiolcarbamates, azole-ureas, benzoic acids, anilides, nitriles, triones and sulfonamides, as well as from the herbicides amitrol, benfuresate, bentazone, cinmethylin, clomazone, chlopyralid, difenzoquat, dithiopyr, ethofumesate, flurochloridone, indanofane, isoxaben, oxaziclomefone, pyridate, pyridafol, quinchlorac, quinmerac, tridiphane and flamprop; and optionally c) to antagonise the herbicide, an antidotally effective amount of a safener selected from clo
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: March 29, 2011
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Jutta Glock, Adrian Alberto Friedmann, Derek Cornes
  • Publication number: 20110071134
    Abstract: A heterocyclic inhibitor having the formula I, with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role:
    Type: Application
    Filed: April 26, 2010
    Publication date: March 24, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Zhan Shi, Brendan S. Chen, Jane F. Schmidt, John C. Reader, Neal D. Hone, Jeffrey P. Ciavarri
  • Publication number: 20100311593
    Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.
    Type: Application
    Filed: March 11, 2010
    Publication date: December 9, 2010
    Applicant: Bayer Cropscience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Jan Dittgen, Dieter Feucht, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
  • Publication number: 20100256355
    Abstract: The present invention provides a novel oxazolidinone derivative of the formula (I): wherein Ring A is (A-1) a 7-membered monocyclic heterocycle containing three N atoms; (A-2) a 7-membered monocyclic heterocycle containing two N atoms and one O atom; or (A-3) a 7-membered monocyclic heterocycle containing two N atoms and one S atom, SO or SO2, wherein said monocyclic heterocycle is optionally substituted, optionally unsaturated and optionally fused with another ring; X1 is a single bond, or a heteroatom-containing group selected from the group consisting of —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2—, wherein R2, R3, R4, R5 and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom-containing group; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; and R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolid
    Type: Application
    Filed: October 1, 2008
    Publication date: October 7, 2010
    Inventors: Hideyuki Suzuki, Iwao Utsunomiya, Koichi Shudo, Tsutomu Iwaki, Tatsuro Yasukata
  • Publication number: 20100240635
    Abstract: Compounds of formula (I): wherein: R1 and R2, which may be the same or different, each represent a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, acyl, alkoxycarbonyl, carboxy, hydroxy, hydroxyalkyl, cyano, nitro, amino, substituted or unsubstituted aminocarbonyl, aminosulphonyl, alkylsulphonylaminoalkyl, N-hydroxy-carboximidamide or benzyloxy group, R3 represents a hydrogen atom or an alkyl, cycloalkyl or cycloalkylalkyl group, R4 represents a hydrogen atom or a substituted or unsubstituted alkyl group Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator and/or an NMDA receptor antagonist.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 23, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
  • Publication number: 20100234348
    Abstract: The present invention provides compounds that potentiate the activity of antibiotic agents, particularly quinolones such as norflaxin. The invention further provides compositions, e.g., pharmaceutical compositions, comprising the inventive compounds. The invention also provides compositions comprising an antibiotic (e.g., a quinolone) and a compound that potentiates activity of the antibiotic. The invention further provides methods of treating a subject comprising administering any of the inventive compounds or compositions to the subject. The invention also provides screening methods to identify compounds that potentiate the activity of an antibiotic, e.g., a quinolone.
    Type: Application
    Filed: August 2, 2007
    Publication date: September 16, 2010
    Applicant: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Guillaume Cottarel, Timothy S. Gardner, Xiaoguang Lei, John Porco, Scott E. Schaus, Jamey Wierzbowski, Kollol Pal
  • Patent number: 7795246
    Abstract: A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that provides greatly improved bioavailability of orally administered fused pyrrolocarbazole compounds.
    Type: Grant
    Filed: November 20, 2003
    Date of Patent: September 14, 2010
    Assignee: Cephalon, Inc.
    Inventors: Dave Dickason, Bradley T. McIntyre, Piyush R. Patel
  • Publication number: 20100179318
    Abstract: A process to make lestaurtinib, also known as (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one is disclosed.
    Type: Application
    Filed: January 11, 2008
    Publication date: July 15, 2010
    Applicant: ABBOTT LABORATORIES
    Inventor: Eric J. Stoner
  • Patent number: 7741479
    Abstract: The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: June 22, 2010
    Assignee: Locus Pharmaceuticals, Inc.
    Inventors: Enrique Luis Michelotti, Eric Bruce Springman, Duyan Nguyen, Rupa S. Shetty, Younghee Lee, Kristofer Kent Moffett, Jennifer Lee Ludington, Ted Tsutomis Fujimoto, Zenon D. Konteatis, Bin Liu, Frank Hollinger, Bruce D. Dorsey
  • Publication number: 20100144703
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: February 17, 2010
    Publication date: June 10, 2010
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
  • Publication number: 20100048534
    Abstract: Crystalline lestaurtinib hydrates and crystalline lestaurtinib hemihydrate hemicetonitrileate and crystalline lestaurtinib hemihydrate hemitetrahydrofuranate, processes to reproducibly make them and methods of treating patients using them are disclosed.
    Type: Application
    Filed: November 3, 2009
    Publication date: February 25, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Walter Dziki, Gowdahalli N. Subbarao, Rodger F. Henry
  • Publication number: 20100048890
    Abstract: Provided herein are linker compounds and conjugates that include the linker compounds. In one embodiment, the linker compounds comprise 2 or 3 residues of 6-aminohexanoic acid and optionally 7-10 residues of polyethyleneglycol (PEG). The linker compounds are useful in forming conjugates with one or more components useful in biopharmaceutical or bioanalytical applications. In particular, the biopharmaceutically useful compounds are kinase inhibitors. The conjugates described herein have utility in a variety of diagnostic, separation, and therapeutic applications.
    Type: Application
    Filed: June 30, 2009
    Publication date: February 25, 2010
    Inventors: Robert M. Grotzfeld, Zdravko V. Milanov, Hitesh K. Patel, Andiliy G. Lai, Shamal A. Mehta, David J. Lockhart
  • Publication number: 20100048533
    Abstract: Lestaurtinib Crystalline Form 1, isolated crystalline lestaurtinib anhydrate and amorphous lestaurtinib, processes to reproducibly make them and methods of treating patients using them.
    Type: Application
    Filed: October 28, 2009
    Publication date: February 25, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Walter Dziki, Gowdahalli N. Subbarao, Rodger F. Henry
  • Publication number: 20090299059
    Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A is optionally substituted or fused and represents (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; R1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent, and an antibacterial agent containing the same.
    Type: Application
    Filed: March 30, 2007
    Publication date: December 3, 2009
    Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
  • Patent number: 7612200
    Abstract: The present invention is directed to a compound having the formula wherein R1, R2, R3, R4, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The present invention is also directed to compounds that stabilize the open conformation of a protein kinase, a crystallized protein kinase in the open conformation, and uses thereof. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: November 3, 2009
    Assignee: Locus Pharmaceuticals, Inc.
    Inventors: Enrique Luis Michelotti, William R. Moore, Jr., Eric Bruce Springman
  • Patent number: 7608420
    Abstract: Staurosporine of the formula (I) is recovered from a fermentation broth in a process comprising an ultrafiltration and a diafiltration step.
    Type: Grant
    Filed: April 19, 2004
    Date of Patent: October 27, 2009
    Assignee: Lonza AG
    Inventors: Kurt Eyer, Georges Kalbermatten, Jean-Peal Roduit, Alain Wellig
  • Patent number: 7598376
    Abstract: A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of N,N?-diacyl-hydrazines with 2,2?-disubstituted diethyl ethers to form 4,5-diacyl-[1,4,5]-oxadiazepines and reaction of the latter compounds with a hydrohalic acid.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: October 6, 2009
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Beat Jau, Marian Parak
  • Patent number: 7589194
    Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(carboxylate)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-k1]pyrrolo[3,4-i][1,6]benzodiazocin-1-one methanolate pentahydrate and ways to make it are disclosed.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: September 15, 2009
    Assignee: Abbott Laboratories
    Inventor: Rodger F. Henry
  • Patent number: 7585972
    Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one bis(tetrahydrofuranate) and ways to make it are disclosed.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: September 8, 2009
    Assignee: Abbott Laboratories
    Inventor: Rodger F. Henry
  • Patent number: 7569517
    Abstract: The invention relates to novel 4-biphenyl-substituted 4-substituted pyrazolidine-3,5-diones of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted 4-substituted pyrazolidine-3,5-diones and a crop plant compatibility-improving compound.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: August 4, 2009
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
  • Publication number: 20090192307
    Abstract: The present invention is directed to a compound having the formula wherein R1, R2, R3, R4, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The present invention is also directed to compounds that stabilize the open conformation of a protein kinase, a crystallized protein kinase in the open conformation, and uses thereof. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease.
    Type: Application
    Filed: December 7, 2005
    Publication date: July 30, 2009
    Inventors: Enrique Luis Michelotti, William R. Moore, JR., Eric Bruce Springman
  • Publication number: 20090170830
    Abstract: The present invention is directed to tricyclic compounds of formula (I) 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: Application
    Filed: July 28, 2006
    Publication date: July 2, 2009
    Inventor: Philippe G. Nantermet
  • Publication number: 20090143356
    Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.
    Type: Application
    Filed: October 26, 2006
    Publication date: June 4, 2009
    Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Publication number: 20090137552
    Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
    Type: Application
    Filed: November 3, 2005
    Publication date: May 28, 2009
    Inventors: Pascale Hoehn, Bernd Koch, Michael Mutz
  • Publication number: 20090131403
    Abstract: The compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof specifically binds CCR5, so it is useful for preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacterial infection diabetes cancer metastasis and so on.
    Type: Application
    Filed: March 9, 2007
    Publication date: May 21, 2009
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shinya Kusuda, Toshihiko Nishiyama, Kazuya Hashimura, Junya Ueda, Shiro Shibayama
  • Publication number: 20090124800
    Abstract: A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of 4,5-diacyl-[1,4,5]-oxadiazepines with a base.
    Type: Application
    Filed: October 25, 2005
    Publication date: May 14, 2009
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Dominik Faber, Beat Jau
  • Patent number: 7482337
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: October 28, 2003
    Date of Patent: January 27, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
  • Publication number: 20080255087
    Abstract: The present invention relates to the use of specific compounds related to the indolocarbazole K252a, for the preparation of pharmaceutical compositions for the treatment of various forms of cancer.
    Type: Application
    Filed: December 14, 2007
    Publication date: October 16, 2008
    Applicant: Tautatis, Inc.
    Inventor: Hanno Roder
  • Publication number: 20080249080
    Abstract: The invention concerns benzodiazepine derivatives of formula wherein Y it is SO2 or NR, wherein R is H or C1-C6 alkyl; X is H, C1-C12 alkyl, —CO, —SO, —SO2, or —CO—R2, SO—R2, SO2—R2, wherein R2 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, each para-, meta- or ortho-substituted independently of each other with 0 to 3 substituents selected from halogen, —CN, —NH2, —OH, —NO2, COOR3, wherein R3 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, or C2-C6 alkoxy carbonyl; phenyl, benzyl, naphtyl, biphenyl, or heterocycle n is 0-6; R4 is selected from H, OH, COOH, CN, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, —CO, —SO, —SO2, or —CO—R5, SO—R5, SO2—R2, —OCO—R5, OSO—R5, SO2—R5, COOR5, SOOR5, SO2OR5, NHR5, NHCOR5, NHSO2R5, SR5, SCOR5, wherein R5 is selected from H, C1-C6 alkyl, C1-C6 alkoxy, C2-C6
    Type: Application
    Filed: May 26, 2006
    Publication date: October 9, 2008
    Inventors: Romano Silvestri, Gabriella Marfe', Elisabetta Abruzzese, Gianfranco Catalano, Carla Di Stefano, Ettore Novellino, Paola Sinibaldi Salimei, Maria Gabriella De Martino, Giuseppe La Regina, Antonio La-Vecchia
  • Publication number: 20080188371
    Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.
    Type: Application
    Filed: August 2, 2004
    Publication date: August 7, 2008
    Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Losel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
  • Patent number: 7407949
    Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: August 5, 2008
    Assignee: Ferring B.V.
    Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
  • Publication number: 20080171868
    Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(carboxylate)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-k1]pyrrolo[3,4-i][1,6]benzodiazocin-1-one methanolate pentahydrate and ways to make it are disclosed.
    Type: Application
    Filed: January 10, 2008
    Publication date: July 17, 2008
    Applicant: ABBOTT LABORATORIES
    Inventor: Rodger F. Henry
  • Publication number: 20080171867
    Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one bis(tetrahydrofuranate) and ways to make it are disclosed.
    Type: Application
    Filed: January 10, 2008
    Publication date: July 17, 2008
    Applicant: ABBOTT LABORATORIES
    Inventor: Rodger F. Henry
  • Publication number: 20080171866
    Abstract: A crystalline (9S-(9?,10?,12?))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-k1]pyrrolo[3,4-i][1,6]benzodiazocin-1-one bis(methanolate) and ways to make it are disclosed.
    Type: Application
    Filed: January 10, 2008
    Publication date: July 17, 2008
    Applicant: ABBOTT LABORATORIES
    Inventor: Rodger F. Henry
  • Publication number: 20080096864
    Abstract: The present invention relates to the use of a combination comprising (a) imatinib or a pharmaceutically acceptable salt thereof and midostaurin or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of gastrointestinal stromal tumors, e.g. imatinib-resistant gastro-intestinal stromal tumors.
    Type: Application
    Filed: September 17, 2004
    Publication date: April 24, 2008
    Inventors: Sasa Dimitrijevic, Jonathan A. Fletcher, Sandra Leta Silberman
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Publication number: 20080051578
    Abstract: The present invention relates to compounds of general formula (I) wherein A, B, L, R1, R2, R3a and R3b are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: August 24, 2006
    Publication date: February 28, 2008
    Inventors: Georg Dahmann, Kai Gerlach, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar
  • Patent number: 7244843
    Abstract: The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
    Type: Grant
    Filed: October 5, 2004
    Date of Patent: July 17, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dean A. Wacker, Jeffrey G. Varnes
  • Patent number: 7238684
    Abstract: The present invention relates to compounds of formula (I): wherein Rv, R1, R2, Rx, Ry, R3, R4, R5, R6, Rz and v are as defined within; pharmaceutically acceptable salts, solvates, solvates or such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: April 23, 2003
    Date of Patent: July 3, 2007
    Assignee: AstraZeneca AB
    Inventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, Mats Peter Nordberg, Suzanne Alenfalk, Andreas Christer Wallberg, Stig Jonas Bostrom
  • Patent number: 7192953
    Abstract: Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula —N(OH)CH(?O) or formula —C(?O)NH(OH); Y represents —C(?O)—, —C(?S)—, —S(?O)—, or —SO2—; R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of formula —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, halogen, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, C1–C3 alkyl-O—C1–C3 alkyl, C1–C3 alkyl-S—C1–C3 alkyl, cycloalkyl(C1–C3 alkyl)-, aryl(C1–C3alkyl)-, heterocyclyl(C1–C3 alkyl)-, or R1R2N—C1–C3 alkyl group wherein R1 represents hydrogen or C1–C3 alkyl and R2 represents C1–C3 alkyl, or R1R2N-represents a cyclic amino group; R3 and R4 taken together with the nitrogen atoms to which they are respectively attached form a saturated heterocyclic ring of from 4 to 7 ring atoms, which may be fused to a second carbocyclic or heterocyclic ring, either of which rings may optionall
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: March 20, 2007
    Assignee: Vernalis (Oxford) Limited
    Inventor: Stephen Peter East
  • Patent number: 7132416
    Abstract: The present invention relates to compounds of formula (I) wherein Rv, R1, R2, Rx, Ry, M, Rz, v, R3, R4, R5 and R6 are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: November 7, 2006
    Assignee: AstraZeneca AB
    Inventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, David Blomberg, Suzanne Alenfalk, Tore Skjaret, Malin Lemurell
  • Patent number: 7060818
    Abstract: An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: June 13, 2006
    Assignee: Carnegie Mellon University
    Inventors: Colin P. Horwitz, Anindya Ghosh
  • Patent number: 7038043
    Abstract: Indolocarbazoles are furanosylated (e.g., 7) with acetals (e.g., 8) or their open chain congeners (e.g., 9) under conditions known to promote acetal exchange or formation, such as protic or Lewis acids. Furanosylated indolocarbazoles (e.g., 10) are also prepared via ring contraction of pyranosylated indolocarbazoles (e.g., 11) under conditions know to effect oxidation and benzylic acid type rearrangements, and pyranosylated indolocarbazoles (e.g., 11) are prepared via ring expansion of the furanosylated congeners (e.g.
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: May 2, 2006
    Assignee: Yale University
    Inventors: John L. Wood, Brian M. Stoltz, Hans-Jurgen Dietrich, Derek A. Pflum
  • Patent number: 6921759
    Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 10, 2001
    Date of Patent: July 26, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa Egbertson, John S. Wai, Linghang Zhuang, Mark Embrey, Jeffrey Y. Melamed, H. Marie Langford, James P. Guare, Thorsten E. Fisher, Samson M. Jolly, Michelle S. Kuo, Debra S. Perlow, Jennifer J. Bennett, Timothy W. Funk
  • Patent number: 6875865
    Abstract: Disclosed herein are selected indolocarbazole derivatives which are represented by the general formula: The compounds are useful for enhancing the function and/or survival of a trophic factor responsive cell. They inhibit interleukin-2 production and have immunosuppressive activity.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: April 5, 2005
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, John P. Mallamo, Masami Hamano, Rieko Tanaka, Chikara Murakata